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Alfacalcidol

Vitamin · Bone metabolism regulator

Also known as 1 α-OHD₃

VitaminBone metabolism regulator
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
none in our sources
PREGNANCY
not curated

Mechanism

Alfacalcidol is a prodrug that is rapidly hydroxylated in the liver to 1,25 (OH)₂D₃ or calcitriol. Calcitriol increases the synthesis of calcium channels and a carrier protein for Ca2+ (calcium binding protein or Calbindin) to promote intestinal absorption of calcium and phosphate. It binds to a cytoplasmic vitamin D receptor (VDR), translocates to the nucleus, and increases synthesis of specific mRNA to regulate protein synthesis.

Indications

Renal bone diseaseVitamin D dependent ricketsVitamin D resistant ricketsHypoparathyroidismOsteoporosisShort bowel syndrome (nutritional deficiencies)secondary hyperparathyroidism in patients with chronic kidney disease (CKD)

Dosing

Adult
1–2 µg/day orally
Pediatric
Children < 20 kg: 0.5 µg/day orally
Hepatic adjustment
No adjustment needed; metabolic activation in liver does not pose a problem even in severe liver disease.

Pharmacokinetics

Metabolism
Rapidly hydroxylated in the liver to 1,25 (OH)₂D₃ (calcitriol)
Excretion
Renal (as calcitriol)

Contraindications

  • Hypercalcaemia
  • Hypervitaminosis D
  • Increased sensitivity to vitamin D

Side effects

Common
WeaknessFatigueVomitingDiarrhoeaSluggishnessPolyuriaAlbuminuria
Serious
  • Hypercalcaemia
  • Ectopic Ca2+ deposition (in soft tissues, blood vessels, parenchymal organs)
  • Renal stones
  • Nephrocalcinosis
  • Hypertension
  • Growth retardation (in children)
  • Coma
  • hypercalcemia
  • hypercalciuria
  • hyperphosphatemia

Related guidelines

Other Vitamin drugs

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-10 · House clinical team