Zyban: instructions for use, analogues, composition, release forms

Smoking is a real problem of our time. Hundreds of millions of people around the world are addicted to nicotine. Quitting smoking is accompanied by a number of symptoms, which in terms of severity can be compared with withdrawal symptoms in an alcoholic when giving up alcohol. Of course, in the process of becoming addicted to nicotine, other receptors are involved, and the mechanism is also different, but the essence is the same. Reviews of Zyban report that this drug makes the process of quitting smoking easy. The medicine is also prescribed as an antidepressant and anti-anxiety agent.

Composition and release form

The active ingredient of the antidepressant is bupropion hydrochloride.
Tablets contain different concentrations of the active ingredient: 75, 100, 150, 300 mg.

They taste bitter, are white in color, and round in shape. There is a groove in the middle, which makes it easier to divide the dose in half.

The product dissolves well in water.

Zyban is produced in tablet form. The product has a prolonged effect. The tablets are round in shape and have a yellow or cream coating. They are placed in plastic bottles, which are packaged in cardboard packaging.

The active ingredient in Zyban is bupropion. Auxiliary ingredients include glyceryl tribehenate, alcohol, povidone, etc.

Briefly about the main thing

Bupropion is a substance that is included in such drugs as Zyban, Voxra, Budeprion, Wellbutrin. It refers to medications that represent a group of antidepressants that affect a person’s psychological addiction. Its use is indicated in the treatment of nicotine addiction.

The antidepressant effect helps reduce the discomfort that is caused by quitting smoking.

The country of origin of bupropion is the USA. It was patented in the 70s of the XX century. Initially, the drug was prescribed at a dosage of 400-600 mg per day. During the use of the drug, it was revealed that it increases the risk of developing epilepsy. Therefore, bupropion was banned.

Signs of an epileptic seizure

Later, experts discovered that the manifestation of side symptoms directly depends on the amount of the substance taken. At a dosage not exceeding 450 mg per day, the occurrence of seizures was not detected.

Effects of the drug "Zyban"

Anti-smoking tablets "Zyban", produced by the famous Austrian company GlaxoSmithKline, are one of the first drugs that do not contain nicotine. The main active ingredient of Zyban is bupropion, an antidepressant widely used abroad, which prevents the neutralization of a special chemical in the body - dopamine, otherwise called the “pleasure hormone”.

The mechanism is simple: during the painful experience of quitting, the smoker receives a kind of “crutch” that maintains him in a state of physiological oppression. Thanks to this supply, the concentration of dopamine increases, and the eternally unhappy quitter, deprived of his little joy, feels less psychological discomfort.

That is, treatment with Zyban is not nicotine replacement therapy aimed at maintaining the usual level of nicotine in the blood when quitting smoking (most other smoking cessation drugs operate on this principle). "Zyban" acts directly on the brain structures responsible for receiving pleasure. That is why Zyban is one of the most effective and popular tools to help you quit smoking.

That is, treatment with Zyban is not nicotine replacement therapy aimed at maintaining the usual level of nicotine in the blood when quitting smoking (most other smoking cessation drugs operate on this principle). "Zyban" acts directly on the brain structures responsible for receiving pleasure. That is why Zyban is one of the most effective and popular tools to help you quit smoking.

Purchasing medicine and its analogues

The substance is used as an antidepressant and, as part of complex therapy, helps get rid of nicotine addiction.

Zyban is the first nicotine-free drug intended for the treatment of tobacco dependence in patients over 18 years of age. In the USA, the drug was registered quite a long time ago - in 1997, and in the UK - in 2000.

The active component of the drug, bupropion, was invented by Nariman Mehta, an employee of the famous company GlaxoSmithKline. The substance appeared on the pharmaceutical market under the trade name Wellbutrin, which was prescribed to treat depression. But taking the drug often caused convulsions; it was later found out that such a complication directly depends on the dosage.

After correction of the treatment regimen and drug formula, a long-acting form of Wellbutrin was registered and recommended for use. But gradually the medication was replaced by a new generation of antidepressants - Zoloft, Prozac, etc.

Currently, bupropion is sold abroad under the trade name Zyban. The drug is prescribed to treat nicotine addiction.

Application and dosage

Taking Zyban begins a week before the expected date of quitting tobacco, which allows you to gradually prepare the body to get rid of nicotine addiction. First of all, the craving for smoking decreases. Thanks to the excipients, Zyban also inhibits the weight gain that occurs when quitting smoking - which worries many quitting women.

