Cholecalciferol

Cholecalciferol Uses, Dosage, Side Effects, Food Interaction and all others data.

Vitamin D is essential for normal bone growth and development and to maintain bone density. It is also necessary for utilization of both Calcium and Phosphorus. Vitamin D acts as a hormone and increases reabsorption of Calcium and Phosphorus by the kidneys and increased bone turnover.

The in vivo synthesis of the predominant two biologically active metabolites of vitamin D occurs in two steps. The first hydroxylation of vitamin D3 cholecalciferol (or D2) occurs in the liver to yield 25-hydroxyvitamin D while the second hydroxylation happens in the kidneys to give 1, 25-dihydroxyvitamin D . These vitamin D metabolites subsequently facilitate the active absorption of calcium and phosphorus in the small intestine, serving to increase serum calcium and phosphate levels sufficiently to allow bone mineralization . Conversely, these vitamin D metabolites also assist in mobilizing calcium and phosphate from bone and likely increase the reabsorption of calcium and perhaps also of phosphate via the renal tubules . There exists a period of 10 to 24 hours between the administration of cholecalciferol and the initiation of its action in the body due to the necessity of synthesis of the active vitamin D metabolites in the liver and kidneys . It is parathyroid hormone that is responsible for the regulation of such metabolism at the level of the kidneys .

Trade Name Cholecalciferol
Availability Rx and/or OTC
Generic Cholecalciferol
Cholecalciferol Other Names Calciol, Cholecalciferol, Cholecalciferolum, Colecalciferol, Colecalciferolum, Oleovitamin D3, Vitamin D-3, Vitamin D3
Related Drugs Vitamin D3, ergocalciferol, Drisdol, D3, D3-50, Enfamil D-Vi-Sol, Replesta, Carlson D
Type Oral capsule, 14,000 intl units, 2000 intl units, 25,000 intl units, 400 intl units, 50,000 intl units, 5000 intl units), oral liquid, oral solution, oral tablet, oral tablet, chewable, oral tablet, disintegrating, oral wafer
Formula C27H44O
Weight Average: 384.6377
Monoisotopic: 384.33921603
Protein binding

The protein binding documented for cholecalciferol is 50 to 80% . Specifically, in the plasma, vitamin D3 (from either diet or the skin) is bound to vitamin D-binding protein (DBP) produced in the liver, for transport to the liver. Ultimately, the form of vitamin D3 reaching the liver is 25-hydroxylated, and such 25-hydroxycholecalciferol is bound to DBP (α2-globulin) whilst circulating in the plasma .

Groups Approved, Nutraceutical
Therapeutic Class Vitamin in bone formation, Vitamin-D preparations
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Cholecalciferol
Cholecalciferol

Uses

Vitamin D is used to treat and prevent bone disorders (such as rickets, osteomalacia). Vitamin D is made by the body when skin is exposed to sunlight. Sunscreen, protective clothing, limited exposure to sunlight, dark skin, and age may prevent getting enough vitamin D from the sun.

Vitamin D with calcium is used to treat or prevent bone loss (osteoporosis). Vitamin D is also used with other medications to treat low levels of calcium or phosphate caused by certain disorders (such as hypoparathyroidism, pseudohypoparathyroidism, familial hypophosphatemia). It may be used in kidney disease to keep calcium levels normal and allow normal bone growth.

Cholecalciferol is also used to associated treatment for these conditions: Calcium and Vitamin D Deficiencies, Deficiency of Vitamin D3, Deficiency, Vitamin A, Deficiency, Vitamin D, Fracture Bone, Hip Fracture, Hypoparathyroidism, Hypophosphatemia, Familial, Menopause, Osteomalacia, Osteoporosis, Postmenopausal Osteoporosis, Vertebral Fractures, Vitamin D Resistant Rickets, Vitamin Deficiency, Severe Bone Resorption, Spine fracture, Calcium supplementation, Nutritional supplementation, Vitamin D Supplementation, Vitamin supplementation

How Cholecalciferol works

Most individuals naturally generate adequate amounts of vitamin D through ordinary dietary intake of vitamin D (in some foods like eggs, fish, and cheese) and natural photochemical conversion of the vitamin D3 precursor 7-dehydrocholesterol in the skin via exposure to sunlight .

Conversely, vitamin D deficiency can often occur from a combination of insufficient exposure to sunlight, inadequate dietary intake of vitamin D, genetic defects with endogenous vitamin D receptor, or even severe liver or kidney disease . Such deficiency is known for resulting in conditions like rickets or osteomalacia, all of which reflect inadequate mineralization of bone, enhanced compensatory skeletal demineralization, resultant decreased calcium ion blood concentrations, and increases in the production and secretion of parathyroid hormone . Increases in parathyroid hormone stimulate the mobilization of skeletal calcium and the renal excretion of phosphorus . This enhanced mobilization of skeletal calcium leads towards porotic bone conditions .

