Sonapax coated pills 10mg N60
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Active ingredients
Thioridazine
Release form
Pills
Composition
1 tablet contains: Active ingredient: thioridazine hydrochloride 10 mg. Auxiliary substances: corn starch - 8 mg, colloidal silicon dioxide - 1.5 mg, lactose monohydrate - 26.4 mg, gelatin - 0.1 mg, stearic acid - 1 mg, talc - 3 mg. The composition of the shell: sucrose - 35.799 mg, acacia gum - 0.5 mg, talc - 13.70 mg, crimson dye (Ponzo 4R) - 0.001 mg.
Pharmacological effect
Thioridazine is a piperidine derivative of phenothiazine, affecting the central and peripheral nervous system. It has an antipsychotic, tranquilizing, anti-depressive, antipruritic and anti-emetic effect. The mechanism of antipsychotic action is due to the blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain. The central antiemetic effect is due to the inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the brain stem, and the peripheral blockade of the vagus nerve in the gastrointestinal tract. Also has α-adrenoblokiruyuschim and m-anticholinergic effects. The blockade of histamine H1 receptors and m-cholinergic receptors is most pronounced among all antipsychotics. In small doses, it has an anxiolytic effect, reduces the feeling of tension and anxiety, in higher doses, it exhibits antipsychotic (neuroleptic) properties. Increases pituitary secretion of prolactin. Thioridazine prolongs the QTc interval in a dose-dependent manner, which can lead to severe life-threatening ventricular arrhythmias, including pirouette tachycardia.
Pharmacokinetics
Absorption is high, the time to reach Cmax in blood plasma is 1-4 hours after ingestion. About 90% of thioridazine binds to plasma proteins. Metabolized in the liver to form active metabolites (mezoridazin and sulphoridazin). T1 / 2 - 6-40 hours. Mezoridazine is pharmacologically more active than the original substance, has a greater T1 / 2, less binds to plasma proteins, the free fraction is higher than that of thioridazine. It is excreted unchanged and in the form of metabolites - by the kidneys (35%), by the intestines. It is excreted in breast milk.
Indications
Schizophrenia, incl. paranoid, schizoaffective disorders. psychosis, incl. involutionary. psychosomatic disorders.depression, accompanied by a feeling of fear. abstinence syndrome in chronic alcoholism, itching (severe, painful) in skin diseases, behavioral disorders (increased psychomotor activity) in children.
Contraindications
Hypersensitivity (including to phenothiazine derivatives), depression (acute condition), coma, pheochromocytoma, porphyria, hematopoietic insufficiency, I term and last week of pregnancy, children under 4 years of age.
Precautionary measures
With caution used in prostatic hypertrophy with difficulty urinating, angle-closure glaucoma, myasthenia gravis, Parkinson's disease, diseases of the cardiovascular system, peptic ulcer disease, renal and / or liver failure. With long-term treatment, it is necessary to control the blood picture. Should not be used while working drivers of vehicles and people whose profession is associated with increased concentration of attention. During treatment eliminated the use of alcohol. Cancel the drug should be gradually.
Use during pregnancy and lactation
In pregnancy, the use of the drug is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. Adequate and well-controlled studies of the safety of the drug during pregnancy have not been conducted. If necessary, the appointment of the drug during lactation breastfeeding should be discontinued.
Dosage and administration
Inside Dosage regimen is individual (depending on indications and therapeutic response). In psychosis: adults usually - 150-400 mg / day in 3-4 doses on an outpatient basis, in the hospital - 250-800 mg / day. Treatment usually starts with low doses, 25–75 mg / day, gradually increasing them to the optimal therapeutic dose, which is achieved within 7 days (the antipsychotic effect is noted after 10–14 days). The course of treatment is several weeks. Supporting daily dose - 75-200 mg once before bedtime. Older people usually use low doses of 30–100 mg / day. Drug should be canceled gradually. For mild mental and emotional disorders: therapeutic dose - 50-200 mg / day. Treatment should begin with low doses, gradually increasing them to the optimal therapeutic dose. In psychosomatic disorders - 10–75 mg / day. To suppress severe itching: the dose of the drug is set individually, and it should not exceed 200 mg.Children from 4 to 7 years old - 10–20 mg / day in 2-3 doses per day; from 8 to 14 years - 20–30 mg / day in 3 doses per day; From 15 to 18 years old - 30–50 mg / day in 2–3 doses per day.
Side effects
From the nervous system and sensory organs, parkinsonism syndrome, dyskinesia, akathisia, drowsiness, apathy, irritability, depression, delirium, convulsive seizures, impaired thermoregulation. leukopenia, eosinophilia, pancytopenia, thrombocytopenic purpura. From the side of the digestive tract organs constipation, cholestatic jaundice. From the side of the skin allergic reactions, discoid lupus, photosensitization. Other hyper- or hypoglycemia, gynecomastia, menstrual disorders, decrease in libido.
