Pentazocine: Difference between revisions

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{{Drugbox|
| IUPAC_name = (1''S'',9''S'',13''S'')-1,13-dimethyl-10-(3-methylbut-2-en-1-yl)-<br>10-azatricyclo[7.3.1.0<sup>2,7</sup>]trideca-2,4,6-trien-4-ol
| image = pentazocine.png
| width = 180
| CAS_number = 359-83-1
| ATC_prefix = N02
| ATC_suffix = AD01
| PubChem = 441278
| DrugBank = APRD01173
| C = 19 |H = 27 |N = 1 |O = 1
| molecular_weight = 285.424 [[Gram|g]]/[[Mole (unit)|mol]]
| bioavailability = ~20% orally
| metabolism = [[Liver|Hepatic]]
| elimination_half-life = 2 to 3 hours
| excretion = [[Kidney|Renal]]
| pregnancy_category = C/D <small>([[United States|U.S.]])</small>
| legal_status = [[Schedule IV]] <small>(U.S.)</small>
| routes_of_administration = Oral
}}
'''Pentazocine''' is a synthetically-prepared [[narcotic]] ([[opioid]] [[analgesic]]) drug used to treat mild to moderately severe pain. Pentazocine is sold under several brand names, such as '''Talwin''' (with [[naloxone]]) and '''Talacen''' (with [[acetaminophen]]).  It should be noted that this compound may exist as one of two enantiomers, named (+)-pentazocine and (-)-pentazocine.  (-)-pentazocine is a kappa-opioid receptor agonist, while (+)-pentazocine is not, and displays selectivity to the related sigma receptor.


==Adverse effects==
Side effects are similar to those of [[morphine]], but ''Pentazocine'' may be more likely to cause [[hallucinations]] and other psychotomimetic effects; cardiovascular effects make it unsuitable for use in myocardial infarction. Unlike morphine its respiratory [[depressant]] action is subject to a "ceiling" effect. It can be used as analgesics for dental extractions except in heroin addict patients.
[[Image:pentazocine.jpg|frame|left]]
==Recreational use==
In the [[1980s]], recreational drug users discovered that combining pentazocine with the [[antihistamine]] [[tripelennamine]] (most commonly dispensed under the brand name [[Pyribenzamine]]) produced a euphoric sensation much like that brought on by [[heroin]]. Users who were already addicted to the latter often used this combination when heroin was unavailable to them.  Since tripelennamine tablets are typically blue in color, the pentazocine/tripelennamine combination acquired the [[slang]] name ''Ts and blues''. After health-care professionals and drug-enforcement officials became aware of this scenario, the narcotic-antagonist [[naloxone]] was added to preparations containing pentazocine, and the reported incidence of its abuse has declined precipitously since.  It is commonly asserted that the use of pentazocine with tripelennamine originated amongst dentists, doctors, and nurses in the Middle Western United States. A more recent development is that pentazocine is combined with [[methylphenidate]] (Ritalin) via the oral route or insufflation.
==Administration==
Pentazocine is administered by [[subcutaneous]], [[intramuscular]], and [[intravenous]] injection as the [[lactic acid|lactate]]: The usual dose is the equivalent of pentazocine 30 to 60 mg every 3 to 4 hours; it should not be necessary to exceed 360 mg daily. It is also available in 25mg pills. 
In a study published in the [[March 24]], [[2003]] issue of the [[Proceedings of the National Academy of Sciences]], a team led by [[McGill University]] researcher Jeffrey Mogil found that women with [[red hair]] require less pentazocine for pain relief than do women with other hair colours or men of any hair colour.
==Legal status==
Pentazocine is still classified in Schedule IV under the [[Controlled Substances Act]] in the [[United States]], even with the addition of the naloxone. Internationally, pentazocine is a Schedule III drug under the [[Convention on Psychotropic Substances]].[http://www.incb.org/pdf/e/list/green.pdf]
==External links==
*[http://www.eurekalert.org/pub_releases/2003-03/mu-rwr032403.php Eurekalert report on PNAS article]
{{Analgesics}}
[[de:Pentazocin]]
[[Category:Azocines]]
[[Category:Opioids]]
[[Category:Drugs]]
[[pl:Pentazocyna]]
{{WikiDoc Sources}}

Revision as of 19:07, 9 June 2014