Active substanceChlorpromazineChlorpromazine
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  • Chlorpromazine hydrochloride
    solution w / m in / in 
  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the solution contains chlorpromazine hydrochloride - 25 mg;

    auxiliary substances: sodium sulfite - 1 mg, sodium disulfite - 1 mg, ascorbic acid - 2 mg, sodium chloride - 6 mg, water for injection - up to 1 ml

    Description:Transparent colorless or slightly yellowish-greenish solution
    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.A.01   Chlorpromazine

    Pharmacodynamics:

    Neuroleptic from the group of phenothiazine derivatives. Has a pronounced antipsychotic, sedative and antiemetic effect. Relaxes or completely eliminates, delusions and hallucinations, stops psychomotor agitation, reduces affective reactions; anxiety, anxiety, reduces motor activity.

    The mechanism of antipsychotic action is due to the blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain.Has a blocking effect on alpha-adrenergic receptors and inhibits the release of hormones of the pituitary and hypothalamus, but the blockade of dopamine receptors increases the secretion of the pituitary gland, prolactin. Antiemetic effect is caused by oppression or blockade of dopamine D2 receptors in the chemoreceptor triggering region of the brainstem, peripheral by the blockade of the vagus nerve in the gastrointestinal tract. Sedative action is due to blockade of central adrenoreceptors. Has antihistamine and moderate anticholinergic effects, competitively blocks m-cholinergic receptors.

    Pharmacokinetics:

    Chlorpromazine is found in the blood 15 minutes after the administration of the therapeutic dose, the maximum concentration in the blood is reached after 1-2 hours. Has a high degree of binding to plasma proteins (90-99%), widely distributed in the body,

    penetrates the blood-brain barrier, while its concentration in the brain is higher than in the plasma. Intensively metabolized in the liver with the formation of a number of active and inactive metabolites. The half-life of chlorpromazine is 15-30 hours. It is excreted in urine and feces.

    Indications:

    Psychomotor, excitement (including in patients with schizophrenia); acute delirious states, manic and hypomaniacal arousal in manic-depressive psychosis, chronic psychosis; mental illness of various genesis, accompanied by fear, anxiety, excitation of insomnia; psychopathy including in patients with epilepsy and organic diseases of the central nervous system), alcoholic psychosis.

    Severe nausea and vomiting, persistent hiccough.

    Diseases accompanied by increased muscle tone: after disorders of cerebral circulation, tetanus (in combination with barbiturates), etc.

    Premedication and potentiation of general anesthesia in anesthesiology.

    Acute "intermittent" porphyria.

    Contraindications:

    Hypersensitivity to the drug components and other phenothiazine derivatives; severe cardiovascular diseases (decompensated heart failure, severe arterial - hypotension); marked suppression of central nervous system functions and comatose states of any etiology; progressive systemic diseases of the brain and spinal cord, intracranial hypertension, brain trauma; pregnancy, lactation, children's age (up to 6 months).

    Carefully:Alcoholism (predisposition to hepatotoxic reactions), pathological changes in blood (hemopoiesis), breast cancer (as a result of phenothiazine-induced prolactin secretion, the potential risk increases progression of the disease and resistance to treatment with endocrine and cytotoxic drugs), closed-angle glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and / or renal insufficiency; diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease; epilepsy; myxidem; chronic diseases accompanied by respiratory failure (especially in children); Reye syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia; elderly age
    Pregnancy and lactation:

    Chlorpromazine, like other antipsychotics, is contraindicated in pregnancy because of the potential risk of developing extrapyramidal disorders and / or withdrawal syndrome in newborns (stimulation, increase or decrease in muscle tone, tremor, drowsiness, severe breathing difficulties, and difficulty in feeding) to mothers who were taking the drug during the third trimester of pregnancy.The use of chlorpromazine in pregnant women is allowed if the benefit to the mother significantly exceeds the risk to the fetus.

    Chlorpromazine and its metabolites penetrate the placental barrier, are excreted in breast milk. If you need to use the drug during lactation, breastfeeding should be interrupted.

    Dosing and Administration:

    The drug is administered intramuscularly and intravenously. The doses and treatment regimens are set individually by the doctor, depending on the indicationth and the patient's condition.

