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Ibandronate Sodium

Pronunciation

Pronunciation: eye-BAN-droe-nate SOE-dee-um
Class: Bisphosphonate

Trade Names

Boniva
- Tablets 150 mg
- Injection, solution 1 mg/mL

Pharmacology

Inhibits osteoclast activity and reduces bone resorption and turnover.

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Pharmacokinetics

Absorption

Absorption from an oral dose is in the upper GI tract. T max is 0.5 to 2 h (oral). Compared with IV administration, oral bioavailability is 0.6%. Bioavailability decreased by 90% with food.

Distribution

Rapidly binds to bone or is excreted in the urine. Vd is at least 90 L. The amount removed from circulation via bone is estimated to be 40% to 50%. Protein binding in human serum is approximately 86% (IV) or ranges from 85.7% to 99.5% (oral).

Metabolism

No evidence of metabolism.

Elimination

Cl is 84 to 160 mL/min. The portion not removed from the circulation via bone absorption (approximately 50% to 60% of absorbed dose) is eliminated unchanged by the kidney. Unabsorbed drug is eliminated unchanged in the feces. Terminal half-life ranges from 37 to 157 h (150 mg tablet) or 4.6 to 25.5 h (IV).

Special Populations

Renal Function Impairment

Patients with CrCl 40 to 70 mL/min had 55% higher AUC and patients with CrCl 30 mL/min had more than a 2-fold increase in exposure.

Hepatic Function Impairment

No studies have been performed; ibandronate is not metabolized in the human liver.

Elderly

Progressive age-related changes in renal function may alter the elimination of ibandronate in elderly patients.

Children

Pharmacokinetics have not been studied in patients younger than 18 y of age.

Gender

Bioavailability and pharmacokinetics are similar in men and women.

Race

Pharmacokinetic differences because of race have not been studied.

Indications and Usage

Treatment (injection, tablets) and prevention (tablets) of osteoporosis in postmenopausal women.

Unlabeled Uses

Bone metastases; hypercalcemia of malignancy (injection).

Contraindications

Inability to stand or sit upright for at least 60 min (tablets); hypocalcemia; abnormalities of the esophagus that delay esophageal emptying, such as stricture or achalasia (oral); hypersensitivity to any component of the product.

Dosage and Administration

Adults

PO One 150 mg tablet once monthly on the same date of each month. Should be taken with plain water at least 60 min before the first food or drink (other than water) of the day or before taking any oral medication or supplement, including antacids, calcium, or vitamins.

Adults

IV 3 mg every 3 mo, administered over 15 to 30 sec.

General Advice

  • Tablets
  • If the once-monthly dose is missed and the patient's next scheduled ibandronate day is more than 7 days away, instruct the patient to take 1 ibandronate 150 mg tablet in the morning following the date that it is remembered. The patient then should return to taking 1 ibandronate 150 mg tablet every month in the morning on their chosen day, according to the original schedule. The patient must not take two 150 mg tablets within the same week. If the patient's next scheduled ibandronate day is only 1 to 7 days away, instruct the patient to wait until their next scheduled ibandronate day to take the tablet. The patient then should return to taking 1 ibandronate 150 mg tablet every month in the morning of their chosen day, according to their original schedule.
  • Advise patient not to administer tablets with any liquid other than plain water.
  • Instruct patient that ibandronate tablets should be swallowed whole with a full glass of plain water (180 to 240 mL) while standing or sitting in an upright position. Instruct patients to not lie down for 60 minutes after taking ibandronate.
  • Advise patients to not chew or suck the tablet, or keep it in their mouths to melt or dissolve because of the potential for oropharyngeal ulceration.
  • Instruct patients to take the ibandronate 150 mg tablet on the same date each month (ie, the patient's ibandronate day).
  • Advise patients to take supplemental calcium or vitamin D if dietary intake is inadequate.
  • Injection
  • Injection must be administered IV by a health care provider. Do not administer intra-arterially or paravenously; this could lead to tissue damage.
  • Administer injection using the enclosed needle.
  • Prefilled syringes are for single use only; discard unused portion.
  • Do not mix injection with calcium-containing solutions or other IV-administered drugs.
  • If a dose is missed, administer injection as soon as it can be rescheduled. Schedule subsequent injections every 3 mo from the date of last injection and not more frequently than once every 3 mo.
  • Patient must receive supplemental calcium and vitamin D.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Antacids, calcium supplements, or other products containing calcium, or other multivalent cations (eg, aluminum, iron, magnesium)

May interfere with oral absorption of ibandronate. Ibandronate should be taken at least 60 min before any other oral medication, including multivalent cations.

Aspirin, NSAIDs

Possible additive GI adverse reactions.

Histamine H 2 antagonists (eg, ranitidine)

Ibandronate bioavailability may be increased; however, the amount of change is not expected to be clinically important.

