Aminazine

General characteristics. Structure:

Active ingredient: chlorpromazine;

1 ml of solution contains Chlorpromazinum a hydrochloride of 25 mg;

excipients: sodium sulfite anhydrous (Е 221), sodium metabisulphite (Е 223), ascorbic acid, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Chlorpromazinum – a neuroleptic of group of aliphatic derivatives of a fenotiazin. Shows the expressed antipsychotic action, eliminates psychomotor excitement. reduces feeling of fear, aggression, psychomotor block. Except antipsychotic and sedative, has antiemetichesky, hypothermal, hypotensive and antiserotoninovy effects. Blocks the central and dofaminergichesky interneural contacts. Exponentiates action of analgetik, mestnoanesteziruyushchy, somnolent and anticonvulsant drugs.

Pharmacokinetics. Chlorpromazinum is metabolized in a liver, forming both active, and inactive metabolites. It is removed with urine and a stake, passes through a hematoencephalic barrier, at the same time its concentration in a brain exceeds concentration in a blood plasma. Elimination half-life rather long (4 weeks and more).

Pharmaceutical characteristics.

The main physical and chemical svoystva:prozrachny colourless liquid of either yellowish, or greenish-yellowish color.

Incompatibility. Not to mix in one syringe with other medicines.

Indications to use:

Chronic paranoid and hallucinatory paranoid conditions, conditions of psychomotor excitement at patients with schizophrenia (hallucinatory and crazy, hebephrenic, catatonic syndromes), alcoholic psychosis, maniacal excitement at patients maniacal депресивным psychosis, mental disorders at patients with epilepsy, the agitated depression at patients presenile, maniacal депресивным psychosis, and also at other diseases which are followed by excitement, tension. The neurotic diseases accompanied with increase in a muscle tone. Persistent pain, including kauzalgiya (in a combination with analgetics), racks a sleep disorder (in a combination to hypnagogues and tranquilizers). Menyer's disease, vomiting of pregnancy, treatment and prevention of vomiting at treatment by antineoplastic means and at radiation therapy. Dermatozny itch. As a part of "lytic mixes" in anesthesiology.

Route of administration and doses:

Drug is appointed intramusculary and intravenously. Doses and schemes of treatment the doctor establishes individually depending on indications and a condition of the patient. At intramuscular introduction the highest single dose makes 150 mg, daily – 600 mg. Usually intramusculary no more than 3 times a day enter 1-5 ml of 2,5% of solution. A course of treatment – several months, in high doses – to 1,5 months, then pass to treatment with maintenance doses, gradually lowering a dose by 25-75 mg a day. At an acute hyperphrenia enter intramusculary 100-150 mg (4-6 ml of 2,5% of solution) or intravenously 25-50 mg (1-2 ml of 2,5% of solution of aminazine part in 20 ml 5% or 40% of solution of glucose), in need of 100 mg (4 ml of 2,5% of solution – in 40 ml of solution of glucose). Enter slowly. At intravenous administration the highest single dose – 100 mg, daily – 250 mg.

At intramuscular or intravenous administration to children 1 years are aged more senior the single dose makes 250-500 ¬¼ú/kg body weights; to children 5 years (body weight to 23 kg) – 40 mg a day are aged more senior, than 5-12 years (body weight – 23-46 kg) – 75 mg a day.

To the weakened patients and patients of advanced age appoint up to 300 mg a day intramusculary or to 150 mg a day – intravenously.

Features of use:

It is not recommended to use drug to patients with a hypothyroidism, a pheochromocytoma, a myasthenia.

With extra care under careful control drug is used for treatment of patients with pathological changes of a picture of blood, rheumatism, a rheumatic carditis, a drunkenness, a syndrome to Reja, and also at a breast cancer, the expressed arterial hypertension, tendency to development of glaucoma, at Parkinson's disease, chronic diseases of a respiratory organs (especially at children), epileptic attacks.

It is necessary to appoint with care to patients of advanced age (increase in risk of excessive sedative and hypotensive action), the emaciated and weakened patients.

In case of development of a hyperthermia which is one of symptoms of a malignant antipsychotic syndrome it is necessary to stop drug use immediately.

Children, especially with acute diseases, at use of drug have a bigger risk of development of extrapyramidal symptoms.