Ordinarily, while vitamin D3 is made naturally via photochemical processes in the skin, both itself and vitamin D2 can be found in various food and pharmaceutical sources as dietary supplements. The principal biological function of vitamin D is the maintenance of normal levels of serum calcium and phosphorus in the bloodstream by enhancing the efficacy of the small intestine to absorb these minerals from the diet . At the liver, vitamin D3 or D2 is hydroxylated to 25-hydroxyvitamin D and then finally to the primary active metabolite 1,25-dihydroxyvitamin D in the kidney via further hydroxylation . This final metabolite binds to endogenous vitamin d receptors, which results in a variety of regulatory roles - including maintaining calcium balance, the regulation of parathyroid hormone, the promotion of the renal reabsorption of calcium, increased intestinal absorption of calcium and phosphorus, and increased calcium and phosphorus mobilization of calcium and phosphorus from bone to plasma to maintain balanced levels of each in bone and the plasma .

In particular, calcitriol interacts with vitamin D receptors in the small intestine to enhance the efficiency of intestinal calcium and phosphorous absorption from about 10-15% to 30-40% and 60% increased to 80%, respectively . Furthermore, calcitriol binds with vitamin D receptors in osteoblasts to stimulate a receptor activator of nuclear factor kB ligand (or RANKL) which subsequently interacts with receptor activator of nuclear factor kB (NFkB) on immature preosteoclasts, causing them to become mature bone-resorbing osteoclasts . Such mature osteoclasts ultimately function in removing calcium and phosphorus from bone to maintain blood calcium and phosphorus levels . Moreover, calcitriol also stimulates calcium reabsorption from the glomerular filtrate in the kidneys .

Additionally, it is believed that when calcitriol binds with nuclear vitamin D receptors, that this bound complex itself binds to retinoic acid X receptor (RXR) to generate a heterodimeric complex that consequently binds to specific nucleotide sequences in the DNA called vitamin D response elements . When bound, various transcription factors attach to this complex, resulting in either up or down-regulation of the associated gene's activity. It is thought that there may be as much as 200 to 2000 genes that possess vitamin D response elements or that are influenced indirectly to control a multitude of genes across the genome . It is in this way that cholecalciferol is believed to function in regulating gene transcription associated with cancer risk, autoimmune disorders, and cardiovascular disease linked to vitamin D deficiency . In fact, there has been some research to suggest calcitriol may also be able to prevent malignancies by inducing cellular maturation and inducing apoptosis and inhibiting angiogenesis, exhibit anti-inflammatory effects by inhibiting foam cell formation and promoting angiogenesis in endothelial colony-forming cells in vitro, inhibit immune reactions by enhancing the transcription of endogenous antibiotics like cathelicidin and regulate the activity and differentiation of CD4+ T cells, amongst a variety of other proposed actions .

Dosage

Cholecalciferol dosage

Oral solution: Colecalciferol (Vitamin D3) is recommended 5-10 mcg or 1-2ml (200-400 IU)/day or as directed by the physician.

Chewable tablet: Cholecalciferol (Vitamin D3) is recommended 100 IU (1 tablet) daily, or as directed by physician. Take the medicine with food or within 1 hour after a meal. Place the tablet in mouth swallow after chewing.

Injection:

  • Treatment of Cholecalciferol deficiency: 40,000 lU/week for 7 weeks, followed by maintenance therapy (1400-2000 lU/day). Follow-up 25 (OH) D measurements should be made approximately 3 to 4 months after initiating maintenance therapy to confirm that the target level has been achieved.
  • Prevention of Vitamin D deficiency: 20,000 lU/Month.
  • Treatment of Vitamin D deficiency: 12-18 years: 20,000 IU, once every 2 weeks for 6 weeks. Prevention of Vitamin D deficiency, 12-18 years: 20,000 IU, once every 6 weeks.

Side Effects

Generally all nutritional supplements are considered to be safe and well tolerable. However, few side-effects can generally occur including hypercalcaemia syndrome or Calcium intoxication (depending on the severity and duration of hypercalcaemia), occasional acute symptoms include anorexia, headache, nausea, vomiting, abdominal pain or stomach ache and constipation with the administration of Colecaciferol.

