Peringatan Keamanan

Chronic or acute administration of excessive doses of cholecalciferol may lead to hypervitaminosis D, manifested by hypercalcemia and its sequelae F4027, F4042, F4048. Early symptoms of hypercalcemia may include weakness, fatigue, somnolence, headache, anorexia, dry mouth, metallic taste, nausea, vomiting, vertigo, tinnitus, ataxia, and hypotonia F4027, F4042, F4048. 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 F4027, F4042, F4048.

Safety of doses in excess of 400 IU (10mcg) of vitamin D3 daily during pregnancy has not been established F4027, F4042, F4048. 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 F4027, F4042, F4048. Hypercalcemia during pregnancy may also lead to suppression of parathyroid hormone release in the neonate, resulting in hypocalcemia, tetany, and seizures F4027, F4042, F4048.

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.

Cholecalciferol

DB00169

small molecule approved nutraceutical

Deskripsi

Vitamin D, in general, is a secosteroid generated in the skin when 7-dehydrocholesterol located there interacts with ultraviolet irradiation - like that commonly found in sunlight L5689. Both the endogenous form of vitamin D (that results from 7-dehydrocholesterol transformation), vitamin D3 (cholecalciferol), and the plant-derived form, vitamin D2 (ergocalciferol), are considered the main forms of vitamin d and are found in various types of food for daily intake L5689. Structurally, ergocalciferol differs from cholecalciferol in that it possesses a double bond between C22 and C23 and has an additional methyl group at C24 L5689. Finally, ergocalciferol is pharmacologically less potent than cholecalciferol, which makes vitamin D3 the preferred agent for medical use L5689.

Appropriate levels of vitamin D must be upheld in the body in order to maintain calcium and phosphorus levels in a healthy physiologic range to sustain a variety of metabolic functions, transcription regulation, and bone metabolism A223, L5689, L1782, L5771, F4027, F4042, F4048. However, studies are also ongoing to determine whether or not cholecalciferol may also play certain roles in cancer, autoimmune disorders, cardiovascular disease, and other medical conditions that may be associated with vitamin D deficiency L5689.

Struktur Molekul 2D

Berat 384.6377
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) At this time, there have been resources that document the half-life of cholecalciferol as being about 50 days [T527] 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 [L1782]. 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 [A32185].
Volume Distribusi 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 [A176417].
Klirens (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 [A176417].

Absorpsi

Cholecalciferol is readily absorbed from the small intestine if fat absorption is normal F4027, F4042, F4048. Moreover, bile is necessary for absorption as well F4027, F4042, F4048. 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 A176447.

Metabolisme

Within the liver, cholecalciferol is hydroxylated to calcifediol (25-hydroxycholecalciferol) by the enzyme vitamin D-25-hydroxylase F4027, F4042, F4048. At the kidney, calcifediol subsequently serves as a substrate for 1-alpha-hydroxylase, yielding calcitriol (1,25-dihydroxycholecalciferol), the biologically active form of vitamin D3 F4027, F4042, F4048.

Rute Eliminasi

It has been observed that administered cholecalciferol and its metabolites are excreted primarily in the bile and feces T527.

