Tizercin® [Levomepromazine]

Pharmacological properties

Tizercin is an antipsychotic of the phenothiazine series, which has an antipsychotic, analgesic and moderate antiemetic effect. relieves psychomotor agitation, has a sedative effect, exhibits antidepressant, adrenergic blocking, moderate anticholinergic and antihistamine activity. causes hypotension.

The maximum concentration in the blood plasma is reached 30–90 minutes after the i / m administration. The metabolite formed as a result of demethylation has pharmacological activity, others are inactive. The elimination half-life is 15–78 hours. It is eliminated with urine and feces.

Indications

Psychomotor agitation of various etiologies: manic stage of manic-depressive psychosis, depressive-paranoid form of schizophrenia, catatonic agitation, reactive depression, alcoholic psychosis and other psychotonic conditions, accompanied by anxiety, fear;

neurotic disorders with increased excitement, sleep disturbance;

diseases accompanied by pain: trigeminal neuralgia, herpes zoster, etc .;

itchy dermatoses (as a means of adjunctive therapy);

epilepsy, oligophrenia (as part of combination therapy);

to potentiate the effects of analgesics, anesthetics.

Application

In psychotic conditions, the daily dose is 25-50 mg (1-2 tablets), if necessary, the dose can be increased to 150-250 mg / day (6-10 tablets per day). You can not take 10 tablets per day.

To reduce anxiety, the initial daily dose is 12.5–25 mg (¹/₂-1 tablet) per day. If necessary, this dose can be increased to 75-100 mg / day (3-4 tablets per day). After improving the condition, the dose can be reduced and the maintenance dose selected.

Parenteral administration of the drug is indicated in cases where oral administration is not possible. The daily dose is usually 75-100 mg 1-2 times a day (3-4 ml of the drug) under the control of blood pressure and heart rate. Injections must be done deeply in oil. With iv administration, the solution should be diluted and administered only in the form of a drip infusion (50-100 mg of the drug in 250 ml of isotonic sodium chloride solution or glucose solution).

Contraindications

Tablets and tizercin solution should not be used:

with an allergy to phenothiazine or any of the ingredients that make up the drug;

during pregnancy (or planning) or breastfeeding;

with severe liver disease, changes in blood counts, circulatory failure;

in case of a sudden decrease in blood pressure;

in the treatment of an antidepressant belonging to MAO inhibitors;

in the treatment of drugs to reduce blood pressure (especially guanethidine and an ACE inhibitor).

The drug should not be administered to children and persons who are unconscious, intoxicated or under the influence of drugs.

Side effects

The most common side effect is postural hypotension. in this case, loss of consciousness, dizziness, drowsiness, or increased fatigue may occur. in addition, side effects such as dry mouth, tachycardia, constipation and / or difficulty urinating may be noted. cases of impotence, frigidity, and cessation of menstrual bleeding were noted.

In some cases, the blood composition changed and neurological symptoms occurred (extrapyramidal disorders are possible with a predominance of the akinetic-hypotonic syndrome, for example, inability to stand still, tremor). Also, allergic reactions and photosensitization reactions can sometimes develop.

special instructions

If the patient has already taken MAO inhibitors, then before starting treatment with tisercin, it is necessary to take a break of at least 14 days, during which not to take any medication.

Before and during treatment, the composition of peripheral blood and the functional state of the liver, kidneys, heart should be regularly monitored, and in elderly patients, blood pressure.

During treatment, the use of alcoholic beverages is prohibited.

In debilitated and elderly patients, it is recommended to reduce the dose.

At the beginning of treatment, patients taking the drug should refrain from potentially hazardous activities that require increased attention and a quick reaction. In the future, these restrictions depend on the individual reaction to the drug.

Interactions

MAO inhibitors increase the risk of extrapyramidal disorders during treatment with tisercin due to a decrease in inactivation of the drug in the liver.

The simultaneous administration of Tizercin and drugs that depress the central nervous system, leads to an increase in central depressive action. Tizercin blocks dopaminergic receptors and therefore has an antagonistic effect when used simultaneously with levodopa. Under the influence of Tizercin, the antiparkinsonian effect of levodopa is sharply reduced.

With the simultaneous use of Tizercin and antihypertensive drugs, the risk of orthostatic hypotension increases.

Overdose

Symptoms: convulsive syndrome, coma.

Treatment: resuscitation and symptomatic therapy.

Storage conditions

In the dark place at a temperature of 15-25 ° C.