Cholecalciferol

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Cholecalciferol Quick Reference
Cholecalciferol
IUPAC Name
N/A
Chemical Information
Empirical Formula C27H44O
Molecular Weight 384.6
General Drug Information
Classification Vitamin D Analog
Schedule Legend
How Supplied Oral Tablets
Trade Names Delta-D
Pregnancy Category C
Breast Feeding No data available.
Generic Availability Generic available (Not available in U.S.)
Patent Expiration Date N/A
Administration Information
Route(s) Oral
Method(s) (When administered with Alendronate): Take one tablet at least 30 minutes before the first food, beverage or medication of the day. Take this medication once a week in the morning.
Pharmacokinetic Information
Absorption F = similar to taking cholecalciferol alone (F is unknown).
tmax = ~11 hours
Distribution Vd = Rapidly distributed to liver
Protein binding = Binds to vitamin D-binding protein
Metabolism metabolized in the liver first then in the kidney
Excretion T1/2 = ~14 hours
Urine (2.4%) and feces (4.9%) as metabolites

Contents

Brand/Trade Names of Drug

Fosamax Plus D

Generic Name of Drug

Cholecalciferol (kole e kal SI fer ole) Cholecalciferol Pronunciation Click Here

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Description

Cholecalciferol is vitamin D3 which involves in normal bone formation. It is not available in U.S. as a single drug. A combination of cholecalciferol and alendronate was approved by FDA for the treatment and prevention of osteoporosis.


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Mechanism of action

Cholecalciferol is vitamin D3 which is required for normal bone formation. It is converted to 25-hydroxyvitamin D3 in the liver and then further converted to 1,25-dihydroxyvitamin D3 (calcitriol) in the kidney. This conversion is stimulated by parathyroid hormone and hypophosphatemia. As a result, 1,25-dihydroxyvitamin D3 increases the absorption of calcium and phosphate in the intestines.[1]

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Time Required for Therapeutic Response

  • Data not available.[1]

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Pharmacokinetics

Absorption

The time for cholecalciferol to have peak effects is about 11 hours.[2]

Distribution

It is primarily distributed through the liver.[2] It binds to vitamin D-binding protein in the circulation.[1]

Metabolism

It is metabolized primarily by liver and kidney hydroxylation. Glucuronidation has minimal effects.[2]

Excretion

Cholecalciferol is excreted as metabolites in urine (2.4%) and feces (4.9%). The half-life (t1/2) of cholecalciferol is about 14 hours.[2]

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Special Population Pharmacokinetics

  • Renal insufficiency: The production of 1,25-dihydroxyvitamin D3 may be reduced.[1]
  • Hepatic insufficiency: The absorption of cholecalciferol may reduce in patints with inadequate bile production.[1]
  • Hemodialysis: Unknown.[2]
  • Geriatric: Elderly may have a higher dietary requirement for cholecalciferol.[1]
  • Pediatric: Unknown.[2]
  • Gender: Unknown.[2]

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Indications

FDA Approved Indications

  • Dietary supplement[2]
  • Treatment of vitamin D deficiency[2]
  • Prophylaxis of deficiency[2]

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Dosage

  • Starting & Maintenance Dose: Oral: 400-1000 units/day.[2]
  • Maximum Dosage Limits
    • Oral: 1000 units/day.[2]
  • Dosage Adjustment
    • Renal insufficiency: Unknown.[2]
    • Hepatic insufficiency: Unknown.[2]
    • Hemodialysis: Unknown.[2]
    • Geriatric: Unknown.[2]
    • Gender: Unknown.[2]


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Administration

  • Route: Oral
  • Method: Swallow the tablet with a full glass (8oz.) of plain water.

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Monitoring Parameters

  • None

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Contraindications/Precautions

Contraindications

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Precautions

  • None Known

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Pregnancy indications

  • Pregnancy category: Category C.[2]

