Aminazine

Aminazine has an antiemetic and sedative effect. It is also a neuroleptic.

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Indications Aminazin

It is used to get rid of the following disorders:

• paranoid behavior, either acute or chronic;
• hallucinosis;
• schizophrenia, against the background of which there is excitement of a psychomotor nature;
• agitation with manic symptoms;
• epilepsy, which is accompanied by severe psychotic disorders;
• pain syndrome;
• agitated form of depression;
• alcohol overdose-induced psychosis;
• increased muscle tone;
• epistatus;
• constant insomnia;
• dermatoses that are itchy in nature (this list includes neurodermatitis or eczema);
• strengthening of anesthesia.

As a substance capable of relieving vomiting, it is prescribed to people with Meniere's disease, as well as to pregnant women and people undergoing radiation therapy.

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Release form

The substance is released in the form of dragees with tablets and in the form of an injection liquid.

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Pharmacodynamics

An antipsychotic from the phenothiazine category, a representative of the 1st generation of neuroleptics. Its neuroleptic effect is associated with the blocking of dopamine endings inside individual brain structures. Due to the blocking of such endings, the pituitary gland begins to produce prolactin more actively. At the same time, the drug blocks α-adrenergic receptors, and this leads to the development of a sedative effect.

The central antiemetic effect is provided by blocking D2-endings within a certain cerebellar region, and the peripheral one is provided by blocking the vagus intestinal nerve. Among other things, the antiemetic effect of the drug is associated with its antihistamine, sedative and anticholinergic effects.

The antipsychotic effect provides relief from delusional hallucinations, reduces tension and anxiety, as well as the feeling of restlessness and fear. At the same time, it stops agitation of psychomotor origin. The sedative effect occurs quickly, which is why the drug is used in acute forms of psychosis. Aminazine is not used to treat depression.

Among other properties of the drug are hypothermic, anti-shock, anti-hiccup and anti-arrhythmic. It also has a moderate extrapyramidal effect.

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Pharmacokinetics

It is absorbed at a high rate, but not completely, after oral administration. It reaches the Cmax level after 3-4 hours. It undergoes the first liver passage, due to which its values in the blood when taken orally are lower than the drug values when administered parenterally.

Metabolic processes occur inside the liver, which allows the formation of active and inactive decay products. Synthesis with intraplasmic protein is 95-98%. The substance penetrates the BBB. Its values inside the brain are always higher than inside the blood. The effectiveness of the drug does not depend on the intraplasmic level of the active element with its metabolic products.

Half-life is 30+ hours. Metabolic products are excreted in bile and urine.

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Dosing and administration

The method of administration (oral or parenteral) is determined by the clinical picture.

Intravenous injections for adults – 1-2 ml (25-50 mg). If necessary, the procedure is repeated at intervals of 3-12 hours.

For intramuscular injections, the medicine (2 ml) must be diluted in 0.9% NaCl. For intravenous injections, 20 ml of the drug must be diluted in a similar solution. The maximum permissible adult dose is 0.15 g (intramuscular) and 0.1 g (intravenous).

If there is a feeling of anxiety before the operation, the patient should be administered 0.5-1 ml of the drug intramuscularly (120 minutes before the procedure).

The single dose for children (intravenous or intramuscular) is 250-500 mcg/kg.

The initial dosage of the drug (orally) for an adult is 25-100 mg (single dose or 4 times a day). If necessary, the dosage can be increased to 0.7-1 g/day. Only a single dose can be increased to 1.2-1.5 g/day. A maximum of 300 mg of the drug can be taken at one time, and no more than 1500 mg per day.

During a long course of therapy, it is necessary to monitor the patient's blood composition and PTI levels.

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Use Aminazin during pregnancy

Aminazine should not be prescribed to pregnant women.

