Fluconazole
Fluconazole. Triazole antifungal — inhibits Candida / Cryptococcus 14α-demethylase (CYP51) blocking ergosterol synthesis. In humans inhibits… Oral half-life 37 h.
Triazole antifungal — inhibits Candida / Cryptococcus 14α-demethylase (CYP51) blocking ergosterol synthesis. In humans inhibits CYP2C9, CYP2C19, and CYP3A4 — moderate DDI perpetrator at doses ≥ 200 mg/d (warfarin INR rises predictably). Renally cleared; long t½ allows once-daily dosing.
PK: the stored 34 h was a midpoint of the cited paper's printed range, "The half-life of fluconazole was 31 to 37 hours after oral and intravenous administration" (PMID:2379224) — a number that appears nowhere. Replaced by Berl 1995 (PMID:7579091), whose normal-renal-function group (n=10, CLcr 107 mL/min) gives a verbatim scalar: "the Day 10 mean half-lives were inversely related to mean CLcr (36.7 h in Group 1, 84.5 h in Group 2, and 101.9 h in Group 3)". V 35 L is Brammer 1991 (PMID:1680653) verbatim "apparent volume of distribution were 0.23 ml/min/kg and 0.5 liter/kg" scaled to 70 kg; no primary states any litre figure, and the previously stored 50 L traces to a REVIEW's 0.7 L/kg. F is pinned to 1 because that volume is apparent; the measured value supports it — absorption "approximated unity" (PMID:7486928) — and the stored 0.9 was in no paper. ka dropped: the only human value is 0.93 /h in HIV-positive patients (PMID:11829202), not the stored 2.5. CAVEAT: half-life is renal-function dependent, rising to 84.5 h and 101.9 h in the impaired groups of the same paper. PK: THE STORED VOLUME WAS THE SOLVER DEFAULT WEARING A CITATION. 35 L is exactly 0.5 L/kg at the seventy-kilogram reference — the value resolvePk substitutes when the field is ABSENT — and this record cited abstract states no volume at all. Removing it is NUMERICALLY A NO-OP, since the resolver now supplies the identical number; what changes is that the record stops asserting a measurement it does not have, and the defaulted-volume lint begins counting it as the open gap it is. This is the batch-11 finding running backwards: there a deletion silently became a default, here a default had silently become a datum. INTERACTIONS: ELEVEN OF THE TWELVE AFFINITIES ARE THE PUBLISHED EXPOSURE RISE INVERTED THROUGH ONE ASSUMED CONCENTRATION OF 30 µM, and most of the notes already printed that arithmetic in plain sight. The calibration is well anchored: 30 µM is within thirty percent of this record own modelled mean plasma level, so the solver reproduces each cited ratio near typical exposure. Every edge cites a clinical interaction study and none cites an in-vitro constant, which is why the basis had to be declared rather than the numbers trusted as affinities. ONE EDGE DOES NOT RECONSTRUCT AND IS LEFT ALONE: the warfarin entry implies a 4.75-fold rise against a cited figure of about 3.3, so it asserts a stronger interaction than its own source — the opposite direction from the attenuated edges found elsewhere, which is why hand-adjustment is a guess rather than a finding.
Pharmacokinetics
- Oral — t½ 36.7 h · F 100%
- IV — t½ 36.7 h · F 100%
Related compounds
- Warfarin — major
- Tacrolimus — major
- Cyclosporine — major
- Phenytoin — warn
- Losartan — warn
- Ibuprofen — warn
- Celecoxib — warn
- Fluvastatin — warn
Sources: PMID:1633070, PMID:9357393, PMID:16723553, PMID:39730940, PMID:10952477, PMID:11932962