Velbutrin

Velbutrin is a psychoanaleptic from the category of other antidepressants.

Indications of the velbutrin

It is used in the treatment of depressive states of high severity.

[1], [2], [3]

Release form

The release is made in tablets, in an amount of 10 pieces inside the blister plate. The box contains 6 such plates.

[4], [5]

Pharmacodynamics

Bupropion is a substance with a selective retardation effect on the processes of neuronal capture of catecholamines (dopamine with norepinephrine). This component has minimal effect on the processes of capture of indolamine (serotonin), and also does not suppress the activity of MAO.

[6]

Pharmacokinetics

Suction.

When bupropion was administered by volunteers during the study, peak values of the substance inside the plasma were noted after 3 hours.

The information obtained after 3 clinical tests suggests that the values of bupropion may increase with the use of the tablet along with the food. After application with food, the peak plasma parameters of the component increase by 11%, as well as 16% and 35%, and the AUC values increase by 17%, 17%, and 19% in 3 tests.

Bupropion along with its metabolic products has linear pharmacokinetic characteristics with prolonged use of drugs in portions of 150-300 mg / day.

Distribution processes.

Bupropion has a high index of the distribution volume - it is approximately 2000 liters. The active element of the drug with its metabolic product (hydroxybupropion) is moderately synthesized with blood plasma proteins (by 84%, and also 77%, respectively). The degree of protein synthesis of triohydrobupropion is approximately half that of bupropion.

Metabolic processes.

Inside the body, an intensive metabolism of bupropion occurs. Inside the plasma, there are 3 pharmacoactive metabolic products: hydroxybupropion together with its aminoalkolic isomers - treohydrobupropion, as well as erythrohydrobupropion.

Excretion.

About 87% of the active element is excreted in the urine (less than 10% of the substance - in the form of active decay products), and up to 10% is excreted with feces. Withdrawal, unchanged bupropion is only 0.5%.

The average clearance of the substance after using the drug is approximately 200 liters / hour, and the average value of its half-life is about 20 hours.

[7], [8], [9]

Dosing and administration

The drug begins to affect the body at least 2 weeks after the start of therapy. A full-fledged effect from its use can be expected only after several weeks of the course, as in the case of taking other antidepressants.

Tablets are swallowed whole, not chewing, and also not grinding / dividing them, because as a result, the risk of developing side-effects (for example, seizures) may increase.

Dose sizes for adults.

The size of the maximum single dose is 0.15 g. Tablets should be consumed twice a day at intervals of at least 8 hours.

Quite often, patients taking a pill have insomnia, which is often temporary. Reduce the frequency of this symptom can be by abstaining from taking drugs before going to bed (with an 8-hour interval between applications) or reducing the size of the portion, if it is acceptable.

The size of the initial portion is a single dose of 150 mg per day.

For people who are not enough to take 0.15 grams of drugs per day, you can achieve improvement by increasing the portion to the maximum values of 0.3 g / day (0.15 g twice a day).

When eliminating acute depressive episodes, take antidepressants for at least six months. It is determined that a drug at a dosage of 0.3 g / day will have a medicinal effect for a long therapeutic period (up to 12 months).

Dosage for the elderly.

Due to the fact that it is not possible to exclude the possibility of intolerance to Velbutrin in some elderly patients, it may be necessary to reduce the frequency of application or the size of the portion of the drug.

Serving size for people with kidney problems.

Therapy starts with reduced dosages or with a lower frequency of reception, because bupropion with metabolic products accumulates in this category of treated more severely than under standard conditions.

Portions for people with disorders of hepatic activity.

People with hepatic diseases should carefully use the drug. Because of the rather high variability of pharmacokinetic properties of drugs, people with disorders in the liver that have a mild or moderate form, it is required to take the medication once a day in a dose of 0.15 g.

People with liver cirrhosis in severe form should take very careful pills. For these patients, the maximum serving size is 0.15 g with a daily dose of LS.

[12], [13], [14]

Use of the velbutrin during pregnancy

Separate epidemiological tests of Velbutrin's effect on pregnancy during pregnancy revealed an associated risk of intrauterine damage to the SSS in the fetus in the case of drug use in the 1st trimester. This information in different tests was not the same.

The treating doctor should consider the option of prescribing alternative therapy for a woman who is at the planning stage of pregnancy, or for an already pregnant woman. Prescribe the same drug should be only in situations where the likely benefits of the application will be higher than the risk of complications in the fetus.

Due to the fact that bupropion with its breakdown products can be excreted together with mother's milk, during treatment with Velbutrin it is required to refuse from breast-feeding for a while.

