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: & nbspsolution for intravenous and intramuscular administration

Composition:

In 1 ml of solution contains: active substance: chlorpromazine hydrochloride in terms of 100% substance (aminazine) - 25.0 mg; Excipients: nagriya sulfite anhydrous - 1,0 mg, sodium disulfite 1.0 mg, ascorbic acid 2.0 mg, sodium chloride 6.0 mg, water for injection up to 1.0 ml.

Description:

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.A.01 Chlorpromazine

Pharmacodynamics:

Antipsychotic agent (neuroleptic), a phenothiazine derivative with an aliphatic side chain. Has a pronounced antipsychotic, sedative, antiemetic, vasodilating (alpha-adrenoblokiruyuschim), moderate M-holinoliticheskim, as well as a weak hypothermic effect, soothes hiccups; has a locally irritating effect.

The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical system.Antipsychotic effect is manifested in the elimination of productive symptoms of psychosis (delirium, hallucinations). Suppresses various types of psychomotor agitation, reduces psychotic fear, aggressiveness.

Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brain stem. One of the main features of Aminazine (in comparison with other phenothiazines) is the presence of a pronounced sedative effect, manifested by inhibition of conditioned reflex activity (primarily motor defensive reflexes), a decrease in spontaneous motor activity, relaxation of skeletal muscles, a decrease in sensitivity to endogenous and exogenous stimuli with conserved consciousness.

Start sedation after 15 minutes after intramuscular injection.

Antiemetic effect is due to blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.

Aminazine reduces the permeability of capillaries, lowers blood pressure, has a weak antihistamine effect. Has a local irritant effect.

Pharmacokinetics:

Good and quickly absorbed after intramuscular injection. The maximum concentration in the blood plasma after intramuscular injection is achieved after 1-2 hours. Connection with blood plasma proteins - 90-99%. Quickly removed from the bloodstream, 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 plasma concentration and therapeutic effect.

Has the effect of "first pass" through the liver, where the drug is intensely metabolized by oxidation (30%), hydroxylation (30%) and desmethylation (20%). Pharmacological activity has hydroxylated metabolites that are inactivated by binding to glucuronic acid, or by further oxidation with formation of inactive sulfoxides.

It is excreted by the kidneys and with bile. The half-life is 15-30 hours. For a day about 20% of the dose received, 1-6% of the dose is excreted by the kidneys in an unchanged form. Traces of metabolites can be detected in the urine after 12 months or more after discontinuation of treatment.Due to high binding to proteins, it is practically not eliminated during hemodialysis.

Indications:

Use strictly according to the doctor's prescription to avoid complications!

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

In therapeutic, neurological and surgical practice Aminazine is used to stop psychomotor agitation; as an antiemetic (including surgical intervention), a means to enhance the action of analgesics in case of persistent pain, with diseases accompanied by increased muscle tone (after cerebral blood flow disorders, etc.), to calm the hiccups, to lower body temperature in anesthesiology in the so-called "lytic mixtures".

Contraindications:

- Increased individual sensitivity;

- Chronic heart failure (decompensation);

- arterial hypotension;

- marked suppression of central nervous system function and coma of any etiology;

- craniocerebral trauma;

- progressive systemic diseases of the brain and spinal cord;

- pregnancy, lactation period

- Children's age (up to 6 months).

Carefully:

Active alcoholism (increased likelihood of developing hepatotoxic reactions), pathological changes in blood levels (hemopoiesis), breast cancer (tumor growth progression and resistance to endocrine and cytostatic drugs), closed-angle glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and / or kidney failure; diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease, epilepsy, myxedema, chronic diseases accompanied by respiratory failure (especially in children), Reye's syndrome in the anamnesis (increased risk of developing hepatotoxicity in children and adolescents); cachexia,vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other medicines), elderly age.

Pregnancy and lactation:

Aminazine penetrates the placental barrier, is excreted in breast milk, has a teratogenic effect, prolongs labor. Application during pregnancy is contraindicated. If you need to use the drug during lactation at the time of treatment should stop breastfeeding.

