Aminazin-Zdorovye, the tab. on 25 mg No. 20

General characteristics. Structure:

International and chemical names: Chlorpromazinum; chlorpromazine; 3-(2-chlorine-N, N-dimetil-10H-phenothiazin-10-silt) - N, N-dimetilpropa-1-amine a hydrochloride;
main physical and chemical properties: tablets, coated, from yellow till light orange color, biconvex. On cross section two layers are visible; structure: 1 tablet contains Chlorpromazinum of a hydrochloride 25 mg;
excipients: calcium hydrophosphate anhydrous, cellulose microcrystallic, potato starch, silicon dioxide colloid, calcium stearate, stearic acid, macrogoal 4000, talc, gipromeloza, titanium dioxide, dye yellow "Sunset" of E110.

Pharmacological properties:

Pharmacodynamics. Antipsychotic, antipsychotic, sedative, myorelaxation, antiemetic. Has the blocking effect on dofaminergichesky and adrenergic receptors. The main feature of drug is the combination of antipsychotic action to ability to influence the emotional sphere.
The mechanism of antipsychotic action is caused by blocking of postsynaptic dofaminergichesky receptors in mesolimbic structures of a brain. Are as a result weakened or completely the nonsense and hallucinations are eliminated, psychomotor excitement is stopped, affective reactions, alarm, concern decrease, a physical activity decreases. As a result of blockade of dofaminergichesky receptors secretion by a prolactin hypophysis increases.
Blocking a-adrenoceptors, shows the expressed sedation. Existence of strong sedative action is one of the main features of Chlorpromazinum in comparison with other neuroleptics. The cumulative calming effect is combined with oppression of uslovnoreflektorny activity and first of all motive and protective reflexes, reduction of a spontaneous physical activity, relaxation of skeletal muscles, decrease in reactivity to endogenous and exogenous incentives at consciousness preservation.
Shows the expressed central and peripheral antiemetic effect; the central effect is caused by oppression or blockade dopamine D2 receptors in a hemoretseptorny trigger zone of a cerebellum, peripheral – blockade of a vagus nerve in digestive tract. The antiemetic effect amplifies thanks to anticholinergic, sedative and antihistaminic properties of Chlorpromazinum.
The anticholinergic effect is caused by competitive blockade M-holinoretseptorov; anxiolytic, sedative and analgeziruyushchy – weakening of excitement in a reticular formation of a brainstem.
Moderately reduces expressiveness of inflammatory reaction, reduces permeability of vessels, lowers activity of kinin and hyaluronidase, has weak antihistaminic effect. Reduces systolic and diastolic arterial pressure, causes tachycardia. Has the expressed kataleptogenny properties. Suppresses release of hormones of a hypothalamus and a hypophysis (however strengthens prolactin secretion). Shows weak or moderate extrapyramidal action. Has hypothermal effect.
Exponentiates action of analgetics, mestnoanesteziruyushchy, somnolent and anticonvulsants.

Pharmacokinetics. In digestive tract it is soaked up badly. The maximum concentration in blood is reached in 2–4 hours. Linkng with proteins of plasma – 95–98%. Is exposed to effect of "the first passing". It is widely distributed in an organism, gets through a blood-brain barrier, at the same time its concentration in a brain becomes higher, than in plasma. Chlorpromazinum and its metabolites get through a placental barrier, are allocated with breast milk. It is intensively metabolized in a liver with formation of a number of active and inactive metabolites. It is removed in the form of metabolites by kidneys and through intestines with bile. The elimination half-life makes about 30 h; elimination of metabolites can be longer.
The expressed variability of pharmacokinetic parameters at the same patient is noted. There is no direct correlation between concentration of Chlorpromazinum and its metabolites in plasma and therapeutic effect.

Indications to use:

Chronic paranoid and hallucinatory paranoid conditions, conditions of psychomotor excitement at schizophrenia (hallucinatory and crazy, hebephrenic, catatonic syndromes), alcoholic psychosis, maniacal excitement at maniac-depressive psychosis, mental disorders at epilepsy, the agitated depression at patients with presenile psychosis, maniac-depressive psychosis, and also other diseases which are followed by excitement, tension.
- The neurologic diseases which are followed by increase in a muscle tone.
- Menyer's disease, vomiting, treatment and prevention of vomiting at treatment by antineoplastic means and at radiation therapy.
- Pruritic dermatosis.
- As a part of complex therapy: persistent pains, including kauzalgiya (in combination with analgetics), sleep disorders of resistant character (in a combination to hypnotic drugs and tranquilizers).

