Zyban is an atypical antidepressant used to treat disorders of the emotional-volitional sphere. Another point of application for Zyban is the treatment of nicotine addiction. Thanks to a special mechanism of action on the central nervous system, the drug makes it easier to quit smoking.
pharmachologic effect
The pharmacological action of zyban is due to the effect of bupropion on the body. Bupropion is not a homogeneous substance in its composition. In the body, it breaks down into several metabolites, each of which has its own effect on the cells of the central nervous system.
Bupropion is a selective norepinephrine and dopamine reuptake inhibitor. This means that the drug prevents the entry of the listed mediators from the synaptic cleft into the neurons. At the same time, the concentration of these substances increases and they more often bind to neuron receptors, which are also located in the synaptic cleft. The more dopamine and norepinephrine affect the receptors, the better the patient feels.
The development of depression is associated with a decrease in serotonin, norepinephrine and dopamine in the brain. Bupropion increases the concentration of the last two mediators, which helps improve mood. However, these are not all the effects of the drug.
By acting on dopamine receptors, bupropion reduces hunger and helps combat obesity more effectively. In addition, the substance helps cope with nicotine addiction. Bupropion is able to bind to nicotine receptors, thereby deceiving the brain and helping to quit smoking tobacco.
Zyban: composition, release forms, methods and duration of use.
Zyban has been produced in England for more than 20 years and has proven itself as an antidepressant in the fight against smoking. The medicine is supplied to Russia by an Austrian company, a subsidiary of the English manufacturer.
It is over-the-counter, but due to the mechanism of action, it requires mandatory consultation with a narcologist, since there is a risk of getting rid of the craving for nicotine, but becoming dependent on an antidepressant.
Zyban is a generic drug, that is, it is not produced under a patented name; it has many synonyms in different countries. The drug comes to us in the form of round tablets in a cachet, which prolong the effect of its active substances in the body. The “GS5FV” imprint is clearly visible on each one.
The tablets are packaged in special polyethylene bottles with a moisture absorber, 7, 30, 90 pieces each.
Indications
Many studies have been conducted to determine the effectiveness of Zyban in the treatment of a particular pathological condition. As a result, diseases for which it is advisable to prescribe this drug were identified. These diseases include:
- First episode of mild to moderate depression;
- Recurrent depressive disorder;
- Bipolar affective disorder, current episode of depression;
- Nicotine addiction;
- Obesity;
- Decreased libido, including those caused by other antidepressants;
- Attention deficit hyperactivity disorder in adults.
Zyban has not been proven effective for other mental disorders. For example, a study conducted on reducing anxiety showed that Zyban does not have an anti-anxiety component. However, in some cases it can be used for social phobias.
Indications, side effects, drug interactions, doses
Zyban is used for the purpose of:
- Complex therapy and prevention of depressive conditions.
- Social phobias.
- Nicotine addiction.
- Sexual dysfunction of depressive origin.
- Obesity.
- Seasonal affects.
- Lack of concentration and attention.
It is this polyetiological nature of the prescription that explains many of the side effects of the drug:
- Irritability.
- Apathy.
- Symptoms of intoxication.
- Dyspepsia.
- Migraine.
- Fainting.
- Cachexia.
- Sweating.
- Convulsive, epileptic syndrome.
- Hives.
- Insomnia.
- Tides.
- Asthenia.
- Quincke's edema.
- Asthmoid bronchospasm.
- Memory losses.
- Dysuria.
- Loss of coordination.
- Depersonalization.
Drug compatibility
The human body has a special gene, CYP2D6, which is a metalloprotein and is responsible for the metabolism of 25% of all known drugs, including antidepressants.
If you take medications together with Zyban that also require participation in the utilization of this gene, the patient will develop slow metabolism syndrome. This will significantly slow down the clearance of drugs and lead to an inadequate response to the administered dose of medication. Therefore, the following are not prescribed simultaneously with Zyban: Clopidogrel, Orphenadrine, Cyclofosamide and many other drugs of these groups.
Zyban blocks the CYP2D6 gene isoenzyme, and therefore it is not combined with beta blockers, selective serotonin reuptake inhibitors (SSRI group), antiarrhythmic and antipsychotic drugs, cytochrome inhibitors (Ritonavir, Phenytoin, Phenobarbital).
