Tizercin - instructions for use, dose, side effects, contraindications

Active substanceLevomepromazineLevomepromazine

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Tizerzin®

solution w / m d / infusion

EGIS ZAO Pharmaceutical Plant Hungary

Tizerzin®

pills inwards

EGIS ZAO Pharmaceutical Plant Hungary

Dosage form: & nbspcoated tablets

Composition:

Active substance: 25 mg of levomepromazine (equivalent to 33.8 mg of levomepromazine hydro-maleate),

additives: magnesium stearate 1 mg, sodium starch glycolate 2 mg, povidone 8 mg, cellulose microcrystalline 10 mg, potato starch 15.2 mg, lactose 40 mg, shell tablets: titanium dioxide 0.758 mg, hypromellose 2.632 mg, dimethicone 0.355 mg, magnesium stearate 0.255 mg.

Description:Round, slightly biconcave coated tablets, white in color, odorless.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.A The phenothiazine derivatives with an aliphatic structure

N.05.A.A.02 Levomepromazine

Pharmacodynamics:Antipsychotic agent (antipsychotic) phenothiazine series. Has antipsychotic, sedative (hypnotics), analgesic, moderate antiemetic, hypothermic, moderate antihistaminic and M-cholinoblocking action. It causes a decrease in blood pressure (BP).

The antipsychotic effect is due to the blockade of dopamine D2-receptor mesolimbic and mesocortical system.

Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2-receptors of the trigger zone of the emetic center; hypothermic action - blockade of dopamine receptors of the hypothalamus.

Extrapyramidal side effects in levomepromazine are less pronounced than in "classical" neuroleptics. Levomepromazine increases the pain threshold. Due to the ability to enhance the effects of analgesics, this drug can be used for auxiliary therapy in acute and chronic pain syndrome.

Pharmacokinetics:

The maximum concentration of the drug in the blood plasma is achieved 1-3 hours after ingestion. Passes through the histohematological barriers, including the blood-brain barrier, distributed in organs and tissues.

Levomepromazine is rapidly metabolized in the liver by demethylation with the formation of sulfate and glucuronide conjugates, which are excreted in the urine. Metabolite, formed as a result of demethylation (N-desmetilon mono-metotrimeprazine), has pharmacological activity, other metabolites are inactive. A small part of the administered dose (1%) is excreted unchanged in urine and feces. The half-life is 15-30 hours.

Indications:

Psychomotor agitation of various etiologies:

- in schizophrenia (acute and chronic)

- in bipolar disorders

- at senile, intoxication and other psychoses

- with oligophrenia

- with epilepsy

as well as other mental disorders occurring with:

- agitation

- anxiety

- panic

- phobias

- resistant insomnia

Strengthening the action of analgesics, means for general anesthesia, antihistamines.

Pain syndrome (trigeminal neuralgia, facial nerve neuritis, shingles).

Contraindications:

- simultaneous administration of antihypertensive agents,

- increased sensitivity to phenothiazines,

- overdose of drugs that cause inhibition of the central nervous system (alcohol, general anesthetics, hypnotics),

- angle-closure glaucoma,

- retention of urine,

- Parkinson's disease,

- multiple sclerosis,

- myasthenia gravis, hemiplegia,

- chronic heart failure in the stage of decompensation,

- marked renal / hepatic insufficiency,

- severe arterial hypotension,

- oppression of bone marrow hematopoiesis (granulocytopenia),

- porphyria,

- lactation,

- children under 12 years.

Carefully:Epilepsy, patients with a history of cardiovascular disease, especially in the elderly (impaired conduction of the heart muscle, arrhythmias, congenital lengthening syndrome QT).

Pregnancy and lactation:Pregnancy

The drug should not be used during pregnancy, unless there is a careful comparison of the risk to the fetus and benefits to the mother.