Dosing and Administration:

The drug is administered intramuscularly and intravenously in the form of a 2.5% solution (25 mg / ml).

With intramuscular injection dilute 2-5 ml of 0.25-0.5% solution of novocaine (procaine) or 0.9% solution of sodium chloride. The solution is injected deep into the muscle.

When administered intravenously, the required amount of solution is diluted with 20 ml of a 5% dextrose solution or 0.9% sodium chloride solution. Enter slowly, for 5 minutes under the control of blood pressure.

When administered intramuscularly, the daily dose usually does not exceed 600 mg. The course of treatment is from 2 weeks to 2-4 months or more. Until the end of the course of treatment, the dose of the drug is gradually reduced (by 25-50 mg per day).

When expressed psychomotor agitation, convulsive syndrome, vomiting, a single initial dose with intramuscular injection is 100-150 mg. For relief of acute excitement, Aminazine is administered to a vein in doses of 50-75 mg (2-3 ml of a 2.5% solution) 1-2 times per day.

Higher doses of aminazine for adults intravenously: single dose - 100 mg, daily - 250 mg, intramuscularly: single-dose 150 mg, daily - 1000 mg.

Children Aminazine is prescribed depending on the age: from 3 years and older intramuscularly at 0.55 mg / kg or 15 mg /m²body surface if necessary every 6-8 hours.

Children under 5 years old (body weight up to 23 kg) - should not be administered more than 40 mg / day, from 5 to 12 years (body weight 23-46 kg) - 75 mg / day.

Weakened and elderly patients, depending on the age, appoint up to 300 mg / day.

For the relief of psychomotor agitation in cases of cerebral circulation, hiccup attacks and indomitable vomiting, Aminazine is used in the so-called "lytic mixtures" containing 1-2 ml of a 2.5% solution of Aminazine, 2 ml of a 2.5% solution of diprazine or 2 ml 2% solution of dimedrol, 1 ml of a 2% solution of promedol. The mixture is administered intravenously or intravenously 1-2 times a day.

Side effects:

At the beginning of treatment can be observed drowsiness, dizziness, dry mouth,loss of appetite, constipation, paresis of accommodation, moderately pronounced orthostatic hypotension, tachycardia, sleep disorders, difficulty urinating, decreased potency, frigidity, allergic reactions from the skin and mucous membranes (photosensitivity, angioedema and facial edema); less often - a sharp drop in blood pressure.

With long-term use in high doses (0.5-1.5 g / day) - extrapyramidal disorders (dyskinesia - paroxysmally arising cramps of the muscles of the neck, tongue, bottom of the oral cavity, akinetorhidic phenomena, akathisia, hyperkinesia, tremor and vegetative disorders), phenomena psychic indifference, belated reaction to external stimuli, neuroleptic depression, cholestatic jaundice, cardiac arrhythmias, lympho- and leukopenia, anemia, agranulocytosis, hypercoagulation, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, ota, vomiting, diarrhea, oliguria, skin pigmentation, clouding of the lens and cornea; in isolated cases - convulsions (as correctors used antiparkinsonian drugs - tropachin, trihexyphenidyl and other; dyskinesias are suppressed by subcutaneous injection of 2 ml of 20% caffeine-benzoate sodium solution and 1 ml of 0.1% atropine solution), malignant neuroleptic syndrome.

Local reactions: with intramuscular injection, infiltrates may occur, with intravenous injection - phlebitis, in case of contact with the skin and mucous membranes - tissue irritation.

When neuroleptics of the phenothiazine series are taken, cases of sudden death (including possibly caused by cardiac causes) are noted; can prolong the interval QT - the risk of ventricular rhythm disturbances (especially against the background of the initial bradycardia, hypokalemia, elongated QT).

Overdose:

Symptoms: areflexia or hyperreflexia, blurred vision, mydriasis, dry mouth, hyperpyrexia or hypothermia, muscle stiffness, vomiting, respiratory depression, possible pulmonary edema;

cardiotoxic action (development of circulatory insufficiency, arterial hypotension, shock, rhythm disturbance (tachycardia, QRS tooth change, ventricular fibrillation, asystole);

neurotoxic effect (agitation, confusion, convulsions, disorientation, drowsiness, stupor or coma).

