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.
Your Narcologist warns: pregnancy and childhood
These are the two cases when the drug is prescribed only on the recommendation of a doctor and is strictly monitored by him. This exclusivity is explained by the fact that there is no official data (despite numerous tests of the drug) on the effect of Zyban on pregnancy and lactation.
To be fair, it should be said that there are no cases of negative effects on the expectant mother or fetus when adequate dosages are prescribed. During lactation, restrictions are associated with the penetration of the drug into breast milk.
In the case of children (under 18 years of age), emphasis is placed on their unstable psyche and tendency to suicidal thoughts.
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.
Possible negative reactions of the body
Wellbutrin can have a wide variety of side effects. They appear especially often in the first weeks of use.
Treatment may be accompanied by the following side effects:
- allergic reaction (swelling of the face, lips, throat or tongue, difficulty breathing, rash);
- dry mouth;
- agitation;
- headache;
- vomit;
- nausea;
- increased sweating;
- dizziness;
- visual impairment;
- insomnia;
- anorexia;
- hallucinations;
- confusion;
- unusual dreams;
- aggressiveness;
- tremor;
- irritability;
- seizure disorders;
- fainting;
- impaired coordination of movements;
- visual impairment;
- tachycardia;
- heartbeat;
- constipation;
- urinary disturbance;
- chest pain;
- fever;
- skin itching.
Many patients who decide to use Bupropion after quitting smoking do not complete the treatment they begin due to side effects. Such as:
- tremor;
- skin redness;
- increased libido.
But experts recommend not to stop treatment, because all such manifestations disappear after 1.5-2 weeks from the moment you start taking the medicine. In addition to these effects, taking Bupropion can provoke the development of other negative manifestations.
Often:
- tremor;
- tachycardia;
- increased blood pressure;
- nausea and vomiting;
- bowel dysfunction;
- loss of appetite;
- ringing and buzzing in the ears;
- visual impairment;
- dry mouth;
- soreness of the sternum;
- feverish conditions;
- increased anxiety;
- increased sweating;
- loss of taste;
- allergies (hives, itching, rash);
- disruption of usual sleep patterns.
Sometimes:
- confusion;
- loss of concentration;
- ataxia (rolling and unsteady gait);
- drowsiness or increased excitability.
Rarely:
- Quincke's edema;
- hallucinations;
- bronchospasms;
- anaphylactic shock;
- increased urination;
- jumps in plasma sugar concentration;
- atralgia and myalgia (pain in muscles and joints);
- irritability reaching the point of aggressiveness.
The most common problems after taking medications that contain Bupropion are:
- dizziness;
- headache;
- sweating;
- tremor;
- dry mucous membranes;
- dyspepsia;
- nausea;
- galactorrhea;
- paroxysmal phenomena.
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.
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.
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.
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.
- Possible negative reactions of the body
- Drug interactions
- Features of the medicine
- Side effects
- Indications, side effects, drug interactions, doses
- Side effects
- Precautionary measures
- Description and Instructions
- Narcogenic potential
- Application diagram
- Bupropion
There are certain symptoms that you should immediately consult a doctor if they appear. These include the following:
- Depression, panic, increased anxiety,
- Thoughts of suicide or suicidal actions
- Hallucinations,
- manias,
- 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.
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.
Special instructions, storage methods
Zyban, although used to facilitate the process of quitting smoking, does not lose its antidepressant properties. Therefore, when prescribing it, a preliminary complete clinical and laboratory examination and the development of an individual dosage and administration regimen are necessary. Dynamic monitoring of the patient.
However, the risk of seizures and epilepsy increases with increasing dose. Provoking factors are considered to be a history of traumatic brain injury, a tumor process in the central nervous system, simultaneous use of prohibited drugs: antidepressants of another group, hypoglycemics, sedatives, drugs, appetite suppressants, hepatoprotectors. Violation of the conditions of admission can lead to manic-depressive psychosis and suicide. Moreover, suicidal thoughts appear more often in young patients, under the age of 25 years. Such manifestations dictate the abolition of the medication.
Patients with bipolar disorders are at risk of developing phobia or mania as a complication.
In this case, therapy is carried out with mood stabilizers.
Suffering from diseases of the cardiovascular system should remember the possibility of developing a hypertensive crisis, blockade of the conduction system of the heart. However, such complications rarely occur.
Another risk from taking Zyban is uncertain driving, which a priori requires clear consciousness and a clear, instant reaction on the road. Therefore, the course of drug therapy, of course, is not canceled, but the dose and the body’s reaction to it are constantly monitored.
There are countless analogues of Zyban, since it is a generic. There is no point in listing them all. It must be remembered that the active substance of similar tablets is also wellbutrin or bupropion.
Storage conditions and shelf life
The drug is stored in a cool place, securely protected from children, for up to one and a half years.
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
Release form and composition of the product
Bupropion is available in the form of extended-release tablets.
The tablets are coated on top and have a creamy white or pale yellow color. The shape of the tablets is round, on one side there is an inscription in black letters “GS5FV”. The tablets are placed in high-density polyethylene-based bottles that contain a desiccant container. The bottles are contained in cardboard boxes. The bottles contain 7, 30 and 90 tablets.
Ingredients:
- active element - bupropion in dosages of 150 and 300 mg;
- additional elements - polyvinyl alcohol, glyceryl tribehenate;
- shell components - ethylcellulose-100, povidone, macrogol-1450, methacrylic acid and ethyl acrylate copolymer [1:1] (contains 0.7% sodium lauryl sulfate, 2.3% polysorbate-80), silicon dioxide, triethyl citrate, black ink.
Overdose
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.
Narcogenic potential
According to Kekelidze's conclusion, bupropion can be used to obtain a psychoactive effect.
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“In this case, the route of administration changes from oral to intranasal, and the dosages are many times higher than therapeutic ones, which leads to an increased risk of seizures, since the use of bupropion can lower the threshold of convulsive readiness of the brain,” the expert writes.
However, apparently, the possibility of using the drug for non-medical purposes exists only in theory.
“According to the Moscow Scientific and Practical Center for Narcology of the Moscow Department of Health, over the past ten years, there have been no cases of bupropion abuse in the drug treatment services of the constituent entities of the Russian Federation. In addition, during chemical-toxicological studies in samples of biological fluids of examined citizens, no cases of detection of bupropion were recorded,” says the conclusion of the director of the institution, Sergei Koporov.
“Obtaining ephedron in this way requires deep knowledge of organic chemistry and appropriate qualifications, so most often ephedron is obtained from ephedrine,” explains Boris Izotov, chief freelance specialist in analytical and forensic toxicology of the Ministry of Health.
When asked by RT whether the Ministry of Health will take any action to “legalize” bupropion, taking into account the opinion of experts, the department did not answer.
Precautionary measures
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.
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.
