Haloperidol ratiopharm oral drops 2mg ml 30ml
Condition: New product
995 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Haloperidol
Release form
Drops
Composition
The composition of 1 ml: haloperidol 2 mg, Excipients: methyl parahydroxybenzoate - 90 mg, propyl parahydroxybenzoate - 10 mg, lactic acid - 170 mg, purified water - 99.7 g
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. Slows down the release of mediators, reducing the permeability of presynaptic membranes. 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 α-adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2-receptors in the trigger zone of the vomiting center; hypothermic action and galactorrhea - blockade of the 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. Eliminates persistent changes in personality, delusions, hallucinations, mania, increases interest in the environment.
Pharmacokinetics
Oral absorption - 60%. Cmax in plasma is achieved by ingestion after 3 h, after i / m administration -10-20 min. Vd - 15-35 l / kg. Plasma protein binding - 92%. Easily passes through histohematogenous barriers, including the blood-brain barrier. Penetrates into breast milk. Metabolized in the liver, exposed to the effect of the first passage through the liver. Haloperidol metabolism is accelerated by enzyme-inducing substances (phenobarbital, phenytoin, and carbamazepine). CYP2D6, CYP3A3, CYP3A5, CYP3A7 isoenzymes are involved in the metabolism of haloperidol. Is an inhibitor of CYP2D6. There are no active metabolites. T1 / 2 when taken orally - 24 hours (12-37 hours). It is excreted in bile and urine: after oral administration, 15% is excreted in bile, 40% in urine (including 1% - unchanged). Due to the large Vd and low plasma concentration, only a very small amount of haloperidol is removed by dialysis.
Indications
The drug is used strictly as prescribed by a doctor.Haloperidol-ratiopharm -drops are used in the following cases: Basic therapy of psychotic disorders in acute and subacute psychosis (schizophrenia, manic-depressive psychosis, oligophrenia, epileptic, alcoholic and other endogenous and exogenous-organic psychoses). Basic and so-called supportive therapy of chronic delusional and hallucinatory psychosis. Behavioral disorders in elderly and children, a variety of psychosomatic disorders.
Contraindications
Haloperidol-ratiopharm-drops is contraindicated in the following cases: Hypersensitivity to haloperidol and / or other butyrophenone derivatives or other substances of the finished dosage form. Acute intoxication with alcohol, opiates, hypnotics or psychogropic drugs that suppress the central nervous system. Coma. Pregnancy and lactation period. Children under 3 years. Patients with intolerance to alkyl-4-hydroxybenzoate. Haloperidol-ratiopharm-drops should be used with extreme caution in the following cases: Insufficiency of the liver and / or kidneys. Previous heart disease. Prolactin-dependent tumors, for example, breast cancer. Severe hypotension or orthostatic disregulation. Parkinson's disease. Endogenous depression. Diseases of the hematopoietic system. Malignant neuroleptic syndrome in history. Epilepsy and organic diseases of the brain. Hyperthyroidism. Children and adolescents, sick in old age. Before the start of treatment with haloperidol-ratiopharm-drops, it is necessary to conduct a blood test with the establishment of a differentiated picture of the blood corpuscles with the obligatory counting of the number of platelets. If pathology is detected, the use of haloperidol ratiopharm drops is possible only in case of urgent need and with mandatory repeated studies of the blood picture. The use during pregnancy and during breastfeeding: The use of haloperidol ratiopharm drops during pregnancy and during breastfeeding is contraindicated. Therefore, before starting treatment with a drug, a pregnancy test should be carried out, and during treatment, whenever possible, pregnancy should be avoided.During the period of treatment it is necessary to take measures to prevent the onset of pregnancy. The use of the drug haloperidol-ratiopharm -drops during breastfeeding is also advisable to avoid. In the event of the need for treatment with haloperidol during breastfeeding, the attending physician should carefully weigh the benefit / risk ratio.