"Zyban" is able to treat tobacco addiction, including in people who smoke more than ten cigarettes per day, influencing certain brain structures that form a biochemical dependence on nicotine. Its effectiveness has been demonstrated in clinical studies involving 7,000 patients.

Almost a third of patients experience symptoms of a substance overdose. Such phenomena occur when more than 450 mg of the drug is consumed. In this case, the following symptoms occur:

Increased drowsiness;
Nausea;
Increased pressure;
Lethargy;
Epilepsy;
Sinus tachycardia.

In case of excessive use of the drug, maintenance therapy is carried out. Your doctor may prescribe barbiturates or benzodiazepines intravenously. Activated carbon is also prescribed.

If the daily norm is violated or the dosage is sharply increased, signs of overdose may appear.

They are expressed in drowsiness, changes in ECG data (arrhythmia, prolongation of the QRS complex, etc.).

To neutralize the activity of the active substance, it is recommended to urgently seek medical help.

A specific antidote for Bupropion is still unknown.

After hospitalization, ECG data and vital parameters are regularly monitored. Pulmonary ventilation and oxygenation are performed to ensure airway patency.

Sorbents are also prescribed to remove toxins from the body.

Taking Zyban begins a week before the expected date of quitting tobacco, which allows you to gradually prepare the body to get rid of nicotine addiction. First of all, the craving for smoking decreases. Thanks to the excipients, Zyban also inhibits the weight gain that occurs when quitting smoking - which worries many quitting women.

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.

Contraindications to taking the drug

But, like all antidepressants, Zyban is fraught with certain dangers. If you give up nicotine addiction, you may become addicted to the drug. Many who quit using Zyban noted that as soon as they stopped taking the medicine, the craving for smoking returned again. Another factor that makes it difficult to choose Zyban is its relatively high cost (although incomparable, of course, with the price of a healthy life), prescription (although any doctor will write a prescription without any problems) and most importantly, the lack of registration on the domestic market. pharmaceutical market. In Russia, it is only possible to buy a generic (analogue) of Zyban - bupropion.

The website has an article “Does Zyban pose a threat to the patient.” Highly recommended reading.

The website has an article “Does Zyban pose a threat to the patient.” Highly recommended reading.

Drug interactions

Reviews of Zyban report that the drug is usually well tolerated. Unlike the famous SSRI drugs, starting to take Zyban is almost never accompanied by disturbances such as tremor, insomnia, nausea and loss of appetite. all these symptoms are very smoothed out, or even completely absent.

In the world of psychiatry, there is debate as to whether it is advisable to prescribe Zyban tablets alone as an independent remedy in cases of severe depressive disorder. Reviews from patients with severe depressive or any other affective disorder report that the drug is especially effective in combination with antidepressants of other groups. It is rarely prescribed with TCAs, as well as with SSRIs. But many psychiatrists like to experiment with Mirtazapine and Venlafaxine, prescribing Zyban in parallel.” Reviews about this combination vary, but in any case, taking such combinations of drugs should proceed exclusively under the supervision of the treating psychiatrist or psychotherapist.

Indications for use

The pharmacological product is used in the treatment of depression and nicotine addiction.

If after a treatment course an adequate result is achieved, the drug is prescribed to prevent exacerbations and relapses of depression.

The active substance provides a high therapeutic effect for the following problems:

attention deficit disorder;
anxiety;
obesity;
hyperactivity;
seasonal disorders;
violations in the sexual sphere;
neuropathic pain.

The pharmacological agent is included in the complex therapy of Crohn's disease and psoriasis. The drug helps reduce the inflammatory mediator tumor factor alpha.

An antidepressant is also used

Bupropion and Metformin for weight loss

Recently, clinical trials have resumed of other combinations that help the body rebuild its rhythm of life and diet.

Zyban tablets are prescribed in the following situations:

Getting rid of nicotine addiction.
Prevention of relapses of depression.
Treatment of depression of varying severity - the drug is used as part of complex therapy.
Neuroses of various origins.
Complex therapy for social phobia and anxiety – these conditions often accompany depression.
Obesity and sexual dysfunction associated with depression.
Attention deficit syndrome.
Seasonal affective disorders.

The instructions for Zyban prohibit its use in the following situations:

The appearance of allergies and individual intolerance to the components of the substance.
The presence of convulsive disorders and epileptic seizures.
Use of MAO inhibitors - there should be an interval of at least 2 weeks between the use of these drugs.
Abrupt withdrawal of alcohol and sedative medications.
The use of other drugs with the same active ingredient.
A history of bulimia nervosa or anorexia.
Age less than 18 years.