Particular caution should be exercised when combining Zyban with drugs against Parkinson's disease (Levodopa, Amantadine), as there is a possibility of developing psychoneurotic conditions.
Bupropion cannot be combined with Nicorette drugs for transdermal delivery of nicotine into the body, as it provokes an increase in blood pressure.
If before the course of Zyban the patient was treated with antibiotics or tranquilizers, the light period should be at least two weeks. During this time, previously taken medications will be completely eliminated from the body naturally.
Dosage
Zyban is taken once a day, in the morning, 1 tablet (150 mg), daily maximum 300 mg. In rare cases, if a double dose of the drug is unsuccessful, increase the dose to 450 mg.
The course of treatment is more effective with long-term (more than a year) use of the medicine.
At the initial stage of renal and liver failure, the drug is taken with caution, increasing the interval between doses.
Overdose
More than 600 mg per day is considered an overdose, which gives a pronounced clinical picture: arrhythmia and rapid heartbeat, desire to sleep, high blood pressure, nausea, allergic rashes, epileptic seizures, lethargy, apathy, delirium, visions, coma.
These are serious events that should be avoided as there is no antidote for Zyban. Use detoxification.
An overdose may occur on the third day after taking the drug. In the hospital, the state of the brain is monitored using encephalography. Death occurs rarely, more often from complications: acidosis, hypoxia, cardiac arrest.
This happens when an overdose of a drug to relieve an epileptic attack occurs.
Contraindications
Zyban should not be prescribed for the following conditions:
- Epilepsy;
- Nervous tics, including Tourette's syndrome;
- Benzodiazepine tranquilizer withdrawal syndrome;
- Eating disorders;
- Oncological diseases of the brain;
- Arterial hypertension of the third degree;
- Renal or liver failure in the stage of decompensation;
- Childhood and adolescence.
In addition, taking Zyban with monoamine oxidase inhibitors is prohibited. There should be a gap of two weeks between taking these medications.
Practical application experience
Review by a doctor and reviews of ordinary people about the drug Bupropion.
Bupropion is a slow-acting antidepressant. The medication helps normalize the mental state, relieves mental disorders, depression, panic attacks, and also helps with nicotine addiction.
It is worth considering that the medicine has a delayed effect, so it takes a long time to get results; usually it needs to be taken for 1 year. Side effects appear in the first two weeks, then everything disappears.
Psychiatrist
I liked Zyban because it does not have a quick effect, thereby not causing a depressive state, which I often experience when taking antidepressant medications. I took it to eliminate panic attacks and social phobia.
A psychiatrist prescribed it to me. After a year of taking it, I felt much better, although at first there were side effects in the form of headache, nausea and abdominal pain, but after 2 weeks everything went away.
Svetlana, 45 years old
I have long wanted to quit smoking, but could not do it on my own. I decided to go to the doctor to consult. I was prescribed to take the drug Bupropion, it helps with nicotine addiction. I took it for a year, but of course the effect was not immediate. But at the moment I haven’t smoked for six months, I think I won’t smoke again.
Egor, 38 years old
Side effects
Side effects of Zyban mainly affect the nervous system. The most common of these are epileptic seizures, tics and hand tremors. The drug is especially dangerous for patients who already have seizures or other neurological disorders.
Another common complication is headache, dizziness, and nausea. These symptoms develop in the first days of use and soon disappear. Approximately 1% of those taking the drug may develop arterial hypertension, most often its isolated systolic variant. It does not matter whether the patient had this disease before taking it or not.
A rare side effect of Zyban is galactorrhea, which is the secretion of milk from the mammary glands outside of pregnancy or lactation. Another rare complication of treatment with this drug is toxic liver damage.
With long-term use of Zyban and sudden cessation of treatment, withdrawal syndrome is possible. Other side effects are currently unknown; post-marketing studies of the drug are currently underway to expand this list.
Pharmacological profile
The drug has an antidepressant effect. The active element of the drug is selectively captured using dopamine transport.
The main effect of the drug is observed during norepinephrine reuptake inhibition.
Bupropion Formula
Medicines containing the active component bupropion are classified as antagonists of nicotinic acetylcholine receptors. The medication has a reducing effect on the convulsive activity of the brain.
