Levorphanol
Morphinans
Receptors, Opioid, mu
Morphine
Nalorphine
Receptors, Opioid
Receptors, Opioid, delta
Enkephalin, Leucine-2-Alanine
Narcotics
Enkephalin, Leucine
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
Naloxone
Enkephalins
Enkephalin, D-Penicillamine (2,5)-
Analgesics, Opioid
Receptors, Opioid, kappa
Naltrexone
Sodium Bicarbonate
Fentanyl
Buprenorphine
Cinnamates
Thebaine
Papaver
Diprenorphine
Opium
Encyclopedias as Topic
Drug and Narcotic Control
United States Department of Agriculture
North Carolina
Research Subjects
Methyltestosterone
Nonselective coupling of the human mu-opioid receptor to multiple inhibitory G-protein isoforms. (1/106)
The human mu-opioid receptor was expressed in Saccharomyces cerevisiae. Binding of [3H]diprenorphine to yeast spheroplasts was specific and saturable (Kd = 1 nm, Bmax = 0.2-1 pmol x mg-1 of membrane proteins). Inhibition of [3H]diprenorphine binding by antagonists and agonists with varying opioid selectivities (mu, delta and kappa) occurred with the same order of potency as in mammalian tissues. Affinities of antagonists were the same with yeast spheroplasts as in reference tissues whereas those of agonists, except etorphine and buprenorphine, were 10-fold to 100-fold lower. Addition of heterotrimeric Gi,o-proteins purified from bovine brain shifted the mu-opioid receptor into a high-affinity state for agonists. Using individually purified Galpha-subunits re-associated with betagamma-dimers, we showed that alphao1, alphao2, alphai1, alphai2 and alphai3 reconstituted high-affinity agonist binding with equal efficiency. This suggests that the structural determinants of the mu-opioid receptor responsible for G-protein coupling are not able to confer a high degree of specificity towards any member of the Gi,o family. The selective effects of opioid observed in specialized tissues upon opioid stimulation may be a result of regulation of G-protein activity by cell-specific factors which should conveniently be analysed using the reconstitution assay described here. (+info)Human mu-opioid receptor overexpressed in baculovirus system and its pharmacological characterizations. (2/106)
AIM: To overexpress human mu-opioid receptor (muOR) with characteristics similar to those of mammalian origin. METHODS: Human muOR with a tag of 6 consecutive histidines at its carboxyl terminus was expressed in recombinant baculovirus infected Sf9 insect cells. Then the pharmacological characterizations of the product were studied by receptor binding assay and cAMP assay. RESULTS: The maximal binding capacity for the [3H]diprenorphine and [3H]ohmefentanyl (Ohm) were 9.1 +/- 0.7 and 6.52 +/- 0.23 nmol/g protein, respectively. The [3H]diprenorphine or [3H] Ohm binding to the receptor expressed in Sf9 cells was strongly inhibited by alpha-selective agonists [D-Ala2, N-methyl-Phe4, glyol5] enkephalin (DAGO), Ohm, and morphine, but neither by the delta-selective agonist [D-Pen2, D-Pen5] enkephalin (DPDPE) nor by the kappa-selective agonist inverted question marktrans-(+/-)-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexyl] inverted question mark benzacetamide (U50488). NaCl 100 mmol.L-1 and guanosine triphosphate (GTP) 50 mumol.L-1 could reduce mu agonists Ohm and etorphine affinity binding to the expressed muOR. DAGO and Ohm effectively inhibited forskolin-stimulated cAMP accumulation. This agonist-dependent effect was blocked by opioid antagonist naloxone. CONCLUSION: The overexpression of human muOR with a tag of six consecutive histidines at its carboxyl terminus in Sf9 insect cells retained the characteristics of wild-type human muOR. (+info)Immunosuppressive effects of intravenous self administration of dihydroetorphine on lymphocyte functions in rats. (3/106)
AIM: To study the effects of dihydroetorphine (DHE) on lymphocyte functions in rats and to further assess the abuse potential of DHE. METHODS: An intravenous self administration (SA) procedure in rats was used to determine the SA liability of DHE. Concanavalin A (Con A)-stimulated lymphocyte proliferation and lymphokine production of rat splenocytes were measured. RESULTS: DHE 178 +/- 13 micrograms established a stable and typical rat model of psychological dependence, suppressed lymphocyte proliferation (129 +/- 11 Bq) compared with control group (620 +/- 36 Bq), and inhibited the activity of interleukin-2 (IL-2) (A570 = 0.28 +/- 0.06) compared with control group (A570 = 0.51 +/- 0.03). CONCLUSION: DHE had a high abuse potential and inhibited the Con A-induced lymphocyte proliferation and interleukin-2 production in rats. (+info)Differential G-protein activation by alkaloid and peptide opioid agonists in the human neuroblastoma cell line SK-N-BE. (4/106)
