Pentazocine

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Pentazocine , sold under the Talwin trademark among others, is a pain reliever used to treat moderate to severe pain. It is believed to work by activating (agonizing)? -opioid receptors (KOR) and blocking (antagonizing)? -opioid receptors (MOR). Such is called an opioid because it gives its effect on pain by interacting with opioid receptors. It shares many other opioid side effects such as constipation, nausea, itching, drowsiness and decreased effort to breathe, but unlike most other opioids, it quite often leads to hallucinations, nightmares and delusions. This, too, unlike most other opioids, is subject to the ceiling effect, ie when at certain doses (different from person to person) no more pain relievers, or side effects, are obtained by increasing the dose further.

Chemically it is classified as benzomorphan and it comes in two enantiomers, which are molecules that are the exact reflection of one another.

Usually, in oral formulations, combined with naloxone prevents people from destroying the tablet, dissolving it in a solvent (like water) and injecting it into a high (such as naloxone, if taken, does not produce any effect). If injected, however).

Video Pentazocine

Use

Medical

Pentazocine is used primarily to treat pain, although its analgesic effect is subject to the effect of the palate. It has been terminated by its corporate sponsor in Australia, although it may be available through a special access scheme.

Recreation

In the 1970s, drug users planned to find that combining pentazocine with tripleennamine (the first-ever antihistamine ethylenediamine most often omitted under the brand name Pelamine and Pyribenzamine) resulted in euphoric sensation. Since tripleennamine tablets are usually blue in color and the Pentazocine brand name is known as Talwin (hence "Ts"), the combination of pentazocine/tripleennamine earns the name of the slang Ts and blues . After health care professionals and law enforcement officers are aware of this scenario, the naloxone antagonist mu-opioid is added to oral preparations containing pentazocine to prevent perceived "misuse" by injection, and the reported incidence of recreational use has dropped dramatically. since.

Research

In small clinical studies open dose, add-on, one-day, acute dose, pentazocine was found rapidly and substantially reduced the symptoms of mania in individuals with bipolar disorder who were in the manic phase of the condition. It postulates that the observed efficacy is due to the receptor-mediated mediated-amelioration of hyperdopaminergia in the reward pathway. Minimal sedation and no adverse effects include psychotomimetic effects or worsening of psychosis observed at given doses.

Maps Pentazocine

Adverse effects

Side effects are similar to morphine, but pentazocine, because its action on kappa opioid receptors is more likely to trigger a psychotomimetic effect. High doses can cause high blood pressure or high heart rate. It may also improve cardiac work after myocardial infarction when administered intravenously and hence this use should be avoided if possible. Respiratory depression is a common side effect, but is subject to the ceiling effect, so at a certain dose the rate of respiratory depression will not increase again with increasing doses. It is also rarely associated with agranulocytosis, erythema multiforme and toxic epidermal necrolysis.

Network damage at injection site

Necrosis and sepsis at the site of severe injection have occurred (sometimes requiring limb amputation) with multiple lactate multipazocine injections. In addition, animal studies show that Pentazocine is poorly tolerated subcutaneously rather than intramuscularly.

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History

Pentazocine was developed by the Sterling Drug Company, the Sterling-Winthrop Research Institute, from Rensselaer, New York. It was approved by the Food and Drug Administration in June 1967 after being reviewed well after testing in 12,000 patients in the United States. Analgesic compounds were first made in Sterling in 1958. US tests were conducted between 1961 and 1967. By mid-1967 Pentazocine was already sold in Mexico, the United Kingdom, and Argentina, under different trade names.

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Society and culture

Legal status

Pentazocine was originally classified in Schedule V under the Controlled Substance Act but the petition filed with D.E.A. on October 1, 1971, to change 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 Lawyering program for Public Interest. The petition was accepted for review on November 10, 1971 D.E.A. issued the Final Rule that transferred it to the IV schedule on 10 January 1979, with the effective date of 9 February 1979 This is understood as the first example of a successful petition to reclassify a substance under the recently enacted Control Substances Act. Pentazocine is still classified in Schedule IV under the Controlled Substance Act in the United States, even with the addition of Naloxone. although some countries classify it in Schedule II (Illinois and South Carolina (injection form only)) or Schedule III (Kentucky). Internationally, pentazocine is a drug Schedule III under the Convention on Psychotropic Substances. Pentazocine has DEA ACSCN 9720; As Schedule IV substance, DEA does not set annual production quotas for pentazocine for the United States.

Brand name

Pentazocine is sold under several brand names, such as Fortral, Sosegon, Talwin NX (with naloxone), Talwin, Talwin PX, Fortwin and Talacen (with paracetamol (acetaminophen)).

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See also

• Cyclazocin (hallucinogen)
• Volazocine

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References

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External links

• Eurekalert report on PNAS article

Source of the article : Wikipedia