ChemicalBook > Product Catalog > API > Vitamins and Minerals medicines > Vitamins AD drugs > Alfacalcidol
Basic information Description Physical and Chemical Properties Pharmacological effects Pharmacodynamics Indications Instructions Adverse reactions Precautions Drug Interactions Uses Referrence Safety Related Supplier
Alfacalcidol Chemical Properties
- Melting point:134-136°C
- Boiling point:531.5±50.0 °C(Predicted)
- Density 1.01±0.1 g/cm3(Predicted)
- storage temp. −20°C
- solubility Practically insoluble in water, freely soluble in ethanol (96 per cent), soluble in fatty oils.
- form White crystalline solid
- λmax264nm(Diethyl ether)(lit.)
- Merck 14,4819
- CAS DataBase Reference41294-56-8(CAS DataBase Reference)
- EPA Substance Registry SystemAlphacalcidol (41294-56-8)
Alfacalcidol Usage And Synthesis
- DescriptionAlfacalcidol is a vitamin D analog. It is important for the regulation of the bone metabolism. Alfacaldidol is a regulator of calcium and phosphorus metabolism, which helps calcium and phosphorus to be absorbed more effectively in the intestines. Thus, alfacalcidol is used to treat renal (kidney) bone diseases, rickets, osteoporosis, and patients with high or low activity of the parathyroid gland. Also, it is used to maintain normal calcium levels within the body. Alfacalcidol has significant effects on the immune system, including regulatory T cells. Alfacalcidol is furthermore used as a poultry feed additive to prevent tibial dyschondroplasia and increases phytate bioavailability.
- Physical and Chemical PropertiesWhite crystal or crystalline powder, insoluble in water and hexane, soluble in methanol, ethanol, chloroform, methylene chloride, acetone or ether. Perishable in case of air and light .
- Pharmacological effectsAlfacalcidol is quickly converted by the liver into 1,25-dihydroxyvitamin D3, regulates calcium balance in the body, because of the enhancing of 1,25-dihydroxyvitamin D3 levels in vivo circulating , thereby increases the calcium and phosphorus intestinal absorption, promotes bone mineralization, decreases parathyroid hormone levels in plasma and reduces calcium resorption, relieves bone, muscle pain and improves osteoporosis and menopause, aging and steroid-induced intestinal related calcium malabsorption.
Alfacalcidol increases the intestinal and renal tubular reabsorption of calcium and inhibit parathyroid hyperplasia, reduces parathyroid hormone synthesis and release, inhibits bone resorption. Promotes collagen and bone matrix protein synthesis.Regulates Calcium metabolism of muscles , promotes muscle cells differentiation, enhances muscle strength, increases neuromuscular coordination, tends to reduce falls. Suitable for the treatment of rickets and osteomalacia, renal osteodystrophy, osteoporosis and hypoparathyroidism. Youth are limited to young people with idiopathic osteoporosis and glucocorticoid-induced osteoporosis too.
The above information is edited by the chemicalbook of Tian Ye.
- Pharmacodynamics This product after oral administration, is rapidly absorbed into the bloodstream from the gut, 25-hydroxy enzyme of the liver microsomal make 25-hydroxy of side chain compound to generate 1α, 25-(OH) 2D3, distributed in the intestine and bone and other target tissues, upon binding to the receptor, it can promote intestinal absorption of calcium, causing a series of physiological activities, such as bone salt dissolving and bone formation . Rats removed of the kidney and rats deficient in vitamin D, are given this product experiments, which shows that the level of promoting intestinal absorption of calcium, elevates serum calcium.Due to renal completely removed in rats removed of the kidney , the majority of bone resorption and bone-like cavity layer, low-calcified layer next layer increases, give this product 30d to experiment, the bone freshmen is observed. Therefore alfacalcidol promotes bone formation. Elderly patients with osteoporosis given this product ,iliac bone biopsy is performed by electronic and optical microscope to find that active osteoblasts, osteocytes, bone calcification small chamber increases, improves bone tissue.
- IndicationsSymptoms alfacalcidol can be used to improve chronic renal insufficiency, hypoparathyroidism, vitamin D-dependent rickets, a softening of bone disease caused by vitamin D metabolism, such as hypocalcemia, hand, foot cramps, pain , bone disease and osteoporosis embolism.
- Instructions For osteoporosis, oral: initial amount of 0.5μg/d, maintenance dose of 0.25~0.50μg, qd.
Dialysis patients with chronic hypocalcemia, 0.5~3.0μg/d, divided 2 to 3 times daily.
