Nalorphine
Levorphanol
Pentazocine
Levallorphan
Naloxone
Narcotics
Morphine
Drug and Narcotic Control
Meperidine
Analgesics, Opioid
Morphinans
Opium
Alphaprodine
Hormone Antagonists
Dextropropoxyphene
Dopamine Antagonists
Excitatory Amino Acid Antagonists
Neurokinin-1 Receptor Antagonists
Fentanyl
Dose-Response Relationship, Drug
Methadone
Oxymorphone
Histamine H2 Antagonists
Interleukin 1 Receptor Antagonist Protein
Heroin
Codeine
Muscarinic Antagonists
GABA Antagonists
Histamine H1 Antagonists
Purinergic P1 Receptor Antagonists
Preanesthetic Medication
Rats, Sprague-Dawley
Histamine Antagonists
Nicotinic Antagonists
Adenosine A2 Receptor Antagonists
Adrenergic alpha-1 Receptor Antagonists
Naltrexone
Purinergic P2 Receptor Antagonists
Spasm
Hydrocodone
Pain
Inert Gas Narcosis
Serotonin 5-HT3 Receptor Antagonists
Receptors, Opioid
Serotonin 5-HT2 Receptor Antagonists
Dibenzocycloheptenes
Alcoholics Anonymous
Adenosine A1 Receptor Antagonists
Drug Tolerance
Leukotriene Antagonists
Angiotensin Receptor Antagonists
Receptors, Opioid, mu
Anesthesia
Isonipecotic Acids
Substance Withdrawal Syndrome
Rats, Wistar
Discriminative stimulus effects of naltrexone after a single dose of morphine in the rat. (1/1824)
The discriminative stimulus effects of an acute morphine (MOR) --> naltrexone (NTX) combination were characterized and compared with the stimulus effects of NTX-precipitated and spontaneous withdrawal from chronic MOR administration. Adult male Sprague-Dawley rats (n = 6-8) were trained to discriminate between two drug treatments in a discrete-trial avoidance/escape procedure: MOR (10 mg./kg, s.c., 4 h) --> NTX (0.3 mg/kg, s.c., 0.25 h) versus saline (SAL, 1 ml/kg, s. c., 4 h) --> NTX (0.3 mg/kg, s.c., 0.25 h). Subjects responded only on the SAL --> NTX-appropriate lever when SAL was given 3.75 h after MOR or 3.75 h before any dose of NTX (0.3-100 mg/kg). Responding was dose dependent and MOR --> NTX-appropriate when NTX (0.01-0.1 mg/kg) followed MOR. Full MOR --> NTX-appropriate responding was dependent on the pretreatment dose and time of MOR, with full effects observed only when MOR (10 mg/kg) was given 3 to 4 h before NTX. While subjects were maintained on either 20- or 40 mg/kg/day of MOR via osmotic pump, NTX produced full dose-dependent, MOR --> NTX-appropriate responding. When the MOR-filled pumps were removed, partial MOR --> NTX-appropriate responding occurred, peaking at 6 to 12 h. The physical withdrawal signs produced by NTX after acute or during chronic MOR exposure were of smaller magnitude compared with the ones that occurred during abrupt withdrawal from chronic MOR. A qualitatively unique "withdrawal" stimulus that is dose- and time-dependent appears to be the basis of this MOR --> NTX discrimination. (+info)Modulation of Ca2+/calmodulin-dependent protein kinase II activity by acute and chronic morphine administration in rat hippocampus: differential regulation of alpha and beta isoforms. (2/1824)
Calcium/calmodulin-dependent protein kinase II (CaMK II) has been shown to be involved in the regulation of opioid receptor signaling. The present study showed that acute morphine treatment significantly increased both Ca2+/calmodulin-independent and Ca2+/calmodulin-dependent activities of CaMK II in the rat hippocampus, with little alteration in the protein level of either alpha or beta isoform of CaMK II. However, chronic morphine treatment, by which rats were observed to develop apparent tolerance to morphine, significantly down-regulated both Ca2+/calmodulin-independent and Ca2+/calmodulin-dependent activities of CaMK II and differentially regulated the expression of alpha and beta isoforms of CaMK II at protein and mRNA levels. Application of naloxone or discontinuation of morphine treatment after chronic morphine administration, which induced the withdrawal syndrome of morphine, resulted in the overshoot of CaMK II (at both protein and mRNA levels) and its kinase activity. The phenomena of overshoot were mainly observed in the beta isoform of CaMK II but not in the alpha isoform. The effects of both acute and chronic morphine treatments on CaMK II could be completely abolished by the concomitant application of naloxone, indicating that the effects of morphine were achieved through activation of opioid receptors. Our data demonstrated that both acute and chronic morphine treatments could effectively modulate the activity and the expression of CaMK II in the hippocampus. (+info)Reproductive experience and opioid regulation of luteinizing hormone release in female rats. (3/1824)
The objective of the present study was to determine whether reproductive experience that produces shifts in opioid regulation of prolactin secretion and behavioural functions also alters opioid regulation of LH during the oestrous cycle or lactation. In Expt 1 the effect of naloxone administration (i.v.) on LH was compared between age-matched, nulliparous and primiparous, catheterized female rats on dioestrus II. In Expt 2, the effects of multiple reproductive experiences on opiate control of LH were investigated using cyclic, nulliparous and multiparous (three litters) rats. In both experiments, no differences in naloxone-stimulated LH release were found between groups even though multiple reproductive experiences resulted in the prolongation of oestrous cyclicity. In Expt 3, day 8 lactating primiparous rats were administered 2, 5, 10 or 25 mg naloxone kg-1 i.v. The three lowest naloxone doses, but not the 25 mg kg-1 dose, significantly increased LH concentrations. The possible effects of prior reproductive experience on opioid control of LH during lactation were then investigated. Naloxone at 0.5 mg kg-1, but not at 2 mg kg-1 or 10 mg kg-1, stimulated a significantly greater rise in LH in multiparous (two litters) than in primiparous females. Overall, these data indicate that while modest differences were found in naloxone-induced LH responses between multiparous and primiparous animals during lactation, reproductive experience did not significantly alter opioid regulation of LH during subsequent oestrous cycles at the naloxone doses examined. Hence, the effects of reproductive experience on opioid regulation of LH are less pronounced than those previously found for opioid regulation of prolactin and behaviour. (+info)Morphine preconditioning attenuates neutrophil activation in rat models of myocardial infarction. (4/1824)
Previous results from our laboratory have suggested that morphine can attenuate neutrophil activation in patients with acute myocardial infarction. To elucidate if morphine preconditioning (PC) has the same effects via activation of neutrophil endopeptidase 24.11 (NEP), we measured serum levels of intercellular adhesion molecule-1 (ICAM-1), gp100MEL14 and NEP in adult Wistar rats subjected to ten different protocols (n = 10 for each) at baseline, immediately after and 2 h after morphine PC. All groups were subjected to 30 min of occlusion and 2 h of reperfusion. Similarly, morphine-induced PC was elicited by 3-min drug infusions (100 micrograms/kg) interspersed with 5-min drug-free periods before the prolonged 30-min occlusion. Infarct size (IS), as a percentage of the area at risk (AAR), was determined by triphenyltetrazolium staining. Pretreatment with morphine increased NEP activities (9.86 +/- 1.98 vs. 5.12 +/- 1.10 nmol/mg protein in control group; p < 0.001). Naloxone (mu-opioid receptor antagonist) (4.82 +/- 1.02 nmol/mg protein) and phosphoramidon (NEP inhibitor) (4.66 +/- 1.00 nmol/mg protein) inhibited morphine-activated NEP, whereas glibenclamide (ATP-sensitive potassium channel antagonist) and chelerythrine (protein kinase C inhibitor) had no effects. The ICAM-1 and gp100MEL14 of the third sampling were lowest for those with morphine PC (280 +/- 30 ng/ml and 2.2 +/- 0.7 micrograms/ml; p < 0.001), but naloxone (372 +/- 38 ng/ml and 3.8 +/- 0.9 micrograms/ml) and phosphoramidon (382 +/- 40 ng/ml and 4.2 +/- 1.1 micrograms/ml) abolished the above phenomenon. IS/AAR were definitely lowest for those with morphine PC (24 +/- 7%; p < 0.05). Morphine preconditioning increases NEP activities to attenuate shedding of gp100MEL14 and to ICAM-1 and, thus, provides myocardial protection. (+info)Rapid detoxification of heroin dependence by buprenorphine. (5/1824)
AIM: To evaluate the clinical efficacy of buprenorphine (Bup) in treatment of acute heroin withdrawal. METHODS: Bup was given sublingually daily to 60 cases of heroin addicts in 3 groups: low, medium, and high doses. Withdrawal signs and symptoms of heroin were rated by Clinical Institute Narcotic Assessment. Craving for heroin during detoxification was assessed by Visual Analogue Scale. The side effects of Bup was assessed by Treatment Emergent Symptom Scale. RESULTS: The mean daily consumption of Bup in low, medium, and high group was 2.0, 2.9, and 3.6 mg, respectively. Bup not only suppressed objective signs and withdrawal symptoms for heroin withdrawal, but also reduced the duration for heroin detoxification over 7-8 d. CONCLUSION: Bup is an effective and rapid detoxification agent with fewer side effects for treatment of acute heroin withdrawal. (+info)Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line. (6/1824)
The sigma binding site present in the Jurkat human T lymphocyte cell line was investigated. Jurkat cell membranes were found to have a single saturable binding site for [3H]haloperidol, a sigma ligand (dissociation constant, 3.9 +/- 0.3 nM). The binding of [3H]haloperidol was inhibited by several sigma ligands. Northern analysis and reverse transcription-polymerase chain reaction provided evidence for the expression of the recently cloned type 1 sigma-receptor (sigma-R1) in Jurkat cells. The sigma-R1 cDNA cloned from these cells was functional in heterologous expression systems. When expressed in mammalian cells, the cDNA-induced binding was saturable with dissociation constants of 1.9 +/- 0.3 nM for [3H]haloperidol and 12 +/- 2 nM for (+)-pentazocine. The binding of [3H]progesterone, a putative endogenous ligand to sigma-R1, to the Jurkat cell sigma-receptor could be directly demonstrated by using heterologously expressed sigma-R1 cDNA. The binding of [3H]progesterone was saturable, with a dissociation constant of 88 +/- 7 nM. Progesterone and haloperidol interacted with the receptor competitively. Reverse transcription-polymerase chain reaction also produced evidence for the existence of an alternatively spliced sigma-R1 variant in Jurkat cells. This splice variant was found to be nonfunctional in ligand binding assays. This constitutes the first report on the molecular characterization of the sigma-receptor in immune cells. (+info)Modulation of amphetamine-stimulated [3H]dopamine release from rat pheochromocytoma (PC12) cells by sigma type 2 receptors. (7/1824)
An important regulatory mechanism of synaptic dopamine (DA) levels is activation of the dopamine transporter (DAT), which is a target for many drugs of abuse, including amphetamine (AMPH). sigma receptors are located in dopaminergic brain areas critical to reinforcement. We found previously that agonists at sigma2 receptors enhanced the AMPH-stimulated release of [3H]DA from slices of rat caudate-putamen. In the present study, we modeled this response in undifferentiated pheochromocytoma-12 (PC12) cells, which contain both the DAT and sigma2 receptors but not neural networks that can complicate investigation of individual neuronal mechanisms. We found that enhancement of AMPH-stimulated [3H]DA release by the sigma agonist (+)-pentazocine was blocked by sigma2 receptor antagonists. Additionally, the reduction in the effect of (+)-pentazocine by the inclusion of ethylene glycol bis(beta-aminoethyl ether)-N,N,N', N'-tetraacetic acid led us to hypothesize that sigma2 receptor activation initiated a Ca2+-dependent process that resulted in enhancing the outward flow of DA via the DAT. The source of Ca2+ required for the enhancement of reverse transport did not appear to be via N- or L-type voltage-dependent Ca2+ channels, because it was not affected by nitrendipine or omega-conotoxin. However, two inhibitors of Ca2+/calmodulin-dependent protein kinase II blocked enhancement in AMPH-stimulated release by (+)-pentazocine. Our findings suggest that sigma2 receptors are coupled to the DAT via a Ca2+/calmodulin-dependent protein kinase II transduction system in PC12 cells, and that sigma2 receptor antagonists might be useful in the treatment of drug abuse by blocking elevation of DA levels via reversal of the DAT. (+info)Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity. (8/1824)
