Drug and Narcotic Control
Excitatory Amino Acid Antagonists
Neurokinin-1 Receptor Antagonists
Dose-Response Relationship, Drug
Histamine H2 Antagonists
Interleukin 1 Receptor Antagonist Protein
Histamine H1 Antagonists
Purinergic P1 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Adrenergic alpha-1 Receptor Antagonists
Purinergic P2 Receptor Antagonists
Inert Gas Narcosis
Serotonin 5-HT3 Receptor Antagonists
Serotonin 5-HT2 Receptor Antagonists
Adenosine A1 Receptor Antagonists
Angiotensin Receptor Antagonists
Receptors, Opioid, mu
Substance Withdrawal Syndrome
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 a synthetic opioid antagonist that is used to reverse the effects of opioid overdose. It works by binding to opioid receptors in the brain and body, blocking the effects of opioids such as morphine, heroin, and oxycodone. Nalorphine can be administered as an injection or nasal spray and is typically used in emergency situations to reverse the respiratory depression, sedation, and other symptoms of opioid overdose. It can also be used to treat opioid addiction by blocking the euphoric effects of opioids and reducing cravings. Nalorphine is a Schedule I controlled substance in the United States and is only available by prescription from a qualified healthcare provider.
Levorphanol is a synthetic opioid analgesic medication that is used to relieve moderate to severe pain. It is a derivative of the opiate morphine and is similar in structure to other opioids such as oxycodone and hydrocodone. Levorphanol is available in both oral and injectable forms and is often used in hospitals and other medical settings to manage pain in patients who are recovering from surgery or who have chronic pain conditions. It is a Schedule II controlled substance in the United States, which means that it has a high potential for abuse and dependence. Like other opioids, levorphanol can cause side effects such as drowsiness, nausea, constipation, and respiratory depression. It is important to use levorphanol only under the guidance of a healthcare professional and to follow their instructions carefully to minimize the risk of adverse effects.
Pentazocine is a synthetic opioid pain medication that is used to treat moderate to severe pain. It is a centrally acting analgesic that works by binding to opioid receptors in the brain and spinal cord, which reduces the perception of pain and produces feelings of euphoria. Pentazocine is available in both immediate-release and extended-release forms, and it is typically prescribed for short-term use only. It is often used to treat postoperative pain, as well as pain associated with chronic conditions such as cancer, arthritis, and fibromyalgia. Pentazocine can cause side effects such as dizziness, nausea, constipation, and respiratory depression. It can also be habit-forming and may lead to addiction if used for an extended period of time. As such, it is typically only prescribed to patients who have not responded to other pain medications or who cannot tolerate the side effects of other opioids.
Levallorphan is a synthetic opioid analgesic that is a metabolite of the drug levorphanol. It is a Schedule II controlled substance in the United States and is used in the treatment of moderate to severe pain. Levallorphan is also used as an antitussive (cough suppressant) and is sometimes used in combination with other drugs to treat opioid dependence. It is a potent opioid agonist that binds to the mu-opioid receptor in the brain and spinal cord, producing analgesic and sedative effects. However, levallorphan can also produce respiratory depression, constipation, and other side effects at high doses. It is important to note that levallorphan is not currently approved for use in the United States and is only available through special channels for research purposes.
Naloxone is a medication used to reverse the effects of opioid overdose. It works by binding to opioid receptors in the brain and body, blocking the effects of opioids and causing the person to breathe normally again. Naloxone is often administered as an injection, but it can also be administered nasally or intravenously. It is commonly used in emergency medical settings to treat opioid overdose, but it can also be used in non-emergency situations, such as in the management of chronic pain or opioid addiction.
Cyclazocine is a synthetic opioid analgesic that was developed in the 1960s. It is a centrally acting drug that is used to treat moderate to severe pain. Cyclazocine is a Schedule II controlled substance in the United States, which means that it has a high potential for abuse and dependence. It is typically administered orally or intravenously and can cause side effects such as dizziness, nausea, vomiting, constipation, and respiratory depression. Cyclazocine is not commonly used in the medical field due to its potential for abuse and the availability of other safer and more effective pain medications.