Differences in the specificity of coupling of delta-opioid receptor with G-protein have been reported in the literature. We have observed a differential desensitization of delta-opioid receptors, endogenously expressed in the neuroblastoma cell line SK-N-BE, induced by peptide and alkaloid agonists. By combining photoaffinity labelling of receptor-activated G-proteins with [alpha-(32)P]azidoanilide-GTP and an anti-sense oligodeoxynucleotide strategy, we examined whether the chemical nature of opioid agonists, alkaloid or peptide, has a critical role in determining a G(i)alpha/G(o)alpha-protein-selective activation by the human delta-opioid receptors. Etorphine, a non-selective alkaloid agonist, was shown to stimulate the incorporation of [alpha-(32)P]azidoanilide-GTP into G(i)alpha1, G(i)alpha2, G(i)alpha3 and pertussis-toxin-insensitive Galpha subunits. In contrast, [d-Pen(2),d-Pen(5)]enkephalin (DPDPE; Pen is penicillamine) and Tyr-d-Ala-Phe-Asp-Val-Val-Gly-NH(2) (deltorphin I), selective peptide agonists, mainly activated G(i)alpha2 and G(o)alpha2 subunits. The 'knock-down' of G(o)alpha2 subunits by anti-sense oligodeoxynucleotides selectively decreased the inhibition of adenylate cyclase induced by DPDPE and deltorphin I, whereas anti-sense oligodeoxynucleotides directed against G(i)alpha2 subunits only decreased the potency of etorphine in inhibiting cAMP accumulation. These results suggest that the nature of the agonist, peptide or alkaloid is critical in determining the interaction between human delta-opioid receptors and Galpha subunits. (+info)Dihydroetorphine-induced place preference was mediated by dopamine D1 receptors in rats. (5/106)
AIM: To study the influence of dopamine (DA) receptor antagonists upon the rewarding property of dihydroetorphine (DHE). METHODS: Conditioned place preference (CPP) paradigm was used to characterize the rewarding effect of DHE. DA receptor antagonists were injected administered subcutaneously or peritoneally and microinjected into nucleus accumbens (NAcc). RESULTS: DHE (0.05, 0.5, and 5.0 micrograms.kg-1, s.c.) produced place preference (P < 0.01). Both the DA receptor antagonist haloperidol and the selective D1 receptor antagonist Sch-23390 attenuated the place preference produced by DHE (0.5 microgram.kg-1, s.c.). l-Sulpiride and spiperone, selective D2 receptor antagonists, had no such effects. CONCLUSION: The D1 (but not D2) receptors in NAcc are crucial in the mediation of the rewarding effect of DHE. (+info)Dissociation of functional roles of dynamin in receptor-mediated endocytosis and mitogenic signal transduction. (6/106)
Dynamin plays a critical role in the membrane fission mechanism that mediates regulated endocytosis of many G protein-coupled receptors. In addition, dynamin is required for ligand-induced activation of mitogen-activated protein kinase by certain receptors, raising a general question about the role of dynamin in mitogenic signal transduction. Here we report that endocytosis of mu and delta opioid receptors is not required for efficient ligand-induced activation of mitogen-activated protein kinase. Nevertheless, mitogenic signaling mediated by these receptors is specifically dynamin-dependent. Thus a functional role of dynamin in mitogenic signaling can be dissociated from its role in receptor-mediated endocytosis, suggesting a previously unidentified and distinct role of dynamin in signal transduction by certain G protein-coupled receptors. (+info)Functional dissociation of mu opioid receptor signaling and endocytosis: implications for the biology of opiate tolerance and addiction. (7/106)
Opiate analgesia, tolerance, and addiction are mediated by drug-induced activation of the mu opioid receptor. A fundamental question in addiction biology is why exogenous opiate drugs have a high liability for inducing tolerance and addiction while native ligands do not. Studies indicate that highly addictive opiate drugs such as morphine are deficient in their ability to induce the desensitization and endocytosis of receptors. Here, we demonstrate that this regulatory mechanism reveals an independent functional property of opiate drugs that can be distinguished from previously established agonist properties. Moreover, this property correlates with agonist propensity to promote physiological tolerance, suggesting a fundamental revision of our understanding of the role of receptor endocytosis in the biology of opiate drug action and addiction. (+info)A previously unidentified acepromazine metabolite in humans: implications for the measurement of acepromazine in blood. (8/106)
