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

Active substanceChlorpromazineChlorpromazine

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Aminazine®

pills inwards

VALENTA PHARM, PAO Russia

Aminazine

solution w / m in / in

VALENTA PHARM, PAO Russia

Aminazine®

pills inwards

VALENTA PHARM, PAO Russia

Chlorpromazine hydrochloride

solution w / m in / in

Health to the people - Kharkov Pharmaceutical Enterprise, LLC Ukraine

Dosage form: & nbsppills

Composition:

One dragee contains:

active substance: chlorpromazine hydrochloride in terms of 100% substance 0.025 g (25 mg) or 0.05 g (50 mg) or 0.1 g (100 mg);

Excipients: sucrose (sugar) 0.211335 g or 0.282358 g or 0.37385 g, starch treacle 0.011651 g or 0.015778 g or 0.022461 g, gelatin 0.000119 g or 0.000166 g or 0.000239 g, wax 0.0000325 g or 0.0000455 g or 0.000065 g, talc 0.0000325 g or 0.0000455 g or 0.000065 g, titanium dioxide 0.00178 g or 0, 00127 g or 0.00019 g, sunflower oil 0.00005 g or 0.00007 g or 0.0001 g iron oxide red oxide (for dragees 50 mg and 100 mg) 0.000267 g or 0.00303 g.

Description:The dragees are spherical in white (for a dosage of 25 mg), brownish-pink (for a dosage of 50 mg) and brown (for a dosage of 100 mg). Droplets of brown and brownish-pink color of a darker color are allowed on the surface.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.A.01 Chlorpromazine

Pharmacodynamics:

Aminazine® (chlorpromazine) - antipsychotic agent (neuroleptic), from the group of aliphatic derivatives of phenothiazine

Has a pronounced antipsychotic and sedative effect, reduces motor activity, increases the duration and intensity of the action of hypnotics, analgesics, local anesthetics, anticonvulsants and alcohol, causes extrapyramidal disorders, increases the secretion of prolactin by the pituitary gland. The mechanism of antipsychotic action of Aminazina® is associated with the blocking of postsynaptic mesolimbic and mesocortical dopaminergic receptors in the brain. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brain stem. The drug has antiemetic effect (blockade of dopamine D₂receptors of the trigger zone of the vomiting center) and soothes hiccups. Also, Aminazine ® has hypothermic action (blockade of dopamine receptors of the hypothalamus), has a pronounced α-adrenoblocking effect with a weak effect on cholinergic receptors. It reduces or eliminates the increase in blood pressure and other effects caused by epinephrine (the hyperglycemic effect of epinephrine is not eliminated). Has a strong cataleptogenic effect.

Aminazine ® inhibits interoceptive reflexes, reduces the permeability of capillaries, has a weak antihistamine effect. Under the influence of Aminazina®, blood pressure decreases, tachycardia often develops. Aminazine® has a locally irritating effect.

Pharmacokinetics:After ingestion, it is not absorbed completely. The maximum concentration in the blood plasma is noted 2-4 hours after ingestion. More than 90 % it binds to blood plasma proteins, so it practically does not undergo hemodialysis.

Quickly removed from the circulatory system and unevenly accumulated in various organs. Easily penetrates the blood-brain barrier, while its concentration in the brain exceeds the concentration in the plasma. There is no direct correlation between the concentrations in the blood plasma of chlorpromazine and its metabolites and the therapeutic effect.

Has the effect of "first passage" through the liver, where the drug is intensively metabolized as a result of oxidation (30%), hydroxylation (30%) and dezamethylation (20%). Pharmacological activity is possessed by oxidized hydroxylated metabolites,which are inactivated by binding to glucuronic acid, or by further oxidation to form inactive sulfoxides. It is excreted by the kidneys and with bile. The half-life period averages 30 hours. Per day displays about 20 % of the accepted dose, 1-6 % dose is excreted in the urine in an unchanged form. Traces of chlorpromazine metabolites can be detected in the urine after 12 months or more after discontinuation of treatment.

Indications:

In psychiatric practice, Aminazin® is used in various types of psychomotor agitation and psychotic states in patients with schizophrenia, manic agitation in manic-depressive psychosis and in other mental illnesses of different genesis, accompanied by fear, anxiety, agitation, insomnia; in mood disorders in psychopathies, in psychotic disorders in patients with epilepsy and organic diseases of the central nervous system, to alleviate withdrawal conditions for alcoholism and substance abuse.

Persistent hiccups.

