HALOPERIDOL DROPS 2MG/ML 30ML

Dosage form

oral drops, solution for intravenous and intramuscular administration, solution for intramuscular administration, solution for intramuscular administration [oil], tablets

Mechanism of action

Antipsychotic (neuroleptic), butyrophenone derivative. It has a pronounced antipsychotic effect, blocks postsynaptic dopamine receptors in the mesolimbic and mesocortical structures of the brain. High antipsychotic activity is combined with a moderate sedative effect (in small doses it has an activating effect) and a pronounced antiemetic effect. Causes extrapyramidal disorders, almost no anticholinergic action. Sedative effect due to blockade of alpha-adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2-receptors of the trigger zone of the vomiting center; hypothermic action and galactorrhea - blockade of dopamine receptors of the hypothalamus. Long-term use is accompanied by a change in the endocrine status, in the anterior lobe of the pituitary gland, prolactin production increases and decreases - gonadotropic hormones. Haloperidol decanoate in comparison with haloperidol has a longer effect.Eliminates persistent changes in personality, delusions, hallucinations, mania, increases interest in the environment. Effective in patients resistant to other neuroleptic drugs. It has some activating effect. In hyperactive children eliminates excessive motor activity, behavioral disorders (impulsivity, difficulty concentrating, aggressiveness). The therapeutic effect of the prolonged form can last up to 6 weeks.

Indications and usage

Psychoses (manic-depressive, epileptic, on the background of schizophrenia, alcoholic, medicinal, including "steroid"), psychomotor agitation of various genesis, delusions and hallucinations (paranoid states, acute psychosis), Tourette's disease, oligophrenia, agitated depression, Huntington's disease, prolonged persistent and resistant to therapy, hiccups, nausea and vomiting during Chemotherapy, stuttering, behavioral disturbance in the elderly and children (including hyper-reactivity in children, childhood autism), psychosomatic disorders.

Contraindications

Hypersensitivity, severe depression of CNS function against the background of xenobiotic intoxication, coma of various origins, CNS diseases accompanied by pyramidal or extrapyramidal symptoms (including Parkinson’s disease), depression, hysteria, pregnancy, lactation, childhood (up to 3 years). With caution. Decompensated diseases of the cardiovascular system (includingangina, impaired intracardiac conduction, lengthening the QT interval or susceptibility to this - hypokalemia, the simultaneous use of other drugs that can cause lengthening of the QT interval), epilepsy, angle-closure glaucoma, hepatic and / or renal insufficiency, thyrotoxicosis (with thyroid toxicosis) -cardiac and respiratory failure (including in COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Adverse reactions

On the part of the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, agitation, fear, akathisia, euphoria or depression, lethargy, epileptic seizures, the development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, including tardive dyskinesia (smacking and puckering of the lips, puffing up of the cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), late dystonia (frequent blinking or eyelid spasms, unusual facial expression or body position, uncontrollable flexing movements of the neck, body, hands and feet) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, muscle stiffness, epileptic seizures, loss of consciousness).From the side of the cardiovascular system: when used in high doses - lowering blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (lengthening of the Q-T interval, signs of ventricular flutter and fibrillation). On the part of the digestive system: when used in high doses - loss of appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, abnormal liver function, up to the development of jaundice. On the part of the blood-forming organs: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis. On the part of the urogenital system: urinary retention (with prostatic hyperplasia), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinemia, menstrual disorders, reduced potency, increased libido, priapism. From the senses: cataract, retinopathy, blurred vision. Allergic reactions: maculopapular and acne-like skin changes, photosensitivity, rarely - bronchospasm, laryngism. Laboratory indicators: hyponatremia, hyper- or hypoglycemia. Other: alopecia, weight gain. Overdose. Symptoms: muscle stiffness, tremor, drowsiness, decrease in blood pressure, sometimes - increase in blood pressure. In severe cases - coma, respiratory depression, shock. Treatment: by ingestion - gastric lavage, activated charcoal. When respiratory depression - ALV. To improve blood circulation in / injected plasma or albumin solution, norepinephrine.Epinephrine in these cases is strictly prohibited to use! Reduction of extrapyramidal symptoms - central holinoblockers and anti-parkinsonian drugs. Dialysis is ineffective.

