General characteristics:
international and chemical names: chlorpromazine; 2-chloro-10-(3-dimethylaminopropyl) phenothiazine hydrochloride;
main physicochemical properties: tablets are biconvex, coated, from light orange to dark orange in color. Two layers are visible on the cross section;
composition: 1 tablet contains chlorpromazine hydrochloride 0.05 g or 0.1 g;
excipients: celactose, aerosil, aluminum hydroxide (hydrargillite), calcium stearate, stearic acid, talc, hypromellose (hydroxypropylmethylcellulose), titanium dioxide, sunset yellow dye.
Release form.
The pills are coated.
Pharmacotherapeutic group.
Agents acting on the nervous system. Antipsychotics. ATC code N05A A01.
Pharmacological properties.
Pharmacodynamics. Blocks central adrenergic and dopaminergic receptors. Has a strong sedative effect (compared to other neuroleptics). General sedation is combined with inhibition of conditioned reflex activity, primarily motor-defensive reflexes, reduction of spontaneous motor activity, relaxation of skeletal muscles, reduction of reactivity. The use of large doses causes a hypnotic effect. Suppresses various interoceptive reflexes, has pronounced antiemetic and antiicteric effects, antihistamine, m-cholinoblocking and prolactinogenic activity. Has a hypothermic effect. Moderately reduces the severity of the inflammatory reaction, reduces vascular permeability, reduces the activity of kinins and hyaluronidase. Reduces systolic and diastolic blood pressure, causes tachycardia. Has pronounced cataleptogenic properties. The main feature of Aminazine is the combination of antipsychotic action with the ability to influence the emotional sphere. It relieves various types of psychomotor agitation, delusions and hallucinations, fear and anxiety in patients with psychoses and neuroses.
Pharmacokinetics. It is poorly absorbed in the gastrointestinal tract. The maximum concentration in the blood is reached after 2-4 hours. A significant part is metabolized in the liver with the formation of a number of active and inactive metabolites. It has a high degree of binding to plasma proteins (95-98%). It is widely distributed in the body, penetrates the blood-brain barrier, while its concentration in the brain exceeds the concentration in plasma. The half-life is about 30 hours, the elimination of metabolites is longer. It is excreted in the urine and bile in the form of metabolites.
Indications for use.
In psychiatry - acute and chronic paranoid and / or hallucinatory states, psychomotor agitation, including in patients with schizophrenia (hallucinatory-delusional, hebephrenic, catatonic syndromes); manic agitation in manic-depressive psychosis; agitated depression (in presenile and manic-depressive psychosis); as well as other diseases with productive symptoms and agitation. In neurology - increased muscle tone, torpid pain syndrome, persistent insomnia. As an antiemetic - Meniere's disease, incessant vomiting during treatment with antitumor drugs, radiation therapy.
Method of administration and doses.
Doses and treatment regimens are set individually depending on the indications and patient's condition. Take after meals.
In the treatment of mental illnesses, the daily dose of Aminazine for adults when taken orally is 0.3-0.6 g (in 1-3 doses) per day. The course of treatment is from 3 weeks to 2-4 months or more.
In some cases, the daily dose of Aminazin when used internally can be increased to 0.7-1.0 g (especially in patients with a chronic course of the disease and psychomotor agitation). In this case, the daily dose is divided into 4 doses (morning, afternoon, evening and night). The duration of treatment with large doses of the drug should not exceed 1-1.5 months, with insufficient effect it is advisable to switch to treatment with other drugs.
Debilitated patients and elderly patients are prescribed up to 300 mg/day.
Higher doses for adults orally: single - 0.3 g, daily - 1.5 g.
Children aged 3-5 years are recommended to use Aminazin tablets of 0.025 g.
For alcoholic psychoses, Aminazine is prescribed orally at 0.2-0.4 g per day.
Side effect.