To enhance the action of analgesics with persistent pain.

Diseases accompanied by increased muscle tone (after disorders of cerebral circulation, etc.).

Contraindications:

- Increased individual sensitivity;

- oppression of the central nervous system and comatose states of any etiology;

- brain trauma;

- diseases of the liver, kidneys and hematopoietic organs with impaired functions;

- progressive systemic diseases of the brain and spinal cord;

- with peptic ulcer of the stomach and duodenum in the period of exacerbation;

- heart disease in the stage of decompensation (heart defects, myocardial dystrophy, rheumatic carditis, etc.), severe arterial hypotension, diseases accompanied by a risk of thromboembolic complications;

- bronchoectatic disease in the stage of decompensation;

- angle-closure glaucoma (risk of increased intraocular pressure);

- hyperplasia of the prostate;

- myxedema;

- pregnancy, the period of breastfeeding;

- children up to 3 years.

Carefully:Parkinson's disease, active alcoholism (risk of hepatotoxic effects), breast cancer, epilepsy, chronic diseases accompanied by breathing disorders (especially in children), Reye syndrome, cachexia, elderly age, vomiting (antiemetic effect of phenothiazines can mask vomiting associated with overdose other drugs).

Dosing and Administration:

Dragee Aminazin® is prescribed inside (after eating), without chewing, squeezed with enough water.

The initial daily dose for ingestion is 25-100 mg / day 1-4 times a day, then, taking into account the tolerability, the dose is gradually increased by 25-50 mg every 3-4 days, until the desired therapeutic effect is achieved. In case of ineffective average doses of aminazine, the dose is increased to 700-1000 mg / day, in some, extremely resistant cases without somatic contraindications, the dose can be increased to 1200-1500 mg / day. When treated in large doses, the daily dose is divided into 4 parts (the last - before going to bed). The duration of treatment with large doses should not exceed 1-1.5 months, in the absence of effect, it is advisable to switch to treatment with other drugs.

Higher doses of Aminazine® for adults inside: single 0.3 g, daily 1.5 g.

Children Aminazin® is prescribed depending on the age: from 3 years old and upwards inside by

550 μg / kg (0.55 mg / kg) or 15 mg per 1 m of body surface if necessary every 6-8 hours.

Children 3-5 years old (body weight up to 23 kg) should not be administered more than 40 mg per day; children 5-12 years (body weight from 23 to 46 kg) should not be administered more than 75 mg per day.

For use in pediatric practice, it is advisable to use dosage forms for children.

Weakened and elderly patients, depending on the age, appoint up to 0.3 g / day.

Side effects:

After applying the drug, regardless of the method of administration, patients should lie for 1.5-2 hours; A sharp transition to a vertical position can cause an orthostatic collapse.

The use of aminazine ® is often accompanied by extrapyramidal disorders (dyskinesias, akipeto-rigidity phenomena, akathisia, hyperkinesia, tremor, vegetative disorders), in single cases convulsions. As correctors used atiparkinsonic means - tropacin, trihexyphenidyl (cyclodol), etc. Dyskinesia paroxysmally arising cramps in the muscles of the neck, tongue, bottom of the mouth, oculogic crises) are stopped by caffeine-benzoate sodium (2 ml 20% solution subcutaneously) and atropine (1 ml, 1 % solution subcutaneously).

With prolonged reception, it is possible to develop tardive dyskinesia, less often malignant neuroleptic syndrome.

At the beginning of treatment, drowsiness, dizziness, dry mouth, anorexia, accommodation disorders, mild orthostatic hypotension, tachycardia, dry mouth, sleep disorders, difficulty urinating, constipation may occur.

Also, cardiac rhythm disturbances are possible (risk of ventricular rhythm disturbances, especially in the background of initial bradycardia, hypokalemia, elongated RT), nausea, vomiting, diarrhea, hyperprolactinaemia, galactorrhea, gynecomastia, amenorrhea, oliguria, impotence, frigidity.

There may be allergic reactions from the skin and mucous membranes, angioedema, facial edema, and photosensitization of the skin (patients should not therefore be exposed to UV radiation).

When using Aminazina®, there may appear phenomena of psychic indifference, a belated reaction to external stimuli and other changes in the psyche. When using Aminazina ®, there may be a so-called neuroleptic depression. To reduce neuroleptic depression, antidepressants and stimulants of the central nervous system are used.