Treatment:

When arrhythmia - intravenous phenytoin 9-11 mg / kg, with circulatory failure - cardiac glycosides, with a marked decrease in blood pressure - intravenous fluid or vasopressor drugs such as norepinephrine, phenylephrine (avoid the appointment of alpha and beta-adrenomimetics, such as epinephrine, since it is possible a paradoxical reduction in blood pressure due to blockade of alpha-adrenergic receptors with chlorpromazine), with convulsions - diazepam (avoiding the appointment of barbiturates due to possible subsequent depression of the central nervous system and respiratory depression), Parkinsonism - diphenyltropine, diphenhydramine.

Control of cardiovascular function for at least 5 days, central nervous system function, respiration, body temperature measurement, psychiatrist consultation. Dialysis is ineffective.

Interaction:

Aminazine weakens the vasoconstrictive effect of ephedrine.

May mask some manifestations of ototoxicity (tinnitus, dizziness) of ototoxic drugs, especially antibiotics.

Reduces the antiparkinsonian effect of levodopa (due to the blockade of dopamine receptors), as well as the effects of amphetamines, clonidine and guanethidine.

Strengthens the anticholinergic effects of other drugs, while its own antipsychotic effect may decrease.

With the simultaneous use of aminazine with a related chemical structure of prochlorperazine, an overdose and prolonged loss of consciousness may occur. Compatible with other antipsychotic drugs, anxiolytics and antidepressants.

Undesirable prolonged combination with analgesics and antipyretics (hyperthermia may develop).

When used simultaneously with other drugs that have a depressing effect on the central nervous system (general anesthetic agents, anticonvulsant drugs, narcotic analgesics, ethanol and drugs containing it, barbiturates and other sleeping pills, anxiolytics, (tranquilizers), and others), it is possible to enhance and prolong the depressant effect, as well as respiratory depression.The appointment together with tricyclic antidepressants, maprotiline or monoamine oxidase inhibitors increases the risk of developing a malignant neuroleptic syndrome.

With drugs for the treatment of thyrotoxicosis increases the risk of agranulocytosis.

With other drugs that cause extrapyramidal reactions, Aminazine increases the incidence and severity of extrapyramidal disorders.

With hypotensive drugs increases the severity of lowering blood pressure in orthostasis.

Antacids, antiparkinsonian, lithium preparations may interfere with the absorption of aminazine.

Hepatotoxic drugs when used together with Aminazine increase the risk of developing toxic effects on the liver.

Against the background of the treatment with aminazine should avoid the introduction of epinephrine (due to the possibility of distortion of the effect of epinephrine and further decrease in blood pressure).

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

Special instructions:

During treatment, it is necessary to monitor blood pressure, pulse, and regularly monitor liver, kidney and blood.

To avoid a sharp decrease in blood pressure after intramuscular or intravenous administration, the procedure is performed in the patient's "lying" position, after using the drug, patients should remain in the "lying" position for at least 1.5-2 hours (a sharp transition to the vertical position may cause an orthostatic collapse ). Patients should not be exposed to ultraviolet radiation, since the drug can cause photosensitization.

During the treatment should not allow the use of ethanol.

It is necessary to exclude the possibility of getting the drug on the skin and mucous membranes.

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

Aminazine can not be assigned during work to drivers of vehicles and people whose profession requires increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 25 mg / ml.

Packaging:

AT ampoules of 1 ml, 2 ml, 5 ml or 10 ml. For 10 ampoules together with the instruction for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard, or 5 or 10 ampoules per contour cell pack.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampoule in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Storage conditions:

In the dark place at a temperature of 5 to 25 ° C.

Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:P N000302 / 01

Date of registration:23.08.2011 / 08.12.2016

Expiration Date:Unlimited

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

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp07.08.2017

Illustrated instructions

Instructions

Aminazine (Aminazine)