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Haloperidol (Haloperidolum Haloperidoli) - neuroleptic, antipsychotic, sedative, antiemetic.
Blocks postsynaptic dopaminergic receptors located in the mesolimbic system (antipsychotic effect), hypothalamus (hypothermic effect and galactorrhoea), trigger zone of the vomiting center of the extrapyramidal system; It depresses the central alpha-adrenergic receptors. Inhibits release of mediators, reducing the permeability of the presynaptic membrane, it breaks the reverse neuronal capture and sequestration.
Removes persistent personality changes, delirium, hallucinations, delusions, reinforces the interest in the environment. It affects the autonomic functions (reduces the tone of hollow organs, gastrointestinal motility and secretion, eliminates the vascular spasms) in diseases involving excitement, anxiety, fear of death. The long reception accompanied by changes in endocrine status, in the anterior pituitary prolactin increases production and decreases - gonadotrophic hormones.
When ingestion absorbed 60%. Binding to plasma proteins - 92%. Tmax ingestion - 3-6 hours, with the / m introduction - 10-20 min, in / m introduction prolonged form (haloperidol decanoate) - 3-9 days (in some patients, especially in the elderly, - 1 day ). Intensively distributed in the fabric, since easily passes gistogematicalkie barriers, including GEB. Vss is 18 l / kg. It is metabolized in the liver, subjected to the effect of the first passage through the liver. A strict correlation between plasma concentration and effect has not been established. T1 / 2 at intake - 24 hours (12-37 hours), with the / m introduction - 21 hours (17-25 hours), with I / O - 14 hours (10-19 hours), haloperidol decanoate - 3 week (single or multiple doses). Excreted by the kidneys and the bile.
Efficient in patients resistant to other antipsychotic agents. It has some activating effect. In hyperactive children eliminates excessive motor activity, behavioral disorders (impulsivity, difficulty concentrating, aggressiveness).
Haloperidol should not be used as first-line therapy for treatment of behavioral and psychological symptoms of dementia. Its use in patients with dementia is only possible if a clear and imminent risk of dangerous consequences and causes severe pain symptoms, but preferably on the basis of the original specialist information and informed consent of the patient and the caregiver.
Haloperidol acts more actively in the productive symptoms (delusions, hallucinations) than negative. The evidence of its superiority is not received in relieving negative symptoms. Additionally, haloperidol and may itself provoke secondary negative symptoms (called neuroleptic-induced syndrome ficiency - NIDS).
In general, the new atypical antipsychotics have a more favorable safety profile (though and have their shortcomings) and are recommended as first-line drugs. Haloperidol should be used in the provision of emergency although atypical antipsychotics begin to displace him from that segment .
Application of the substance Haloperidol:
Precautions Haloperidol substance:
Increased mortality in elderly patients with psychosis associated with dementia. According to the Food and Drug Administration (FDA) 1, antipsychotic drugs increase mortality in elderly patients in the treatment of psychosis on dementia. An analysis of 17 placebo-controlled studies (duration 10 weeks) in patients treated with atypical antipsychotic drugs showed increased mortality associated with taking drugs, 1.6-1.7 times compared with patients receiving placebo. During a typical 10-week controlled studies percentage mortality associated with drug intake, it was about 4.5%, whereas in the placebo group - 2.6%. Although the causes of death were varied, most of them have been associated with cardiovascular problems (such as heart failure, sudden death) or pneumonia. Observational studies suggest that, similar to atypical antipsychotics, conventional antipsychotics treatment may also be associated with increased mortality.
Tardive Dyskinesia. As in the case of other antipsychotics haloperidol reception associated with the development of tardive dyskinesia - a syndrome characterized by involuntary movements (may occur in some patients during chronic treatment, or occur after drug treatment was discontinued). The risk of tardive dyskinesia higher in elderly patients with high-dose therapy, especially in women. The symptoms are persistent and in some patients - irreversible: involuntary rhythmic movements of the tongue, face, mouth or jaw (eg protrusion of tongue, inflating cheeks, puckering lips, uncontrolled chewing movements), sometimes they may be accompanied by involuntary movements of the limbs and trunk. With the development of tardive dyskinesia is recommended removal of the drug.
Dystonic extrapyramidal disorders are most frequent in children and young people, as well as at the beginning of treatment; may subside within 24-48 hours after discontinuation of haloperidol. Parkinsonian extrapyramidal effects are more likely to develop in older people and are identified in the first few days of treatment, or during prolonged therapy.
Cardiovascular Effects. Cases of sudden death, QT prolongation and torsades de pointes have been reported interval in patients treated with haloperidol. Caution should be exercised when treating patients with predisposing factors for prolongation of the QT interval, including electrolyte imbalance (particularly hypokalemia and hypomagnesemia), concomitant use of drugs prolonging the QT interval. When haloperidol is necessary to conduct regular monitoring of ECG, blood counts, to assess the level of liver enzymes. During therapy, patients should refrain from activities potentially hazardous activities that require attention, rapid mental and motor responses.
Symptoms: severe extrapyramidal disorders, hypotension, drowsiness, lethargy, in severe cases - coma, respiratory depression, shock.
Treatment: No specific antidote. Perhaps gastric lavage, followed by the appointment of activated charcoal (if an overdose is associated with ingestion). If respiratory depression - AV, with marked decrease in blood pressure - the introduction of plasma-liquids, plasma norepinephrine (but not the adrenaline!), To reduce the severity of extrapyramidal disorders - central holinoblokatory and antiparkinsonian agents.
The mode set individually. For relief of agitation adults - 5-10 mg / m or / in the possible single or double re-introduction in 30-40 minutes. Inside, the initial dose for adults - 0.5-5 mg 2-3 times a day, then gradually increase the dose until a sustained therapeutic effect (on average up to 10-15 mg / day for chronic forms of schizophrenia - up to 20-60 mg / day), followed by transition to a lower maintenance dose. The maximum daily dose - 100 mg.
The dose for children over 3 years calculated according to body weight.
Elderly or debilitated patients administered at a lower dose.
Solution for injection containing haloperidol decanoate - strictly in / m, the initial dose - 25-75 mg 1 every 4 weeks.
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