Reviews from patients with depression and anxiety disorders

“Zyban” (an analogue of which is “Bupropion”, costs a little less, and is also sold strictly by prescription) is actively prescribed in modern psychiatry also for varying degrees of severity of depressive disorders. Reviews from patients report that, compared to other antidepressants, drugs containing bupropion do not cause side effects.

The mood quickly levels out. There is no euphoria and stimulation of the psyche, as, for example, when taking Prozac. There is no painful drowsiness or “vegetable” state, as when taking drugs based on paroxetine. Medicines with bupropion as the main active ingredient really help people improve their psycho-emotional state, with a minimum of side effects - you don’t have to take sick leave or go to the hospital, but carry out treatment in parallel with work.

Can Zyban be considered an anti-smoking pill?

So, meet the new sensational drug. Known as Zyban, also known as Wellbutrin, also known as Bupropion. And its oldest name, which few people know, is “Amphebutamon”.

These are all the same anti-smoking pills, they are just produced under different names. Why does the same remedy have so many names? To make you understand this, I will tell you a story.

A young soldier comes to the first-aid post in a military unit. Before his eyes, the doctor breaks an aspirin tablet in two and says: “Drink this half for the head, and this half for the stomach.” So in the case of Zyban, this is an elementary marketing ploy.

Like all its many variations, this drug is an antidepressant. It is promoted by one of the world's oldest and largest pharmaceutical companies, GlaxoSmithKline. Zyban has been around since 1985. Remarkably, just a year later it was banned for use. The reason for this was numerous episodes of epileptic seizures in people who took it.

Subsequently, it turned out that the cause of such side effects was an overdose of this drug. Manufacturers waited three years, and already in 1989 anti-smoking pills reappeared on sale. This time, the instructions already indicated the maximum permissible dose - 450 mg per day.

However, the problem of side effects has not been solved. Numerous reviews from smokers have spoken about this. Zyban continued to cause tremors, sweating, tinnitus, diarrhea, nausea, and rash in people. And these are just the most harmless symptoms. If you are still interested in what other side effects Zyban has, you can read these materials (in English).

Take the test and in a minute you will find out whether it will be easy for you to quit smoking

The American Food and Drug Administration has required pharmaceutical manufacturers to include warnings on the packaging of antidepressants. It is enclosed in a black frame and informs that the drug can cause suicidal tendencies in patients under 25 years of age. And it’s also on the packaging of the drug we’re looking at today.

Why are people even sure that antidepressants can cope with nicotine addiction? What the reviews sayAre you former smokers? Let's figure it out.

Everyone knows that a person who quits smoking becomes nervous, irritable and sometimes unbearable for loved ones. According to smokers, they attribute this condition to withdrawal syndrome.

In a sense, this can be considered true. In a smoking person, many natural functions of the body are disrupted, and it takes time to restore them. But it is very important to understand that when trying to quit smoking, psychosis is caused not so much by the refusal of this “bad habit” itself, but by the person’s internal struggle with his desire to smoke a cigarette.

That is why the simplest and easiest way to quit is to get rid of the very desire to smoke. To do this, you need to understand (and not only at the intellectual level) that cigarettes do not bring pleasure or anything else. They make no sense at all!

As soon as the smoker gets rid of the illusion, he immediately quits smoking. After all, there is neither desire nor temptation to take a cigarette. And he doesn't need antidepressants. Sounds like fantasy? But it's true. The “Easy Way” proved it!

Zyban is a medication that helps cope with anxiety, depression, and neuroses caused by disruptions in the nervous system. The product also helps you quit smoking. Therefore, it is often used as an effective substance for the treatment of nicotine addiction.

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.

Instructions for use

Before you start taking the medicine, you need to carefully read the instructions from the annotation.

The product has a prolonged effect.

It should be consumed whole, washed down with purified water (150-200 ml).

You should not chew the tablets, as this leads to an increased risk of side effects.

Treatment regimen using the drug:

you need to start with a dose of 150 mg;
number of doses per day – once (in the morning);
in the absence of a therapeutic response, the daily dose increases to 300 mg;
the maximum daily dose recommended in rare cases is 450 mg;
The duration of the course is determined individually (from several months to a year).

If it is necessary to increase the daily dose, the following restrictions are observed: the dose is changed by no more than 100 mg for 3 days.

Zyban: use

Zyban comes in the form of tablets to take by mouth. Zyban is usually taken three or four times a day. When treating seasonal affective disorder, the drug is usually taken once a day in the morning, starting in early fall through winter until early spring.

