Lorazepam - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Anxiolytics

Included in the formulation

Lorafen

pills inwards

Tarkhominsky pharmaceutical factory "Polfa", A.O. Poland

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

N.05.B.A.06 Lorazepam

N.05.B.A Benzodiazepine derivatives

Pharmacodynamics:

Benzodiazepine derivative of medium duration of action; causes depression of the central nervous system from mild sedation to coma depending on the dose, agonist of benzodiazepine receptors, promotes the enhancement of the effects of γ-aminobutyric acid (the main inhibitory neurotransmitter of the central nervous system) by stronger binding to type A receptors.

Pharmacokinetics:

Absorption after ingestion and intramuscular injection is rapid and complete. Bioavailability is 90%. The connection with plasma proteins is 85%. It can pass through the placenta, the blood-brain barrier, into breast milk. T_Cmax after sublingual administration - 1 h, after intramuscular injection - 1-1.5 h. C_max after taking 2 mg - 20 ng / ml (range of therapeutic concentration of 15-25 ng / ml). C_ss in plasma is usually achieved within 2-3 days. Biotransformation in the liver by conjugation with glucuronic acid. Half-life- 10-20 hours (average duration of action), its conjugate with glucuronic acid - 18 hours. Elimination by the kidneys (up to 88%, of which 75% in the form of glucuronide).Accumulation with a reappointment is minimal, excretion after cessation of treatment is rapid. After withdrawal, the concentration in the plasma is reduced to subclinical within 24 hours. It is not removed during hemodialysis. In elderly patients the pharmacokinetics of lorazepam does not change.

Indications:

Anxiety (including associated with depression), sleep disorders caused by anxiety or a short-term stressful situation, neuroses and neurosis-like conditions, panic disorders; endogenous psychoses: manic states, catatonic states, anxiety and excitation in schizophrenia; acute alcohol delirium; premedication in anesthesiology; epilepsy (as part of combination therapy), epileptic status; symptomatic convulsive conditions; psychosomatic disorders and headaches.

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F21 Chrysotile disorder

V.F20-F29.F22 Chronic delusional disorders

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F40-F48.F40 Phobic anxiety disorders

V.F40-F48.F41 Other anxiety disorders

V.F40-F48.F41.2 Mixed anxiety and depressive disorder

V.F40-F48.F48.0 Neurasthenia

VI.G40-G47.G40 Epilepsy

VI.G40-G47.G41 Epileptic status

XVIII.R25-R29.R25.2 Cramp and spasm

XVIII.R50-R69.R51 Headache

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified

Contraindications:

Hypersensitivity to lorazepam or any other benzodiazepine, or component of the dosage form.

Closed-angle glaucoma (acute attack or predisposition).

Acute poisoning with narcotic analgesics, sleeping pills and psychoactive drugs.

Acute respiratory failure.

The phenomenon of addiction in the anamnesis (drugs, alcohol, except for the treatment of alcohol withdrawal syndrome), nighttime apnea syndrome, pregnancy, breast-feeding.

Carefully:

Coma, shock, myasthenia gravis (severe form), acute alcohol poisoning (with impaired vital functions), severe chronic obstructive pulmonary disease (progression of respiratory failure), severe depression (suicidal tendencies may manifest).

Pregnancy and lactation:In pregnancy, especially in the first trimester, apply only on strict indications. Lorazepam and / or its metabolites can be excreted in breast milk.It should be borne in mind that in newborns, benzodiazepines are metabolized more slowly than in adults, so it is possible to accumulate the active substance and / or its metabolites in the child's body.

Category of recommendations FDA - D.

Dosing and Administration:

Adults and adolescents with oral administration - 0.5-4 mg 1-3 times a day. With intramuscular or intravenous administration, a single dose is 50 μg / kg, the frequency of administration is determined depending on the indications and the clinical situation.

