Instructions for use Aminazin-Zdorovye film-coated tablets 25 mg blister No. 20
Composition
active ingredient: 1 tablet contains chlorpromazine hydrochloride 25 mg;
excipients: calcium hydrogen phosphate, microcrystalline cellulose, potato starch, colloidal anhydrous silicon dioxide, calcium stearate, stearic acid, macrogol 4000, talc, hypromellose, titanium dioxide (E 171), Sunset Yellow FCF dye (E 110).
Dosage form
Film-coated tablets.
Main physicochemical properties: film-coated tablets, yellow to light orange, biconvex. Two layers are visible on cross-section.
Pharmacotherapeutic group
Antipsychotics. Chlorpromazine. ATX code N05A A01.
Pharmacological properties
Pharmacodynamics. Antipsychotic, neuroleptic, sedative, muscle relaxant, antiemetic. It has a blocking effect on dopaminergic and adrenergic receptors. The main feature of the drug is the combination of antipsychotic action with the ability to influence the emotional sphere.
The mechanism of antipsychotic action is due to the blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain. As a result, delusions and hallucinations are weakened or completely eliminated, psychomotor agitation is stopped, affective reactions, anxiety, restlessness are reduced, and motor activity is reduced. As a result of the blockade of dopaminergic receptors, the secretion of prolactin by the pituitary gland increases.
Blocking α-adrenergic receptors, chlorpromazine exhibits a pronounced sedative effect. The presence of a strong sedative effect is one of the main features of chlorpromazine compared to other neuroleptics. The general sedative effect is combined with the suppression of conditioned reflex activity and, above all, motor-defensive reflexes, a decrease in spontaneous motor activity, relaxation of skeletal muscles, a decrease in reactivity to endogenous and exogenous stimuli while maintaining consciousness.
It has a pronounced central and peripheral antiemetic effect; the central effect is due to inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, the peripheral effect is due to blockade of the vagus nerve in the digestive tract. The antiemetic effect is enhanced by the anticholinergic, sedative and antihistamine properties of chlorpromazine.
The anticholinergic effect is due to competitive blockade of M-cholinoreceptors; the anxiolytic, sedative and analgesic effect is due to the weakening of excitation in the reticular formation of the brainstem.
Moderately reduces the severity of the inflammatory reaction, reduces vascular permeability, reduces the activity of kinins and hyaluronidase, exhibits a weak antihistamine effect. Reduces systolic and diastolic blood pressure, causes tachycardia. Has pronounced cataleptogenic properties. Suppresses the release of hypothalamic and pituitary hormones (however, enhances the secretion of prolactin). Has a weak or moderate extrapyramidal effect. Has a hypothermic effect.
Potentiates the effects of analgesics, local anesthetics, hypnotics, and anticonvulsants.
Pharmacokinetics. It is poorly absorbed in the digestive tract. The maximum concentration in the blood is reached after 2-4 hours. Binding to plasma proteins is 95-98%. It is subject to the "first pass" effect. It is widely distributed in the body, penetrates the blood-brain barrier, while its concentration in the brain becomes higher than in blood plasma. Chlorpromazine and its metabolites penetrate the placental barrier, into breast milk. It is intensively metabolized in the liver with the formation of a number of active and inactive metabolites. It is excreted in the form of metabolites by the kidneys and through the intestines with bile. The half-life is about 30 hours; elimination of metabolites may be longer.
There is marked variability in pharmacokinetic parameters in the same patient. There is no direct correlation between the concentrations of chlorpromazine and its metabolites in blood plasma and the therapeutic effect.
Indication
Adults. Chronic paranoid and hallucinatory-paranoid states, states of psychomotor agitation in schizophrenia (hallucinatory-delusional, 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 other diseases accompanied by agitation, tension; neurological diseases accompanied by increased muscle tone; Meniere's disease, vomiting, treatment and prevention of vomiting during treatment with antitumor agents and during radiation therapy; prolonged hiccups; itchy dermatoses; as part of complex therapy: persistent pain, incl. causalgia (in combination with analgesics), persistent sleep disorders (in combination with hypnotics and tranquilizers).
Children. Schizophrenia, autism.
Contraindication
Increased individual sensitivity to chlorpromazine and other components of the drug; severe disorders of the liver (cirrhosis, hepatitis, hemolytic jaundice) and/or kidneys (nephritis, acute pyelitis, renal amyloidosis), hematopoietic organs; progressive systemic diseases of the brain and spinal cord (slow neuroinfections, for example, multiple sclerosis); gastric and duodenal ulcers during the exacerbation period; myxedema; severe cardiovascular diseases (decompensated heart failure and heart defects, severe myocardial dystrophy, severe arterial hypotension, rheumatic carditis in the late stages); thromboembolism; late stage of bronchiectasis; angle-closure glaucoma; urinary retention due to prostatic hyperplasia; stroke, acute period of craniocerebral trauma; cholelithiasis and urolithiasis; acute infectious diseases; pronounced depression of the central nervous system, coma, brain injuries, simultaneous use with barbiturates, alcohol, drugs.
