Overview
11 DESCRIPTION Risedronate sodium delayed-release tablets contain a pH-sensitive enteric coating and a chelating agent (EDTA). Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism. Each risedronate sodium delayed-release tablet for oral administration contains the equivalent of 35 mg of risedronate sodium (amorphous).
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Risedronate has an affinity for hydroxyapatite crystals in bone and acts as an antiresorptive agent. At the cellular level, risedronate inhibits osteoclasts. The osteoclasts adhere normally to the bone surface, but show evidence of reduced active resorption (for example, lack of ruffled border). Histomorphometry in rats, dogs, and minipigs showed that risedronate treatment reduces bone turnover (activation frequency, that is, the rate at which bone remodeling sites are activated) and bone resorption at remodeling sites. 12.2 Pharmacodynamics Risedronate treatment decreases the elevated rate of bone turnover that is typically seen in postmenopausal osteoporosis.
Indications
- 1 INDICATIONS AND USAGE Risedronate sodium delayed-release tablets are bisphosphonate in a delayed-release formulation and is indicated for treatment of postmenopausal osteoporosis (1.1) Limitations 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 (1.2). 1.1 Postmenopausal Osteoporosis Risedronate sodium delayed-release tablets are indicated for the treatment of osteoporosis in postmenopausal women.
Common Doses
- 35 mg
Dosage
2 DOSAGE AND ADMINISTRATION One 35 mg delayed-release tablet once-a-week (2.1) Instruct patients to: • Take risedronate sodium delayed-release tablets in the morning immediately following breakfast with at least 4 ounces of plain water (2.2) • Avoid lying down for 30 minutes after taking risedronate sodium delayed-release tablets (2.2) • Take supplemental calcium and vitamin D if dietary intake is inadequate (2.3) 2.1 Treatment of Postmenopausal Osteoporosis [ see Indications and Usage (1.
Contraindications
- 4 CONTRAINDICATIONS Risedronate sodium delayed-release tablets contraindicated in patients with the following conditions: 1. Abnormalities of the esophagus which delay esophageal emptying such as stricture or achalasia [ see Warnings and Precautions (5.2) ] 2. Inability to stand or sit upright for at least 30 minutes [ see Dosage and Administration (2), Warnings and Precautions (5.2) ] 3. Hypocalcemia [ see Warnings and Precautions (5.3) ] 4. Known hypersensitivity to any component of this product.
Side Effects
- 6 ADVERSE REACTIONS Most common adverse reactions (greater than 5%) include: diarrhea, influenza, arthralgia, back pain, and abdominal pain (6.1) Hypersensitivity reactions (angioedema, generalized rash, bullous skin reactions, Stevens-Johnson syndrome, and toxic epidermal necrolysis), and eye inflammation (iritis, uveitis) have been reported rarely (6.2) To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries Inc. at 1-800-818-4555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.
Interactions
- 7 DRUG INTERACTIONS Risedronate is not metabolized and does not induce or inhibit hepatic microsomal drug-metabolizing enzymes (for example, Cytochrome P450). Calcium supplements, antacids, proton pump inhibitors (PPIs), H 2 blockers, magnesium-based supplements or laxatives, and iron preparations interfere with the absorption of risedronate sodium (7.1, 7.2) 7.1 Calcium Supplements/Antacids When risedronate sodium was administered following breakfast, the co-administration of a tablet containing 600 mg of elemental calcium and 400 international units vitamin D reduced risedronate...