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Pethidine Intermediate B
Norpethidine (normeperidine, pethidine intermediate B) is a 4-phenylpiperidine derivative that is both a precursor to, and the toxic metabolite of, pethidine (meperidine). It is scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9233. The 2014 annual manufacturing quota was . Norpethidine is a controlled drug because of its potential uses in manufacturing both pethidine itself and a range of ''N''-substituted derivatives, but it has little opioid activity in its own right. Instead, norpethidine acts as a stimulant and causes convulsions. Bioaccumulation of norpethidine is a major complication when pethidine is used in medicine as an analgesic, as when pethidine is used in high doses or administered by intravenous infusion, norpethidine can accumulate in the body at a faster rate than it is being excreted, particularly in elderly patients or those with compromised liver or kidney fu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Phenylpiperidine
4-Phenylpiperidine is a chemical compound. It features a benzene ring bound to a piperidine ring. 4-Phenylpiperidine is the base structure for a variety of opioids, such as pethidine (meperidine), ketobemidone, alvimopan, loperamide, and diphenoxylate. See also * MPTP MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a prodrug to the neurotoxin MPP+, which causes permanent symptoms of Parkinson's disease by destroying dopaminergic neurons in the substantia nigra of the brain. It has been used to study d ... References External links * {{DEFAULTSORT:Phenylpiperidine, 4- 4-Piperidinyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Furethidine
Furethidine is a 4- phenyl piperidine derivative that is related to the clinically used opioid analgesic drug pethidine (meperidine), but with around 25x higher potency. According to another source, Furethidine is 500/30 = 16.7 x the potency of pethidine (table VII). Furethidine is not currently used in medicine and is a Class A/ Schedule I drug which is controlled under UN drug conventions. It has similar effects to other opioid derivatives, such as analgesia, sedation, nausea and respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapnia .... In the United States it is a Schedule I Narcotic controlled substance with the ACSCN of 9626. References External links UNODC Bulletin on Narcotics 1961 Synthetic opioids Tetrahydrofurans 4-Phenylpiperidines Carb ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic Opioids
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent Drug withdrawal, withdrawal. Opioids can cause death and have been used for Capital punishment in the United States, executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause Drug tolerance, tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsants
A convulsant is a drug which induces convulsions and/or epileptic seizures, the opposite of an anticonvulsant. These drugs generally act as stimulants at low doses, but are not used for this purpose due to the risk of convulsions and consequent excitotoxicity. Most convulsants are antagonists (or inverse agonists) at either the GABAA or glycine receptors, or ionotropic glutamate receptor agonists. Many other drugs may cause convulsions as a side effect at high doses (e.g. bupropion, tramadol, pethidine, dextropropoxyphene, clomipramine) but only drugs whose primary action is to cause convulsions are known as convulsants. Nerve agents such as sarin, which were developed as chemical weapons, produce convulsions as a major part of their toxidrome, but also produce a number of other effects in the body and are usually classified separately. Dieldrin which was developed as an insecticide blocks chloride influx into the neurons causing hyperexcitability of the CNS and convulsi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pethidine Intermediate C
Pethidinic acid (meperidinic acid, pethidine intermediate C) is a 4-phenylpiperidine derivative that is both a metabolite of and a precursor to pethidine (meperidine). It is scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9234. The 2014 annual manufacturing quota was 6 grams. Pethidinic acid is a controlled drug because of its potential uses in manufacturing both pethidine itself and some of its substituted derivatives, but it has little opioid activity in its own right. Metabolism of pethidine to pethidinic acid is carried out mainly by the carboxylesterase enzyme hCE-1 in the liver, and since the activity of this enzyme can vary between individuals, the rate and extent of pethidinic acid production can vary. Frank Wätjen used pethidinic acid as a precursor chemical to a heterocyclic moiety. See also * Moramide intermediate * Methadone intermediate * Pethidine intermediate A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pethidine Intermediate A
Pethidine intermediate A is a 4- phenyl piperidine derivative that is a precursor to the opioid analgesic drug pethidine (meperidine). It is not known to have any analgesic activity in its own right, however other derivatives of pethidine with a 4-cyano group in place of the carboxylate ethyl ester have been found to be active, so pethidine intermediate A might also show opioid effects. It is scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9232. The 2014 annual manufacturing quota was 6 grammes (as an end product, presumably for research use). See also * Moramide intermediate * Methadone intermediate * Pethidine intermediate B (norpethidine) * Pethidine intermediate C Pethidinic acid (meperidinic acid, pethidine intermediate C) is a 4-phenylpiperidine derivative that is both a metabolite of and a precursor to pethidine (meperidine). It is scheduled by UN Single Convention on N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methadone Intermediate
