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Description medications: pentazocine (Pentazocinum)

Pentazocine (Pentazocinum). (#) 2-Hydroxy-5, 9-dimethyl-2- (3, 3-dimethylallyl) -6, 7 benzomorphans.

Synonyms: Leksir, Fortran, Dolapent, Fortal, Fortalgesic, Fortral , Fortralin, Lexir, Magadolin, Pentagin, Pentazocine, Sosegon, Sosenyl, Sosigon, Talwin and others.

Pentazocine - synthetic compound containing benzomorfanovoe core molecule of morphine, but deprived of oxygen bridge and the third six-member core group of compounds characteristic of morphine.

Nitrogen in the piperidine nucleus is substituted dimetilallilom [CH 2 - CH = C (CHs) 2]

The preparation obtained according to the principle modifications morphine molecule including some previously synthesized compounds similar to morphine, but not containing an oxygen bridge (levorphanol or lemorane, et al.), Possess high analgesic activity; however dimetilallilny balance is an important part of the molecule nalorphine (cm.) obladayushego largely morphine antagonist properties. It was assumed that such a modification of the morphine molecule lead to the preparation of compounds with analgesic activity greater than nalorphine, but with fewer side effects than morphine. Pentazocine to a certain extent meet these requirements. It has analgesic activity, although to a lesser degree than morphine, but less respiratory depression, less likely to cause constipation and urinary retention. Currently available agonist-antagonists, greater than pentazocine (nalbuphine et al.).

Pentazocine is well absorbed when taken orally and parenterally administered. The peak plasma concentration observed at 15 minutes - 1 hour after intramuscular administration and 1 - 3 hours after ingestion. The half-life is 2 - 3 hours.

Indications are basically the same as that for morphine.

For acute pain medication is administered parenterally, for chronic pain inside.

The dose for adults subcutaneously, intramuscularly or intravenously is usually 0.03 g (30 mg), and in severe pain - 0.045 g (45 mg). Intravenously injected slowly. If necessary, repeat administration subcutaneously or intramuscularly through 3 -4 hours, intravenous - 2 - 3 hours.

Inside designate an adult to 0.05 g (50 mg = 1 tablet) 3 - 4 times a day (before meals). When severe pain is sometimes a single dose increased to 0.1 g

The daily dose for adults should not exceed the ingestion of 350 mg.

Children aged 1 to 6 years parenterally administered drug: intramuscular and subcutaneous - a rate less than 1 mg per 1 kg of body weight per day, intravenously - no more than 0.5 mg / kg per day. Children aged 6 to 12 years are designated inwards to 0,025 g (25 mg = 1/2 tablet) every 3 - 4 hours.

Pentazocine usually well tolerated. However, possible nausea, vomiting, dizziness, sweating, redness of the skin, respiratory depression. Sometimes there may be euphoria, confusion, urinary retention.

With the sudden discontinuation after long-term use of the drug in relatively high doses may phenomenon abstinence (abdominal cramps, nausea, vomiting, agitation, tremors, etc.).