The instruction for use
medicine for experts
the Trade name
the International unlicensed
name Disulfiramum Dosage Form
of the Tablet of 500 mg
One tablet contains
active agent – Disulfiramum of 500 mg,
excipients: PVP K30 povidone, starch corn, cellulose microcrystalline PH 102, silicon dioxide colloidal (aerosil 200), sodium of starch glikolit (explotab), magnesium stearate.
of the Tablet of white color with crosswise risky on one party
the Drugs used in alcohol addiction.
The code of automatic telephone exchange N07BB01
Pharmacokinetics At properties intake extent of absorption of Disulfiramum is non-constant, is distributed, first of all, in kidneys, a pancreas, a liver, intestines and fatty tissue. Disulfiramum is quickly metabolized in diethyldithiocarboxilic acid (DDK) which is conjugated with glucuronic acid, is oxidized to sulfate, methylated and breaks up to diethyl amine which is removed by kidneys and carbon disulphide which is removed by lungs. It is removed, mainly, through kidneys.
Effect of Disulfiramum, first of all, is connected with an irreversible inactivation of an atsetaldegiddegidrogenaza. In lack of enzyme the metabolism of ethanol is blocked and intracellular concentration of ethyl aldehyde increases. The symptoms arising from reaction Disulfiramum-alcohol depend on ethyl aldehyde level. Also transformation of dopamine into noradrenaline and reduction of noradrenaline in heart tissues is inhibited that allow ethyl aldehyde to affect directly these fabrics, leading to rush of blood, tachycardia and lowering of arterial pressure.
In addition to this action of an atsetaldegiddegidrogenaza, Disulfiramum inhibits other fermental systems, including dopamine – a beta hydroxylase (turns dopamine into noradrenaline) and microsomal oxidases of a liver (responsible for metabolism of many drugs). Thus, Disulfiramum can exponentiate the effect of drugs which are exposed to metabolism by means of these enzymes.
– an alcoholism.
The route of administration and doses
Treatment is carried out under observation of the doctor.
Treatment by Alkoson has to be begun, at least, 12 hours later after the alcohol intake termination. Treatment begin with the maximum dose 500 mg/days within the 1 or 2 weeks once a day. The maintenance dose has to be 250 mg/days (150-500 mg/day) and should not exceed 500 mg.
the Side effects connected with Alkoson depend on concentration of alcohol in blood
– garlic or metal smack in a mouth
– drowsiness, feeling of fatigue, a headache
– psychological disorders
– an optic neuritis, a polyneuritis of the lower extremities, disturbance
of sense of smell, peripheral mono – and polyneuropathy
– a skin itching, rash, a small tortoiseshell, dermatitis
– a loss of consciousness
– disturbances of activity of a cardiovascular system
– exacerbation of gastritis, peptic ulcer of a stomach and
– acute psychoses, an acute alcoholic paranoid, acute alcoholic
the Contraindication tremens
– hypersensitivity to Disulfiramum and other derivatives of Teturamum
– mental diseases
– endocrine diseases (a thyrotoxicosis, diabetes)
– a pronounced cardiosclerosis, coronary insufficiency
– before – and postinfarction states
– an aortic aneurysm
– arterial hypertension of II and III stages
– atherosclerosis of brain vessels
– serious vascular diseases of a brain
– heart and vascular diseases in a decompensation stage
– diseases of the haematogenic bodies
– a pulmonary tuberculosis with a pneumorrhagia
– fresh tubercular infiltrate
– bronchial asthma
– the profound emphysema of lungs
– the bleeding stomach ulcer
– diseases of a liver and a kidney
– epilepsy and epileptiform syndromes
– neuritis of acoustical and eye nerves
– infectious diseases of a brain
– malignant tumors
– an idiosyncrasy to Teturamum
Alkoson lowers plasma clearance of diazepam and chlordiazepoxide. At treatment benzodiazepine drugs preferable are oxazepam, to alprazola or lorazepam.
Alkoson can have toxic effect at combined use with Phenytoinum, warfarin or antipyrine.
