Alpha D3 Product Introduction

Alpha D3 (Alfacalcidol) is an artificial synthesized pro-active vitamin D3, and is converted to 1,25-(OH) D3 by 25-hydroxylase in the liver. Because of the liver conversion process, Alpha D3 is more effective in maintaining a consistent higher circulating level of 1,25-(OH) D3, and exhibits a longer elimination half-time (T1/2) after the administration, but the therapy does not increase the risk of hypercalcemia.

Alpha D3 has a 25 years experience of the clinical application in the chronic renal failure patients. Extensive clinical researches indicate that it is safe and effective for the prevention of renal bone disease in the early stage of renal failure. Early administration of Alpha D3 can safely and beneficially alter the natural course of renal bone disease in patients with mild to moderate renal failure.

Alpha D3 is more flexible in administration. Routine therapy with Alpha D3 involving a daily small dosage by oral, and an intermittent therapy by oral or intravenously 2-3 times a week, both therapies have satisfactory effects. High-dose pulse therapy is highly effective and safely. In the meantime, the laboratory values for serum calcium and serum phosphate level remains constantly. There is no obvious change before and after the Alpha D3 treatment.

Alpha D3 is a highly potent agent that can control the hyperparathyroidism secondary to the chronic renal failure. Early administration is one of the most important method to prevent the renal bone disease.

Alpha D3 has a high safety and tolerance. It is easy to adjust the dosage according to the individual patient condition. Alpha D3 has the same clinical effect to Calcitriol, but the incidence of hypercalcemia is relatively lower.

Alpha D3

Composition
Alpha D3 Capsule
 Each soft gelatin capsule contains:
 Alfacalcidol (1 alpha -OH D3)  0.25mcg     or
1mcg

Character
 Transparent thickness fluid with colorless or a bit yellow, pick oval capsule for 0.25mcg and orange oval capsule for 1mcg.

Pharmacology and Toxicology
 1. Alfacalcidol increases intestinal absorption of calcium and phosphate, promotes bone mineralisation, decreases plasma parathyroid hormone levels as well as to decrease bone resorption, with relief of bone and muscle pain.
 2. Alfacalcidol induces osteoblastogenesis, the synthesis and activity of bone growth factors like TGF-beta, IGF-I, and thus bone formation.
 3. Alfacalcidol increases muscle strength and neuromuscular coordination, decrease balance disorders and risk of falls.

Pharmacokinetics
 Alfacalcidol undergoes rapid hepatic conversion to 1,25-dihydroxyvitamin D3 and also conversion by osteoblast. The peak of blood concentration of 1,25-(OH)2D3 appears after taking 17.6 hours (t1/2).

Indications
1. Rickets and osteomalacia
2. Renal bone disease (renal osteodystrophy)
3. Osteoporosis
4. Hypoparathyroidism

Dosage and Administration
 The dosage and administration of Alpha D3 can be adjusted from 0.25mcg/day to 1mcg/day.

Adverse Reactions
 Adverse effects generally are infrequent if dosage below 1mcg/day, in the case of high dosage or combination with calcium, maybe caused hypercalcaemia or hypercalciuria.

Contraindication
 Alfacalcidol should not be administered in patients with evidence of Vitamin D toxicity or known hepersensitivity to the effects of Vitamin D or hypercalcaemia.

Precaution
1. Alfacalcidol therapy requires regular monitoring of calcium, creatinine, blood urine nitrogen, calciuria, and urine creatinine and other appropriate biochemical parameters.
2. For young people, alfacalcidol only can be administrated in idiopathic juvenile osteoporosis and glucocorticoid-induced osteoporosis.
3. If hypercalcaemia occur, this can be corrected rapidly by stopping treatment with Alpha D3 until plasma calcium levels return to normal, usually in about a week. Alpha D3 may then be restarted at half the last dose used.

Use in Pregnancy and Breastfeeding
 There is insufficient evidence on which to assess the safety of alfacalcidol use during pregnancy.

Drug Interactions
1. Calcium: The risk of hypercalcaemia is increased in patients taking calcium-containing preparations with alfacalcidol.
2. Thiazide Diuretics: The risk of hypercalcaemia is increased since it enhances calcium absorption by kidney.
3. Digitalis: Hypercalcaemia in patients taking digitalis preparation may precipitate cardiac arrhythmias. Patients taking digitalis concurrently with alfacalcidol must therefore be closely monitored.
4. Barbiturates / Anticonvulsant: Patients on barbiturates or anticonvulsant may require an increased dose of Alpha D3 to produce the desired effect.
5. Drugs affecting intestine absorption: Absorption of alfacalcidol may be impaired by concurrent use of cholestyramine and large amounts of aluminium-based antacids.
6. Phosphate: The risk of hyperphosphatemia is increased in patients taking phosphate-containing preparations with alfacalcidol.

Package
(1) 0.25mcg/cap, 20caps/box
(2) 0.25mcg/cap, 10caps/box
(3) 1mcg/cap, 10caps/box

Storage
 Sealed, under cold condition

Period of Validity
 Three years

A Brief Introduction to TEVA