Aminazine - instructions for use, analogs, reviews and release forms (pills or tablets 25 mg, 50 mg and 100 mg, injections in injections 2.5%) for the treatment of psychoses in adults, children and pregnancy. Interaction with alcohol

In this article, you can read the instructions for using the drug Aminazine. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors specialists on the use of Aminazine in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Aminazine in the presence of existing structural analogues. Use to treat psychoses and schizophrenia in adults, children, as well as during pregnancy and breast-feeding. Interaction of the drug with alcohol.

Aminazine - antipsychotic agent (neuroleptic) from the group of phenothiazine derivatives. Has a pronounced antipsychotic, sedative, antiemetic effect. Relaxes or completely eliminates delirium and hallucinations, stops psychomotor agitation, reduces affective reactions, anxiety, anxiety, reduces motor activity.

The mechanism of antipsychotic action is associated with the blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain. It also has a blocking effect on alpha-adrenoceptors and inhibits the release of pituitary and hypothalamic hormones. However, blockade of dopamine receptors increases the secretion of the pituitary gland prolactin.

The central antiemetic effect is caused by oppression or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, peripheral by the blockade of the vagus nerve in the digestive tract. Antiemetic effect is enhanced, apparently due to anticholinergic, sedative and antihistamine properties. Sedative action is due, apparently, to alpha-adrenoblocking activity. Has a moderate or weak extrapyramidal effect.

Composition

Chlorpromazine + auxiliary substances.

Pharmacokinetics

When ingestion Aminazine quickly, but sometimes not completely absorbed from the digestive tract. Exposed to the effect of "first passage" through the liver. In connection with this effect, plasma concentrations after ingestion are less than those after intramuscular injection. Intensively metabolized in the liver with the formation of a number of active and inactive metabolites. Pathways of chlorpromazine metabolism include hydroxylation, conjugation with glucuronic acid, N-oxidation, oxidation of sulfur atoms, dealkylation. Chlorpromazine has a high binding to plasma proteins (95-98%). Widely distributed in the body, penetrates the blood-brain barrier (BBB), while the concentration in the brain is higher than in the plasma.

Indications

• chronic paranoid and hallucinatory-paranoid conditions;
• the state of psychomotor agitation in schizophrenia (hallucinatory-delirious, hebephrenic, catatonic syndromes);
• alcoholic psychosis;
• Manic agitation in manic-depressive psychosis;
• mental disorders in epilepsy;
• agitated depression in patients with presenile psychosis, manic-depressive psychosis, as well as in other diseases accompanied by excitation, stress;
• neurotic diseases accompanied by increased muscle tone;
• persistent pain, incl. causalgia (in combination with analgesics);
• sleep disturbances of a persistent nature (in combination with sleeping pills and tranquilizers);
• Meniere's disease;
• vomiting of pregnant women;
• treatment and prevention of vomiting in the treatment of antitumor agents and radiation therapy;
• itching dermatoses;
• in the composition of "lytic mixtures" in anesthesiology.

Forms of release

Dragee 25 mg, 50 mg and 100 mg (sometimes mistakenly called tablets).

Solution for intravenous and intramuscular injection 2.5% (injections in ampoules for injection).

Instructions for use and effective doses

It is installed individually. When administered orally for adults, a single dose is 10-100 mg, a daily dose of 25-600 mg; for children aged 1-5 years - 500 μg / kg every 4-6 hours, for children older than 5 years, you can use 1 / 3-1 / 2 of the adult dose.

With intramuscular or intravenous administration for adults, the initial dose is 25-50 mg.With a / m or / in the introduction of children older than 1 year, a single dose is 250-500 mcg / kg.

The frequency of oral or parenteral use depends on the indications and the clinical situation.

The maximum single doses: for adults with oral administration - 300 mg, with the / m introduction - 150 mg, with the / in the introduction - 100 mg.

The maximum daily doses: for adults with oral administration - 1.5 g, with the / m introduction - 1 g, with the / in the introduction - 250 mg; for children under 5 years old (body weight up to 23 kg) when ingested, in / m or / in the introduction - 40 mg, for children over the age of 5 years (body weight more than 23 kg) with oral administration, in / m or in / in the introduction - 75 mg.

