Cholecalciferol

Cholecalciferol (Vitamin D3) is a fat-soluble vitamin produced in the skin upon exposure to sunlight and obtained from diet and supplements. It is essential for effective calcium and phosphate absorption required for healthy bones and teeth. Vitamin D3 helps prevent rickets, osteomalacia, and osteoporosis. It is also essential to prevent pre-eclampsia during pregnancy and breastfeeding as it is an essential nutrient for a growing infant. Vitamin D3 has a vital role in immunity boost up. The active form Calcitriol exerts its effect by binding to Vitamin D receptors (VDRs) which are widely distributed through many body tissues.

• Vitamin D3 deficiency
• Rickets
• Osteomalacia
• Osteoporosis
• Tetany caused by hypocalcaemia
• Prevention of pre-eclampsia during pregnancy
• Immunity boost up

The active form of Vitamin D3, Calcitriol, exerts its effect by binding to the Vitamin D receptors (VDRs) which are widely distributed through many body tissues. Vitamin D3 has a half life of about 50 days as it is fat soluble. Vitamin D3 is absorbed in the small intestine and bound to specific α-globulins and transported to the liver where it is metabolised to 25-hydroxy Vitamin D3 (Calcidiol). A second hydroxylation to 1,25-dihydroxy Vitamin D3 (Calcitriol) occurs in the kidney. This metabolite is responsible for the vitamin's ability to increase the absorption of calcium. Non-metabolised Vitamin D3 is stored in tissues such as fat and muscle. Vitamin D3 is eliminated via faeces and urine.

The active form of Vitamin D3, Calcitriol, binds to Vitamin D receptors to increase calcium and phosphate absorption and regulate bone mineralization.

Capsule (Adults):

• Treatment of deficiency: 40,000 IU once weekly for 7 weeks, then maintenance: 1400-2000 IU/day
• Prevention: 20,000 IU every 4 weeks
• Osteoporosis: 20,000 IU once a month

Capsule (Children 12-18 years):

• Treatment: 20,000 IU every 2 weeks for 6 weeks
• Prevention: 20,000 IU every 6 weeks

Tablet (1000 IU): 1-2 tablets daily, with food or within 1 hour after a meal.

Oral Solution: Up to 1 year: 400 IU/day; 1-18 years: 600 IU/day.

Injection (Treatment): Rickets: 1 ampoule every 2 weeks for 1 month, then every 4 months; Osteoporosis/Osteomalacia: 1 ampoule every 2 weeks for 3 months; Tetany: 1 ampoule every 4 months (up to 2 ampoules); Menopause: 1 ampoule every 6 months.

Injection (Prevention): Pregnancy: ½ ampoule at 6th/7th month; Breastfeeding: ½ ampoule every 6 months; Children up to 5 years: 1 ampoule every 6 months; Adolescent: 1 ampoule every 6 months; Elderly: ½ ampoule every 3 months.

Take with food or within 1 hour after a meal. Swallow capsules/tablets whole. Chew chewable tablets. Injection: For oral use, pour into a spoon and mix with water/milk; for IM use, inject intramuscularly.

If you miss a dose of Cholecalciferol, take it as soon as you remember. If it is almost time for the next dose, skip the missed dose. Do not double the dose.

Common Side Effects:

• Anorexia (loss of appetite)
• Headache
• Nausea
• Vomiting
• Abdominal pain
• Constipation

Serious Side Effects (Rare - Overdose): Hypercalcemia, polyuria, weakness, apathy, thirst, vascular and organ calcification.

• Monitor plasma-calcium concentration in patients receiving high doses, in renal impairment, and during pregnancy & lactation.
• People using Digoxin and Thiazide Diuretics should consult a healthcare practitioner.
• People with liver or kidney disease, primary hyperthyroidism, lymphoma, tuberculosis and granulomatous disease should consult a healthcare practitioner.

• All diseases associated with hypercalcaemia
• Hypersensitivity to Vitamin D3 or any excipients
• Evidence of Vitamin D3 toxicity

Phenytoin or barbiturates can decrease the effect of vitamin D. Glucocorticoids can decrease the effect of vitamin D. Digitalis and other cardiac glycosides effects may be accentuated with calcium combined with vitamin D. Cholestyramine or paraffin oil may reduce gastrointestinal absorption of vitamin D. Actinomycin and imidazole antifungal agents interfere with vitamin D activity.

Take with food or within 1 hour after a meal.

Studies have shown safe use of doses up to 4000 IU during pregnancy. The recommended daily intake for pregnant women is 400 IU, however, higher doses may be required in deficiency. Pregnant women should follow their medical practitioner's advice.

Vitamin D3 and its metabolites are excreted in breast milk. Overdose in infants induced by nursing mothers has not been observed; however, caution is required.

Pediatric dose: Up to 1 year: 400 IU/day; 1-18 years: 600 IU/day; 12-18 years (capsule): Treatment 20,000 IU every 2 weeks for 6 weeks, Prevention 20,000 IU every 6 weeks.

Elderly: ½ ampoule every 3 months (injection) or 1000-2000 IU/day (oral).

Monitor plasma-calcium concentration in renal impairment. Consult a doctor for kidney disease.

The most serious consequence of acute or chronic overdose is hypercalcaemia. Symptoms include nausea, vomiting, polyuria, anorexia, weakness, apathy, thirst, constipation. Chronic overdose can lead to vascular and organ calcification. Treatment: Stop vitamin D intake and rehydration.

Store in a cool (below 25°C) and dry place protected from light. Keep away from the reach of children.

Cholecalciferol (Vitamin D3)