Take the tablets whole; do not divide, chew or crush them. Follow the directions in the instructions or ask your doctor or pharmacist for more details. Take the drug exactly as indicated in the instructions. Do not take more or less of it, or more often than prescribed by your doctor.

Your doctor will likely start you on a low dose of Zyban and increase your dose gradually. Continue taking Zyban even if you feel well. Do not stop taking Zyban without talking to your doctor. The doctor will reduce the dose gradually.

What does Zyban treat?

Why do pharmaceutical companies even offer powerful antidepressants to people trying to quit smoking? Answering this question requires a brief background.

A few years ago it was “fashionable” to treat any illness (no matter whether it was obesity, migraine or depression) with antidepressants. Just remember Valium and Lydium, the mention of which many psychologists still shudder.

Let's look at the list of disorders for which Zyban (as well as its analogues Wellbutrin and Bupropion) is intended to treat. It includes:

depression (including seasonal). This at least seems logical for an antidepressant;
social phobia (anxiety disorder). According to reviews from patients (we are not talking about smokers yet), after taking Bupropion they experienced agitation - excessive emotional arousal, accompanied by a feeling of fear and anxiety. Agitation can manifest itself as a need to move or in the form of speech anxiety. A person simply cannot sit still; he pronounces words and sentences “automatically.” He cannot think normally and analyze the situation;
sexual dysfunction;
affective disorders;
Crohn's disease ;
psoriasis;
obesity. Antidepressants have traditionally been used to keep people who are struggling with excess weight in good shape;
attention deficit disorder and hyperactivity disorder (which, in fact, are not diseases). Let's take a closer look here. The fact is that doctors and teachers did not notice much difference in the behavior of hyperactive teenagers. Well, since Bupropion didn’t help here, let’s try to distribute it as smoking pills. There is no logic at all. Nevertheless, an experiment was carried out. And it became shocking. The teenagers were divided into two groups. The first was given Bupropion, the second a placebo. As a result, more subjects in the first group started smoking. In other words, taking this drug later turned people into smokers;
nicotine addiction (no matter how strange it may be, given the experiment described above).

How to quit smoking yourself?

Application of the substance

Indications for use:

depression;
anxiety;
nicotine addiction;
sexual dysfunction;
obesity;
attention deficit disorder.

The most common problems after taking medications that contain Bupropion are:

dizziness;
headache;
sweating;
tremor;
dry mucous membranes;
dyspepsia;
nausea;
galactorrhea;
paroxysmal phenomena.

Bupropion is included in Wellbutrin XL tablet. 150 mg No. 30. This is an antidepressant that is prescribed to treat nervous disorders, including during recovery from nicotine addiction.

Our specialists will help you find the drug at the nearest pharmacy in Moscow, St. Petersburg, Yekaterinburg, Krasnoyarsk, Novosibirsk, Samara, Tyumen or Chelyabinsk. If you receive a request from another region, we will help you on an individual basis.

Pregnancy, lactation period

The pharmacological agent has not undergone clinical trials in humans.

Lack of information and lack of research data is the basis for limiting its use during pregnancy and lactation due to the potential risk to the fetus (infant).

Bupropion is used during a sensitive period for a woman in exceptional cases when the threats outweigh the risks.

If therapy coincides with the lactation period, breastfeeding is artificially interrupted.

Choice among drugs containing bupropion and analogues

The active ingredient called bupropion is included in a limited number of drugs. On the domestic market, one of the analogues is represented by Wellbutrin, which is included in the Russian pharmacological reference book.

The second drug with a similar composition is Zyban. It is certified for use in the treatment of nicotine addiction. However, the drug is not registered in Russia, so domestic experts rarely focus on the use of Zyban.

The choice among analogues of bupropion drugs in terms of action is extensive (they contain other active substances). The list is presented as follows:

Prozac;
Trittico;
Ludiomil;
Adepress.

Bupropion cannot be replaced by the patient with analogues on his own. Each of the drugs has its own specific application. Therefore, the appointment of any of them should be carried out by a specialist.

Bupropion, being a representative of antidepressants, requires careful use. Using the product for other purposes will lead to negative consequences. Taking it according to the doctor’s recommendations and taking into account the specific development of side symptoms will allow you to achieve a positive result in treatment. Changing the drug to analogues can only be recommended by a doctor after examining the patient.