Side effect

• blurred vision;
• dystonic extrapyramidal reactions;
• parkinsonian syndrome;
• tardive dyskinesia;
• thermoregulation disorders;
• convulsions;
• arterial hypotension (especially with intravenous administration);
• tachycardia;
• dyspeptic phenomena (with oral administration);
• cholestatic jaundice;
• leukopenia, agranulocytosis;
• difficulty urinating;
• menstrual cycle disorders;
• impotence;
• gynecomastia;
• increase in body weight;
• skin rash;
• itching;
• exfoliative dermatitis;
• erythema multiforme;
• skin pigmentation;
• photosensitization;
• deposition of chlorpromazine in the anterior structures of the eye (cornea and lens), which can accelerate the processes of normal lens aging.

Contraindications

• violations of the liver, kidneys, hematopoietic organs;
• progressive systemic diseases of the brain and spinal cord;
• myxedema;
• severe cardiovascular diseases;
• thromboembolic disease;
• late stage of bronchiectasis;
• angle-closure glaucoma;
• urinary retention associated with prostatic hyperplasia;
• marked depression of the central nervous system;
• coma;
• brain injury.

Application in pregnancy and lactation

If you need to use Aminazine during pregnancy, you should limit the treatment period, and at the end of pregnancy, if possible, reduce the dose. It should be borne in mind that chlorpromazine prolongs childbirth.

If it is necessary to use lactation, breastfeeding should be discontinued.

Aminazine and its metabolites penetrate the placental barrier, excreted in breast milk.

Clinical studies have shown that chlorpromazine can have a teratogenic effect.When using chlorpromazine in high doses during pregnancy in newborns, in some cases, there were digestive disorders associated with atropine-like action, extrapyramidal syndrome.

Application in elderly patients

Aminazine should be used with caution in elderly patients (increased risk of excessive sedation and hypotensive effect).

Use in children

Use in children is possible according to the dosing regimen.

In children, especially with acute diseases, the use of phenothiazines is more likely to develop extrapyramidal symptoms.

special instructions

With special care, phenothiazines are used in patients with pathological changes in the blood picture, liver function abnormalities, alcohol intoxication, Reye's syndrome, as well as in breast cancer, cardiovascular diseases, predisposition to the development of glaucoma, Parkinson's disease, gastric ulcer and duodenal ulcer , urinary retention, chronic respiratory diseases (especially in children), epileptic seizures.

In the case of hyperthermia, which is one of the symptoms of the NSA, chlorpromazine should be immediately withdrawn.

In children, especially with acute diseases, the use of aminazine is more likely to develop extrapyramidal symptoms.

During the treatment period, do not drink alcohol.

Impact on the ability to drive vehicles and manage mechanisms

It should be used with caution in patients engaged in potentially dangerous activities that require a high rate of psychomotor reactions.

Drug Interactions

With the simultaneous use of drugs that have a depressing effect on the central nervous system, ethanol (alcohol), ethanol-containing drugs, it is possible to intensify the inhibitory effect on the central nervous system, as well as respiratory depression.

With the simultaneous use of tricyclic antidepressants, maprotiline, MAO inhibitors, an increased risk of ZNS development is possible.

With simultaneous use with anticonvulsants, the threshold of convulsive readiness may be reduced; with funds for the treatment of hyperthyroidism - increased risk of agranulocytosis; with drugs that cause extrapyramidal reactions - it is possible to increase the frequency and severity of extrapyramidal disorders; with drugs that cause arterial hypotension - possibly additive effect on blood pressure,which leads to severe arterial hypotension, increased orthostatic hypotension.

With simultaneous use with amphetamines possible antagonistic interaction; with anticholinergics - strengthening of anticholinergic action; with anticholinesterase agents - muscle weakness, worsening of myasthenia flow.

With simultaneous use with antacids, containing aluminum and magnesium hydroxide, the concentration of chlorpromazine in the blood plasma decreases due to a violation of its absorption from the gastrointestinal tract.