Precautionary measures
On the part of the nervous system: headache, dizziness, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, agitation, fear, akathisia, euphoria, depression, lethargy, epilepsy attacks, the development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, including tardive dyskinesia (smacking and puckering of lips, inflation of cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of arms and legs), late dystonia (rapid blinking or eyelid spasms, unusual facial expression, unusual body position, uncontrollable curving neck movements, trunk, arms and legs), neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, mouse -lingual rigidity, seizures, loss of consciousness). Since the cardiovascular system: when used in high doses - lowering blood pressure, orthostatic hypotension, arrhythmia, tachycardia, ECG changes (prolongation of the QT interval, fluttering and ventricular fibrillation). On the part of the respiratory system: respiratory rhythm disturbance, shortness of breath, pneumonia (bronchopneumonia). On the part of the digestive system: when used in high doses - loss of appetite, dryness of the oral mucosa, hyposalivation, nausea, vomiting, diarrhea, constipation, abnormal liver function, jaundice. From the side of blood-forming organs: transient leukopenia or leukocytosis, agranulocytosis, erythropenia, 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.
Use during pregnancy and lactation
The use of the drug Haloperidol-ratiopharm during pregnancy is contraindicated. Before starting treatment, a pregnancy test should be performed. During drug treatment, it is necessary to use effective methods of contraception. Haloperidol is excreted in breast milk. The use of the drug Haloperidol-ratiopharm during breastfeeding is contraindicated.
Dosage and administration
Individual dosage is prescribed by the attending physician and depends on the clinical picture, the characteristics of the course of the disease, age and tolerability of the drug. The antipsychotic effect reaches its maximum only after 1-3 weeks of continuous treatment, the sedative effect appears almost immediately. In the outpatient setting, it is preferable to continuously build up single and daily dosages. In stationary conditions, treatment can begin immediately with the appointment of high doses, which allows you to quickly achieve the desired therapeutic effect. Sharp changes in dosage levels increase the risk of side effects. With long-term use of haloperidol, dosage reduction should be step-like and very slow (the next dose reduction should be carried out at sufficiently large intervals). The daily dose is divided into 1-3 doses, with high doses it is possible to take individual doses more frequently. If the doctor has not prescribed a different dosage, then the following treatment regimens are usually used. Haloperidol ratiopharm -drops are taken with food, metered with a teaspoon, added to drinks or food, or on a piece of sugar (except diabetics). Adults and adolescents at the beginning of treatment usually take 0.5-1.5 mg of haloperidol 2-3 times a day (initial daily dose of 0.5-5 mg). Then the dose is gradually increased by 0.5-2 mg per day (in resistant cases by 2-4 mg per day) until the desired therapeutic effect is achieved. When arresting acute symptoms in stationary conditions, the initial daily doses may be increased to 15 mg of haloperidol, in therapeutically resistant cases and higher. The maximum daily dose should not exceed 100 mg of haloperidol.The average therapeutic dose is usually 10-15 mg / day, in chronic forms of schizophrenia - 20-40 mg / day, in resistant cases - up to 50-60 mg / day. Maintenance doses (without exacerbation) on an outpatient basis can vary from 0.5 to 5.0 mg / day. Children older than 3 years (inside and parenterally) Treatment begins with a dose of 0.025-0.05 mg / kg body weight, divided into 2-3 doses. Increasing the dosage is possible up to 0.2 mg / kg body weight. Elderly patients and physically weakened patients (by mouth and parenterally). Treatment begins with single doses not exceeding 0.5-1.5 mg. It is desirable not to increase the daily dose above 5 mg. For children, elderly people and debilitated patients, doses are increased very slowly, no more than once every 3-5 days. SPECIAL INDICATIONS Haloperidol ratiopharm drops can cause extrapyramidal disorders in children, even at very low dosages, and also form poorly soluble complexes with black tea and coffee, which makes resorption difficult. With the simultaneous appointment of lithium and Halo-idol-ratiopharm-drops, the dosages of both drugs should be as low as possible.