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Breast-feeding indications

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Drug-Drug Interactions

Cholecalciferol Drug/Drug Interaction Chart[1][2]
Severity Level Click here to see Severity Level Legend Increased Effect/Toxicity Decreased Effect
4 None Known None Known
3 magaldrate[3][4] The concentration of magnesium may be increased by vitamin D analog when cholecalciferol is co-administered with magaldrate.magnesium citrate[3][4] The concentration of magnesium may be increased by vitamin D analogs when cholecalciferol is co-administered with magnesium citrate.magnesium hydroxide[3][4] The concentration of magnesium may be increased by vitamin D analogs when cholecalciferol is co-administered with magnesium hydroxide.phosphorus salts[3][4] The risk of hyperphosphatemia increased by vitamin D analogs when cholecalciferol is co-administered with phosphorus salts.vitamin D analogs[3][4] The risk of hyperphosphatemia is increased by vitamin D analogs when cholecalciferol is co-administered with other vitamin D analogs. None Known
2 None Known barbiturates[5] The metabolism of cholecalciferol is increased when cholecalciferol is co-administered with barbiturates.phenytoin[5] The metabolism of cholecalciferol is increased when cholecalciferol is co-administered with phenytoin.fosphenytoin[5] The metabolism of cholecalciferol is increased when cholecalciferol is co-administered with fosphenytoin.thiazide diuretics[1] The metabolism of cholecalciferol is increased when cholecalciferol is co-administered with thiazide diuretics.cholestyramine[6] The absorption of vitamin D is reduced when cholecalciferol is co-administered with cholestyramine.colestipol[7] The absorption of vitamin D is reduced when cholecalciferol is co-administered with colestipol.mineral oil[8] The absorption of vitamin D is reduced when cholecalciferol is co-administered with mineral oil.orlistat[9] The absorption of vitamin D is reduced when cholecalciferol is co-administered with orlistat.ketoconazole[3] The conversion of cholecalciferol to calcitriol may be reduced when cholecalciferol is co-administered with ketoconazole.
1 corticosteroids[10] Corticosteroids decrease the absorption of calcium, which opposes the effect of cholecalciferol. None Known

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Drug-Food-Herb Interactions

Cholecalciferol Drug/Food/Herb Interaction Chart
Severity Level Click here to see Severity Level Legend Increased Effect/Toxicity Decreased Effect
4 None Known None Known
3 None Known Food[1] The abosorption of cholecalciferol is decreased when co-administered with certain foods eg. olestra.
2 None Knownn None Known
1 None Known None Known


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Adverse Reactions/Side Effects

Cholecalciferol Adverse Reactions Chart (Frequency not defined)[2]
Body System Adverse Reactions
CNS Irritability, headache, somnolence, overt psychosis (rare)
Cardiovascular Arrhythmia, hyper-/hypotension, cardiac arrhythmia
Dermatologic Pruritus
Endocrine & metabolic Polydipsia
GI Nausea, vomiting, anorexia, pancreatitis, metallic taste, dry mouth, constipation, weight loss
Neuromuscular & skeletal Bone pain, myalgia, weakness, muscle pain
Genitourinary Albuminuria, polyuria
Hepatic Increased liver function test
Ocular Conjunctivitis, photophobia
Renal Azotemia, nephrocalcinosis


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Overdosage Measures

No current recommendations. [2]

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Product Information and Distribution

Cholecalciferol is not available as a single agent in U.S.

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Patient Information

  • Take as directed.
  • Avoid OTC medications unless instructed by your physician.
  • Possible side effects include headache, nausea, vomiting and bone pain.
  • Inform your doctor if you are or intend to become pregnant.

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References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 Fosamax Plus D® (alendronate sodium and cholecalciferol) package insert.Whitehouse Station. NJ;Merck & Co.Inc; 2006 Feb.
  2. ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 2.11 2.12 2.13 2.14 2.15 2.16 2.17 2.18 2.19 2.20 2.21 2.22 2.23 2.24 2.25 Lexi-Comp (2003). Drug Information Handbook. 11th Edition., APhA.
  3. ↑ 3.0 3.1 3.2 3.3 3.4 3.5 Rocaltrol® (calcitriol) package insert. Nutley, NJ: Roche Laboratories, Inc.; 2004 Jul.
  4. ↑ 4.0 4.1 4.2 4.3 4.4 Hectorol® (doxercalciferol) package insert. Middleton, WI: Bone Care International, Inc.; 2005 Jun.
  5. ↑ 5.0 5.1 5.2 McNamara JO. Drugs effective in the therapy of the epilepsies.Gilman AG, Hardman JG, Limbird LE, (eds.) In: Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed., New York, McGraw-Hill Companies. 2001:530—2.
  6. ↑ Questran® and Questran® Light (cholestyramine) package insert. Spring Valley, NY: Par Pharmaceutical Inc; 2002 July.
  7. ↑ Colestid® and Flavored Colestid® (colestipol) package insert. Kalamazoo, MI: Pharmacia & Upjohn Company; 2002 July.
  8. ↑ Drisdol® (ergocalciferol) package insert. New York, NY: Sanofi-Synthelabo, Inc.; 2003 Dec.
  9. ↑ Xenical® (orlistat) package insert. Nutley, NJ: Roche Laboratories Inc.; 2005 Jan.
  10. ↑ Drisdol® (ergocalciferol) package insert. New York, NY: Sanofi-Synthelabo, Inc.; 2003 Dec.