High-performance liquid chromatography-diode-array detection results obtained during the investigation of two cases involving acepromazine prompted us to study the stability of the drug in blood. It was found that acepromazine can undergo in vitro conversion by human red blood cells to 2-(1-hydroxyethyl)promazine, a product that has been reported as a minor urinary metabolite in horse urine but not previously identified in humans. Further, our analytical findings in the two cases examined suggest that 2-(1-hydroxyethyl)promazine may be the major unconjugated metabolite of acepromazine in humans. These findings have important implications for the analytical toxicology of acepromazine. (+info)Etorphine is a potent synthetic opioid analgesic drug that is primarily used for the immobilization and veterinary purposes in large animals. It is not commonly used in human medicine due to its high potency and potential for serious side effects, including respiratory depression and death. In medical context, etorphine is classified as a Schedule II controlled substance in the United States, due to its high abuse potential.
Etorphine works by binding to opioid receptors in the brain and spinal cord, which leads to pain relief, sedation, and decreased breathing rate. It is typically administered via injection and its effects can last for several hours. In veterinary medicine, etorphine may be used to immobilize animals such as elephants, rhinos, and large deer species for medical procedures or relocation.
It's important to note that due to its high potency and potential for serious side effects, etorphine should only be administered by trained professionals in a controlled setting.
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.
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.
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 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.
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.
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).
Opioid delta receptors, also known as delta opioid receptors (DORs), are a type of G protein-coupled receptor found in the nervous system and other tissues throughout the body. They belong to the opioid receptor family, which includes mu, delta, and kappa receptors. These receptors play an essential role in pain modulation, reward processing, and addictive behaviors.
Delta opioid receptors are activated by endogenous opioid peptides such as enkephalins and exogenous opioids like synthetic drugs. Once activated, they trigger a series of intracellular signaling events that can lead to inhibition of neuronal excitability, reduced neurotransmitter release, and ultimately, pain relief.
Delta opioid receptors have also been implicated in various physiological processes, including immune function, respiratory regulation, and gastrointestinal motility. However, their clinical use as therapeutic targets has been limited due to the development of tolerance and potential adverse effects such as sedation and respiratory depression.
In summary, delta opioid receptors are a type of opioid receptor that plays an essential role in pain modulation and other physiological processes. They are activated by endogenous and exogenous opioids and trigger intracellular signaling events leading to various effects, including pain relief. However, their clinical use as therapeutic targets is limited due to potential adverse effects.
Enkephalins are naturally occurring opioid peptides in the body that bind to opiate receptors and help reduce pain and produce a sense of well-being. There are several different types of enkephalins, including Leu-enkephalin and Met-enkephalin, which differ based on their amino acid sequence.
Leucine-enkephalin (Leu-Enk) is a specific type of enkephalin that contains the amino acids tyrosine, glycine, glutamic acid, leucine, and methionine in its sequence. The Leucine-2-Alanine variant of Leu-Enk refers to a synthetic form of this peptide where the leucine at position 2 is replaced with alanine. This modification can affect the stability, activity, and pharmacological properties of the enkephalin molecule.