Side effects

The drug may cause unwanted reactions in the body. These include the following:

Increased drowsiness;
Dizziness;
Excitement;
Anxiety;
Nausea and vomiting;
Feeling of dryness in the mouth;
Headache;
Sleep problems;
Discomfort in the abdomen;
Tinnitus;
Excessive sweating;
Pain in the throat;
Decreased appetite;
Reducing body weight;
Increased urination;
Constipation.

Refusal to take the drug and consultation with a specialist is also required in the following situations:

Rash and itching sensation;
Fever;
Hoarseness in the voice;
Hives;
Swelling of the tongue, limbs, throat, lips;
Pain in the chest;
Impaired respiratory and swallowing functions.

The drug may cause other adverse reactions. You should notify your doctor if you notice any suspicious symptoms. Improper use of a substance increases the risk of undesirable consequences. That is why it is so important to strictly follow the instructions and dosage.

Manufacturers warn in the annotation that the medicine can provoke a negative reaction in the body, especially if you are allergic to the active substance.

This manifests itself in the following symptoms:

angioedema:
hives;
bronchospasm (shortness of breath);
myalgia;
arthralgia;
anaphylactic shock.

Long-term therapy with Bupropion affects the metabolic functions of the body. During this period, the patient experiences weight loss (even to the point of anorexia), and the concentration of glucose in the blood changes.

Changes also occur in the psycho-emotional background, which is facilitated by:

insomnia;
unreasonable irritability;
hallucinations;
aggressive behavior, etc.

The official instructions provide a wide list of side effects caused by the active substance of the product being described. Effects are observed in the central nervous system, cardiovascular system, visual apparatus, etc.

To avoid an unwanted reaction, you need to carefully read the possible problems and strictly follow the treatment regimen recommended by your doctor.

This is especially true for the daily dosage and duration of treatment.

Overdose and side effects are not uncommon

Almost a third of patients experience an overdose of the drug, which happens when taking more than 450 mg of the drug per day.

An overdose may be accompanied by the following symptoms:

sinus tachycardia;
state of drowsiness;
nausea;
increased blood pressure;
state of lethargy;
epileptic condition.

During an overdose, supportive therapeutic treatment should be carried out. Intravenous injections of benzodiazepines or barbiturates are given, and activated charcoal is given.

The following negative conditions often occur while taking the medication:

manifestations of urticaria, allergies in the form of rash, itching, excessive sweating;
a state of anorexia, loss of appetite, sleep problems, increased anxiety and agitation may occur;
the occurrence of tremors, problems with taste, ringing in the ears, problems with vision;
tachycardia, high blood pressure;
Nausea, dry mouth, vomiting, constipation, pain in the abdominal area may appear;
chest pain, asthenia, fever;
weight loss, depression, confusion, decreased concentration.

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The following conditions may rarely occur:

the appearance of Quincke's edema, signs of anaphylactic shock, bronchospasm, myalgia, arthralgia;
slower reactions;
increased or decreased blood sugar levels;
problems with coordination of movements, memory problems;
irritation, signs of aggression;
frequent urination;
increased heart rate;
the occurrence of convulsions, paresthesia, fainting;
the activity of liver enzymes may increase, causing hepatitis and jaundice;
involuntary muscle twitching;
state of anxiety, delirium, vivid dreams.

Similar to those of most antidepressants. These include dry mouth, abdominal pain, and stool disorders. Possible drowsiness or excitability, tremors of the limbs (shaking), ataxia (unsteadiness of gait), dizziness, mood swings (from tearfulness to rage), decreased libido, changes in appetite. Cases of skin itching or skin rash, acne-like rashes have been reported.

Most side effects disappear in the first 7-10 days of use, however, if they become chronic or too pronounced, and also if any changes in health, sensations, or reactions appear during the period of taking Bupropion, you should immediately contact to the doctor, telling him what drug was taken (Bupropion) and for what purpose.

Characteristics of the drug

The medicine is widely used to combat nicotine addiction. However, its active ingredient, bupropion, was initially used for other purposes. This component is included in the category of atypical antidepressants and is an amphetamine.

The medicine has a very powerful effect. It has 2 characteristic differences from similar drugs:

No nicotine.
Another principle of action is the reuptake of dopamine and norepinephrine. Other antidepressants work in the same way with serotonin.

The substance has been produced since 1997. It has a certificate indicating that it can be used to combat cigarette addiction. In the Russian Federation, Zyban is not registered as a drug. That’s why doctors rarely prescribe it.

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.

Restrictions on use

Like any pharmacological agent, Bupropion has a number of contraindications for use.

