Treatment and prevention of nausea, vomiting and dizziness. Thieleerperazine effectively inhibits and prevents nausea and vomiting after surgery, cancer chemotherapy, radiotherapy or treatment with emetic drugs (opiates, ergot alkaloids, theophylline), cranial and brain injuries, intracranial hypertension, migraine and kinetoses, uremia and gastrointestinal disorders intestinal, liver and bile ducts. The preparation is used to treat vertigo in Meniere's disease and other labyrinth disorders, after shaking the brain, the syndrome after shaking the brain and cerebrovascular atherosclerosis. In the prevention and treatment of nausea and vomiting after chemotherapy, thiethylperazine is effective for chemotherapeutics with mild to moderate vomiting ( Fluorouracil, doxorubicin), while in the case of drugs with strong vomiting (cisplatin) is relatively ineffective.
Composition:
1 tabl powl. contains 6.5 mg of thiethylperazine in the form of dimalequat. The preparation contains lactose.
Action:
Antiemetic. A derivative of phenothiazine, a blocker of dopaminergic receptors. The antiemetic effect of the preparation is the result of the action on the emetic center in the reticular formation of the medulla and the chemoreceptor zone that causes the gag reflex in the IV cerebral ventricle. Blocking these structures causes the interruption of efferent signals that stimulate the effectors that are instruments of the emetic process. It is probably thiethylperazine that also inhibits the afferent impulses of the autonomic nervous system through the vagus nerve. The antiemetic action occurs 30 min after oral administration of the drug and lasts about 4 hours. The effect of thiethylperazine headache is based on the coordination in reticular formation, which cooperate in coordinating the balance of the body by agreeing the stimuli of the organ of balance in the inner ear and the locomotor system. The drug is well absorbed from the digestive tract. The maximum concentration is reached 2-4 h after oral administration. It has high lipophilicity and a high percentage of binding to plasma membranes and proteins (over 85%). It accumulates in organs with high blood flow and easily penetrates through the placenta. It can not be removed from the body by dialysis. It is metabolised mainly in the liver, only 3% of the dose is excreted unchanged by the kidneys. T0,5 is about 12 hours.
Contraindications:
Hypersensitivity to the active substance, phenothiazine derivatives or to any of the excipients. Severe CNS depression or disturbance of consciousness. Clinically significant hypotension. Children under 15 years due to the risk of unwanted extrapyramidal activities. Children and adolescents with symptoms or suspicion of Reye's syndrome due to similarity to the toxyl-dezine side effects and the ability to mask the symptoms of the disease.
Precautions:
Due to the additive antihypertensive effect of thiethylperazine, the drug should be used with caution in patients with anesthesia or concurrently using β-adrenergic blockers. The antihypertensive effect of the preparation is also dangerous in pregnant women with preeclampsia, because it can lead to a significant reduction in blood pressure. The drug should be used with caution in patients with a history of dyskinesia and in patients with moderate or severe hepatic impairment. In the case of a neuroleptic malignant syndrome, treatment should be stopped immediately. During therapy, there is a risk of extrapyramidal symptoms, the risk is increased in children and adolescents; if such symptoms occur, a dose reduction or discontinuation should be considered. In patients with bone marrow depression, use the medicine only if the potential benefits outweigh the risk. Elderly patients are advised to limit the duration of treatment. The preparation may mask symptoms of some diseases of the digestive system and o.u.n., and toxic effects of other drugs.The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
Avoid using the drug during pregnancy - the drug can only be used if the potential benefits to the mother outweigh the threat to the fetus. Use during breastfeeding is not recommended.
Side effects:
Uncommon: drowsiness, dizziness, headache, anxiety. Rarely: convulsions and extrapyramidal effects (torticollis, posterior tetanus, involuntary looking with rotation of the knobs, muscle stiffness and facial grimacing - these symptoms appear primarily in children and adolescents, and in elderly patients, after prolonged use of the drug may be delayed dyskinesia - involuntary movements), clouding of the lens and blurred vision (after long-term treatment), dry mouth and anorexia, gynecomastia (after long-term treatment), peripheral swelling of the limbs and face. Very rare: tachycardia, hypotension (primarily after parenteral administration), trigeminal neuralgia, congestive jaundice. Some of the phenothiazine-specific adverse reactions were not found with the use of thiethylperazine, but should be taken into account when prescribing the drug: changes in the blood picture (severe agranulocytosis, leukopenia, thrombocytopenia, aplastic anemia, pancytopenia, eosinophil leukocytosis), paralytic ileus, miosis, erythema, exfoliative dermatitis, T-wave ECG abnormalities and endocrine disorders (menstrual cycle disorders, altered libido, gynecomastia and weight gain).
Dosage:
Orally. Adults: the recommended dose is 1-3 tabl. daily taken individually. The duration of treatment depends on the dynamics of the disease, usually the preparation is given for 1 day, it can also be administered for several days or weeks.Special groups of patients. In elderly patients (75 years and above), a maximum of two months treatment is recommended due to the risk of delayed dyskinesia. In patients with renal or hepatic impairment, a dose reduction should be considered. Do not give the drug to children under 15 years of age (the dosage of thiethylperazine in children has not been established).
(C)
