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Pharmacological action Lorazepam 1 mg
Lorazepam Anxiolytic drug (tranquilizer), a derivative of benzodiazepine. Has anxiolytic, sedative, hypnotic, anticonvulsant, muscle relaxant central, antiemetic effect. The mechanism of the anxiolytic, sedative and hypnotic action is associated with increased inhibitory effect of GABA in the CNS. Anticonvulsant action, apparently in part due to increased presynaptic inhibition, suppressed the spread of epileptogenic activity, occurring in epileptogenic foci in the cortex, thalamus and limbic structures, but not removed the excited state of the hearth. Muscle relaxant effect is primarily associated with the suppression of spinal polysynaptic afferent pathways and, presumably, inhibition of monosynaptic afferent pathways, possibly also a direct inhibitory effect on motor nerves and muscle function.
Pharmacokinetics Lorazepam 1 mg
If ingestion bioavailability of 95-99%. Binding to plasma proteins – about 80%. Vd – 1.3 L / kg. Lorazepam is metabolized in the liver by conjugation to form inactive metabolites. T1 / 2 at 8-15 h. Write mainly by the kidneys.
Statement Lorazepam 1 mg
Anxiety (including related to depression), sleep disorders due to anxiety or transient stressful situation, neuroses and neurosis-like states, panic disorder, endogenous psychoses: mania, and catatonic states of anxiety and excitement of schizophrenia, acute delirium tremens; Premedication in anesthesia, epilepsy (in combination therapy), status epilepticus, symptomatic convulsive status, psychosomatic disorders and headaches.
Dosage regimen Lorazepam 1 mg
Adults and adolescents at intake – at 0.5-4 mg 1-3 times / day. In V / m or / in the introduction of a single dose of 50 mg / kg, the dose frequency is set depending on the evidence and the clinical situation.
The maximum dose when administered daily dose – 10 mg, with a / m or / in a single dose – 4 mg.
Side effect Lorazepam 1 mg
Central nervous system: rarely – dizziness, ataxia, fatigue, muscle weakness, and in some cases – the episodes of amnesia.
Part of the digestive system: rarely – dry mouth, dysphagia, nausea, diarrhea, constipation, appetite disorders, and in some cases – liver function abnormalities.
Allergic reactions: seldom – skin rash, itching.
From the laboratory parameters: changes in peripheral blood.
Local reactions: with / in the introduction can phlebitis or venous thrombosis.
Contraindications Lorazepam 1 mg
Myasthenia gravis, angle-closure glaucoma, acute intoxication with psychotropic drugs, acute alcohol intoxication, increased sensitivity to lorazepam.
Pregnancy and breastfeeding
During pregnancy, especially in the I trimester, apply only under strict indications. Lorazepam and / or its metabolites are excreted in breast milk. It should be borne in mind that newborns benzodiazepines metabolized more slowly than adults, so it is possible the accumulation of the active substance and / or its metabolites in the body of the child.
Cautions Lorazepam 1 mg
With extreme caution is used in closed-angle glaucoma is suspected, severe chronic obstructive pulmonary disease, in a coma, shock, epilepsy, renal dysfunction, hyperkinesis, hypoproteinemia, severe depression, organic brain disease, porphyria, psychosis with suspected sleep apnea. If abnormal liver function observed a minimal increase of T1 / 2 of lorazepam.
The development of adverse reactions are more likely at the beginning of treatment and in cases of exceeding the recommended doses.
With prolonged use of lorazepam may develop addiction and drug dependence.
In the case of lorazepam for sedation may require reducing the dose of fentanyl derivative used for induction of anesthesia, with the possible reduction of time before the mind with induction doses.
Effects on ability to drive and control mechanisms
Patients receiving lorazepam should refrain from activities in potentially hazardous activities that require attention and psychomotor speed of reaction.
Drug Interactions
When applied simultaneously with the means of providing a dampening effect on the CNS, with ethanol, etanolsoderzhaschih drugs increased inhibitory effect on the CNS. After simultaneous application of lorazepam and ethanol may develop agitation, aggression, pathological intoxication (the development of this condition does not depend on the amount received ethanol).
With simultaneous application of decreasing the effectiveness of oral contraceptives.
With simultaneous application of enhanced action of depolarizing relaxants.
When applied simultaneously with nicotine increases the metabolism of lorazepam, and decreases its activity.
With simultaneous use of probenecid may interfere with the binding of lorazepam with glucuronic acid, resulting in higher concentrations in blood plasma, and by enhancing the therapeutic effect may develop excessive sedation.