They must be taken into account when selecting medications for therapy.

The restrictions apply to the following cases:

allergy to bupropion hydrochloride;
convulsions;
stopping taking sedatives (alcohol);
use of other bupropion-containing drugs;
bulimia (anorexia due to nervousness);
use of drugs with monoamine oxidase inhibitors.

You can start taking an antidepressant no earlier than 2 weeks after you stop using irreversible monoamine oxidase inhibitors.

A direct contraindication is considered to be age under 18 years.

Patients with problems with the kidneys, liver and cardiovascular system should first consult with a doctor about the safety of using the medicine.

Instructions

Unlike most anti-smoking products, Zyban has pronounced therapeutic properties. The drug helps you quit nicotine, but can also cause unwanted reactions. Therefore, before starting use, you should consult your doctor to determine contraindications and carefully read the instructions for use.

Release form

Available in the form of tablets for oral administration.

Compound

The main active ingredient of the drug is bupropion at a dosage of 0.15 g (150 mg) per tablet.

It is an atypical antidepressant, a selective norepinephrine and dopamine reuptake inhibitor.

The exact mechanism of action of bupropion is not fully known. According to the results of clinical studies, the drug is effective both in smokers with a history of depression and in patients who have never suffered from this disease.

It is believed that the effect of bupropion is associated with inhibition of the reuptake of norepinephrine and dopamine. However, the drug does not affect the activity of serotonin and monoamine oxidase. Bupropion stimulates the nutrition of serotonin neuronal structures, which is associated with improved return flow of other neurotransmitters.

Pharmacokinetic parameters have not been fully studied. It is known that with regular use, the half-life of the drug ranges from 12 to 30 hours. Equilibrium concentration in the blood is achieved on the 8th day of treatment.

Peak levels of bupropion are observed 2.5 to 3 hours after taking the tablet. But bioavailability after oral administration is low - up to 20%. Moreover, these data were obtained in clinical experiments involving animals.

Food intake affects the pharmacokinetics of bupropion, but the effect is minor. The active substance of the drug Zyban is 85% bound to plasma proteins.

Bupropion undergoes biotransformation with the participation of liver enzymes. As a result, three active metabolites are formed - hydroxybuproprion, threohydrobupropion and erythrohydrobupropion. These compounds differ in their half-life (from 15 hours to 2 days). Buproprion and its metabolites are predominantly excreted in the urine (up to 87%) and feces (up to 10%).

The instructions for use provide pharmacokinetic indicators for certain categories of patients:

Kidney diseases. Clinical trials have confirmed a slower elimination of bupropion and its metabolites in patients with severe pathology of the urinary tract.
Liver diseases. Drug metabolism was compared in patients with liver cirrhosis and healthy patients. In the first group, biotransformation was slower by more than 50%.
Smoking. Does not have a significant effect on the metabolism of the drug.
Diseases of the cardiovascular system. Do not affect the pharmacokinetics of bupropion.
Age. Clinical studies included patients from 18 to 89 years of age. No differences in pharmacokinetics have been identified, but doctors warn about the risk of accumulation of bupropion and its metabolites in people over 65 years of age.

Pharmacokinetic parameters were compared in men and women. It was revealed that the peak concentration of bupropion was 13% higher in the first group of patients. But this difference is considered not clinically significant.

Bupropion is chemically different from nicotine and structurally similar compounds that are often used to treat nicotine addiction. Molecular weight - 276.0, structural formula - С13Н18ClNO. Bupropion is a white crystalline powder, highly soluble in water. When it comes into contact with the mucous membrane, it causes a feeling of numbness, which is why Zyban tablets are coated with an enteric film coating.

The main indications for taking Zyban are:

nicotine addiction, accompanied by a desire to stop smoking;
preventing cravings for nicotine after quitting smoking.

The active ingredient of the drug under the trade name Wellbutrin is used to treat depression and anxiety disorders. Moreover, unlike other medications, Zyban does not cause erectile dysfunction. There is evidence of the effectiveness of bupropion in the complex treatment of obesity.

The list of contraindications for use includes the following items:

seizure disorders;
pregnancy;
lactation;
children and adolescents up to 18 years of age;
history of bulimia and anorexia;
simultaneous use of monoamine oxidase inhibitors and for 2 weeks after stopping treatment;
individual intolerance to bupropion and auxiliary components.

Zyban is not prescribed to patients at the stage of treatment for alcohol and drug addiction, addiction to benzodiazepines, barbiturates, and potent analgesics.

