Aminazine

General characteristics. Structure:

Active agent: Chlorpromazinum hydrochloride of 100 mg.

Pharmacological properties:

Antipsychotic means (neuroleptic) from group of derivatives of a fenotiazin. Renders the expressed antipsychotic, sedative, antiemetic action. Weakens or completely eliminates nonsense and hallucinations, stops psychomotor excitement, reduces affective reactions, alarm, concern, lowers a physical activity.
The mechanism of antipsychotic action is connected with blockade of postsynaptic dopaminergic receptors in mesolimbic structures of a brain. Has also blocking effect on α-adrenoceptors and suppresses release of hormones of a hypophysis and a hypothalamus. However blockade of dopamine receptors increases secretion by a prolactin hypophysis.
The central antiemetic action is caused by oppression or blockade dopamine D2 receptors in a hemoretseptorny trigger zone of a cerebellum, peripheral - blockade of a vagus nerve in a GIT. The antiemetic effect amplifies, apparently, thanks to anticholinergic, sedative and antihistaminic properties. Sedative action is caused, apparently, by alpha and adrenoceptor blocking activity. Has moderate or weak extrapyramidal effect.

Pharmacokinetics. At intake Chlorpromazinum quickly, but sometimes is not completely soaked up from a GIT. Cmax in a blood plasma is reached in 2-4 h. Is exposed to effect of "the first passing" through a liver. Due to the specified effect of concentration in plasma after intake it is less, than concentration after introduction in oil.
It is intensively metabolized in a liver with formation of a number of active and inactive metabolites.
Ways of metabolism of Chlorpromazinum include a hydroxylation, a konjyugirovaniye with glucuronic acid, N-oxidation, oxidation of sulfur atoms, dealkylation.
Chlorpromazinum possesses high linkng with proteins of plasma (95-98%). It is widely distributed in an organism, gets through GEB, at the same time concentration in a brain is higher, than in plasma.
The expressed variability of pharmacokinetic parameters at the same patient is noted. There is no direct correlation between concentration in plasma of Chlorpromazinum and its metabolites and therapeutic effect.
T1/2 of Chlorpromazinum makes about 30 h; believe that elimination of its metabolites can be longer. It is removed with urine and with bile in the form of metabolites.

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 at other diseases which are followed by excitement, tension. The neurotic diseases which are followed by increase in a muscle tone. Persistent pains, including kauzalgiya (in combination with analgetics), sleep disorders of resistant character (in a combination to hypnotic drugs and tranquilizers). Menyer's disease, vomiting of pregnant women, treatment and prevention of vomiting at treatment by antineoplastic means and at radiation therapy. Pruritic dermatosis. As a part of "lytic mixes" in anesthesiology.

Route of administration and doses:

Is established individually. At intake for adults the single dose makes 10-100 mg, a daily dose - 25-600 mg; for children at the age of 1-5 years - on 500 mkg/kg each 4-6 h, for children are more senior than 5 years it is possible to apply 1/3-1/2 doses of the adult.
Use frequency inside or parenterally depends on indications and a clinical situation.
Maximum single doses: for adults at intake - 300 mg.
Maximum daily doses: for adults at intake - 1.5 g, for children are aged younger than 5 years (body weight to 23 kg) at intake - 40 mg, for children are aged more senior than 5 years (body weight more than 23 kg) at reception inside - 75 mg.

Features of use:

With extra care of a fenotiazina apply at patients with pathological changes of a picture of blood, at abnormal liver functions, a drunkenness, a syndrome to Reja, and also at a breast cancer, cardiovascular diseases, predisposition to development of glaucoma, Parkinson's disease, a peptic ulcer of a stomach and a duodenum, an ischuria, chronic diseases of a respiratory organs (especially at children), epileptic seizures.
Fenotiazina it is necessary to apply with care at patients of advanced age (increase in risk of excessive sedative and hypotensive action), at the exhausted and weakened patients.
In case of a hyperthermia which is one of ZNS symptoms Chlorpromazinum should be cancelled immediately.
At children, especially with acute diseases, at use of fenotiazin development of extrapyramidal symptoms is more probable.
During treatment not to allow alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms
It is necessary to apply with care at the patients who are engaged in potentially dangerous types of activity demanding the high speed of psychomotor reactions.

Side effects:

- From TsNS: the akathisia, a sight illegibility are possible; seldom - dystonic extrapyramidal reactions, a parkinsonichesky syndrome, late dyskinesia, disturbances of thermal control, ZNS; in isolated cases - spasms.
- From cardiovascular system: are possible arterial hypotension (especially at in introduction), tachycardia.
- From the alimentary system: the dispeptic phenomena (are possible at intake); 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 mnogoformny 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 of the medicines exerting the oppressing impact on TsNS, ethanol, etanolsoderzhashchy drugs strengthening of the oppressing action on TsNS, and also respiratory depressions is possible.

