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Active ingredient: Ibandronate - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antiresorptives
  • Bisphosphonates
  • Antihypocalcemic Agents

Dosage Forms

  • Liquid
  • Tablet (2.5 and 150 mg, film-coated)

Brands / Synonyms

Boniva; Ibandronate; Ibandronate sodium; Ibandronate sodium monohydrate; Ibandronic Acid; Ibandronic acid [BAN:INN]

Indications

For the treatment and prevention of osteoporosis in postmenopausal women.

Pharmacology

Ibandronate is a nitrogen-containing bisphosphonate in the same class as alendronate and risedronate. Ibandronate inhibits osteoclast-mediated bone resorption. All of the bisphosphonates prevent the breakdown of bone by bone cells called osteoclasts. In persons who are at high risk for osteoporosis, bisphosphonates not only result in increased amounts of bone and bone strength, they also reduce the risk of hip fractures and other bone fractures.

Mechanism of Action

The action of ibandronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting farnesyl pyrophosphate (FPP) synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

Absorption

Poorly absorbed (mean bioavailability following a 2.5 mg oral dose is about 0.6% compared to intravenous dosing). Absorption is impaired by any kind of food or drink other than plain water.

Toxicity

LD50 = 811 mg/kg (rat, oral), side effects include bronchitis, pneumonia and urinary tract infections.

Biotrnasformation / Drug Metabolism

No evidence of ibandronate being metabolized in humans.

Contraindications

· Known hypersensitivity to BONIVA or to any of its excipients

· Uncorrected hypocalcemia

· Inability to stand or sit upright for at least 60 minutes

Drug Interactions

Calcium Supplements/Antacids

Products containing calcium and other multivalent cations (such as aluminum, magnesium, iron) are likely to interfere with absorption of Ibandronate. Ibandronate should be taken at least 60 minutes before any oral medications containing multivalent cations (including antacids, supplements or vitamins).

H2 Blockers and Proton Pump Inhibitors (PPIs)

Of over 3500 patients enrolled in the Ibandronate osteoporosis Treatment and Prevention Studies, 15% used anti-peptic agents (primarily H2 blockers and PPIs). Among these patients, the incidence of upper gastrointestinal adverse experiences in the patients treated with Ibandronate was similar to that in placebo-treated patients. Similarly, of over 1600 patients enrolled in a study comparing once-monthly with daily dosing regimens of ibandronate, 14% of patients used anti-peptic agents. Among these patients, the incidence of upper gastrointestinal adverse experiences in the patients treated with Ibandronate 150 mg once monthly was similar to that in patients treated with Ibandronate 2.5 mg once daily.

Aspirin/Nonsteroidal Antiinflammatory Drugs (NSAIDs)

In the large, placebo-controlled osteoporosis Treatment Study, aspirin and nonsteroidal anti-inflammatory drugs were taken by 62% of the 2946 patients. Among aspirin or NSAID users, the incidence of upper gastrointestinal adverse events in patients treated with ibandronate 2.5 mg daily (28.9%) was similar to that in placebo-treated patients (30.7%). Similarly, in the 1-year monthly comparison study, aspirin and nonsteroidal anti-inflammatory drugs were taken by 39% of the 1602 patients. The incidence of upper gastrointestinal events in patients concomitantly taking aspirin or NSAIDs was similar in patients taking ibandronate 2.5 mg daily (21.7%) and 150 mg once monthly (22.0%). However, since aspirin, NSAIDs, and bisphosphonates are all associated with gastrointestinal irritation, caution should be exercised in the concomitant use of aspirin or NSAIDs with Ibandronate.

Drug/Laboratory Test Interactions

Bisphosphonates are known to interfere with the use of bone-imaging agents. Specific studies with ibandronate have not been performed.

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