It takes 7 to 8 days to reach equilibrium concentrations of bupropion, so use should not be combined with abrupt nicotine withdrawal. The patient is prescribed a specific day (during the second week of therapy) when to quit smoking.

The tablet is taken at any time, regardless of food intake, swallowed whole and washed down with a sufficient amount of water. The maximum daily dosage should not exceed 0.3 g.

The duration of treatment is 7 - 12 weeks. If the therapy does not bring the desired effect, stop taking the drug. To improve the outcome of treatment, the patient is recommended additional psychotherapy. Psychological support from family and friends is important.

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The following side effects are possible during use:

the appearance of suicidal thoughts;
convulsions;
emotional instability;
manic disorders;
psychoses and other neuropsychological reactions;
allergic manifestations.

But the listed side effects are typical for all antidepressants, and occur in isolated cases while taking them.

The following adverse reactions have been reported during post-marketing studies:

neck pain;
tides;
increased blood pressure;
feeling of dry mouth;
increased appetite or anorexia;
arthralgia, myalgia;
sleep disorders;
headache;
dizziness.

Nausea and vomiting, abdominal pain, nasal congestion, and disturbing dreams were extremely rarely reported. Deterioration of visual acuity and diplopia are also possible.

Due to the pharmacokinetics and mechanism of action, Zyban is combined with caution with:

Ticlodipine, Clopidogrel and other antiplatelet agents;
antiviral agents (Ritonavir, Lopinavir, etc.);
sedatives, tranquilizers (Phenobarbital, Phenytoin, barbiturates);
other antidepressants (Venflaxin, Nortriptyline, Paroxetine, etc.);
β-adrenergic receptor blockers;
antiarrhythmic drugs;
hormones of the adrenal cortex;
dopaminergic medications;
cardiac glycosides.

Avoid concomitant use of Zyban and antibiotics that are metabolized by the liver (both tablet and injection forms).

Consumption of alcoholic beverages during administration is contraindicated.

Although Zyban is intended to combat nicotine addiction, the drug belongs to the group of antidepressants. Like other medications of this class, it can exacerbate suicidal tendencies, especially in young patients (18 - 24 years old). No cases of suicide have been reported during treatment, but patients suffering from depression are advised to use other methods of quitting smoking.

The patient himself, his family and friends are warned about the likelihood of suicidal thoughts. Therefore, if signs of emotional instability appear, you should immediately consult a doctor.

Zyban may also trigger seizures, especially if the recommended daily dose (0.3 g) is exceeded. The risk of such a complication depends on the general condition of the patient and other medications taken.

The likelihood of developing seizures increases with:

organic lesions of the central nervous system (tumors, injuries, infections);
kidney diseases (hyponatremia);
liver pathologies;
diabetes mellitus;
alcohol consumption.

In patients predisposed to hypertension, Zyban may cause a persistent increase in blood pressure. In this situation, regular monitoring of the patient’s condition and additional consultation with a cardiologist are required.

There is no data on use during pregnancy, but experts admit the teratogenic and embryotoxic effects of bupropion. Therefore, during the period of bearing a child, women are recommended psychotherapy. The active substance of the drug is excreted in breast milk, so use is contraindicated during lactation.

Due to possible neurological disorders, it is recommended to refrain from driving.

Overdose

If the recommended dose is exceeded, the following are possible:

convulsions;
hallucinations;
loss of consciousness;
tachycardia;
fever;
skeletal muscle rigidity;
decrease in blood pressure.

There is no specific antidote. In case of overdose, hospitalization and monitoring of basic parameters of the kidneys, liver and cardiovascular system are required. If necessary, carry out symptomatic treatment.

Storage conditions

The package with the drug is stored at room temperature, protected from moisture, direct sunlight and access to children.

Best before date

Indicated on the package and blister of tablets.

Effects of the drug "Zyban"

The product has a pronounced therapeutic effect. The medicine is not a nicotine replacement medicine. Its effectiveness is ensured by the presence of bupropion in the composition. It is this substance that acts on the mechanism of addiction.

Zyban affects certain areas of the brain that are responsible for experiencing pleasure. It also supports dopamine synthesis. Due to the properties of an antidepressant, the medicine reduces the patient’s psychological discomfort when getting rid of a bad habit and prevents craving for cigarettes. As a result, the person loses the desire to smoke.

When including Bupropion in complex therapy, its compatibility with other pharmacological products is taken into account.

Its simultaneous use with certain medications is prohibited.