At prolonged treatment by drug it is necessary to control composition of blood, a prothrombin ratio, function of a liver and kidneys. After a drug injection patients need to lie down within 1-1,5 hours; sharp transition to vertical position can cause an orthostatic collapse.

Apply antidepressants and stimulators of the central nervous system to reduction of a neurolytical depression. During therapy because of a possibility of a fotosensebilization of skin it is necessary to avoid long stay in the sun. Drug does not show antiemetic action in case nausea is a consequence of vestibular stimulation or local irritation of a digestive tract. At drug use by the patient with an atony of a digestive tract and an akhiliya it is recommended to appoint at the same time gastric juice or hydrochloric acid (because of the oppressing influence of Chlorpromazinum on motility and secretion of a gastric juice), to watch a diet and functioning of intestines. At patients who use drug the need for Riboflavinum can be increased.

Antipsychotic fenotiazina can strengthen lengthening of an interval of QT that increases risk of ventricular arrhythmias, including the pirouette type which can potentially lead to a sudden lethal outcome. Before purpose of drug it is necessary to inspect the patient (the biochemical status, an ECG) for the purpose of an exception of possible risk factors (for example, heart diseases, lengthening of an interval of QT in the anamnesis, metabolic disturbances, such as a hypopotassemia, a hypocalcemia, a hypomagnesiemia; starvation, an alcohol abuse, the accompanying therapy with other medicines which cause lengthening of an interval of QT). It is necessary to carry out control of an ECG in an initiation of treatment by drug and, if necessary, during treatment.

Ability to influence speed of response at control of motor transport or work with other mechanisms. During treatment by aminazine it is necessary to refrain from control of motor transport or work with other mechanisms.

Side effects:

From the central nervous system: at prolonged use development of an antipsychotic syndrome is possible: parkinsonism, akathisia, mental indifference and other changes of mentality, overdue reaction to external irritations, sight illegibility; seldom – a distonichesika extrapyramidal reactions, late dyskinesia, an antipsychotic depression, thermal control disturbance, a malignant antipsychotic syndrome; in isolated cases – spasms, sleeplessness, excitement.

From a cardiovascular sistemy:vozmozhna arterial hypotension (especially at intravenous administration), tachycardia; very seldom – changes on an ECG (lengthening of an interval of QT, a depression of a ST segment, change of teeth Ti of U, arrhythmia).

From a digestive trakta:redko – cholestatic jaundice, nausea, vomiting; very seldom – dryness in a mouth.

From system кровообразования:редко – a leukopenia, an agranulocytosis.

From an urinary sistemy:redko – difficulty of an urination; very seldom – a priapism.

From outside to an endocrine sistemy:narushenia of a menstrual cycle, impotence, gynecomastia, increase in body weight; very seldom – a galactorrhoea.

Allergic reaktsii:vozmozhna skin rashes, itch; seldom – exfoliative dermatitis, a multiformny erythema; very seldom – a Quincke's disease, a bronchospasm, a small tortoiseshell, a system lupus erythematosus.

Dermatological реакции:редко – a xanthopathy, a photosensitization. At hit of solutions on mucous membranes, on skin and under skin – irritation of fabrics; after intramuscular introduction – emergence of painful infiltrates in an injection site is frequent; at intravenous administration damage of an endothelium of vessels is possible. For prevention of these phenomena solutions of aminazine part with nastvor of novocaine, glucose, 0,9% chloride sodium solution.

From bodies of a zreniya:pra 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 natural aging of a crystalline lens.

Interaction with other medicines:

Sedative action of Chlorpromazinum amplifies at simultaneous use with zolpidemy млм zopiklony; antipsychotic – with estrogen. Concentration of Chlorpromazinum in a blood plasma is umenshat by the antacids containing aluminum and magnesium hydroxide (increase absorption of Chlorpromazinum from a digestive tract), barbiturates (strengthen metabolism of Chlorpromazinum in a liver). Concentration of Chlorpromazinum in a blood plasma is increased by chloroquine, sulphadoxine/Pyrimethaminum. Cimetidinum can decrease or increase concentration of Chlorpromazinum in blood.

Chlorpromazinum can reduce or further completely to oppress anti-hypertensive action of a guanetidin, to increase concentration of Imipraminum in blood, to oppress effect of a levodopa; to raise or reduce concentration of Phenytoinum in blood, to reduce effect of cardiac glycosides.