Morphine is a powerful opioid medication that is used to relieve severe pain. It is derived from the opium poppy and is one of the most potent naturally occurring opioids. Morphine works by binding to specific receptors in the brain and spinal cord, which can reduce the perception of pain and produce feelings of euphoria. It is often prescribed for patients who are experiencing severe pain, such as those with cancer or after surgery. Morphine can be administered in a variety of ways, including orally, intravenously, or through injection. It can also be used in combination with other medications to enhance its pain-relieving effects. However, morphine can also be highly addictive and can lead to dependence and withdrawal symptoms if used for an extended period of time. It is important for patients to use morphine only as directed by their healthcare provider and to avoid taking more than the recommended dose.
Meperidine is a synthetic opioid medication that is used to relieve moderate to severe pain. It is also known by the brand name Demerol. Meperidine works by binding to opioid receptors in the brain and spinal cord, which can result in a decrease in pain perception and an increase in feelings of relaxation and sedation. Meperidine is available in both oral and injectable forms and is typically prescribed for short-term use only, as it can be habit-forming and can lead to dependence if used for an extended period of time. It is also important to note that meperidine can have a number of side effects, including nausea, vomiting, dizziness, constipation, and respiratory depression. In recent years, the use of meperidine has declined due to concerns about its potential for abuse and addiction, as well as its potential for causing serious side effects. As a result, many healthcare providers are now using alternative pain management options, such as non-opioid medications or non-pharmacological treatments like physical therapy or acupuncture.
In the medical field, "Analgesics, Opioid" refers to a class of drugs that are used to relieve pain. Opioids are a subclass of analgesics that are derived from the opium poppy or synthesized in the laboratory. Opioids work by binding to specific receptors in the brain and spinal cord, which can reduce the perception of pain and produce feelings of euphoria. They are commonly used to treat moderate to severe pain, such as that caused by surgery, injury, or chronic conditions like cancer. However, opioids can also be addictive and can cause side effects such as drowsiness, nausea, constipation, and respiratory depression. As a result, they are typically prescribed only for short-term use and under close medical supervision.
Morphinans are a class of drugs that are derived from the opium poppy and are used to relieve pain. They work by binding to specific receptors in the brain and spinal cord, known as mu-opioid receptors, which are involved in the body's response to pain. Morphinans are used to treat a wide range of painful conditions, including acute pain, chronic pain, and cancer pain. They are available in various forms, including tablets, capsules, injections, and transdermal patches. However, they can also be addictive and can cause side effects such as nausea, vomiting, constipation, dizziness, and respiratory depression.
Opium is a natural substance derived from the opium poppy plant (Papaver somniferum). It contains a variety of alkaloids, including morphine, codeine, and thebaine, which have potent analgesic, sedative, and euphoric effects. In the medical field, opium and its derivatives are used as pain relievers, cough suppressants, and to treat diarrhea. Morphine, one of the most potent alkaloids in opium, is often used to treat severe pain, such as that caused by cancer or after surgery. Codeine, a milder analgesic, is often used for mild to moderate pain and as a cough suppressant. However, opium and its derivatives can also be highly addictive and can cause dependence, tolerance, and withdrawal symptoms when stopped abruptly. As a result, their use is closely regulated and monitored by medical professionals to minimize the risk of abuse and addiction.
Alphaprodine is a synthetic opioid analgesic that is similar in structure to meperidine (Demerol) and is used to relieve moderate to severe pain. It is a Schedule III controlled substance in the United States, meaning it has a moderate to low potential for abuse and dependence. Alphaprodine is available only by prescription and is typically used for short-term pain relief. It is not recommended for use in patients with respiratory depression, severe liver or kidney disease, or a history of addiction to opioids.
Hormone antagonists are medications that block or inhibit the effects of hormones in the body. They are often used in medical treatments to counteract the effects of hormones that are either overactive or underactive. Examples of hormone antagonists include: 1. Selective estrogen receptor modulators (SERMs): These medications block the effects of estrogen in some tissues but not others. They are used to treat conditions such as breast cancer and osteoporosis. 2. Progestins: These medications mimic the effects of the hormone progesterone and are used to treat conditions such as menopause symptoms and endometriosis. 3. Androgens: These medications block the effects of testosterone and are used to treat conditions such as prostate cancer and hirsutism (excessive hair growth in women). 4. Gonadotropin-releasing hormone (GnRH) antagonists: These medications block the release of gonadotropins, hormones that stimulate the ovaries and testes to produce sex hormones. They are used to treat conditions such as endometriosis and prostate cancer. Overall, hormone antagonists are an important tool in the medical field for treating a variety of conditions related to hormonal imbalances.