As Alkoson can increase a prothrombin time, correction of a dose at the patients accepting oral anticoagulants is necessary. At combined use of an isoniazid and Alkoson there can be a shaky gait and a behavior disorder. In that case, treatment by Alkoson has to be stopped.
If Alkoson is accepted together with metronidazole perhaps development of toxic psychosis. If it occurred, the termination of reception of one of drugs is necessary.
Chlorpromazinum and amitriptyline can increase weight of reactions Alkoson-akogol, and diazepam can reduce. Also some symptoms can be reduced by Chlorpromazinum.
instructions ALKOSON NOT OWES BE APPLIED WITHOUT the CONSENT of the PATIENT TAKING ALCOHOL.
Patients have to be informed on consequences of reaction of Alkoson-alkogol. It is impossible to take alcohol and alkogolsoderzhashchy products, drugs and also to apply the personal hygiene means containing alcohol (i.e. sauces, cough syrups, aftershave lotions). The reactions caused by combined use of drug and alcohol can be shown even 14 days later after alcohol intake.
Reaction of Alkoson-alkogol
Symptoms: an enanthesis, heartbeat, a headache, short wind, nausea, vomiting, the increased perspiration, thirst, stethalgias and hallucinations. If, despite these symptoms to continue treatment, there can be complications in the form of cardiovascular collapse, arrhythmias, a myocardial infarction, an acute heart failure and, in hard cases, a lethal outcome.
Treatment: oxygen or mix of 95% of oxygen and 5% of carbon dioxide, intravenously vitamin C (1 g) and ephedrine sulfate are appointed. Symptomatic treatment.
At heavy reaction (a severe headache with feeling of a raspiraniye and pulsation, sharp difficulty of breath, a considerable lowering of arterial pressure, black-outs, psychomotor excitement, spasms) lasting 1 1/2 h 15-20 ml of 1% of aqueous solution methylene blue intravenously enter, glucose solution with ascorbic acid, under skin – Cordiaminum, Corazolum or camphor, intramusculary – Cytitonum or lobeline, ephedrine, strychnine, make oxygen inhalation. In heartaches apply validol, Corvalol and if it is necessary, nitroglycerine. At low arterial blood pressure enter a phenylephine hydrochloride or ephedrine. In case of sharp oppression of warm activity enter intravenously 0.25 – 0.5 ml of 0.05% of solution of strophanthin into 20 ml of isotonic solution of sodium of chloride or 5% of solution of glucose, in spasms – intramusculary 10 ml of 25% of solution of magnesium of sulfate. In severe nausea and vomiting enter intravenously 10 ml of 10% of solution of Calcii chloridum or a gluconate, give in 0.015 g of extract of a belladonna, under skin enter 0.5 ml of 0.1% of solution of atropine.
In case of convulsive reactions enter Chlorali hydras (15 – 20 ml of 6% of water and starched solution) in the form of an enema or apply tranquilizers, at psychomotor excitement enter intramusculary 1-2 ml of 2.5% of solution of aminazine.
At the beginning and during treatment, the level of transaminases in blood serum and the developed blood test has to be determined each 6 months.
It is necessary to apply with care at patients with a renal failure, diseases of a liver and kidneys, diabetes and epilepsy.
Use in pediatric practice
Safety and efficiency of use for children was not established.
Pregnancy and a lactation
Safety of use of this drug for pregnant women is not established. Therefore Disulfiramum has to be applied according to the decision of the doctor only if the expected advantage exceeds possible risk.
It is unknown whether this drug with breast milk is emitted. Therefore Disulfiramum should not be applied by nursing mothers.
The feature of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms
of Patients should inform on the danger connected with control of automobiles, service of the mechanical equipment and other potentially dangerous types of activity.
Symptoms: coma, collapse, various neurologic phenomena.
Form of release and packing
of the Tablet of 500 mg. On 14 or 25 tablets in a polyethylene bottle together with the instruction for use.
To Store storage conditions at a temperature not above 25 °C, in the dry, protected from light place.
To store out of children’s reach!
Not to apply an expiration date of 5 years after an expiration date.
According to the prescription
Republic of Kazakhstan JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Producer
Almaty, Shevchenko St. 162 E.