Extrapyramidal disorders (parkinsonian syndrome, tremor, akathisia, indifference, slow reactions, blurred vision, dystonic reactions), tardive dyskinesia, depression, decreased blood pressure, tachycardia, thermoregulation disorders, dyspeptic phenomena (nausea, vomiting, constipation). Rarely - convulsions, jaundice, agranulocytosis, leukopenia, skin pigmentation, lens opacity, difficulty urinating, menstrual disorders, impotence, weight gain, allergic reactions (rash, edema, photosensitization, exfoliative dermatitis, erythema multiforme).
Contraindication.
Individual sensitivity or hypersensitivity (allergy) to the components of the drug. Severe hepatic and renal failure, progressive systemic diseases of the brain and spinal cord (slow neuroinfections, multiple sclerosis), brain injuries, comatose states, decompensated heart defects, active rheumatism, thromboembolic syndrome, severe inhibition of hematopoiesis, myxedema, angle-closure glaucoma. Gallstone and urolithiasis, exacerbation of erosive-ulcerative diseases of the gastrointestinal tract, acute pyelonephritis, urinary retention in prostatic hyperplasia. Pregnancy and lactation.
Overdose.
Symptoms: neuroleptic syndrome (parkinsonism, akathisia, indifference, slowed reaction to external stimuli, prolonged depression), persistent hypotension, hypothermia, coma, later - toxic hepatitis. Treatment: symptomatic therapy. To reduce depression, central nervous system stimulants (sidnocarb) are prescribed. Neurological complications are reduced or stopped by prescribing anti-parkinsonian drugs (cyclodol, tropacin). In collaptoid states, the administration of cordiamine, caffeine, mezaton is recommended.
Application features.
Aminazine is excreted in breast milk; if necessary, its use during lactation, breastfeeding should be discontinued.
It is used with extreme caution in the treatment of patients with pathological changes in the blood picture, liver and kidney dysfunction, alcohol intoxication, Reye's syndrome, breast cancer, cardiovascular diseases, a tendency to glaucoma, Parkinson's disease, gastric and duodenal ulcers, urinary retention, chronic respiratory diseases, epileptic seizures, in the elderly (increased risk of excessive sedative and hypotensive effects), in weakened patients. Working with mechanisms and driving a car is not allowed.
During the treatment period, alcohol consumption is not allowed. In case of hypothermia, the drug should be discontinued. When using the drug in patients with intestinal atony and achillea, it is recommended to simultaneously prescribe gastric juice or hydrochloric acid, monitor the diet and bowel function. During treatment with aminazine, patients should not be exposed to UV radiation due to the possibility of skin photosensitization. During long-term treatment with the drug, monitoring of blood counts, liver and kidney function is necessary.
Interaction with other drugs.
With simultaneous use with drugs that depress the central nervous system, as well as with ethanol or ethanol preparations, increased central nervous system depression, respiratory depression are possible; with tricyclic antidepressants, maprotiline or monoamine oxidase inhibitors - an increase in the risk of developing neuroleptic malignant syndrome, with anticonvulsants - a decrease in the seizure threshold; with drugs for the treatment of hyperthyroidism - the risk of developing agranulocytosis increases; with drugs that cause extrapyramidal reactions - an increase in the frequency and severity of extrapyramidal disorders; with antihypertensive drugs - pronounced orthostatic hypotension is possible; with ephedrine - a weakening of the vasoconstrictor effect. Aminazine weakens the effect of cardiac glycosides; potentiates the anticholinergic effects of other drugs, while its antipsychotic effect may decrease.
Barbiturates enhance the metabolism of Aminazine, inducing microsomal liver enzymes, and reduce its concentration in the blood. Antacids, cimetidine, antiparkinsonian drugs, lithium preparations impair the absorption of Aminazine, estrogens enhance its neuroleptic effects.
Storage conditions and shelf life. In a dry, dark place, out of reach of children, at a temperature not exceeding 25 °C. Shelf life - 3 years.
Packaging.
Film-coated tablets, 0.05 g or 0.1 g, No. 10, No. 10x2, No. 20 in contour blister packs.
