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Calcitriol

Active vitamin D3 metabolite (hormone) · Calcium/Vitamin D

Also known as 1,25-dihydroxycholecalciferol, Rocaltrol, Calcijex

START
Baseline calcium, phosphate, PTH, 25-OH vitamin D, creatinine. Ensure phosphate controlled before starting (Ca x P product <55 mg²/dL²).
TYPICAL MAX
2mcg/day. Monitor for hypercalcemia (constipation, confusion, polyuria, polydipsia).
STOP IF
Serum calcium >10.5 mg/dL (or 2.65 mmol/L), Ca x P product >55, signs of ectopic calcification, anaphylaxis.
WATCH
Calcium and phosphate monthly during titration, then every 3 months. PTH every 3 months (target per KDIGO). Adynamic bone disease risk if PTH suppressed too low. Concurrent phosphate binders often needed in CKD.
CDSCO approvedJan AushadhiATC A11CC04
Dose laddermg/d
0Start (mcg)0.001Step-up (mcg)0.002Max (mcg)
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo renal adjustment; indicated specifically for CKD patients90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
4hONSET4.5hPEAK6.5h3dDURATION
ONSET
4h · Calcium absorption 2-6 hours
PEAK
4.5h · Tmax 3-6 hours
6.5h · t½ 5-8 hours
DURATION
3d · Effects persist 3-5 days
EXCRETION
Fecal (~50%), renal metabolites
route + CYP
INTERACTIONS
8 major
SEVERE in our sources
PREGNANCY
Use only if clearly needed; monitor calcium closely. Crosses placenta; may affect fetal calcium metabolism.
FDA category + note
Top interactionssee all 12
  • BurosumabSevereDatabaseDDInter
  • CalcifediolSevereDatabaseDDInter
  • CholecalciferolSevereDatabaseDDInter
  • DihydrotachysterolSevereDatabaseDDInter
Available in India

15 branded formulations and 86 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

The biologically active form of vitamin D. Binds to vitamin D receptor (VDR) in intestine, bone, kidney, and parathyroid gland, increasing intestinal calcium and phosphate absorption, promoting bone mineralization, and suppressing PTH synthesis. Does not require renal 1α-hydroxylation (unlike cholecalciferol/ergocalciferol).

Indications

Secondary hyperparathyroidism in CKD (stages 3-5D)Hypocalcemia in hypoparathyroidismRickets / osteomalacia (vitamin D-dependent types, malabsorption)Psoriasis (topical)Osteoporosis (with calcium, in patients unable to activate vitamin D)

Dosing

Adult
CKD (dialysis): 0.25mcg PO daily initially, titrate by 0.25mcg q2-4 weeks to target PTH 150-300 pg/mL (KDOQI) or 2-9x ULN (KDIGO). Usual range 0.25-1mcg daily. Hypoparathyroidism: 0.25mcg BID, titrate to normocalcemia. Max 2mcg/day.
Pediatric
CKD: 0.01-0.05mcg/kg/day. Hypoparathyroidism: 0.04-0.08mcg/kg/day in 2 divided doses.
Renal adjustment
No adjustment (active form; no renal activation needed).
Hepatic adjustment
No adjustment.
Geriatric
Start at low end; increased hypercalcemia risk; monitor calcium and creatinine closely.
Max dose
2mcg/day (oral)

Pharmacokinetics

Onset
Intestinal calcium absorption increases within 2-6 hours; PTH suppression within days
Peak effect
Tmax 3-6 hours (oral); PTH suppression: 1-2 weeks
Duration
3-5 days (effects persist after discontinuation)
Half-life
~5-8 hours (plasma); biological effects persist longer
Bioavailability
~70%
Protein binding
~99.9% (VDBP and albumin)
Metabolism
Hepatic via CYP24A1 (24-hydroxylation) to inactive calcitroic acid; also excreted in bile
Excretion
Fecal (~50%); renal (~16% as metabolites)

Contraindications

  • Hypercalcemia
  • Vitamin D toxicity
  • Hypersensitivity to calcitriol
  • Nephrolithiasis (calcium-based)
  • Metastatic calcification

Side effects

Common
HypercalcemiaHyperphosphatemiaHeadacheNauseaPruritusPolyuria
Serious
  • Severe hypercalcemia (nephrocalcinosis, arrhythmias)
  • Nephrolithiasis
  • Metastatic calcification (vascular, soft tissue)
  • Ectopic calcification
  • Adynamic bone disease (PTH oversuppression)

Pregnancy & lactation

Pregnancy

Use only if clearly needed; monitor calcium closely. Crosses placenta; may affect fetal calcium metabolism.

Lactation

Excreted in breast milk; may affect infant calcium metabolism. Monitor infant for hypercalcemia signs.

Drug interactions

Burosumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Calcifediol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cholecalciferol
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Dihydrotachysterol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Doxercalciferol
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Erdafitinib
Severe
Database

Drug interaction classified as: others

Source: DDInter

Ergocalciferol
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Paricalcitol
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Phenobarbitone
Moderate
Textbook

Prolonged use can cause rickets/osteomalacia.

Not explicitly stated, but implies monitoring bone health and vitamin D status, and possibly increasing calcitriol dose or supplementing calcium.

Source: KDT 7e · p343

Magnesium Containing Antacids
Moderate
Database

Increased magnesium absorption in CKD patients; risk of hypermagnesemia.

Avoid magnesium-containing products in CKD patients on calcitriol.

Source: Kimi deep-research + Cla

Phenytoin
Moderate
Database

Enzyme inducers increase calcitriol metabolism, reducing efficacy.

Monitor PTH and calcium; may need calcitriol dose increase.

Source: Kimi deep-research + Cla

Thiazide Diuretics
Moderate
Database

Thiazides reduce urinary calcium excretion; additive with calcitriol increases hypercalcemia risk.

Monitor calcium closely; may need calcitriol dose reduction.

Source: Kimi deep-research + Cla

Related guidelines

Ask House about Calcitriol

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19