Overdose
Symptoms: Since the cardiovascular system: arrhythmias, lowering blood pressure, shock, ECG changes, prolonged QT and PR intervals, nonspecific ST segment and T wave changes, bradycardia, sinus angina pectoris, AV blockade, ventricular tachycardia, ventricular fibrillation, pirouette tachycardia, myocardial function depression. For the central nervous system: sedation, extrapyramidal disorders, confusion, agitation, hypothermia, hyperthermia, convulsions, areflexia, coma. For the autonomic nervous system: mydriasis, miosis, dry skin and mucous th shell of the mouth, nasal congestion, urinary retention, blurred vision. On the part of the respiratory system: respiratory depression, apnea, pulmonary edema. On the part of the digestive system: decreased motility, constipation, intestinal obstruction. From the urinary system: oliguria, uremia. Toxicity begins to manifest when the concentration of thioridazine in the plasma is more than 10 mg / l, at a concentration of 20-80 mg / l death occurs. Treatment: It is necessary to ensure the patency of the respiratory tract and to establish adequate oxygenation and pulmonary ventilation. Immediately begin long-term monitoring of cardiovascular activity (ECG). Treatment consists of the correction of electrolyte disturbances and acid-base balance, the introduction of lidocaine (caution is recommended due to the increased risk of seizures), phenytoin, isoproterenol, up to the installation of artificial pacemakers and defibrillation. In view of the possible additional lengthening of the QT interval, the use of disopyramide, iodine and quinidine should be avoided. Correction of reduced blood pressure may require the introduction of infusion solutions and vazopressorov.With persistently low blood pressure, administration of fsilephrine, norepinephrine, or metaraminol is indicated. Alpha-adrenergic blocking properties of phenothiazine derivatives do not allow the use of non-selective alpha- and beta-adrenomimetics (epinephrine, dopamine) - the risk of paradoxical vasodilation. To remove an unabsorbed dose of the drug, it is recommended to perform gastric lavage with activated carbon. Induction of vomiting is less preferable due to the risk of dystopia and the potential aspiration of vomitus. Acute extrapyramidal disorders stop by diphenhydramine or trihexyphenidyl. When arresting seizures, the introduction of barbiturates should be avoided (risk of exacerbation of respiratory depression). Due to the high volume of distribution and strong binding to plasma proteins, forced diuresis, hemoperfusion, hemodialysis, and changes in urine pH most likely do not affect the elimination of phenothiazine derivatives from the body.
Interaction with other drugs
Synergism of action with general anesthetics, narcotic analgesics, barbiturates, ethanol, atropine. Intensifies the hepatotoxic effect of hypoglycemic agents. With amphetamine, it acts antagonistically. With levodopa, it reduces the anti-Parkinsonian effect. Used with epinephrine, it can lead to a sudden and pronounced decrease in blood pressure. the action of anticoagulants. The action of thioridazine may weaken anticonvulsant drugs, cimetidine. Quinidine potentiates the cardiodepressive action Ephedrine contributes to a paradoxical decrease in blood pressure. Sympathomimetics increase arrhythmogenic effects. Probucol, aardicitis, cisapride, disopyramide, erythromycin, pimozide, procainamide, and quinidine contribute to an additional lengthening of the QT interval, which increases the risk of ventricular tachycardia. means reducing appetite (with the exception of fenfluramine). Reduces the effectiveness of the emetic effect of apomorphine,enhances its inhibitory effect on TsNS.Povyshaet prolactin concentration in the plasma and prevents the action bromokriptina.Pri simultaneous use of tricyclic antidepressants, maprotiline, MAO inhibitors, blockers of histamine H1-receptor may elongation and increased sedation and anticholinergic effektov.S m-thiazide diuretics - gain With lithium preparations - reduction of absorption in the gastrointestinal tract, an increase in the rate of removal of lithium ions by the kidneys, increased severity of extrapyramidal disorders, wounds Symptoms of lithium intoxication (nausea and vomiting) can be masked by the antiemetic effect of thioridazine. In combination with beta-blockers, the hypotensive effect is enhanced, the risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia is increased. Interaction with drugs that prolong the QT interval (cytrophytes) and tardive dyskinesia. inhibitors of the isoenzyme CYP2D6 (fluoxetine, paroxetine), may contribute to the occurrence of arrhythmias, including pirouetnoy tachycardia. When interacting with fluvoxamine, propranolol, pindolol may increase the content of thioridazine in the blood plasma, which increases the risk of arrhythmias.
special instructions
During the period of treatment it is necessary to control the morphological composition of the blood; refrain from using ethanol. Influence on the ability to drive vehicles and control mechanisms The drug weakens motor coordination and reduces the speed of psychomotor reactions, especially at the beginning of treatment, therefore during the period of drug treatment one should refrain from controlling vehicles and servicing moving mechanisms.