Pyridoxamine

vitamin · nervous · renal · endocrine · Oral

Pyridoxamine, a vitamin. The aminomethyl vitamer of vitamin B6, converted in vivo to the active cofactor pyridoxal-5-phosphate with only minimal conversion to…

The aminomethyl vitamer of vitamin B6, converted in vivo to the active cofactor pyridoxal-5-phosphate with only minimal conversion to pyridoxine — which is the stated rationale for preferring it, since pyridoxine is the vitamer whose high-dose neurotoxicity limits B6 therapy. Independently of the vitamer role it is an advanced-glycation-endproduct inhibitor: PMID:22034637 verbatim, "Pyridoxamine dihydrochloride (Pyridorin, NephroGenex) inhibits formation of advanced glycation end products and scavenges reactive oxygen species and toxic carbonyls, but whether these actions translate into renoprotective effects is unknown." PMID:34229268 verbatim adds the framing: "While PN toxicity is known to complicate several treatments, PM has shown promise in relation to the treatment of metabolic and age-related diseases by blocking oxidative degradation and scavenging toxic dicarbonyl compounds and reactive oxygen species." DISTINCT FROM `pyridoxine` and `p5p`, the two B6 vitamers already in this catalog.

PubChem free base CID 1052 (C8H12N2O2, 168.19); the dihydrochloride is CID 10664 (C8H14Cl2N2O2, 241.11). Both re-queried 2026-09-26. THE SALT/BASE SPLIT IS UNRESOLVED AND MATTERS: every clinical dose below is of the dihydrochloride, and 168.19/241.11 = 0.6976 would be the dose_moiety_fraction if a record ever needed one — it is NOT set here, because the record authors no curve for it to correct and because PMID:34229268 writes "200 mg PM" without saying whether that is salt or base. HUMAN DATA, verbatim (PMID:34229268, 5 healthy volunteers, oral, NCT02954588, pyridoxamine the subject): "After a single oral dose of 200 mg PM, plasma PM increased in the first 3 h to a maximum of 2324 +/- 266 nmol/L." Note Tmax is a WINDOW ("in the first 3 h"), not a point value, and is not stored as one. METABOLITE FIGURES FROM THE SAME ABSTRACT BELONG TO OTHER ANALYTES AND ARE NOT THIS RECORD'S PK: "PLP increased to a maximum of 2787 +/- 329 nmol/L and reached a plateau" and "a small increase of PN to a maximum of 13.5 +/- 2.1 nmol/L". AN ARITHMETIC THAT IS DELIBERATELY NOT STORED, written out so nobody re-derives it silently: 200 mg / 168.19 g/mol = 1.18913 mmol = 1,189,130 nmol; / 2324 nmol/L = 511.7 L. It is not authored because the numerator may be salt rather than base, because an endogenous baseline was not subtracted, because conversion to PLP is saturable and first-pass, and because the division ignores elimination during absorption — so it is a ceiling, not a volume. DOSES: 200 mg single oral and "a three daily dose of 67 mg PM" (PMID:34229268, route explicit); and as Pyridorin (PMID:22034637, 317 patients, 52 weeks) "Pyridorin, 150 mg twice daily; or Pyridorin, 300 mg twice daily" — that trial abstract never writes "oral", so the route for the Pyridorin arms is inferred. typical is set to 200 mg, the one dose whose route the literature states in words. NO AGE-INHIBITION CONSTANT IS STORED: `pyridoxamine AND dicarbonyl AND methylglyoxal AND IC50` returns 0 hits, and PMID:9038143 names pyridoxamine only qualitatively in a paper whose subject is aminoguanidine and a kinetic method. WRONG-VITAMER TRAPS: PMID:21079545 is doxylamine-PYRIDOXINE (Diclectin) and PMID:4056565 measures pyridoxal-phosphate clearance — neither is this molecule.

Sources: PMID:34229268, PMID:22034637, PMID:25532068