Everything about Calcitriol totally explained
| PubChem = 134070
| DrugBank = APRD00246
| C=27 | H=44 | O=3
| molecular_weight = 416.64 g/mol
| bioavailability =
| metabolism =
Renal
| elimination_half-life = 5–8 hours
| excretion = Renal
| pregnancy_category = B3
(Au), C
(U.S.)
| legal_status = S4
(Au), POM
(UK)
| routes_of_administration = Oral,
IV, topical
}}
Calcitriol (
INN) or
1,25-dihydroxycholecalciferol (abbreviated
1,25-(OH)2D3) (also known as calitrol) is the active form of
vitamin D found in the body (1,25(OH)2D3). It increases the absorption of
calcium and
phosphate from the
gastrointestinal tract and
kidneys and inhibits release of
calcitonin.
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 (PO
43−), and an increase in
parathyroid hormone (PTH) and/or
prolactin 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
calcitonin. Calcitriol acts in concert with
parathyroid hormone (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:
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.
[Further Information]
Get more info on 'Calcitriol'.
|
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