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Dosage form
coated tablets
Pharmachologic effect:
Antipsychotic agent (neuroleptic), a derivative of thioxanthene (in structure and pharmacological properties similar to phenothiazines derivatives of piperazine). It also has a sedative, antiemetic, hypothermic, antidepressant and antihistamine effect. The antipsychotic effect is due to the blockade of the dopamine D2 receptors of the mesolimbic and mesocortical system. It has antiserotoninovoy, cholino-, adreno-, dopamine-blocking activity. The sedative effect is due to the blockade of the adrenoreceptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2-receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus; antihistamine - blockade of histamine H1 receptors. Suppresses the release of most hormones of the hypothalamus and pituitary gland. At the same time, as a result of the blockade of prolactin-inhibiting factor inhibiting the release of prolactin from the pituitary gland, the concentration of prolactin increases.
Indications:
Reactive and neurotic depressions with predominant anxiety symptoms, agitation (fear, tension), brain injuries, psychosis (including delirious, with schizophrenia, manic states), psychotherapy (auxiliary drugs), withdrawal syndrome in drug addiction and alcoholism; anxiety causing difficulty falling asleep; dyscirculatory encephalopathy, premedication, condition after operations, anxiety (including in patients with burns), pruritic dermatosis, menopausal depression. Long-term therapy: agitation, anxiety. In child psychiatry, psychosomatic and neurotic disorders, behavioral disorders; in pediatrics and therapy - insomnia, allergic diseases, bronchospasm, gastrointestinal spasm, vomiting, pain syndrome (in combination with analgesics).
Contraindications:
Hypersensitivity (including to phenothiazines), pathological changes in blood, bone marrow suppression, collapse, CNS depression or comatose states caused by the use of drugs, pregnancy, lactation, children (up to 6 years).C caution. Alcoholism (depression of the central nervous system may increase), cardiovascular diseases (risk of a transient increase in blood pressure), glaucoma (including susceptibility to it), gastric ulcer and duodenal ulcer, respiratory failure associated with acute infectious diseases, asthma or emphysema lung, urinary retention, liver failure, Parkinson's disease (increased extrapyramidal effects), prostatic hyperplasia with clinical manifestations (risk of urine retention), Reye's syndrome (increased risk of hepatotoxic action), ep ilepsia (as a result of a decrease in the convulsive threshold, seizures may increase).
Side effects:
On the part of the nervous system: fatigue, dizziness, psychomotor retardation, mild extrapyramidal hypokinetic-hypertensive syndrome, akathisia (during the first 6 hours after administration), dystonic reactions, persistent tardive dyskinesia, rarely - malignant neuroleptic syndrome, late dystonia. On the part of the cardiovascular system: orthostatic hypotension, tachycardia, a change in the Q-T interval on the ECG. From the sensory organs: clouding of the cornea and / or lens with a possible visual impairment, paresis of accommodation. On the part of the digestive system: dry mouth, constipation, cholestatic jaundice (more likely between 2-4 weeks of treatment). From the side of blood-forming organs: rarely - agranulocytosis (more likely between 4-10 weeks of treatment), leukopenia, hemolytic anemia. On the part of the endocrine system: dysmenorrhea, galactorrhea, gynecomastia, diabetes mellitus, decreased potency and / or libido, increased appetite, altered carbohydrate metabolism, increased body weight, increased sweating. On the part of the urinary system: urinary retention. Allergic reactions: skin rash, dermatitis, photosensitivity. Other: the syndrome of "cancellation", "flushes" of blood to the face. Overdose. Symptoms: convulsions, respiratory failure, severe drowsiness, coma, tachycardia, hyperthermia, decreased blood pressure, tremor, muscle twitching, stiffness or uncontrolled movements, miosis, agitation, excessive fatigue or weakness. Treatment: early gastric lavage, the appointment of Activated carbon and saline laxative, symptomatic and supportive therapy. Dialysis is ineffective. Do not try to induce vomiting, as dystonic reactions are possible in the head and neck, which can lead to aspiration of vomitus.
Dosage and administration
Inside Adults with neurosis - 10-15 mg at bedtime, if necessary - 30 mg at bedtime; with psychosis - usually 1 single dose at bedtime (100-600 mg), if necessary, an additional dose may be administered during the day, the highest dose is prescribed in the evening; with itching - 15-100 mg in 4 divided doses. Children 6-12 years old with neurosis - 5-30 mg per day; with psychosis - 100-200 mg per day or more. For elderly and debilitated patients, the initial dose should be reduced, and if necessary (taking into account tolerance), the dose should be gradually increased.
Special instructions:
In very rare cases, a paradoxical increase in anxiety is possible, and a transition to an antipsychotic drug with a more pronounced effect (haloperidol) is recommended. It must be borne in mind that during therapy it is possible to obtain a false positive result when conducting an immunobiological test of urine for pregnancy, false indicators of hyperbilirubinemia. In order to avoid the development of "cancellation" syndrome, it is necessary to stop treatment gradually. Dystonic reactions are most frequent in children and young patients; usually appear early in the treatment process and may subside within 24-48 hours after stopping treatment. Parkinsonian extrapyramidal effects may occur in the first few days of treatment, but usually their frequency increases with increasing dose; may be more frequent in older patients and older children. Late dyskinesia at the beginning of treatment is dose-dependent, but its frequency may increase with prolonged treatment and as the total dose is reached; may persist after discontinuing the use of thioxanthenes. A malignant neuroleptic syndrome may occur at any time during the period of treatment with antipsychotic drugs (neuroleptics), but more often it develops soon after the start of therapy or after transferring a patient from another neuroleptic, during combined treatment with another psychoactive drug or after increasing the dose. Although not all of the side effects listed are specifically associated with every thioxanten, there is a possibility that they may occur with the use of any drug from this group. During the period of treatment, it is necessary to carry out a blood test and determination of leukocyte formula, monitoring of liver function indicators, an ophthalmologic examination, as well as careful observation to detect early signs of tardive dyskinesia and dystonia. The likelihood of hypotensive and extrapyramidal reactions in adolescents is higher than in adults. During treatment, you should refrain from taking ethanol, exposure to extremely high temperatures (the risk of heat stroke), insolation, and also be careful when driving vehicles and occupying others.potentially hazardous activities that require increased concentration of attention and quickness of psychomotor reactions.
Interaction:
Increases the effect of antihypertensive drugs, reduces - levodopa. Reduces the hypotensive effect of guanethidine due to its displacement from adrenergic neurons and the inhibition of its capture by these neurons. Reduces the effect of antiepileptic drugs (due to increased threshold of seizure activity), which may require correction of the dosage regimen. May mask the symptoms of ototoxicity (tinnitus, dizziness) of ototoxic drugs (especially antibiotics). The perversion of the peripheral vasoconstrictive action caused by dopamine in high doses, epinephrine and ephedrine (the presence of Chlorprothixene alpha-adreno-blocking action) is possible. Preliminary administration of thioxanthenes can reduce the vasoconstrictor effect of phenylephrine. Due to hyperprolactinemia, a correction of the Bromocriptine dosage regimen may be required. Epinephrine increases the risk of hypotension and tachycardia; phenothiazines, Metoclopramide , Haloperidol , reserpine - the risk of extrapyramidal disorders. M-anticholinergic drugs enhance the anticholinergic effect. Compatible with thymoleptics (including Amitriptyline , nortriptyline, imipramine, dosulepin). Quinidine - increased risk of side effects from the heart.Ethanol, general anesthetics, narcotic analgesics, sedatives, hypnotics and antipsychotic drugs increase the inhibitory effect on the central nervous system.