Haloperidol-Richter pills 5 mg N50
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Description
Tablets Haloperidol-Richter - an 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. Does not possess antihistaminergic or anticholinergic activity.
Active ingredients
Haloperidol
Release form
Pills
Composition
Active ingredient: haloperidol. Excipients: potato starch, colloidal silicon dioxide, gelatin, magnesium stearate, talc, corn starch, lactose monohydrate.
Pharmacological effect
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. Does not possess antihistaminergic or anticholinergic activity. The sedative effect is due to the blockade of the α-adrenoreceptors of the reticular formation of the brain stem, the antiemetic effect by the blockade of the dopamine D2 receptors of the trigger zone of the vomiting center, the hypothermic action and the galactorrhea by the blockade of the dopamine receptors of the hypothalamus. As a result of exposure to the basal ganglia, it causes extrapyramidal disorders (dystonia, akathisia, parkinsonism). Prolonged use is accompanied by a change in the endocrine status, prolactin production increases in the anterior pituitary gland and gonadotropic hormone production decreases. Haloperidol is highly effective in treating hallucinations and delusions. It has a pronounced soothing effect on psychomotor agitation, is effective in mania and other agitations, as well as an additional tool in the treatment of chronic pain.
Pharmacokinetics
Suction. When ingestion is absorbed by passive diffusion, in non-ionized form, mainly from the small intestine. Bioavailability - 60-70%.With oral administration, Cmax in the blood is reached in 2-6 hours, with i / m - in 20 minutes. The therapeutic effect occurs at a plasma concentration of 20-25 mg / l. Distribution. Haloperidol is 90% bound to plasma proteins, 10% is the free fraction. Vd in the equilibrium state - 7.9 ± 2.5 l / kg. The ratio of the concentration in erythrocytes to the concentration in plasma is 1:12. The concentration of haloperidol in the tissues is higher than in the blood; the drug tends to accumulate in the tissues. Easily passes through histohematogenous barriers, including placental and BBB. Penetrates into breast milk. Metabolism. Exposed to the "first pass" effect through the liver. Metabolized in the liver by oxidative N-dealkylation and glucuronidation. CYP2D6, CYP3A3, CYP3A5, CYP3A7 isoenzymes are involved in the metabolism of the drug. Is an inhibitor of CYP2D6. There are no active metabolites. Inference. T1 / 2 from blood plasma when administered orally - 24 hours (12-37 hours), after the / m injection - 21 hours (17-25 hours), after the / in - 14 hours (10-19 hours). Excreted in the form of metabolites with feces - 60% (including with bile - 15%), with urine - 40% (including 1% - unchanged).
Indications
Acute and chronic psychosis accompanied by agitation, hallucinatory and delusional disorders, manic states, psychosomatic disorders, behavioral disorders, personality changes (paranoid, schizoid and others), Gilles de la Tourette syndrome, both in childhood and in adults, tics, Gottington's chorea, prolonged and non-treatment vomiting, incl. associated with antitumor therapy, and hiccup, premedication before surgery.
Contraindications
Severe toxic depression of CNS function caused by xenobiotics, coma of various origins, CNS diseases accompanied by pyramidal and extrapyramidal disorders (Parkinson’s disease), pregnancy, lactation, children weighing up to 60 kg, lactase deficiency, lactose intolerance, glucose-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galacto-galactoctose. hypersensitivity to butyrophenone derivatives, hypersensitivity to the drug components.
Precautionary measures
The drug should be prescribed with caution in decompensated diseases of the cardiovascular system (including angina pectoris, impaired intracardiac conduction, prolongation of the QT interval on the ECG or susceptibility to this - hypokalemia, simultaneous use of other drugs that may cause prolongation of the QT interval), epilepsy, angle-closure glaucoma, hepatic and / or renal failure,hyperthyroidism (with symptoms of thyrotoxicosis), pulmonary cardiac and respiratory failure (including in COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.
Use during pregnancy and lactation
Haloperidol-Richter is contraindicated for use during pregnancy and lactation.
