Hydrocodone
Hydrocodone. Prodrug — CYP2D6 O-demethylates to hydromorphone, which is the more potent active metabolite. CYP2D6 poor metabolisers get reduced… Oral half-life 3.8 h.
Prodrug — CYP2D6 O-demethylates to hydromorphone, which is the more potent active metabolite. CYP2D6 poor metabolisers get reduced analgesia. µ-opioid receptor agonist (same family as morphine). Most commonly co-formulated with acetaminophen, whose 4 g/day ceiling sets the hard dose cap.
PK: ITS CITATION IS AN EXTENDED-RELEASE, ABUSE-DETERRENT FORMULATION STUDY PROPPING UP AN IMMEDIATE-RELEASE ROW, and it states none of the four stored values. A half-life is available verbatim from a human arm: "A mean peak serum drug concentration of 23.6 ng/ml and a terminal half-life of 3.8 h resulted from the human study". F 0.5 AND V 230 L ARE UNSOURCEABLE AND RETAINED ONLY BECAUSE THE DEFAULTS WOULD BE WORSE — there is no human intravenous hydrocodone arm anywhere, so an absolute bioavailability has never been measured and every candidate study reports a RELATIVE one; the record own reference concedes "relatively little is known about its pharmacokinetics". THE PRODRUG PREMISE IN OUR OWN PROSE IS REFUTED, and this is a defect in our text rather than in the data: a controlled crossover found that "EMs and PMs were equally responsive to oral hydrocodone, and quinidine had no consistent effect on their responses", concluding "only a small role of hydromorphone". Hydrocodone is an active mu agonist in its own right, so the stored pharmacokinetics and occupancy describe the RIGHT analyte.
Pharmacokinetics
- Oral — t½ 3.8 h · F 50% · Vd 230 L
Sources: PMID:25301538, PMID:17786418, PMID:1851921, PMID:856847, PMID:9103485