Metolazone
Metolazone. Thiazide-like diuretic — same NCC blockade as HCTZ but works synergistically with loop diuretics in diuretic-resistant heart failure.… Oral half-life 14 h.
Thiazide-like diuretic — same NCC blockade as HCTZ but works synergistically with loop diuretics in diuretic-resistant heart failure. Powerful natriuresis when sequentially blocking distal tubule downstream of loop-treated proximal segments.
PK PROVENANCE, moved here from source_label when that field was shortened to a citation that names the label revision: Zaroxolyn (metolazone) label — F ~65%, t half ~14 h. Label-grade: the cited study reports only dose-proportionality and a fed/fasted tmax ratio, and dosed 0.5/1/2 mg tablets — the rapid-acting Mykrox product, NOT interchangeable with the Zaroxolyn 2.5-20 mg this record doses. PK: A COMPLETE CITATION FAILURE PLUS A FORMULATION MISMATCH, AND THE MISMATCH IS PROVABLE FROM THE DOSE BLOCK. The cited study states not one of the four stored values — only that "The AUC and Cmax showed dose proportionality", that "The tmax of metolazone was increased by approximately 100% in the fed condition", and a null sex comparison — and it was the record ONLY reference. It also dosed 0.5, 1 and 2 mg tablets, the rapid-acting low-dose product, while this record is aliased Zaroxolyn and doses 2.5 to 20 mg; the two formulations differ about twofold and are explicitly not interchangeable. NO VERBATIM REPLACEMENT EXISTS: the canonical primary pharmacokinetic paper for this drug HAS NO ABSTRACT IN PUBMED AT ALL, only a title, and everything else indexed is rat, urinary-excretion pharmacodynamics or assay methodology. The four numbers are therefore kept and re-provenanced honestly to the label rather than left under a citation that cannot support them.
Pharmacokinetics
- Oral — t½ 14 h · F 65% · Vd 113 L
Sources: PMID:29145890