Promazin (Promazinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation
  • Propazin
    pills inwards 
    TATHIMFARMPREPARATY, JSC     Russia
    • АТХ:

    N.05.A.A   The phenothiazine derivatives with an aliphatic structure

    N.05.A.A.03   Promazin

    Pharmacodynamics:

    Action antipsychotic (neuroleptic), sedative, antiemetic.

    Reduces the manifestations of psychosis: delusions and hallucinations. The antipsychotic effect is associated with the blockade of dopamine D2 receptors in the mesolimbic and mesocortical system. A block of dopamine D2-receptors in the chemoreceptor trigger zone of the vomiting center causes an antiemetic effect. Oppression of dopamine D2 receptors in the basal ganglia (nigrostriral zone) leads to drug parkinsonism (extrapyramidal disorders). The inhibition of D2- and D5-dopamine receptors in the tuberoinfundibular system causes hyperprolactinaemia, hypothermia, increased appetite and obesity. The block of central alpha2-adrenergic and H1-histamine receptors is a sedative effect. Peripheral alpha-adrenoblocking and H1-histamine-blocking effects are manifested by a decrease in blood pressure and an antiallergic effect. Has a strong sedative, anticholinergic and hypotensive effect, moderate antiemetic effect.

    Pharmacokinetics:Binding to plasma proteins - 90%. Cmax is achieved in 2-4 hours.Undergoes biotransformation in the liver with the formation of inactive metabolites. Excreted mainly by the kidneys.
    Indications:Acute and chronic psychoses accompanied by psychomotor agitation, hallucinatory and delusional disorders of any ethology; schizophrenia, manic conditions, agitated depression, psychotic disorders of any etiology, to alleviate withdrawal symptoms in narcological practice. Vomiting of various etiologies.
    ICD-10

    V.F20-F29.F20   Schizophrenia

    V.F20-F29.F21   Chrysotile disorder

    V.F20-F29.F22   Chronic delusional disorders

    V.F99.F99   Mental disorder without further clarification

    V.F20-F29.F25   Schizoaffective disorder

    V.F20-F29.F29   Inorganic psychosis, unspecified

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    Contraindications:

    Hypersensitivity, severe cardiovascular diseases (decompensated chronic heart failure, arterial hypotension, diseases accompanied by a risk of thromboembolic complications, severe oppression of the central nervous system and coma of any etiology, brain trauma, progressive systemic diseases of the brain and spinal cord, diseases of the liver, kidneys and hematopoietic organs with impaired functions, gastritis, peptic ulcer and 12 duodenal ulcer during an exacerbation, bronchiectatica disease in the stage of decompensation, angle-closure glaucoma, hyperplasia of the prostate with clinical manifestations, myxedema, pregnancy, lactation, children under 12 years.

    Carefully:Alcoholism (predisposedHepatotoxically(as a result of phenothiazine-induced prolactin secretion, the potential risk of disease progression and resistance to hormonal and cytostatic drugs increases), hepatic and / or renal failure, Parkinson's disease (extrapyramidal effects increase ), epilepsy, chronic diseases accompanied by respiratory failure (especially in children), Reye's syndrome (increased risk of hepatotoxicityand in children and adolescents); cachexia, vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs), elderly age.
    Pregnancy and lactation:

    Recommendations FDA category C. Long-term jaundice can develop in newborn children, hypo- and hyperreflexia, extrapyramidal symptoms.

    There is no information on the penetration into breast milk.

    ApplicationIn pregnancy, it is only possible if the benefit to the mother exceeds the potential risk to the fetus. For the duration of treatment, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside (after eating) 25-50 mg 2-4 times a day, gradually increasing to 0.4-0.6 g / day. The maximum daily dose is 1 g. Intramuscularly - 10-100 mg every 4-6 hours. The highest daily dose is 1 g. Elderly, debilitated or weakened patients require a smaller initial dose, if necessary gradually increase it.

    Use in children with psychotic disorders.
    Up to 12 years - is contraindicated; 12-18 years - 10-25 mg every 4-6 hours.

    Side effects:

    From the nervous system and sensory organs: dyspnea, dyskinesia, tardive dyskinesia, malignant neuroleptic syndrome, paradoxical reaction, cerebral edema, dyskinesia,convulsive seizures (especially in patients with EEG disorders or history of epilepsy), catalepsy, decreased motivation, headache, dizziness, increased intraocular pressure.

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): reduction of blood pressure, orthostatic hypotension (usually after the first parenteral administration), tachycardia, oppression of bone marrow hematopoiesis (agranulocytosis, anemia, leukopenia), prolongation of the QT interval, risk of ventricular rhythm disturbances (especially in the background of initial bradycardia, hypokalemia, prolonged QT interval).

    From the genitourinary system: atony of the bladder, difficulty urinating, priapism, amenorrhea, galactorrhea, decreased sexual function.

    On the part of the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, dry mouth, cholestatic hepatitis, intestinal atony, constipation.

