Calcitriol

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Calcitriol
Systematic (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
Identifiers
CAS number 32222-06-3
ATC code A11CC04 D05AX03
PubChem 134070
DrugBank APRD00246
Chemical data
Formula C27H44O3 
Mol. mass 416.64 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism Renal
Half life 5–8 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B3 (Au), C (U.S.)

Legal status

S4 (Au), POM (UK)

Routes Oral, IV, topical

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Overview

Calcitriol (INN) (pronounced /ˌkælsɨˈtraɪɒl/, /ˌkælˈsɨtriːɒl/) 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:[1]

Calcitriol is also sometimes used topically in the treatment of psoriasis, however the evidence to support its efficacy is inconclusive.[2] 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.[1]

See also

Additional images

References

  1. 1.0 1.1 Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
  2. Calcitriol. In: Klasco RK, editor. Drugdex system. vol 128. Greenwood Village (CO): Thomson Micromedex; 2006.


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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .

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