Pentazocine
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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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Pharmacokinetic data | |||
Bioavailability | ~20% orally | ||
Metabolism | Hepatic | ||
Onset of action | 15 min[2] | ||
Elimination half-life | 2 to 3 hours | ||
Excretion | Renal | ||
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Pentazocine,
Chemically it is classed as a
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]
Use
Medical
Pentazocine is used primarily to treat pain, although its analgesic effects are subject to a ceiling effect.[6] It has been discontinued by its corporate sponsor in Australia, although it may be available through the special access scheme.[4]
Recreational
In the 1970s, recreational drug users discovered that combining pentazocine with tripelennamine (a first-generation ethylenediamine antihistamine most commonly dispensed under the brand names Pelamine and Pyribenzamine) produced a euphoric sensation. Since tripelennamine tablets are typically blue in color and brand-name Pentazocine is known as Talwin (hence "Ts"), the pentazocine/tripelennamine combination acquired the slang name Ts and blues.[7][8][9] After health-care professionals and drug-enforcement officials became aware of this scenario, the
Research
In an open-label, add-on, single-day, acute-dose small clinical study, pentazocine was found to rapidly and substantially reduce symptoms of
Adverse effects
Side effects are similar to those of
Tissue damage at injection sites
Severe injection site necrosis and sepsis has occurred (sometimes requiring amputation of limb) with multiple injection of pentazocine lactate. In addition, animal studies have demonstrated that Pentazocine is tolerated less well subcutaneously than intramuscularly.[12]
History
Pentazocine was developed by the Sterling Drug Company, Sterling-Winthrop Research Institute, of Rensselaer, New York. The analgesic compound was first made at Sterling in 1958. U.S. testing was conducted between 1961 and 1967. It was approved by the Food and Drug Administration in June 1967 after being favorably reviewed following testing on 12,000 patients in the United States. By mid 1967 Pentazocine was already being sold in Mexico, England, and Argentina, under different trade names.[13]
Society and culture
Legal status
Pentazocine was originally unclassified under the Controlled Substances Act. A petition was filed with the Drug Enforcement Administration on October 1, 1971, to shift it to Schedule III. The petition was filed by Joseph L. Fink III, a pharmacist and law student at Georgetown University Law Center as part of the course Lawyering in the Public Interest. That petition was accepted for review on November 10, 1971.[14] D.E.A. published a Final Rule transferring it to schedule IV on January 10, 1979, with an effective date of February 9, 1979.[15] This is understood to be the first instance of a successful petition to reclassify a substance under the relatively recently enacted Controlled Substances Act.[citation needed] Pentazocine is still classified in Schedule IV under the Controlled Substances Act in the United States, even with the addition of Naloxone. Some states classify it in Schedule II, such as Illinois[16] and South Carolina (injectable form only),[17] or Schedule III such as Kentucky.[18]) Internationally, pentazocine is a Schedule III drug under the Convention on Psychotropic Substances.[19] Pentazocine has a DEA ACSCN of 9720; being a Schedule IV substance, the DEA does not assign an annual manufacturing quota for pentazocine for the United States.
Brand names
Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX (with naloxone), Talwin, Talwin PX, Fortwin and Talacen (with paracetamol (acetaminophen)).
See also
- hallucinogenic)
- Volazocine
References
- ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
- ISBN 9780781737623.
- ^ US Patent 4105659 Analgesia producing benzazocines
- ^ a b c d e f g Brayfield A, ed. (9 January 2017). "Pentazocine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 1 September 2017.
- ISBN 9783527607495.
- ^ ISBN 978-0-85711-084-8.
- S2CID 21976943.
- S2CID 6288581.
- PMID 7932913.
- ^ "Pentazocine and Naloxone tablets". DailyMed. National Institute of Health. Retrieved 2011-12-10.
- ^ PMID 26733781.
- ^ "TALWIN (pentazocine lactate) injection, solution". DailyMed. National Institute of Health. Retrieved 2011-12-10.
- New York Times, June 27, 1967, pg. 41.
- ^ 36 Fed.Reg. 217. November 1971.
- ^ 44 Fed. Reg. 2169. 1979.
- ^ "Illinois Controlled Substances Act". Illinois General Assembly.
- ^ "South Carolina DHEC Controlled Substance Schedule". South Carolina Department of Health and Environmental Control.
- ^ "Kentucky Scheduled Drug List" (PDF). Kentucky Cabinet for Health and Family Services.
- ^ "List of psychotropic substances under international control" (PDF). Green List - Annex to the annual statistical report on psychotropic substances (form P) (27th ed.). International Narcotics Control Board. 2016.