    Allergic reactions: photosensitivity, skin pigmentation, angioedema.

    Other: swelling of mammary glands in women, gynecomastia in men, false positive pregnancy test, hyperglycemia / hypoglycemia, glucosuria, increased appetite and body weight, paralysis of accommodation, pigmentary retinopathy, melanosis, thermoregulation (thermal shock).

    When receiving neuroleptic phenothiazine series were cases sudden death (including possibly caused by cardiac causes).

    Overdose:

    Symtomas: slurring of speech, staggering gait, difficulty breathing, severe weakness, confusion, weakening of reflexes, drowsiness, agitation, disorientation, stupor, coma, convulsions, blurred vision, cardiotoxic effects (arrhythmia, heart failure, decreased blood pressure, shock, tachycardia, changes tooth QRS, ventricular fibrillation, cardiac arrest), mydriasis, xerostomia, hyperpyrexia or hypothermia, muscle rigidity, emesis, lung edema.

    Treatment: symptomatic. With arrhythmia - in / in phenytoin 9-11 mg / kg, with heart failure - cardiac glycosides, with a pronounced decrease in blood pressure - iv injection of liquid or vasopressor agents such as norepinephrine, phenylephrine (avoid the appointment of alpha and beta-adrenomimetics, such as epinephrine), with convulsions - diazepam, with parkinsonism - diphenyltropine, diphenhydramine. Control of cardiovascular function for at least 5 days, CNS function, respiration, body temperature measurement, psychiatrist consultation. There is no specific antidote. It is not removed during hemodialysis.

    Interaction:

    Bromocriptine - simultaneous use of promazine with bromocriptine can increase plasma concentrations of prolactin and reduce the effect of bromocriptine.

    Levodopa. With simultaneous use with promazine, the antiparkinsonian effect of levodopa is reduced due to the blocking of dopamine receptors.

    Maprotiline, tricyclic antidepressants or MAO inhibitors - an increased risk of developing a malignant neuroleptic syndrome.

    Epinephrine. When treatment with promazine should avoid the introduction of epinephrine, tk. possibly a perversion of the effect of epinephrine, which can lead to a drop in blood pressure.

    Ephedrine. With the simultaneous use of promazine with ephedrine, the vasoconstrictive effect of ephedrine may be reduced.

    When used simultaneously with drugs that exert a depressing effect on the central nervous system (including anxiolytics, opioid analgesics, hypnotics, anticonvulsants, anesthetics), it is possible to increase the oppressive effect on the central nervous system.

    Anticonvulsants - it is possible to lower the convulsive threshold.

    Drugs for the treatment of hyperthyroidism - increases the risk of agranulocytosis.

    Drugs that cause extrapyramidal reactions - may increase the frequency and severity of extrapyramidal disorders.

    Hypotensive drugs - possible pronounced orthostatic hypotension.

    Apomorphine - promazine reduces the effectiveness of the emetic action of apomorphine, enhances its inhibitory effect on the central nervous system.

    Promazin reduces the effect of funds that reduce appetite (with the exception of fenfluramine).

    Promazine can suppress the effects of amphetamines, clonidine, guanethidine.

    The drug enhances the anticholinergic effects of other drugs, while the antipsychotic effect of neuroleptic is reduced.

    When used simultaneously with a prochlorperazine related to the chemical structure, a prolonged loss of consciousness may occur.

    Incompatible with alcohol (additive effects and hypotension are possible).

    Special instructions:

    Usually the sedative effect of promazine is desirable, but in some cases promazine may cause undesired drowsiness.

    Extrapyramidal disorders were noted in hospitalized patients with high doses. These symptoms were reversible and passed with a lower dose or additional appointmentantiparkinsonian means. If symptoms are severe, treatment with promazine should be discontinued. In rare cases, persistent dyskinesia (involving the face, tongue, jaws), which is irreversible, was observed, especially in elderly patients with previous brain damage.

    The use of phenothiazines in patients with epilepsy in the history is possible only on absolute indications, in these cases, concomitant adequate adequate anticonvulsant therapy is necessary. It should be used with caution promazine in patients working at elevated temperatures, as well as in contact with phosphorus-containing insecticides (promazine can potentiate the effects of organic phosphates).

    Antiemetic action may mask the toxicity symptoms of other drugs, make it difficult to diagnose other diseases (eg, intestinal obstruction).

    Agranulocytosis develops between the 4th and 10th week of therapy. During this period, patients should particularly closely monitor the appearance of sore throat or symptoms of infection. With a significant decrease in the number of leukocytes, the drug should be stopped and appropriate therapy started.

    During treatment promazin requires careful monitoring of blood pressure and pulse, regular examination of the liver, kidneys, peripheral blood picture, examination of the oculist.

    During the treatment period, do not drink alcohol.

    Influence on the ability to drive vehicles and control mechanisms: When taking the drug should be abandoned driving vehicles or management mechanisms.

    Instructions
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