Mental diseases with physical and psychomotor agitation, paranoid syndromes (schizophrenia). As a supportive medicine in some of the accompanying symptoms of epilepsy, mental retardation, depressed with anxiety. In small doses in anxiety syndromes (in a single evening dose in sleep disorders). Intensification of analgesia. Preparation and deepening of general anesthesia.
Composition:
1 ampoule of 1 ml contains 25 mg of levopromazine.
Action:
Poor neuroleptic drug from the group of phenothiazine. Levomepromazine is an analogue of chlorpromazine with a stronger than chlorpromazine inhibitory effect on psychomotor functions. By acting on dopaminergic receptors in the thalamus, hypothalamus, reticular and limbic systems, levomepromazine results in the suppression of sensory stimuli, reduced motor activity and strong sedation; in addition, it also has antagonistic effects on other neurotransmitter systems (noradrenergic, serotoninergic, histaminergic, cholinergic). As a result, it has antiemetic, antihistamine, anti-adrenal and anticholinergic effects. The extrapyramidal side effects are weaker than after strong neuroleptics. The drug is a potent α-adrenergic antagonist, but shows weak anticholinergic activity. Levomepromazine increases the pain threshold (analgesic effectiveness is similar to morphine) and causes an amnesic effect. Due to the ability to enhance the effect of analgesics, the drug can be used as an auxiliary treatment in severe acute and chronic pain. The maximum analgesic effect occurs within 20-40 minutes after intramuscular administration and lasts for approx. 4 hours.max after intramuscular administration, it is 1-3 hours. Levomepromazine is extensively metabolised to metabolites conjugated with sulphate and glucuronide, subsequently excreted by the kidneys. A small fraction of the dose (1%) is excreted in the urine and faeces unchanged. T0,5 elimination is 15-30 h.
Contraindications:
Hypersensitivity to phenothiazines. Administration with hypotensive drugs. Overdose of depressants at o.u.n. (alcohol, general anesthesia, sleeping pills). Glaucoma with a narrow angle of perception. Urinary retention. Parkinson's disease. Multiple sclerosis. Myasthenia, hemiplegia. Severe cardiomyopathy (failure of circulation). Severe kidney or liver problems. Clinically significant hypotonia. Haematopoietic system disease. Porphyria. Breast-feeding. Children under 12 years.
Precautions:
Use of the drug should be discontinued immediately if any hypersensitivity reaction occurs. The simultaneous use of the drug with depressants with o.n.n.n., MAO inhibitors and anticholinergic drugs requires great caution. Due to the risk of accumulation and toxicity, use in patients with impaired kidneys and / or liver requires special attention. Elderly people (especially with dementia) are more susceptible to orthostatic hypotension and more sensitive to the anticholinergic and sedative effects of phenothiazines; in addition, they show an excessive tendency to extrapyramidal symptoms and therefore in such cases it is particularly important that the treatment start with small initial doses and gradually increase them. After the first dose, the patient should lie for about 1/2 hour to avoid orthostatic hypotension. If you feel dizzy after taking the medicine, it is recommended to lie down in bed after each dose. In patients with a history of cardiovascular disease, especially in elderly patients and patients with congestive heart failure, conduction disorders, arrhythmias, long QT syndrome or circulatory disorders, caution is advised. Before starting treatment with ECG, an ECG should be performed to exclude any possible heart disease that could be a contraindication for treatment. If hyperthermia occurs during antipsychotic treatment, the possibility of a neuroleptic malignant syndrome (NMS) should always be excluded.Due to the risk of NMS, treatment with the product should be discontinued if elevated creatinine phosphokinase (CPK), myoglobinuria (rhabdomyolysis) and acute renal failure occur, and also when there is a high fever of unclear origin during treatment, even in the absence of overt clinical symptoms of NMS . If the patient's condition still requires antipsychotic treatment after NMS has resolved, the drug should be selected carefully. The tolerance to the sedative effects of phenothiazines and cross-tolerance between different antipsychotics has been observed. Levomepromazine reduces the seizure threshold and causes epileptiform changes in the EEG record - in patients with epilepsy, careful clinical control and EEG control are required during the dose escalation period. During chronic treatment, regular blood count monitoring is recommended (rare cases of agranulocytosis and leukopenia have been reported). Before and during the treatment, regular monitoring of the following parameters is recommended: blood pressure (especially in patients with circulatory disorders and patients prone to hypotension); liver function (especially in patients with existing liver dysfunction); blood count with smear (in the case of fever, sore throat or suspicion of leukopenia or agranulocytosis, at the beginning of treatment and during long-term use of the drug), ECG (in patients with cardiovascular disease and in elderly patients).
Pregnancy and lactation:
The medicine should not be used during pregnancy unless careful risk-benefit assessment is carried out. The use of the drug during breastfeeding is contraindicated.
Side effects:
Common: orthostatic hypotension, disorientation, confusion, visual hallucinations, speechlessness, epileptic seizures, elevated intracranial pressure, recurrence of psychotic symptoms, catatonia, deposits in the lens and cornea, retinitis dye, dry mouth, abdominal discomfort, nausea, vomiting constipation. Uncommon: tachycardia, MAS syndromes, QT prolongation (arrhythmia typetorsade de pointes), change in the color of the urine, difficulty passing urine. Rare: pancytopenia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, extrapyramidal symptoms (dyskinesia, dystonia, parkinsonism, opistotonus, exaggerated reflexes), photosensitivity, erythema, urticaria, hyperpigmentation, exfoliative dermatitis, galactorrhea, menstrual disorders, weight loss, jaundice, cholestasis, laryngeal edema, peripheral edema, anaphylactoid reactions, asthma. Very rare: pituitary adenoma (more research is needed to establish causation with treatment), abnormal uterine contractions. In addition, you may experience: very high fever, vitamin deficiency. After the sudden discontinuation of large or long-term doses of the drug, the following symptoms may occur: nausea, vomiting, headache, tremors, sweating, tachycardia, insomnia, restlessness.
Dosage:
Parenteral administration is used when it is impossible to use the medicine orally. The daily dose is usually 75-100 mg (in 2-3 divided doses) when the patient is lying in bed and monitoring blood pressure and heart rate. When used intramuscularly, the drug should be administered in a deep intramuscular injection. Intravenous administration may only be used as a diluted solution in a slow infusion (50-100 mg of the preparation in 250 ml of saline or in a Glucose solution). If possible, the injection site should be changed as the preparation may cause local irritation and tissue damage.