Zolafren

Zolafren is a psycholeptic from the category of antipsychotics.

Indications Zolafren

It is used for therapy in schizophrenia in people who have previously been shown to be medically affected during the active treatment phase.

It is used to treat various exacerbations, as well as with prolonged maintenance therapy to prevent relapses in people with schizophrenia and other psychotic disorders that have an intense productive (the appearance of automatisms and hallucinations) or negative symptoms (weakening of emotionality, deterioration of social activity, poor speech), and in addition to this with concomitant affective disorders.

Also appointed at the BAR - for the treatment of mixed or manic (acute) attacks (may be accompanied / not accompanied by psychotic symptoms and rapid change of stages).

[1], [2]

Release form

Release of the medication is realized in tablets, which are packed into 30 pieces inside a blister pack. In a pack - 1 packing with tablets.

Pharmacodynamics

Olanzapine is an atypical antipsychotic (neuroleptic), which is a selective antagonist of monoaminergic elements, and has an affinity for the following endings: serotonin (5HT2a / 2c, and 5HT3 and 5HT6), dopamine (D1 and D2, and in addition D3, D4 and D5) , cholinergic muscarin (M1-5), histamine (H1), and with it α1-adrenergic. Olanzapine selectively affects the mesolimbic system without exerting a noticeable effect on the extrapyramidal system.

The exact pattern of the therapeutic effect of olanzapine, like other drugs used in schizophrenia, remains unknown. It was concluded that the effect of the drug in schizophrenia is provided by combining a dopamine antagonist and serotonin of the 5HT2 category.

Olanzapine exhibits a stronger bond with 5HT2 termini (compared to synthesis with D2 endings). With the last ending, the medicine binds worse than simple antipsychotics. This therapeutic profile explains the positive effect of the drug on pathological symptoms, and additionally it affects the appearance of extrapyramidal disorders and dyskinesia of late type, associated with therapy, in which olanzapine is used.

The antagonistic effect with respect to the other, in addition to the dopamine and 5HT2 endings, explains the other individual medicinal effects and the negative effects of olanzapine. The antagonistic effect on the M1-5 endings of muscarin can explain its anticholinergic properties. Antagonism of the substance with respect to H1 endings of histamine can provoke a feeling of drowsiness, and antagonism with respect to α1-adrenergic endings explains the development of orthostatic collapse.

Pharmacokinetics

Orally administered olanzapine is well absorbed from the gastrointestinal tract, reaching peak blood values after 5-8 hours. Eating does not affect the absorption of the substance.

The metabolism of the medication is carried out in the liver - by synthesis with oxidation (40% servings). The main decay product is the 10-N-glucoronide element, which does not have the ability to pass through the BBB. For the most part, the therapeutic effect of Zolafrene depends on the activity of olanzapine, which has not undergone biotransformation.

The half-life is in the range of 21-54 hours (the average figure is 30 hours), and the plasma clearance level is 12-47-L / h (average value is 25 L / h).

Olanzapine excretion is mainly carried out in the form of decomposition products - about 57% together with urine, and 30% - with feces.

The indices of the drug inside the blood plasma are linear depending on the size of the used dosage of the drug. With a single use of drugs per day for 7 days, a stable index is created inside the blood plasma, corresponding to a double value after a 1-time dosage.

Plasma parameters, half-life and the level of clearance of a substance can vary with age and sex of patients, as well as smoking. Plasma values for drug clearance are lower in women, elderly people and non-smokers. But it should be noted that all these factors do not have special significance in the treatment.

[3], [4]

Dosing and administration

The medicine is consumed once a day, without binding to the reception of food. First dosage of drugs per day should be 10 mg, and later it can fluctuate within 5-20 mg. The optimum portion suitable for the patient is selected taking into account his condition, and its increase by more than 10 mg / day should be justified by clinical indications. If necessary, in adjusting the portion, you need to increase it or lower it by 5 mg.

A day is allowed to use no more than 20 mg of the drug (to raise the dose to a mark more than 15 mg / day is allowed at least 4 days after therapy).

Elderly people or people with low weight are recommended to take 5 mg of medicine per day, but provided that such dosage is sufficient to improve the condition. A similar dosage should be taken and people with deficiency of renal or hepatic function.

[5]

Use Zolafren during pregnancy

Do not use Zolafrenom during pregnancy or lactation.