Interaction with other medicinal products and other types of interactions
When used simultaneously with other medicines, it is possible:
· with drugs that depress the central nervous system, as well as with ethanol or ethanol-containing drugs - increased central nervous system depression, as well as respiratory depression;
· with tricyclic antidepressants, maprotiline or monoamine oxidase inhibitors - prolongation and enhancement of sedative and anticholinergic effects, increased risk of developing neuroleptic malignant syndrome;
· with anticonvulsant drugs – lowering the threshold of seizure readiness;
· with drugs for the treatment of hyperthyroidism - increased risk of developing agranulocytosis;
· with drugs that cause extrapyramidal reactions - increased frequency and severity of extrapyramidal disorders;
· with antihypertensive drugs – severe arterial hypotension, increased orthostatic hypotension;
· with ephedrine – weakening of the vasoconstrictor effect of the latter;
· with amphetamines – antagonistic interaction;
· with anticholinergic agents - increased anticholinergic effect;
· with anticholinesterase agents – muscle weakness, worsening of myasthenia gravis;
· with epinephrine - distortion of the effects of the latter, resulting in a further decrease in blood pressure and the development of severe hypotension and tachycardia;
· with amitriptyline – increased risk of developing tardive dyskinesia, possible development of paralytic ileus;
· with diazoxide – severe hyperglycemia;
· with doxepin – potentiation of hyperpyrexia;
· with lithium carbonate – pronounced extrapyramidal symptoms, neurotoxic effect;
· with morphine – development of myoclonus;
· with cisapride – additive prolongation of the QT interval on the ECG;
· with nortriptyline in patients with schizophrenia - possible worsening of the clinical condition, despite an increased level of chlorpromazine in the blood;
· with zolpidem or zopiclone - increased sedative effect of chlorpromazine;
· with estrogens - increased neuroleptic effect of chlorpromazine;
· with guanethidine – reduction or even complete inhibition of the antihypertensive effect of guanethidine;
· with levodopa – suppression of the effects of levodopa;
· with cardiac glycosides - reduction of their effect.
The concentration of chlorpromazine in the blood plasma is reduced by antacids containing aluminum and magnesium hydroxide (they disrupt the absorption of chlorpromazine from the digestive tract), barbiturates (they enhance the metabolism of chlorpromazine in the liver). The concentration of chlorpromazine in the blood plasma is increased by chloroquine, sulfadoxine/pyrimethamine. Cimetidine can reduce or increase the concentration of chlorpromazine in the blood. Chlorpromazine can increase the concentration of imipramine in the blood, increase or decrease the concentration of phenytoin in the blood.
Application features
Use with extreme caution in the treatment of patients with pathological changes in the blood picture, with moderate liver and kidney dysfunction, alcohol intoxication, Reye's syndrome, with breast cancer, moderate cardiovascular diseases, a tendency to glaucoma, Parkinson's disease, prostatic hyperplasia with clinical manifestations, chronic respiratory diseases (especially in children), epileptic seizures, diseases accompanied by an increased risk of thromboembolic complications, rheumatism, rheumatic carditis, diabetes mellitus, elderly patients (increased risk of excessive sedative and hypotensive effects), in weakened patients.
Children are more likely to develop extrapyramidal symptoms, especially during the first 4 days of treatment or after increasing the dose.
In the event of hyperthermia, which is one of the symptoms of neuroleptic malignant syndrome, the drug should be discontinued immediately.
To reduce neuroleptic depression, use antidepressants and central nervous system stimulants.
During long-term treatment with the drug, it is necessary to monitor blood composition, prothrombin index, liver and kidney function.
Due to the possibility of skin photosensitization, prolonged exposure to the sun should be avoided.
When using the drug in patients with atony of the digestive tract and achilia, it is recommended to simultaneously prescribe gastric juice or hydrochloric acid (due to the inhibitory effect of chlorpromazine on motility and secretion of gastric juice), monitor the diet and intestinal functioning.
Patients using the drug may have an increased need for riboflavin.
The drug is not recommended for use in patients with hypothyroidism, pheochromocytoma, or myasthenia gravis.