PUBMED References

Efficacy Trial Articles

  1. Aloia JF, Talwar SA, Pollack S, Yeh J.A randomized controlled trial of vitamin D3 supplementation in African American women.Arch Intern Med. 2005 Jul 25;165(14):1618-23.
  2. Avenell A, Gillespie WJ, Gillespie LD, O'Connell DL.Vitamin D and vitamin D analogues for preventing fractures associated with involutional and post-menopausal osteoporosis.Cochrane Database Syst Rev. 2005 Jul 20;(3).
  3. Bischoff-Ferrari HA, Dawson-Hughes B, Willett WC, Staehelin HB, Bazemore MG, Zee RY, Wong JB.Effect of Vitamin D on falls: a meta-analysis.JAMA. 2004 Apr 28;291(16):1999-2006.
  4. Chapuy MC, Arlot ME, Duboeuf F, Brun J, Crouzet B, Arnaud S, Delmas PD, Meunier PJ.Vitamin D3 and calcium to prevent hip fractures in the elderly women.N Engl J Med. 1992 Dec 3;327(23):1637-42.
  5. Dawson-Hughes B, Harris SS, Krall EA, Dallal GE.Effect of calcium and vitamin D supplementation on bone density in men and women 65 years of age or older.N Engl J Med. 1997 Sep 4;337(10):670-6.
  6. Epstein S.The problem of low levels of vitamin D and osteoporosis: use of combination therapy with alendronic acid and colecalciferol (vitamin D3).Drugs Aging. 2006;23(8):617-25.
  7. Grant WB.Cholecalciferol, not ergocalciferol, should be used for vitamin D supplementation.Age Ageing. 2006 Nov;35(6):645; author reply 645. Epub 2006 Sep 18.
  8. Meunier P.Prevention of hip fractures by correcting calcium and vitamin D insufficiencies in elderly people.Scand J Rheumatol Suppl. 1996;103:75-8; discussion 79-80.
  9. Tokar EJ, Ancrile BB, Ablin RJ, Webber MM.Cholecalciferol (vitamin D3) and the retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) are synergistic for chemoprevention of prostate cancer.J Exp Ther Oncol. 2006;5(4):323-33.
  10. Trivedi DP, Doll R, Khaw KT.Effect of four monthly oral vitamin D3 (cholecalciferol) supplementation on fractures and mortality in men and women living in the community: randomised double blind controlled trial.BMJ. 2003 Mar 1;326(7387):469.
  11. Uyar M, Sezer S, Arat Z, Elsurer R, Ozdemir FN, Haberal M.1,25-dihydroxyvitamin D(3) therapy is protective for renal function and prevents hyperparathyroidism in renal allograft recipients.Transplant Proc. 2006 Sep;38(7):2069-73.
  12. Woo TC, Choo R, Jamieson M, Chander S, Vieth R.Pilot study: potential role of vitamin D (Cholecalciferol) in patients with PSA relapse after definitive therapy.Nutr Cancer. 2005;51(1):32-6.


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Therapeutic Class Comparison Articles

  1. Richy F, Schacht E, Bruyere O, Ethgen O, Gourlay M, Reginster JY.Vitamin D analogs versus native vitamin D in preventing bone loss and osteoporosis-related fractures: a comparative meta-analysis.Calcif Tissue Int. 2005 Mar;76(3):176-86.
  2. Ringe JD, Faber H, Fahramand P, Schacht E.Alfacalcidol versus plain vitamin D in the treatment of glucocorticoid/inflammation-induced osteoporosis. J Rheumatol Suppl. 2005 Sep;76:33-40.

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Adverse Effects Articles

  1. Okamoto N, Aruga S, Tomita K, Takeuchi T, Kitamura T.Chronic acid ingestion promotes renal stone formation in rats treated with vitamin D.Int J Urol. 2007 Jan;14(1):60-6.

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External Links


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Monograph created by Khlee3

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