Peringatan Keamanan

The reported LD50 for orally administered ergocalciferol in the rat is of 10 mg/kg.MSDS Overdosage with this agent is reported to produce hypervitaminosis characterized by hypercalcemia, renal impairment, calcification of soft tissues, a decline in the rate of linear growth and increase in bone mineralization.L6094

Once an overdose state is registered, immediate withdrawal of vitamin D is required along with a calcium diet, generous intake of fluids and symptomatic treatment. The administration of loop diuretics is an option to increase renal calcium excretion. On the other hand, dialysis and administration of citrates, sulfates, phosphates, corticosteroids, EDTA and mithramycin are recommended.L6094

There haven't been long term studies analyzing the carcinogenic and mutagenic potential of ergocalciferol or its effects in fertility.

Ergocalciferol

DB00153

small molecule approved nutraceutical

Deskripsi

Ergocalciferol is an inactivated vitamin D analog.A177526 It is synthesized by some plants in the presence of UVB light.T577 The production of ergocalciferol was prompted by the identification of dietary deficiency, more specifically vitamin D, as the main causative factor for the development of rickets. Ergocalciferol was isolated for the first time from yeast in 1931 and its structure was elucidated in 1932.T580

Ergocalciferol is considered the first vitamin D analog and is differentiated from cholecalciferol by the presence of a double bond between C22 and C23 and the presence of a methyl group at C24. These modifications reduce the affinity of ergocalciferol for the vitamin D binding protein resulting in faster clearance, limits its activation, and alters its catabolism.A177637

The first approved product containing ergocalciferol under the FDA records was developed by US Pharm Holdings and was FDA approved in 1941.L6058

Struktur Molekul 2D

Berat 396.6484
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ergocalciferol can be found circulation for 1-2 days. This quick turnover is presented due to hepatic conversion and uptake by fat and muscle cells where it is transformed to the active form.[T577]
Volume Distribusi The amount of circulating ergocalciferol is very limited as this compound is rapidly stored in fat tissue such as adipose tissue, liver and muscle. This is very obvious in reports that indicate that circulating ergocalciferol is significantly reduced in obese patients.[T577]
Klirens (Clearance) There are no formal reports regarding the clearance rate of ergocalciferol. Due to the structural similarity, it is recommended to consult this parameter with [cholecalciferol]. On the other hand, the proposed renal clearance of calcitriol is of 31 ml/min.[T140]

Absorpsi

Ergocalciferol is absorbed in the intestine and carried to the liver in chylomicrons. Its intestinal absorption does not present limitations unless the presence of conditions related to fat malabsorption.T577 However, for absorption to take place, the presence of bile is required.L6088

Metabolisme

Ergocalciferol is inactive and hence, the first step in the body is ruled by the conversion of this parent compound to 25-hydroxyvitamin D by the action of CYP2R1 followed by the generation of the major circulating metabolite, 1,25-dihydroxyvitamin D or calcitrol.T577 The generation of this major metabolite is ruled by the activity of CYP27B1 which is a key 1-hydroxylase and CYP24A1 which is responsible for the 25-hydroxylation.A177637 As part of the minor metabolism, ergocalciferol is transformed into 25-hydroxyvitamin D in the liver by the activity of D-25-hydroxylase and CYP2R1. As well, the formation of 24(R),25dihydroxyvitamin D is performed mainly in the kidneys by the action of 25-(OH)D-1-hydroxylase and 25-(OH)D-24-hydroxylase.T580 Additionally, there are reports indicating significant activity of 3-epimerase in the metabolism of ergocalciferol which modifies the hydroxy group in C3 from the alpha position to a beta. The epimers formed seemed to have a reduced affinity for the vitamin D plasma proteins and to the vitamin D receptor.A177637 An alternative activation metabolic pathway has been reported and this process is characterized by the activity of CYP11A1 and its hydroxylation in the C-20. This 20-hydroxylated vitamin D seems to have similar biological activity than calcitriol.A177637

Rute Eliminasi

The active form of ergocalciferol, calcitrol, cannot be maintained for long periods in storage tissue mainly in periods of dietary or UVB deprivation.T577 Therefore, ergocalciferol and its metabolites are excreted via the bile with a minor contribution of renal elimination. This major fecal elimination is explained due to the cubilin-megalin receptor system-mediated renal reuptake of vitamin D metabolites bound to vitamin D binding protein.L6091

Interaksi Obat

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

Target Protein

Vitamin D3 receptor VDR
Voltage-dependent calcium channel CACNG1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23735861
    Porter A, Gilmartin C, Srisakul U, Arruda J, Akkina S: Prevalence of 25-OH vitamin D deficiency in a population of hemodialysis patients and efficacy of an oral ergocalciferol supplementation regimen. Am J Nephrol. 2013;37(6):568-74. doi: 10.1159/000351185. Epub 2013 May 30.
  • PMID: 24719588
    Lee JY, So TY, Thackray J: A review on vitamin d deficiency treatment in pediatric patients. J Pediatr Pharmacol Ther. 2013 Oct;18(4):277-91. doi: 10.5863/1551-6776-18.4.277.
  • PMID: 29080648
    Gallagher JC, Bikle DD: Vitamin D: Mechanisms of Action and Clinical Applications. Endocrinol Metab Clin North Am. 2017 Dec;46(4):xvii-xviii. doi: 10.1016/j.ecl.2017.09.001. Epub 2017 Sep 28.
  • PMID: 20662333
    Sahay M, Sahay RK: Refractory rickets in the tropics. J Pediatr Endocrinol Metab. 2010 Jun;23(6):597-601.
  • PMID: 27940098
    Hymoller L, Jensen SK: Plasma transport of ergocalciferol and cholecalciferol and their 25-hydroxylated metabolites in dairy cows. Domest Anim Endocrinol. 2017 Apr;59:44-52. doi: 10.1016/j.domaniend.2016.11.002. Epub 2016 Nov 16.
Textbook
  • ISBN: 978-012-374118-9
    Coulston A. and Boushey C. (2008). Nutrition in the Prevention and Treatment of Disease (2nd ed.). Academic Press.
  • ISBN: 978-0-8493-9771-4
    Eitenmiller R., Ye L. and Landen W. (2008). Vitamin analysis for the health and food sciences (2nd ed.). Taylor and Francis.
  • ISBN: 978-1-4612-9793-2
    Rajiv Kumar (1984). Vitamin D: Basic and Clinical Aspects. Martinus Nijhoff Publishing.
  • Speeckaert M., Speeckaert R., Geel N. and Delanghe J. (2014). Advances in Clinical Chemistry. Elsevier.

Contoh Produk & Brand

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Menampilkan 8 dari 164 produk.
International Brands
  • Deltalin — Lilly

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