    With intramuscular injection, the chlorpromazine solution is diluted with 2-5 ml of 0.25-0.5% procaine solution or 0.9% sodium chloride solution. Enter deep into the muscle. With intravenous administration, the required amount of chlorpromazine solution is diluted with 5% or 40% dextrose solution, or 0.9% sodium chloride solution, administered slowly under the control of blood pressure.

    Psychotic disorders.

    Intramuscularly administered 25-50 mg (1-2 ml) once, if necessary, the dose is repeated after 1 hour, and then, if necessary, and taking into account tolerability every 3-12 hours for several days. In acute psychic excitement, 50-75 mg (2-3 ml) is administered intravenously in 20 ml of a 40% dextrose solution.

    In anesthesiology, for the relief of anxiety before surgery, 12.5-25 mg (0.5-1 ml) is administered intramuscularly 1-2 hours before the operation.

    Severe nausea and vomiting.

    Enter intravenously once 25 mg (1 ml), if necessary and taking into account the tolerability dose is increased by 25-50 mg (1-2 ml) every 3-4 hours before the termination of vomiting. In anesthesiology, to stop nausea and vomiting during surgery, injected intramuscularly or intravenously. Intramuscular injection of 12.5 mg (0.5

    ml) once, if necessary and taking into account the tolerability dose is repeated after 30 minutes. Intravenous 25 mg, diluted to a concentration of 1 mg / ml 0.9% solution of sodium chloride, at a rate of not more than 2 mg / min.

    Persistent hiccups.

    Enter intramuscularly 25-50 mg (1-2 ml) 3-4 times a day or intravenously 25-50 mg (1-2 ml), diluted in 500-1000 ml of 0.9% sodium chloride solution at a rate of 1 mg / min.

    For relief of psychomotor agitation, attacks of vomiting and hiccups in cases of cerebral circulation disorders, it is prescribed as part of a "lytic mixture" containing 25-50 mg (1-2 ml) of chlorpromazine, 50 mg of promethazine solution or 40 mg of diphenhydramine solution, 20 mg of trimeridine solution. The "lytic mixture" is administered intramuscularly or intravenously 1-2 times a day.

    Diseases accompanied by increased muscle tone.

    Tetanus: Intramuscularly administered 25-50 mg (1-2 ml) 3-4 times a day, if necessary, and taking into account tolerability, the dose is gradually increased. Intravenous 25-50 mg, diluted to a concentration of about 1 mg / ml 0.9% solution of sodium chloride, with

    at a rate of 1 mg / ml.

    Acute "intermittent" porphyria:

    Enter intramuscularly 25 mg (1 ml) every 6-8 h until the patient can take chlorpromazine inside.

    Elderly, as well as weakened or emaciated patients, treatment with the drug begins with a lower dose, gradually increasing it with a view to the necessity and tolerability.

    For children from 6 months to 12 years, the drug is administered: with psychotic disorders, intramuscularly 0.55 mg / kg (15 mg / m) every 6-8 hours; with nausea, vomiting during surgery - intramuscularly 0.275 mg / kg, if necessary taking into account the tolerability dose is repeated after 30 minutes, or intravenously 0.275 mg / kg, diluted to a concentration of about 1 mg / ml 0.9% solution of sodium chloride at a rate of 1 mg / 2 min; for relief of anxiety before surgery - intramuscularly 0.55 mg / kg for 1-2 hours before surgery; for tetanus - intramuscularly 0.55 mg / kg every 6-8 hours or intravenously 0.55 mg / kg, diluted to a concentration of approximately 1 mg / ml with 0.9% sodium chloride solution at a rate of 1 mg / 2 min.

    The maximum daily intake of chlorpromazine for adults with intramuscular injection is 1000 mg, with intravenous administration 250 mg.

    Precautions for use

    Chlorpromazine, like other neuroleptic phenothiazines, can potentiate interval lengthening QT, increasing the risk of ventricular arrhythmias. Before appointment the patient should be examined (biochemical status, ECG) for the purpose of elimination of possible risk factors (cardiovascular diseases, lengthening interval QT, in anamnesis or with concomitant therapy, metabolic disorders, such as hypoglycaemia, hypocalcemia, hypomagnesemia). When taking neuroleptics phenotiazinovogo number of cases of sudden death, including, possibly, caused by cardiac causes.