Two 14beta-p-nitrocinnamoyl derivatives of dihydrocodeinone, 14beta-(p-nitrocinnamoylamino)-7,8-dihydrocodeinone (CACO) and N-cyclopropylmethylnor-14beta-(p-nitrocinnamoylamino)- 7, 8-dihydrocodeinone (N-CPM-CACO), and the corresponding chlorocinnamoylamino analogs, 14beta-(p-chlorocinnamoylamino)-7, 8-dihydrocodeinone (CAM) and N-cyclopropylmethylnor-14beta-(p-chlorocinnamoylamino) -7, 8-dihydrocodeinone (MC-CAM), were tested in opioid receptor binding assays and the mouse tail-flick test to characterize the opioid affinity, selectivity, and antinociceptive properties of these compounds. In competition binding assays, all four compounds bound to the mu opioid receptor with high affinity. When bovine striatal membranes were incubated with any of the four dihydrocodeinones, binding to the mu receptor was inhibited in a concentration-dependent, wash-resistant manner. Saturation binding experiments demonstrated that the wash-resistant inhibition of mu binding was due to a decrease in the Bmax value for the binding of the mu-selective peptide [3H][D-Ala2, MePhe4,Gly(ol)5] enkephalin and not a change in the Kd value, suggesting an irreversible interaction of the compounds with the mu receptor. In the mouse 55 degrees C warm water tail-flick test, both CACO and N-CPM-CACO acted as short-term mu-selective agonists when administered by i. c.v. injection, whereas CAM and MC-CAM produced no measurable antinociception at doses up to 30 nmol. Pretreatment of mice for 24 h with any of the four dihydrocodeinone derivatives produced a dose-dependent antagonism of antinociception mediated by the mu but not the delta or kappa receptors. Long-term antagonism of morphine-induced antinociception lasted for at least 48 h after i.c. v. administration. Finally, shifts in the morphine dose-response lines after 24-h pretreatment with the four dihydrocodeinone compounds suggest that the nitrocinnamoylamino derivatives may produce a greater magnitude long-term antagonism of morphine-induced antinociception than the chlorocinnamoylamino analogs. (+info)Nalorphine is defined as a morphine derivative that antagonizes the effects of opiate agonists, such as morphine and heroin, by competing for binding sites in the central nervous system. It was initially used as an analgesic but has since been replaced by other drugs due to its potential for abuse and adverse psychological effects. Currently, it is primarily used in research and to reverse opioid overdose.
Levorphanol is a potent opioid analgesic medication used to treat moderate to severe pain. It is a synthetic compound with a chemical structure similar to that of morphine, but it has more potent analgesic and sedative effects. Levorphanol works by binding to opioid receptors in the brain and spinal cord, which reduces the perception of pain and produces a sense of well-being or euphoria.
Levorphanol is available in oral tablet form and is typically used for short-term pain management in patients who are not able to take other opioid medications or who have developed tolerance to them. It has a long duration of action, with effects lasting up to 24 hours after a single dose.
Like all opioids, levorphanol carries a risk of dependence and addiction, as well as serious side effects such as respiratory depression, sedation, and constipation. It should be used with caution in patients with a history of substance abuse or mental illness, and it is not recommended for use in pregnant women or children.
Pentazocine is a synthetic opioid analgesic, chemically unrelated to other opiates or opioids. It acts as an agonist at the kappa-opioid receptor and as an antagonist at the mu-opioid receptor, which means it can produce pain relief but block the effects of full agonists such as heroin or morphine. Pentazocine is used for the management of moderate to severe pain and is available in oral, intramuscular, and intravenous formulations. Common side effects include dizziness, lightheadedness, sedation, nausea, and vomiting.
Narcotic antagonists are a class of medications that block the effects of opioids, a type of narcotic pain reliever, by binding to opioid receptors in the brain and blocking the activation of these receptors by opioids. This results in the prevention or reversal of opioid-induced effects such as respiratory depression, sedation, and euphoria. Narcotic antagonists are used for a variety of medical purposes, including the treatment of opioid overdose, the management of opioid dependence, and the prevention of opioid-induced side effects in certain clinical situations. Examples of narcotic antagonists include naloxone, naltrexone, and methylnaltrexone.
Levallorphan is a opioid antagonist and agonist, often used as an analgesic (pain reliever) and antitussive (cough suppressant). It works by binding to the opioid receptors in the brain, blocking the effects of certain opioid agonists such as morphine while also acting as a weak agonist itself. This means that it can both block the pain-relieving effects and produce some of the unwanted side effects of opioids, such as respiratory depression. It is used in clinical settings to reverse or reduce the effects of opioid overdose, and also for the treatment of severe cough.
It's important to note that Levallorphan has a complex pharmacology and its use should be restricted to medical professionals due to its potential for abuse and dependence.
Naloxone is a medication used to reverse the effects of opioids, both illicit and prescription. It works by blocking the action of opioids on the brain and restoring breathing in cases where opioids have caused depressed respirations. Common brand names for naloxone include Narcan and Evzio.
Naloxone is an opioid antagonist, meaning that it binds to opioid receptors in the body without activating them, effectively blocking the effects of opioids already present at these sites. It has no effect in people who have not taken opioids and does not reverse the effects of other sedatives or substances.
Naloxone can be administered via intranasal, intramuscular, intravenous, or subcutaneous routes. The onset of action varies depending on the route of administration but generally ranges from 1 to 5 minutes when given intravenously and up to 10-15 minutes with other methods.
The duration of naloxone's effects is usually shorter than that of most opioids, so multiple doses or a continuous infusion may be necessary in severe cases to maintain reversal of opioid toxicity. Naloxone has been used successfully in emergency situations to treat opioid overdoses and has saved many lives.
It is important to note that naloxone does not reverse the effects of other substances or address the underlying causes of addiction, so it should be used as part of a comprehensive treatment plan for individuals struggling with opioid use disorders.
Cyclazocine is a synthetic opioid drug that acts as a partial agonist at mu and kappa opioid receptors, and as an antagonist at delta opioid receptors. It has analgesic (pain-relieving) effects, but its use as an analgesic is limited due to its potential for abuse and the occurrence of unpleasant psychotomimetic side effects such as dysphoria, delusions, and hallucinations.
Cyclazocine was first synthesized in 1957 and has been studied for its potential use in the treatment of opioid addiction, but it is not currently approved for medical use in many countries, including the United States. It is classified as a Schedule I controlled substance in the US, indicating that it has a high potential for abuse and no accepted medical use.
Narcotics, in a medical context, are substances that induce sleep, relieve pain, and suppress cough. They are often used for anesthesia during surgical procedures. Narcotics are derived from opium or its synthetic substitutes and include drugs such as morphine, codeine, fentanyl, oxycodone, and hydrocodone. These drugs bind to specific receptors in the brain and spinal cord, reducing the perception of pain and producing a sense of well-being. However, narcotics can also produce physical dependence and addiction, and their long-term use can lead to tolerance, meaning that higher doses are required to achieve the same effect. Narcotics are classified as controlled substances due to their potential for abuse and are subject to strict regulations.
Morphine is a potent opioid analgesic (pain reliever) derived from the opium poppy. It works by binding to opioid receptors in the brain and spinal cord, blocking the transmission of pain signals and reducing the perception of pain. Morphine is used to treat moderate to severe pain, including pain associated with cancer, myocardial infarction, and other conditions. It can also be used as a sedative and cough suppressant.
Morphine has a high potential for abuse and dependence, and its use should be closely monitored by healthcare professionals. Common side effects of morphine include drowsiness, respiratory depression, constipation, nausea, and vomiting. Overdose can result in respiratory failure, coma, and death.
"Drug and narcotic control" refers to the regulation and oversight of drugs and narcotics, including their production, distribution, and use. This is typically carried out by governmental agencies in order to ensure public safety, prevent abuse and diversion, and protect the health of individuals. The goal of drug and narcotic control is to strike a balance between making sure that medications are available for legitimate medical purposes while also preventing their misuse and illegal sale.
Drug control policies may include measures such as licensing and registration of manufacturers, distributors, and pharmacies; tracking and monitoring of controlled substances; setting standards for prescription practices; and enforcement of laws and regulations related to drug use and trafficking. Narcotic control specifically refers to the regulation of drugs that have a high potential for abuse and are subject to international treaties, such as opioids.
It's important to note that while these regulations aim to protect public health and safety, they can also be controversial and have unintended consequences, such as contributing to drug shortages or creating barriers to access for people who need controlled substances for legitimate medical reasons.
Meperidine is a synthetic opioid analgesic (pain reliever) that works by binding to opioid receptors in the brain and spinal cord, blocking the transmission of pain signals. It is also known by its brand name Demerol and is used to treat moderate to severe pain. Meperidine has a rapid onset of action and its effects typically last for 2-4 hours.
Meperidine can cause various side effects such as dizziness, sedation, nausea, vomiting, sweating, and respiratory depression (slowed breathing). It also has a risk of abuse and physical dependence, so it is classified as a Schedule II controlled substance in the United States.
Meperidine should be used with caution and under the supervision of a healthcare provider due to its potential for serious side effects and addiction. It may not be suitable for people with certain medical conditions or those who are taking other medications that can interact with meperidine.