Side effects
In the treatment of Haloperidol-ratiopharm, drops, many patients have side effects such as early dyskinesia (spasms of the chewing muscles, ocular crises, tension of the back muscles, jerky tongues, dystonic phenomena), Sindom Parkinson's (tremor, congestion) and akathia (motor restlessness) . It should be borne in mind that in children extrapyramidal syndrome often develops already at low dosages. In the event of early dyskinesia or Parkinson's syndrome, it is necessary to reduce the dosage or begin treatment with antiparkinsonian drugs (anticholinergics, for example, cyclodol). Treatment of akathisia is more complicated. At the beginning of treatment, try to reduce the dosage. If unsuccessful, they try to treat with sedative and hypnotic drugs and beta-blockers. Sometimes, especially at the beginning of treatment, hypotension or orthostatic dysregulation and reflex tachycardia occur. At the beginning of treatment, there may be a feeling of fatigue, and later - anxiety, tension, depressive mood disorders (especially with long-term treatment), insomnia, dizziness, and headaches.in rare cases, delirious symptoms and convulsive seizures. When using high doses, sometimes symptoms of vegetative dysregulation can be observed, such as accommodation disturbance, dry mouth, nasal congestion, increased intraocular pressure, constipation, nausea, retching, diarrhea, loss of appetite. In some cases, such violations of the blood picture are revealed, such as leukopenia, thrombocytopenia, eosinophilia, pancytopenia. in very rare cases - agranulocytosis. In some cases, galactorrhea, gynecomastia, sexual dysfunction, increased body weight may occur, and rarely vein thrombosis of the lower extremities may occur. In very rare cases, allergic reactions can be observed. In extremely rare cases, the development of a life-threatening malignant neuroleptic syndrome is observed. There is no effective treatment for this syndrome. When using haloperidol, it is necessary to regularly monitor the blood picture (every 2-4 weeks). In the case of a decrease in the number of leukocytes to or lower than 3000 / mm3 or other disorders, haloperidol treatment is stopped. It is also necessary to regularly check the functional state of the kidneys, liver and cardiovascular system (comparing the initial and current data of ECG studies). Patients should be informed that in cases of a rise in body temperature, gum inflammation or stomatitis, sore throat, signs of sore throat or sore throat during the first 3 months after treatment with haloperidol, they should not start self-treatment When a high temperature and muscle tension occurs, it is always necessary to remember about the possibility of a malignant neuroleptic syndrome, which is often mistakenly confused with catatonia. The treatment of this syndrome is very difficult and includes the following measures - the abolition of haloperidol. - treatment of hyperthermia with the help of cooling, since antipyretics are often ineffective.- treatment of disorders of water and electrolyte balance, cardiovascular disorders, infections, respiratory and renal complications. - specific treatment with dantrolene infusions (3-10 mg / day) in combination with bromocriptine (7.5-30 mg / day) orally. Treatment of drug addicts with cocaine intoxication can exacerbate extrapyramidal disorders. Warning During the administration of haloperidol, the imposition of vehicles and the maintenance of machinery, as well as other types of work that require high concentration of attention and fast motor reactions, are prohibited.
Overdose
Because of the broad therapeutic index, intoxication usually develops only in cases of severe overdose. Overdose symptoms: severe extrapyramidal disorders: acute dyskinetic or dystonic symptoms, glossopharyngeal syndrome, gaze cramps, spasms of the larynx, pharynx, drowsiness, sometimes coma, agitation and confusion with delirium, less often - epileptic seizures, hyperthermia or hypothermia, heart, heart, and hypothermia, heart disorder, delirium, hyperthermia, or hypothermia. decrease or increase in blood pressure, tachycardia or bradycardia, ECG changes, such as prolongation of the PQ and QT intervals, atrial flutter and ventricular fibrillation, cardiovascular insufficiency, rarely - m-cholino lokiruyuschie effects: blurred vision, increased intraocular pressure attack, paresis of the intestine, urinary retention, rare - respiratory complications: cyanosis, respiratory depression, respiratory failure, aspiration pneumonia. Treatment is symptomatic and supportive, in compliance with the general principles of treatment of overdose, and the following circumstances should be taken into account. Attempts to induce vomiting may be hampered by the antiemetic effect of antipsychotic drugs. Due to rapid absorption, gastric lavage is recommended only in cases of early diagnosis of overdose. Forced diuresis and dialysis are not very effective. Analeptics are contraindicated, because against the background of the use of haloperidol due to the decrease in the threshold of convulsive readiness, there is a tendency to develop epileptic seizures. If severe extrapyramidal symptoms develop, anti-parkinsonian drugs should be used, for example, biperiden in / in, it may be necessary to use anti-parkinsonian