Route of administration and doses:

Appoint inside after food. Doses, the frequency of reception and the scheme of treatment are established individually depending on indications and a condition of the patient. Doses should be selected by increase, since minimum. Treatment duration – from 3 weeks to 2 – 4 months and more. Schizophrenia, other psychoses and psychomotor excitement. For adults the initial dose makes 25–75 mg (1–3 tablets) a day, divided into 2 – 3 receptions. Further the dose can be raised gradually to 300–600 mg (12–24 tablets) a day, dividing it into 3 – 4 receptions. The highest single dose – 300 mg, daily – 1 g.
At elderly patients, at diseases of a liver and cardiovascular system the dose is reduced by 2 – 3 times.
To children (schizophrenia and autism), aged from 5 up to 12 years, appoint 1/3 – ½ doses of the adult; the highest daily dose – 75 mg (3 tablets). To children, aged from 1 year up to 5 years, each 4–6 h appoint 0,5 mg/kg; the highest daily dose – 40 mg.
Long hiccups. The adult appoint 25–50 mg (1 – 2 tablets) 3 – 4 times a day.

Features of use:

With extra care apply to treatment of patients with pathological changes of a picture of blood, at abnormal liver functions, kidneys, a drunkenness, a syndrome to Reja, at a breast cancer, cardiovascular diseases, predisposition to glaucoma, Parkinson's disease, a peptic ulcer of a stomach and a duodenum (in the period of an aggravation), a prostate hyperplasia with clinical manifestations, chronic diseases of a respiratory organs (especially at children), the epileptic attacks, diseases which are followed by the increased risk of tromboembolic episodes, rheumatism, a rheumatic carditis, a diabetes mellitus at elderly patients (increase in risk of excessive sedative and hypotensive action), at the weakened patients.
At children, especially with acute diseases, at use of drug development of extrapyramidal symptoms is more probable.
In case of development of a hyperthermia which is one of symptoms of a malignant antipsychotic syndrome, it is necessary to stop administration of drug immediately.
At prolonged treatment by drug it is necessary to control composition of blood, a prothrombin ratio, function of a liver and kidneys.
Due to a possibility of a photosensitization of skin it is necessary to avoid long stay in the sun.
Drug has no antiemetic effect in case nausea is result of vestibular stimulation or local irritation of digestive tract.
At drug use by patients with an atony of an intestinal path and an akhiliya it is recommended to appoint at the same time gastric juice or hydrochloric acid (in connection with the oppressing influence of Chlorpromazinum on motility and secretion of a gastric juice), to watch a diet and functioning of intestines.
At the patients using drug the need for Riboflavinum can be increased.
During treatment alcohol intake is not allowed.
Use during pregnancy and feeding by a breast. At urgent need of use of drug during pregnancy it is necessary to limit treatment term, and at the end of pregnancy, whenever possible, to reduce a dose. Chlorpromazinum prolongs childbirth. In need of use in the period of a lactation, feeding by a breast should be stopped.
Influence on an opportunity to manage vehicles and mechanisms. During treatment it is necessary to abstain from control of motor transport and performance of potentially dangerous types of activity which demand concentration of attention and the increased speed of psychomotor reactions.

Side effects:

From the central nervous system: the akathisia, a sight illegibility are possible; seldom – dystonic extrapyramidal reactions, a parkinsonichesky syndrome, late dyskinesia, thermal control disturbances, a malignant antipsychotic syndrome; very seldom – spasms. From cardiovascular system: arterial hypotension, tachycardia are possible. From system of digestion: the dispepsichesky phenomena are possible; seldom – cholestatic jaundice. From system of a hemopoiesis: seldom – a leukopenia, an agranulocytosis. From an urinary system: seldom – difficulty of an urination. From endocrine system: disturbances of a menstrual cycle, impotence, gynecomastia, increase in body weight. Allergic reactions: skin rash, an itch are possible; seldom – exfoliative dermatitis, a multiformny erythema. Dermatological reactions: seldom – a xanthopathy, a photosensitization. From an organ of sight: at prolonged use in high doses adjournment of Chlorpromazinum in front structures of an eye (a cornea and a crystalline lens) is possible that can accelerate processes of normal aging of a crystalline lens.

