Antabuse
Antabuse (Dissulfiram)Pharmacological action
Agent for treatment of alcoholic dependence. Inhibiting impact on enzyme aldehyde a dehydrogenase which participates in a metabolism of ethyl alcohol makes. It leads to rising of concentration of a metabolite of ethyl alcohol of the acetaldehyde causing rushes of blood to the person, nausea, vomiting, a febricula, a tachycardia, dropping of a BP which do extremely unpleasant the use of alcohol after Disulfiramum reception.
Pharmacokinetics
After intake occurs fast, but incomplete (70-90 %) absorption of active substance from GASTROINTESTINAL TRACT.
Thanks to high solubility in lipids, Disulfiramum is widely distributed in an organism and collects in various fatty depots.
Disulfiramum is quickly metabolized and is partially deduced in the form of a carbon disulfide with exhaled air and partially metabolized in a liver in methyl-ddk. Last turns to an active metabolite. Cmax in a blood plasma methyl-dtk is reached through 4 h after Disulfiramum reception, but the maximum inhibiting activity in the relation dehydrogenase aldehyde is observed for the first time in 3 days of reception.
T1/2 Methyl-dtk makes nearby 10 h, thus inhibiting activity in the relation dehydrogenase aldehyde proceeds much more longly. The effect, thus, can remain within 7-14 days after cancellation.
At weak or moderate deterioration of function of a liver, the metabolism does not vary. On the contrary, at a cirrhosis rising of concentration of metabolites in blood is observed.
Metabolites are deduced mainly with urine. The part is deduced with exhaled air in the form of a carbon disulfide. 20 % in the form of not changed Disulfiramum are deduced through an intestine.
To 20 % of a dose can remain in an organism within 1 week and more.
After implantation Disulfiramum gets into blood. The minimum maintenance of Disulfiramum in blood - nearby 20 ng/ml. . However, despite these very low levels, reactions Disulfiramum-ethanol can arise during 5-9 months after implantation.
Indications
For intake: preventive maintenance of relapses during alcoholism treatment.
For implantation: alcoholism treatment, as a disintoxication agent at a chronic poisoning with nickel.
Dosage regimen
At intake the dose makes 125-500 mg/sut, the treatment scheme is defined individually.
At implantation into a subcutaneously-fatty fat by means of a special technique enter 800 mg.
Side effect
From the alimentary system: metal smack in a mouth is possible; seldom - hepatitises.
From party TSNS: polyneurites of the bottom extremities, psychological disorders, memory depression, a disorientation, a headache are possible.
Allergic reactions: the dermal eruption, an itch are possible.
The reactions caused by association Disulfiramum-ethanol: a collapse, disturbances of a warm rhythm, stenocardia attacks, a myocardial infarction, wet brain.
Contraindications
Serious cardiovascular diseases, serious hepatic insufficiency, diabetes, epilepsy, psychological diseases; simultaneous reception of Phenytoinum, Isoniazidum, metronidazole, the simultaneous use of the drinks containing alcohol or reception of medicinal preparations, containing ethanol, and also their use during 24 h after Disulfiramum reception; pregnancy, a lactemia; a hypersensibility to Disulfiramum.
Pregnancy and lactemia
It is contraindicative to application at pregnancy and in a lactemia.
Before implantation carrying out it is necessary to exclude pregnancy. Against Disulfiramum action it is necessary to apply reliable agents of contraception.
Special indicatings
With care to apply at patients with renal insufficiency, diseases of a liver, respiratory system.
Medicinal interaction
Disulfiramum can strengthen toxic effects of Antipyrinum, Phenytoinum, Chlordiasepoxidum and Diazepamum by inhibition of their metabolism.
Disulfiramum inhibits oxidation and a renal egestion of rifampicin. In experimental researches it is shown, that Disulfiramum can influence Morphinum and amphetamine metabolism in the same way.
Inhibits at simultaneous application of the preparations metabolized in a liver, rising of their concentration in a blood plasma is possible.
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