It's important to note that while Leu-Enk and its analogs have potential therapeutic applications in pain management, they are also subject to abuse and addiction due to their opioid properties. Therefore, their use is tightly regulated and requires careful medical supervision.
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.
Enkephalins are naturally occurring opioid peptides in the body that bind to opiate receptors and help reduce pain and produce a sense of well-being. There are two major types of enkephalins: Met-enkephalin and Leu-enkephalin, which differ by only one amino acid at position 5 (Leucine or Methionine).
Leu-enkephalin, also known as YGGFL, is a type of enkephalin that contains the amino acids Tyrosine (Y), Glycine (G), Glycine (G), Phenylalanine (F), and Leucine (L) in its sequence. It is involved in pain regulation, mood, and other physiological processes.
Leu-enkephalin is synthesized from a larger precursor protein called proenkephalin and is stored in the secretory vesicles of neurons. When released into the synaptic cleft, Leu-enkephalin can bind to opioid receptors on neighboring cells, leading to various physiological responses.
Leu-enkephalin has a shorter half-life than Met-enkephalin due to its susceptibility to enzymatic degradation by peptidases. However, it still plays an essential role in modulating pain and other functions in the body.
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.
Enkephalins are naturally occurring opioid peptides that bind to opiate receptors in the brain and other organs, producing pain-relieving and other effects. They are derived from the precursor protein proenkephalin and consist of two main types: Leu-enkephalin and Met-enkephalin. Enkephalins play a role in pain modulation, stress response, mood regulation, and addictive behaviors. They are also involved in the body's reward system and have been implicated in various physiological processes such as respiration, gastrointestinal motility, and hormone release.
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.
Morphine derivatives are substances that are synthesized from or structurally similar to morphine, a natural opiate alkaloid found in the opium poppy. These compounds share many of the same pharmacological properties as morphine and are often used for their analgesic (pain-relieving), sedative, and anxiolytic (anxiety-reducing) effects.
Examples of morphine derivatives include:
1. Hydrocodone: A semi-synthetic opioid that is often combined with acetaminophen for the treatment of moderate to severe pain.
2. Oxycodone: A synthetic opioid that is used for the management of moderate to severe pain, either alone or in combination with other medications.
3. Hydromorphone: A potent semi-synthetic opioid that is used for the treatment of severe pain, typically in a hospital setting.
4. Oxymorphone: A synthetic opioid that is similar to hydromorphone in its potency and use for managing severe pain.
5. Codeine: A naturally occurring opiate alkaloid that is less potent than morphine but still has analgesic, cough suppressant, and antidiarrheal properties. It is often combined with other medications for various therapeutic purposes.
6. Fentanyl: A synthetic opioid that is significantly more potent than morphine and is used for the management of severe pain, typically in a hospital or clinical setting.
It's important to note that while these derivatives can be beneficial for managing pain and other symptoms, they also carry a risk of dependence, addiction, and potentially life-threatening side effects such as respiratory depression. As a result, their use should be closely monitored by healthcare professionals and prescribed cautiously.
Opioid receptors, also known as opiate receptors, are a type of G protein-coupled receptor found in the nervous system and other tissues. They are activated by endogenous opioid peptides, as well as exogenous opiates and opioids. There are several subtypes of opioid receptors, including mu, delta, and kappa.
Kappa opioid receptors (KORs) are a subtype of opioid receptor that are widely distributed throughout the body, including in the brain, spinal cord, and gastrointestinal tract. They are activated by endogenous opioid peptides such as dynorphins, as well as by synthetic and semi-synthetic opioids such as salvinorin A and U-69593.
KORs play a role in the modulation of pain, mood, and addictive behaviors. Activation of KORs has been shown to produce analgesic effects, but can also cause dysphoria, sedation, and hallucinations. KOR agonists have potential therapeutic uses for the treatment of pain, addiction, and other disorders, but their use is limited by their side effects.
It's important to note that opioid receptors and their ligands (drugs or endogenous substances that bind to them) are complex systems with many different actions and effects in the body. The specific effects of KOR activation depend on a variety of factors, including the location and density of the receptors, the presence of other receptors and signaling pathways, and the dose and duration of exposure to the ligand.
