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Description medications: Naloxone (Naloxonum)

NALOXONE (Naloxonum). (-) N-Allyl-14-oksinordigidromorfinon or (-) -17-allyl-4 -epoxy 3, 14-digidroksimorfinan-6-one.

Synonyms: Naloxone hydrochloride, Narcan, Narcanti.

The chemical structure close to nalorfinu naloxone, with the nitrogen atom it also contains an allyl radical, and differs mainly in the presence of oxo (= O) substituent instead of hydroxyl (-OH) at position 14.

Pharmacologically naloxone characterized in that a << clear >> opiate antagonist devoid of morphine-like activity. He acts according to the type of competitive antagonism by blocking the binding of agonists or displacing them from opiate receptors. The highest affinity naloxone has to m - x and receptors. At high doses, the drug may make small agonistic effect has not, however, practical value.

Enter naloxone intramuscularly or intravenously, ingestion is ineffective, as is rapidly metabolized in the liver. For parenteral administration acts quickly (after 1 - 3 min), but relatively short-lived (from 0.5 to 3 - 4 hours), depending on dose and method of application.

Apply naloxone mainly in acute intoxication narcotic analgesics. It is also effective in alcohol coma and various types of shock, due, apparently, to activation in shock and some forms of stress endogenous opioid system and reduce the capacity of naloxone to hypotension.

The short duration of action of naloxone limited its use for the treatment of drug addiction (see. Naltrexone).

Introduction naloxone suffering from drug addiction is a typical attack symptoms than is sometimes used to detect the disease.

Applied naloxone as antagonist >> << pure agonist usually at 0.4 - 0.8 mg. For removal of intoxication when applying antagonists agonists (pentazocine, nalbuphine, butorfonala) require large doses of naloxone (10 - 15 mg).

For the diagnosis of drug addiction is administered 0.5 mg of naloxone in the use of the net << >> agonists and higher doses when used agonistovantagonistov.

Product: in 1 ml ampoules containing 0.4 mg of naloxone hydrochloride. Available as a special formulation for use in infants - Narcan neonatal containing 0.02 mg of naloxone in 1 mL of solution.