Pharmacology - Ketazolam (Sedotime)

[Jatelka]

There's not as much info here as I'd like. Unfortunately Ketazolam is marketed mainly in Spain and Germany, and my language skills aren't up to the translations.

Here's what I've found: Please feel free to add more!

Ketazolam is 11-Chlor-2,8-dimethyl-12b-phenyl-8,12b-dihydro-4H [1,3] oxazino [3,2-d] [1,4] benzodiazepin-4,7 (6H) – dion
.
It’s formula is C20H17ClN2O3 and it’s molecular mass is 368.8.

Pharmacokinetics

Ketazolam is rapidly absorbed after oral administration, and it is rapidly metabolised to N-desmethyl ketazolam, with a smaller proportion being metabolised to diazepam. The elimination half-life of ketazolam is 6-25 hours, with the elimination half-life of the N-desmethyl metabolite being approximately 52 hours. Ketazolam is approximately 93% protein bound. It is excreted (mainly as glucuronides) by the kidney.

Indications

Ketazolam is indicated for the short-term treatment of anxiety, and also for the relief of muscle spasm associated with Stroke and spinal injury.

Dosage

Initial therapeutic dose (in anxiety) is 15-30mg at night. In muscle spasm doses up to 60mg (or sometimes higher) are used in divided doses.

Smaller doses are used in older patients, and in renal and hepatic insufficiency.

Interactions

Additive depressant effect with other CNS depressants. Higher plasma levels when taken with liver enzyme inhibitors, and reduced effects when taken with liver enzyme inducers. Ketazolam itself is also thought to act as a liver enzyme inducer, so may reduce the plasma levels of anticonvulsants, as well as other benzodiazepines.

Contraindications:

The usual (hypersensitivity to ketazolam or it’s exipients, severe respiratory disease, obstructive sleep apnoea, severe hepatic insufficiency, pregnancy and lactation)

Adverse Effects

Again, the usual: Anterograde amnesia, hangover effect, reduced motor coordination, physical tolerance/dependence and withdrawal after as little as 14 days continued use.

Overdose

Somnolence, ranging through to coma, respiratory depression and hypotension