2010/06/08

Haloperidol

Mode of action:
Antipsychotic drug (neuroleptic), a derivative butyrophenones. Possesses strong antipsychotic effect, blocking postsynaptic dopamine receptors in Mesolimbic and Mesocortical brain structures. High antipsychotic activity combined with moderate sedation (in small doses has a stimulative effect) and pronounced effect of antiemetics. Cause extrapyramidal disorders, has almost no anticholinergic action. Sedation due to the blockade of alpha-adrenergic receptors of the reticular formation of the brain; antiemetic effect - the blockade of dopamine D2-receptor trigger zone of the vomiting center; hypothermic effect and galactorrhea - blockade of dopamine receptors of the hypothalamus. The long reception accompanied by changes in endocrine status, in the anterior pituitary prolactin production increases and decreases - gonadotrophic hormones. Haloperidol decanoate in comparison with haloperidol has a more prolonged effect. Removes persistent personality changes, delirium, hallucinations, delusions, reinforces the interest in his surroundings. It is effective in patients resistant to other neuroleptic drugs. Has some activating effect. Do hyperactive children eliminates excessive motor activity, behavioral disorders (impulsivity, difficulty in concentration, aggressiveness). Therapeutic effect of prolonged form can last up to 6 weeks.

Indications:
Psychoses (manic-depressive, epileptic, against the background of schizophrenia, alcohol, drug, including "steroid"), psychomotor agitation of various origins, delusions and hallucinations (paranoid state, acute psychosis), Tourette's disease, mental retardation, agitated depression, Huntington's chorea, long persistent and resistant to therapy hiccups, nausea and vomiting during chemotherapy, stuttering, behavioral disorders in the elderly and childhood (including hyperreactivity in children with infantile autism), psychosomatic disorders.

Contraindications:
Hypersensitivity, severe depression of central nervous system functions against the toxic xenobiotics, the coma of various origins, central nervous system disease, accompanied by pyramidal and extrapyramidal symptoms (including Parkinson's disease), depression, hysteria, pregnancy, lactation, infancy (up to 3 years). C carefully. Decompensated disease CAS (including angina, a violation of intracardiac conduction, long QT, or predisposition to it - hypokalemia, the simultaneous use of other drugs that can cause lengthening of the interval QT), epilepsy, closure glaucoma, liver and / or renal failure , thyrotoxicosis (with symptoms of thyrotoxicosis), pulmonary heart and respiratory failure (including patients with COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Side effects:
Of the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), the state of anxiety, anxiety, agitation, anxiety, akathisia, euphoria or depression, lethargy, epilepsy, development of a paradoxical reaction - exacerbation of psychosis and hallucinations, with long-term care - extrapyramidal disorders, including tardive dyskinesia (prichmokivanie and puckering his lips, bombast, fast, and vermiform movements of the tongue, uncontrolled chewing movements uncontrolled movements of hands and feet), late dystonia (rapid blinking or spasms of eyelids, unusual facial expression or body position, curving uncontrolled movement of the neck, torso , hands and feet), and neuroleptic malignant syndrome (difficulty or shortness of breath, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, incontinence, muscle rigidity, seizures, loss of consciousness). On the part of the SSA: the use of high dose - lowering blood pressure, orthostatic hypotension, arrhythmia, tachycardia, ECG changes (prolongation of the interval QT, signs flutter and ventricular fibrillation). On the part of the digestive system: the application of high doses - decreased appetite, dry mouth, sialoschesis, nausea, vomiting diarrhea or constipation, abnormal liver function, until the development of jaundice. From the side of hematopoiesis: rarely - temporary leukopenia or leukocytosis, agranulocytosis, and the tendency to eritropeniya monocytosis. On the part of the genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema Pain in breasts, gynecomastia, hyperprolactinemia, menstrual disorders, lower potency, increase libido, priapism. On the part of the senses: cataract, retinopathy, blurred vision. Allergic reactions: maculopapular and akneobraznye skin changes, photosensitivity, rarely - bronchospasm, laryngism . Laboratory indicators: hyponatremia, hyper-or hypoglycemia. Other: alopecia, increased weight tela.Peredozirovka. Symptoms: muscular rigidity, tremor, somnolence, decrease blood pressure, sometimes - increase blood pressure. In severe cases - coma, respiratory depression, shock. Treatment: ingestion - gastric lavage, activated charcoal. When respiratory depression - AV. To improve blood circulation in / injected plasma or albumin solution, norepinephrine. Epinephrine in these cases use is strictly prohibited! Reduced extrapyramidal symptoms - central holinoblokatory and antiparkinsonian drugs. Dialysis is ineffective.