Dextropropoxyphene is a centrally acting analgesic medication that is used to relieve moderate to severe pain. It is a synthetic opioid that is similar in structure to codeine and is available in both immediate-release and extended-release formulations. Dextropropoxyphene is often used to treat conditions such as headaches, back pain, and osteoarthritis. It is available both alone and in combination with other medications, such as acetaminophen (paracetamol) or aspirin. However, dextropropoxyphene has been associated with serious side effects, including respiratory depression, addiction, and liver damage, and its use has been restricted or banned in some countries.
In the medical field, analgesics are drugs that are used to relieve pain without causing loss of consciousness. They are commonly used to treat a wide range of conditions, including headaches, toothaches, menstrual cramps, and injuries. There are several types of analgesics, including nonsteroidal anti-inflammatory drugs (NSAIDs), opioids, and local anesthetics. NSAIDs, such as aspirin and ibuprofen, work by reducing inflammation and blocking the production of prostaglandins, which are chemicals that cause pain and inflammation. Opioids, such as morphine and oxycodone, work by binding to receptors in the brain and spinal cord, which reduces the perception of pain. Local anesthetics, such as lidocaine, work by numbing a specific area of the body. It is important to note that while analgesics can be effective in relieving pain, they can also have side effects and may not be appropriate for everyone. It is always best to consult with a healthcare provider before taking any medication.
Opioid-related disorders refer to a group of conditions that result from the use of opioids, which are a class of drugs that include heroin, prescription painkillers, and synthetic opioids like fentanyl. These disorders can range from mild to severe and can have a significant impact on a person's physical and mental health, as well as their social and occupational functioning. The three main types of opioid-related disorders are: 1. Opioid Use Disorder (OUD): This is a chronic condition characterized by a compulsive pattern of opioid use despite negative consequences. Symptoms of OUD can include cravings, withdrawal symptoms, and continued use despite physical or psychological problems. 2. Opioid Dependence: This is a more severe form of OUD that involves a physical dependence on opioids. Symptoms of opioid dependence can include withdrawal symptoms when the drug is stopped, tolerance to the drug, and a strong desire to continue using opioids. 3. Opioid Addiction: This is a chronic, relapsing brain disorder characterized by compulsive drug seeking and use, despite negative consequences. Addiction is considered a disease of the brain and can be difficult to treat. Other opioid-related disorders include overdose, which can be fatal, and co-occurring disorders such as depression, anxiety, and post-traumatic stress disorder (PTSD). Treatment for opioid-related disorders typically involves a combination of medication, behavioral therapy, and support from healthcare professionals and loved ones.
Fentanyl is a synthetic opioid pain medication that is approximately 100 times more potent than morphine. It is used to treat severe pain, such as that caused by cancer or after surgery. Fentanyl is available in a variety of forms, including tablets, lozenges, patches, and injections. It is also sometimes used in combination with other medications, such as hydromorphone or oxycodone, to increase their effectiveness. Fentanyl can be highly addictive and can cause respiratory depression, which can be life-threatening. It is important to use fentanyl only under the guidance of a healthcare professional and to follow their instructions carefully.
Methadone is a synthetic opioid medication that is used to treat opioid addiction and withdrawal symptoms. It is a long-acting opioid that works by binding to the same receptors in the brain as other opioids, such as heroin and morphine, but with a longer duration of action. Methadone is typically administered orally, either as a liquid or a tablet, and is usually taken once or twice a day. Methadone is often used as part of a comprehensive treatment program for opioid addiction, which may also include counseling, behavioral therapy, and other medications. It can help to reduce cravings for opioids, prevent withdrawal symptoms, and reduce the risk of relapse. However, methadone can also be addictive and can cause side effects, such as drowsiness, nausea, and respiratory depression. It is important for individuals taking methadone to be monitored closely by a healthcare provider to ensure safe and effective use.
