Dronabinol
Dronabinol. Synthetic Δ9-THC — same CB1/CB2 partial agonism. FDA-approved for chemotherapy-induced nausea + AIDS-related anorexia. Schedule III… Oral half-life 4 h.
Synthetic Δ9-THC — same CB1/CB2 partial agonism. FDA-approved for chemotherapy-induced nausea + AIDS-related anorexia. Schedule III for the synthetic; CB1-mediated dysphoria + tachycardia limit dose escalation.
PK: V 700 L is the label APPARENT volume of 10 L/kg, and pairing it with a bioavailability of 0.1 UNDER-PREDICTED PLASMA CONCENTRATION TENFOLD; it is dropped rather than re-paired, since no true volume exists. The half-life of 2.75 h was a SIMULATION OUTPUT in a four-subject subgroup on a different formulation, and is shorter than even the alpha phase of the true biphasic profile, whose distribution phase is about 4 h and terminal phase 25 to 36 h; the alpha value is stored with that caveat. F 0.1 was the lower endpoint of a label range and is replaced by a measured 6% against an intravenous reference, with the caveat that its vehicle was a cookie rather than a sesame-oil capsule. ANALYTE: the 11-hydroxy metabolite is present "in approximately equal concentrations in plasma", is more potent, and its ratio to parent is route-dependent, so a parent-only curve represents about half the active material after oral dosing. EFFECT IS DECOUPLED WITH DOCUMENTED HYSTERESIS: "The appearance of high lagged behind the increase in plasma concentrations", and oral effects occur "at much lower plasma concentrations" than by other routes. Absorption is lagged and erratic with a fourfold food effect, so ka 0.5 is dropped.
Pharmacokinetics
- Oral — t½ 4 h · F 6%
Sources: PMID:38054364, PMID:17641667, PMID:25311884, PMID:6250760