Ibandronate

319.23

319.23

UMD7G2653W

DTXSID5048340

C65874

M05BA06|M - Musculo-skeletal system

2931900090

158.15000

-0.65

Solid

1.449±0.06 g/cm3(Predicted)

84 °C (decomp)

587.8±60.0 °C(Predicted)

309.3±32.9 °C

1.538

Freely soluble

-20°C Freezer

2.88E-16mmHg at 25°C

|Warning|H302 (95%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 20 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

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.

Ibandronate's protein binding in serum varies from 85.7-99.5% over a concentration of 0.5-10ng/mL, but is generally 86% across a concentration range of 20-2000ng/mL.

For the treatment and prevention of osteoporosis in postmenopausal women.|FDA Label|Treatment of osteoporosis in postmenopausal women at increased risk of fracture (see section 5.1). A reduction in the risk of vertebral fractures has been demonstrated, efficacy on femoral neck fractures has not been established.|Bondronat is indicated for:prevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases;treatment of tumour-induced hypercalcaemia with or without metastases.|Concentrate for solution for infusionPrevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases.Treatment of tumour-induced hypercalcaemia with or without metastases.Film-coated TabletsPrevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases.|Ibandronic acid is indicated in adults for, , , Prevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases., Treatment of tumour induced hypercalcaemia with or without metastases., , , Treatment of osteoporosis in postmenopausal women at increased risk of fracture (see section 5.1)., , A reduction in the risk of vertebral fractures has been demonstrated, efficacy on femoral neck fractures has not been established.,|Ibandronic acid 50mgIbandronic Acid Teva is indicated for the prevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases.Ibandronic acid 150mgTreatment of osteoporosis in postmenopausal women at increased risk of fracture. A reduction in the risk of vertebral fractures has been demonstrated, efficacy on femoral neck fractures has not been established.|Ibandronic acid Sandoz is indicated for the prevention of skeletal events (pathological fractures, bone complications requiring radiotherapy or surgery) in patients with breast cancer and bone metastases.,|Treatment of osteoporosis in post-menopausal women at increased risk of fracture.A reduction in the risk of vertebral fractures has been demonstrated. Efficacy on femoral-neck fractures has not been established.|Treatment of tumour-induced hypercalcaemia with or without metastases.|Treatment of osteoporosis|Combination treatment of osteoporosis

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.

Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS. (See all compounds classified as Bone Density Conservation Agents.)

Oral ibandronate is 0.63% bioavailable. In a study of healthy males, a 10mg oral dose had a T_max of 1.1±0.6h and a C_max of 4.1±2.6ng/mL. The T_max is approximately 1 hour, while C_max 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.|Ibandronate is predominantly eliminated in the urine and the unabsorbed drug is eliminated unchanged in the feces.|The apparent terminal volume of distribution of ibandronate is 90-368L in headlthy subjects and 103L in postmenopausal women with osteopenia.|The total clearance of ibandronate is 84-160mL/min.

Ibanronate is not metabolized in humans.

The half life of ibandronate in postmenopausal women ranges from 37-157 hours.

Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis. Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act. Osteoclasts mediate resorption of bone. When osteoclasts bind to bone they form podosomes, ring structures of F-actin. Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption. Nitrogen containing bisphosphonates such as ibandronate are known to induce apoptosis of hematopoietic tumor cells by inhibiting the components of the mevalonate pathway farnesyl diphosphate synthase, farnesyl diphosphate, and geranylgeranyl diphosphate. These components are essential for post-translational prenylation of GTP-binding proteins like Rap1. The lack of prenylation of these proteins interferes with their function, and in the case of Rap1, leads to apoptosis. ibandronate also activated caspase-3 which contribute to apoptosis.

(1-hydroxy-3-(methylpentylamino)propylidene)bisphosphonate

Human drugs -> Bonviva -> EMA Drug Category|Drugs for treatment of bone diseases -> Human pharmacotherapeutic group|Human drugs -> Bondronat -> EMA Drug Category|Human drugs -> Iasibon -> EMA Drug Category|Human drugs -> Ibandronic acid Accord -> EMA Drug Category|Human drugs -> Ibandronic Acid Teva -> EMA Drug Category|Human drugs -> Ibandronic Acid Sandoz -> EMA Drug Category|Drugs for treatment of bone diseases, Bisphosphonates -> Human pharmacotherapeutic group|Human drugs -> Bondenza (previously Ibandronic Acid Roche) -> EMA Drug Category|Human drugs -> Destara -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients