Meldonium
Meldonium. Structural analogue of gamma-butyrobetaine and an inhibitor of gamma-butyrobetaine hydroxylase, the last enzyme of carnitine… IV half-life 6.5 h.
Structural analogue of gamma-butyrobetaine and an inhibitor of gamma-butyrobetaine hydroxylase, the last enzyme of carnitine biosynthesis. Lowering carnitine limits long-chain fatty-acid transport into mitochondria and shifts myocardial and neural metabolism toward glucose oxidation, which needs less oxygen per ATP — the basis of its anti-ischaemic use and of the cognitive/anti-fatigue claims made for it in the territories where it is marketed. Banned by WADA since 2016.
PubChem CID 123868 (C6H14N2O2). PK: Peng 2010 (PMID:20116348), healthy Chinese volunteers — verbatim "After single intravenously administration of 250, 500 and 1000 mg mildronate, the elimination half-life (t(1/2)) were (5.56+/-1.55), (6.46+/-1.07) and (6.55+/-1.17) h, respectively." The 500 mg arm value is stored as the mid-strength dose; the three arms are close enough that the choice barely matters, but it is a STATED arm rather than a computed average. Multiple-dose IV 500 mg b.i.d. in the same paper gives a longer t½ (15.34+/-3.14 h) with explicit accumulation — that is a different regimen, not a better estimate of the single-dose parameter, so it is not stored. PO IS A DECLARED DANGLING ROUTE: the oral capsule is the common form and the reason the route is listed at all, but no indexed abstract states an oral half-life or bioavailability for meldonium, so authoring PO would mean inventing one. A dose logged against PO renders no curve until that is sourced; logged in AUTHORING_GAPS.md. No volume is published; IV defaults. Indication reference PMID:16007237 ("Mildronate: an antiischemic drug for neurological indications").
Pharmacokinetics
- IV — t½ 6.5 h · F 100%
Sources: PMID:20116348, PMID:16007237