Contraindications

Main contraindications:

• the presence of intolerance to the components of the drug;
• failure affecting the kidneys or liver and having a severe degree of intensity;
• stroke;
• coma;
• brain injuries (acute stage);
• pronounced degree of suppression of hematopoietic function;
• hypothyroidism;
• heart failure of a decompensated nature (in individuals with heart defects);
• thromboembolism;
• bronchiectasis (in severe stages);
• closed-angle glaucoma;
• cholelithiasis or urolithiasis;
• ulcers present inside the gastrointestinal tract (at the stage of their exacerbation);
• breast-feeding;
• infants up to 1 year old.

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Side effects Aminazin

The use of the medication may cause the following side effects:

• a feeling of restlessness and fidgeting, extrapyramidal disorders, problems with thermoregulation, Parkinsonism. Convulsions occasionally occur;
• decrease in blood pressure (after intravenous injection) or tachycardia;
• dyspeptic symptoms (after oral use);
• agranulocytosis or leukopenia;
• problems with urination;
• development of gynecomastia or impotence, menstrual irregularities and weight gain;
• itching with rash, erythema with dermatitis and skin pigmentation.

Long-term use of the drug can lead to deposition of the substance inside the lens with the cornea, which causes the former to age faster. Infiltrates may appear after an intramuscular injection, and intravenous injections can lead to phlebitis.

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Overdose

Aminazine intoxication leads to a persistent decrease in blood pressure, the development of neuroleptic syndrome, toxic hepatitis and hypothermia.

The disorders can be eliminated by prescribing symptomatic measures.

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Interactions with other drugs

The injection liquid must not be mixed with other substances inside the same syringe.

Combined oral administration of drugs with medications that suppress the central nervous system (ethyl alcohol, anticonvulsants with narcotic analgesics, and in addition barbiturates and other sleeping pills) can potentiate their suppressive effect, and at the same time lead to suppression of the respiratory process.

The drug reduces the effects of amphetamines and clonidine with ephedrine and guanethidine.

It is prohibited to use it for a long time together with analgesics.

Aminazine inhibits the effect of levodopa, and extrapyramidal manifestations may also increase.

Combination with cholinesterase inhibitors causes severe muscle weakness; with amitriptyline – increases the likelihood of dyskinesia in the gastrointestinal tract; with the substance diazoxide – leads to severe hyperglycemia; with the drug zopiclone – there is an increase in the sedative effect.

Combination with antacids interferes with the absorption of the drug from the gastrointestinal tract and reduces its level in the blood; with the drug cimetidine - the indicator in the blood also decreases.

Combined use with morphine results in myoclonus. Use with lithium carbonate potentiates neurotoxic properties and results in severe extrapyramidal symptoms.

Use together with trazodone reduces the values of blood pressure; with the substance propranolol - a mutual increase in drug indicators is observed. Combination with trifluoperazine causes severe hyperpyrexia; with the drug phenytoin - changes its values in the blood.

Combination with fluoxetine increases the likelihood of developing extrapyramidal symptoms, and combination with sulfadoxine or chloroquine maximally increases the risk of developing toxic properties of Aminazine.

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Storage conditions

It is recommended to keep Aminazine at temperatures not exceeding 25°C.

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Shelf life

Aminazine may be prescribed within 24 months from the date of release of the therapeutic agent.

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Analogues

The analogues of the drug are Perphenazine with Levomepromazine, and in addition Thioproperazine with Fluphenazine and Trifluoperazine.

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Reviews

Aminazine receives quite mixed reviews. Most people believe that the drug has a powerful sedative, but weak antipsychotic effect. And this is true - representatives of the same category of phenothiazines, Fluphenazine with Trifluoperazine, have neuroleptic properties that are 20 times more effective than Aminazine, but their sedative effect is significantly lower.

Because of this, the drug is recommended for use in emergency care – to eliminate acute emotional or psychomotor agitation.

Some reviews indicate that the drug was used in long courses (tablets) during withdrawal from alcohol binge drinking, against the background of which weak productive signs were noted (such as hallucinations with delirium).