Oxymorphone is a synthetic opioid pain medication that is used to treat moderate to severe pain. It is a semi-synthetic derivative of the naturally occurring opioid alkaloid morphine. Oxymorphone is available in both immediate-release and extended-release forms, and it is typically administered orally. Oxymorphone works by binding to opioid receptors in the brain and spinal cord, which can result in a decrease in pain perception and an increase in feelings of relaxation and euphoria. It is a Schedule II controlled substance in the United States, which means that it has a high potential for abuse and addiction. Oxymorphone is commonly used to treat chronic pain conditions such as cancer pain, post-operative pain, and pain associated with fibromyalgia. It can also be used to manage acute pain, such as pain from injuries or surgeries. Like other opioids, oxymorphone can cause side effects such as dizziness, nausea, constipation, and respiratory depression. It can also be habit-forming and lead to dependence and addiction if not used as directed. Therefore, it is important to use oxymorphone only under the guidance of a healthcare professional and to follow the prescribed dosage and duration of use.
Interleukin 1 Receptor Antagonist Protein (IL-1Ra) is a protein that acts as an antagonist to the Interleukin 1 (IL-1) cytokine family. IL-1 is a group of signaling molecules that play a crucial role in the immune response and inflammation. IL-1Ra binds to the IL-1 receptor and prevents IL-1 from binding to its receptor, thereby inhibiting its pro-inflammatory effects. IL-1Ra is produced by various cells in the body, including monocytes, macrophages, and fibroblasts, and is released in response to inflammation or injury. It is also found in high concentrations in synovial fluid, which is the fluid that lubricates the joints. IL-1Ra has been shown to have anti-inflammatory and immunosuppressive effects, and it has been used in clinical trials to treat various inflammatory and autoimmune diseases, such as rheumatoid arthritis, psoriasis, and inflammatory bowel disease. It is also being studied as a potential treatment for COVID-19, as it may help to reduce inflammation and prevent severe illness.
Heroin is a highly addictive opioid drug that is derived from morphine, a natural substance found in the opium poppy plant. It is typically used for its euphoric and pain-relieving effects, but it can also cause respiratory depression, nausea, vomiting, and other serious side effects. Heroin is a Schedule I controlled substance under the United States Controlled Substances Act, meaning it is considered to have a high potential for abuse and no accepted medical use. It is illegal to manufacture, distribute, or possess heroin without a valid prescription.
Codeine is a semi-synthetic opioid medication that is used to relieve moderate to severe pain. It is a Schedule II controlled substance in the United States, meaning that it has a high potential for abuse and addiction. Codeine is often combined with other medications, such as acetaminophen (Tylenol) or aspirin, to increase its effectiveness and reduce side effects. It is also sometimes used as a cough suppressant. Codeine is available in both prescription and over-the-counter forms, but its use is generally restricted to adults and children over the age of 12.
Pain, Postoperative refers to the discomfort or pain experienced by a patient after undergoing surgery. It is a common and expected complication of surgery, and can range from mild to severe. Postoperative pain can be caused by a variety of factors, including tissue damage, inflammation, and nerve stimulation. It is typically managed with a combination of pain medications, such as opioids, nonsteroidal anti-inflammatory drugs (NSAIDs), and local anesthetics, as well as other treatments such as physical therapy, ice packs, and relaxation techniques. Proper management of postoperative pain is important for promoting healing, reducing the risk of complications, and improving the patient's overall comfort and quality of life.
Piperidines are a class of organic compounds that contain a six-membered ring with nitrogen atoms at positions 1 and 4. They are commonly used in the pharmaceutical industry as a building block for the synthesis of a wide range of drugs, including analgesics, anti-inflammatory agents, and antihistamines. Piperidines are also found in natural products, such as alkaloids, and have been used in traditional medicine for their various therapeutic effects. In the medical field, piperidines are often used as a starting point for the development of new drugs, as they can be easily modified to produce a wide range of pharmacological activities.