Dosage and administration:
Inside, during or after a meal, with a full (240 ml) glass of water or milk, the initial dose for adults - 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 schizophrenia - up to 20-60 mg). The maximum dose - 100 mg / day. Duration of treatment - 2-3 months. Reduce dose slowly, maintenance doses - 5.10 mg / day. Older or debilitated patients at the beginning of treatment prescribed by mouth, by 0.5-2 mg 2-3 times daily. Children 3-12 years old (or weighing 15-40 kg) with psychotic disorders - by mouth, 0.05 mg / kg / day in divided doses 2-3, if necessary, taking into account the tolerance dose increased to 0.5 mg 1 every 5-7 days to a total dose of 0.15 mg / kg / day. In non-psychotic behavioral disorders, Tourette's disease - mouth, initially 0.05 mg / kg / day in 2-3 divided doses, then dose increased to 0.5 mg 1 every 5-7 days to 0.075 mg / kg / day. In infantile autism - inside, 0.025-0.05 mg / kg / day. In the absence of effect within 1 month of therapy is not recommended to continue. In acute conditions, and in cases where oral intake is impossible - in / or / m In the "indomitable" vomiting - at 1.5-2 mg 2 times a day. The average single dose for the i / m - 2.5 mg, the interval between the injections - 4-8 hours in acute psychosis - 5-10 mg / in or / m The given dose can be re-enter 1-2 times at intervals of 30-40 minutes to obtain the desired effect. The maximum daily dose - 100 mg. In acute alcoholic psychosis - a / c, 5-10 mg, with ineffective conduct additional infusion at a dose of 10-20 mg at a rate not exceeding 10 mg / min. Solution for injection containing haloperidol decanoate, strictly V / m, 25 mg every 15-30 days, if necessary, may increase the dose to 100-150 mg (interval between doses and dose adjust at intervals of not less than 1 month).

Cautions:
During therapy patients should regularly monitor the ECG, hemogram, "liver" tests. Parenteral haloperidol should be carefully monitored by a physician (especially in elderly patients and children) in achieving the therapeutic effect should go to the reception inside. With the development of late dyskinesia recommend a gradual reduction in dose (up to a full withdrawal of the drug). Be careful when carrying out hard physical work, taking a hot bath (development of heat stroke due to suppression of central and autonomic thermoregulation in the hypothalamus). During the treatment should not be taken "protivoprostudnye" OTC drugs (may increase anticholinergic effects and risk of heat stroke). It is to protect exposed skin from excessive solar radiation due to increased risk of photosensitivity. Treatment stopped gradually to avoid the syndrome of "cancel". antiemetic effect may mask signs of drug toxicity and complicate diagnosis states the first symptom of which is the nausea. By mixing the concentrated solution for oral haloperidol with coffee, tea or lithium citrate as a syrup free haloperidol may precipitate. Before the appointment of a prolonged form should first transfer the patient from any other in the neuroleptic haloperidol (prevention of an unexpected high sensitivity to haloperidol). It is noted that the dose for children 6 mg cause additional improvement in behavioral disturbances and ticks. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and quickness of psychomotor reactions .

Interactions:
Increases expression of inhibitory effect of ethanol on the CNS, tricyclic antidepressants, opioid analgesics, barbiturates and sleeping drugs, funds for general anesthesia. Intensifies the effect of peripheral m-holinoblokatorov and the majority of antihypertensive drugs (reduces the effect of guanetidina due to the displacement of its alpha-adrenergic neurons and suppression of its capture these neurons). inhibits metabolism of tricyclic antidepressants and MAO inhibitors, with increases (relatively) of their sedative effects and toxicity. With simultaneous application with bupropion reduces epileptic threshold and increases the risk of large seizures. reduces the effect of anticonvulsants (decreased convulsant threshold for haloperidol) . Attenuates vasoconstrictor effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (an alpha-adrenergic blockade of haloperidol, which may lead to a distortion of epinephrine and a paradoxical decrease in BP). Reduces the antiparkinsonian effect of (an antagonistic effect on dopaminergic structures of the CNS). Modifies (may increase or decrease) the effect of anticoagulants. Reduces the effect of bromocriptine (may require dose adjustment). In the application of methyldopa increases the risk of developing mental disorders (including the disorientation in space, to slow and the difficulty of thought processes). Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their inducing effect (haloperidol blockade of alpha-adrenergic receptors). Anticholinergic, antihistamine (I generation), and antiparkinsonian drugs may increase the m-anticholinergic effects of haloperidol and reduce its antipsychotic action (may require dosage adjustment). Long-term appointment of carbamazepine, barbiturates and other inducers of microsomal oxidation of reduced haloperidol concentrations in plasma. In combination with drugs Li + (especially in high doses) may develop encephalopathy (may cause irreversible neurointoxications) and increased extrapyramidal symptoms. With simultaneous reception with fluoxetine increases the risk of side effects from the CNS, particularly extrapyramidal reactions. With simultaneous use with drugs that cause extrapyramidal reactions, increases the frequency and severity estrapiramidnyh disorders. The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.