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.
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.
Sodium bicarbonate, also known as baking soda, is a chemical compound with the formula NaHCO3. It is a white solid that is crystalline but often appears as a fine powder. It has a slightly salty, alkaline taste and is commonly used in cooking as a leavening agent.
In a medical context, sodium bicarbonate is used as a medication to treat conditions caused by high levels of acid in the body, such as metabolic acidosis. It works by neutralizing the acid and turning it into a harmless salt and water. Sodium bicarbonate can be given intravenously or orally, depending on the severity of the condition being treated.
It is important to note that sodium bicarbonate should only be used under the supervision of a healthcare professional, as it can have serious side effects if not used properly. These may include fluid buildup in the body, electrolyte imbalances, and an increased risk of infection.
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.
Buprenorphine is a partial opioid agonist medication used to treat opioid use disorder. It has a lower risk of respiratory depression and other adverse effects compared to full opioid agonists like methadone, making it a safer option for some individuals. Buprenorphine works by binding to the same receptors in the brain as other opioids but with weaker effects, helping to reduce cravings and withdrawal symptoms. It is available in several forms, including tablets, films, and implants.
In addition to its use in treating opioid use disorder, buprenorphine may also be used to treat pain, although this use is less common due to the risk of addiction and dependence. When used for pain management, it is typically prescribed at lower doses than those used for opioid use disorder treatment.
It's important to note that while buprenorphine has a lower potential for abuse and overdose than full opioid agonists, it still carries some risks and should be taken under the close supervision of a healthcare provider.
Cinnamates are organic compounds that are derived from cinnamic acid. They contain a carbon ring with a double bond and a carboxylic acid group, making them aromatic acids. Cinnamates are widely used in the perfume industry due to their pleasant odor, and they also have various applications in the pharmaceutical and chemical industries.
In a medical context, cinnamates may be used as topical medications for the treatment of skin conditions such as fungal infections or inflammation. For example, cinnamate esters such as cinoxacin and ciclopirox are commonly used as antifungal agents in creams, lotions, and shampoos. These compounds work by disrupting the cell membranes of fungi, leading to their death.
Cinnamates may also have potential therapeutic benefits for other medical conditions. For instance, some studies suggest that cinnamate derivatives may have anti-inflammatory, antioxidant, and neuroprotective properties, making them promising candidates for the development of new drugs to treat diseases such as Alzheimer's and Parkinson's. However, more research is needed to confirm these effects and determine their safety and efficacy in humans.
Thebaine is a naturally occurring alkaloid found in the opium poppy (Papaver somniferum) and is defined medically as follows:
A benzylisoquinoline alkaloid, Thebaine is a potent opioid agonist with complex pharmacology. It acts as an antagonist at mu and delta receptors while exhibiting agonist activity at kappa receptors. Due to its strong physiological effects and potential for abuse, thebaine has limited therapeutic use. However, it serves as a crucial intermediate in the semi-synthesis of various opioid analgesics, such as oxycodone, hydrocodone, and nalbuphine.
Please note that this definition is intended for informational purposes only and should not be used as a substitute for professional medical advice, diagnosis, or treatment.
"Papaver" is the genus name for the poppy plant family, which includes several species of plants that are known for their showy flowers and often contain medicinal alkaloids. The most well-known member of this family is probably Papaver somniferum, also known as the opium poppy. This particular species contains a number of pharmacologically active compounds, including morphine, codeine, and papaverine, which have been used in various medical contexts for their analgesic, sedative, and vasodilatory effects. However, it's worth noting that the use of Papaver somniferum and its derivatives is tightly regulated due to their potential for abuse and addiction.
Diprenorphine is a potent opioid antagonist, which is used primarily in veterinary medicine as an antidote for overdoses of opioid drugs or accidents involving exposure to opioids in wildlife. It works by blocking the effects of opioids on the brain and reversing their potentially harmful or deadly symptoms, such as respiratory depression, sedation, and decreased heart rate.