Adenosine A2 receptor antagonists are a class of drugs that block the action of adenosine A2 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including blood flow, heart rate, and inflammation. The A2 receptors are a subfamily of adenosine receptors that are found in many different tissues throughout the body. Adenosine A2 receptor antagonists are used to treat a variety of conditions, including hypertension (high blood pressure), heart failure, and asthma. They work by blocking the action of adenosine on the A2 receptors, which can help to relax blood vessels and reduce blood pressure. In heart failure, A2 receptor antagonists can help to improve heart function and reduce the workload on the heart. In asthma, they can help to reduce inflammation and bronchoconstriction (narrowing of the airways). Some examples of adenosine A2 receptor antagonists include cilostazol, pirenzepine, and ZM-241385. These drugs are typically administered orally or intravenously, and their side effects can include headache, nausea, and dizziness. It is important to note that the use of adenosine A2 receptor antagonists should be closely monitored by a healthcare provider, as they can interact with other medications and may have potential side effects.
Adrenergic alpha-1 receptor antagonists are a class of medications that block the action of alpha-1 adrenergic receptors in the body. These receptors are found in various tissues, including blood vessels, the heart, and the smooth muscle of the bronchial tubes. When activated by the hormone adrenaline (also known as epinephrine), alpha-1 receptors cause constriction of blood vessels, increased heart rate, and bronchoconstriction. Adrenergic alpha-1 receptor antagonists are used to treat a variety of conditions, including high blood pressure, heart disease, and certain types of anxiety disorders. They work by relaxing blood vessels, reducing blood pressure, and slowing the heart rate. They can also help to relieve symptoms of anxiety and panic attacks by reducing the physical symptoms of stress, such as rapid heart rate and sweating. Some examples of adrenergic alpha-1 receptor antagonists include prazosin (Minipress), doxazosin (Cardura), and terazosin (Hytrin). These medications are usually taken by mouth and are generally well-tolerated, although they can cause side effects such as dizziness, lightheadedness, and low blood pressure.
Naltrexone is a medication that is used to treat alcohol and opioid addiction. It works by blocking the effects of opioids and alcohol on the brain, which can help reduce cravings and prevent relapse. Naltrexone is available in both oral and injectable forms, and it is typically prescribed as part of a comprehensive treatment plan that may also include counseling and support. It is important to note that naltrexone is not effective for everyone, and it may not be suitable for people with certain medical conditions or who are taking certain medications. It is always important to discuss the potential risks and benefits of any medication with a healthcare provider before starting treatment.
In the medical field, a spasm is a sudden, involuntary contraction or tightening of a muscle or group of muscles. Spasms can occur in any part of the body and can be caused by a variety of factors, including injury, nerve damage, muscle fatigue, dehydration, electrolyte imbalances, and certain medications. Spasms can range in severity from mild twitches to severe, painful contractions that can interfere with normal movement and function. Some common examples of spasm include muscle cramps, Charcot-Marie-Tooth disease, and spasmodic dysphonia. Treatment for spasm depends on the underlying cause and can include medications, physical therapy, and lifestyle changes. In some cases, surgery may be necessary to address the underlying issue and prevent further spasms.
Hydrocodone is a prescription opioid medication used to treat moderate to severe pain. It is a synthetic opioid that is similar to codeine but is stronger and more potent. Hydrocodone is often combined with acetaminophen (as in the medication Vicodin) to increase its effectiveness and reduce the risk of side effects. Hydrocodone works by binding to opioid receptors in the brain and spinal cord, which can help to reduce pain and produce feelings of euphoria. It can also cause drowsiness, constipation, and nausea. Hydrocodone is typically prescribed for short-term use only, as it can be habit-forming and lead to dependence if used for an extended period of time. It is also important to note that hydrocodone can interact with other medications and can be dangerous if taken in large amounts or with alcohol or other substances.
In the medical field, pain is defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. Pain is a complex phenomenon that involves both physical and emotional components, and it can be caused by a variety of factors, including injury, illness, inflammation, and nerve damage. Pain can be acute or chronic, and it can be localized to a specific area of the body or can affect the entire body. Acute pain is typically short-lived and is a normal response to injury or illness. Chronic pain, on the other hand, persists for more than three months and can be caused by a variety of factors, including nerve damage, inflammation, and psychological factors. In the medical field, pain is typically assessed using a pain scale, such as the Visual Analog Scale (VAS), which measures pain intensity on a scale of 0 to 10. Treatment for pain depends on the underlying cause and can include medications, physical therapy, and other interventions.