Toxicity

Chronic or acute administration of excessive doses of cholecalciferol may lead to hypervitaminosis D, manifested by hypercalcemia and its sequelae . Early symptoms of hypercalcemia may include weakness, fatigue, somnolence, headache, anorexia, dry mouth, metallic taste, nausea, vomiting, vertigo, tinnitus, ataxia, and hypotonia . Later and possibly more serious manifestation include nephrocalcinosis, renal dysfunction, osteoporosis in adults, impaired growth in children, anemia, metastatic calcification, pancreatitis, generalized vascular calcification, and seizures .

Safety of doses in excess of 400 IU (10mcg) of vitamin D3 daily during pregnancy has not been established . Maternal hypercalcemia, possibly caused by excessive vitamin D intake during pregnancy, has been associated with hypercalcemia in neonates, which may lead to supravalvular aortic stenosis syndrome, the features of which may include retinopathy, mental or growth retardation, strabismus, and other effects . Hypercalcemia during pregnancy may also lead to suppression of parathyroid hormone release in the neonate, resulting in hypocalcemia, tetany, and seizures .

Vitamin D is deficient in maternal milk; therefore, breastfed infants may require supplementation. Use of excessive amounts of Vitamin D in nursing mothers may result in hypercalcemia in infants. Doses of Vitamin D3 in excess of 10 µg daily should not be administered daily to nursing women.

Precaution

People with the following conditions should exercise caution when considering taking vitamin D supplements: High blood Calcium or Phosphorus level, Heart problems, Kidney disease.

Vitamin D must be taken with adequate amounts of both Calcium and Magnesium supplementation. When Calcium level is low (due to insufficient vitamin D and calcium intake), the body activates the parathyroid gland, which produces PTH (parathyroid hormone). This hormone kick starts vitamin D hormone production and assists removal of Calcium from the bones to be used in more important functions such as neutralizing body acidity.

Interaction

Cholecalciferol is known to interact with Carbamazepine, Dactinomycin, Diuretics, Fosphenytoin, Miconazole, Phenobarbital, Phenytoin, Primidone

Food Interaction

No interactions found.

Volume of Distribution

Studies have determined that the mean central volume of distribution of administered cholecalciferol supplementation in a group of 49 kidney transplant patients was approximately 237 L .

Elimination Route

Cholecalciferol is readily absorbed from the small intestine if fat absorption is normal . Moreover, bile is necessary for absorption as well .

In particular, recent studies have determined aspects about the absorption of vitamin D, like the fact that a) the 25-hydroxyvitamin D metabolite of cholecalciferol is absorbed to a greater extent than the nonhydroxy form of cholecalciferol, b) the quantity of fat with which cholecalciferol is ingested does not appear to largely affect its bioavailability, and c) age does not apparently effect vitamin D cholecalciferol .

Half Life

At this time, there have been resources that document the half-life of cholecalciferol as being about 50 days while other sources have noted that the half-life of calcitriol (1,25-dihydroxyvitamin D3) is approximately 15 hours while that of calcidiol (25-hydroxyvitamin D3) is about 15 days .

Moreover, it appears that the half-lives of any particular administration of vitamin d can vary due to variations in vitamin d binding protein concentrations and genotype in particular individuals .

Clearance

Studies have determined that the mean clearance value of administered cholecalciferol supplementation in a group of 49 kidney transplant patients was approximately 2.5 L/day .

Elimination Route

It has been observed that administered cholecalciferol and its metabolites are excreted primarily in the bile and feces .

Pregnancy & Breastfeeding use

There is no evidence to suggest that vitamin D is teratogenic in humans even at very high doses. Colecalciferol should be used during pregnancy only if the benefits outweigh the potential risk to the fetus.

It should be assumed that exogenous Colecalciferol passes into the breast milk. In view of the potential for hypercalcaemia in the mother and for adverse reactions from Colecalciferol in nursing infants, mothers may breastfeed while taking Colecalciferol, provided that the serum Calcium levels of the mother and infant are monitored.

Contraindication

Colecalciferol is contraindicated in all diseases associated with hypercalcaemia. It is also contraindicated in patients with known hypersensitivity to Colecalciferol (or medicines of the same class) and any of the constituent excipients. Colecalciferol is contraindicated if there is evidence of vitamin D toxicity.

Acute Overdose

Symptoms: anorexia, headache, vomiting, constipation, dystrophy (weakness, loss of weight), sensory disturbances, possibly fever with thirst, polyuria, dehydration, apathy, arrested growth and urinary tract infections. Hypercalcaemia ensues, with metastatic calcification of the renal cortex, myocardium, lungs and pancreas.

Treatment: Immediate gastric lavage or induction of vomiting to prevent further absorption. Liquid paraffin should be administered to promote faecal excretion. Repeated serum calcium determinations are advisable. If elevated calcium levels persist in the serum, phosphates and corticosteroids may be administered and measures instituted to bring about adequate diuresis.

