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Ibandronate: A Clinical Pharmacological and Pharmacokinetic Update
Author(s) -
Barrett Joanne,
Worth Eric,
Bauss Frieder,
Epstein Solomon
Publication year - 2004
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270004267594
Subject(s) - bisphosphonate , medicine , pharmacokinetics , bone resorption , osteoporosis , pharmacology , bioavailability , osteoclast , bone disease , bone remodeling , receptor
Ibandronate is a potent nitrogen‐containing bisphosphonate. It has a strong affinity for bone mineral and potently inhibits osteoclast‐mediated bone resorption. Ibandronate is effective for the treatment of hypercalcemia of malignancy, metastatic bone disease, postmenopausal osteoporosis, corticosteroid‐induced osteoporosis, and Paget's disease. Oral ibandronate is rapidly absorbed (t max < 1 hour), with a low bioavailability (0.63%) that is further reduced (by up to 90%) in the presence of food. Ibandronate has a wide therapeutic index and is not metabolized and, therefore, has a low potential for drug interactions. Given its metabolic stability, ibandronate is eliminated from the blood by partitioning into bone (40%‐50%) and through renal clearance (CL R ∼60 mL/min). The CL R of ibandronate is linearly related to creatinine clearance. The sequestration of ibandronate in bone (V D > 90 L) results in a multiphasic elimination (t 1/2 range ∼10–60 hours), characterized by the slow release of ibandronate from the bone compartment. The potency of ibandronate and its sequestration into bone allow ibandronate to be developed as oral and intravenous injection formulations that can be administered with convenient extended between‐dose intervals.