    To avoid an abrupt change in blood pressure, parenteral administration of chlorpromazine is performed in the patient's prone position, after administration, patients should stay in the reclining position for at least 1-1.5 hours (a sharp transition to a vertical position can lead to an orthostatic collapse).

    When parenteral administration of chlorpromazine should avoid the possibility of getting the drug on the mucous membranes and skin because of the risk of developing contact dermatitis.

    Neuroleptic malignant syndrome can occur at any time during treatment with neuroleptics and lead to death. In elderly patients with psychoses due to dementia, the development of irreversible dyskinesia is possible. When there are signs of neuroleptic syndrome and tardive dyskinesia, treatment should be canceled. Hyperthermia is one of the symptoms of malignant neuroleptic syndrome, so when it occurs chlorpromazine it should immediately be canceled and the cause of its occurrence established.

    During the period of therapy, due to the possibility of developing photosensitization of the skin, UV irradiation should be avoided, including prolonged exposure to the sun.

    During the treatment period, do not drink alcohol.

    Side effects:

    The frequency and severity of side effects of chlorpromazine depends on the dose of the drug, the duration of its use and the presence of concomitant diseases in the patient.

    The incidence of side effects is classified according to WHO recommendations: very often -> or = 10%, often -> or = 1%, but <10%; infrequently -> or = 0,1%, but <1%; rarely -> or = 0.01%, but <0.1%; very rarely, <0.01.

    From the side of the central nervous system: often - drowsiness, dizziness, anorexia, dry mouth, sleep disorders; rarely with prolonged administration in large doses - extrapyramidal reactions (dyskinesia, akineto-rigid phenomena, akathisia, hyperkinesia, tremor, vegetative disorders), phenomena of mental indifference, depression, thermoregulatory disorders, malignant neuroleptic syndrome; very rarely - cramps, catatonia.

    From the cardiovascular system: often - lowering blood pressure (especially with intravenous administration), tachycardia; rarely with compliance with the requirements for parenteral administration - orthostatic hypotension, arrhythmia, prolongation of the QT interval on the ECG.

    From the side of the digestive system: often - nausea, dyspepsia, constipation; infrequently - vomiting, diarrhea; rarely cholestatic jaundice.

    From the hemopoietic system: rarely - leukopenia, anemia, agranulocytosis, hypercoagulation.

    From the side of the urinary system: rarely - difficulty urinating, oliguria.

    On the part of the endocrine system: infrequently - amenorrhea, galactorrhea, hyperprolactinaemia, gynecomastia, weight gain, decreased potency.

    Allergic reactions: often - allergic reactions from the skin and mucous membranes (skin rash, itching); rarely - exfoliative dermatitis, erythema multiforme.

    From the side of the eye: often - blurred vision; infrequent - clouding of the lens and cornea.

    From the skin: rarely - skin pigmentation, photosensitivity.

    Local reactions: ingestion of chlorpromazine solutions under the skin, on the skin and mucous membranes can cause tissue irritation; the introduction into the muscle is often accompanied by the appearance of painful infiltrates; when injected into a vein, endothelial damage is possible.

    Overdose:

    Symptoms: areflexia or hyperreflexia, convulsions, confusion, severe breathing disorder, pulmonary edema, severe drowsiness or coma, tachycardia, arrhythmia, lowering of blood pressure, heart failure, shock, QRS tooth change on ECG, ventricular fibrillation up to cardiac arrest, trembling, muscle twitching, muscle stiffness, vomiting, uncontrolled movements, hyperpyrexia or hypothermia, narrowing of the pupils, blurred vision, dry mouth, agitation, later develops hepatitis.

    Treatment: There is no specific antidote. Assign a gastric lavage, Activated carbon. Induction of vomiting should be avoided, as a disturbance of consciousness and dystonic reactions from the muscles of the neck and head caused by an overdose can lead to aspiration of vomit.