Dosage and Administration

The drug should be taken orally, during or after a meal, drinking a full (240 ml) glass of water or milk, the initial dose for adults is 0.5-5 mg 2-3 times a day. If necessary, gradually increase the dose to achieve the desired therapeutic effect (on average - up to 10-15 mg, in chronic forms of schizophrenia - up to 20-60 mg). The maximum dose is 100 mg / day. Duration of treatment - 2-3 months. Reduce the dose slowly, maintenance doses - 5-10 mg / day. Elderly or debilitated patients at the beginning of treatment prescribed by mouth, 0.5-2 mg 2-3 times a day. Children 3-12 years old (or 15-40 kg body weight) for psychotic disorders - by mouth, 0.05 mg / kg / day in 2-3 divided doses; if necessary, taking into account tolerance, the dose is increased by 0.5 mg 1 time for 5-7 days to a total dose of 0.15 mg / kg / day. For non-psychotic behavior disorders, Tourette's disease is by mouth, initially 0.05 mg / kg / day in 2-3 divided doses, then the dose is increased by 0.5 mg 1 time in 5-7 days to 0.075 mg / kg / day. In childhood autism, by mouth, 0.025-0.05 mg / kg / day. In the absence of effect for 1 month, treatment is not recommended to continue. In acute conditions and in cases when oral administration is impossible, - in / in or in / m. When "indomitable" vomiting - 1.5-2 mg 2 times a day. The average single dose for i / m is 2–5 mg, the interval between injections is 4–8 hours. In acute psychosis, 5–10 mg i / i or i / m.The specified dose can be re-administered 1-2 times with an interval of 30-40 minutes to obtain the desired effect. The maximum daily dose is 100 mg. In acute alcoholic psychosis - in / in, 5-10 mg; with inefficiency, an additional infusion is performed at a dose of 10–20 mg at a rate of no more than 10 mg / min. The solution for injection, containing haloperidol decanoate, strictly i / m, 25 mg every 15-30 days, if necessary, may increase the dose to 100-150 mg (the interval between doses and dose is adjusted at intervals of at least 1 month).

Special notes

During therapy, patients should regularly monitor the ECG, blood count, "liver" samples. Parenteral administration of haloperidol should be carried out under the close supervision of a physician (especially in elderly patients and children); when therapeutic effect is achieved, it should be administered orally. With the development of tardive dyskinesia, a gradual reduction in the dose is recommended (up to the complete withdrawal of the drug). Care must be taken when doing hard physical work, taking a hot bath (thermal shock may develop due to suppression of central and peripheral thermoregulation in the hypothalamus). During treatment, one should not take "anti-cold" non-prescription drugs (perhaps increased anticholinergic effects and the risk of heat stroke). Open skin should be protected from excessive solar radiation due to increased risk of photosensitivity. Treatment is stopped gradually in order to avoid the appearance of the syndrome of "cancellation". An antiemetic effect may mask the signs of drug toxicity and make it difficult to diagnose conditions whose first symptom is nausea. When mixing a concentrated solution of haloperidol for ingestion with coffee, tea or lithium citrate as a syrup, free haloperidol may precipitate. Before prescribing a prolonged form, you must first transfer the patient from any other neuroleptic to haloperidol (prevention of unexpected hypersensitivity to haloperidol). It is noted that the doses for children 6 mg / day cause an additional improvement in behavioral disorders and tics. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Interaction:

Increases the severity of the inhibitory effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotic drugs, means for general anesthesia. Enhances the action of peripheral m-cholinergic blockers and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from alpha adrenergic neurons and the suppression of its capture by these neurons). It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, while their sedative effect and toxicity increase (mutually).When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of large epileptic seizures. Reduces the effect of anticonvulsants (reduction of convulsive threshold by haloperidol). Weaken the vasoconstrictor action of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of alpha-adrenoreceptors with haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure). Reduces the effect of anti-parkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system). Changes (may increase or decrease) the effect of anticoagulants. Reduces the effect of Bromocriptine (a dose adjustment may be required). When used with methyldopa, it increases the risk of developing mental disorders (including disorientation in space, slowing down and difficulty of thinking processes). Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psychostimulating effect (blockade by haloperidol alpha adrenoreceptors). Anticholinergic, antihistamine (first generation) and antiparkinsonian drugs can increase the m-anticholinergic blocking effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required). Prolonged use of Carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in the plasma.In combination with Li + drugs (especially in high doses), encephalopathy may develop (it may cause irreversible neurointoxication) and extrapyramidal symptoms may increase. When taken simultaneously with Fluoxetine, the risk of side effects from the central nervous system, especially extrapyramidal reactions, increases. With simultaneous use with drugs that cause extrapyramidal reactions, it increases the frequency and severity of estrapiramide disorders. The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.