Ibandronic acid

Absorption

Oral ibandronate is 0.63% bioavailable. In a study of healthy males, a 10mg oral dose had a Tmax of 1.1±0.6h and a Cmax of 4.1±2.6ng/mL. The Tmax is approximately 1 hour, while Cmax varies depending on dose.
A 2mg intravenous dose of ibandronate has an AUC of 316ng*h/mL, a 4mg intravenous dose of ibandronate has an AUC of 581ng*h/mL, and a 6mg intravenous dose of ibandronate has an AUC of 908ng*h/mL.

Toxicity

Patients experiencing an overdose may present with hypocalcemia, hypophosphatemia, upset stomach, dyspepsia, esophagitis, and uclers. Oral overdose can be managed by giving patients milk or antacids to bind excess unabsorbed ibandronate. Overdoses can be managed by providing intravenous electrolytes and dialysis is not expected to remove excess drug from serum.

Description

This third generation biphosphonate was launched in Austria and Germany for the treatment of bone disorders such as hypercalcemia in malignancy and ostedysis, Paget's disease and osteoporosis. It does not effect bone mineralization, therefore, the potential risk of osteomalacia is prevented. This was a problem with first generation derivatives. While the exact mode of action is not understood, they are inhibitors of osteroclast mediated bone resorption. These compounds strongly interact with hydroxyapatite crystals and have a half-life in the skeleton of several years. Despite this observation ibandronate was well tolerated and safe.

Chemical properties

White Solid

Originator

Boehringer Mannheim (Germany)

The Uses of Ibandronic acid

Labelled Ibandronic Acid (I120000). A bisphosphonate antiresorptive agent. Bone resorption inhibitor.

The Uses of Ibandronic acid

A biphosphonate bone resorption inhibitor.

The Uses of Ibandronic acid

A labeled biphosphonate bone resorption inhibitor.

The Uses of Ibandronic acid

A bisphosphonate antiresorptive agent. Bone resorption inhibitor.

Background

Ibandronate, or BM 21.0955, is a third generation, nitrogen containing bisphosphonate similar to zoledronic acid, minodronic acid, and risedronic acid. It is used to prevent and treat postmenopausal osteoporosis. Ibandronate was first described in the literature in 1993 as a treatment for bone loss in dogs.
Ibandronate was granted FDA approval on 16 May 2003.

Indications

For the treatment and prevention of osteoporosis in postmenopausal women.

What are the applications of Application

Ibandronic Acid is a biphosphonate bone resorption inhibitor

brand name

Bondronat

Pharmacokinetics

Ibandronate is a nitrogen containing bisphosphonate used to treat and prevent osteoporosis in postmenopausal women. The therapeutic index is wide as overdoses are not especially toxic, and the duration of action is long as the half life can be up to 157 hours. Patients should be counselled regarding the risk of upper GI adverse reactions, hypocalcemia, musculoskeletal pain, osteonecrosis of the jaw, atypical fractures of the femur, and severe renal impairment.

Clinical Use

Bisphosphonate:

Reduction of bone damage in bone metastases in breast cancer

Hypercalcaemia of malignancy

Postmenopausal osteoporosis

Metabolism

Ibanronate is not metabolized in humans.

Metabolism

After initial systemic exposure, ibandronic acid rapidly binds to bone or is excreted into urine. There is no evidence that ibandronic acid is metabolised in animals or humans. The absorbed fraction of ibandronic acid is removed from the circulation via bone absorption (estimated to be 40-50% in postmenopausal women) and the remainder is eliminated unchanged by the kidney. The unabsorbed fraction of ibandronic acid is eliminated unchanged in the faeces. Renal clearance accounts for 50-60% of total clearance and is related to creatinine clearance. The difference between the apparent total and renal clearances is considered to reflect the uptake by bone.