Dosage and administration
Is taken orally, during or after a meal, with a full (240 ml) glass of water or milk. The dose depends on the clinical response of the patient. Most often this means a gradual increase in dose in the acute phase of the disease, in the case of maintenance doses, a gradual reduction in dose to ensure the lowest effective dose. High doses are used only in cases of inefficiency of smaller doses. Medium doses are suggested below. The initial daily dose for adults is 1.5-5 mg, divided into 2-3 doses. If necessary, gradually increase the dose by 1.5-3 mg (in resistant cases to 5 mg) until the desired therapeutic effect is achieved. The maximum daily dose is 100 mg. The average therapeutic dose is 10-15 mg / day, in chronic forms of schizophrenia - 20-40 mg / day, if necessary, the dose can be increased to 50-60 mg / day. The maximum dose is 100 mg / day. On average, the duration of treatment is 2-3 months. Maintenance doses (without exacerbation) - from 0.5-0.75 mg to 5 mg / day (the dose is reduced gradually). In acute psychosis - a single dose of 1.5-5 mg (up to 10 mg) in pills, as a rule, every 4-8 hours. The daily dose for oral administration of the drug is not more than 100 mg. Maintenance therapy: vntry - from 0.5 mg to 20 mg / day. A minimum dose is applied that is able to maintain remission. With non-psychotic behavior disorders, Gilles de la Tourette syndrome, by mouth, initially 0.05 mg / kg / day in 2-3 doses, then the dose is gradually increased 1 time every 5-7 days to a total dose of 0.075 mg / kg / day. In childhood autism - inside 0.025-0.05 mg / kg / day. With ticks, Huntington's chorea - inside 0.025-0.05 mg / kg / day. If there is no effect for 1 month, treatment is not recommended to continue. With long-term persistent and resistant to therapy, vomiting - 1.5-2 mg 2 times / day. Elderly or debilitated patients are prescribed 1 / 3-1 / 2 of the usual dose for adults, the dose is increased no more often than every 2-3 days. For children with a body weight of 60 kg or more for psychotic disorders - by mouth 0.05 mg / kg / day in 2-3 doses, if necessary taking into account tolerability, gradually increase the dose once every 5-7 days to a total dose of 0.15 mg / kg / day.
Side effects
On the part of the nervous system: headache, dizziness, insomnia or drowsiness (varying severity), anxiety, akathisia, euphoria, depression, convulsive disorders, extrapyramidal disorders, with prolonged treatment - late dyskinesia (smacking of lips and puckering, cheekbones, 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, uncontrolled from ibayuschiesya movement of the neck, torso, arms and legs), and neuroleptic malignant syndrome (hyperthermia, muscle rigidity, labored or tachypnea, tachycardia, arrhythmia, increase or decrease in blood pressure, sweating, urinary incontinence, convulsive disorder, depression of consciousness). Since the cardiovascular system: when used in high doses - lowering blood pressure, orthostatic hypotension, arrhythmias (ventricular arrhythmias such as "pirouette"), ECG changes (lengthening of the QT interval, signs of fluttering and ventricular fibrillation), sudden death. 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 hematopoietic system: transient leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis. On the part of the urinary system: urinary retention (for example, with prostatic hyperplasia), peripheral edema. On the part of the reproductive system and the mammary gland: pain in the mammary glands, gynecomastia, hyperprolactinemia, menstrual disorders, decreased potency, increased libido, priapism. On the part of the organ of vision: cataract, retinopathy, blurred vision. Metabolism: hyponatremia, hyper or hypoglycemia. Dermatological reactions: maculopapular and acne-like skin changes, photosensitization. Allergic reactions: bronchospasm, laryngism. Other: alopecia, weight gain, heat stroke.
