In the complex treatment of alcohol dependence, foreign drugs are often used, one of which is Acamprosat. This tool is unique and has no exact analogues.
Acamprosat
Alcoholism is a drug addiction, it is very difficult to get rid of it yourself, because one of the main provoking factors is a hereditary predisposition. It is necessary to have complex treatment, in which the patient is prescribed medications.
Acamprosat has long been used in Europe and America. It is an innovative drug that reduces dependence on alcohol. According to some studies, the drug reduces the risk of recurrence by 80%.The action of Acamprosate is based on calcium acetylgomotaurinate. It restores the disturbed balance of chemicals and the functional activity of biochemical receptors.
In Russia Acamprosat has not yet passed the state registration. It is usually ordered in foreign pharmacies, where the price of the
package of the drug is an average of 145 euros. The drug is produced by German company Merck Serono.
Composition
One tablet of Acamprosate contains 0.333 g of active substance calcium acetylgomotaurinate, as well as auxiliary components:
- crospovidone;
- microcrystalline cellulose;
- magnesium stearate;
- carboxymethyl starch;
- colloidal anhydrous silica;
- magnesium silicate;
- propylene glycol;
- talcum powder;
- dye Eudragit ® L 30.
Dosage forms
Produced by Acamprosate in the form of solid tablets for oral administration. Their color varies from cream to white.
The biconvex tablets are covered with a smooth coating, the inscription "333" is printed on one side. They are packed in plastic blisters of 12 pieces each. One package contains 7 blisters.
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Pharmacological action
Long-term abuse of alcoholic beverages has a negative effect on brain structures, especially on the neurotransmitter system. The same happens as a result of a sharp cessation of the intake of ethyl alcohol in the body.
As a result of regular intake of the drug, dependence on alcohol decreases, a person begins to drink much less. In general, the pharmacological action of Acamprosate is not fully understood, but there are research data in which one group of volunteers was given a drug, the other a dummy. Those who took this medicine, increased the duration of abstinence from alcohol.
Researchers suggest that calcium acetylgomotaurinate in the composition of Acamprosate modulates the functional activity of a number of neurotransmitter systems.
According to the test results of the drug, the following positive effects are achieved as a result of its administration:
- Suppression of excessive production of neurotransmitters.
- Normalization of the CNS.
- Neuroprotective action.
- Neutralization of free radicals.
Pharmacodynamics
Calcium acetylgomotaurinate slows down neurotransmission due to its structural similarity to the endogenous neurotransmitter GABA.It is assumed that Ca 2+ in the drug suppresses the activity of L-glutamate, the main neurotransmitter responsible for excitation.
The neuroprotective effect of Acamprosate is achieved through exposure to calcium channels, which activates some enzymes, among them:
- phospholipase;
- endonuclease;
- protease.
As a result, neurons are protected from the effects of ethanol toxins. Dependence on alcohol gradually decreases.
Researchers have reason to believe that Acamprosat counteracts glutamatergic neurotransmission, which causes the development of chemical dependence on alcohol. Also, as a result of the tests, it was established that the medicine is a relatively safe and effective means of preventing relapses due to modulation of the central neurotransmission.
The pharmacokinetics of the drug. Absorption of Acamprosate from the digestive tract occurs within 4 hours. Provided a daily intake in a week, a stable concentration of the drug is achieved. Acamprosate overcomes the hemato-encephalic barrier, because it weakly binds to blood proteins. The half-life of the drug from the body of a healthy person is 13 hours. The agent is not practically metabolized, most of it is excreted by the kidneys.
The effect of other drugs on the pharmacokinetics of Acamprosate is poorly expressed, so it can theoretically be taken simultaneously with antidepressants and disulfiram-based drugs. According to a study by scientists at the University of Lausanne, the combination with esperal even increases the effect of the drug.
Pharmacokinetic patterns of Acamprosate practically do not change in the presence of moderate disorders of kidney and liver functions. The drug is well tolerated by patients, and its long reception does not lead to the formation of dependence.
Acamprosate does not take its biotransformation in the kidneys, as the manufacturer claims. Bioavailability of the drug is about 11%.
Indications
The main indication for Acamprosate is chronic alcoholism. The drug is prescribed to the patient after taking it out of drinking-bout and carrying out detoxification of the body.
During treatment, you can not drink alcohol, otherwise the therapeutic effect will be significantly reduced. If the patient has withdrawal symptoms, then before receiving Acamprosate they must be quenched.
Instruction for use
The optimal duration of treatment with Acamprosate is 1 year. The minimum course duration is 15 days.
The dosage of the drug is chosen by the doctor, based on the clinical case and body weight of the patient.
