13 Oct Cholecalciferol
Available dosage forms:
|Oil||30,000 / 50,000 / 75,000 / 100,000 / 120,000 / 125,000 / 150,000 / 200,000 / 250,000 / 300,000 IU/Dose|
|Injection||300,000 / 600,000 IU/Dose|
|Capsules||4,000 / 5,000 / 10,000 / 20,000 / 25,000 / 50,000 / 100,000 IU/Dose|
|Powder||50,000 / 100,000 / 150,000 / 200,000 IU/Dose|
Cholecalciferol is used for:
- Prevention and treatment of Vitamin D deficiency
- Treatment of osteoporosis
- Prevention of corticosteroid-induced osteoporosis
How it Works
Cholecalciferol regulates calcium homeostasis and bone metabolism. Increases intestinal absorption and renal absorption of calcium and phosphate. Cholecalciferol also promotes bone mineralisation.
- Obesity – may need higher than usual doses to achieve adequate status
- Hyperphosphataemia – risks of ectopic calcification
- Severe renal impairment
- Pregnancy – in high doses
- Breastfeeding – in high doses
Most adverse effects are due to the effects of hypercalcaemia such as:
- Muscle weakness
We make Cholecalciferol in oil and powder form. We use Olive oil as a carrier and this can be made in the form of a capsule or as a syringe. Dosages will vary depending on your requirements and can be anything from 4000IU up to 300,000IU. Cholecalciferol is best taken with food, however, avoid caffeine consumption half an hour before or after taking as this can interfere with the absorption. If you don’t like the taste of the olive oil it can be spread onto a piece of bread or even mixed with orange juice.
The oil formulation capsules or syringe need to be kept refrigerated but the powder can be kept at room temperature.
Pharmacologic Category: Pro-Hormone
Vitamin D is a fat-soluble vitamin and has two primary forms: cholecalciferol (vitamin D3) and ergocalciferol (vitamin D2). Various foods are fortified with vitamin D, including milk and cereal. Other dietary sources include fish liver oils, fatty fish, and eggs from hens that have been supplemented with vitamin D. The chemical structure differences between the two forms of vitamin D do not affect the metabolism or clinical responses once activated within the body.
Mechanism of Action
Cholecalciferol is metabolized to its active form, calcitriol (1.25-dihydroxyvitamin D); all vitamin D activity is due to this metabolite. Calcitriol promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium mobilization from bone to plasma. Calcitriol promotes intestinal absorption of calcium through binding to a specific receptor in the mucosal cytoplasm of the intestine.
Cholecalciferol is administered orally. Maximal clinical effects from a given dosage are usually observed in 4 weeks. Dietary vitamin D is absorbed from the GI tract in the presence of bile salts and is initially bound to chylomicrons, then is slowly transferred to vitamin D binding protein (DBP) in the serum. The uptake by chylomicrons results in vitamin D update by adipose tissue and muscle; remaining vitamin D in circulation is then metabolized by the liver.
Of relevance to breast-fed children, the 25-hydroxyvitamin D metabolite is distributed into maternal breast milk; however, the concentration in breast milk is dependent upon the maternal serum concentration. Typical breast milk concentrations of vitamin D are < 25 International Units/L to 78 International Units/L, without maternal vitamin D supplementation; these levels of vitamin D will not be sufficient to prevent vitamin D deficiency in infants who are exclusively breast-fed.
Administration of high-dose vitamin D supplementation to nursing mothers has been shown to increase the concentration of vitamin D in breast milk and favorably increase 25(OH)D levels in infants; however, the results have not been validated and supplementation to infants is still recommended.3
Persons with body mass index (BMI) of >= 30 have lower 25(OH)D levels as compared to those with a lower BMI. In addition, people who are obese may require higher doses of vitamin D to achieve 25(OH)D levels comparable to non-obese people. The increased amounts of subcutaneous fat in these persons sequester more vitamin D and alter its release into the circulation.
Also, obese patients who have undergone gastric bypass surgery will become vitamin D deficient over time without sufficient supplementation, since part of the small intestine where vitamin D is absorbed is bypassed and vitamin D mobilization from fat stores will not compensate over time.1
Clinically, cholecalciferol is similar to ergocalciferol; therefore, clinicians should also take contraindications and precautions for ergocalciferol into consideration when initiating cholecalciferol therapy.