Hypoparathyroidism, 0.25~3.00μg/d, divided 2 to 3 times daily.
Renal bone atrophy, the next day 0.25~3.00μg, divided 2 to 3 times daily.
Vitamin D-dependent rickets, 1μg/d, divided 2 to 3 times daily.
Familial hypophosphatemia, 2μg/d, divided 2 to 3 times daily.
- Adverse reactions Small amount alone is usually no more adverse reactions, long-term large doses of medication or in combination with calcium can cause hypercalcemia and hypercalciuria.patients in Long-term high doses and patients with renal impairment may be nausea, loss of appetite, dizziness, skin itching, rash, constipation, anorexia, vomiting, abdominal pain, high calcium signs ,it can be restored to normal after treatment. Vitamin D and its analogues allergies, hypercalcemia, vitamin D poisoning signs patients are banned. Early medication serum calcium levels should be determined weekly, when a stable dose, they are measured every 2 to 4 weeks, especially renal dysfunction serum calcium levels should be measured regularly. when hypercalcemia occurs, It Shall be discontinued and deal with hypercalcemia. After serum calcium returns to normal , the dose is dministered half of the last dose. Alfacalcidol combination with calcium can cause elevated serum calcium, when it combined with thiazide diuretics can cause the danger of hypercalcemia . When treated with digitalis drugs, care should be taken to develop the amount of this drug.The amount of Alfacalcidol should be increased when combined with barbiturates, anticonvulsants .
- Precautions If hypercalcemia occurs,it should be stopped taking until serum calcium returns to normal (about a week), and then press the last half dose administration. patients have Vitamin D symptoms or known allergy to vitamin D and its analogues is unfit for use. Patients Should avoid taking vitamin D drugs at the same time, so as not to cause vitamin D intoxication.
- Drug InteractionsUsing Alfacalcidol and magnesium formulation (magnesium oxide, magnesium carbonate, etc.) sometimes causes hypermagnesemia.
Using Alfacalcidol and Cardiac preparations may cause cardiac arrhythmia.
Using Alfacalcidol and vitamin D and its derivatives (calcitriol) , it is possible to cause hypercalcemia.
Using Alfacalcidol and calcium , Thiazide diuretics, digitalis drugs , can cause hypercalcemia.
And barbiturates, anti-seizure drugs may reduce the efficacy of the drug.
Gastrointestinal absorption inhibitors can reduce the absorption of the drug.
Combination with large doseas of Phosphorus compounds, can induce hyperphosphatemia.
When Alfacalcidol and calcium preparations (calcium lactate, calcium carbonate, etc.) are used together, there may be hypercalcemia.
- UsesFor the treatment of osteoporosis, vitamin D-dependent rickets and osteomalacia
- JD Ringe, H Faber, P Fahramand, E Schacht, Alfacalcidol versus plain vitamin D in the treatment of glucocorticoid/inflammation-induced osteoporosis, J. Rheumatol. Suppl., 2005, vol. 76, 33-40
- Chemical PropertiesWhite Solid
- UsesA synthetic analog of Calcitiol (the hormonal form of vitamin D3), which shows identical potency with respect to stimulation of intestinal calcium absorption and bone mineral mobilization. Vitamin D source
- DefinitionChEBI: A member of the class of D3 vitamins that is calciol in which the hydrogen at the 1alpha position is replaced by a hydroxy group. It is an active metabolite of cholecalciferol, which performs important functions in reg lation of the calcium balance and the bone metabolism.
- Methimazole Calcitonin salmon Alfuzosin Vitamin D3 ALFACALCIDOL - REFERENCE SPECTRUM Alfacalcidol-d7,Oxydevit-d7 Alfacalcidol,Vitamin ALFUZOSIN IMPURITY A Methyl cyclopentenolone 1,3-Cyclopentadiene Vitamin D2 Paricalcitol Alfacalcidol Calcitriol METHYLCYCLOPENTADIENE DIMER Diethylstilbestrol Allyloxypolyethyleneglycol 1,3-CYCLOOCTADIENE
- Company Name:Chemvon Biotechnology Co., Ltd Gold
- Company Name:Pure Chemistry Scientific Inc. Gold
- Tel:001-857-928-2050 or 1-888-588-9418
- Company Name:Hydragon Pharma Ltd Gold
- Company Name:Zhengzhou Kangshan Biological Co., Ltd. Gold
- Company Name:Shaanxi kelkai Pharmaceutical Technology Co., Ltd Gold