Aminazine

Aminazine has an antiemetic and sedative effect. Is also neuroleptic.

[1], [2], [3], [4], [5]

Indications of the aminazine

It is used to get rid of such disorders:

• paranoid behavior with acute or chronic degree;
• hallucinosis;
• schizophrenia, against which there is an excitation that has a psychomotor nature;
• arousal with manic symptoms;
• epilepsy, which is accompanied by strong psychotic disorders;
• pain syndrome;
• agitated form of depression;
• caused by alcohol overdose psychosis;
• increased muscle tone;
• an epistatus;
• constant insomnia;
• dermatoses having an itchy character (in this list, neurodermatitis or eczema);
• intensification of anesthesia.

As a substance capable of relieving vomiting, is prescribed to people with Meniere's disease, and also to pregnant women and persons undergoing radiotherapy procedures.

[6], [7], [8]

Release form

Release of the substance is carried out in a tablet with tablets and in the form of an injection liquid.

[9],

Pharmacodynamics

Antipsychotic from the category of phenothiazines, a representative of the first generation of neuroleptics. Its neuroleptic effect is associated with blocking the end of dopamine within individual cerebrospinal structures. Due to the blocking of such endings, the pituitary gland begins to produce prolactin more actively. Along with this, the drug blocks α-adrenoreceptors, and this leads to the development of sedative effects.

The central antiemetic effect is ensured by blocking the D2-termini within a certain cerebellar region, and the peripheral by blocking the wandering intestinal nerve. Among other things, the antiemetic effect of drugs is associated with its antihistamine, sedative and anticholinergic effects.

Antipsychotic effect provides relief from hallucinations with delirium, reduces stress and anxiety, and besides a feeling of anxiety and fear. Together with this it stops the excitation of psychomotor origin. Sedative effects occur quickly, which is why the drug is used in acute forms of psychosis. Aminazine is not used to treat depression.

Among other properties of drugs - hypothermic, anti-shock, anti-icic and antiarrhythmic. Has also a moderate extrapyramidal effect.

[10], [11]

Pharmacokinetics

At high speed, but not fully, it is absorbed after oral administration. Level Cmax reaches after 3-4 hours. It is subjected to the 1st hepatic passage, because of what its values inside the blood are lower than the LS in case of parenteral use.

Exchange processes take place inside the liver, which makes it possible to form active and inactive decay products. Synthesis with intracellular protein is 95-98%. The substance penetrates the BBB. Its values inside the brain are always higher than inside the blood. The effectiveness of drugs does not depend on the intraplasma level of the active element with its metabolic products.

The half-life is 30+ hours. Metabolism products are excreted with bile and urine.

[12], [13]

Dosing and administration

The method of use (either orally or parenterally) is determined by the clinical picture.

Intravenous injection for adults - 1-2 ml (25-50 mg). If there is a need, the procedure is repeated at intervals of 3-12 hours.

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

If there is a sense of anxiety before the operation, you should inject the patient intramuscularly with 0.5-1 ml of LS (120 minutes before the procedure).

The size of a child's single-dose dosage (intravenously or intramuscularly) is 250-500 mcg / kg.

The initial dosage of the drug (orally) to an adult is 25-100 mg (single dose or 4-fold reception per day). If necessary, you can increase the dosage to 0.7-1 g / day. Only a single portion is allowed to increase to 1.2-1.5 g / day. For 1 reception, you can use a maximum of 300 mg of drugs, and for the whole day - no more than 1500 mg.

During a prolonged course of therapy, it is necessary to monitor the blood composition and level of PTI in a patient.

[18], [19], [20]

Use of the aminazine during pregnancy

You can not prescribe aminazine for pregnant women.

Contraindications

The main contraindications:

• the presence of intolerance relative to the elements of the drug;
• insufficiency affecting the kidney or liver, and having a severe degree of intensity;
• stroke;
• coma;
• cerebral trauma (acute stage);
• expressed degree of suppression hematopoietic function;
• hypothyroidism;
• heart failure, having a decompensated character (in persons with heart defects);
• thromboembolism;
• bronchiectasis (in the severe stage);
• closed-angle form of glaucoma;
• cholelithiasis or urolithiasis;
• Ulcers present within the gastrointestinal tract (at the stage of their exacerbation);
• breast-feeding;
• infants up to 1 year old.

[14], [15]

Side effects of the aminazine

The use of medication can cause the appearance of such side effects:

• anxiety and restlessness, extrapyramidal disorders, problems with thermoregulation, parkinsonism. Occasionally there are cramps;
• decrease in blood pressure (after intravenous injection) or tachycardia;
• symptoms of dyspepsia (after oral administration);
• agranulocytosis or leukopenia;
• problems with urination function;
• development of gynecomastia or impotence, menstrual disorders and weight gain;
• itching with eruptions, erythema with dermatitis and skin pigmentation.

Continuous use of drugs can lead to the deposition of matter inside the lens with the cornea, which causes the aging of the former to occur faster. After an intramuscular injection, infiltrates may appear, and intravenous injections can lead to the appearance of phlebitis.

[16], [17]

Overdose

Intoxication with aminazine leads to a persistent lowering of the level of blood pressure, the development of neuroleptic syndrome, toxic hepatitis and hypothermia.

Elimination of violations can be done by the appointment of symptomatic measures.

[21], [22], [23]

Interactions with other drugs

Injection liquid is not allowed to mix with other substances inside one syringe.

Combined oral administration of drugs with drugs that suppress the activity of 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 medication reduces the effects of amphetamines and clonidine with ephedrine and guanethidine.

It is forbidden to be used for a long time together with analgesics.

Aminazine depresses the effect of levodopa, and extrapyramidal manifestations can also increase.

The combination with cholinesterase inhibitors causes strong weakness in the muscles; 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 sedation.

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

Combined use with morphine leads to the appearance of myoclonus. Application together with lithium carbonate potentiates neurotoxic properties and leads to the emergence of strong extrapyramidal traits.

Use with trazodone reduces blood pressure; with the substance propranolol - there is a mutual increase in the indices of drugs. The combination with trifluoperazine causes severe hyperpyrexia; with the drug phenytoin - changes its values inside the blood.

Combination with fluoxetine increases the likelihood of developing extrapyramidal signs, and the combination with sulfadoxine or chloroquine maximizes the risk of toxic effects of aminazine.

[24], [25], [26], [27], [28], [29]

Storage conditions

Aminazine is recommended to contain at temperature marks not exceeding 25 ° C.

[30], [31], [32], [33]

Shelf life

Aminazine is allowed to be administered within 24 months of the release of the therapeutic agent.

[34], [35], [36]

Analogues

Analogues of the drug are preparations of Perfenazine with Levomepromazine, and in addition, Thioproperazine with Fluphenazine and Trifluoperazine.

[37], [38], [39], [40], [41], [42]

Reviews

Aminazine receives quite diverse reviews. Most people believe that the drug has a powerful sedative, but a weak antipsychotic effect. And this is really so - 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 much lower.

Because of this, the drug is recommended to be used to provide first aid - to eliminate the acute or acute emotional or psychomotor agitation.

In separate reviews, it is indicated that the drug was used for long-term courses (tablets) during exits from alcoholic drinking, against which weak productive signs (such as hallucinations with delirium) were noted.