Analgesics, opioid are a class of drugs used for the treatment of pain. They work by binding to specific receptors in the brain and spinal cord, blocking the transmission of pain signals to the brain. Opioids can be synthetic or natural, and include drugs such as morphine, codeine, oxycodone, hydrocodone, hydromorphone, fentanyl, and methadone. They are often used for moderate to severe pain, such as that resulting from injury, surgery, or chronic conditions like cancer. However, opioids can also produce euphoria, physical dependence, and addiction, so they are tightly regulated and carry a risk of misuse.
Morphinans are a class of organic compounds that share a common skeletal structure, which is based on the morphine molecule. The morphinan structure consists of a tetracyclic ring system made up of three six-membered benzene rings (A, C, and D) fused to a five-membered dihydrofuran ring (B).
Morphinans are important in medicinal chemistry because many opioid analgesics, such as morphine, hydromorphone, oxymorphone, and levorphanol, are derived from or structurally related to morphinans. These compounds exert their pharmacological effects by binding to opioid receptors in the brain and spinal cord, which are involved in pain perception, reward, and addictive behaviors.
It is worth noting that while all opiates (drugs derived from the opium poppy) are morphinans, not all morphinans are opiates. Some synthetic or semi-synthetic morphinans, such as fentanyl and methadone, do not have a natural origin but still share the same basic structure and pharmacological properties.
Opium is defined as the dried latex obtained from incisions made in the unripe seedpods of the opium poppy (Papaver somniferum). It contains a number of alkaloids, including morphine, codeine, and thebaine. Opium has been used for its pain-relieving, euphoric, and sedative effects since ancient times. However, its use is highly regulated due to the risk of addiction and other serious side effects.
Alphaprodine is a synthetic opioid medication that is primarily used for its analgesic (pain-relieving) effects. It belongs to the class of drugs known as narcotic analgesics, which work by binding to specific receptors in the brain and spinal cord to reduce the perception of pain.
Alphaprodine is a controlled substance due to its potential for abuse and dependence. It can produce euphoria, drowsiness, respiratory depression, and constipation, among other side effects. Long-term use or misuse of alphaprodine can lead to physical dependence and withdrawal symptoms upon discontinuation.
Alphaprodine is not commonly used in clinical practice today due to the availability of safer and more effective pain medications. It is also not available as a generic medication, and only one branded formulation (Nisentil) was approved by the FDA for use in the United States, but it has been discontinued from the market.
Hormone antagonists are substances or drugs that block the action of hormones by binding to their receptors without activating them, thereby preventing the hormones from exerting their effects. They can be classified into two types: receptor antagonists and enzyme inhibitors. Receptor antagonists bind directly to hormone receptors and prevent the hormone from binding, while enzyme inhibitors block the production or breakdown of hormones by inhibiting specific enzymes involved in their metabolism. Hormone antagonists are used in the treatment of various medical conditions, such as cancer, hormonal disorders, and cardiovascular diseases.
'Drug legislation' refers to the laws and regulations that govern the production, distribution, sale, possession, and use of medications and pharmaceutical products within a given jurisdiction. These laws are designed to protect public health and safety by establishing standards for drug quality, ensuring appropriate prescribing and dispensing practices, preventing drug abuse and diversion, and promoting access to necessary medications. Drug legislation may also include provisions related to clinical trials, advertising, packaging, labeling, and reimbursement. Compliance with these regulations is typically enforced through a combination of government agencies, professional organizations, and legal penalties for non-compliance.
Dextropropoxyphene is a mild narcotic analgesic (pain reliever) that is prescribed for the relief of moderate to moderately severe pain. It is a synthetic opioid and works by binding to opiate receptors in the brain, spinal cord, and other areas of the body to reduce the perception of pain. Dextropropoxyphene is available in immediate-release and extended-release tablets, usually in combination with acetaminophen (also known as paracetamol).
Dextropropoxyphene has a narrow therapeutic index, which means that there is only a small range between the effective dose and a potentially toxic dose. It also has a high potential for abuse and addiction, and its use has been associated with serious side effects such as respiratory depression, seizures, and cardiac arrhythmias. In 2010, the U.S. Food and Drug Administration (FDA) withdrew approval for all dextropropoxyphene-containing products due to these safety concerns.
Analgesics are a class of drugs that are used to relieve pain. They work by blocking the transmission of pain signals in the nervous system, allowing individuals to manage their pain levels more effectively. There are many different types of analgesics available, including both prescription and over-the-counter options. Some common examples include acetaminophen (Tylenol), ibuprofen (Advil or Motrin), and opioids such as morphine or oxycodone.
The choice of analgesic will depend on several factors, including the type and severity of pain being experienced, any underlying medical conditions, potential drug interactions, and individual patient preferences. It is important to use these medications as directed by a healthcare provider, as misuse or overuse can lead to serious side effects and potential addiction.
In addition to their pain-relieving properties, some analgesics may also have additional benefits such as reducing inflammation (like in the case of nonsteroidal anti-inflammatory drugs or NSAIDs) or causing sedation (as with certain opioids). However, it is essential to weigh these potential benefits against the risks and side effects associated with each medication.
When used appropriately, analgesics can significantly improve a person's quality of life by helping them manage their pain effectively and allowing them to engage in daily activities more comfortably.
Dopamine antagonists are a class of drugs that block the action of dopamine, a neurotransmitter in the brain associated with various functions including movement, motivation, and emotion. These drugs work by binding to dopamine receptors and preventing dopamine from attaching to them, which can help to reduce the symptoms of certain medical conditions such as schizophrenia, bipolar disorder, and gastroesophageal reflux disease (GERD).
There are several types of dopamine antagonists, including:
1. Typical antipsychotics: These drugs are primarily used to treat psychosis, including schizophrenia and delusional disorders. Examples include haloperidol, chlorpromazine, and fluphenazine.
2. Atypical antipsychotics: These drugs are also used to treat psychosis but have fewer side effects than typical antipsychotics. They may also be used to treat bipolar disorder and depression. Examples include risperidone, olanzapine, and quetiapine.
3. Antiemetics: These drugs are used to treat nausea and vomiting. Examples include metoclopramide and prochlorperazine.
4. Dopamine agonists: While not technically dopamine antagonists, these drugs work by stimulating dopamine receptors and can be used to treat conditions such as Parkinson's disease. However, they can also have the opposite effect and block dopamine receptors in high doses, making them functionally similar to dopamine antagonists.
Common side effects of dopamine antagonists include sedation, weight gain, and movement disorders such as tardive dyskinesia. It's important to use these drugs under the close supervision of a healthcare provider to monitor for side effects and adjust the dosage as needed.
Excitatory amino acid antagonists are a class of drugs that block the action of excitatory neurotransmitters, particularly glutamate and aspartate, in the brain. These drugs work by binding to and blocking the receptors for these neurotransmitters, thereby reducing their ability to stimulate neurons and produce an excitatory response.
Excitatory amino acid antagonists have been studied for their potential therapeutic benefits in a variety of neurological conditions, including stroke, epilepsy, traumatic brain injury, and neurodegenerative disorders such as Alzheimer's disease and Parkinson's disease. However, their use is limited by the fact that blocking excitatory neurotransmission can also have negative effects on cognitive function and memory.
There are several types of excitatory amino acid receptors, including N-methyl-D-aspartate (NMDA), alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), and kainite receptors. Different excitatory amino acid antagonists may target one or more of these receptor subtypes, depending on their specific mechanism of action.
Examples of excitatory amino acid antagonists include ketamine, memantine, and dextromethorphan. These drugs have been used in clinical practice for various indications, such as anesthesia, sedation, and treatment of neurological disorders. However, their use must be carefully monitored due to potential side effects and risks associated with blocking excitatory neurotransmission.
Neurokinin-1 (NK-1) receptor antagonists are a class of drugs that block the action of substance P, a neuropeptide involved in pain transmission and inflammation. These drugs work by binding to NK-1 receptors found on nerve cells, preventing substance P from activating them and transmitting pain signals. NK-1 receptor antagonists have been studied for their potential use in treating various conditions associated with pain and inflammation, such as migraine headaches, depression, and irritable bowel syndrome. Some examples of NK-1 receptor antagonists include aprepitant, fosaprepitant, and rolapitant.
Opioid-related disorders is a term that encompasses a range of conditions related to the use of opioids, which are a class of drugs that include prescription painkillers such as oxycodone and hydrocodone, as well as illegal drugs like heroin. The Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5) identifies the following opioid-related disorders:
1. Opioid Use Disorder: This disorder is characterized by a problematic pattern of opioid use that leads to clinically significant impairment or distress. The symptoms may include a strong desire to use opioids, increased tolerance, withdrawal symptoms when not using opioids, and unsuccessful efforts to cut down or control opioid use.
2. Opioid Intoxication: This disorder occurs when an individual uses opioids and experiences significant problematic behavioral or psychological changes, such as marked sedation, small pupils, or respiratory depression.
3. Opioid Withdrawal: This disorder is characterized by the development of a substance-specific withdrawal syndrome following cessation or reduction of opioid use. The symptoms may include anxiety, irritability, dysphoria, nausea, vomiting, diarrhea, and muscle aches.
4. Other Opioid-Induced Disorders: This category includes disorders that are caused by the direct physiological effects of opioids, such as opioid-induced sexual dysfunction or opioid-induced sleep disorder.
It is important to note that opioid use disorder is a chronic and often relapsing condition that can cause significant harm to an individual's health, relationships, and overall quality of life. If you or someone you know is struggling with opioid use, it is essential to seek professional help from a healthcare provider or addiction specialist.
Fentanyl is a potent synthetic opioid analgesic, which is similar to morphine but is 50 to 100 times more potent. It is a schedule II prescription drug, typically used to treat patients with severe pain or to manage pain after surgery. It works by binding to the body's opioid receptors, which are found in the brain, spinal cord, and other areas of the body.
Fentanyl can be administered in several forms, including transdermal patches, lozenges, injectable solutions, and tablets that dissolve in the mouth. Illegally manufactured and distributed fentanyl has also become a major public health concern, as it is often mixed with other drugs such as heroin, cocaine, and counterfeit pills, leading to an increase in overdose deaths.
Like all opioids, fentanyl carries a risk of dependence, addiction, and overdose, especially when used outside of medical supervision or in combination with other central nervous system depressants such as alcohol or benzodiazepines. It is important to use fentanyl only as directed by a healthcare provider and to be aware of the potential risks associated with its use.
A dose-response relationship in the context of drugs refers to the changes in the effects or symptoms that occur as the dose of a drug is increased or decreased. Generally, as the dose of a drug is increased, the severity or intensity of its effects also increases. Conversely, as the dose is decreased, the effects of the drug become less severe or may disappear altogether.