Maximum doses: if administered orally, the daily dose is 10 mg; at intramuscular or intravenous administration of a single dose of 4 mg.

Side effects:

Hematological: anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia.

From the cardiovascular system: tachycardia / palpitations, hypotension, bradycardia, cardiac arrest (with parenteral use, especially in the elderly, seriously ill, including chronic obstructive pulmonary disease, unstable hemodynamics, or exceeding the rate of intravenous administration).

From the digestive tract: pain or cramps in the abdomen, constipation, diarrhea, dry mouth or increased thirst, nausea or vomiting, heartburn, decreased appetite, bulimia.

From the respiratory system: increased bronchial secretion or increased salivation, apnea (with parenteral use, especially in the elderly, seriously ill, including chronic obstructive pulmonary disease, with unstable hemodynamics or exceeding the speed of intravenous administration, a dose reduction is recommended), respiratory depression (3% in children).

Increases the risk of aspiration in newborns and young children, elderly and recumbent patients, patients with chronic respiratory diseases.

From the urinary system: urinary disorders - urinary incontinence or retention, impaired renal function.

From the nervous system: anxiety, confusion (especially in the elderly and with brain damage), depression, cognitive impairment, including mania, depersonalization or disorientation, behavioral disorders, including bizarre behavior or decreased deterrence, extrapyramidal and dystonic disorders, paradoxical reactions including agitation, aggressive behavior, hallucinations, anger or hostility, insomnia, unusual arousal, irritability, nervousness (require drug withdrawal),convulsions, ataxia (especially in children and weakened patients), dizziness (requires treatment only if prolonged or worrisome patient), drowsiness, including daytime use as a sleeping pill (especially in elderly and weakened patients, dose-dependent and more pronounced with initial therapy and may decrease with its continuation), slurred speech, changes in libido, euphoria, headache, tremor, unusual weakness or fatigue, memory loss, fatigue, catalepsy.

Overdose:

Treatment is symptomatic.

Interaction:

A solution of lorazepam for injection is incompatible with a solution of buprenorphine for injection.

Scintigraphy using sodium iodide 123I and sodium iodide 131I - benzodiazepines can reduce the accumulation of the radioisotope in the thyroid gland.

With the simultaneous use, the effectiveness of oral contraceptives decreases.

With simultaneous use, the effect of depolarizing muscle relaxants is enhanced.

At simultaneous application with nicotine the metabolism of lorazepam increases and its activity decreases.

With the simultaneous use of probenecid can disrupt the binding of lorazepam with glucuronic acid, which leads to an increase in its concentration in the blood plasma,and by increasing the therapeutic effect, it is possible to develop an excessive sedative effect.

Special instructions:

Effective with epileptic status (exceeds phenytoin, diazepam), depression (in combination with tranquilizers), for premedication, in anxious states (comparable to buspirone, zolpidem, inferior to hydroxyzine), panic disorder, insomnia (surpasses diazepam, comparable with midazolam, nitrazepam), epilepsy (in combination with other antiepileptic drugs), convulsions against the background of alcohol abstinence; endogenous psychoses accompanied by excitation, with vomiting caused by chemotherapy (potentiates the action of ondansetron, metoclopramide, glucocorticoids), alcoholic delirium (in combination with chlorpromazine, haloperidol).

Preparation of dosage forms and application features

Concentrated solution for oral administration (5 mg / ml): the dose is collected by measuring pipette supplied with the drug. Each dose is carefully dissolved in a liquid or mushy food product (water, carbonated water, apple juice, pudding) immediately after the fence.The resulting mixture should be used immediately after preparation: it is not subject to storage.

Solution for injection: immediately before intravenous injection diluted with an equal volume of sterile water for injection, 0.9% solution of sodium chloride or 5% dextrose. Do not use when changing color or precipitation.

Immediately after dilution, it is possible to inject directly into the vein or tube of the infusion system.

Instructions

Lorazepam (Lorazepamum)