VITAMIN-D

Cholecalciferol (D3)
AND
Ergocalciferol (D2)

BY RABOSIGO, N1
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 Introduction

Vitamin D is a fat soluble vitamin.

2 Forms;
• Ergo-calciferol (Vit-D2): Synthesized by plants and
ingested in diet
• Chole-calciferol (Vit-D3): Synthesized by humans through
the skin by utilization of sunlight, a small portion obtained
from animal sources i.e oily fish, egg york. Activated to
calcitriol (1, 25-(OH)2D3 the active form.
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Vitamin D is necessary for adequate gastrointestinal
absorption of calcium. Insufficient amounts of vitamin D
result in low serum calcium and can trigger a release of
parathyroid hormone. This may produce secondary
hyperparathyroidism, leading to mobilization of calcium from
bone and a reduction in bone mineral density.

Long-term vitamin D deficiency can lead to muscle weakness

and increase the risk for osteoporotic fractures, falls, rickets,
and osteomalacia. Supporting on epidemiologic evidence,
researchers suggest vitamin D deficiency may increase the risk
for certain chronic illnesses, including various cancers,
autoimmune diseases, and cardiovascular disease, (Medscape,
2016).
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VITAMIN-D SYNTHESIS & BIOTRANSFORMATION

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 Biotransformation cont…

OH

25
OH

HO 1st activation
(occurs in liver)

2nd activation
(occurs in kidney)
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 Functions of Vit-D

• Facilitates the absorption of calcium and phosphorus

by the body; therefore essential in building and
maintenance of healthy bone
• Decrease renal excretion of phosphorus and calcium
• Prevention and treatment of bone disorders

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The role of Vit-D in the bone
mineral homeostasis

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 Active forms of Vitamin D

• Ergocalciferol→ Calciferol/ 1,25 Hydroxyvitamin

D2(Active form)
• Calciferol available as 50, 000 units vit D eq. per film
coated capsule

• Cholecalciferol → Calcitriol/ 1, 25 Hydroxyvitamin

D3 (Active form)
• Calcitriol available as Rocaltrol 0.25mcg and 0.5 mcg
capsules

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 Calcitriol indications

• Vitamin-D resistant conditions

• Hypoparathyroidism
• Renal osteodystrophy: 0.25mcg- 1mcg daily or eod
• Post-menopausal osteoporosis (2nd line): 0.25mcg BD
• Paediatrics (under 1 year): 0.03mcg/kg/day

NB: Daily calcium intake not to exceed 1000mg

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 Calciferol indications
• Vitamin-D deficiencies associated with
malabsorbtion -50,000- 100,000 units daily
• Rickets (children) and osteomalacia (adult): 50, 000 IU
twice weekly followed by 50, 000 IU fortnightly
• Hypocalcemia
• Psoriasis
• Chronic liver disease: 50, 000-100, 000 IU/day
• Renal osteodystrophy
• Hypoparathyroidism: 50, 000- 200, 000 IU daily
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Publications including (Armas 2004, Houghton 2006)
demonstrate that cholecalciferol is 1.7 to 3 times more
potent and has a longer duration of action compared
to ergocalciferol in increasing serum levels of the
active form of vitamin D in humans.

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 . Armas et al study demonstrates the difference in
duration of effect and potency
Healthy volunteers were given a single 50,000 unit dose of either
vitamin D2 (ergocalciferol) or vitamin D3 (cholecalciferol)

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 Vitamin-D drug interactions

• Drugs that interfere with absorption such as

colestyramine, liquid paraffin
• CYP450 oxidative enzymes inducing agents;
PhenobarbitalS, phenytoin

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 Adverse effects

• Elevated calcium and phosphate serum levels

• Organ failure (lungs, heart)
• Growth retardation in children
• Seizures

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 Conclusion

• Ergocalciferol and cholecalciferol are not bioequivalent and

should not be considered interchangeable.
• Few comparison trials exist, but based on pharmacokinetic
studies cholecalciferol is preferred over ergocalciferol.
• However, despite its shorter half-life and decreased potency,
in the setting of severe deficiency a high-dose ergocalciferol
is often only given once weekly.

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 References
• (http://www.medscape.com/viewarticle/746941)
• http://home.intekom.com/pharm/lennon/calcifer.html----insert
• Armas LA, Hollis BW, Heaney RP. Vitamin D2 is much less effective than vitamin D3 in
humans. J ClinEndocrinolMetab. 2004 Nov;89(11):5387-91. PMID 15531486.
• Trang HM, Cole DE, Rubin LA, et al. Evidence that vitamin D3 increases serum 25-
hydroxyvitamin D more efficiently than does vitamin D2. Am J ClinNutr. 1998 Oct;68(4):854-
8. PMID 9771862
• Houghton LA, Vieth R. The case against ergocalciferol (vitamin D2) as a vitamin supplement.
Am J ClinNutr. 2006 Oct;84(4):694-7. PMID 17023693.
• Bjelakovic G, Gluud LL, Nikolova D, et al. Vitamin D supplementation for prevention of
mortality in adults. Cochrane Database Syst Rev. 2014 Jan 10;1:CD007470. PMID 24414552.
• http://www.medscape.com/viewarticle/767843_2
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• Bickle, D. 2012. Agents That Affect Bone Mineral
Homeostasis. Ch42 in Katzung, B., Masters, S. &
Trevor, A., 2012. Basic and Clinical Pharmacology,
New York, Mcgraw Hill.
• Rossiter, D. 2014. Vitamins in The South African
Medicines Formulary, Cape Town, Health and
Medical Publishing Group.

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