Interaksi Obat

475 Data
Aluminum hydroxide The serum concentration of Aluminum hydroxide can be increased when it is combined with Cholecalciferol.
Danazol Danazol may increase the hypercalcemic activities of Cholecalciferol.
Sucralfate The serum concentration of Sucralfate can be increased when it is combined with Cholecalciferol.
Orlistat Orlistat can cause a decrease in the absorption of Cholecalciferol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Cholecalciferol.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Cholecalciferol.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Cholecalciferol.
Magnesium salicylate The serum concentration of Magnesium salicylate can be increased when it is combined with Cholecalciferol.
Magaldrate The serum concentration of Magaldrate can be increased when it is combined with Cholecalciferol.
Magnesium hydroxide The serum concentration of Magnesium hydroxide can be increased when it is combined with Cholecalciferol.
Magnesium trisilicate The serum concentration of Magnesium trisilicate can be increased when it is combined with Cholecalciferol.
Magnesium chloride The serum concentration of Magnesium chloride can be increased when it is combined with Cholecalciferol.
Magnesium carbonate The serum concentration of Magnesium carbonate can be increased when it is combined with Cholecalciferol.
Talc The serum concentration of Talc can be increased when it is combined with Cholecalciferol.
Magnesium silicate The serum concentration of Magnesium silicate can be increased when it is combined with Cholecalciferol.
Hydrotalcite The serum concentration of Hydrotalcite can be increased when it is combined with Cholecalciferol.
Magnesium aspartate The serum concentration of Magnesium aspartate can be increased when it is combined with Cholecalciferol.
Magnesium peroxide The serum concentration of Magnesium peroxide can be increased when it is combined with Cholecalciferol.
Magnesium orotate The serum concentration of Magnesium orotate can be increased when it is combined with Cholecalciferol.
Magnesium levulinate The serum concentration of Magnesium levulinate can be increased when it is combined with Cholecalciferol.
Magnesium lactate The serum concentration of Magnesium lactate can be increased when it is combined with Cholecalciferol.
Digoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Digoxin.
Acetyldigitoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Acetyldigitoxin.
Deslanoside The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Deslanoside.
Ouabain The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Ouabain.
Oleandrin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Oleandrin.
Cymarin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Cymarin.
Proscillaridin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Proscillaridin.
Metildigoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Metildigoxin.
Lanatoside C The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Lanatoside C.
Gitoformate The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Gitoformate.
Acetyldigoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Acetyldigoxin.
Peruvoside The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Peruvoside.
Digitoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Cholecalciferol is combined with Digitoxin.
Mineral oil Mineral oil can cause a decrease in the absorption of Cholecalciferol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methyclothiazide The risk or severity of hypercalcemia can be increased when Methyclothiazide is combined with Cholecalciferol.
Bendroflumethiazide The risk or severity of hypercalcemia can be increased when Bendroflumethiazide is combined with Cholecalciferol.
Benzthiazide The risk or severity of hypercalcemia can be increased when Benzthiazide is combined with Cholecalciferol.
Cyclothiazide The risk or severity of hypercalcemia can be increased when Cyclothiazide is combined with Cholecalciferol.
Hydroflumethiazide The risk or severity of hypercalcemia can be increased when Hydroflumethiazide is combined with Cholecalciferol.
Chlorothiazide The risk or severity of hypercalcemia can be increased when Chlorothiazide is combined with Cholecalciferol.
Hydrochlorothiazide The risk or severity of hypercalcemia can be increased when Hydrochlorothiazide is combined with Cholecalciferol.
Trichlormethiazide The risk or severity of hypercalcemia can be increased when Trichlormethiazide is combined with Cholecalciferol.
Polythiazide The risk or severity of hypercalcemia can be increased when Polythiazide is combined with Cholecalciferol.
Mebutizide The risk or severity of hypercalcemia can be increased when Mebutizide is combined with Cholecalciferol.
Cyclopenthiazide The risk or severity of hypercalcemia can be increased when Cyclopenthiazide is combined with Cholecalciferol.
Buthiazide The risk or severity of hypercalcemia can be increased when Buthiazide is combined with Cholecalciferol.
Calcitriol The risk or severity of adverse effects can be increased when Calcitriol is combined with Cholecalciferol.
Calcifediol The risk or severity of adverse effects can be increased when Calcifediol is combined with Cholecalciferol.
Ergocalciferol The risk or severity of adverse effects can be increased when Ergocalciferol is combined with Cholecalciferol.
Paricalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Paricalcitol.
Dihydrotachysterol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Dihydrotachysterol.
Alfacalcidol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Alfacalcidol.
Seocalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Seocalcitol.
Inecalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Inecalcitol.
Becocalcidiol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Becocalcidiol.
Eldecalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Eldecalcitol.
1alpha,24S-Dihydroxyvitamin D2 The risk or severity of adverse effects can be increased when Cholecalciferol is combined with 1alpha,24S-Dihydroxyvitamin D2.
Elocalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Elocalcitol.
Maxacalcitol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Maxacalcitol.
Doxercalciferol The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Doxercalciferol.
1alpha-Hydroxyvitamin D5 The risk or severity of adverse effects can be increased when Cholecalciferol is combined with 1alpha-Hydroxyvitamin D5.
Previtamin D(3) The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Previtamin D(3).
Calcium acetate The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium acetate.
Calcium glucoheptonate The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium glucoheptonate.
Calcium glubionate anhydrous The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium glubionate anhydrous.
Calcium pangamate The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium pangamate.
Calcium levulinate The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium levulinate.
Calcium cation The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium cation.
Calcium polycarbophil The risk or severity of adverse effects can be increased when Cholecalciferol is combined with Calcium polycarbophil.
Colestipol The serum concentration of Cholecalciferol can be decreased when it is combined with Colestipol.
Sevelamer The serum concentration of Cholecalciferol can be decreased when it is combined with Sevelamer.
Colesevelam The serum concentration of Cholecalciferol can be decreased when it is combined with Colesevelam.
Cholestyramine The serum concentration of Cholecalciferol can be decreased when it is combined with Cholestyramine.
Tixocortol The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Tixocortol.
Fluocortin The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluocortin.
Fluperolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluperolone.
Fluclorolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluclorolone.
Flunisolide The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Flunisolide.
Beclomethasone dipropionate The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Beclomethasone dipropionate.
Betamethasone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Betamethasone.
Fluticasone propionate The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluticasone propionate.
Fluocinolone acetonide The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluocinolone acetonide.
Triamcinolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Triamcinolone.
Prednisone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Prednisone.
Fludrocortisone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fludrocortisone.
Hydrocortisone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Hydrocortisone.
Prednisolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Prednisolone.
Methylprednisolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Methylprednisolone.
Trilostane The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Trilostane.
Budesonide The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Budesonide.
Dexamethasone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Dexamethasone.
Corticotropin The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Corticotropin.
Cortisone acetate The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Cortisone acetate.
Paramethasone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Paramethasone.
Aldosterone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Aldosterone.
Fluticasone furoate The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluticasone furoate.
Fluprednidene The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluprednidene.
Fluprednisolone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Fluprednisolone.
Meprednisone The therapeutic efficacy of Cholecalciferol can be decreased when used in combination with Meprednisone.