Lactation

Levomepromazine penetrates into breast milk. In connection with this, as well as in the absence of controlled studies, its use in breastfeeding is contraindicated. If you need to take the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside, starting with a daily dose of 25-50 mg for several doses (the maximum part of the daily dose should be prescribed before bedtime), increasing it daily by 25-50 mg until the patient's condition improves.In patients resistant to other neuroleptics, the daily dose can be increased faster, adding 50-75 mg per day. The average daily doses are 200-300 mg.

After the patient's condition is improved, the dose should be reduced to a maintenance dose, the value of which is determined individually.

In outpatient practice, patients with neurotic disorders are prescribed in a daily dose of 12.5-50 mg (1 / 2-2 tablets).

Patients with psychoses, with expressed psychomotor agitation, it is advisable to begin therapy with levomepromazine from parenteral administration.

To prevent the development of orthostatic collapse during treatment requires compliance with bed rest.

Side effects:The cardiovascular system: the most frequent side effect is a decrease in blood pressure and orthostatic hypotension. Also possible tachycardia, Morgagni-Adams-Stokes syndrome, lengthening interval QT (arrhythmogenic effect, tachycardia of the "pirouette" type) (see also the section "Contraindications").

Hematopoietic system: pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia.

central nervous system: confusion, slurred speech,extrapyramidal symptoms with predominance of akineto-hypotonic syndrome, epileptic seizures, increased intracranial pressure, neuroleptic malignant syndrome (NZS).

Endocrine system and metabolism: galactorrhea, menstrual irregularities, weight loss. Some patients who have been receiving phenothiazines for a long time have described the development of pituitary adenoma, but further studies are needed to establish its causal relationship with these drugs.

Genitourinary system: discoloration of urine, urination disorders.

Gastrointestinal tract: dry mouth, discomfort in the abdomen, nausea, vomiting, constipation, liver damage (jaundice, cholestasis).

Skin Reactions: photosensitization, erythema, pigmentation.

Vision: with prolonged use of deposits in the lens and cornea, pigment retinopathy.

Allergic reactions: laryngeal edema, peripheral edema, anaphylactoid reactions, bronchospasm, urticaria, exfoliative dermatitis.

Other: hyperthermia (may be the first sign of NZS), pain and swelling at the injection sites.

Overdose:

Symptoms: Arterial hypotension, conduction disorders in the cardiac muscle (lengthening of the interval QT, ventricular tachycardia of the "pirouette" type, atrioventricular blockade), oppression of consciousness of varying severity (up to coma), extrapyramidal symptoms, sedative effect, epileptic seizures.

Treatment: resuscitation, symptomatic therapy.

Specific antidote is not known. Forced diuresis, hemodialysis and hemoperfusion are not effective.

Interaction:It is necessary to avoid simultaneous reception of the following means:
- Antihypertensive because of the risk of a marked decrease in blood pressure.
- MAO monoamine oxidase inhibitors, since it is possible to increase the duration of the effect of Tizercin® and the severity of its side effects.

Care should be taken when combining with the following:

- Anticholinergic drugs (tricyclic antidepressants, blockers H₁- histamine receptors; some anti-Parkinsonics; atropine, scopolamine, succinylcholine) due to increased anticholinergic effects (paralytic intestinal obstruction, urinary retention, glaucoma).When combined with scopolamine, extrapyramidal side effects were observed.

- The drugs that oppress the central nervous system (narcotic analgesics, general anesthetics, anxiolytics, sedatives and hypnotics, tranquilizers, tricyclic antidepressants) increase the inhibitory effect of the drug on the central nervous system.

- CNS stimulating agents (for example, amphetamine derivatives) - a decrease in the psycho-stimulating effect.

- Levodopa: the effect of this drug is weakened.

- Oral antidiabetics: their effectiveness is reduced, which requires dose adjustment.

- Means that extend the interval QT (some antiarrhythmic drugs, macrolide antibiotics, some antifungal azoles, cisapride, some antidepressants, some antihistamines, and diuretics that lower potassium levels) - increase the risk of lengthening the interval QT and, therefore, increase the risk of arrhythmia.

