Alendon-10 (alendronate sodium) tablets 10 mg. №30

Description

Composition

active substance:  sodium alendronate; 1 tablet contains sodium alendronate equivalent to alendronic acid 10 mg or 70 mg;

excipients:  microcrystalline cellulose, corn starch, magnesium stearate, sodium starch glycolate (type A), povidone (K 30).

Pharmacotherapeutic group

drugs affecting the structure and mineralization of bones.

ATX code M05V A04.

Pharmacological properties

Pharmacodynamics.

Alendronate sodium belongs to the group of aminobisphosphonates. It is a synthetic analog of natural pyrophosphate. Suppresses the precipitation of calcium phosphate, blocks its transformation into hydroxyapatite, delays the aggregation of apatite crystals with the formation of larger crystals, and accelerates the reverse dissolution of these crystals. The selective action is due to the high affinity of bisphosphonates with the mineral components of bones. Acts as an effective non-hormonal specific inhibitor of osteoclast-mediated bone resorption. The exact mechanisms of this process have not been fully elucidated. Restores a positive balance between bone resorption and restoration. Increases the mineral density of the bones of the spine, pelvis, etc., promotes the formation of bone tissue with a normal histological structure. Prevents the appearance of new bone fractures. Reduces the level of calcium in the blood serum by inhibiting bone resorption and reducing the release of calcium from bone tissue. The calcium-lowering effect of the drug, mediated by inhibition of osteoclasts, is observed after 1-2 days.

Pharmacokinetics. 

Alendronate sodium is absorbed in the gastrointestinal tract by 25%. Absolute bioavailability for tablets (from 5 to 10 mg) taken on an empty stomach 2 hours before a meal is 0.64% (for women) and 0.59% (for men). Bioavailability decreases (by approximately 40%) when alendronate is taken half an hour to an hour before the usual breakfast. The bioavailability of alendronate is negligible when it is taken with food or within two hours after a meal. Combined intake of alendronate with drinks (including mineral water, coffee, orange juice) reduces its bioavailability by 60%. Studies conducted on laboratory rats have shown that when administered intravenously at a dose of 1 mg/kg, alendronate is temporarily distributed in soft tissues, but then quickly redistributes. Half of the absorbed dose is excreted mainly by the kidneys in an unchanged form within 72 hours, and the rest accumulates in bone tissue for a long time, is eliminated very slowly due to binding with bone tissue. The half-life of alendronate from bone is several years.

Approximately 78% of alendronate binds to blood plasma proteins and is not metabolized. The concentration of the drug in blood plasma is insignificant (less than 5 ng/ml) and decreases by 95% within 6 hours after intravenous infusion.

After a single internal administration of 10 mg of alendronate, its renal clearance was 71 ml/min, and systemic clearance did not exceed 200 ml/min.

Indication

For alendronate sodium tablets of 10 mg.

• Treatment and prevention of osteoporosis in postmenopausal women to prevent fractures, including hip and spine fractures (compression fractures).
• Treatment of osteoporosis in men to prevent fractures.
• Treatment and prevention of glucocorticoid osteoporosis.

For alendronate sodium tablets of 70 mg.

Treatment of postmenopausal osteoporosis. The drug reduces the risk of vertebral and hip fractures.

Contraindication

• Hypersensitivity to alendronate sodium or any other component of the drug;
• inability to stand or sit straight within 30 minutes after taking the drug; hypocalcemia;
• lesions of the esophagus that complicate peristalsis, such as strictures or achalasia of the esophagus;
• severe renal failure (creatinine clearance < 35 ml/min);
• simultaneous use of other bisphosphonates.