Contraindications

The main contraindications:

• patients who are intolerant of bupropion or other elements of the drug;
• people suffering from seizures;
• persons who at the moment have suddenly stopped using sedative drugs or drinking alcohol;
• appointment to people who at the same time take any other medicine that contains bupropion - because the frequency of the appearance of convulsive seizures is determined by the size of the dosage of this substance;
• presence in the patient's anamnesis, or anorexia or bulimia of a nervous nature present right now, because this category of patients had frequent seizures when bupropion was used with a rapid release stage;
• combined use with MAOI. The interval between stopping the reception of MAOI irreversible and the initiation of therapy with Velbutrin should be at least 2 weeks.

[10]

Side effects of the velbutrin

The use of medication can cause the following side effects:

• lesions affecting immunity: often there are signs of intolerance, for example, urticaria. Single notes of more severe symptoms of high sensitivity, including bronchial spasm / dyspnea, Quincke edema or anaphylaxis. Myalgia with arthralgia, as well as a febrile condition, occur together with rash and other manifestations of delayed intolerance. Similar symptoms are slightly similar to serum sickness;
• metabolic manifestations and digestive disorders: anorexia is often observed. Sometimes weight loss occurs. Disorder of glucose values inside the blood;
• mental disorders: often there is insomnia. Possible development of sleep disorders. Quite often there is a feeling of anxiety or excitement. Sometimes there is a state of disorientation, dysphoria or depression. Individual feelings of anxiety, aggression, irritability, and hostility appear; strange dreams or hallucinations arise, and besides this, paranoid thoughts, delusions and a state of depersonalization develop. There may be psychoses, thoughts of suicide, and also suicidal behavior. Perhaps the development of mania, euphoria, hypomania and changes in the state of the psyche;
• disorders affecting the central nervous system: often headaches are noted. Quite often there are dizziness, memory problems, tremor, myoclonus, migraine, dystonia, and also a sense of anxiety and taste disorders. Sometimes it can develop vertigo, dysarthria, problems with care and concentration, as well as akathisia. Disorders of ECG and convulsions occur occasionally. Paresthesia, ataxia, problems with motor coordination, dystonia, syncope and tremor paralysis are sometimes observed. Perhaps the development of delirium, dyskinesia, coma and problems with sensitivity;
• lesions in the field of visual organs: a visual violation is often noted. Occasionally, diplopia develops. Sometimes noted mydriasis. It is possible to increase IOP values;
• disorders affecting the auditory organs: often there is an ear ring;
• symptoms in the heart: sometimes there are heart rhythm disorders, tachycardia and changes in ECG values. Occasionally, myocardial infarction develops. It is also possible to increase blood pressure and the appearance of edemas. Single noted increased heart rate;
• reactions of the vascular system: often there is an increase in the level of blood pressure (sometimes significant), and in addition redness. Orthostatic collapse or vasodilation develops;
• signs of digestive disorders: often there are problems in the work of the digestive tract (among them vomiting with nausea) and dryness of the oral mucosa. Often there are dyspeptic symptoms, constipation and abdominal pain. Sometimes there is irritation in the gums and the appearance of toothaches. Intestinal perforation is also possible;
• disorders of the hepatobiliary system: there is a single hepatitis or jaundice, and besides this, the index of liver enzymes increases;
• damage to the subcutaneous layers and skin: often marked by hyperhidrosis, rash and itching. Single appears Stevens-Johnson syndrome or erythema multiforme, and in addition psoriasis worsens. Possible development of alopecia;
• lesions of respiratory organs: occasionally there is an embolism of the lungs. There may be bronchitis;
• Dysfunction of ODD and connective tissue: muscle twitching is observed single-handedly. Rhabdomyolysis or arthritis may be expected;
• problems in the work of the urogenital system and kidneys: most often mark infections that affect the urinary organs. Sometimes there is a weakening of the libido. Urination is often more frequent, or there is a delay in urination. Possible disorders of the menstrual cycle, the development of glucosuria, impotence, nocturia, gynecomastia, as well as the appearance of swelling in the testicles;
• systemic disorders: often there are pain in the sternum, a state of fever and asthenia;
• problems with hematopoietic processes: there may be thrombocytopenic or leukopenia, as well as leukocytosis.

[11]

Overdose

In addition to the symptoms that are indicated among the side effects, intoxication leads to such manifestations as loss of consciousness, a feeling of drowsiness and changes in ECG readings (conduction disorder, for example, prolongation of QRS-interval values) or arrhythmia. There is also evidence of a fatal outcome.

To eliminate the overdose, it is necessary to hospitalize the victim who needs to be monitored for ECG indications and the work of vital organs. It is necessary to make sure that the patency of the respiratory ducts is not disturbed, that there are no problems with ventilation and oxygenation. Also it is necessary to take activated charcoal. Induction of vomiting is not needed. Bupropion does not have a specific antidote.