Overdose
In case of overdose of the drug, acute neuroleptic reactions may occur.Symptoms: muscle stiffness, tremor, drowsiness, decrease, sometimes increase in blood pressure, in severe cases - coma, respiratory depression, shock, prolongation of the QT interval on an ECG, arrhythmia. It should especially alarm the rise in body temperature, which may be one of the symptoms of neuroleptic malignant syndrome. In severe cases of overdose, various forms of impairment of consciousness can be observed, including coma, convulsive reactions. Treatment: by ingestion - gastric lavage, activated charcoal. With respiratory depression, mechanical ventilation may be required. With a decrease in blood pressure and collapse, plasma or concentrated albumin, dopamine or norepinephrine are injected to maintain blood circulation. Epinephrine in these cases is strictly prohibited to apply, because its administration may cause severe hypotension. For the relief of extrapyramidal symptoms - central m-holinoblokatory and anti-Parkinsonian drugs. Diazepam, a solution of dextrose, nootropes, vitamins of groups B and C are injected into / into. Dialysis is not effective. There is no specific antidote.
Interaction with other drugs
Increases the severity of the inhibitory effect on the central nervous system of ethanol, tricyclic antidepressants, narcotic analgesics, barbiturates and hypnotic drugs, agents for general anesthesia. Enhances the action of peripheral m-cholinoblockers and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from α-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 threshold for convulsive readiness and increases the risk of major epileptic seizures. Reduces the effect of anticonvulsants (reduction of the seizure threshold by haloperidol). It weakens the vasoconstrictor action of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of α-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 (blockade of dopamine receptors in 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 (haloperidol blocking of α-adrenoreceptors). M-cholinoblockers, histamine H1-receptor blockers of the 1st generation and anti-Parkinsonian drugs may enhance the m-cholinoblocking effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required). Prolonged use of carbamazepine, barbiturates and other inducers of liver microsomal enzymes decreases plasma haloperidol concentrations. In combination with lithium preparations (especially in high doses), encephalopathy may develop (it may cause irreversible neurointoxication) and reinforcement of extrapyramidal symptoms. With simultaneous use with fluoxetine increases the risk of side effects from the central nervous system, especially extrapyramidal reactions. 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.
special instructions
Parenteral administration should be carried out under the strict supervision of a physician, especially in elderly and pediatric patients. Upon reaching a therapeutic effect, one should switch to the oral form of treatment. Prescribing antipsychotic drugs (including haloperidol) to treat psychotic disorders associated with dementia in elderly patients poses a risk of death. During a 10-week, placebo-controlled clinical study, mortality in the group of patients receiving antipsychotic drugs was about 4.5%, compared with a frequency of about 2.6% in the placebo group. Most deaths were due to cardiovascular (for example, heart failure, sudden death) and / or infectious (for example, pneumonia) causes. Observational clinical studies have shown that traditional antipsychotic therapy can increase mortality.During treatment, ECG, blood formulas, and liver samples should be monitored regularly. Since haloperidol can cause lengthening of the QT interval, care should be taken if there is a risk of prolonging the QT interval (long QT interval syndrome, hypokalemia, use of drugs that cause the QT interval lengthening), especially when administered parenterally. Due to the fact that haloperidol is metabolized in the liver, it is important to exercise caution when prescribing the drug to patients with impaired liver function. Cases of the development of seizures caused by haloperidol are known. Patients with epilepsy and patients, in conditions that predispose to the development of convulsive syndrome (alcoholism, brain injury in history), the drug should be prescribed with extreme caution. For the relief of extrapyramidal disorders, anti-Parkinsonian drugs (cyclodol), nootropics, vitamins are prescribed, and their use is continued even after discontinuation of haloperidol, if they are eliminated from the body faster than haloperidol, in order to avoid an increase in extrapyramidal symptoms. With the development of tardive dyskinesia should not abruptly cancel the drug, it is recommended a gradual reduction in dose. Treatment is stopped gradually in order to avoid withdrawal. Care must be taken when performing heavy 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 "cough" over-the-counter drugs (possibly enhancing m-anticholinergic effects and the risk of heat stroke). Open skin should be protected from excessive solar radiation due to increased risk of photosensitivity. An antiemetic effect may mask the signs of drug toxicity and make it difficult to diagnose conditions whose first symptom is nausea. During drug treatment, alcohol consumption is not recommended. Effect on the ability to drive vehicles and control mechanisms: during the use of the drug is prohibited to drive vehicles and engage in other activities that require high concentration of attention and speed of psychomotor reactions.