Pentazocine
Opioid medication / From Wikipedia, the free encyclopedia
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Pentazocine,[3] sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain. It is believed to work by activating (agonizing) κ-opioid receptors (KOR) and μ-opioid receptors (MOR). As such it is called an opioid as it delivers its effects on pain by interacting with the opioid receptors. It shares many of the side effects of other opioids like constipation, nausea, itching, drowsiness and respiratory depression, but unlike most other opioids it fairly frequently causes hallucinations, nightmares and delusions. It is also, unlike most other opioids, subject to a ceiling effect, which is when at a certain dose (which differs from person-to-person) no more pain relief, or side effects, is obtained by increasing the dose any further.[4]
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AHFS/Drugs.com | Monograph (hydrochloride) Monograph (lactate) | ||
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Routes of administration | Oral, IV, IM | ||
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Bioavailability | ~20% orally | ||
Metabolism | Hepatic | ||
Onset of action | 15 min[2] | ||
Elimination half-life | 2 to 3 hours | ||
Excretion | Renal | ||
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ECHA InfoCard | 100.006.032 | ||
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Formula | C19H27NO | ||
Molar mass | 285.431 g·mol−1 | ||
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Chemically it is classed as a benzomorphan and it comes in two enantiomers, which are molecules that are exact (non-superimposable) mirror images of one another.
It was patented in 1960 and approved for medical use in 1964.[5] Usually, in its oral formulations, it is combined with naloxone so as to prevent people from crushing the tablets, dissolving them in a solvent (like water) and injecting them for a high (as orally administered naloxone produces no opioid-negating effects, whereas intravenous or intramuscular administration does).[4]