Follow-up therapy is determined by the condition of the victim or the recommendations of the special institution dealing with the treatment of intoxications (if any).

[15], [16], [17], [18], [19], [20], [21],

Interactions with other drugs

The metabolic process leads to the conversion of bupropion to its main active degradation product - hydroxybupion. This process occurs mainly with the participation of hemoprotein P450 IIB6 (type CYP2B6). Because of this, caution is required when combining drugs with drugs that affect isoenzyme CYP2B6 (such as ifosfamide with clopidogrel, cyclophosphamide with orfenadrine, and ticlopidine).

While bupropion is not metabolized with isoenzyme CYP2D6, in vitro 450 tests demonstrated that this element together with hydroxybupropion slows the metabolic process of the CYP2D6 enzyme. During pharmacokinetic tests, the use of bupropion increased the plasma values of desipramine. This effect was noted for at least 7 days after the last bupropion was taken. When combined with drugs that are metabolized mainly with this isoenzyme (eg, antiarrhythmics, SSRIs, antipsychotics, tricyclics and individual beta-blockers), it is necessary to start treatment with minimal portions of such drugs. When Velbutrin is included in the scheme of therapy of a person who is already taking a drug metabolized with the participation of the element CYP2D6, it is necessary to evaluate the variant with a decrease in the dosage of this drug, especially for drugs that have a narrow drug index.

Medicines whose effective action requires metabolic activation with the aid of the CYP2D6 element (such as tamoxifen) are able to reduce their drug exposure when combined with drugs that slow the activity of the CYP2D6 component (bupropion).

Although citalopram is not subjected to primary metabolism involving the element CYP2D6, the data of one test shows that bupropion increases the peak values and AUC level of citalopram by 30% and 40%, respectively.

Because of the intensive metabolism of bupropion, the combination of a substance with drugs that potentiate metabolism (among such phenytoin, carbamazepine, efavirenz with phenobarbital, and in addition ritonavir), or oppressing it, can lead to a change in the drug effect of drugs.

The results of a series of clinical tests with the participation of volunteers showed that ritonavir (with double intake per day 0.1 g or 0.6 g of LS) or 0.1 g of ritonavir with 0.4 g of lopinavir (twice daily intake) depending on the size portions of approximately 20-80% reduced the values of bupropion with its major metabolic products.

Similarly, a single dose of efavirenz in a 0.6 g dose per day for 14 days reduces by approximately 55% the level of bupropionol.

This effect of ritonavir with lopinavir, as well as efavirenz, is due to the induction of a metabolic effect on bupropion. People who use any of these drugs, in combination with medicines that have bupropion, may require the use of higher doses of bupropion, but it is prohibited to exceed the maximum allowable limits of recommended servings.

While the results of clinical tests did not show the presence of pharmacokinetic interaction of the active element of drugs with alcoholic beverages, there is some evidence that the CNS developed negative manifestations or there was a decrease in tolerance for alcohol in persons who consumed such drinks during therapy with Velbutrin . The use of alcohol for the period of therapy should be reduced to a minimum or discontinued completely.

There is evidence of an increase in the frequency of development of toxic effects relative to the central nervous system when the drug is combined with amantadine and levodopa. Use medicine with people who use amantadine or levodopa with caution.

Combined use of medication and NTS can lead to an increase in blood pressure.

Impact on the results of laboratory studies.

There is information about the presence of drug interaction with tests, which are used to quickly identify the presence of drugs in the urine. Studies can produce false positive results, especially if amphetamines are detected. To confirm a positive result, you need to use the chemical method as an alternative.

[22]

Storage conditions

Velbutrin is required to be kept out of the reach of children. Temperature values are a maximum of 25 ° C.

[23],

Shelf life

Velbutrin can be used for 2 years from the date of manufacture of the drug.

[24]

Reviews

Wellbutrin receives quite a few reviews, and the opinions of the patients in them are quite polar. The medicine is very successfully used to eliminate depressions. In addition, it is often written that the drug can help ease the condition during the cessation of smoking.

With the task of curing depression, the medication is very effective, but it has a significant disadvantage - the presence of unpleasant side effects that develop during the 1-2 weeks of use. Among the advantages for men, it can be noted that the drug does not suppress erectile function.

To achieve the required medication, and to minimize the risk of side effects, therapy should be started with taking 0.15 g of Velbutrin. Sometimes it is also necessary to select the optimal time for taking drugs, there are people for whom the pill is most appropriate before bedtime, but there are also those who need to take the drug early in the morning (at 5-6 hours).

Also among the shortcomings of the medicine:

• to get it, you need a prescription;
• too many negative symptoms;
• sufficiently high price.