Loprazolam
- Atc Codes:N05CD11
- CAS Codes:61197-73-7
- PHARMGKB ID:61197-73-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
Brand Names
Europe
Belgium: Dormonoct; France: Havlane; Netherlands: Dormonoct; Portugal: Dormonoct; Spain: Somnovit; UK: Loprazolam.
Latin America
Argentina: Dormonoct.
Asia
Japan: Havlane.
Drug combinations
Chemistry
Loprazolam: C~23~H~21~ClN~6~O~3~. Mw: 464.90. (Z)-6-(o-Chlorophenyl)-2,4-dihydro-2-[(4-methyl-1-piperazinyl)methylene]-8-nitro-1H-imidazol[1,2-a][1,4]benzodiazepin-1-one. CAS-61197-73-7.
Pharmacologic Category
Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05CD11).
Mechanism of action
Benzodiazepines have widespread action as a result of their enhancing release of gamma-aminobutyric acid (GABA). Effective as anti-convulsants, muscle relaxants, anti-anxiety agents, pre-medications and sedative hypnotics.
Therapeutic use
Indicated for short-term treatment of insomnia including difficulty in falling asleep and/or frequent nocturnal awakenings.
Pregnancy and lactiation implications
Crosses placenta. Associated with fetal malformations. Hypotonia, hypothermia, withdrawal symptoms, respiratory and feeding difficulties reported in infant following maternal use. Women should avoid pregnancy while taking this medication and should not breast-feed.
Unlabeled use
Contraindications
Sensitivity to benzodiazepines, acute pulmonary insufficiency, severe respiratory insufficiency, myasthenia gravis, phobic or obsessional states and sleep apnea syndrome. Monotherapy in depression or anxiety associated with depression and chronic psychosis and alcohol intake.
Warnings and precautions
Disinhibiting effects may be manifested in various ways. Suicide may be precipitated in patients who are depressed and who exhibit aggressive behavior towards self and others. Extreme caution should therefore be used in prescribing benzodiazepines in personality disorders. In general, dependence potential of benzodiazepines is low but increases when high doses are attained, especially when given over long periods and particularly in history of alcoholism or drug abuse. However, withdrawal symptoms occur even with normal therapeutic doses given for short periods of time. Withdrawal from benzodiazepines may be associated with physiological and psychological symptoms of withdrawal including depression, anxiety, tension, restlessness, confusion, irritability and headaches. Rebound insomnia may also occur. May be accompanied by other reactions such as changes in mood, anxiety, sleep disturbances and restlessness. Use with caution in chronic pulmonary insufficiency, cerebrovascular disease and chronic renal or hepatic impairment. Benzodiazepines should be used to treat insomnia only when it is severe, disabling or subjecting individual to extreme distress.