- Preparations that cause photosensitivity: this effect can increase.

- Alcohol: increased inhibition of the central nervous system and increased the likelihood of extrapyramidal side effects.

- Antacids: reduce absorption in the gastrointestinal tract (levomepromazine should be prescribed 1 hour before or 4 hours after taking antacid drugs).

Special instructions:

- Use of the drug should be discontinued in the event of an allergic reaction.

- In pregnancy, the drug should be given after a careful comparison of risk and benefit (see the section "Pregnancy and lactation period").

- Simultaneous use with agents oppressing the central nervous system, MAO inhibitors and anticholinergic substances requires special care (see section "Interactions").

- Particular caution is needed when prescribing drugs for patients with renal and / or liver failure due to the risk of cumulation of the drug.

- Elderly patients have a predisposition to orthostatic hypotension, as well as anticholinergic and sedative effects of phenothiazines. In addition, they often have extrapyramidal side effects. Therefore, low initial doses and their gradual increase are especially important in this category of patients.

- To avoid the development of orthostatic hypotension, the patient should lie for half an hour after the administration of the first dose. If after the introduction of the drug there is dizziness, you should observe bed rest after each dose.

- If there is hyperthermia during antipsychotic therapy, it is necessary to exclude malignant neuroleptic syndrome (NZS). NZS is a deadly disease characterized by the following symptoms: hyperthermia, muscle stiffness, confusion, dysfunction of the autonomic nervous system (unstable blood pressure, tachycardia, arrhythmia, increased sweating), increasing the concentration of creatine phosphokinase (CK), myoglobinuria (rhabdomyolysis), and acute renal failure. If they occur, and if during the treatment there is a hyperthermia of unclear etiology without the remaining clinical symptoms of NZS, the administration of Tizerincin® should be stopped immediately.

- After a sudden discontinuation of the drug, used in high doses or for a long time, nausea, vomiting, headache, tremor, increased sweating, tachycardia, insomnia and anxiety, as well as the development of tolerance to the sedative effects of phenothiazines and cross tolerance to various antipsychotics. For this reason, the drug should be discontinued gradually.

- Many antipsychotics, including levomepromazine, can reduce the threshold of convulsive readiness and cause epileptiform changes in the EEG. Therefore, when selecting a dose of Tizercin® in patients with epilepsy, clinical indicators and EEG should be constantly monitored.

- The development of cholestatic jaundice depends on the individual sensitivity of the patient and completely disappears after discontinuation of the drug administration. Therefore, long-term treatment requires regular monitoring of liver function.

- With prolonged therapy, regular monitoring of the blood formula is recommended.

- It is necessary to prohibit the use of alcoholic beverages during treatment and until the effects of the drug disappear (within 4-5 days after the discontinuation of the administration of Tizerincin®).

It is recommended that the following indicators be regularly monitored before and during treatment:

- arterial pressure,

- liver function (especially in patients with liver disease),

- the formula of blood,

- ECG (for cardiovascular diseases and in elderly patients).

Effect on the ability to drive transp. cf. and fur:During the treatment period, you should refrain from driving the car and performing work associated with an increased risk of accidents.

Form release / dosage:The coated tablets are 25 mg.

Packaging:

For 50 tablets in a bottle of brown glass with PE cover, with the control of the first opening and shock absorber-accordion. 1 bottle with instructions for use in a cardboard box.

Storage conditions:

The drug belongs to the list of 1 potent substances of the Standing Committee on Drug Control M3 RF.

Store at 15-25 ° C, out of the reach of children.

Shelf life:5 years. Shelf life is indicated on the box. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011307 / 01

Date of registration:25.02.2010

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS PHARMACEUTICALS, Plc Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp29.10.2015

Illustrated instructions

Instructions

Tizerzin® (Tisercin®)