Target Protein

Vitamin D3 receptor VDR

Referensi & Sumber

Synthesis reference: Jean Jolly, Primo Rizzi, Jean Taillardat, "1.alpha.,25.alpha.-Dihydroxy-cholecalciferol and methods for the production thereof." U.S. Patent US4435325, issued May, 1977.
Artikel (PubMed)
  • PMID: 15531486
    Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91.
  • PMID: 28346348
    Jean G, Souberbielle JC, Chazot C: Vitamin D in Chronic Kidney Disease and Dialysis Patients. Nutrients. 2017 Mar 25;9(4). pii: nu9040328. doi: 10.3390/nu9040328.
  • PMID: 19803923
    Heaney RP: Alendronate plus cholecalciferol for the treatment of osteoporosis. Womens Health (Lond). 2006 Jan;2(1):23-7. doi: 10.2217/17455057.2.1.23.
  • PMID: 15585789
    DeLuca HF: Overview of general physiologic features and functions of vitamin D. Am J Clin Nutr. 2004 Dec;80(6 Suppl):1689S-96S.
  • PMID: 22936122
    Benaboud S, Urien S, Thervet E, Prie D, Legendre C, Souberbielle JC, Hirt D, Friedlander G, Treluyer JM, Courbebaisse M: Determination of optimal cholecalciferol treatment in renal transplant recipients using a population pharmacokinetic approach. Eur J Clin Pharmacol. 2013 Mar;69(3):499-506. doi: 10.1007/s00228-012-1378-3. Epub 2012 Aug 31.
  • PMID: 24885631
    Jones KS, Assar S, Harnpanich D, Bouillon R, Lambrechts D, Prentice A, Schoenmakers I: 25(OH)D2 half-life is shorter than 25(OH)D3 half-life and is influenced by DBP concentration and genotype. J Clin Endocrinol Metab. 2014 Sep;99(9):3373-81. doi: 10.1210/jc.2014-1714. Epub 2014 Jun 2.
  • PMID: 24915331
    Borel P, Caillaud D, Cano NJ: Vitamin D bioavailability: state of the art. Crit Rev Food Sci Nutr. 2015;55(9):1193-205. doi: 10.1080/10408398.2012.688897.
Textbook
  • ISBN: 0429863632
    Caroline Ashley, Aileen Dunleavy (2018). The Renal Drug Handbook: The Ultimate Prescribing Guide for Renal Practitioners, 5th Edition (5th ed.). CRC Press.

Contoh Produk & Brand

Produk: 1005 • International brands: 4
Produk
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    Tablet • - • Oral • US
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    Tablet • - • Oral • Canada • OTC • Approved
  • Acti-cal/mag 2:1 + Zinc and D Caplet
    Tablet • - • Oral • Canada • OTC • Approved
  • Actical Plus Calcium-magnesium-vitamin D3-silicon Chewable
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Menampilkan 8 dari 1005 produk.
International Brands
  • Delta-D
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  • Optimal-D — RV Nutritional, LLC
  • Vigantol

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