    Treatment of symptomatic and maintenance therapy: with cardiac insufficiency appoint cardiac glycosides, with a marked decrease in blood pressure, the introduction of fluid, intravenously norepinephrine, phenylephrine (epinephrine it is impossible to apply, since it is possible to reduce the arterial pressure paradoxically due to the blockade of alpha-adrenergic receptors with chlorpromazine), with convulsions - diazepam (should avoid the appointment of barbiturates due to possible depression of the central nervous system and respiratory depression), with severe extrapyramidal reactions - diphenylhydramine. Dialysis is ineffective.

    For the next not less than 5 days, the cardiovascular system, central nervous system, liver and kidney function, body temperature, psychotic status of the patient should be monitored.

    Interaction:

    With the simultaneous use of chlorpromazine with drugs,which have a depressing effect on the central nervous system (tranquilizers, hypnotics, anesthetics, narcotic analgesics, lithium preparations, alcohol and ethanol-containing drugs), possible the potentiation of the depressant effect, as well as respiratory depression. Simultaneous administration of chlorpromazine with tricyclic antidepressants, maprotiline or inhibitors and monoamine oxidase increases the risk of neuroleptic malignant syndrome; with antithyroid drugs - the risk of agranulocytosis; with hepatotoxic agents - potentiates hepatotoxicity; with drugs that cause extrapyramidal disorders - increases the incidence and severity of extrapyramidal disorders; with hypotensive drugs - increases the reduction in blood pressure. Joint application with beta-adrenoblockers promotes strengthening of the hypotensive effect, increases the risk of developing irreversible retinopathy, arrhythmia and tardive dyskinesia.

    Chlorpromazine reduces the effect of indirect anticoagulants, the effectiveness of antiepileptic drugs, the antiparkinsonian effect of levodopa, the effects of amphetamines, clonidine and guanethidine,weakens the vasoconstrictive effect of ephedrine, distorts the effect of epinephrine - perhaps a paradoxical decrease in blood pressure, pressure due to blockade of alpha-adrenergic receptors with chlorpromazine.

    Chlorpromazine enhances the anticholinergic effects of other drugs, while its antipsychotic effect may be reduced. With simultaneous use with prochlorperazine a high risk of overdose and, as a result, a prolonged loss of consciousness.

    Chlorpromazine can mask the manifestation of ototoxicity of drugs, especially antibiotics.

    Barbiturates increase the metabolism of chlorpromazine, inducing microsomal enzymes of the liver, reduce its concentration in the blood.

    The long-term administration of chlorpromazine in combination with analgesics and antipyretics (hyperthermia may develop).
    Special instructions:

    During treatment with chlorpromazine, it is necessary to control blood pressure, heart rate, with prolonged use because of the risk of development of leukopenia, neutropenia, agranulocytosis, monitor the hematologic blood profile (including prothrombin index), ECG, monitor liver, kidney, vision.

    Chlorpromazine has no antiemetic effect in the case when nausea is a consequence of vestibular stimulation or local irritation of the digestive tract. The antiemetic effect of chlorpromazine can mask vomiting associated with an overdose of other drugs, or make it difficult to diagnose diseases, the primary manifestation of which is nausea. In patients who use the drug, the demand for riboflavin may be increased.

    In patients taking long-term chlorpromazine, there is an increase in body weight.

    To avoid local side reactions, solutions of chlorpromazine before administration should be diluted with solutions of procaine, dextrose or 0.9% sodium chloride solution.

    The appointment of phenothiazines should be discontinued no less than 48 hours before the proposed myelography (resume perhaps within 24 hours).

    To avoid withdrawal syndrome with prolonged use of the drug, the dose of chlorpromazine is reduced gradually.

    Effect on the ability to drive transp. cf. and fur:

    Patients receiving chlorpromazine, care should be taken when driving vehicles and engaging in potentially hazardous activities,requiring a high rate of psychomotor reactions.

    Form release / dosage:Solution for intravenous and intramuscular injection 25 mg / ml.
    Packaging:

    2 ml in the ampoule; 10 ampoules in a cardboard box.

    5 ampoules in a blister, 2 blisters in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001715
    Date of registration:02.07.2012
    The owner of the registration certificate:Health to the people - Kharkov Pharmaceutical Enterprise, LLC Health to the people - Kharkov Pharmaceutical Enterprise, LLC Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp29.09.2015
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