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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Ketazolam
Ketazolam is a long-acting depressant in the 1,4-benzodiazepine class. It belongs to the benzodiazepine class, which has anxiolytic, hypnotic-sedative, muscle-relaxant, and anticonvulsant actions.1 It is used to manage anxiety, insomnia, and spasticity. Its effectiveness for anxiety is similar to diazepam,2 while adverse effects, including sedation, appear to be less pronounced and tend to be milder when they occur.3 Ketazolam is habit-forming.4
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Ketazolam positively modulates GABA-A receptors by binding at their benzodiazepine site. This enhances GABA-mediated chloride conductance, making neurons less likely to fire. The binding site lies at the interface between alpha and gamma subunits, with alpha-1, alpha-2, alpha-3, and alpha-5 subunits able to participate.
Pharmacokinetics
Ketazolam undergoes sequential metabolic conversion beginning in the blood, and a half-life of 26-200 hours is reported. Its downstream products are eliminated mainly in urine, predominantly after glucuronide conjugation.5 Ketazolam is classified as a CYP3A4 substrate and inhibitor, with inhibitor strength unspecified, and as a P-glycoprotein substrate. Computational predictions suggest intestinal absorption, intestinal cell permeability, and blood-brain barrier penetration, as well as inhibition of CYP2C9 and CYP2C19. Predictions differ on whether it inhibits P-glycoprotein.
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
Ketazolam can be habit-forming.8
Physical
Chronic ketazolam use can cause physical dependence, with benzodiazepine withdrawal symptoms following discontinuation or dose reduction.
Toxicity
Ketazolam overdose can cause somnolence, confusion, coma, and reduced reflexes.9
History & Culture
In Canada, ketazolam was marketed as Loftran by SmithKline Beecham from December 31, 1992, to September 12, 1996. In South Africa, GlaxoSmithKline marketed it under the brand name Solatran.
Legality
International
Ketazolam is approved or marketed in some countries, but the approved jurisdictions are not specified.
By Country
References
Citations
Article Status
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