The dose-response relationship is an important concept in pharmacology and toxicology because it helps to establish the safe and effective dosage range for a drug. By understanding how changes in the dose of a drug affect its therapeutic and adverse effects, healthcare providers can optimize treatment plans for their patients while minimizing the risk of harm.
The dose-response relationship is typically depicted as a curve that shows the relationship between the dose of a drug and its effect. The shape of the curve may vary depending on the drug and the specific effect being measured. Some drugs may have a steep dose-response curve, meaning that small changes in the dose can result in large differences in the effect. Other drugs may have a more gradual dose-response curve, where larger changes in the dose are needed to produce significant effects.
In addition to helping establish safe and effective dosages, the dose-response relationship is also used to evaluate the potential therapeutic benefits and risks of new drugs during clinical trials. By systematically testing different doses of a drug in controlled studies, researchers can identify the optimal dosage range for the drug and assess its safety and efficacy.
Methadone is a synthetic opioid agonist, often used as a substitute for heroin or other opiates in detoxification programs or as a long-term maintenance drug for opiate addiction. It works by changing how the brain and nervous system respond to pain signals. It also helps to suppress the withdrawal symptoms and cravings associated with opiate dependence.
Methadone is available in various forms, including tablets, oral solutions, and injectable solutions. It's typically prescribed and dispensed under strict medical supervision due to its potential for abuse and dependence.
In a medical context, methadone may also be used to treat moderate to severe pain that cannot be managed with other types of medication. However, its use in this context is more limited due to the risks associated with opioid therapy.
Oxymorphone is a semi-synthetic opioid analgesic, which is a strong painkiller. It is derived from thebaine, a constituent of opium. Medically, it is used to treat moderate to severe pain and is available under various brand names such as Opana and Numorphan.
Oxymorphone works by binding to the mu-opioid receptors in the brain and spinal cord, which results in pain relief, relaxation, and sedation. It has a high potential for abuse and addiction due to its euphoric effects, and its use should be closely monitored and controlled.
Like other opioids, oxymorphone can cause physical dependence and withdrawal symptoms if discontinued abruptly after prolonged use. Common side effects of oxymorphone include dizziness, lightheadedness, sedation, nausea, vomiting, constipation, and sweating. Serious side effects may include respiratory depression, low blood pressure, and decreased heart rate.
It is important to follow the prescribing physician's instructions carefully when taking oxymorphone and to report any bothersome or worsening side effects promptly.
Histamine H2 antagonists, also known as H2 blockers, are a class of medications that work by blocking the action of histamine on the H2 receptors in the stomach. Histamine is a chemical that is released by the body during an allergic reaction and can also be released by certain cells in the stomach in response to food or other stimuli. When histamine binds to the H2 receptors in the stomach, it triggers the release of acid. By blocking the action of histamine on these receptors, H2 antagonists reduce the amount of acid produced by the stomach, which can help to relieve symptoms such as heartburn, indigestion, and stomach ulcers. Examples of H2 antagonists include ranitidine (Zantac), famotidine (Pepcid), and cimetidine (Tagamet).
Interleukin-1 Receptor Antagonist Protein (IL-1Ra) is a naturally occurring protein that acts as a competitive inhibitor of the interleukin-1 (IL-1) receptor. IL-1 is a pro-inflammatory cytokine involved in various physiological processes, including the immune response and inflammation. The binding of IL-1 to its receptor triggers a signaling cascade that leads to the activation of inflammatory genes and cellular responses.
IL-1Ra shares structural similarities with IL-1 but does not initiate the downstream signaling pathway. Instead, it binds to the same receptor site as IL-1, preventing IL-1 from interacting with its receptor and thus inhibiting the inflammatory response.
Increased levels of IL-1Ra have been found in various inflammatory conditions, such as rheumatoid arthritis, inflammatory bowel disease, and sepsis, where it acts to counterbalance the pro-inflammatory effects of IL-1. Recombinant IL-1Ra (Anakinra) is used clinically as a therapeutic agent for the treatment of rheumatoid arthritis and other inflammatory diseases.
Heroin is a highly addictive drug that is processed from morphine, a naturally occurring substance extracted from the seed pod of the Asian opium poppy plant. It is a "downer" or depressant that affects the brain's pleasure systems and interferes with the brain's ability to perceive pain.
Heroin can be injected, smoked, or snorted. It is sold as a white or brownish powder or as a black, sticky substance known as "black tar heroin." Regardless of how it is taken, heroin enters the brain rapidly and is highly addictive.
The use of heroin can lead to serious health problems, including fatal overdose, spontaneous abortion, and infectious diseases like HIV and hepatitis. Long-term use of heroin can lead to physical dependence and addiction, a chronic disease that can be difficult to treat.
Codeine is a opiate analgesic, commonly used for its pain-relieving and cough suppressant properties. It is typically prescribed for mild to moderately severe pain, and is also found in some over-the-counter cold and cough medications. Codeine works by binding to opioid receptors in the brain and spinal cord, which helps to reduce the perception of pain. Like other opiates, codeine can produce side effects such as drowsiness, constipation, and respiratory depression, and it carries a risk of dependence and addiction with long-term use. It is important to follow your healthcare provider's instructions carefully when taking codeine, and to inform them of any other medications you are taking, as well as any medical conditions you may have.
Muscarinic antagonists, also known as muscarinic receptor antagonists or parasympatholytics, are a class of drugs that block the action of acetylcholine at muscarinic receptors. Acetylcholine is a neurotransmitter that plays an important role in the parasympathetic nervous system, which helps to regulate various bodily functions such as heart rate, digestion, and respiration.
Muscarinic antagonists work by binding to muscarinic receptors, which are found in various organs throughout the body, including the eyes, lungs, heart, and gastrointestinal tract. By blocking the action of acetylcholine at these receptors, muscarinic antagonists can produce a range of effects depending on the specific receptor subtype that is affected.
For example, muscarinic antagonists may be used to treat conditions such as chronic obstructive pulmonary disease (COPD) and asthma by relaxing the smooth muscle in the airways and reducing bronchoconstriction. They may also be used to treat conditions such as urinary incontinence or overactive bladder by reducing bladder contractions.
Some common muscarinic antagonists include atropine, scopolamine, ipratropium, and tiotropium. It's important to note that these drugs can have significant side effects, including dry mouth, blurred vision, constipation, and confusion, especially when used in high doses or for prolonged periods of time.
GABA (gamma-aminobutyric acid) antagonists are substances that block the action of GABA, which is the primary inhibitory neurotransmitter in the central nervous system. GABA plays a crucial role in regulating neuronal excitability and reducing the transmission of nerve impulses.
GABA antagonists work by binding to the GABA receptors without activating them, thereby preventing the normal function of GABA and increasing neuronal activity. These agents can cause excitation of the nervous system, leading to various effects depending on the specific type of GABA receptor they target.
GABA antagonists are used in medical treatments for certain conditions, such as sleep disorders, depression, and cognitive enhancement. However, they can also have adverse effects, including anxiety, agitation, seizures, and even neurotoxicity at high doses. Examples of GABA antagonists include picrotoxin, bicuculline, and flumazenil.
Postoperative pain is defined as the pain or discomfort experienced by patients following a surgical procedure. It can vary in intensity and duration depending on the type of surgery performed, individual pain tolerance, and other factors. The pain may be caused by tissue trauma, inflammation, or nerve damage resulting from the surgical intervention. Proper assessment and management of postoperative pain is essential to promote recovery, prevent complications, and improve patient satisfaction.
Histamine H1 antagonists, also known as H1 blockers or antihistamines, are a class of medications that work by blocking the action of histamine at the H1 receptor. Histamine is a chemical mediator released by mast cells and basophils in response to an allergic reaction or injury. It causes various symptoms such as itching, sneezing, runny nose, and wheal and flare reactions (hives).
H1 antagonists prevent the binding of histamine to its receptor, thereby alleviating these symptoms. They are commonly used to treat allergic conditions such as hay fever, hives, and eczema, as well as motion sickness and insomnia. Examples of H1 antagonists include diphenhydramine (Benadryl), loratadine (Claritin), cetirizine (Zyrtec), and doxylamine (Unisom).
Purinergic P1 receptor antagonists are a class of pharmaceutical drugs that block the activity of purinergic P1 receptors, which are a type of G-protein coupled receptor found in many tissues throughout the body. These receptors are activated by extracellular nucleotides such as adenosine and ATP, and play important roles in regulating a variety of physiological processes, including cardiovascular function, neurotransmission, and immune response.
Purinergic P1 receptor antagonists work by binding to these receptors and preventing them from being activated by nucleotides. This can have various therapeutic effects, depending on the specific receptor subtype that is targeted. For example, A1 receptor antagonists have been shown to improve cardiac function in heart failure, while A2A receptor antagonists have potential as anti-inflammatory and neuroprotective agents.
However, it's important to note that the use of purinergic P1 receptor antagonists is still an area of active research, and more studies are needed to fully understand their mechanisms of action and therapeutic potential.
Preanesthetic medication, also known as premedication, refers to the administration of medications before anesthesia to help prepare the patient for the upcoming procedure. These medications can serve various purposes, such as:
1. Anxiolysis: Reducing anxiety and promoting relaxation in patients before surgery.
2. Amnesia: Causing temporary memory loss to help patients forget the events leading up to the surgery.
3. Analgesia: Providing pain relief to minimize discomfort during and after the procedure.
4. Antisialagogue: Decreasing saliva production to reduce the risk of aspiration during intubation.
5. Bronchodilation: Relaxing bronchial smooth muscles, which can help improve respiratory function in patients with obstructive lung diseases.
6. Antiemetic: Preventing or reducing the likelihood of postoperative nausea and vomiting.
7. Sedation: Inducing a state of calmness and drowsiness to facilitate a smooth induction of anesthesia.
Common preanesthetic medications include benzodiazepines (e.g., midazolam), opioids (e.g., fentanyl), anticholinergics (e.g., glycopyrrolate), and H1-antihistamines (e.g., diphenhydramine). The choice of preanesthetic medication depends on the patient's medical history, comorbidities, and the type of anesthesia to be administered.
Piperidines are not a medical term per se, but they are a class of organic compounds that have important applications in the pharmaceutical industry. Medically relevant piperidines include various drugs such as some antihistamines, antidepressants, and muscle relaxants.
A piperidine is a heterocyclic amine with a six-membered ring containing five carbon atoms and one nitrogen atom. The structure can be described as a cyclic secondary amine. Piperidines are found in some natural alkaloids, such as those derived from the pepper plant (Piper nigrum), which gives piperidines their name.
In a medical context, it is more common to encounter specific drugs that belong to the class of piperidines rather than the term itself.
Sprague-Dawley rats are a strain of albino laboratory rats that are widely used in scientific research. They were first developed by researchers H.H. Sprague and R.C. Dawley in the early 20th century, and have since become one of the most commonly used rat strains in biomedical research due to their relatively large size, ease of handling, and consistent genetic background.
