Fluvastatin
Fluvastatin. First entirely synthetic statin (1994). CYP2C9 metabolism — different interaction profile than CYP3A4-metabolised statins. Lower… Oral half-life 1.2 h.
First entirely synthetic statin (1994). CYP2C9 metabolism — different interaction profile than CYP3A4-metabolised statins. Lower potency than newer statins — clinical use declining.
PK: TOTAL PROVENANCE FAILURE AND NOT ONE NUMBER SHOULD MOVE — THIS IS THE CONTRACT WARNING CASE, LIVE. The cited review contains none of the four stored values; the absorption rate is a back-derivation that solves to a peak at 1.0002 h from a Tmax sitting in this record OWN references, "the time to reach C(max) (t(max)) ... were ... 60.0 +/-30.0 minutes"; the bioavailability is exactly the midpoint of a verbatim "the estimated bioavailability from the 2- and 10-mg doses was only 19 to 29%" and is also the label figure, so midpoint arithmetic and label copying cannot be distinguished; and the volume is a per-kilogram computation absent from every abstract fetched. YET THE RECORD REPRODUCES OBSERVED 40 MG EXPOSURE TO WITHIN 1.0 TO 1.3x. The reason is saturable first-pass metabolism: that bioavailability was measured at 2 to 10 mg, both sources report over-proportional exposure at 40 to 80 mg, and a low clearance is cancelling a low bioavailability. The verbatim clearance is "0.97 L/hour/kg" against the model 14.15 L/h — 4.8x apart — SO CORRECTING EITHER IN ISOLATION WOULD BREAK A CURRENTLY ACCURATE RECORD. Class 6 is definitively acquitted: a human intravenous arm exists, "an absolute bioavailability study using doses of 2 mg intravenously or 10 mg orally". MY EXTENDED-RELEASE PRIOR IS REFUTED — the parameters are immediate-release shaped and nowhere near the extended-release peak — but the DOSE BLOCK mixes the two, its maximum being an extended-release-only strength.
Pharmacokinetics
- Oral — t½ 1.2 h · F 24% · ka 1.59 h⁻¹ · Vd 24.5 L
Sources: PMID:11368292, PMID:11509920, PMID:1640002