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Pharmacological properties
Pharmacodynamics. disulfiram inhibits the action of many enzymes. inhibition of acetaldehyde dehydrogenase leads to an increase in the concentration of acetaldehyde, a metabolite of ethyl alcohol, which causes unpleasant symptoms: intense facial flushing, nausea, vomiting, discomfort, tachycardia and hypotension.
Pharmacokinetics. When taken orally, disulfiram is rapidly but not completely absorbed (70-90%). It is rapidly metabolized: it turns into diethyldithiocarbamate, which is then excreted in the form of a glucuronide or transformed into diethylamine and carbon disulfide. Part of the carbon disulfide is excreted by the lungs. The remainder is metabolized and excreted in the urine.
Indications
Adjuvant therapy to prevent relapse of alcohol dependence.
Application
The preparation is intended for oral use. It is recommended that adults take 1 tablet per day. the tablet should be washed down with water (1/2 cup), taken in the morning during breakfast, after refraining from drinking alcohol for at least 24 hours. The duration of the course of treatment is determined by the doctor individually.
Contraindications
Hypersensitivity to disulfiram or any of the components of the preparation. severe liver failure. kidney failure. severe respiratory failure. diabetes. neuropsychiatric disorders. cardiovascular diseases. use of alcoholic beverages or medicines containing alcohol during the last 24 hours of pregnancy and lactation.
Side effects
Side effects caused directly by disulfiram
From the digestive tract: nausea, vomiting, stomach pain, diarrhea, metallic taste in the mouth, bad breath (halitosis), bad breath in patients with colostomy.
From the side of the liver: an increase in the level of transaminases is often observed; rarely - hepatitis, including fulminant and fatal forms of hepatitis.
From the side of the central nervous system: polyneuritis of the lower extremities, optic neuritis.
Neuropsychiatric disorders: memory loss, confusion, drowsiness and fatigue at the beginning of treatment, headache.
From the skin: allergic rashes on the skin, cross-sensitivity to rubber is possible.
Side effects associated with the disulfiram-ethyl alcohol combination are intense flushing of the face, erythema, nausea and vomiting, malaise, tachycardia, and hypotension.
In some cases: cardiac arrhythmia, angina attack, cardiovascular insufficiency, myocardial infarction, respiratory depression and neurological symptoms (confusion, encephalopathy and epileptic seizures or convulsions), sudden death.
special instructions
The preparation Esperal can be prescribed only after a comprehensive medical examination (including laboratory testing).
Liver function tests, including determination of serum transaminase levels, should be performed prior to disulfiram treatment (see CONTRAINDICATIONS section), and then these functional tests should be performed at regular intervals, especially during the first 3 months of treatment. An increase in the level of transaminases in the blood serum, three times the upper limit of normal, requires immediate discontinuation of treatment without subsequent recovery. Patients should be closely monitored until normal liver function tests are established.
The preparation should be used with caution in patients with nickel dermatitis due to an increased risk of hepatitis.
The preparation should never be administered to patients without their knowledge.
Because there are reports of very rare cases of fulminant hepatitis, therefore, in the event of signs of precursors (asthenia, anorexia, nausea, vomiting, abdominal pain or jaundice), the patient should immediately undergo a medical examination of the patient and determine the laboratory parameters of liver function tests (see. SIDE EFFECTS).
The patient should be informed about the risk of developing a disulfiram reaction in case of simultaneous use of the preparation and alcoholic beverages, even in small quantities. Patients should be warned about the alcohol content of certain medicines (especially oral solutions), foods, and certain cosmetic products such as aftershave and eau de toilette or cologne.
Unpleasant symptoms (intense flush on the face, erythema, nausea and vomiting, malaise, tachycardia and hypotension) develop within 10 minutes after drinking alcohol and last from 30 minutes to several hours.
Reactions caused by the use of alcohol may occur within 2 weeks after discontinuation of preparation treatment. There are reports of more severe reactions: cardiac arrhythmias, angina attacks, cardiovascular failure, myocardial infarction, sudden death, respiratory depression and neurological symptoms (confusion, encephalopathy and epileptic seizures or convulsions).
During pregnancy and breastfeeding. Animal studies have shown Esperal to be teratogenic. The teratogenic effect of the preparation is enhanced by alcohol, which by its nature is already teratogenic and fetotoxic in chronic use in large quantities.
There is insufficient information to assess the potential teratogenic and fetotoxic effects of the preparation if administered during pregnancy. Among a limited number of patients who took the preparation during pregnancy, the manifestation of side effects was mainly observed in the case of simultaneous use of the preparation with alcohol. Therefore, the use of the preparation during pregnancy is not recommended. However, this is not a basis for recommending termination of pregnancy in women taking disulfiram, but rather requires caution in the use and specific antenatal monitoring of fetal development.
It is not recommended to use the preparation during breastfeeding.
Influence on the ability to drive a car and perform work requiring increased attention. The patient must be warned that drowsiness may occur while taking the preparation, so it is not recommended to drive a car and perform work that requires increased attention.
Interactions
Not recommended combinations
Alcohol: the development of a disulfiram reaction (flushing, redness, vomiting and tachycardia). Alcoholic beverages or medicines containing alcohol should be avoided.
Isoniazid: violation of behavior and coordination of movements.
Preparations of the 5-nitroimidazole group (metronidazole, ordinazole, secnidazole, tinidazole): Bouffées délirantes (a type of short reactive psychosis), confusion.
Phenytoin: a significant and rapid increase in the level of phenytoin in the blood plasma with toxic manifestations (due to inhibition of its metabolism).
Combinations requiring caution when used together
Warfarin (with extrapolation to other oral anticoagulants): increased effect of oral anticoagulants and risk of bleeding (decreased liver metabolism).
Tricyclic antidepressants: may increase the reaction of alcohol intolerance.
Overdose
An overdose of disulfiram alone can cause neurological effects: extrapyramidal syndrome, disorders of consciousness (coma, confusion and encephalopathy). symptomatic treatment.
As a result of an overdose of the disulfiram-ethanol combination, coma or confusion syndrome, cardiovascular failure, sometimes with neurological complications, may occur. Treatment is symptomatic.
Storage conditions
Store in a dry place at room temperature no higher than 25°C.
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