Inert gas narcosis is a condition that occurs when a person is exposed to high concentrations of inert gases, such as nitrogen or helium, for an extended period of time. These gases can accumulate in the bloodstream and the body's tissues, leading to a variety of symptoms, including dizziness, confusion, disorientation, and loss of consciousness. Inert gas narcosis is most commonly associated with diving, as it can occur when a person breathes compressed air that contains high levels of nitrogen. The condition can also occur in people who work in enclosed spaces that are filled with inert gases, such as in the aerospace industry. Inert gas narcosis is a serious medical condition that can be life-threatening if not treated promptly. Treatment typically involves removing the person from the source of the inert gas and providing supportive care to manage the symptoms. In some cases, hyperbaric oxygen therapy may be used to help the body eliminate the excess inert gases from the bloodstream.
Substance-related disorders are a group of mental health conditions that are caused by the use of drugs or alcohol. These disorders can range from mild to severe and can have a significant impact on a person's life. Substance-related disorders are diagnosed when a person's use of drugs or alcohol causes problems in their daily life, such as problems at work or school, problems with relationships, or legal problems. Substance-related disorders can also lead to physical health problems, such as liver damage or heart disease. Treatment for substance-related disorders typically involves a combination of behavioral therapy and medication.
Receptors, Opioid are specialized proteins found on the surface of cells in the body that bind to opioid drugs, such as morphine, heroin, and oxycodone. These receptors are part of the body's natural pain-relieving system and are involved in regulating pain, mood, and reward. When opioid drugs bind to these receptors, they can produce a range of effects, including pain relief, sedation, and euphoria. However, long-term use of opioid drugs can lead to dependence and addiction, as the body becomes accustomed to the presence of the drug and requires more of it to achieve the same effect.
Dibenzocycloheptenes are a class of organic compounds that contain two benzene rings fused to a cycloheptane ring. They are commonly found in natural products and have been studied for their potential medicinal properties. Some dibenzocycloheptenes have been shown to have anti-inflammatory, anti-cancer, and anti-viral effects. They are also being investigated as potential treatments for a variety of diseases, including Alzheimer's disease, Parkinson's disease, and cancer.
Alcoholics Anonymous (AA) is a mutual support group for individuals struggling with alcohol addiction. It was founded in 1935 and is based on the belief that recovery from alcoholism is possible through a spiritual program that includes admitting powerlessness over alcohol, seeking help from a higher power, making amends for past wrongs, and working with others in recovery. In the medical field, AA is often recommended as a complementary treatment for individuals with alcohol use disorder (AUD) who are also receiving medical or psychological treatment. AA meetings can provide a supportive environment for individuals to share their experiences, receive encouragement, and learn from others who have successfully overcome addiction. While AA is not a substitute for medical treatment, it can be an important part of a comprehensive treatment plan for individuals with AUD. Some studies have shown that participation in AA can improve outcomes for individuals with AUD, including reduced drinking, improved quality of life, and increased social support.
Adenosine A1 receptor antagonists are a class of drugs that block the action of adenosine A1 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including heart rate, blood pressure, and sleep. Adenosine A1 receptors are found in many different tissues throughout the body, including the brain, heart, and lungs. Adenosine A1 receptor antagonists are used to treat a variety of conditions, including Parkinson's disease, schizophrenia, and overactive bladder. They work by blocking the action of adenosine at A1 receptors, which can help to improve symptoms and reduce the risk of side effects associated with other treatments. Some examples of adenosine A1 receptor antagonists include caffeine, theophylline, and modafinil.
Oxycodone is a prescription opioid medication used to treat moderate to severe pain. It is a semi-synthetic opioid derived from the opium poppy and is similar in structure to other opioids such as morphine and heroin. Oxycodone works by binding to opioid receptors in the brain and spinal cord, which can result in pain relief, sedation, and euphoria. Oxycodone is available in various forms, including tablets, capsules, and extended-release tablets, and is typically prescribed for short-term use only. It can be habit-forming and can lead to dependence and addiction if used improperly or for an extended period of time. Oxycodone is also a controlled substance and is regulated by the Drug Enforcement Administration (DEA) in the United States.