Sprague-Dawley rats are outbred, which means that they are genetically diverse and do not suffer from the same limitations as inbred strains, which can have reduced fertility and increased susceptibility to certain diseases. They are also characterized by their docile nature and low levels of aggression, making them easier to handle and study than some other rat strains.
These rats are used in a wide variety of research areas, including toxicology, pharmacology, nutrition, cancer, and behavioral studies. Because they are genetically diverse, Sprague-Dawley rats can be used to model a range of human diseases and conditions, making them an important tool in the development of new drugs and therapies.
Histamine antagonists, also known as histamine blockers or H1-blockers, are a class of medications that work by blocking the action of histamine, a substance in the body that is released during an allergic reaction. Histamine causes many of the symptoms of an allergic response, such as itching, sneezing, runny nose, and hives. By blocking the effects of histamine, these medications can help to relieve or prevent allergy symptoms.
Histamine antagonists are often used to treat conditions such as hay fever, hives, and other allergic reactions. They may also be used to treat stomach ulcers caused by excessive production of stomach acid. Some examples of histamine antagonists include diphenhydramine (Benadryl), loratadine (Claritin), and famotidine (Pepcid).
It's important to note that while histamine antagonists can be effective at relieving allergy symptoms, they do not cure allergies or prevent the release of histamine. They simply block its effects. It's also worth noting that these medications can have side effects, such as drowsiness, dry mouth, and dizziness, so it's important to follow your healthcare provider's instructions carefully when taking them.
Nicotinic antagonists are a class of drugs that block the action of nicotine at nicotinic acetylcholine receptors (nAChRs). These receptors are found in the nervous system and are activated by the neurotransmitter acetylcholine, as well as by nicotine. When nicotine binds to these receptors, it can cause the release of various neurotransmitters, including dopamine, which can lead to rewarding effects and addiction.
Nicotinic antagonists work by binding to nAChRs and preventing nicotine from activating them. This can help to reduce the rewarding effects of nicotine and may be useful in treating nicotine addiction. Examples of nicotinic antagonists include mecamylamine, varenicline, and cytisine.
It's important to note that while nicotinic antagonists can help with nicotine addiction, they can also have side effects, such as nausea, vomiting, and abnormal dreams. Additionally, some people may experience more serious side effects, such as seizures or cardiovascular problems, so it's important to use these medications under the close supervision of a healthcare provider.
Adenosine A2 receptor antagonists are a class of pharmaceutical compounds that block the action of adenosine at A2 receptors. Adenosine is a naturally occurring molecule in the body that acts as a neurotransmitter and has various physiological effects, including vasodilation and inhibition of heart rate.
Adenosine A2 receptor antagonists work by binding to A2 receptors and preventing adenosine from activating them. This results in the opposite effect of adenosine, leading to vasoconstriction and increased heart rate. These drugs are used for a variety of medical conditions, including asthma, chronic obstructive pulmonary disease (COPD), and heart failure.
Examples of Adenosine A2 receptor antagonists include theophylline, caffeine, and some newer drugs such asistradefylline and tozadenant. These drugs have different pharmacological properties and are used for specific medical conditions. It is important to note that adenosine A2 receptor antagonists can have side effects, including restlessness, insomnia, and gastrointestinal symptoms, and should be used under the guidance of a healthcare professional.
Adrenergic alpha-1 receptor antagonists, also known as alpha-blockers, are a class of medications that block the effects of the neurotransmitter norepinephrine at alpha-1 receptors. These receptors are found in various tissues throughout the body, including the smooth muscle of blood vessels, the bladder, and the eye.
When norepinephrine binds to alpha-1 receptors, it causes smooth muscle to contract, leading to vasoconstriction (constriction of blood vessels), increased blood pressure, and other effects. By blocking these receptors, alpha-blockers can cause relaxation of smooth muscle, leading to vasodilation (expansion of blood vessels), decreased blood pressure, and other effects.
Alpha-blockers are used in the treatment of various medical conditions, including hypertension (high blood pressure), benign prostatic hyperplasia (enlarged prostate), and pheochromocytoma (a rare tumor of the adrenal gland). Examples of alpha-blockers include doxazosin, prazosin, and terazosin.
It's important to note that while alpha-blockers can be effective in treating certain medical conditions, they can also have side effects, such as dizziness, lightheadedness, and orthostatic hypotension (a sudden drop in blood pressure when standing up). As with any medication, it's important to use alpha-blockers under the guidance of a healthcare provider.
Naltrexone is a medication that is primarily used to manage alcohol dependence and opioid dependence. It works by blocking the effects of opioids and alcohol on the brain, reducing the euphoric feelings and cravings associated with their use. Naltrexone comes in the form of a tablet that is taken orally, and it has no potential for abuse or dependence.
Medically, naltrexone is classified as an opioid antagonist, which means that it binds to opioid receptors in the brain without activating them, thereby blocking the effects of opioids such as heroin, morphine, and oxycodone. It also reduces the rewarding effects of alcohol by blocking the release of endorphins, which are natural chemicals in the brain that produce feelings of pleasure.
Naltrexone is often used as part of a comprehensive treatment program for addiction, along with counseling, behavioral therapy, and support groups. It can help individuals maintain abstinence from opioids or alcohol by reducing cravings and preventing relapse. Naltrexone is generally safe and well-tolerated, but it may cause side effects such as nausea, headache, dizziness, and fatigue in some people.
It's important to note that naltrexone should only be used under the supervision of a healthcare provider, and it is not recommended for individuals who are currently taking opioids or who have recently stopped using them, as it can cause withdrawal symptoms. Additionally, naltrexone may interact with other medications, so it's important to inform your healthcare provider of all medications you are taking before starting naltrexone therapy.
Purinergic P2 receptor antagonists are pharmaceutical agents that block the activity of P2 receptors, which are a type of cell surface receptor that binds extracellular nucleotides such as ATP and ADP. These receptors play important roles in various physiological processes, including neurotransmission, inflammation, and platelet aggregation.
P2 receptors are divided into two main subfamilies: P2X and P2Y. The P2X receptors are ligand-gated ion channels that allow the flow of ions across the cell membrane upon activation, while the P2Y receptors are G protein-coupled receptors that activate intracellular signaling pathways.
Purinergic P2 receptor antagonists are used in clinical medicine to treat various conditions, such as chronic pain, urinary incontinence, and cardiovascular diseases. For example, the P2X3 receptor antagonist gefapixant is being investigated for the treatment of refractory chronic cough, while the P2Y12 receptor antagonists clopidogrel and ticagrelor are used to prevent thrombosis in patients with acute coronary syndrome.
Overall, purinergic P2 receptor antagonists offer a promising therapeutic approach for various diseases by targeting specific receptors involved in pathological processes.
A spasm is a sudden, involuntary contraction or tightening of a muscle, group of muscles, or a hollow organ such as the ureter or bronchi. Spasms can occur as a result of various factors including muscle fatigue, injury, irritation, or abnormal nerve activity. They can cause pain and discomfort, and in some cases, interfere with normal bodily functions. For example, a spasm in the bronchi can cause difficulty breathing, while a spasm in the ureter can cause severe pain and may lead to a kidney stone blockage. The treatment for spasms depends on the underlying cause and may include medication, physical therapy, or lifestyle changes.
Hydrocodone is an opioid medication used to treat severe pain. It works by changing how the brain and nervous system respond to pain. Medically, it's defined as a semisynthetic opioid analgesic, synthesized from codeine, one of the natural opiates found in the resin of the poppy seed pod.
Hydrocodone is available only in combination with other drugs, such as acetaminophen or ibuprofen, which are added to enhance its pain-relieving effects and/or to prevent abuse and overdose. Common brand names include Vicodin, Lortab, and Norco.
Like all opioids, hydrocodone carries a risk of addiction and dependence, and it should be used only under the supervision of a healthcare provider. It's also important to note that misuse or abuse of hydrocodone can lead to overdose and death.
Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. It is a complex phenomenon that can result from various stimuli, such as thermal, mechanical, or chemical irritation, and it can be acute or chronic. The perception of pain involves the activation of specialized nerve cells called nociceptors, which transmit signals to the brain via the spinal cord. These signals are then processed in different regions of the brain, leading to the conscious experience of pain. It's important to note that pain is a highly individual and subjective experience, and its perception can vary widely among individuals.
Inert Gas Narcosis (IGN), also known as nitrogen narcosis or raptores narcosis, is a reversible alteration in consciousness, perception, and behavior that can occur in divers who breathe gas mixtures with high partial pressures of inert gases, such as nitrogen or helium, at depth. It is caused by the anesthetic effect of these gases on the central nervous system and is often described as feeling drunk or euphoric. The symptoms typically occur at depths greater than 30 meters (100 feet) and can include impaired judgment, memory, and coordination, which can increase the risk of accidents and injuries underwater. IGN is managed by ascending to shallower depths, where the partial pressure of the inert gas decreases, and by using gas mixtures with lower fractions of inert gases.
Serotonin 5-HT3 receptor antagonists are a class of medications that work by blocking the serotonin 5-HT3 receptors, which are found in the gastrointestinal tract and the brain. These receptors play a role in regulating nausea and vomiting, among other functions.
When serotonin binds to these receptors, it can trigger a series of events that lead to nausea and vomiting, particularly in response to chemotherapy or surgery. By blocking the 5-HT3 receptors, serotonin cannot bind to them and therefore cannot trigger these events, which helps to reduce nausea and vomiting.
Examples of 5-HT3 receptor antagonists include ondansetron (Zofran), granisetron (Kytril), palonosetron (Aloxi), and dolasetron (Anzemet). These medications are commonly used to prevent and treat nausea and vomiting associated with chemotherapy, radiation therapy, and surgery.
Substance-related disorders, as defined in the Diagnostic and Statistical Manual of Mental Disorders (DSM-5), refer to a group of conditions caused by the use of substances such as alcohol, drugs, or medicines. These disorders are characterized by a problematic pattern of using a substance that leads to clinically significant impairment or distress. They can be divided into two main categories: substance use disorders and substance-induced disorders. Substance use disorders involve a pattern of compulsive use despite negative consequences, while substance-induced disorders include conditions such as intoxication, withdrawal, and substance/medication-induced mental disorders. The specific diagnosis depends on the type of substance involved, the patterns of use, and the presence or absence of physiological dependence.
Opioid receptors are a type of G protein-coupled receptor (GPCR) found in the cell membranes of certain neurons in the central and peripheral nervous system. They bind to opioids, which are chemicals that can block pain signals and produce a sense of well-being. There are four main types of opioid receptors: mu, delta, kappa, and nociceptin. These receptors play a role in the regulation of pain, reward, addiction, and other physiological functions. Activation of opioid receptors can lead to both therapeutic effects (such as pain relief) and adverse effects (such as respiratory depression and constipation).
