Disulfiram

Disulfiram (sometimes also called tetrabenzylthiouram disulfide) is a drug that is used to treat chronic alcohol dependence. It works by blocking the enzyme acetaldehyde dehydrogenase, which causes acetaldehyde to build up in the body, which in turn causes unpleasant physical reactions when even small amounts of alcohol are consumed. It creates an aversion to alcohol and can help people with alcohol dependence to stop drinking.

The use of disulfiram should be carried out only under the supervision of a doctor, as it can cause serious side effects and has a number of contraindications. This is necessary to prevent possible complications and undesirable interactions with other drugs.

It is important to note that disulfiram does not treat alcohol dependence itself, but only helps to control alcohol consumption by creating an aversion to it. Along with the drug, psychological and medication treatment is usually also provided for full recovery.

Indications Disulfiram

1. Treatment chronic alcohol dependence: Disulfiram can be prescribed to help people with alcohol dependence stop drinking alcohol. It creates an aversion to alcohol by causing unpleasant physical reactions when drinking it.
2. Relapse prevention: After successful cessation of alcohol consumption, disulfiram can be used to prevent relapse and maintain abstinence from alcohol.

It is important to note that disulfiram should be used only as part of a comprehensive treatment of alcohol dependence, which may include psychological support, medication and other methods. The use of disulfiram should be carried out under the supervision of a doctor, as the drug can cause serious side effects and has a number of contraindications.

Release form

Disulfiram is usually supplied as tablets to be taken orally (by mouth). The tablets may have different dosages, depending on the prescription and your doctor's instructions.

Pharmacodynamics

Its pharmacodynamics are related to its ability to block the activity of the enzyme acetaldehyde dehydrogenase (ALDH), which normally breaks down acetaldehyde, an intermediate product of ethyl alcohol (alcohol) metabolism, into more harmless compounds.

When a person consumes alcohol along with disulfiram, the resulting acetaldehyde accumulates in the body, causing a number of unpleasant symptoms such as nausea, vomiting, dizziness, headache, and even palpitations. These symptoms, known as the disulfiram-ethanol reaction (disulfiram-ethanol reaction), serve as a negative reinforcer that should help the patient associate drinking alcohol with negative consequences and, therefore, quit drinking.

Thus, disulfiram acts as an additional support in the treatment of alcohol dependence, helping the patient to restrain from drinking alcohol because of the unpleasant symptoms that arise.

Pharmacokinetics

1. Absorption: Disulfiram is rapidly and completely absorbed from the gastrointestinal tract after oral administration.
2. Metabolism: The main metabolite of disulfiram is diethyldithiocarbamate (DDC), which is formed in the liver. Metabolism occurs mainly by oxidation and hydrolysis.
3. Excretion: Disulfiram and its metabolites are excreted mainly through the kidneys. About 20% of the dose is excreted through the intestine. The elimination half-life is about 60-120 hours.
4. Concentration: Stable blood concentrations of disulfiram are usually reached 1-4 hours after administration.
5. Pharmacodynamics: Disulfiram acts as an inhibitor of acetaldehyde dehydrogenase, an enzyme involved in the metabolism of ethyl alcohol. This leads to impaired acetaldehyde metabolism, which causes unpleasant symptoms such as nausea, vomiting, dizziness, and rapid heartbeat when a person consumes alcohol. This creates an additional motivation to abstain from drinking alcohol.
6. Duration of action: The effects of disulfiram may last up to several weeks after discontinuation due to the long time that its metabolites remain in the body.
7. Interactions with other drugs: Disulfiram may interact with a variety of medications, including alcohol, leading to various undesirable effects or decreased efficacy of other medications. Therefore, it is important to carefully evaluate interactions with other drugs when prescribing disulfiram.

Dosing and administration

Disulfiram is usually taken in the form of tablets, which are taken orally. The dosage and dosage regimen may vary depending on the doctor's recommendations, individual patient characteristics, and treatment goals. However, the following is usually recommended:

1. Initial dose: Usually start with a small dose, such as 250 mg once daily.
2. MaintenanceDose: After the initial period, a maintenance dose of between 125-500 mg per day is usually recommended, depending on individual needs and body response.
3. Course length: The course length may also vary depending on the doctor's recommendations. Usually, a course of disulfiram can last several months or even longer to help treat alcohol dependence.
4. Follow yourdoctor's recommendations: It is important to follow your doctor's recommendations regarding dosage and regimen, and not to change the dosage or stop taking it without consulting your doctor.

