Short-term and short-term: for the treatment of sleep disorders - difficulty in falling asleep, frequent awakenings, early morning awakening; in premedication, in preparation for troublesome diagnostic tests. Conditions of tension and anxiety associated with everyday problems are not an indication for the use of the drug.
Composition:
1 tabl contains 0.5 mg or 1 mg of lormetazepam.
Action:
Benzodiazepine derivative. It affects many structures o.u.n., above all the limbic system and hypothalamus, that is, the structures associated with the regulation of emotional activities. It intensifies the inhibitory action of GABAergic neurons within the cerebral cortex, hippocampus, cerebellum, thalamus and hypothalamus. The drug increases the affinity of the GABAergic receptor to gamma-aminobutyric acid (GABA), which is an endogenous inhibitory neurotransmitter. The product works hypnotically, has a calming and anxiolytic effect and weak anticonvulsant and skeletal muscle relaxants. After oral administration, it is well absorbed from the gastrointestinal tract. The maximum concentration in the blood occurs after about 1 hour. The constant concentration of the drug reaches after 3 days of use. Plasma protein binding is around 85%. It penetrates the barrier - blood - cerebrospinal fluid and through the placenta. T0,5 is 10-12 h. The drug is metabolised in the liver. It is excreted in the urine, 94% in unchanged form directly conjugated with glucuronic acid.
Contraindications:
Hypersensitivity to benzodiazepine derivatives or other components of the preparation. Severe respiratory failure, regardless of the cause. Severe hepatic failure. Night sleep apnea syndrome. Disturbances of consciousness. Myasthenia gravis. Glaucoma. acute porphyria. Alcohol poisoning or depressive drugs at o.u.n.
Precautions:
Before starting treatment, the cause of insomnia should be determined; persistence of insomnia or its recurrence after 7-14 days of treatment may indicate the existence of primary mental or physical disorders. Psychological and physical addiction may develop during treatment - particularly cautiously use in patients with an addiction to alcohol, drugs or other medicines in the past. Regular use can lead to the development of tolerance. After the end of treatment with the preparation, so-called insomnia from rebound (recurrence of more severe symptoms). Due to the risk of post-accidental obstruction, the patient should be provided with 7-8 hours of uninterrupted sleep after taking the drug. In the event of psychological and paradoxical reactions, the drug should be discontinued. Use in patients with severe hepatic impairment and in patients with psychosis is not recommended. Particularly cautiously use in elderly patients (over 65 years), in patients with symptoms of depression (suicidal risk). Caution should be maintained in patients with chronic respiratory failure, with renal failure and / or liver, with porphyria. The safety and efficacy of using the drug in children under 18 years has not been established. The drug contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the drug in the first trimester of pregnancy is allowed only in case of absolute necessity, and the use of safer counterparts is impossible. If it is necessary to administer in the 3rd trimester of pregnancy or during delivery, hypotension, hypothermia and respiratory failure may occur in the newborn. In children of mothers who take long-term benzodiazepines in the third trimester of pregnancy, addiction may develop, and a withdrawal syndrome may occur in the post-natal period. If it is necessary to administer the medicine during lactation, breast-feeding should be discontinued.
Side effects:
Common: drowsiness, slowness of reaction, pain and dizziness, confusion, confusion, ataxia.Rarely: dysarthria with speech blurred and abnormal pronunciation, memory disorders, libido disorders, blurred vision (blurred vision, double vision), nausea, stomach discomfort, dry mouth, urinary incontinence, muscle twitching, muscle weakness, lack of appetite, general weakness, menstrual disorders, paradoxical reactions (psychomotor anxiety, insomnia, agitation, aggression, muscle tremors, convulsions), allergic skin reactions (rash, pruritus, urticaria). Very rare: slight decrease in blood pressure, syncope, anaphylactic reactions, disturbances in blood morphology (leukopenia, agranulocytosis), slight elevation of aminotransferase, liver dysfunction with jaundice. Psychological and physical addiction may develop during treatment. Abrupt discontinuation of treatment may cause symptoms of withdrawal syndrome: headache, muscle pain, agitation, emotional tension, restlessness, confusion, confusion, irritability, insomnia; in severe cases: loss of sense of reality, personality disorders, hypersensitivity to touch, acoustic stimuli, light, tingling and limb numbness, hallucinations, convulsions. During therapy, pre-existing undiagnosed depression may appear.
Dosage:
Orally. Adults: sleep disorders: usually 0.5-1 mg 1/2 h before bedtime. In individual cases the dose can be increased up to a maximum of 2 mg per day. Premedication, preparation for troublesome diagnostic tests: usually 1 mg 1 hour before surgery or 2 mg 1/2 hour before bedtime on the day before the procedure. Elderly patients should use the lowest possible effective dose, do not exceed half the dose recommended in adult patients, usually administered 0.5 mg. A dose reduction may be necessary in patients with renal and / or renal failure. The drug is used as an ad hoc treatment, the duration of treatment should be kept to a minimum, usually it ranges from a few days to two weeks. In individual cases, treatment may take longer, maximum 4 weeks including the period of gradual withdrawal. In individual cases, this period may be prolonged, but the decision should be made after a thorough assessment of the patient's condition. The preparation should be taken 30 minutes before bedtime, with a small amount of water.
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