WARNINGMIXING OR WITHDRAWAL CAN BE DANGEROUS
Ordinary doses in combination with other depressants can fatally stop breathing. After prolonged dependency, stopping suddenly can also cause seizures or delirium; seek medical help.
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Loprazolam
Loprazolam is an imidazobenzodiazepine1 depressant used for the short-term treatment of moderately severe insomnia. It has sedative, sleep-promoting, anxiety-reducing, anticonvulsant, and muscle-relaxant properties,1 with subjective effects reported to resemble those of diazepam. It is short-acting2 and is used for difficulty falling asleep or maintaining sleep.3 Loprazolam is habit-forming.3 It was patented in 1975 and entered medical use in 1983.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Loprazolam positively modulates GABA-A receptors by binding at the benzodiazepine site on receptors containing an alpha subunit. It enhances GABA-mediated chloride channel opening by increasing the frequency of opening, allowing more chloride ions to enter neurons and strengthening inhibitory signaling.
Pharmacokinetics
After oral administration, combined serum concentrations of loprazolam and its active metabolite peak at about 3.5 hours. Taking it after a meal can delay this peak and reduce peak concentrations.4 Some studies suggest rapid brain penetration.5 In humans, approximately half of each dose is metabolized to a less potent active metabolite, while the other half is excreted unchanged. The metabolite has approximately the same elimination half-life as loprazolam. Elimination is substantially slower in elderly patients, in whom a half-life of 19.8 hours has been reported.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Harm Potential
Addiction & Dependence
Psychological
ModerateClassified as habit-forming with risk of psychological dependence developing with regular use. Abnormal, often severe drug-seeking behavior has been reported following abrupt withdrawal from long-term use.
Physical
HighPhysical dependence develops with regular use, though risk is low if used for less than 4 weeks or very occasionally. Between 30% and 90% of long-term users experience withdrawal symptoms upon discontinuation. Withdrawal symptoms tend to last between 3 weeks to 3 months, with 10-15% experiencing protracted withdrawal persisting for many months or occasionally several years.
Toxicity
Regular use can cause cognitive and psychomotor impairments including drowsiness, confusion, amnesia, ataxia, and impaired balance that may persist into the next day; higher doses may impair long-term memory functions.
Jaundice has been reported as a side effect, suggesting potential hepatic involvement with use.
Blood disorders have been reported as a side effect.
Psychosis Risk
Psychosis, confusion, and visual and auditory hallucinations with delusions can occur as major complications following abrupt or rapid withdrawal, especially from high doses. Paradoxical increase in aggression may also occur during use.
Seizure Risk
Epileptic seizures, which may be fatal, can occur as a major complication after abrupt or rapid withdrawal, especially from high doses. Gradual dose reduction greatly minimizes this risk.
History & Culture
Loprazolam was introduced in 1983.7
Legality
References
Citations
Article Status
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