Innovators Monograph

You find simplified version here Cholecalciferol

Cholecalciferol contains Cholecalciferol see full prescribing information from innovator Cholecalciferol Monograph, Cholecalciferol MSDS, Cholecalciferol FDA label

FAQ

What is Cholecalciferol used for?

Cholecalciferol used to treat vitamin D deficiency. It is also used with calcium to maintain bone strength.

How safe is Cholecalciferol?

You should not use Cholecalciferol if you have had an allergic reaction to vitamin D, or if you have high levels of vitamin D in your body, high levels of calcium in your blood or any condition that makes it hard for your body to absorb nutrients from food.

How does Cholecalciferol work?

Cholecalciferol actions is to increase the uptake of calcium by the intestines.

What are the common side effects of Cholecalciferol?

Common side effects of Cholecalciferol are include:

  • chest pain, feeling short of breath;
  • growth problems (in a child taking cholecalciferol); or.
  • early signs of vitamin D overdose --weakness, metallic taste in your mouth, weight loss, muscle or bone pain, constipation, nausea, and vomiting.

Is Cholecalciferol safe during pregnancy?

Cholecalciferol use is not recommended unless there is a deficiency.

Is Cholecalciferol safe during breastfeeding?

Cholecalciferol use is not recommended unless the clinical condition of the woman requires treatment.

Can I drink alcohol with Cholecalciferol?

No interactions were found between Alcohol and Vitamin D3. This does not necessarily mean no interactions exist. Always consult your healthcare provider.

When should Cholecalciferol be taken?

Cholecalciferol should be taken as soon as you get out of bed in the morning and at least 30 minutes before any food, beverage, or other medicines.

How long does it take for Cholecalciferol to work?

Cholecalciferol may take up to 2 to 3 months to bring levels of vitamin D up, depending on how deficient you are.The recommended daily allowance of vitamin D in the United States is 600 IUs for adults up to age 70 and 800 IUs after age 70.

How long does Cholecalciferol stay in my system?

There are several metabolic products or modified versions of Cholecalciferol.Cholecalciferol has a half-life of about 15 hours, while Cholecalciferol has a half-life of about 15 days.

Can I take Cholecalciferol for long term?

Research suggests that long-term Cholecalciferol supplementation reduces the risk of multiple sclerosis.Cholecalciferol supplements are used to treat adults with severe Cholecalciferol deficiency, resulting in loss of bone mineral content, bone pain, muscle weakness and soft bones.

Can Cholecalciferol be taken daily?

Most experts recommend that you shouldn't take more than 4,000 IU of Cholecalciferol a day.

Who should not take Cholecalciferol?

You should not take Cholecalciferol if you have had an allergic reaction to Cholecalciferol, or if you have high levels of calcium or Cholecalciferol in your body, or any condition that makes it hard for your body to absorb nutrients from food.

How should I take Cholecalciferol?

It may be best to take Cholecalciferol after a meal, but you may take this medicine with or without food.Measure liquid medicine carefully. Use the dosing syringe provided, or use a medicine dose-measuring device.The chewable tablet must be chewed before you swallow it.

What happens if I miss a dose?

Take Cholecalciferol as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose of Cholecalciferol?

Seek emergency medical attention2. An overdose of Cholecalciferol can cause serious or life-threatening side effects.Overdose symptoms may include nausea, loss of appetite, thirst, urinating more or less than usual, body aches, stiffness, confusion, or irregular heartbeats.

What happen If I stop taking Cholecalciferol?

Your doctor will likely advise you to stop taking Cholecalciferol supplements immediately. They may also recommend that you reduce the amount of calcium in your diet temporarily.

When should I take Cholecalciferol morning or night?

Many people prefer to take supplements such as Cholecalciferol first thing in the morning. Not only is it often more convenient, but it's also easier to remember your vitamins in the morning than later in the day.

Is Cholecalciferol good for my skin?

Cholecalciferol plays an integral role in skin protection and rejuvenation.

Can Cholecalciferol cause skin issues?

You may experience red, dry and itchy skin due to Cholecalciferol deficiency. Intake of Cholecalciferol can help you treat such skin problems. It can also reduce skin rashes.

Can Cholecalciferol causes my liver?

There is no evidence that Cholecalciferol causes injury to the liver.

Can Cholecalciferol affect my kidneys?

Cholecalciferol has been reported to have a wide range of benefits. However, a recent case study indicates that excessive use of Cholecalciferol can cause kidney damage in people who are not deficient in the vitamin.

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