drugs for several weeks. Patients in coma undergo intubation. A spasm of the pharyngeal muscles may make it difficult to intubate, in which case it is possible to use short-acting muscle relaxants.In patients with symptoms of intoxication, ECG indicators and the main functional indicators of the body should be constantly monitored until they normalize. In case of arterial hypotension due to increased paradoxical effects, adrenaline preparations (epinephrine (adrenaline)) should not be used, affecting the blood circulation, instead norepinephrine-type preparations (for example, continuous norepinephrine (norepinephrine) drip infusions) or angiotensinamide should be used. Beta adrenomimetics should be avoided due to the fact that they cause increased vasodilation. Hypothermia is treated by slow warming. Infusion solutions for use in patients with hypothermia should be warmed up. In case of a high fever, antipyretic agents should be used, if necessary - ice baths. M-holinoblokiruyuschie symptoms can be stopped by the use of physostigmine (1-2 mg IV) (if necessary, repeat), the use in standard daily practice is not recommended due to the severe undesirable effects of this drug. Anticonvulsants are used to treat repeated epileptiform seizures, provided that artificial respiration is possible, since there is a risk of respiratory depression.
Interaction with other drugs
Simultaneous intake of eianol and haloperidol may increase the effect of alcohol and lead to arterial hypotension. Increases the severity of the inhibitory effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and other hypnotic drugs, agents 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 (lowering the threshold of seizure activity by haloperidol).Weakens the vasoconstrictor action of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of α-adrenoreceptors with haloperidol, can lead to a distortion of the action of epinephrine and to 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 (may require dose adjustment). When used with methyldopa, it increases the risk of developing mental disorders (including disorientation in space, slowing down and difficulties in thinking processes). Amphetamines reduce the antipsychotic effect of haloperidol, which, in turn, reduces their psychoactive effect (haloperidol blocking of α-adrenoreceptors). M-anticholinergic drugs, I-generation histamine H1-receptor blockers and antidiskinetic drugs can enhance the m-holinoblocking 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. With simultaneous use with lithium preparations (especially in high doses), encephalopathy may develop (it may cause irreversible neurointoxication) and increased extrapyramidal symptoms. 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, increases the frequency and severity of extrapyramidal disorders. The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.
special instructions
If you experience, especially in the first three months of treatment, fever, gingivitis and stomatitis, pharyngitis, purulent tonsillitis and flu-like symptoms, you should immediately consult with your doctor. Self-medication with analgesics should be avoided. Before treatment with haloperidol, patients need to conduct a general blood test (including differential calculation of blood corpuscles and platelet count), ECG readings and electroencephalogram. When abnormalities are detected, haloperidol can be used only when absolutely indicated and subject to mandatory control tests of general blood parameters.Before treatment, correction of hypokalemia is necessary. Patients with organic brain damage, arteriosclerotic cerebrovascular diseases and endogenous depression require special caution in haloperidol therapy. Since elderly patients and patients with concomitant diseases of the cardiovascular system may experience impaired intracardiac conduction, regular monitoring of cardiac activity is recommended during therapy. Patients with pheochromocytoma, renal insufficiency, heart failure, or cerebral insufficiency during therapy with haloperidol may develop hypotensive reactions, so these patients require careful monitoring. Although the prevalence of tardive dyskinesias has not been adequately studied, elderly patients (especially older women) are prone to developing this condition. The risk of developing late dyskinesias, especially of an irreversible type, increases with increasing duration of treatment and with the use of antipsychotic doses. Late dyskinesias may develop after short-term treatment in low doses. Antipsychotic treatment at the beginning may mask the symptoms of primary tardive dyskinesia. Symptoms may occur after drug withdrawal. 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 (possibly increasing m-anticholinergic effects and the risk of heat stroke). Open skin should be protected from excessive solar radiation due to the increased risk of photosensitivity reactions. 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 these conditions, the first symptom of which is nausea. Impact on the ability to drive motor vehicles and control mechanisms: During the period of treatment, it is necessary to avoid (especially in the early stages of treatment) or to be careful when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and psychomotor reactions.