The level of bioavailability of the drug ranges from 5% to 20%. Depending on the method of application, this indicator is different; during injection into a vein it is high.
The main component of the drug has a high level of binding to blood plasma proteins, it can be almost 84%. The process of drug metabolism is observed in liver tissues together with the CYP2B6 and 2D6 systems. The half-life is approximately 20 hours. The main amount of the medication is excreted in the urine; about 10% is excreted in feces.
Instructions for use
Zyban is recommended to be used twice a day. The half-life of the drug is less than 24 hours, so it is fundamentally important to divide the daily dose into two doses 12 hours apart (see chart). Treatment should begin with a minimum dosage of 300 mg. To do this, just take one tablet in the morning and one in the evening.
Within two weeks, the dose can be increased to 450 mg per day. In this case, you can take two tablets in the morning and one in the evening, or two in the evening and one in the morning. You can also divide the tablet and take one and a half tablets in the morning and evening.
If necessary, after another two weeks the dosage can be increased again. The maximum permitted amount of the drug consumed per day is 600 mg. This level should not be exceeded due to the risk of side effects.
The drug can be taken regardless of meals. The tablets should be taken with a small amount of water.
The drug does not affect sleep and wakefulness. There are no restrictions on driving any type of transport. There is evidence of the development of dependence on Zyban and the occurrence of withdrawal syndrome when stopping its use. To eliminate the risk of developing this syndrome, you should stop drinking the drug gradually. You should start by reducing the dosage by 150 mg once every two weeks until you completely stop taking the drug.
Mechanism of action, instructions, contraindications
Zyban has medicinal properties, which is confirmed by numerous tests of the drug in the USA and the European Union. Its active substance affects precisely the process of development of cravings for smoking, affecting special centers of the brain responsible for pleasure.
Bupropion stimulates the production of dopamine, the happiness hormone, blocking its natural neutralization after quitting cigarettes. In this way, support for the smoker is achieved at the most difficult moment for him.
Recharge with Zyban reduces discomfort to a minimum, providing psychological stability.
In other words, treatment with the drug, not being nicotine-dependent therapy, does not help maintain the concentration of cigarette poison in the blood, but affects brain structures, simulating the level of pleasure characteristic of a smoked cigarette. Therefore, quitting smoking with Zyban is quite easy. This effect makes it the drug of choice for many experienced smokers.
Instructions
Self-administration of the drug is prohibited. It should be noted that injectable Cypriot antibiotics of the Ceftriaxone group are sold on the Russian market under the name Zyban, which can also be purchased in pharmacies without a prescription.
Therefore, before purchasing the drug, consultation with a specialist is mandatory.
There is no standard treatment regimen, but the basic rules of administration are specified in the instructions for use of the drug Zyban:
- Usually the drug is prescribed once a day, but in any case, the recommended interval between doses is 10 hours (minimum 8).
- Missing an appointment does not affect the selected treatment schedule.
- Doubling the dose is excluded, since it is fraught with the development of negative symptoms: shortness of breath, fainting, hyperhidrosis, visions, tachycardia, dyspepsia, loss of visual acuity, blurred contours of objects, irritability, dizziness.
- Swallow the tablet without chewing, wash it down with water both during and after meals, at any convenient time.
- The minimum course of treatment is 21 days.
Contraindications
Like any antidepressant, Zyban has strict limits. It is not prescribed for:
- Pregnancy and lactation.
- Mental disorders.
- Epileptic seizures and tendency to convulsions.
- Severe impairment of liver and kidney function.
- Allergies and individual intolerance to the components of the drug.
- Brain tumors.
- Lack of appetite with exhaustion and overeating.
- Combination with alcohol, drugs, and other medications due to a decrease in resistance to ethanol and a decrease in the convulsive threshold of the central nervous system.
- Somatic disorders: diabetes, hypertension, heart and vascular diseases.
- if the patient's age is under 18.
Reviews
Kirill N .: “I took Zyban while quitting smoking. At first I didn't notice the effect. I wanted to smoke just as much as before, even my irritability increased a little. But I only had to hold out for a week, then the effect of the drug appeared. This is usually the hardest time, but Zyban helped me overcome it with ease. I almost didn’t want to smoke, I finally quit.”
