Comparative Pharmacology
Head-to-head clinical analysis: ACTONEL versus ACTONEL WITH CALCIUM COPACKAGED.
Head-to-head clinical analysis: ACTONEL versus ACTONEL WITH CALCIUM COPACKAGED.
ACTONEL vs ACTONEL WITH CALCIUM (COPACKAGED)
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Bisphosphonate that inhibits osteoclast-mediated bone resorption by binding to hydroxyapatite in bone and interfering with osteoclast activity.
ACTONEL WITH CALCIUM (COPACKAGED) contains risedronate sodium, a bisphosphonate that inhibits osteoclast-mediated bone resorption by binding to hydroxyapatite crystals in bone and inhibiting farnesyl pyrophosphate synthase (FPPS), an enzyme in the mevalonate pathway. This leads to reduced bone turnover and increased bone mineral density. The calcium component is for supplementation to prevent hypocalcemia.
35 mg orally once weekly or 5 mg orally once daily for osteoporosis; also 30 mg orally once weekly for Paget disease.
Actonel (risedronate) 35 mg orally once weekly, taken with 6-8 oz of plain water at least 30 minutes before breakfast. Calcium supplement (e.g., 1250 mg calcium carbonate) taken with food at a different time of day.
None Documented
None Documented
Terminal elimination half-life: 1.5-2 hours (short for bisphosphonates due to rapid renal clearance); however, bone retention half-life is prolonged (>1 year) due to binding to hydroxyapatite.
Terminal elimination half-life of risedronate is approximately 20 hours for the 5 mg daily dose and 480 hours for the 35 mg weekly dose due to prolonged retention in bone; clinically, the drug accumulates in bone and is slowly released.
Renal: 50-60% unchanged via glomerular filtration and active tubular secretion; Fecal: minor, biliary excretion negligible.
Risedronate is eliminated primarily via renal excretion, with approximately 50% of an absorbed dose excreted unchanged in urine. Unabsorbed drug is eliminated in feces. Total clearance is about 100 mL/min.
Category C
Category C
Bisphosphonate
Bisphosphonate and Calcium Supplement