Diprenorphine is a non-selective antagonist at mu, delta, and kappa opioid receptors, which means it can reverse the effects of all three types of opioid receptors in the body. It has a high affinity for these receptors, making it a very effective antidote for opioid overdoses.
In human medicine, diprenorphine is not commonly used due to its short duration of action and the availability of other longer-acting opioid antagonists such as naloxone. However, it may be used in some specialized medical settings, such as in the management of opioid toxicity during anesthesia or in cases where a longer-acting antagonist is not available.
It's important to note that diprenorphine should only be administered under the supervision of a trained medical professional, as improper use can lead to serious adverse effects or even death.
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.
An encyclopedia is a comprehensive reference work containing articles on various topics, usually arranged in alphabetical order. In the context of medicine, a medical encyclopedia is a collection of articles that provide information about a wide range of medical topics, including diseases and conditions, treatments, tests, procedures, and anatomy and physiology. Medical encyclopedias may be published in print or electronic formats and are often used as a starting point for researching medical topics. They can provide reliable and accurate information on medical subjects, making them useful resources for healthcare professionals, students, and patients alike. Some well-known examples of medical encyclopedias include the Merck Manual and the Stedman's Medical Dictionary.
An antidote is a substance that can counteract the effects of a poison or toxin. It works by neutralizing, reducing, or eliminating the harmful effects of the toxic substance. Antidotes can be administered in various forms such as medications, vaccines, or treatments. They are often used in emergency situations to save lives and prevent serious complications from poisoning.
The effectiveness of an antidote depends on several factors, including the type and amount of toxin involved, the timing of administration, and the individual's response to treatment. In some cases, multiple antidotes may be required to treat a single poisoning incident. It is important to note that not all poisons have specific antidotes, and in such cases, supportive care and symptomatic treatment may be necessary.
Examples of common antidotes include:
* Naloxone for opioid overdose
* Activated charcoal for certain types of poisoning
* Digoxin-specific antibodies for digoxin toxicity
* Fomepizole for methanol or ethylene glycol poisoning
* Dimercaprol for heavy metal poisoning.
"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.
The United States Department of Agriculture (USDA) is not a medical organization or entity, so it does not provide medical definitions. However, I can give you some information about what the USDA is and what it does.
The USDA is a federal executive department of the U.S. government responsible for developing and executing federal laws related to farming, forestry, and food. It was established in 1862 by President Abraham Lincoln and is headed by the Secretary of Agriculture, who is a member of the President's cabinet.
The USDA has several key missions, including:
* Promoting agricultural trade and production
* Ensuring the safety of the food supply
* Providing nutrition assistance to vulnerable populations
* Protecting natural resources and the environment
* Promoting rural development and economic stability
In terms of food and nutrition, the USDA plays an important role in setting dietary guidelines for Americans, establishing standards for school meals and other federal food programs, and regulating the safety of meat, poultry, and egg products. The agency also conducts research on agricultural and food-related topics and provides education and outreach to farmers, ranchers, and consumers.
I'm sorry for any confusion, but "North Carolina" is a geographical location and not a medical term or condition. It is a state located in the southeastern region of the United States. If you have any questions about medical terms or conditions, I'd be happy to help with those!
A research subject, also commonly referred to as a "human subject" or "participant," is an individual who takes part in a research study or clinical trial. Research subjects are essential for the advancement of medical and scientific knowledge, as they provide data that can help researchers understand various phenomena, develop new treatments, and improve existing ones.
The term "research subject" emphasizes the ethical considerations involved in conducting research with human participants. It highlights the importance of protecting their rights, dignity, and well-being throughout the study. Researchers must obtain informed consent from subjects before enrolling them in a study, ensuring that they understand the purpose, procedures, potential risks, and benefits associated with the research.
Additionally, researchers are required to follow strict guidelines and regulations to minimize any harm or discomfort to the research subjects during the study. These guidelines may include requirements for data confidentiality, privacy protection, and monitoring of adverse events. Overall, treating research subjects with respect and care is crucial in maintaining the integrity of medical research and ensuring its societal benefits.
'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.
Methyltestosterone is a synthetic form of the hormone testosterone, which is primarily used in the treatment of low testosterone levels (hypogonadism) in men. It has a methyl group attached to it, which allows it to be taken orally and still have significant effects on the body.