Psychiatrist : “The use of Zyban in our country is very limited. This is a new drug that has a different mechanism of action from other drugs. It has not yet been studied enough and its use raises some concerns for the health of patients. In addition, the cost of the drug does not allow it to be used to treat most patients. At the same time, American colleagues are successfully introducing Zyban into their practice, so we can soon expect its distribution on the domestic pharmaceutical market.”
Content
Instead of reviews
When they start smoking, they rarely think about the consequences. But sooner or later, every smoker begins to realize the seriousness of the problem, the danger of nicotine to the health of both himself and those closest to him. At this very moment the desire comes to say goodbye to the cigarette once and for all. But it's not easy. Narcologists believe that it is easier to give up alcohol with the help of coding and medications than to say a firm “no” to nicotine.
Many drugs have been created to help people quit smoking. Zyban is one of them, but according to experts and former smokers themselves, it is the most reliable and effective. It helps some people quit smoking right away. Some people do two or three courses of therapy. The effect is almost always achieved.
However, we must remember the dose and the fact that Zyban is addictive. Otherwise, having parted with one addiction, you can immediately get another.
Analogs
In case of intolerance to the substance, analogues of Zyban are prescribed. The most effective medications include the following:
- Prozac;
- Ludiomil;
- Trittico.
Prozac is a common medication that helps treat depression. It contains fluoxetine, which is the active ingredient. Prozac is produced in the form of capsules with a dosage of 20 mg.
Ludiomil is used to combat neuroses and stress. The composition contains the active component - maprotiline. It belongs to the tricyclic antidepressants. The medicine is released in tablet form.
Trittico is a medicine that helps fight depression. The active substance is trazodone. The activity of the drug manifests itself over a short period of time. Trittico helps cope with sleep disorders, increased anxiety, and fears. It is produced in the form of tablets.
Advantages and disadvantages of the drug
The key advantages of the substance include the following:
- High effectiveness in the fight against nicotine addiction.
- Reduced withdrawal symptoms.
- Reducing the risk of weight gain after quitting smoking.
- Short period of therapy.
- Low likelihood of adverse reactions.
Good results in eliminating addiction are achieved if the use of the substance was started a week before the expected cessation of cigarettes. This allows the body to smoothly adapt to the absence of nicotine. As a result, stress is reduced and withdrawal symptoms are alleviated.
The effectiveness of therapy is observed even among heavy smokers who consume 2 packs of cigarettes per day. The medicine acts on the brain and leads to the elimination of biochemical dependence.
The presence of additional components helps prevent sudden weight gain after quitting smoking, which is very important for women.
The drug is an antidepressant, eliminates mood swings, depression, and irritability. All these signs often accompany quitting smoking and cause noticeable psychological discomfort.
The disadvantages include the rather impressive price of Zyban. A package of 30 tablets will cost approximately $60-70. Another disadvantage is the likelihood of adverse reactions. Among them, it is worth highlighting headaches, stool disorders, dry mouth, excessive agitation, increased drowsiness, nausea and vomiting.
But these adverse reactions are extremely rare. The more important issue is the risk of addiction to Zyban. This sometimes happens when using antidepressants.
Another disadvantage of the drug is the threat of re-emergence of cravings for cigarettes after discontinuation of the substance. However, no medicine can provide a sustainable effect in the treatment of pathology.
Description and Instructions
Zyban is an antidepressant that is often marketed as a means to facilitate smoking cessation. It contains bupropion. This substance inhibits the reuptake of dopamine and norepinephrine. Serotonin uptake is reduced to a lesser extent. This drug does not affect the metabolism of MAO (the enzyme monoamine oxidase, which is responsible for the transformation of neurotransmitters). It is known that quitting smoking causes irritability and emotional instability in the majority of those who decide to overcome this bad habit. Zyban appears to be aimed at treating these conditions. This product is not registered in the Russian Federation and should not be distributed. Wellbutrin, which is the original version of the medicine, will soon appear in our pharmacies. The latter has been registered as an antidepressant. Interestingly, its instructions do not say anything about easing nicotine withdrawal.
Applicable for:
Relieving the condition of quitting smoking;
Zyban is available in the form of 150 mg tablets. They are taken twice a day (increasing the dose does not increase the effect). Treatment should be long-term - on average, about two months. Since the effect of the medicine develops gradually, it is started to be taken a week before a decisive cessation of smoking. The instructions for the drug Zyban suggest that a person should stop smoking on the 10th day of the course. It is then recommended to continue taking the medication for another six weeks. If during this period you were unable to completely give up your bad habit, you should not continue to drink Zyban.