Serotonin 5-HT2 receptor antagonists are a class of drugs that block the action of serotonin, a neurotransmitter, at 5-HT2 receptors. These receptors are found in the central and peripheral nervous systems and are involved in various physiological functions such as mood regulation, cognition, appetite control, and vasoconstriction.
By blocking the action of serotonin at these receptors, serotonin 5-HT2 receptor antagonists can produce a range of effects depending on the specific receptor subtype that they target. For example, some serotonin 5-HT2 receptor antagonists are used to treat psychiatric disorders such as schizophrenia and depression, while others are used to treat migraines or prevent nausea and vomiting associated with chemotherapy.
Some common examples of serotonin 5-HT2 receptor antagonists include risperidone, olanzapine, and paliperidone (used for the treatment of schizophrenia), mirtazapine (used for the treatment of depression), sumatriptan (used for the treatment of migraines), and ondansetron (used to prevent nausea and vomiting).
Dibenzocycloheptenes are a class of chemical compounds that contain a dibenzocycloheptene moiety, which is a seven-membered ring with two benzene rings fused on either side. This structure gives the molecule a unique set of physical and chemical properties, including its aromaticity and reactivity.
In medical terms, dibenzocycloheptenes are not commonly used as therapeutic agents themselves. However, some derivatives of this class of compounds have been investigated for their potential medicinal properties. For example, certain dibenzocycloheptene derivatives have been shown to have anti-inflammatory, analgesic, and antipyretic effects, making them potentially useful as drugs for treating pain and inflammation.
It's important to note that while some dibenzocycloheptene derivatives may have potential therapeutic uses, they can also have side effects and risks, just like any other medication. Therefore, it's essential to consult with a healthcare professional before using any medication containing this or any other active ingredient.
Alcoholics Anonymous (AA) is a international fellowship of individuals who have had a drinking problem and wish to do something about it. AA is nonprofessional, self-supporting, multiracial, apolitical, and available almost everywhere. There are no age or education requirements, and membership is open to anyone who wants to do something about their drinking problem.
AA's primary purpose is to help alcoholics stop drinking, though the organization also aims to inspire personal growth and improve the quality of life for its members. AA's program of recovery is based on the Twelve Steps, a set of principles that, when practiced as a way of life, can expel the obsession to drink and enable the sufferer to become happily and usefully whole.
The organization holds regular meetings where members share their experiences, strength, and hope to help one another recover from alcoholism. AA also offers sponsorship, where more experienced members work with newer members to guide them through the Twelve Step program.
It's important to note that while AA has helped many people achieve and maintain sobriety, it is not the only path to recovery from alcoholism. Other evidence-based treatments, such as medication-assisted treatment and behavioral therapy, are also effective for some individuals.
Adenosine A1 receptor antagonists are a class of pharmaceutical compounds that block the action of adenosine at A1 receptors. Adenosine is a naturally occurring purine nucleoside that acts as a neurotransmitter and modulator of various physiological processes, including cardiovascular function, neuronal excitability, and immune response.
Adenosine exerts its effects by binding to specific receptors on the surface of cells, including A1, A2A, A2B, and A3 receptors. The activation of A1 receptors leads to a variety of physiological responses, such as vasodilation, negative chronotropy (slowing of heart rate), and negative inotropy (reduced contractility) of the heart, as well as inhibition of neurotransmitter release in the brain.
Adenosine A1 receptor antagonists work by binding to and blocking the action of adenosine at A1 receptors, thereby preventing or reducing its effects on these physiological processes. These drugs have been investigated for their potential therapeutic uses in various conditions, such as heart failure, cardiac arrest, and neurological disorders.
Examples of adenosine A1 receptor antagonists include:
* Dipyridamole: a vasodilator used to treat peripheral arterial disease and to prevent blood clots.
* Caffeine: a natural stimulant found in coffee, tea, and chocolate, which acts as a weak A1 receptor antagonist.
* Rolofylline: an experimental drug that has been investigated for its potential use in treating acute ischemic stroke and traumatic brain injury.
* KW-3902: another experimental drug that has been studied for its potential therapeutic effects in heart failure, cardiac arrest, and neurodegenerative disorders.
It's important to note that adenosine A1 receptor antagonists may have side effects and potential risks, and their use should be monitored and managed by healthcare professionals.
Oxycodone is a semi-synthetic opioid analgesic, which means it's a painkiller that's synthesized from thebaine, an alkaloid found in the poppy plant. It's a strong pain reliever used to treat moderate to severe pain and is often prescribed for around-the-clock treatment of chronic pain. Oxycodone can be found in various forms, such as immediate-release tablets, extended-release tablets, capsules, and solutions.
Common brand names for oxycodone include OxyContin (extended-release), Percocet (oxycodone + acetaminophen), and Roxicodone (immediate-release). As an opioid, oxycodone works by binding to specific receptors in the brain, spinal cord, and gut, reducing the perception of pain and decreasing the emotional response to pain.
However, it's important to note that oxycodone has a high potential for abuse and addiction due to its euphoric effects. Misuse or prolonged use can lead to physical dependence, tolerance, and withdrawal symptoms upon discontinuation. Therefore, it should be taken exactly as prescribed by a healthcare professional and used with caution.
Drug tolerance is a medical concept that refers to the decreased response to a drug following its repeated use, requiring higher doses to achieve the same effect. This occurs because the body adapts to the presence of the drug, leading to changes in the function or expression of targets that the drug acts upon, such as receptors or enzymes. Tolerance can develop to various types of drugs, including opioids, benzodiazepines, and alcohol, and it is often associated with physical dependence and addiction. It's important to note that tolerance is different from resistance, which refers to the ability of a pathogen to survive or grow in the presence of a drug, such as antibiotics.
Leukotriene antagonists are a class of medications that work by blocking the action of leukotrienes, which are chemicals released by the immune system in response to an allergen or irritant. Leukotrienes cause airway muscles to tighten and inflammation in the airways, leading to symptoms such as wheezing, shortness of breath, and coughing. By blocking the action of leukotrienes, leukotriene antagonists can help relieve these symptoms and improve lung function. These medications are often used to treat asthma and allergic rhinitis (hay fever). Examples of leukotriene antagonists include montelukast, zafirlukast, and pranlukast.
Angiotensin receptor antagonists (ARAs), also known as angiotensin II receptor blockers (ARBs), are a class of medications used to treat hypertension, heart failure, and protect against kidney damage in patients with diabetes. They work by blocking the action of angiotensin II, a potent vasoconstrictor and hormone that increases blood pressure and promotes tissue fibrosis. By blocking the binding of angiotensin II to its receptors, ARAs cause relaxation of blood vessels, decreased sodium and water retention, and reduced cardiac remodeling, ultimately leading to improved cardiovascular function and reduced risk of organ damage. Examples of ARAs include losartan, valsartan, irbesartan, and candesartan.
Opioid mu receptors, also known as mu-opioid receptors (MORs), are a type of G protein-coupled receptor that binds to opioids, a class of chemicals that include both natural and synthetic painkillers. These receptors are found in the brain, spinal cord, and gastrointestinal tract, and play a key role in mediating the effects of opioid drugs such as morphine, heroin, and oxycodone.
MORs are involved in pain modulation, reward processing, respiratory depression, and physical dependence. Activation of MORs can lead to feelings of euphoria, decreased perception of pain, and slowed breathing. Prolonged activation of these receptors can also result in tolerance, where higher doses of the drug are required to achieve the same effect, and dependence, where withdrawal symptoms occur when the drug is discontinued.
MORs have three main subtypes: MOR-1, MOR-2, and MOR-3, with MOR-1 being the most widely studied and clinically relevant. Selective agonists for MOR-1, such as fentanyl and sufentanil, are commonly used in anesthesia and pain management. However, the abuse potential and risk of overdose associated with these drugs make them a significant public health concern.
Morphine dependence is a medical condition characterized by a physical and psychological dependency on morphine, a potent opioid analgesic. This dependence develops as a result of repeated use or abuse of morphine, leading to changes in the brain's reward and pleasure pathways. The Diagnostic and Statistical Manual of Mental Disorders, 5th Edition (DSM-5) outlines the following criteria for diagnosing opioid dependence, which includes morphine:
A. A problematic pattern of opioid use leading to clinically significant impairment or distress, as manifested by at least two of the following, occurring within a 12-month period:
1. Opioids are often taken in larger amounts or over a longer period than was intended.
2. There is a persistent desire or unsuccessful efforts to cut down or control opioid use.
3. A great deal of time is spent in activities necessary to obtain the opioid, use the opioid, or recover from its effects.
4. Craving, or a strong desire or urge to use opioids.
5. Recurrent opioid use resulting in a failure to fulfill major role obligations at work, school, or home.
6. Continued opioid use despite having persistent or recurrent social or interpersonal problems caused or exacerbated by the effects of opioids.
7. Important social, occupational, or recreational activities are given up or reduced because of opioid use.
8. Recurrent opioid use in situations in which it is physically hazardous.
9. Continued opioid use despite knowing that a physical or psychological problem is likely to have been caused or exacerbated by opioids.
10. Tolerance, as defined by either of the following:
a. A need for markedly increased amounts of opioids to achieve intoxication or desired effect.
b. A markedly diminished effect with continued use of the same amount of an opioid.
11. Withdrawal, as manifested by either of the following:
a. The characteristic opioid withdrawal syndrome.
b. The same (or a closely related) substance is taken to relieve or avoid withdrawal symptoms.
Additionally, it's important to note that if someone has been using opioids for an extended period and suddenly stops taking them, they may experience withdrawal symptoms. These can include:
- Anxiety
- Muscle aches
- Insomnia
- Runny nose
- Sweating
- Diarrhea
- Nausea or vomiting
- Abdominal cramping
- Dilated pupils
If you or someone you know is struggling with opioid use, it's essential to seek professional help. There are many resources available, including inpatient and outpatient treatment programs, support groups, and medications that can help manage withdrawal symptoms and cravings.
Analgesia is defined as the absence or relief of pain in a patient, achieved through various medical means. It is derived from the Greek word "an-" meaning without and "algein" meaning to feel pain. Analgesics are medications that are used to reduce pain without causing loss of consciousness, and they work by blocking the transmission of pain signals to the brain.
Examples of analgesics include over-the-counter medications such as acetaminophen (Tylenol) and nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen (Advil, Motrin) and naproxen (Aleve). Prescription opioid painkillers, such as oxycodone (OxyContin, Percocet) and hydrocodone (Vicodin), are also used for pain relief but carry a higher risk of addiction and abuse.
Analgesia can also be achieved through non-pharmacological means, such as through nerve blocks, spinal cord stimulation, acupuncture, and other complementary therapies. The choice of analgesic therapy depends on the type and severity of pain, as well as the patient's medical history and individual needs.