Testosterone is an androgen hormone that plays important roles in the development and maintenance of male sex characteristics, such as deepening of the voice, growth of facial and body hair, and increased muscle mass. It also helps maintain bone density, red blood cell production, and sex drive.
Methyltestosterone is available in various forms, including tablets and capsules, and its use should be under the supervision of a healthcare professional due to potential side effects and risks associated with its use, such as liver toxicity, increased risk of cardiovascular events, and changes in cholesterol levels.
It's important to note that methyltestosterone is not approved for use in women, as it can cause virilization (development of male sex characteristics) and other side effects.
I'm sorry for any confusion, but the 'United States Department of Homeland Security' (DHS) is not a medical term or concept. It's a cabinet department of the U.S. federal government, created in response to the September 11 attacks, with the primary responsibilities of protecting the United States from terrorism and managing border control. The DHS includes several components, including the U.S. Coast Guard, Transportation Security Administration (TSA), Federal Emergency Management Agency (FEMA), Customs and Border Protection (CBP), and Immigration and Customs Enforcement (ICE), among others.
If you have any medical questions or terms you would like defined, I'd be happy to help!
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Opioid9
- Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 10,000-30,000 times that of morphine. (wikipedia.org)
- Diprenorphine (Revivon) is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. (wikipedia.org)
- Etorphine is an extremely potent, non-selective full agonist of the μ-, δ-, and κ-opioid receptors. (wikipedia.org)
- Datas from 2022) 6,14-Endoethenotetrahydrooripavine - the central nucleus of all Bentley compound opioids under which class etorphine falls Dihydroetorphine - a close analog of etorphine that has been used as an opioid painkiller for human usage in China Thienorphine Opioid potency comparison Bentley KW, Hardy DG (June 1967). (wikipedia.org)
- Etorphine is an agonist at mu, delta, and kappa opioid receptors. (the-medical-dictionary.com)
- The drugs act at the opioid receptors, which all mammals have, and attach, but when you give the animals naltrexone it bumps the etorphine off the receptors and completely reverses the sedative effects. (fossilrim.org)
- 6 The most common chemical restraint protocols used to induce recumbency in okapi utilize either an opioid (etorphine, carfentanil) in combination with an α 2 -adrenergic agonist (xylazine, detomidine) or medetomidine-ketamine. (vin.com)
- It is a derivative of the more well-known opioid etorphine , which is used as a very potent veterinary painkiller and anesthetic medication, primarily for the sedation of large animals such as elephants, giraffes and rhinos. (wikidoc.org)
- This was despite the use of an opioid-based protocol with etorphine and azaperone, which are known to increase heart rate. (drejtesia.org)
Large Animal Revivon1
- An etorphine antidote Large Animal Revivon contains mainly diprenorphine for animals and a human-specific naloxone-based antidote, which should be prepared prior to the etorphine. (wikipedia.org)
Diprenorphine4
- The human antidote is generally naloxone, not diprenorphine, and is always prepared before the preparation of etorphine to be immediately administered following accidental human exposure to etorphine. (wikipedia.org)
- However, its high potency, combined with the rapid action of both etorphine and its antagonist, diprenorphine, means that it has found a place for use in the capture of large mammals such as rhinoceroses and elephants, where rapid onset and rapid recovery are both very important. (wikipedia.org)
- Investigators who request a Schedule I drug and/or Etorphine HCl or Diprenorphine must provide DEA documentation under which the requested drug is covered under their current DEA registration. (nih.gov)
- Yes, Practitioners authorized to possess carfentanil, etorphine hydrochloride and/or diprenorphine must store these in a GSA Approved Class 5 container, safe or cabinet. (narcoticssafes.com)
Carfentanil2