Leukotriene antagonists are a class of medications that block the action of leukotrienes, which are chemical messengers produced by the immune system. These drugs are used to treat a variety of conditions, including asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis (hay fever). Leukotrienes play a role in the inflammatory response and can cause constriction of the airways, leading to difficulty breathing. By blocking the action of leukotrienes, leukotriene antagonists can help to relax the airways and improve breathing in people with asthma or COPD. There are several different types of leukotriene antagonists available, including montelukast (Singulair) and zafirlukast (Accolate). These drugs are usually taken by mouth and are generally well-tolerated. However, like all medications, they can cause side effects, such as headache, nausea, and dizziness. It is important to talk to a healthcare provider about the potential benefits and risks of leukotriene antagonists before starting treatment.
Angiotensin receptor antagonists (ARAs) are a class of medications used in the medical field to treat high blood pressure (hypertension) and heart failure. These drugs work by blocking the action of angiotensin II, a hormone that narrows blood vessels and increases blood pressure. By blocking this hormone, ARAs help to relax blood vessels and lower blood pressure, which can reduce the risk of heart attack, stroke, and other complications associated with hypertension and heart failure. ARAs are available in both oral and injectable forms and are often used in combination with other blood pressure-lowering medications.
Receptors, Opioid, mu (OPRM1) are a type of protein found on the surface of nerve cells in the brain and throughout the body. These receptors are activated by opioid drugs, such as morphine, heroin, and oxycodone, as well as endogenous opioid peptides, such as endorphins and enkephalins. The mu-opioid receptors play a key role in the body's response to pain, as well as in regulating mood, reward, and stress. They are also involved in the development of addiction to opioid drugs. Mutations in the OPRM1 gene can affect the function of mu-opioid receptors and may be associated with altered responses to opioid drugs and an increased risk of addiction.
Morphine dependence is a condition in which a person becomes physically and/or psychologically dependent on the opioid pain medication morphine. This means that the person requires increasing amounts of the drug to achieve the same level of pain relief, and may experience withdrawal symptoms when the drug is stopped or reduced. Symptoms of morphine withdrawal can include nausea, vomiting, diarrhea, muscle aches, and anxiety. Treatment for morphine dependence typically involves a combination of medication-assisted therapy and behavioral therapy to help the person manage their withdrawal symptoms and learn new coping strategies to avoid relapse.
In the medical field, analgesia refers to the relief of pain without loss of consciousness. It is a common medical intervention used to manage pain caused by various conditions, such as surgery, injury, illness, or chronic conditions. There are different types of analgesia, including: 1. Local analgesia: This type of analgesia involves the use of numbing agents to block pain signals in a specific area of the body, such as during a dental procedure or surgery. 2. Systemic analgesia: This type of analgesia involves the use of medications that are absorbed into the bloodstream and affect the entire body to relieve pain. Examples include opioids, nonsteroidal anti-inflammatory drugs (NSAIDs), and acetaminophen. 3. Neuromodulation: This type of analgesia involves the use of electrical or magnetic stimulation to alter the way the nervous system processes pain signals. Analgesia is an important part of pain management and can help improve a patient's quality of life by reducing pain and discomfort. However, it is important to use analgesia appropriately and with caution, as it can also have side effects and risks, such as addiction, respiratory depression, and constipation.
Anesthesia is a medical procedure that involves the use of drugs or other techniques to induce a state of unconsciousness or a loss of sensation or awareness during a surgical, diagnostic, or therapeutic procedure. The goal of anesthesia is to provide pain relief and to allow medical professionals to perform procedures without the patient experiencing discomfort or distress. There are several types of anesthesia, including general anesthesia, regional anesthesia, and local anesthesia. General anesthesia involves the use of drugs to induce a state of unconsciousness and to relax all the muscles in the body. Regional anesthesia involves the use of drugs to numb a specific area of the body, such as the lower half of the body for a Cesarean section or the arm for a shoulder replacement surgery. Local anesthesia involves the use of drugs to numb a small area of the body, such as the skin for a minor procedure like a vaccination or a biopsy. Anesthesia is typically administered by an anesthesiologist, who is a medical doctor specializing in the field of anesthesia. The anesthesiologist works closely with the surgeon or other medical professionals to ensure that the patient receives the appropriate level of anesthesia for the procedure being performed.