Contraindicated for:
- Epilepsy, low seizure threshold, history of seizures;
- Alcohol withdrawal, abrupt withdrawal of psychotropic drugs, tranquilizers;
- Tumor processes of the central nervous system;
- Anorexia nervosa, bulimia;
- Concomitant use of MAO inhibitors;
- Bipolar disorder;
- Liver diseases;
- Pregnancy and lactation;
- Treatment of minors;
Side effects and overdose
Bupropion, the active ingredient in Zyban, can cause seizures. Therefore, the drug is not prescribed if there is a risk of their development. If the patient has no contraindications to the use of the medicine, he may nevertheless have complaints about:
- Insomnia (the second dose of Zyban should be taken 8 hours after the first, but preferably not before bedtime. For example, at 8 a.m. and 4 p.m.);
- Digestive disorders;
- Dry mouth.
Other side effects are possible. If you notice a change in your health while taking Zyban, be sure to discuss this with your doctor.
An overdose of the drug is dangerous, as it leads to disruptions in the functioning of the cardiovascular and nervous systems. The patient needs to be hospitalized.
Application diagram
The medicine can be taken only as prescribed by a doctor. The course of therapy consists of 2 stages. First, the patient must take 30 tablets, then 90. The first stage lasts approximately 2 weeks. The second course of treatment lasts about 6 weeks.
To avoid a break between courses of therapy, you need to buy 90 tablets in advance. This will give confidence in strict adherence to the treatment regimen.
If insomnia occurs during therapy, it is not recommended to take the medicine at night. People who take 2 tablets per day are recommended to take one of them early in the morning and the second in the afternoon. The interval between taking tablets should be 8 hours.
First stage
At this stage, the instructions for using Zyban recommend taking 30 tablets. This must be done within 2 weeks. You need to take the medicine in the dosage prescribed by your doctor. Typically, experts prescribe 1 tablet of 150 mg once a day for 3 days.
On the fourth day, the dosage is increased to 1 tablet 150 mg twice a day. The interval between taking the medicine is at least 8 hours. Before completing the first course of therapy, you need to get a prescription from your doctor for the next stage.
Second phase
This course of therapy will require 90 Zyban tablets. It lasts a little over 6 weeks. It is recommended to take the medicine as prescribed by a specialist. Usually doctors advise using 1 tablet twice a day. The interval between doses of the drug should be at least 8 hours.
It is strictly forbidden to increase the dosage of the medicine on your own. Be sure to follow your doctor's recommendations. The use of an excessive amount of the substance increases the risk of an epileptic attack - convulsions or paroxysms. If you have liver pathologies, you should consult your doctor about the possibility of using the drug.
During pregnancy and lactation
Medicine can only be prescribed by a doctor during pregnancy. This is due to the lack of data regarding the safety of the drug for child development.
All components of the substance penetrate into breast milk. Therefore, it is prohibited to use during lactation.
For children
Patients of childhood and adolescence are prohibited from using this medicine. This is due to the risk of suicidal thoughts. The medicine can only be taken by persons over 18 years of age.
Precautionary measures
Zyban tablets can cause increased drowsiness. During therapy, doctors do not recommend driving a car or working with complex machinery.
The medicine can increase blood pressure and cause the development of angle-closure glaucoma. Before you start taking Zyban, you need to have your eyes examined. If symptoms appear in the form of nausea, blurred vision, or swelling of the eyes, you should immediately consult a doctor.
In some people, taking the medication provokes behavioral disturbances, depression, and thoughts of suicide. The doctor must be notified of depression, schizophrenia, bipolar disorders and other mental disorders.
There are certain symptoms that you should immediately consult a doctor if they appear. These include the following:
- Depressive state, panic, increased anxiety;
- Suicidal thoughts or actions;
- Hallucinations;
- Mania;
- Aggression, anger;
- Increased anxiety;
- Any other behavioral disorders.
The simultaneous use of the drug with other medications may provoke an attack of epilepsy. Therefore, it is necessary to inform the doctor about all medications that you plan to take during the course of treatment.