At simultaneous use with other medicines perhaps:

with anticholinergics – strengthening of anticholinergic action;

with antikholinesterazny means – muscular weakness, weighting of a current of a myasthenia;

with Epinephrinum – distortion of effects of the last therefore there is a further lowering of arterial pressure and development of heavy arterial hypotension and tachycardia;

with amitriptyline – increase in risk of development of late dyskinesia, development of paralytic Ilheus is possible;

with diazoxide – the expressed hyperglycemia;

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;

with nortriptiliny at patients with schizophrenia – deterioration in a clinical state, despite the increased Chlorpromazinum level in blood is possible;

with tricyclic antidepressants, monoamonoksidaza inhibitors – increase in risk of development of a malignant neurolytical syndrome;

with drugs for treatment of a hyperthyroidism – the risk of development of an agranulocytosis increases;

with other drugs which cause extrapyramidal reactions – possibly increase in frequency and weight of extrapyramidal disturbances;

with drugs which cause arterial hypotension – the expressed orthostatic hypotension is possible;

with ephedrine – easing of vasoconstrictive effect of ephedrine is possible.

At neurotic diseases which are followed by increase in a muscle tone, persistent pains, including kauzalgiya, aminazine can be combined with analgetika, at persistent sleeplessness – with hypnotic drugs and tranquilizers. At simultaneous use of aminazine with anticonvulsant drugs action of the last amplifies; with other drugs which oppress influence on the central nervous system and also with the ethanol and drugs containing ethanol strengthening of a depression of the central nervous system, and also respiratory depression is possible.

Barbiturates strengthen aminazine metabolism, exciting microsomal enzymes of a liver and reducing that its concentration in a blood plasma, as a result, therapeutic effect. Drug can oppress effect of amphetamines, levodopas, a clonidine, guanidine, adrenaline.

Contraindications:

The increased individual sensitivity to Chlorpromazinum of fishers to other components of drug. Damage of a liver (cirrhosis, hepatitis, hemolitic jaundice, a zhelchekamenny disease), kidneys (nephrite, an acute pyelitis, an amyloidosis of kidneys, an urolithiasis), a disease of the hemopoietic bodies, the progressing general diseases of a head and spinal cord (slow neuroinfections, multiple sclerosis), dekompensirovanny heart failure, a serious cardiovascular illness, stomach ulcer and a duodenum in the period of an aggravation, dekompensirovanny heart diseases, the expressed arterial hypotension, a clotting disease, the expressed myocardial dystrophy, a rheumatic carditis at late stages, a myxedema, a late stage of a bronchoectatic disease, zakrytouglovy glaucoma, the ischuria caused by a prostate hyperplasia, the expressed oppression of the central nervous system, coma, brain injuries. Not to appoint along with barbiturates. alcohol, drugs.

Primeneniyev period of pregnancy or feeding by a breast. In need of use of aminazine during pregnancy it is necessary to limit treatment terms, and in ІІІ a pregnancy trimester – whenever possible to reduce a dose. It must be kept in mind that aminazine prolongs childbirth.

At use of aminazine in high doses to pregnant women at newborns sometimes noted the digestion disturbance connected with atropinopodobny action, an extrapyramidal syndrome. In need of use of drug it is necessary to stop feeding by a breast. Aminazine and its metabolites get through a placental barrier, and into breast milk.

Children. Drug is not recommended to be used to children age till 1 year.

Overdose:

Cases of overdose of drug are not described. For the prevention of overdose it is necessary to adhere to strictly recommended drug doses.

At kollaptoidny states introduction of Cordiaminum, caffeine, a phenylephine hydrochloride is recommended. At development of dermatitis treatment by aminazine is stopped and appoint antihistaminic means. Neurologic complications usually decrease at an aminazine dose decline, they can also be reduced one-time purpose of Cyclodolum or Tropacinum.

After long use of high doses of drug (0,5–1,5 g a day) in isolated cases jaundice, acceleration of a blood coagulation, lympho-and a leukopenia, anemia, an agranulocytosis, a xanthopathy, a phacoscotasmus and corneas can be observed.

Storage conditions:

Period of validity 2 years. To store the place, vzashchishchenny from light, to a pritemperatura it is not above 25 °C. To store the place, extra available to children.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule, on 10 ampoules in a blister strip packaging, on 1 blister strip packaging in a pack; on 2 ml in an ampoule, on 10 ampoules in a box.