Among them:

anxiliotics;
other antidepressants;
glucosteroids;
antibiotics of some types (Tsiprolet, Ciprofloxacin);
insulin and sugar-lowering medications;
drugs for the treatment of Parkinson's disease;
beta blockers.

Medicines that alter the activity of the CYP2B6 isoenzyme are recommended in tandem with Bupropion with caution.

Reviews about the compatibility of the drug with alcohol

Drugs containing bupropion are also prescribed when giving up alcohol. It is optimal to start taking it a couple of weeks after your last binge use. As a rule, pills help get rid of mild withdrawal symptoms. If it is strong, then medications with a more powerful effect will be required.

Reviews of Zyban from people with alcohol addiction report that while taking the drugs, the phenomenon of “craving” for ethyl alcohol is noticeably less. It is important not only to take pills, but also to work with a psychotherapist on your addiction, then you can really achieve long-term remission.

Precautionary measures

One of the common adverse reactions is sleep disturbance.

To eliminate the problem, the attending physician recommends reducing the daily dose or increasing the time between doses of the medication. Based on this, you should strictly adhere to the 24 hour interval.

Many antidepressants have a negative effect on sexual function. The likelihood of such a side effect with Bupropion is close to zero (according to statistics).

With long-term use, the drug in question does not cause an increase in body weight. However, a different scheme is proposed for losing weight than for the purpose of restoring the psycho-emotional background. It is determined by the doctor taking into account the characteristics of the body.

During the period of therapy, you should not drive vehicles or other mechanisms that pose a danger to the patient himself or others. The active substance can inhibit motor function and affect psychomotor function.

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.

Contraindications

Contraindications to taking Zyban are:

epilepsy;
convulsions;
anorexia and bulimia;
simultaneous use with certain types of medications;
allergies to medications;
alcohol abuse;
addiction;
brain tumors;
affective insanity;
high blood pressure;
diabetes;
kidney and liver diseases;
heart failure;
pregnancy and lactation.

In some diseases, Zyban can cause seizures, so before prescribing it, the doctor must establish a complete picture of the patient’s health. Concomitant use with alcohol increases the risk of side effects, so it is better to refrain from drinking alcohol during treatment with Zyban.

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.

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

How to take the drug

The tablets must be swallowed whole. When taking the capsules, you do not need to break or chew them; the tablets must be washed down with water.

It is worth considering that the effect of treatment does not occur immediately; the result will be visible after a few weeks.

the highest dose of the drug in the form of tablets with prolonged action is no more than 450 mg per day;
the drug should be taken once a day and at the same time;
if necessary, then 3 days after the start of therapy or during long-term therapeutic treatment, increase the initial dosage by 100 mg.

The initial dose is 150 mg of the substance per day. If the patient’s condition does not improve 14 days after the start of therapy, the dose should be increased to 450 mg.

The duration of therapy is six months or more. The greatest effectiveness of the drug is observed with long-term therapy for a year. If there is a condition of renal failure, then therapy should be started with minimal doses.

Pregnant women should take the medicine only on the recommendation of a doctor.

This is due to the fact that there is no data on the safety of this medicine for the treatment of pregnant women; the active components of the drug can have a negative effect on the child, but such cases have not been registered.

Since the elements included in the medication pass into breast milk, it is not recommended to take it during breastfeeding.

The medicine should not be taken by children and adolescents under 18 years of age. This is due to the fact that when used by children at this age, they may have suicidal thoughts.

Reviews

After a long diet to lose weight, she became irritable and lashed out at friends and acquaintances over trifles.

I stopped recognizing myself.

I lost only 2.5 kg, but my nerves were frayed. At the appointment, the doctor advised me to take Bupropion.

After 3 weeks I felt the first results with my mood and internal state. But the best part is that the weight crept down. In 3 months, my figure returned to normal, as did my psycho-emotional background.

I took the divorce from my wife badly. The result is depression. And it just started with the fact that I didn’t want to see anyone. I've reached a dead end.

A neighbor helped and dragged me to a psychotherapist. He prescribed Bupropion for long-term therapy.

Now I don’t even want to remember the past. Life goes on thanks to the right treatment and antidepressant.

Reviews from experts

According to psychologists, this medication is a fairly effective treatment for patients with psycho-emotional disorders. Good results have been reported from taking Bupropion as a treatment for tobacco addiction.

But narcologists practically do not use the generic as an antidepressant. This is explained by the fact that the drug is not widespread in the Russian Federation. According to reviews from people who have used Bupropion to combat tobacco addiction, the reviews are overwhelmingly positive.