Etaperazin

General characteristics. Structure:

Active ingredient - Perfenazinum.

Pharmacological properties:

Antipsychotic means (neuroleptic), piperazinovy derivative fenotiazina. Believe that antipsychotic action of fenotiazin is caused by blockade of postsynaptic dopamine receptors in mesolimbic structures of a brain. Perfenazinum has strong antiemetic effect which central mechanism is connected with oppression or blockade dopamine D2 receptors in a hemoretseptorny trigger zone of a cerebellum, and peripheral - with blockade of a vagus nerve in a GIT. Has alpha and adrenoceptor blocking activity. Anticholinergic activity and sedation can be shown from intensity, weak to moderate degree, hypotensive action is expressed poorly. Has the expressed extrapyramidal effect. The antiemetic effect can amplify anticholinergic and sedative properties. Renders the muscular weakening action.

Pharmacokinetics. Clinical data on pharmacokinetics of Perfenazinum are limited.

Fenotiazina possess high linkng with proteins of plasma. Are removed mainly by kidneys and partially with bile.

Indications to use:

Treatment of psychotic frustration, especially at a hyperactivity and excitement, schizophrenia; the neurosises which are followed by fear, tension. Treatment of nausea and vomiting of various etiology. Skin itch.

Route of administration and doses:

Inside (after food). The dose is selected individually, depending on indications, duration of a disease, portability, etc. The initial dose for patients with the mental diseases which were earlier not treated by neuroleptics — on 4–10 mg 1–2 times a day, if necessary a dose can be increased. Duration of a course of treatment — of 1–4 months and more. As an antiemetic, and also at neurosises — 4–8 mg 3 times a day, the maximum daily dose — 24 mg. At patients of advanced age and the weakened patients use smaller doses.

Features of use:

Extrapyramidal frustration arise at reception of high doses more often. Late dyskinesia develops at patients of advanced age, especially more often at women whereas dystonia — is more often at more young people. At emergence of signs or symptoms of late dyskinesia it is necessary to consider the possibility of the termination of treatment by a neuroleptic (however treatment continuation, despite existence of a syndrome can be required by some patients). The probability of damage of a liver, deposits in a crystalline lens and a cornea, irreversible dyskinesia is higher at long therapy.

Antiemetic action of Perfenazinum can mask the toxicity symptoms caused by overdose of other HP and also complicate diagnosis of such diseases as a brain tumor, intestinal impassability.

Perfenazinum can reduce a convulsive threshold at predisposed patients therefore it should be applied with care at convulsive frustration and at alcohol cancellation. At simultaneous treatment by Perfenazinum and anticonvulsant drugs increase in a dose of the last can be required.

Alcohol intake since the additive effect and hypotension can be observed is excluded. The risk of a suicide and danger of overdose of a neuroleptic can be increased at patients who during treatment abuse alcohol.

It is necessary to apply with care Perfenazinum at patients with earlier observed serious side effects at reception of other fenotiazin. Some of adverse reactions of Perfenazinum appear at reception of high doses more often.

With care to apply at the patients working in the conditions of the increased temperature and also at having contact with phosphorus insecticides.

With care to use at the patients receiving atropine or similar HP (the additive anticholinergic effect is possible).

In the course of treatment it is necessary to exercise control of function of a liver, kidneys (at long therapy), a picture of peripheral blood. At emergence of signs or symptoms of a dyscrasia of blood treatment it is necessary to stop and appoint the corresponding therapy. Treatment also should be stopped at deviations in hepatic tests, at the indicator of ureal nitrogen of blood deviating norm.

The majority of cases of an agranulocytosis was observed between the 4 and 10 week of therapy. During this period patients have to watch closely emergence of a pharyngalgia or symptoms of an infection especially. At considerable decrease in number of leukocytes administration of drug it is necessary to stop and begin the corresponding therapy.

During treatment it is necessary to refrain from occupations potentially dangerous types of activity, works with mechanisms, from driving of the car since Perfenazinum can weaken mental and/or physical effeciency, and also causes drowsiness (especially in the first 2 weeks of treatment).

Considerable rise in body temperature can be caused by individual hypersensitivity. In case of a hyperthermia treatment should be cancelled immediately.

The jaundice developing (seldom) against the background of treatment (between 2 and 4 weeks of therapy) usually is considered as hypersensitivity reaction. At the same time the clinical picture is similar to that at infectious hepatitis, but results of functional hepatic tests are characteristic of obstructive jaundice. Usually it has reversible character, however was reported about cases of chronic jaundice.