Patients who weigh less than 60 kg are advised to take Acamprosate as follows:
- 2 tablets in the morning;
- 1 - during the day;
- 1 - before going to bed.
Patients weighing more than 60 kg.shows increased dosage of the drug:
- 2 tablets in the morning;
- 2 - in the afternoon;
- 2 - at night.
Acamprosate should be taken during meals or immediately after meals. Tablets should be washed down with plenty of clean water.
Contraindications
Contraindications to the appointment of Acamprosat are as follows:
- Age from 65 years.
- Pregnancy and lactation.
- Hypersensitivity to components.
- State of alcohol withdrawal.
- Severe liver pathology.
- Diseases of excretory system and kidneys.
Side effects of
Preclinical trials revealed side effects of Acamprosate, directly related to excessive intake of calcium:
- diarrhea;
- lesions of the kidneys and heart;
- calcification of soft tissues.
Also reported on possible violations of the CNS, among which:
- severe fatigue;
- headache;
- dizziness;
- neuroses;
- depression;
- is syncope.
Among the possible side effects also give rise to noise in the ears, temporary deterioration of hearing. Possible skin rashes, itching, swelling of the larynx.
Some patients complain of a disorder of the respiratory system, among which are:
- cough;
- shortness of breath;
- rhinitis;
- bronchitis;
- epistaxis;
- pharyngitis;
- asthma attacks.
As a result of taking Acamprosate, the urogenital system can fail, which is expressed in:
- a decrease in libido;
- edema;
- changes in diuresis;
- lowering sexual possibilities.
In addition, there may be abnormalities in the work of the gastrointestinal tract:
- deterioration of appetite;
- nausea with vomiting;
- abdominal pain;
- flatulence;
- dry mouth.
Sometimes Acamprosate administration provokes endocrine disorders, which cause:
- increased thirst;
- change in body weight;
- reduced glucose tolerance;
- hypothyroidism.
Reviews
Doctors are generally positive about the drug Acamprosat, indicating its effectiveness in the treatment of alcohol dependence. Doctors lead the results of studies that show that 60% of patients after regular intake of the drug significantly reduced the consumption of alcohol. In this case, only 20% of patients who received placebo, began to drink less.
Alcoholics as a plus of the drug indicate that Acamprosate does not cause disulfiram-like reactions, so the craving for alcohol decreases naturally. Alcohol does not cause disgust, but the need for it gradually disappears.
However, many are not satisfied with the rather high price of these pills, as well as the fact that they have to be ordered via the Internet in foreign pharmacies. Therefore, in general, Acamprosat is not very popular.
Analogues of
There are no exact analogues for Acamprosat. This is the only drug whose action is based on calcium acetylgomotaurinate, but it can be purchased only through the Internet with delivery from abroad.
However, it is possible to identify a number of available medicines that have anticorrosion activity.
These include:
- Bromocriptine.
- Tiapride.
- Gamma-hydroxybutyrate.
- Naltrexone.
- Buspirone.
- Ritanserin and Ondansetron.
- Prozac.
All these drugs in different combinations can be used as part of a complex therapy for chronic alcoholism. They reduce cravings for alcohol and prevent relapse.
So, Bromocriptine was originally designed to treat Parkinson's disease. However, studies show that this drug, being a dopamine agonist, reduces the number of episodes of alcoholism.
Tiapride is an atypical antipsychotic. It affects the dopamine receptors that are sensitized to dopamine. Experiments in mice show that as a result of taking the drug, the severity of the withdrawal syndrome decreases.
Gamma-hydroxybutyrate is similar in mechanism of action with Acamprosate, this drug reduces the frequency of drinking alcohol. However, it shows low effectiveness in the treatment of patients with a hereditary predisposition to alcoholism.
Naltrexone is a popular drug for the treatment of addiction to stimulants. It blocks receptors that allow you to enjoy alcohol. As a result, craving for alcohol is reduced.
Buspirone restores serotonin function. As a result, the alco-addict reduces anxiety and normalizes nervous activity.
Ritanserin and Ondansetron modulate the impulse activity of noradrenergic neurons. According to the results of the studies, these drugs show efficacy in the treatment of alcoholic psychoses.
Prozac simultaneously removes depression and has a stimulating effect. However, it is banned in many countries due to the large number of side effects.
As a result of taking Acamprosate, the urogenital system can fail, which is expressed in:
However, it is possible to identify a number of available medicines that have anticorrosion activity.
Tiapride is an atypical antipsychotic. It affects the dopamine receptors that are sensitized to dopamine. Experiments in mice show that as a result of taking the drug, the severity of the withdrawal syndrome decreases.
Prozac simultaneously removes depression and has a stimulating effect. However, it is banned in many countries due to the large number of side effects.