Anesthesia is a medical term that refers to the loss of sensation or awareness, usually induced by the administration of various drugs. It is commonly used during surgical procedures to prevent pain and discomfort. There are several types of anesthesia, including:
1. General anesthesia: This type of anesthesia causes a complete loss of consciousness and is typically used for major surgeries.
2. Regional anesthesia: This type of anesthesia numbs a specific area of the body, such as an arm or leg, while the patient remains conscious.
3. Local anesthesia: This type of anesthesia numbs a small area of the body, such as a cut or wound, and is typically used for minor procedures.
Anesthesia can be administered through various routes, including injection, inhalation, or topical application. The choice of anesthesia depends on several factors, including the type and duration of the procedure, the patient's medical history, and their overall health. Anesthesiologists are medical professionals who specialize in administering anesthesia and monitoring patients during surgical procedures to ensure their safety and comfort.
Iso Nipecotic Acids are a type of organic compound that are structurally related to nipecotic acid, which is a GABAergic agent. Iso Nipecotic Acids have a similar chemical structure to nipecotic acid, but with the position of the amino group and the carboxylic acid group reversed.
These compounds are known to act as potent and selective antagonists at certain subtypes of nicotinic acetylcholine receptors (nAChRs), which are important targets for the development of drugs for various neurological disorders, including Alzheimer's disease, Parkinson's disease, and schizophrenia.
Iso Nipecotic Acids have been used in research to study the role of nAChRs in the brain and to investigate their potential as therapeutic agents for various neurological disorders. However, it is important to note that these compounds are not approved for use in humans and should only be used in a controlled laboratory setting under the guidance of trained researchers.
Substance Withdrawal Syndrome is a medically recognized condition that occurs when an individual who has been using certain substances, such as alcohol, opioids, or benzodiazepines, suddenly stops or significantly reduces their use. The syndrome is characterized by a specific set of symptoms that can be physical, cognitive, and emotional in nature. These symptoms can vary widely depending on the substance that was being used, the length and intensity of the addiction, and individual factors such as genetics, age, and overall health.
The Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5), published by the American Psychiatric Association, provides the following diagnostic criteria for Substance Withdrawal Syndrome:
A. The development of objective evidence of withdrawal, referring to the specific physiological changes associated with the particular substance, or subjective evidence of withdrawal, characterized by the individual's report of symptoms that correspond to the typical withdrawal syndrome for the substance.
B. The symptoms cause clinically significant distress or impairment in social, occupational, or other important areas of functioning.
C. The symptoms are not better explained by co-occurring mental, medical, or other substance use disorders.
D. The withdrawal syndrome is not attributable to another medical condition and is not better accounted for by another mental disorder.
The DSM-5 also specifies that the diagnosis of Substance Withdrawal Syndrome should be substance-specific, meaning that it should specify the particular class of substances (e.g., alcohol, opioids, benzodiazepines) responsible for the withdrawal symptoms. This is important because different substances have distinct withdrawal syndromes and require different approaches to management and treatment.
In general, Substance Withdrawal Syndrome can be a challenging and potentially dangerous condition that requires professional medical supervision and support during the detoxification process. The specific symptoms and their severity will vary depending on the substance involved, but they may include:
* For alcohol: tremors, seizures, hallucinations, agitation, anxiety, nausea, vomiting, and insomnia.
* For opioids: muscle aches, restlessness, lacrimation (tearing), rhinorrhea (runny nose), yawning, perspiration, chills, mydriasis (dilated pupils), piloerection (goosebumps), nausea or vomiting, diarrhea, and abdominal cramps.
* For benzodiazepines: anxiety, irritability, insomnia, restlessness, confusion, hallucinations, seizures, and increased heart rate and blood pressure.
It is essential to consult with a healthcare professional if you or someone you know is experiencing symptoms of Substance Withdrawal Syndrome. They can provide appropriate medical care, support, and referrals for further treatment as needed.
In the field of medicine, "time factors" refer to the duration of symptoms or time elapsed since the onset of a medical condition, which can have significant implications for diagnosis and treatment. Understanding time factors is crucial in determining the progression of a disease, evaluating the effectiveness of treatments, and making critical decisions regarding patient care.
For example, in stroke management, "time is brain," meaning that rapid intervention within a specific time frame (usually within 4.5 hours) is essential to administering tissue plasminogen activator (tPA), a clot-busting drug that can minimize brain damage and improve patient outcomes. Similarly, in trauma care, the "golden hour" concept emphasizes the importance of providing definitive care within the first 60 minutes after injury to increase survival rates and reduce morbidity.
Time factors also play a role in monitoring the progression of chronic conditions like diabetes or heart disease, where regular follow-ups and assessments help determine appropriate treatment adjustments and prevent complications. In infectious diseases, time factors are crucial for initiating antibiotic therapy and identifying potential outbreaks to control their spread.
Overall, "time factors" encompass the significance of recognizing and acting promptly in various medical scenarios to optimize patient outcomes and provide effective care.
"Wistar rats" are a strain of albino rats that are widely used in laboratory research. They were developed at the Wistar Institute in Philadelphia, USA, and were first introduced in 1906. Wistar rats are outbred, which means that they are genetically diverse and do not have a fixed set of genetic characteristics like inbred strains.
Wistar rats are commonly used as animal models in biomedical research because of their size, ease of handling, and relatively low cost. They are used in a wide range of research areas, including toxicology, pharmacology, nutrition, cancer, cardiovascular disease, and behavioral studies. Wistar rats are also used in safety testing of drugs, medical devices, and other products.
Wistar rats are typically larger than many other rat strains, with males weighing between 500-700 grams and females weighing between 250-350 grams. They have a lifespan of approximately 2-3 years. Wistar rats are also known for their docile and friendly nature, making them easy to handle and work with in the laboratory setting.
Pain measurement, in a medical context, refers to the quantification or evaluation of the intensity and/or unpleasantness of a patient's subjective pain experience. This is typically accomplished through the use of standardized self-report measures such as numerical rating scales (NRS), visual analog scales (VAS), or categorical scales (mild, moderate, severe). In some cases, physiological measures like heart rate, blood pressure, and facial expressions may also be used to supplement self-reported pain ratings. The goal of pain measurement is to help healthcare providers better understand the nature and severity of a patient's pain in order to develop an effective treatment plan.
Xorphanol
Conorfone
Alazocine
7-PET
Oripavine
BU-48
LY-88329
Phenazocine
Buprenorphine
Peripherally acting μ-opioid receptor antagonist
Huda Akil
Methylnaltrexone
Oxilorphan
Butorphanol
Accelerans nerve
Pethidine
Chlornaltrexamine
Drug injection
Diphenpipenol
AD-1211
MT-45
Max Fink
Pharmaco-electroencephalography
Noroxymorphone
British Columbia Ambulance Service
Jaime Murray
Nalmexone
Nalorphine dinicotinate
Equipment of an American combat medic
List of MeSH codes (D27)
Alcohol-Related Psychosis Medication: Benzodiazepines, Antipsychotics, Antialcoholic agents, Atypical antipsychotics, Narcotic...
Treatment of drug overdosage with naloxone, a specific narcotic antagonist
Alcohol-Related Psychosis Medication: Benzodiazepines, Antipsychotics, Antialcoholic agents, Atypical antipsychotics, Narcotic...
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The cardiovascular responses to mu opioid agonist and antagonist in conscious normal and obese rats
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Plus it
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Shamrock Labels 2020 Catalog
Diphen HCL Atropine
RX List database - use generic or medication brand name - GlobalRPH
Do opioid antagonists such as naltrexone help people to stop smoking? | Cochrane
Antinociceptive Activity of Trichilia catigua Hydroalcoholic Extract: New Evidence on Its Dopaminergic Effects
Urban, individuals of color are impacted by fentanyl-contaminated heroin.