It was occasionally reported about cases of sudden death at the patients receiving fenotiazina. In certain cases the cardiac standstill, in others — asphyxia owing to insufficiency of a tussive reflex was a cause of death.

Side effects:

From a nervous system and sense bodys: extrapyramidal frustration (especially dystonic) — a spasm of muscles of a back and neck, person, language, a tonic masticatory spasm, difficulty at a conversation and swallowing, okulogirny crises, a spasm and extremity pain, rigidity of hands and legs, an akathisia, late dyskinesia, parkinsonism, an ataxy; drowsiness, block, slackness, muscular weakness, decrease in motivational activity, dizziness, a miosis, a mydriasis, a sight illegibility, glaucoma, a pigmental retinopathy, deposits in a crystalline lens and a cornea, paradoxical reactions — an aggravation of psychotic symptomatology, a katalepsy, katatonikopodobny states, paranoid reactions, a lethargy, paradoxical arousing, concern, a hyperactivity, night confusion of consciousness, strange dreams, an insomniya.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): decrease/increase in the ABP, orthostatic hypotension, pulse rate change, tachycardia (especially at unexpected substantial increase of a dose), bradycardia, arrhythmia, a faint, changes on an ECG, a leukopenia, an agranulocytosis, an eosinophilia, hemolitic anemia, a trombopenichesky purpura, a pancytopenia.

From bodies of a GIT: nausea, vomiting, a diarrhea/lock, anorexia, increase in appetite and body weight, a polyphagia, an abdominal pain, dryness in mouth/increase in a sialosis, damage of a liver (стаз bile), cholestatic hepatitis.

Allergic reactions: skin rash, small tortoiseshell, erythema, eczema, exfoliative dermatitis, itch, skin photosensitization, asthma, fever, anaphylactoid reactions, Quincke's disease, jaundice.

Others: pallor, a perspiration, an atony of intestines and bladder, an urination delay, a frequent urination or an incontience of urine, a polyuria, obstruction of the nasal channel, damage of kidneys, increase in intraocular pressure, a xanthopathy, photophobia, unusual secretion of breast milk, increase in mammary glands and a galactorrhoea at women, a gynecomastia at men, disturbance of a menstrual cycle, an amenorrhea, change of a libido, decrease in an ejaculation, a syndrome of inadequate secretion of ADG, the false positive test for pregnancy, a hyperglycemia/hypoglycemia, a glucosuria, an antipsychotic malignant syndrome (development is possible against the background of reception of any classical neuroleptics).

Interaction with other medicines:

At simultaneous use with the medicines exerting the oppressing impact on TsNS with ethanol, etanolsoderzhashchy drugs strengthening of oppression of TsNS and function of breath is possible.

At simultaneous use with anticonvulsants reduction of the threshold of convulsive readiness is possible; with means for treatment of a hyperthyroidism - the risk of development of an agranulocytosis increases.

At simultaneous use with the drugs causing extrapyramidal reactions increase in frequency and weight of extrapyramidal disturbances is possible.

At simultaneous use with the drugs causing arterial hypotension the expressed orthostatic hypotension is possible.

At simultaneous use with the means having anticholinergic effects strengthening of their anticholinergic effects is possible, at the same time the antipsychotic effect of a neuroleptic can decrease.

At simultaneous use with tricyclic antidepressants, Maprotilinum, MAO inhibitors the risk of development of ZNS increases.

At simultaneous use of antacids, protivoparkinsonichesky means, salts of lithium absorption of fenotiazin is broken.

At simultaneous use reduction of effect of amphetamines, levodopas, a clonidine, a guanetidin, Epinephrinum is possible.

At simultaneous use with fluoxetine development of extrapyramidal symptoms and dystonia is possible.

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

Contraindications:

Hypersensitivity, coma or the expressed oppression of TsNS, including against the background of purpose of high doses of HP, the oppressing TsNS (barbiturates, alcohol, narcotic means, analgetics, antihistamines), a blood dyscrasia, oppression of a marrowy hemopoiesis, the liver diseases assumed or the established subcortical injury of a brain with/without hypothalamus injury, heart pathology, organic diseases of TsNS.

Overdose:

There are no data.

Storage conditions:

List B. In the dry, protected from light place.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated on 0,004. In packaging of 50 tablets.