Peringatan Keamanan

There is a discrepancy across a number of reported LD50 values for alfacalcidol, which can be attributed to differences in the procedures used in laboratories. Oral LD50 in mice ranges from 440 to 490 mcg/kg. Intravenous in mice was 290 mcg/kg; however, another source presented 56 mcg/kg in female mice and 71 mcg/kg in male mice. Oral LD50 in rats ranges from 340 to 720 mcg/kg.L33284

In case of an acute accidental overdose following oral administration, emesis or gastric lavage can be induced to prevent further drug absorption. Mineral oil may be used to promote fecal drug elimination in instances where the drug was already absorbed in the stomach.L33284

Alfacalcidol overdose can lead to hypercalcemia, hypercalciuria, and hyperphosphatemia. Similarly, a high intake of calcium and phosphate concurrently with a therapeutic dose of alfacalcidol can result in those conditions.L33284 Hypercalcemia most commonly presents with headache, weakness, hypertension, somnolence, dizziness, sweating, anorexia, nausea, vomiting, diarrhea, constipation, polyuria, polydipsia and muscle and bone pain, and metallic taste.L33369 Hypercalcemia should be responded to with discontinuation of alfacalcidol, a low calcium diet and withdrawal of calcium supplements.L33284 Prolonged hypercalcemia can lead to nephrocalcinosis, nephrolithiasis, and reduced kidney function. In cases of severe hypercalcemia, general supportive measures are recommended, which may include forced diuresis and close monitoring of renal function, electrolytes, and electrocardiographs. Monitoring for abnormalities is especially critical in patients receiving digitalis glycosides. Management with glucocorticosteroids, loop diuretics, bisphosphonates, and calcitonin, as well as hemodialysis with low calcium content, may be considered.L33369

Alfacalcidol

DB01436

small molecule approved nutraceutical

Deskripsi

Alfacalcidol, or 1-alpha-hydroxycholecalciferol or 1-alpha-hydroxyvitamin D3, is a non-endogenous analogue of vitamin D.A234044 It plays an essential function in calcium homeostasis and bone metabolism. Alfacaldisol is activated by the enzyme 25-hydroxylase in the liver to mediate its effects in the body, or most importantly, the kidneys and bones. The pharmacological actions of alfacalcidol are prolonged than vitamin D because a negative feedback mechanism regulates the final activation step of vitamin D in the kidneys.A175348,A175351

Alfacalcidol is available in oral and intravenous formulations. In Canada, it is marketed as ONE-ALPHA, which manages hypocalcemia, secondary hyperparathyroidism, and osteodystrophy in adults with chronic renal failure.L33284 In approving European countries, alfacalcidol is also indicated for managing nutritional and malabsorptive rickets and osteomalacia, vitamin D-dependent rickets and osteomalacia, and hypophosphataemic vitamin D resistant rickets and osteomalacia.L33364,L33369

Struktur Molekul 2D

Berat 400.6371
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of alfacalcidol ranges from three to four hours.[L33284,L33369]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Alfacalcidol is absorbed passively and almost completely in the small intestine.L33369

Metabolisme

Alfacalcidol is rapidly converted in the liver to 1,25-dihydroxyvitamin D, which is essentially the metabolite of vitamin D that regulates calcium and phosphate metabolism. Alfacalcidol is further metabolized to other polar inactive metabolites, excreted primarily through the bile.L33369

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not affect the bioavailability.

Interaksi Obat

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

Target Protein

Vitamin D3 receptor VDR
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial CYP27B1
Retinoic acid receptor RXR-alpha RXRA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17438884
    Galesanu C, Ciubotariu C, Melnic G, Galesanu MR: Postmenopausal osteoporosis. Digital Rx radiogrammetry in the diagnosis and follow-up of treatment with alfacalcidol. Rev Med Chir Soc Med Nat Iasi. 2006 Oct-Dec;110(4):833-41.
  • PMID: 17668216
    Ringe JD, Schacht E: Improving the outcome of established therapies for osteoporosis by adding the active D-hormone analog alfacalcidol. Rheumatol Int. 2007 Dec;28(2):103-11. doi: 10.1007/s00296-007-0422-6. Epub 2007 Aug 1.
  • PMID: 23713871
    Vervloet M: Clinical uses of 1-alpha-hydroxycholecalciferol. Curr Vasc Pharmacol. 2014 Mar;12(2):300-5. doi: 10.2174/15701611113119990132.
  • PMID: 15977462
    Richy F, Deroisy R, Lecart MP, Hanssens L, Mawet A, Reginster JY: D-hormone analog alfacalcidol: an update on its role in post-menopausal osteoporosis and rheumatoid arthritis management. Aging Clin Exp Res. 2005 Apr;17(2):133-42. doi: 10.1007/BF03324586.
  • PMID: 10780869
    Shiraishi A, Takeda S, Masaki T, Higuchi Y, Uchiyama Y, Kubodera N, Sato K, Ikeda K, Nakamura T, Matsumoto T, Ogata E: Alfacalcidol inhibits bone resorption and stimulates formation in an ovariectomized rat model of osteoporosis: distinct actions from estrogen. J Bone Miner Res. 2000 Apr;15(4):770-9. doi: 10.1359/jbmr.2000.15.4.770.
  • PMID: 10485984
    Shiraishi A, Higashi S, Ohkawa H, Kubodera N, Hirasawa T, Ezawa I, Ikeda K, Ogata E: The advantage of alfacalcidol over vitamin D in the treatment of osteoporosis. Calcif Tissue Int. 1999 Oct;65(4):311-6. doi: 10.1007/s002239900704.
  • PMID: 18979152
    O'Donnell S, Moher D, Thomas K, Hanley DA, Cranney A: Systematic review of the benefits and harms of calcitriol and alfacalcidol for fractures and falls. J Bone Miner Metab. 2008;26(6):531-42. doi: 10.1007/s00774-008-0868-y. Epub 2008 Nov 1.
  • PMID: 16172518
    Schacht E, Richy F, Reginster JY: The therapeutic effects of alfacalcidol on bone strength, muscle metabolism and prevention of falls and fractures. J Musculoskelet Neuronal Interact. 2005 Jul-Sep;5(3):273-84.

Contoh Produk & Brand

Produk: 10 • International brands: 2
Produk
  • Alfacalcidol Capsules
    Capsule • 0.25 mcg • Oral • Canada • Approved
  • Alfacalcidol Capsules
    Capsule • 1 mcg • Oral • Canada • Approved
  • One-alpha
    Solution / drops • 2 mcg / mL • Oral • Canada • Approved
  • One-alpha
    Solution • 2 mcg / mL • Intravenous • Canada • Approved
  • One-alpha
    Capsule • 0.25 mcg • Oral • Canada • Approved
  • One-alpha
    Capsule • 1 mcg • Oral • Canada • Approved
  • One-alpha
    Capsule • 0.5 mcg • Oral • Canada • Approved
  • One-alpha Sol 0.2mcg/ml
    Liquid • .2 mcg / mL • Oral • Canada • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Alsiodol
  • One Alpha

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