Overview
11 DESCRIPTION BINOSTO (alendronate sodium) is a bisphosphonate that acts as a specific inhibitor of osteoclast-mediated bone resorption. Bisphosphonates are synthetic analogs of pyrophosphate that bind to the hydroxyapatite found in bone. Alendronate sodium is chemically described as (4 amino-1-hydroxybutylidene) bisphosphonic acid, monosodium salt, trihydrate.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Animal studies have indicated the following mode of action. At the cellular level, alendronate shows preferential localization to sites of bone resorption, specifically under osteoclasts. The osteoclasts adhere normally to the bone surface but lack the ruffled border that is indicative of active resorption. Alendronate does not interfere with osteoclast recruitment or attachment, but it does inhibit osteoclast activity. Studies in mice on the localization of radioactive [ 3 H]alendronate in bone showed about 10-fold higher uptake on osteoclast surfaces than on osteoblast surfaces.
Indications
- 1 INDICATIONS AND USAGE BINOSTO is a bisphosphonate indicated for: Treatment of osteoporosis in postmenopausal women ( 1.1 ) Treatment to increase bone mass in men with osteoporosis ( 1.2 ) Limitation of use: Optimal duration of use has not been determined. For patients at low-risk for fracture, consider drug discontinuation after 3 to 5 years of use ( 1.3 ) 1.1 Treatment of Osteoporosis in Postmenopausal Women BINOSTO effervescent tablet 70 mg is indicated for the treatment of osteoporosis in postmenopausal women.
Common Doses
- 70 mg
Dosage
2 DOSAGE AND ADMINISTRATION 70 mg BINOSTO effervescent tablet once weekly. ( 2.1 , 2.2 ) Instruct patients to: ( 2.3 ) Dissolve one tablet of BINOSTO in approximately half a glass of plain room temperature water (4 oz). Wait at least 5 minutes after the effervescence stops, stir the solution for approximately 10 seconds and consume contents. Swallow solution at least 30 minutes before the first food, beverage, or medication of the day. Avoid lying down for at least 30 minutes after taking BINOSTO and until after the first food of the day. 2.
Contraindications
- 4 CONTRAINDICATIONS BINOSTO is contraindicated in patients with the following conditions: Abnormalities of the esophagus which delay esophageal emptying such as stricture or achalasia [see Warnings and Precautions (5.1) ] Inability to stand or sit upright for at least 30 minutes [see Dosage and Administration (2.3) ; Warnings and Precautions (5.1) ] Do not administer BINOSTO to patients at increased risk of aspiration Hypocalcemia [see Warnings and Precautions (5.2) ] Hypersensitivity to any component of this product.
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse drug reactions are described elsewhere in the labeling: Upper Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1) ] Mineral Metabolism [see Warnings and Precautions (5.2) ] Musculoskeletal Pain [see Warnings and Precautions (5.3) ] Osteonecrosis of the Jaw [see Warnings and Precautions (5.4) ] Atypical Fractures Including Femoral Fractures [see Warnings and Precautions (5.5) ] Renal Impairment [see Warnings and Precautions (5.6) ] Patients sensitive to High Sodium Intake [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS Calcium supplements, antacids or oral medications containing multivalent cations interfere with absorption of alendronate. ( 7.1 ) Use caution when co-prescribing aspirin/nonsteroidal anti- inflammatory drugs that may worsen gastrointestinal irritation. ( 7.2 , 7.3 ) 7.1 Calcium Supplements/Antacids Co-administration of BINOSTO and calcium, antacids, or oral medications containing multivalent cations will interfere with absorption of BINOSTO. Therefore, instruct patients to wait at least one-half hour after taking BINOSTO before taking any other oral medications. 7.