Interaction with other medicines:

At simultaneous use with the drugs oppressing the central nervous system and also with ethanol or etanolsoderzhashchy drugs, strengthening of oppression of the central nervous system, and also respiratory depression is possible; with tricyclic antidepressants, Maprotilinum or monoamine oxidase inhibitors – lengthening and strengthening of sedative and anticholinergic effects, increase in risk of development of a malignant antipsychotic syndrome; with anticonvulsant drugs – reduction of the threshold of convulsive readiness; with drugs for treatment of a hyperthyroidism – increase in risk of development of an agranulocytosis; with the drugs causing extrapyramidal reactions – increase in frequency and weight of extrapyramidal disturbances is possible; with hypotensive drugs – the expressed arterial hypotension, strengthening of orthostatic hypotension is possible; with ephedrine – weakening of vasoconstrictive action of the last. At simultaneous use with amphetamines perhaps antagonistic interaction; with anticholinergics – strengthening of anticholinergic action; with antikholinesterazny means – muscular weakness, deterioration in a current of a myasthenia; with Epinephrinum – "perversion" of effects of the last is possible owing to what there is only a stimulation of a-adrenoceptors and development of heavy hypotension and tachycardia. At simultaneous use with amitriptyline the risk of development of late dyskinesia increases, development of paralytic Ilheus is possible; with diazoxide – the expressed hyperglycemia is possible; with doksepiny – potentiation of a hyper pyrexia, from lithium a carbonate – the expressed extrapyramidal symptoms, neurotoxic action; with morphine – development of a myoclonus, with tsizapridy – the additive lengthening of an interval of QT on an ECG. Sedative action of Chlorpromazinum amplifies at simultaneous use with zolpidemy or zopiklony; antipsychotic – with estrogen. Concentration of Chlorpromazinum in a blood plasma is reduced by the antacids containing aluminum and magnesium hydroxide (break absorption of Chlorpromazinum from digestive tract), barbiturates (strengthen metabolism of Chlorpromazinum in a liver); raise – chloroquine, sulphadoxine/Pyrimethaminum. Cimetidinum can reduce or increase concentration of Chlorpromazinum in blood.
Chlorpromazinum can reduce or even completely to oppress anti-hypertensive action of a guanetidin, to increase concentration of Imipraminum in blood, to suppress effects of a levodopa; to raise or reduce concentration of Phenytoinum in blood, to reduce effect of cardiac glycosides.
At simultaneous use with nortriptiliny for patients with schizophrenia deterioration in a clinical state, despite the increased Chlorpromazinum level in blood is possible.

Contraindications:

The increased individual sensitivity to Chlorpromazinum and other components of drug; heavy abnormal liver functions and/or kidneys, the hemopoietic bodies, the progressing general diseases of a head and spinal cord, a myxedema, a serious cardiovascular illness (dekompensirovanny heart failure, heavy arterial hypotension), a thromboembolism; late stage of a bronchoectatic disease; closed-angle glaucoma; the ischuria caused by a prostate hyperplasia; the expressed oppression of the central nervous system, a stroke, the acute period of a craniocereberal injury, zhelchekamenny and urolithic diseases, acute infectious diseases, pregnancy, feeding by a breast, children's age till 1 year.

Overdose:

Symptoms: a speech illegibility, the unsteady gait, bradycardia, the complicated breath, the expressed weakness, confusion of consciousness, weakening of reflexes, drowsiness, spasms, later – toxic hepatitis. Treatment: symptomatic. There is no specific antidote. Is not removed at a hemodialysis. For reduction of a depression appoint stimulators of the central nervous system (Sydnocarbum). Neurologic complications decrease or stopped by purpose of protivoparkinsonichesky means (Cyclodolum, Tropacinum). At kollaptoidny states introduction of Cordiaminum, caffeine, a phenylephine hydrochloride is recommended.

Storage conditions:

To store in the place protected from light at a temperature from 8os to 25 to °s.khranit in the place, unavailable to children.

Period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 25 mg No. 10, No. 20 in blister strip packagings; No. 10x2, No. 20 in blister strip packagings in a pack.