NALOKSON (Naloxonum). (-) N Allil-14- oksinordigidromorfinon, or (-) -17 - allyl-4-epoksi 3, 14-digidroksimorfinan-6- it.

     Synonyms : Naloxone hydrochloride, Narcan, Narcanti.

     On chemical structure similar to nalorfinu naloxone, and nitrogen atom, it also contains allilny Radical and is mainly an oxo (= O) deputy instead of hydroxyl (OH-) in regulation 14.

     Pharmacologically naloxone is that is <<net>> opioid antagonist deprived morfinopodobnoy activity. Is it the kind of competitive antagonism by blocking the binding of agonists or excluding them from opiate receptors. Naloxone is the highest affinity for m-and x receptors. In high doses, the drug can give a small agonistichesky effect, without, however, impractical.

     Enter naloxone intramuscularly or intravenously, when administered ineffectual, as rapidly metabolized in the liver. When parenteral introduce a fast (1 to 3 minutes), but had an on (from 0.5 to 3 to 4 h), depending on the dose and the method of application.

     Naloxone applied mainly in acute drug intoxication analgetikami. It is also effective in alcoholic coma and different types of shock, due apparently to activate in shock and some forms of stress endogenous opioid system, as well as the ability to reduce naloxone hypotension.

     Both of naloxone limit its application to the treatment of drug addiction (see patients).

     Introduction naloxone drug addicts is a characteristic attack symptoms, sometimes used to detect the disease.

     Applied as an antagonist naloxone <<net>> agonists usually dose 0.4 - 0.8 mg. In order to address the phenomenon intoxicated when applying agonistov- antagonists (pentazotsina, nalbufina, butorfonala) require large doses of naloxone (10 - 15 mg).

     For the diagnosis of drug impose 0.5 mg naloxone when consuming <<net>> agonists and higher doses when used agonistovantagonistov.

     Product : in 1 ml ampoules containing 0.4 mg naloxone hydrochloride. Available as a special product formulation for use in newborns, neonatal Narcan with 0.02 mg naloxone in 1 ml.

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