Neuroleptic phenothiazines may increase the QT interval prolongation, which increases the risk of ventricular arrhythmias, including torsades de pointes, which can potentially lead to sudden death. Before prescribing the drug, the patient should be examined (biochemical status, ECG) to exclude possible risk factors (heart disease, history of QT interval prolongation; metabolic disorders (hypokalemia, hypocalcemia, hypomagnesemia); fasting, alcohol abuse, concomitant therapy with other drugs that cause QT interval prolongation). ECG monitoring should be performed at the beginning of treatment with the drug and, if necessary, during treatment.
With special caution in severe arterial hypertension, chronic respiratory diseases (especially in children).
Use during pregnancy or breastfeeding
The drug is not recommended during pregnancy. If the drug is used during pregnancy, the duration of treatment should be limited, and at the end of the third trimester of pregnancy, if possible, the dose should be reduced. Chlorpromazine prolongs labor.
When using Aminazine in high doses in pregnant women, digestive disorders associated with an atropine-like effect and extrapyramidal syndrome were sometimes observed in newborns.
If necessary, use of the drug should stop breastfeeding.
Aminazine and its metabolites penetrate the placental barrier and into breast milk.
Ability to influence reaction speed when driving vehicles or other mechanisms
During the treatment period, you should refrain from driving vehicles and performing potentially dangerous activities that require concentration of attention and increased speed of psychomotor reactions.
Method of administration and doses
Administer orally after meals. Doses, frequency of administration and treatment regimens are determined by the doctor individually depending on the indications and patient's condition. Doses should be selected by increasing, starting from the minimum. Duration of treatment - from 3 weeks to 2-4 months or more.
For adults, the initial dose is 25-75 mg per day, divided into 2-3 doses. The dose can then be gradually increased to an effective maintenance daily dose, which is usually 75-300 mg, divided into 3-4 doses, but some patients may require a daily dose of 1 g.
In elderly patients, with liver and cardiovascular system diseases, the dose should be reduced by 2-3 times.
Prolonged hiccups. Adults should be prescribed 25-50 mg 3-4 times a day.
Children over 5 years of age should be given ⅓ - ½ of the adult dose; the highest daily dose is 75 mg, divided into several doses.
Children
The drug is used in children aged 5 years and older for the treatment of autism and schizophrenia.
Overdose
Symptoms: slurred speech, unsteady gait, bradycardia, difficulty breathing, severe weakness, confusion, decreased reflexes, drowsiness, convulsions, persistent hypotension, hypothermia, prolonged depression, and later toxic hepatitis.
Treatment: symptomatic. There is no specific antidote. It is not removed by hemodialysis. To reduce depression, prescribe central nervous system stimulants (sidnocarb). Neurological complications are reduced or stopped by prescribing antiparkinsonian drugs (cyclodol, tropacin). In collaptoid states, the administration of cordiamine, caffeine, mezaton is recommended.
After prolonged use of large doses of the drug (0.5-1.5 g per day), in rare cases jaundice, accelerated blood clotting, lymphopenia and leukopenia, anemia, agranulocytosis, skin pigmentation, and clouding of the lens and cornea may occur.
Adverse reactions
From the side of the central nervous system: with prolonged use, akathisia, mental indifference and other mental changes, delayed reaction to external stimuli, blurred vision are possible; rarely - dystonic extrapyramidal reactions, parkinsonian syndrome, tardive dyskinesia, neuroleptic depression, thermoregulation disorders, neuroleptic malignant syndrome; in isolated cases - convulsions, insomnia, agitation.
From the cardiovascular system: possible arterial hypotension, tachycardia; very rarely - changes in the ECG (prolongation of the QT interval, ST-segment depression, changes in the T and U waves, arrhythmia).
On the part of the digestive tract: rarely - cholestatic jaundice, dyspeptic phenomena (nausea, vomiting); very rarely - dry mouth, constipation.
From the hematopoietic system: rarely - leukopenia, agranulocytosis, hematological changes, eosinophilia.
From the urinary system: rarely - difficulty urinating; very rarely - priapism.
Dermatological reactions: rarely - skin pigmentation, photosensitivity.
Immune system: hypersensitivity reactions, including skin rashes, itching, bronchospasm, urticaria, angioedema, erythema multiforme, exfoliative dermatitis, systemic lupus erythematosus and other allergic reactions.
On the part of the organs of vision: with prolonged use in high doses, chlorpromazine may be deposited in the anterior structures of the eye (cornea and lens), which can accelerate the natural aging processes of the lens.
Respiratory system: nasal congestion.
General: isolated reports of sudden death while taking the drug.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
Tablets No. 10×2, No. 20 in blisters in a box; No. 20 in a blister.
Vacation category
According to the recipe.
Producer
Limited Liability Company "Pharmaceutical Company "Zdorovya".
Location of the manufacturer and its business address
Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenko street, building 22.
