Triazolam
Triazolam. Short-acting triazolobenzodiazepine — positive allosteric modulator at GABA-A BZD site (α1-preferring). Used for short-term insomnia… Oral half-life 2.6 h.
Short-acting triazolobenzodiazepine — positive allosteric modulator at GABA-A BZD site (α1-preferring). Used for short-term insomnia and procedural sedation. Extensively metabolized by CYP3A4 — sensitive to CYP3A inhibitors (azoles, ritonavir, clarithromycin) which can extend the t½ markedly. Rapid onset, short duration.
PK: the half-life 2.6 h is verbatim and stands, and so does the effect-compartment value, whose stored note quotes its paper accurately and converts correctly from "the mean plasma effect site equilibration half-life was 9.4 minutes" — the one properly-sourced effect model in its group, with documented hysteresis, "Peak plasma triazolam concentrations preceded maximum pharmacodynamic effects". TWO COLLISIONS ARE REMOVED. V 77 L was the study subjects "mean body weight of 77 kg". F 0.44 was the endpoint of "aged 20-44 years" — and the cited study, being oral-only, could not have measured an absolute bioavailability at all. The VALUE 0.44 is nonetheless correct and is re-cited to Kroboth 1995 (PMID:7593708), a three-way crossover with a real intravenous arm: "the observed mean absolute availability was 44% (oral) and 53% (sublingual)". NO VOLUME IS STORED, deliberately: every published triazolam volume is apparent, so pairing one with this measured bioavailability would divide the dose by F twice. ka 1.5 dropped; the only genuine absorption figures are time-of-day dependent, 13.3 minutes in the morning against 21.9 in the evening.
Pharmacokinetics
- Oral — t½ 2.6 h · F 44%
Sources: PMID:9536021, PMID:7593708, PMID:3950055, PMID:8830062