Methadone intermediate is a methadone precursor scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9254. The 2014 annual manufacturing quota was 32 875 kilos.http://www.deadiversion.usdoj.gov/quotas/conv_factor/index.html See also * Moramide intermediate * Pethidine intermediate A * Pethidine intermediate B (norpethidine) * Pethidine intermediate C (pethidinic acid) References Synthetic opioids Drug rehabilitation Dimethylamino compounds {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Moramide Intermediate
Moramide intermediate (3-methyl-4-morpholin-4-yl-2,2-diphenylbutanoic acid, on INCB Yellow List as 2-methyl-3-morpholino-1,1-diphenylpropane carboxylic acid) is a moramide precursor scheduled by UN Single Convention on Narcotic Drugs. In the United States, moramide intermediate is designated as a Schedule II controlled substance, and has an ACSCN of 9802. The 2014 annual manufacturing quota was nil. See also * Moramide * Methadone intermediate Methadone intermediate is a methadone precursor scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9254. The 2014 annual manufacturing quota was ... * Pethidine intermediate A * Pethidine intermediate B (norpethidine) * Pethidine intermediate C (pethidinic acid) References Analgesics 4-Morpholinyl compunds {{organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O-Desmethyltramadol
Desmetramadol (), also known as ''O''-desmethyltramadol (''O''-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 in the same way as codeine, and so similarly to the variation in effects seen with codeine, individuals who have a less active form of CYP2D6 ("poor metabolizers") will tend to get reduced analgesic effects from tramadol. This also results in a ceiling effect (dependent on CYP2D6 availability) which limits tramadol's range of therapeutic benefits to the treatment of moderate pain. Pharmacology Pharmacodynamics (+)-Desmetramadol is a G-protein biased μ-opioid receptor full agonist. It shows comparatively far lower affinity for the δ- and κ-opioid receptors. The two enantiomers of desmetramadol show quite distinct pharmacological profiles; both (+) and (−)-desmetramadol are inactive as serotonin reuptake inhibitors, but (−)-desmetramadol retains activity as a norepinephrine reuptake inhi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nortilidine
Nortilidine is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine. The (1R,2S) isomer has NMDA antagonist activity. The drug also acts as a dopamine reuptake inhibitor. The reversed-ester of nortilidine is also known, as is the corresponding analogue with the cyclohexene ring replaced by cyclopentane, which have almost identical properties to nortilidine. Use Nortilidine has been sold as a designer drug A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Des ..., first being identified in Poland in May 2020. See also * Desmetramadol, another opioid metabolite with additional (non-opioid) mechanisms of analgesia, which has also been sold as a designe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxpheneridine
OxpheneridineCS Patent 109234 is a 4- phenyl piperidine derivative that is related to the opioid analgesic drug pethidine (meperidine). Oxpheneridine is not currently used in medicine. Presumably it has similar effects to other opioid derivatives, such as analgesia, sedation, nausea and respiratory depression. Unlike most opioid derivatives, oxpheneridine is not specifically listed as an illegal drug. In the UNODC narcotics report of 1958, they state that it was not possible to administer oxpheneridine in high doses as it is poorly soluble and highly irritating, and at the low doses administered it did not produce addiction in animals. This appears to be the only time oxpheneridine has been investigated, and so its pharmacological properties have not been well established. Oxpheneridine would probably be regarded as a controlled substance analogue of pethidine on the grounds of its related chemical structure in some jurisdictions such as the United States, Australia and Ne ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piminodine
Piminodine (Alvodine) is an opioid analgesic that is an analogue of pethidine (meperidine). It was used in medicine briefly during the 1960s and 70s, but has largely fallen out of clinical use. It was used particularly for obstetric analgesia and in dental procedures and, like pethidine, could be combined with hydroxyzine to intensify the effects. The duration of action is 2 to 4 hours and 7.5 to 10 mg via the subcutaneous route is the most common starting dose, being equal to 80 to 100 mg of pethidine, 40 to 60 mg of alphaprodine and 10 mg of morphine. Oral formulations were also available. Piminodine has similar effects to other opioids, and produces analgesia, sedation and euphoria. Side effects can include itching, nausea and potentially serious respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
