Calcitriol (oral)

Calcitriol (oral)

Clinical data
Pregnancy category	B3 (Au), C (U.S.)
Routes of administration	Oral, IV, topical
ATC code	A11CC04 (WHO) D05AX03 (WHO)
Legal status
Legal status	S4 (Au), POM (UK)
Pharmacokinetic data
Metabolism	Renal
Elimination half-life	5–8 hours
Excretion	Renal
Identifiers
IUPAC name (1R,3S)- 5-[2-[(1R,3aR,7aS)-1- [(2R)-6-hydroxy-6-methyl-heptan-2-yl]- 7a-methyl-2,3,3a,5,6,7-hexahydro-1H- inden-4-ylidene]ethylidene]- 4-methylidene-cyclohexane-1,3-diol
CAS Number	32222-06-3
PubChem CID	134070
DrugBank	APRD00246
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C27H44O3
Molar mass	416.64 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Calcitriol (INN) (Template:PronEng) or 1,25-dihydroxycholecalciferol (abbreviated 1,25-(OH)₂D₃) is the active form of vitamin D found in the body (vitamin D₃). It increases the absorption of calcium and phosphate from the gastrointestinal tract and kidneys and inhibits release of PTH.

Calcitriol is marketed under various trade names including Rocaltrol (Roche), Calcijex (Abbott) and Decostriol (Mibe, Jesalis).

Production and function

It is produced in the kidneys via 25-Hydroxyvitamin D3 1-alpha-Hydroxylase by conversion from 25-hydroxycholecalciferol (calcidiol).

This is stimulated by a decrease in serum calcium and/or phosphate (PO₄³⁻), and an increase in parathyroid hormone (PTH) levels. It increases blood calcium levels by increasing the absorption of calcium and phosphate from the gastrointestinal tract, increasing calcium and phosphate reabsorption in the kidneys and inhibiting the release of PTH.

Calcitriol is also commonly used as a medication in the treatment of hypocalcemia and osteoporosis.

Metabolism

Calcitriol becomes calcitroic acid through the action of 24-hydroxylase. Calcitroic acid is excreted in the urine.

Indications

Calcitriol is indicated for:

• Treatment of hypocalcaemia – hypoparathyroidism, osteomalacia (adults), rickets (infants, children), renal osteodystrophy, chronic renal dialysis
• Treatment of osteoporosis
• Prevention of corticosteroid-induced osteoporosis

Calcitriol is also sometimes used topically in the treatment of psoriasis, however the evidence to support its efficacy is inconclusive. The vitamin D analogue calcipotriol is more commonly used for psoriasis.

Adverse effects

The main adverse drug reaction associated with calcitriol therapy is hypercalcaemia – early symptoms include: nausea, vomiting, constipation, anorexia, apathy, headache, thirst, sweating, and/or polyuria). Compared to other vitamin D compounds in clinical use (cholecalciferol, ergocalciferol), calcitriol has a higher risk of inducing hypercalcaemia. However, such episodes may be shorter and easier to treat due to its relatively short half-life.

See also

• Vitamin D#Synthesis mechanism .28form 3.29

Additional images

• 

  Calcitriol synthesis

References

de:Calcitriol dv:ކެލްސިޓްރިއޯލް mk:Калцитриол

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