Teturamum

General characteristics. Structure:

Active agent: Disulfiramum of 150 mg.

Pharmacological properties:

Means for treatment of alcohol addiction. Aldehyde a dehydrogenase which participates in alcohol metabolism exerts the inhibiting impact on enzyme. It leads to increase in concentration of a metabolite of alcohol of the acetic aldehyde causing rushes of blood to the person, nausea, vomiting, a febricula, tachycardia, decrease in the ABP which do extremely unpleasant alcohol intake after reception of Disulfiramum.

Pharmacokinetics. After intake there is bystry, but incomplete (70-90%) an absorption of active agent from a GIT.
Thanks to high solubility in lipids, Disulfiramum is widely distributed in an organism and collects in various fat depos.
Disulfiramum is quickly metabolized in diethyldithiocarbamate (DDK) which is partially removed in the form of carbon sulfur with expired air and is partially metabolized in a liver in metil-DDK. The last turns into an active metabolite - diethylthiocarbamic acid methyl ether (metil-DTK). Cmax in a blood plasma metil-DTK is reached in 4 h after reception of Disulfiramum, but the maximum inhibiting activity in the relation dehydrogenase aldehyde for the first time is observed in 3 days of reception.
T1/2 metil-DTK makes about 10 h, at the same time the inhibiting activity in the relation aldehyde of a dehydrogenase proceeds much longer. The effect, thus, can remain within 7-14 days after cancellation.
At weak or moderate deterioration in function of a liver, metabolism does not change. On the contrary, at cirrhosis increase in concentration of metabolites in blood is observed.
Metabolites are removed mainly with urine. A part is removed with expired air in the form of carbon sulfur. 20% in the form of not changed Disulfiramum are removed through intestines.
To 20% of a dose can remain in an organism within 1 week and more.
After implantation Disulfiramum gets into blood. Minimum content of Disulfiramum in blood - about 20 ng/ml. Content in DDK blood and carbon sulfur reaches 0.14 mkg/ml after implantation of 1-1.6 g of Disulfiramum. However, despite these very low levels, reactions Disulfiramum ethanol can arise within 5-9 months after implantation.

Indications to use:

For intake: prevention of a recurrence during treatment of an alcoholism.
For implantation: treatment of an alcoholism, as disintoxication cure for chronic poisoning with nickel.

Route of administration and doses:

At intake the dose makes 125-500 mg/days, the scheme of treatment is defined individually.
At implantation by means of a special technique enter 800 mg into a hypodermic fatty tissue.

Features of use:

With care to apply at patients with a renal failure, diseases of a liver, respiratory system.

Side effects:

From the alimentary system: metal smack in a mouth; seldom - hepatitises.
From TsNS: polyneurites of the lower extremities, psychological frustration, decrease in memory, disorientation, headache.
Allergic reactions: skin rash, itch.
The reactions caused by association Disulfiramum ethanol: collapse, disturbances of a cordial rhythm, stenocardia attacks, myocardial infarction, wet brain.

Interaction with other medicines:

At simultaneous use with anticoagulants derivative coumarin (including with warfarin) anticoagulating action amplifies, the risk of development of bleedings increases.

Disulfiramum inhibits liver enzymes therefore at simultaneous use of the drugs which are metabolized in a liver disturbance of their metabolism is possible.

At simultaneous use of Disulfiramum with the tricyclic antidepressants derivative of a fenotiazin, MAO inhibitors there is a risk of development of the serious side reactions connected with medicinal interaction.

The case of development of a mania in the patient accepting Disulfiramum and буспирон is described.

At simultaneous use the clearance of desipramine and Imipraminum from an organism decreases.

At simultaneous use with amitriptyline strengthening of therapeutic action of Disulfiramum is possible, however also strengthening of toxic effect of amitriptyline on TsNS is possible.

At simultaneous use concentration in a blood plasma of diazepam and chlordiazepoxide, in certain cases followed by dizziness increases. Under the influence of diazepam reduction of intensity of reaction Disulfiramum alcohol is possible. The case of strengthening of toxicity of temazepam is described.

At simultaneous use with an isoniazid cases of development of dizziness, depression are described; with caffeine - removal of caffeine from an organism decreases; with metronidazole - acute psychosis, confusion of consciousness develops; with omeprazoly - the case of development of disturbance of consciousness and a catatonia is described.

At simultaneous use with Perfenazinum it is impossible to exclude development of psychotic symptoms.

At simultaneous use Disulfiramum inhibits metabolism and removal of rifampicin.

At simultaneous use with phenazone phenazone T1/2 increases; with Phenytoinum - effects of Phenytoinum owing to increase in its concentration in a blood plasma amplify, toxic reactions develop.

At simultaneous use with hlorzoksazony concentration of a hlorzoksazon in a blood plasma increases; with Chlorpromazinum - strengthening of arterial hypotension is possible.

Contraindications:

Serious cardiovascular illness, heavy liver failure, diabetes mellitus, epilepsy, psychological diseases; a concomitant use of Phenytoinum, an isoniazid, metronidazole, the simultaneous use of the drinks containing alcohol or reception of the medicines containing ethanol, and also their use during 24 h after reception of Disulfiramum; pregnancy, lactation; hypersensitivity to Disulfiramum.

Use at pregnancy and feeding by a breast
It is contraindicated to use at pregnancy and in the period of a lactation.
Before performing implantation it is necessary to exclude pregnancy. Against the background of action of Disulfiramum it is necessary to apply well-tried remedies of contraception.

Use at abnormal liver functions
It is contraindicated at a heavy liver failure. With care to apply at patients with liver diseases.

Use at renal failures
With care to apply at patients with a renal failure.

Overdose:

It is not described.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 150 mg: 30 or 50 pieces.