At simultaneous use of tricyclic antidepressants, Maprotilinum, MAO inhibitors increase in risk of development of ZNS is possible.

At simultaneous use with anticonvulsants reduction of the threshold of convulsive readiness is possible; with means 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 the drugs causing arterial hypotension - the perhaps additive action on the ABP that leads to the expressed arterial hypotension, strengthening of orthostatic hypotension.

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.

At simultaneous use with the antacids containing aluminum and magnesium hydroxide concentration of Chlorpromazinum in a blood plasma owing to disturbance of its absorption from a GIT decreases.

At simultaneous use barbiturates strengthen metabolism of Chlorpromazinum, inducing microsomal enzymes of a liver and reducing that its concentration in a blood plasma.

At simultaneous use of hormonal contraceptives for intake the case of increase in concentration of Chlorpromazinum in a blood plasma is described.

At simultaneous use with Epinephrinum "perversion" of pressor action of Epinephrinum thereof there is only a stimulation of β-adrenoceptors is possible and there are heavy hypotension and tachycardia.

At simultaneous use with amitriptyline the risk of development of late dyskinesia increases. Cases of development of paralytic Ilheus are described.

At simultaneous use Chlorpromazinum can reduce or even completely to oppress anti-hypertensive action of a guanetidin though at some patients the hypotensive effect of Chlorpromazinum can be shown.

At simultaneous use with diazoxide the expressed hyperglycemia is possible; with doksepiny - potentiation of a hyper pyrexia; with zolpidemy - sedative action considerably amplifies; with zopiklony - strengthening of sedative action is possible; with Imipraminum - concentration of Imipraminum in a blood plasma increases.

At simultaneous use Chlorpromazinum suppresses effects of a levodopa owing to blockade of dopamine receptors in TsNS. Strengthening of extrapyramidal symptoms is possible.

At simultaneous use from lithium a carbonate the expressed extrapyramidal symptoms, neurotoxic action are possible; with morphine - development of a myoclonus is possible.

At simultaneous use of a nortriptilin for patients with schizophrenia deterioration in a clinical state, despite the increased Chlorpromazinum level in a blood plasma is possible. Cases of development of paralytic Ilheus are described.

At simultaneous use with piperazin the case of development of spasms is described; with propranolol - increase in concentration in a blood plasma of propranolol and Chlorpromazinum; with Trazodonum - arterial hypotension is possible; with trigeksifenidily - there are messages on development of paralytic Ilheus; with trifluoperaziny - cases of a heavy hyper pyrexia are described; with Phenytoinum - increase or reduction of concentration of Phenytoinum in a blood plasma is possible.

At simultaneous use with fluoxetine the risk of development of extrapyramidal symptoms increases; with chloroquine, sulphadoxine/Pyrimethaminum concentration of Chlorpromazinum in a blood plasma with risk of development of toxic action of Chlorpromazinum increases.

At simultaneous use of a tsizaprid it is additive QT interval on an ECG is extended.

At simultaneous use with Cimetidinum reduction of concentration of Chlorpromazinum in a blood plasma is possible. Also there are data allowing to assume increase in concentration of Chlorpromazinum in a blood plasma.

At simultaneous use of ephedrine easing of vasoconstrictive effect of ephedrine is possible.

Contraindications:

Abnormal liver functions, kidneys, the hemopoietic bodies, the progressing general diseases of a head and spinal cord, a myxedema, a serious cardiovascular illness, a clotting disease; late stage of a bronchoectatic disease; closed-angle glaucoma; the ischuria connected with a prostate hyperplasia; the expressed oppression TsNS, coma, brain injuries.

Use at pregnancy and feeding by a breast
In need of use of Chlorpromazinum at pregnancy it is necessary to limit treatment terms, and at the end of pregnancy, whenever possible, to reduce a dose. It must be kept in mind that Chlorpromazinum prolongs childbirth.
In need of use in the period of a lactation breastfeeding should be stopped.
Chlorpromazinum and its metabolites get through a placental barrier, is allocated with breast milk.
In clinical trials it is shown that Chlorpromazinum can have teratogenic effect. At use of Chlorpromazinum in high doses at pregnancy at newborns the digestion disturbances connected with atropinopodobny action, an extrapyramidal syndrome were in certain cases noted.

Use at abnormal liver functions
It is contraindicated at abnormal liver functions.

Use at renal failures
It is contraindicated at renal failures.

Use for elderly patients
Fenotiazina it is necessary to apply with care at patients of advanced age (increase in risk of excessive sedative and hypotensive action).

Use for children
Use for children is possible according to the dosing mode.
At children, especially with acute diseases, at use of fenotiazin development of extrapyramidal symptoms is more probable.

Overdose:

There are no data.

Storage conditions:

Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

10 dragees on 50 mg
500 dragees on 50 mg
10 dragees on 100 mg
400 dragees on 100 mg.