Use Disulfiram during pregnancy

Disulfiram can pass through the placenta and harm the developing fetus. This can lead to various health problems in the newborn, such as congenital abnormalities, underdevelopment and nervous system problems.

If a woman takes disulfiram and then discovers that she is pregnant, it is important to consult a doctor immediately. The doctor can suggest a plan of action to minimize the risk to the baby, possibly replacing disulfiram with an alcohol treatment method that is safe for pregnancy.

Contraindications

1. Alcohol intoxication: Disulfiram should not be taken in the presence of alcohol in the body. The use of disulfiram in this case may cause serious side effects.
2. Pregnancy and breastfeeding: Disulfiram is contraindicated in pregnancy and during breastfeeding due to potential effects on fetal development and risk of drug transmission through breast milk.
3. Serious liver disease: In patients with severe liver disease, disulfiram may be contraindicated due to the risk of liver failure and other complications.
4. Cardiovascular disease: Disulfiram may exacerbate cardiovascular problems, so its use may be undesirable in patients with serious heart and vascular disease.
5. Epilepsy and convulsions: Patients with epilepsy or prone to convulsions should avoid disulfiram because of the risk of seizures.
6. Allergic reaction: If the patient has an allergic reaction to disulfiram or other drugs similar to it, use of the drug is contraindicated.
7. Hypersensitivity to the drug: People with hypersensitivity to disulfiram should avoid its use.

Side effects Disulfiram

1. Allergy reactions: Include hives, itching, swelling of the face, lips, tongue or throat, difficulty breathing.
2. Skin reactions: Possible rash, redness, flaking or other skin changes.
3. Nervous system: Dizziness, headache, drowsiness, nervousness or insomnia may occur.
4. Digestive system: There may be stomach upset, nausea, vomiting, change in taste.
5. Muscle and joint pain: In some cases, muscle or joint pain may occur.
6. Mental effects: Depression, anxiety, mood changes may occur.
7. Alcohol side effects: When disulfiram is used in combination with alcohol, it can cause the so-called "Antabuse effect", which manifests as nausea, vomiting, reddening of the skin, rapid heartbeat, arrhythmias and even loss of consciousness.

Overdose

1. Increased side effects: Overdose may lead to increased unwanted effects associated with disulfiram use, such as nausea, vomiting, dizziness, loss of consciousness, palpitations and others.
2. Serious Complications: In the case of a serious overdose, more serious complications such as heart arrhythmias, seizures, coma, and even death may develop.
3. Medical intervention: If an overdose of disulfiram is suspected, medical attention should be sought immediately. Treatment of overdose usually includes maintenance of vital functions, active elimination of the drug from the body, and symptomatic treatment of unwanted effects.
4. Avoiding overdose: To prevent overdose, it is necessary to strictly follow the doctor's recommendations regarding the dosage and regimen of the drug. It is also important to avoid alcohol consumption during treatment with disulfiram, as it may increase the risk of overdose.

Interactions with other drugs

1. Alcohol-containing drugs: Using disulfiram at the same time with drugs or products containing alcohol can cause severe reactions such as low blood pressure, nausea, vomiting, pulse, rapid heart rate, and even serious complications such as intoxication.
2. Drugs for the treatment of heart disease: Some drugs for the treatment of heart disease, such as nitroglycerin and drugs containing nitrates, may increase the undesirable effects of disulfiram.
3. Drugs used to treat neurological diseases: Disulfiram may interact with drugs used to treat neurological diseases, such as metronidazole, causing serious undesirable effects, including vomiting, nausea, dizziness, as well as increasing the risk of toxic effects on the central nervous system.
4. Medications for depression and other psychiatric disorders: Using disulfiram concurrently with certain antidepressants such as serotonin reuptake inhibitors (SSRIs) may increase unwanted effects such as agitation, insomnia, and anxiety.
5. Drugs for the treatment of bacterial infections: Disulfiram may interact with antibiotics such as ceftriaxone, which can lead to serious adverse effects, including life-threatening reactions.

Storage conditions

The following recommendations should be followed for proper storage of disulfiram:

1. Store the drug in the original package or container to avoid damage and contact with moisture.
2. Store disulfiram in a dry place protected from direct sunlight and moisture, as humidity may adversely affect the stability of the drug.
3. The recommended storage temperature for disulfiram is usually between 15 and 30 degrees Celsius. Do not allow the drug to freeze or overheat.
4. Keep disulfiram out of the reach of children to avoid accidental use.
5. It is important to follow the instructions on the package or your doctor's recommendations regarding expiration dates and storage conditions for a particular drug.