Laboratory Test Interactions

May interfere with bone-imaging agents.

Adverse Reactions

Cardiovascular

Hypertension (7%).

CNS

Headache (7%); asthenia, dizziness (4%); fatigue, insomnia, vertigo (3%); depression, nerve root lesion (2%).

EENT

Nasopharyngitis (6%); pharyngitis (3%); ocular inflammation (eg, scleritis, uveitis).

GI

Dyspepsia (12%); abdominal pain (8%); diarrhea (7%); nausea (5%); constipation, tooth disorder (4%); gastroenteritis, vomiting (3%); gastritis (2%); dysphagia, esophageal and gastric ulcer, esophagitis.

Genitourinary

UTI (6%); cystitis (3%).

Local

Redness, swelling (less than 2%).

Musculoskeletal

Back pain (14%); arthralgia (10%); pain in extremity (8%); myalgia (6%); joint disorder (4%); arthritis, localized osteoarthritis (3%); muscle cramp (2%); osteonecrosis of the jaw, severe or incapacitating bone, joint, or muscle pain (postmarketing).

Respiratory

Upper respiratory tract infection (34%); bronchitis (10%); pneumonia (6%); bronchospasm (postmarketing).

Miscellaneous

Acute-phase reaction (10%) ; influenza (8%); flu-like symptoms, hypercholesterolemia (5%); infection (4%); allergic reactions, rash (3%); anaphylaxis, angioedema, hypocalcemia (postmarketing).

Precautions

Monitor

Oral

Monitor patient for signs or symptoms of esophageal reaction (eg, dysphagia, new or worsening heartburn, retrosternal pain). Periodic dental exams for signs of osteonecrosis of the jaw are recommended.

Injection

Measure serum creatinine in patients who receive ibandronate prior to each dosage administration.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Age-related decreases in renal function may alter ibandronate elimination.

Renal Function

Not recommended for use in patients with severe renal impairment (CrCl less than 30 mL/min).

Bone and mineral metabolism disturbances, hypocalcemia, hypovitaminosis D

Treat effectively before starting therapy with ibandronate. Ibandronate injection may cause a transient decrease in serum calcium levels.

GI disorders

May cause upper GI disorders (eg, dysphagia, esophagitis, gastritis esophageal or gastric ulcer). Discontinue use if new or worsening symptoms develop. Use with caution in patients with active upper GI problems (eg, Barrett esophagus, duodentitis, dysphagia, gastritis, ulcer).

Jaw osteonecrosis

Osteonecrosis, primarily in the jaw, has been reported in patients receiving bisphosphonates.

Musculoskeletal pain

Severe and occasionally incapacitating bone, joint, and/or muscle pain has been reported in patients taking bisphosphonates. Consider discontinuing use if severe symptoms develop.

Renal toxicity

May occur, manifesting as deterioration in renal function and, in rare cases, acute renal failure.

Overdosage

Symptoms

Hypocalcemia; hypomagnesemia; hypophosphatemia; upper GI adverse reactions, including dyspepsia, esophagitis, gastritis, ulcer, or upset stomach.

Patient Information

  • Advise patient to read patient information leaflet before starting therapy and with each refill.
  • Instruct patient to take each tablet with plain water immediately upon arising for the day, at least 60 min before the first food, beverage, medication, or supplement (including calcium and vitamins) of the day, and to remain in a standing or sitting position for at least 60 min.
  • Instruct patient to swallow tablet whole with a full glass (6 to 8 oz) of plain water. Caution patient not to chew or suck on tablet.
  • Caution patient not to take the tablets with any liquid other than plain water. Advise patient that taking the tablets with food, other medications, juices, mineral water, coffee, or any other beverage will reduce the absorption and effectiveness of ibandronate.
  • Advise patient taking once-monthly ibandronate 150 mg tablet to take the tablet on the same date each month.
  • Advise patient taking ibandronate once monthly that if the once-monthly dose is missed and the next scheduled dose is more than 7 days away, to take their ibandronate tablet in the morning after the date that it is remembered and then return to taking 1 ibandronate tablet in the morning of their chosen day, according to their original schedule.
  • Advise patient taking ibandronate once monthly that if the once-monthly dose is missed and the next scheduled dose is only 1 to 7 days away, to skip the missed dose and take the next ibandronate tablet in the morning of the patient's chosen day, according to patient's original schedule.
  • Caution patient using 150 mg tablet to never take 2 tablets within the same week.
  • Instruct patient to discontinue therapy and seek medical care if any of the following occur: difficulty swallowing, new or worsening heartburn, pain behind breastbone.
  • Advise patient regarding interventions that help prevent osteoporosis: calcium 1,500 mg/day (diet and supplements), reduction of cigarette smoking and alcohol consumption, vitamin D supplementation, weight-bearing exercise.

Copyright © 2009 Wolters Kluwer Health.

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