Isonipecotic acids are a group of organic compounds that are found in the urine of individuals who have consumed opium or other opiate drugs. They are also produced by the body as a result of the metabolism of certain amino acids, such as leucine and isoleucine. In the medical field, isonipecotic acids are used as a diagnostic tool to detect the use of opiate drugs. They can be detected in urine samples using a variety of analytical techniques, such as gas chromatography-mass spectrometry (GC-MS) or high-performance liquid chromatography (HPLC). Isonipecotic acids are also being studied for their potential therapeutic uses. Some research has suggested that they may have anti-inflammatory and analgesic properties, and they are being investigated as potential treatments for a variety of conditions, including pain, inflammation, and neurodegenerative diseases. However, more research is needed to fully understand the potential therapeutic effects of isonipecotic acids and to determine their safety and efficacy in humans.
Substance Withdrawal Syndrome is a group of physical and psychological symptoms that occur when a person stops using a substance that they have been dependent on. These symptoms can be severe and can cause significant distress and discomfort. Substance withdrawal syndrome can occur when a person stops using alcohol, opioids, benzodiazepines, stimulants, or other addictive substances. The symptoms of substance withdrawal syndrome can vary depending on the substance that was being used and the length and severity of the addiction. Treatment for substance withdrawal syndrome typically involves medical supervision and the use of medications to manage the symptoms and prevent complications.
Heroin Toxicity Medication: Narcotic antagonists, GI decontaminants
Heroin Toxicity Medication: Narcotic antagonists, GI decontaminants
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DeCS 2013 - December 17, 2013 version
- REVEX (nalmefene hydrochloride injection), an opioid antagonist, is a 6-methylene analogue of naltrexone. (nih.gov)
- Diphenoxylate is an antidiarrheal agent chemically related to the narcotic analgesic meperidine. (medscape.com)
- It also detects synthetic opiates related to morphine, such as hydromorphone, and high concentrations of the analgesic meperidine and the narcotic antagonist nalorphine. (smalaboratory.com)
- Evaluations and recommendations are presented for 14 substances in the categories of sedative-hypnotics, opioid agonist-antagonist analgesics, and stimulants. (who.int)
- 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)
- In some cases, there is a general belief that sexual desire is higher in those who use stimulants or narcotics. (brieflands.com)
- used to reverse overdose of narcotics, if patient abuses opoids this drug may cause withdraw, nausea, vomiting, increased BP etc. (freezingblue.com)
- 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)
- 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)
- In addition to analgesia, narcotics may produce drowsiness, changes in mood and mental clouding. (drugcite.com)
- 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)
- Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. (ncats.io)
- In addition, narcotic antagonists - drugs used to treat drug addictions - may be effective in treating compulsive gambling in some people. (theblackoutargument.com)
- H2-receptor antagonists are considered the drugs of choice for children because pediatric doses are well established and the medications are available in liquid form. (medscape.com)
- Two categories of drugs that are usually abused in this regard are amphetamines and narcotics. (brieflands.com)
- Ondansetron belongs to a class of drugs called serotonin antagonists. (medicalnewstoday.com)
- 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)
- This comparative study was performed on 91 men (49 amphetamine and 42 narcotics abusers) from the patients of Yareegar Clinic in Tehran, Iran, within 2019 - 2021. (brieflands.com)
- On their own, antagonists produce no effect by themselves to a receptor, and are said to have neither intrinsic activity nor efficacy. (bvsalud.org)
- The respiratory depressant effects of narcotics and their capacity to elevate cerebrospinal fluid pressure may be markedly exaggerated in the presence of head injury, other intracranial lesions or a preexisting increase in intracranial pressure. (drugcite.com)
- Lotfi Kashani F, Vaziri S, Vaziri A. Effects of Methamphetamine and Narcotics on Sexual High-Risk Behaviors. (brieflands.com)
- Hydrocodone is a semisynthetic narcotic analgesic and antitussive with multiple actions qualitatively similar to those of codeine. (drugcite.com)