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Sufenta (sufentanil) dosing, indications, interactions, adverse effects, and more
Naloxone10
- Accordingly, rats pre-treated subcutaneously with repeated nicotine were given a single dose of the opiate receptor antagonist naloxone (0.1-10.0 mg/kg, i.p.) or saline as a co-treatment with nicotine or saline 10 min prior to acute footshock stress. (nih.gov)
- The present double-blind, randomized study examined behavioral pain responses in healthy human volunteers during mindfulness meditation and a nonmanipulation control condition in response to noxious heat and intravenous administration of the opioid antagonist naloxone (0.15 mg/kg bolus + 0.1 mg/kg/h infusion) or saline placebo. (jneurosci.org)
- To address this question, the present study examined pain reports during meditation in response to noxious heat and administration of the opioid antagonist naloxone and placebo saline. (jneurosci.org)
- is reversed by administration of the opioid antagonist naloxone. (jneurosci.org)
- endogenous or exogenous opioids and the pure narcotic antagonist, naloxone. (druglibrary.org)
- The drugs include naloxone and the longer-acting opioid antagonist naltrexone. (cochrane.org)
- We searched the Cochrane Tobacco Addiction Group Specialised Register for trials of naloxone, naltrexone and other opioid antagonists and conducted an additional search of MEDLINE using 'Narcotic antagonists' and smoking terms in April 2013. (cochrane.org)
- During pregnancy, emergence of endogenous opioid inhibition of oxytocin neurons is revealed by increased oxytocin secretion after administration of the opioid receptor antagonist, naloxone. (ed.ac.uk)
- Naloxone is an opioid antagonist used to treat narcotic overdoses and is generally considered the treatment of choice for immediate administration in instances of opioid overdose. (biospace.com)
- Narcotic Antagonists: Naloxone Actions Opioid antagonists block ( or antagonize ) opiate-receptors sites, principal use is the treatment. (nursesnotehelp.com)
Analgesics5
- The present investigation sought to determine whether the stimulus properties of morphine and lysergic acid diethylamide (LSD) would generalize to several narcotic analgesics which vary in their subjective effects. (erowid.org)
- After discriminated responding was stable, stimulus generalization tests with narcotic analgesics and antagonists showed that the stimulus properties of morphine generalized to methadone and meperidine, and partially to pentazocine, all of which produce morphine-like subjective effects in humans. (erowid.org)
- Patients receiving Buprenex in the presence of other narcotic analgesics, general anesthetics, antihistamines, benzodiazepines, phenothiazines, other tranquilizers, sedative/hypnotics or other CNS depressants (including alcohol) may exhibit increased CNS depression. (druglib.com)
- Using the technique of intracerebroventricular (i.c.v.) microinjection in conscious mice and rats, the possible involvement of putative central nervous system transmitter-substances in the anti-nociceptive effects of morphine and the narcotic-antagonist analgesics nalorphine and pentazocine has been investigated. (aston.ac.uk)
- The picture with regard to the narcotic-antagonist analgesics is less clear, partly because of the inadequacies of the test methods available, and partly because the two agents chosen in this group (nalorphine and pentazocine) appear to possess quite different spectra of pharmacological activity, despite being classified in the same group. (aston.ac.uk)
Morphine3
- Like morphine and heroin, methadone is a narcotic and therefore, by definition, an addicting drug. (druglibrary.org)
- Opioid antagonists are a type of drug which blunts the effects of narcotics such as heroin and morphine, and might help reduce nicotine addiction by blocking some of the rewarding effects of smoking. (cochrane.org)
- Stimulus generalization tests to each other narcotic antagonist, d-amphetamine (0.1-1.6 :ng/kg 8.C.), morphine (0.6 2.5 mg/kg s.c.), and LSD (0.025-0.4 mg/kg s.c.) were performed. (erowid.org)
Opiate2
- Narcotic antagonist treatment using Naltrexone for opiate addicts usually is conducted in outpatient settings although initiation of the medication often begins after medical detoxification in a residential setting. (healthyplace.com)
- Naltrexone is a long-acting synthetic opiate antagonist with few side effects that is taken orally either daily or three times a week for a sustained period of time. (healthyplace.com)
Naltrexone3
- Do opioid antagonists such as naltrexone help people to stop smoking? (cochrane.org)
- Our review identified eight trials of naltrexone, a long-acting opioid antagonist. (cochrane.org)
- The available evidence does not suggest that opioid antagonists such as naltrexone assist smoking cessation. (cochrane.org)
Overdose3
- I believe this underscores the need for additional treatment alternatives for narcotic overdose," said Dr. Dennis J. Carlo, President and Chief Executive Officer of Adamis Pharmaceuticals. (biospace.com)
- If the proper narcotic antagonist (drug to counteract the effects of narcotics) can be given, recovery from an acute overdose occurs within 24 to 48 hours. (medlineplus.gov)
- A narcotic antagonist used in opioid overdose. (drugbank.com)
Agonists1
- Inactive as either antagonists or agonists on the H2-receptor were psilocin, bufotenine, mescaline, different classes of anticonvulsant drugs, barbiturates and narcotic agonists and antagonists, as well as lithium chloride, chlordiazepc, ice, THC and procaine. (erowid.org)
Methadone2
- Thus the antagonists, like methadone, are 'blocking agents. (druglibrary.org)
- A psychiatrist who has had experience with both methadone and antagonist maintenance programs contrasts 'the relaxed, jovial atmosphere of a methadone ward,' where patients are free of the postaddiction syndrome, with 'the tension, frustration, and anxiety that characterize a cyclazocine ward. (druglibrary.org)
Antidepressants2
- Narcotic antagonists and antidepressants can help. (projectstrada.org)
- Some medications used to treat gambling addiction include antidepressants, mood stabilizers, and narcotic antagonists. (liguriapocket.com)
Heroin2
- What the large-scale use of a long-acting narcotic antagonist would in fact produce, however, is a horde of men, women, and adolescents assailed by anxiety and depression, with a continuing craving for heroin and no way to assuage their distress (except, perhaps, via alcoholism). (druglibrary.org)
- While it's prescribed to treat everything from severe diarrhea to cancer pain, "Oxy" also has an extremely high abuse potential, producing feelings of euphoria similar to another opioid narcotic: heroin. (thedailybeast.com)
Nicotine1
- We also reviewed, for descriptive purposes, results from short-term laboratory-based studies of opioid antagonists designed to evaluate psycho-biological mediating variables associated with nicotine dependence. (cochrane.org)
Placebo1
- We considered randomised controlled trials comparing opioid antagonists to placebo or an alternative therapeutic control for smoking cessation. (cochrane.org)
20231
- In May 2023, the Bureau of Narcotic Enforcement will be releasing an update to the Prescription Monitoring Program (PMP) Registry Confidential Drug Utilization Report. (ny.gov)
Treatment2
- treatment involves narcotic antagonists and supportive therapy. (vin.com)
- Methylnaltrexone is used to treat constipation caused by opioid (narcotic) pain medications in people with chronic (ongoing) pain that is not caused by cancer but may be related to a previous cancer or cancer treatment. (medlineplus.gov)
Effects4
- Opioid (narcotic) antagonists are of particular interest to investigators as potential agents to attenuate the rewarding effects of cigarette smoking. (cochrane.org)
- Studies utilizing NMDA-receptor antagonists like ketamine, known for creating narcotic and psychotomimetic effects, aim to understand schizophrenia-related glutamate signaling deficiencies. (news-medical.net)
- Because of the narcotic antagonist activity of Buprenex, use in the physically dependent individual may result in withdrawal effects. (druglib.com)
- It works by protecting the bowel from the effects of opioid (narcotic) medications. (medlineplus.gov)
Smoking cessation1
- To evaluate the efficacy of opioid antagonists in promoting long-term smoking cessation. (cochrane.org)
Agents1
- Agents inhibiting the effect of narcotics on the central nervous system. (nih.gov)
Drugs1
- In 1971, despite the earlier failures of narcotic antagonists, ** interest was renewed in these drugs as a potential 'cure for addiction. (druglibrary.org)
Activity1
- the antagonist activity may provoke withdrawal Sx. (medscape.com)
Pain1
- By 2001, sales of the drug exceeded $1 billion, making Oxy the bestselling nongeneric narcotic pain reliever in the country. (thedailybeast.com)
Long-term1
- It was suggested, for example, that a long-term supply or 'depot' of an antagonist might be implanted somewhere in the addict's body, surrounded by a membrane that would release the drug at the desired rate continuously over a period of a month or even six months. (druglibrary.org)
Patient2
- The other major difference is that since the antagonists are not addicting, a patient can stop taking them at will. (druglibrary.org)
- Generall) with low body an absorption rate and the patient requires a narcotic antagonist. (stonecottagegardens.com)
People1
- Methylnaltrexone is to be taken by people who are taking opioid (narcotic) medications. (medlineplus.gov)
Assist1
- For IV: use only if a narcotic antagonist and facilities are immediately available to assist and control respiration. (oncologynurseadvisor.com)
Naltrexone6
- REVEX (nalmefene hydrochloride injection), an opioid antagonist, is a 6-methylene analogue of naltrexone. (nih.gov)
- Interestingly, neither the non-selective opioid receptor antagonist, naltrexone nor beta-funaltrexamine (beta-FNA), a highly selective MOR antagonist, blocked fentanyl mediated inhibition of TNFalpha-induced CXCL10 expression. (nih.gov)
- Naltrexone, a narcotic antagonist, can be an effective drug in the treatment of opiate addiction. (sbir.gov)
- In spite of the availability of a narcotic antagonist, naltrexone, which could be successful in the attenuation of alcohol drinking behavior, the societal problems of alcohol addiction remain. (sbir.gov)
- Structural analog of naltrexone, q.v., with opiate antagonist activity. (drugfuture.com)
- Neither the MOR-selective antagonist, D-Phe-Cys-Tyr-D-Trp-Arg-Pen-Thr-NH 2 (CTAP) nor the nonselective opioid receptor antagonist, naltrexone inhibited IFNγ + HIV-1 Tat-induced CXCL10 expression. (okstate.edu)
Analgesic3
- Analgesic narcotic antagonists. (wikipedia.org)
- Centrally acting analgesic with mixed narcotic agonist and antagonist action. (freezingblue.com)
- Diphenoxylate is an antidiarrheal agent chemically related to the narcotic analgesic meperidine. (medscape.com)
Humans3
- To assess the discriminative stimulus properties of mixed agonist- antagonist opioids in humans, postaddict volunteers were trained in a three- choice drug discrimination procedure to discriminate among the effects of saline (4 ml i.m.), hydromorphone (3 mg i.m.) and butorphanol (6 mg i.m. (johnshopkins.edu)
- Preston, KL & Bigelow, GE 1994, ' Drug discrimination assessment of agonist-antagonist opioids in humans: A three-choice saline-hydromorphone-butorphanol procedure ', Journal of Pharmacology and Experimental Therapeutics , vol. 271, no. 1, pp. 48-60. (johnshopkins.edu)
- Bigelow, G. E. / Drug discrimination assessment of agonist-antagonist opioids in humans : A three-choice saline-hydromorphone-butorphanol procedure . (johnshopkins.edu)
Selective2
- Afferent's lead investigational candidate, AF-219, is a selective, non-narcotic, orally-administered P2X3 antagonist currently being evaluated in a Phase 2b clinical trial for the treatment of refractory, chronic cough as well as in a Phase 2 clinical trial in idiopathic pulmonary fibrosis (IPF) with cough. (merck.com)
- We have utilized proinflammatory-induced CXCL10 expression in normal human astrocytes (NHA) as a model in which to assess the anti-inflammatory actions of the selective, mu-opioid receptor (MOR) antagonist, β-funaltrexamine (β-FNA). (okstate.edu)
Substances1
- Conveys the views and recommendations of an expert committee commissioned to assess selected narcotic drugs and psychotropic substances and to determine which should be recommended for control under existing international treaties. (who.int)
CTAP1
- Rats received microinjections of the μ-opioid receptor antagonist CTAP before these tests. (edu.au)
Opioids1
- Small increments are used rather than a large bolus injection in order to prevent narcotic withdrawal in the patient who is dependent on opioids. (medscape.com)
Estrogen1
- noun an antagonist for estrogen that is used in the treatment of breast cancer tamoxifen . (niftyword.com)
Inhibition1
- 3 Hl-antagonists (including cyproheptadine) blocked the H2 receptor (as shown by inhibition of dimaprit). (erowid.org)
Gastrointestinal1
- Drug classes that may be considered in the medical management of patients with postcholecystectomy syndrome include bulking agents, gastrointestinal (GI) antispasmodic agents, bile acid sequestrants, histamine H2 antagonists, and proton pump inhibitors (PPIs). (medscape.com)
Clinical2
- Clinical evaluation of narcotic antagonism: T. J. Gal, C. A. DiFazio, Anesthesiology 64, 175 (1986). (drugfuture.com)
- Opioid antagonists reduce the rate of relapse to drinking in clinical trials and reduce reinstatement in animal models of drug seeking. (edu.au)
Potential for abuse1
- It is still an opioid narcotic, however, with potential for abuse, dependency, and the onset of withdrawal symptoms when the user attempts to stop using it. (articlecity.com)
Connection1
- This is a "connection" page, showing publications Tara Wright has written about Narcotic Antagonists. (musc.edu)
Effective1
- Understanding the mechanism by which chemokine expression is suppressed, particularly by the opioid antagonist, beta-FNA, may provide insights into the development of safe and effective treatments for neuroinflammation. (nih.gov)
Reduce1
- Like antacids, H2-receptor antagonists do not reduce the frequency of reflux but do decrease the amount of acid in the refluxate by inhibiting acid production. (medscape.com)