Contraindications

Among the contraindications:

• presence of strong sensitivity with respect to drug elements;
• glaucoma, which has a closed-angle shape. 

Side effects Zolafren

Most often, the use of drugs leads to the appearance of such signs: weight gain, a feeling of drowsiness, asthenia (sensation of weakness), orthostatic collapse, dizziness. In addition, there is an increase in appetite, dryness of the oral mucosa, constipation, fluid retention (the appearance of peripheral edemas), personality disorder, anxiety and akathisia (inability to lie or sit in one place).

Individual manifestations are: Parkinsonism, visual disturbances, vomiting, dyskinesia (problems with the implementation of precise movements, especially affecting the fingers and hands), headaches and dystonia (muscle tone disorder).

At the initial stage of therapy, there may be an increase in prolactin levels within the blood plasma, but in most patients they return to the baseline without interrupting the treatment course.

With a prolonged therapeutic cycle, galactorrhea, the disappearance of menstruation or a cycle disorder, and in addition gynecomastia and an increase in the size of the mammary glands can be recorded. There was no significant effect of olanzapine on the duration of the QT-interval on the ECG. Transient curable increase in liver transaminase activity (ALT with AST) was noted.

There was also an increase in CFC indices. As with other neuroleptics, the change in blood values was recorded. Occasionally reported on the development of strong photophobia.

ZNS may also develop, among the symptoms of which vegetative (tachycardia, hyperhidrosis, diarrhea, heart rhythm disorder and changes in blood pressure level) and motor disorders (convulsions and muscle rigidity), and in addition, a consciousness disorder, an increase in the level of CK, the development of myoglobinaria (in the urine is noted the appearance of myoglobin) or kidney failure in the acute stage. With ZNS no specific therapy is prescribed, it is required to immediately abolish the use of antipsychotics, as well as to monitor the patient's condition and conduct intensive symptomatic measures.

Dyskinesia in the later stages is a potentially incurable set of pathological movements of the trunk and extremities that can not be controlled. High probability of occurrence of similar signs at older persons (in particular of a female). At a late stage of dyskinesia, there is no specific therapy, but there is a possibility that the syndrome completely or partially regresses after stopping the antipsychotic.

Overdose

Among the signs of poisoning: speech disorder, a feeling of drowsiness, eye disorder, pupil dilated, problems with respiratory function, extrapyramidal symptoms and a decrease in the level of pressure.

In the acute stage of intoxication, it is necessary to provide free patency of the respiratory ducts and oxygen supply, and also to monitor the respiratory processes of the patient. It is also necessary to determine whether it is necessary to receive activated charcoal and gastric lavage.

If there is a collapse with hypotension, you need to inject intravenously fluid or norepinephrine. After poisoning with the drug, the victim must be under constant supervision of specialists until a full recovery occurs.

[6], [7]

Interactions with other drugs

Because olanzapine has a primary effect on the central nervous system, the medication should be carefully combined with other drugs that have an effect on the central nervous system.

Since Zolafrene can lead to a decrease in pressure, it is able to potentiate the effect of individual antihypertensive drugs.

The drug has an antagonistic effect on the therapeutic effect of dopamine antagonists and levodopa.

Combination with a substance fluoxetine lowers the level of drug clearance; while carbamazepine has the opposite effect - it increases the values of Zolafren's clearance, like rifampicin and omeprazole.

Single portions of cimetidine, and in addition, oral magnesium or aluminum-containing antacids do not affect the level of bioavailability of the drug taken internally.

Clinical data and in vitro tests suggest that the drug does not affect the metabolic processes of most therapeutic drugs.

[8], [9]

Storage conditions

Zolafrene should be kept in a dry and dark place, closed from the infiltration of young children. The temperature is within the limits of 15-25 ° C.

[10],

Shelf life

Zolafrene can be used within 36 months from the date of manufacture of the drug.

Application for children

It is forbidden to prescribe drugs to people under the age of 18 years.

[11], [12]

Analogues

Analogues of the drug are medications Adagio, Azapine with Ziprexa, Azaleptin and Ketilept, and in addition Azaleptol with Hedonin, Clozapine with Zipreksoy adera and Quetiron. Also on the list are Olan, Leponeks, Seroquel and Nantarid, and also Skizoril, Olanzapin, Egolanza and Parnasan.