- 3) Chemical immobilization using narcotic combinations of carfentanil-xylazine, etorphine-xylazine, carfentanil-xylazine-ketamine, or etorphine-xylazine-ketamine delivered intramuscularly via dart to produce sternal recumbency. (vin.com)
- However despite showing some advantages over etorphine (for instance producing less toxic side effects in giraffes), acetorphine was never widely adopted for veterinary use, and etorphine (along with other tranquillizers such as carfentanil and azaperone ) remains the drug of choice in this application. (wikidoc.org)
Hydrochloride1
- In the US, etorphine is listed as a Schedule I drug with an ACSCN of 9056, although its hydrochloride salt is classified as Schedule II with an ACSCN of 9059. (wikipedia.org)
Immobilon2
- Large Animal Immobilon is a combination of etorphine plus acepromazine maleate. (wikipedia.org)
- Etorphine ( Immobilon ® or M99 ) is a synthetic cousin of morphine and 1000 - 80,000 times more powerful. (the-medical-dictionary.com)
Opioids1
- Haefele pointed out that 25 percent of the etorphine dose for a 600-pound zebra would sedate a 5,000-pound white rhino bull, as rhinos are very sensitive to opioids. (fossilrim.org)
Sedative1
- In the present study, etorphine and the sedative combination butorphanol-azaperone-medetomidine (BAM) were used. (drejtesia.org)
Azaperone2
- A combination of etorphine and azaperone provided a successful immobilisation and translocation for nine free-ranging Masai giraffes. (drejtesia.org)
- This indicates that the azaperone-etorphine combination used here, with its short recovery times and high quality of restraint, is a promising approach to reduce manipulation stress during translocations of free-ranging giraffes. (drejtesia.org)
Morphine1
- The drug we use - etorphine - is in the same class as morphine, but about 1,000 times stronger," Haefele said. (fossilrim.org)
Receptors1
- Conversely, β 2 receptors in these cells undergo etorphine-mediated endocytosis. (elsevierpure.com)
Potent1
- 2016). Our lab previously showed that while U50,488H promoted robust hKOPR phosphorylation and internalization, etorphine induced little phosphorylation and internalization, although both were potent full agonists in enhancing [35S]GTPγS (Li et al. (temple.edu)
Veterinary4
- Etorphine is available legally only for veterinary use and is strictly governed by law. (wikipedia.org)
- Veterinary-strength etorphine is fatal to humans. (wikipedia.org)
- The high incidence of side effects, including severe cardiopulmonary depression, has caused etorphine to fall into disfavor in general veterinary practice. (wikipedia.org)
- Acetorphine was developed for the same purpose as etorphine itself, namely as a strong tranquillizer for use in immobilizing large animals in veterinary medicine. (wikidoc.org)
Dart1
- The high potency of etorphine means that sufficient etorphine can be administered to large wild mammals by projectile syringe (dart). (wikipedia.org)
Substance1
- citation needed] In the UK, under the Misuse of Drugs Act 1971, etorphine is controlled as a Class A substance. (wikipedia.org)
Data1
- Neither enkephalin nor etorphine affects the growth rate of the cells (data not shown). (nih.gov)
Drug1
- In the Netherlands, etorphine is a Schedule I drug of the Opium Law. (wikipedia.org)
Group1
- Acetorphine was developed in 1966 by the Reckitt research group that developed etorphine. (wikidoc.org)
Cells2
- also is increased by incubation of cells in the presence of enkephalin or etorphine. (nih.gov)
- For the chapter 1, in Neuro2a mouse neuroblastoma cells stably transfected with the hKOPR (N2A-3HA-hKOPR), U50,488H robustly induced neurite outgrowth, but etorphine caused outgrowth to a much lower extent. (temple.edu)
Found1
- 2016). Using the SILAC (stable isotope labeling by amino acids in cell culture) approach, we have found that compared to etorphine, U50,488H promoted higher levels of single phosphorylation at T363 and S369 and double phosphorylation at T363+S369 and T357+S369 as well as triple phosphorylation at S356+T357+S369 (Chen et al. (temple.edu)
Includes1
- For this reason the package as supplied to vets always includes the human antidote along with the etorphine. (wikipedia.org)
Increase1
- The basal specific activity of adenylate cyclase continues to rise for 97 hr in the presence of enkaphalin or etorphine, whereas prostaglandin-E}-stimulated activity ceases to increase after 12-25 hr. (nih.gov)