With the simultaneous use of barbiturates increase the metabolism of aminazine, inducing microsomal enzymes of the liver and thereby reducing its concentration in the blood plasma.

With the simultaneous use of hormonal contraceptives for oral administration, a case of increasing the concentration of chlorpromazine in the blood plasma is described.

With the simultaneous use of epinephrine, a "distortion" of the pressor action of epinephrine is possible, as a result, only stimulation of beta-adrenoreceptors occurs and severe hypotension and tachycardia occur.

With simultaneous use with Amitriptyline increases the risk of developing tardive dyskinesia.The cases of paralytic ileus development are described.

With simultaneous use of aminazine can reduce or even completely inhibit the antihypertensive effect of guanethidine, although some patients may exhibit an antihypertensive effect of chlorpromazine.

With simultaneous use with diazoxide, severe hyperglycemia is possible; with doxepin - potentiation of hyperpyrexia; with zolpidem - significantly increased sedative effect; with Zopiclone - may enhance sedation; with imipramine - the concentration of imipramine in the blood plasma increases.

With simultaneous use of chlorpromazine inhibits the effects of levodopa due to blockade of dopamine receptors in the central nervous system. There may be an increase in extrapyramidal symptoms.

When applied simultaneously with lithium carbonate, there may be severe extrapyramidal symptoms, neurotoxic effects; with morphine - the development of myoclonus is possible.

With the simultaneous use of nortriptyline in patients with schizophrenia, clinical deterioration is possible, despite an elevated level of chlorpromazine in the blood plasma.The cases of paralytic ileus development are described.

At simultaneous application with piperazinom the case of development of cramps is described; with Propranolol - an increase in plasma concentrations of propranolol and chlorpromazine; with trazodone - hypotension is possible; with trihexyphenidyl - there are reports of the development of paralytic ileus; with trifluoperazine - cases of severe hyperpyrexia are described; with phenytoin - it is possible to increase or decrease the concentration of phenytoin in the blood plasma.

With simultaneous use with fluoxetine, the risk of developing extrapyramidal symptoms increases; with chloroquine, sulfadoxine / pyrimethamine, the concentration of chlorpromazine in the blood plasma increases with the risk of developing the toxic effect of chlorpromazine.

With simultaneous application of cisapride, the QT interval on the ECG is additively added.

With simultaneous use with cimetidine, a decrease in the concentration of aminazine in the blood plasma is possible. There are also data suggesting an increase in the concentration of chlorpromazine in the blood plasma.

With the simultaneous use of ephedrine, weakening of the vasoconstrictive effect of Ephedrine is possible.

Analogues of the drug Aminazine

Structural analogs for the active substance:

• Chlorpromazine;
• Chlorpromazine hydrochloride.

Analogues for the pharmacological group (antipsychotics):

• Abilifay;
• Azaleprol;
• Azaleptin;
• Betamax;
• Haloper;
• Haloperidol;
• Hedonin;
• Droperidol;
• Zalast;
• Zeldox;
• Zilaxera;
• Ziprasidone;
• Zipsil;
• Clozapine;
• Klozasten;
• Clopixol;
• Lakvel;
• Leptinorm;
• Mazeptil;
• Moditen;
• Neupilept;
• He did not;
• Normiton;
• Olanex;
• Olanzapine;
• Parnasan;
• Piportil;
• Prolinate;
• Propazine;
• Prosulfin;
• It is resilient;
• Ridonex;
• Rilept;
• Rileptid;
• Rispen;
• Risperidone;
• Rispolept;
• Rispolux;
• Risset;
• Saffris;
• Senorm;
• Seroquel;
• Sizodon-san;
• Solian;
• Sonapaks;
• Speridan;
• Sulpiride;
• Terialgen;
• Tiapride;
• Thiodasin;
• Thioridazine;
• Thioril;
• Torendo;
• Trasin;
• Triftazine;
• Truksal;
• Fluanexol;
• Chloroproticsen;
• Eglonyl;
• Escap;
• Etaperazine.

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