After prolonged use of large doses of Aminazina® (0.5-1.5 g per day), cholestatic jaundice, increased coagulability of the blood, lympho- and leukopenia, anemia, agranulocytosis, skin pigmentation, clouding of the lens and cornea, melanosis can be observed.

Overdose:

Symptoms: areflexia or hyperreflexia, blurred vision, cardiotoxic action (arrhythmia, heart failure, lowering blood pressure, shock, tachycardia, tooth change QRS, ventricular fibrillation, cardiac arrest), neurotoxic effects, including agitation, confusion, convulsions, disorientation, drowsiness, stupor or coma; mydriasis, dry mouth, hyperpyrexia or hypothermia, muscle stiffness, vomiting, pulmonary edema, or respiratory depression. Treatment: gastric lavage, the appointment of activated charcoal (avoiding the induction of vomiting, as impaired consciousness and dystonic reactions from the muscles of the neck and head caused by an overdose can lead to aspiration of vomit). Symptomatic treatment: with arrhythmia - in / in phenytoin 9-11 mg / kg, with heart failure - cardiac glycosides, with a pronounced decrease in blood pressure - iv injection of liquid or vasopressor agents such as norepinephrine, phenylephrine (avoid the appointment of alpha and beta-adrenomimetics, such as epinephrine, since a paradoxical decrease in blood pressure is possible due to the blockade of alpha-adrenergic receptors with chlorpromazine), with convulsions - diazepam (avoid the appointment of barbiturates, due to possible subsequent depression of the central nervous system and respiratory depression), with parkinsonism - diphenyltropine, diphenhydramine. Control of cardiovascular function for at least 5 days, functions of the central nervous system, respiration, measurement of body temperature, consultation of a psychiatrist. Dialysis is ineffective.

Interaction:

With the simultaneous use of Aminazina ® with other drugs that have a depressing effect on the central nervous system (drugs for general anesthesia, narcotic analgesics, ethanol (alcohol) and containing drugs, barbiturates, tranquilizers, etc.) may increase the depression of the central nervous system, as well as respiratory depression; undesirable long-term combination with analgesics and antipyretics - it is possible to develop hyperthermia with tricyclic antidepressants, maprotiline or MAO inhibitors - an increased risk of neuroleptic malignant syndrome; with anticonvulsants - it is possible to lower the convulsive threshold; with drugs for the treatment of hyperthyroidism - the risk of advanced agranulocytosis increases; with other drugs that cause extrapyramidal reactions - it is possible to increase the frequency and severity of extrapyramidal disorders;

with antihypertensive drugs - possible pronounced orthostatic hypotension; with ephedrine - it is possible to weaken the vasoconstrictive effect of ephedrine.

In the treatment of Aminazine®, epinephrine (adrenaline) should be avoided, since the effect of epinephrine may be distorted, which can lead to a drop in blood pressure. The antiparkinsonian action of levodopa is reduced due to the blocking of dopamine receptors. Aminazine ® can suppress the effects of amphetamines, clonidine, guanetidine.

Aminazine ® enhances the anticholinergic effects of other drugs, while the antipsychotic effect of the antipsychotic may decrease.

With the simultaneous use of Aminazina® with a prochlorperazine related to the chemical structure, a prolonged loss of consciousness may occur.

Antacids, antiparkinsonian drugs and lithium salts can reduce the absorption of chlorpromazine, in addition, the combination with lithium drugs increases the risk of extrapyramidal complications.

Chlorpromazine can mask some manifestations of ototoxicity (tinnitus, dizziness) of drugs that have ototoxic effect (eg antibiotics with ototoxic effect).

Other hepatotoxic drugs increase the risk of hepatotoxicity.

Means that inhibit bone marrow hematopoies increase the risk of myelosuppression.

Special instructions:

During treatment it is necessary to carry out regular monitoring of blood pressure, pulse and liver, kidney and blood functions.

During the treatment period, do not use alcohol.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Dragee 25 mg, 50 mg and 100 mg.

Packaging:

For 10 dragees in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

3, 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

For 100 contour mesh packages with an equal number of instructions for use in carton boxes or in polyethylene film bags.

For 3200 pieces ± 5% (25 mg dosage), 2285 pieces ± 5% (50 mg dosage), 1600 pieces + 5% (100 mg dosage) in polymer cans made of polyethylene, with parchment or parchment paper package .

18 polymer cans with instructions for use in transport containers (for hospitals).

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Shelf life 5 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000595 / 01

Date of registration:01.03.2011

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp07.08.2017

Illustrated instructions

Instructions

Aminazine® (Aminazine®)