Ibandronic Acid; Uses, Side Effects, Interactions, Pragnancy

Ibandronic Acid; Uses, Side Effects, Interactions, Pragnancy

Ibandronic Acid is a third-generation amino-bisphosphonate with anti-resorptive and anti-hypercalcemic activities. Ibandronic acid binds to and adsorbs onto the surface of hydroxyapatite crystals in the bone matrix, thereby preventing osteoclast resorption. This agent also inhibits farnesyl pyrophosphate synthase, an enzyme involved in the mevalonate pathway. Inhibition of this enzyme prevents the formation of isoprenoids, thereby leading to a reduction in the farnesylation and geranylgeranylation of signaling proteins of G protein-coupled signaling, and, eventually, inducing apoptosis of osteoclasts. By inhibiting osteoclast-mediated bone resorption, ibandronic acid increases bone mineral density, decreases bone remodeling and turnover, as well as reduces bone pain.

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 Ibandronic Acid

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 analogs 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 signaling 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.

Indications of Ibandronic Acid

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Osteoporosis in patients with chronic kidney disease – Management renal impairment.

  •  Ibandronate – Ibandronate is also available in an IV preparation (3 mg IV every three months). However, there is no direct fracture efficacy data for IV ibandronate. While there are no

The use of osteoclast inhibitors in patients with multiple myeloma

monthly intravenous ibandronate has not demonstrated a reduction in skeletal-related events in patients with multiple myeloma (MM). Two randomized trials have evaluated the use of ibandronate in patients with
  • Treatment of hypercalcemia patients may have a better response to ZA. Ibandronate effectively treats hypercalcemia of malignancy. In combined trials with over 320 patients, ibandronate doses of 2 mg IV administered over two hours

  • Osteoclast inhibitors for patients with bone metastases from breast, prostate, and other solid tumors clodronate and ibandronate – Clodronate and ibandronate are approved for use in metastatic bone disease outside the United States. Oral ibandronate has similar efficacy to intravenous ibandronate. Patients

  • Bone metastases in advanced prostate cancer: Management usage and there is no evidence that beta emitting radioisotopes prolong survival. Intravenous ibandronate or other bisphosphonates may offer an alternative to external beam RT for the management of pain.

Overview of the use of osteoclast inhibitors in early breast cancer

Drug Administration (FDA) has approved oral and intravenous bisphosphonates (alendronate, ibandronate, risedronate, and zoledronic acid) for the treatment and prevention of postmenopausal osteoporosis.
  • Treatment of osteoporosis in men less often for the treatment of osteoporosis in men. Intravenous (IV) bisphosphonates, ZA, and ibandronate offer an alternative option for individuals who cannot tolerate oral bisphosphonates or who find.

  • Metabolic bone disease in inflammatory bowel disease alternative option for patients unable to tolerate or absorb oral bisphosphonates. In a small trial, IV ibandronate (1 mg every three months) significantly improved BMD in patients with CD.

Contra-Indications of Ibandronic Acid

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The dosage of Ibandronic Acid

Strengths: 2.5 mg; 150 mg; 3 mg/3 mL

Prevention of Osteoporosis

  • PO Prophylaxis of skeletal events in patients w/ breast cancer and bone metastases 50 mg/day.

Treatment and prophylaxis of postmenopausal osteoporosis

  • 150 mg once mthly on the same date each mth, or 2.5 mg/day. IV Hypercalcaemia of malignancy 2-4 mg as a single infusion. Max: 6 mg.
  • Postmenopausal osteoporosis 3 mg by inj once every 3 mth. Prophylaxis of skeletal events in patients w/ breast cancer and bone metastases 6 mg by infusion 3-4 wkly.

Side Effects of Ibandronic Acid

Common

Rare

Drug Interactions of Ibandronic Acid

The ibandronic acid may interact with following drugs, supplements & may change the efficacy of drugs

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Pregnancy & Lactation Ibandronic Acid

FDA Pregnancy category C

Pregnancy

Ibandronate is not indicated for use in women of reproductive potential. There are no data of ibandronate use during human pregnancy to inform of any drug-associated risks. Based on animal studies and the known class effects of bisphosphonates, fetal harm may occur. Reproductive studies in animals indicate that ibandronate may be associated with increased incidence of fetal renal pelvis ureter (RPU) syndrome, impaired infant neuromuscular development, maternal hypocalcemia, postimplantation fetal loss, dystocia, and maternal periparturient death, and maternal and fetal death.

Lactation

Ibandronic acid tablets are for use only by postmenopausal women and must not be taken by women who could still have a baby. Do not take ibandronic acid if you’re pregnant or breastfeeding.

References

 

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