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Concept
Loprazolam
Summary
Loprazolam (triazulenone) marketed under many brand names is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It is licensed and marketed for the short-term treatment of moderately-severe insomnia.
It was patented in 1975 and came into medical use in 1983.
Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Loprazolam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or have difficulty falling asleep. Hypnotics should only be used on a short-term basis or in those with chronic insomnia on an occasional basis.
The dose of loprazolam for insomnia is usually 1 mg but can be increased to 2 mg if necessary. In the elderly a lower dose is recommended due to more pronounced effects and a significant impairment of standing up to 11 hours after dosing of 1 mg of loprazolam. The half-life is much more prolonged in the elderly than in younger patients. A half-life of 19.8 hours has been reported in elderly patients.
Patients and prescribing physicians should, however, bear in mind that higher doses of loprazolam may impair long-term memory functions.
Side effects of loprazolam are generally the same as for other benzodiazepines such as diazepam. The most significant difference in side effects of loprazolam and diazepam is it is less prone to day time sedation as the half-life of loprazolam is considered to be intermediate whereas diazepam has a very long half-life. The side effects of loprazolam are the following:
drowsiness
paradoxical increase in aggression
lightheadedness
confusion
muscle weakness
ataxia (particularly in the elderly)
amnesia
headache
vertigo
hypotension
salivation changes
gastro-intestinal disturbances
visual disturbances
dysarthria
tremor
changes in libido
incontinence
urinary retention
blood disorders and jaundice
skin reactions
dependence and withdrawal reactions
Residual 'hangover' effects after nighttime administration of loprazolam such as sleepiness, impaired psychomotor and cognitive functions may persist into the next day which may increase risks of falls and hip fractures.
Official source
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