Medication Description: Pentazocine (Pentazocinum)
PENTAZOTSIN (Pentazocinum). (#) 2-Oxy-5, 9-dimethyl-2- (3, 3-dimethylallyl) -6, 7-benzomorfan.
Synonyms: Lexier, Fortral, Dolapent, Fortal, Fortalgesic, Fortral, Fortralin, Lexir, Magadolin, Pentagin, Pentazocine, Sosegon, Sosenyl, Sosigon, Talwin, etc.
Pentazocine is a synthetic compound containing a benzomorphane nucleus of a morphine molecule, but lacking an oxygen bridge and a third six-membered nucleus characteristic of compounds of the morphine group.
Nitrogen in the piperidine core is replaced by dimethylallyl [CH 2 - CH = C (CH 3) 2]
The drug was obtained on the principle of modification of the morphine molecule, taking into account that some previously synthesized compounds close to morphine, but not containing an oxygen bridge (levorphanol, or lemoran, and others), have high analgesic activity; however, the dimethylallyl residue is an important part of the nalorfine molecule (see), which possesses a significant degree of morphine antagonist properties. It was assumed that such a modification of the morphine molecule will result in a compound with greater analgesic activity than that of nalorphine, but with fewer side effects than morphine. Pentazocine to some extent satisfies these requirements. It has analgesic activity, although to a lesser extent than morphine, but less depressing respiration, less often causes constipation and urinary retention. Currently, antagonist agonists, more active than pentazocine (nalbuphine and others).
Pentazocine is well absorbed by ingestion and parenteral administration. The peak concentration in the blood plasma is observed 15 minutes to 1 hour after intramuscular administration and 1 to 3 hours after ingestion. The elimination half-life makes 2 - 3 h.
The indications are basically the same as for morphine.
In acute pains, the drug is administered parenterally, with chronic pain inside.
The dose for adults under the skin, intramuscularly or intravenously is usually 0.03 g (30 mg), and for severe pain it is 0.045 g (45 mg). Intravenous slowly. If necessary, repeat the introduction under the skin or intramuscularly in 3-4 hours, intravenously in 2 to 3 hours.
Inside appoint adults for 0.05 g (50 mg = 1 tablet) 3-4 times a day (before meals). With severe pain, a single dose is sometimes increased to 0.1 g.
The daily dose for adults should not exceed 350 mg.
Children aged 1 to 6 years old are prescribed the drug parenterally: intramuscularly and subcutaneously - at the rate of not more than 1 mg per 1 kg of body weight per day, intravenously - not more than 0.5 mg / kg per day. Children between the ages of 6 and 12 are prescribed an oral dose of 0.025 g (25 mg = 1/2 tablet) every 3 to 4 hours.
Pentazocine is usually well tolerated. However, nausea, vomiting, dizziness, sweating, redness of the skin, respiratory depression are possible. Sometimes there may be euphoria, confusion, urinary retention.
With a sudden cessation of administration after prolonged use of the drug in relatively large doses, abstinence phenomena are possible (abdominal cramps, nausea, vomiting, agitation, tremors, etc.).