Cholecalciferol should not be used in patients with hypercalcemia, hypervitaminosis D, and vitamin D hypersensitivity or hypersensitivity to any of the excipients in the formulation. Hypersensitivity to vitamin D is one etiologic factor in infants of idiopathic hypercalcemia where vitamin D intake must be restricted.4
Ergocalciferol (Vitamin D2) is classified as FDA pregnancy risk category C; dietary supplements of cholecalciferol should be treated similarly with respect to pregnancy. Adverse effects have not been reported with the normal daily intake of Vitamin D within the recommended dietary daily intakes for a pregnant female.
The 25-hydroxyvitamin D metabolite of vitamin D (cholecalciferol) is distributed into human breast milk at concentrations relative to the maternal serum concentration. Typical breast milk concentrations (without maternal supplementation) are not sufficient to prevent vitamin D deficiency in infants that are exclusively breast-fed and do not receive other vitamin D supplementation.
Like ergocalciferol, cholecalciferol can increase serum phosphorus levels. Concurrent administration of phosphorus salts may increase the toxicity of cholecalciferol.10
In general, the use of supplemental vitamin D according to recommended dietary intakes is not associated with serious adverse reactions. Vitamin D may cause side effects in overdose, but such symptoms associated with hypervitaminosis D (and resultant hypercalcemia) are rarely reported. An excess of vitamin D causes abnormally high levels of calcium in the blood and is almost always caused by vitamin D analogs (e.g., calcitriol, doxercalciferol, paricalcitol), rather than vitamin D found in dietary supplements (e.g., cholecalciferol, ergocalciferol).
What are some possible side effects of this medicine?
Constipation; dry mouth; headache; loss of appetite; metallic taste; stomach upset. This list may not describe all possible side effects. Call your doctor for medical advice about side effects. Call your health care provider immediately if you are experiencing any signs of an allergic reaction: skin rash, itching or hives, swelling of the face, lips, or tongue; bone pain; increased thirst; increased urination (especially at night); irregular heartbeat, high blood pressure; seizures; unexpected weight loss; unusually weak or tired
How should I store this medicine?
The oil formulation capsules or syringe need to be kept refrigerated at 2°C to 8°C but the powder can be kept at room temperature at 15°C to 30°C and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the expiration date. Do not flush unused medications or pour down a sink or drain.
Do not share or take any one else’s medicine. Talk with your healthcare provider before starting any new medicine, including over-the-counter, natural products, or vitamins. This patient information summarizes the most important information about your medication; if you would like more information, talk with your doctor.
1. Institute of Medicine (IOM), Food and Nutrition Board. Dietary Reference Intakes for Calcium and Vitamin D. Washington, DC: The National Academies Press, 2011.
2. Jones G. Pharmacokinetics of vitamin D toxicity. Am J Clin Nutr 2008;88(suppl):582S-6S.
3. Wagner CL, Greer FR, and the Section on Breastfeeding and Committee on Nutrition. Prevention of rickets and Vitamin D deficiency in Infants, Children, and Adolescents. Pediatrics 2008;112:1142-1152.
4. Drisdol (ergocalciferol) package insert. New York, NY: Sanofi-Synthelabo, Inc.; 2009 Nov.
5. Kidney Disease Improving Global Outcomes. KDIGO Clinical Practice Guideline for the Diagnosis, Evaluation, Prevention, and Treatment of Chronic Kidney Disease-Mineral and Bone Disorder (CKD_MBD). 2009. http://www.kdigo.org/pdf/KDIGO%20CKD-MBD%20GL%20KI%20Suppl%20113.pdf.
6. Standing Committee on the Scientific Evaluation of Dietary Reference Intakes – Panel on Dietary Reference Intakes, Food and Nutrition Board, Institute of Medicine (IOM). Dietary Reference Intakes for Calcium, Phosphorus, Magnesium, Vitamin D, and Fluoride. The National Academy of Sciences Press, Washington DC; 1997
7. Drisdol (ergocalciferol) package insert. New York, NY: Sanofi-Synthelabo, Inc.; 2009 Nov.
8. Rocaltrol® (calcitriol) package insert. Nutley, NJ: Roche Laboratories, Inc.; 2004 Jul.
9. Hectorol® (doxercalciferol) package insert. Middleton, WI: Bone Care International, Inc.; 2005 Jun.
10. Drisdol® (ergocalciferol) package insert. New York, NY: Sanofi-Synthelabo, Inc.; 2003 Dec.