Risedronate

Pronunciation

(ris ED roe nate)

U.S. Brand Names

Actonel®

Synonyms

Risedronate Sodium

Generic Available

Canadian Brand Names

Actonel®

Use

Paget's disease of the bone; treatment and prevention of glucocorticoid-induced osteoporosis; treatment and prevention of osteoporosis in postmenopausal women

Pregnancy Risk Factor

Pregnancy Implications

Teratogenic and nonteratogenic embryo/fetal effects have been reported in animal studies. There are no adequate and well-controlled studies in pregnant women. Bisphosphonates are incorporated into the bone matrix and gradually released over time. Theoretically, there may be a risk of fetal harm when pregnancy follows the completion of therapy. Based on limited case reports with pamidronate, serum calcium levels in the newborn may be altered if administered during pregnancy.

Lactation

Excretion in breast milk unknown/not recommended

Contraindications

Hypersensitivity to risedronate, bisphosphonates, or any component of the formulation; hypocalcemia; abnormalities of the esophagus which delay esophageal emptying such as stricture or achalasia; inability to stand or sit upright for at least 30 minutes; severe renal impairment (Clcr<30 mL/minute)

Warnings/Precautions

Bisphosphonates may cause upper gastrointestinal disorders such as dysphagia, esophageal ulcer, and gastric ulcer. Use caution in patients with renal impairment; hypocalcemia must be corrected before therapy initiation with alendronate; ensure adequate calcium and vitamin D intake, especially for patients with Paget's disease in whom the pretreatment rate of bone turnover may be greatly elevated.

Adverse Reactions

Seen in patients taking 30 mg/day for Paget's disease:

>10%:

Central nervous system: Headache (18%)

Dermatologic: Rash (11%)

Gastrointestinal: Diarrhea (20%), abdominal pain (11%)

Neuromuscular & skeletal: Arthralgia (33%)

Miscellaneous: Flu-like syndrome (10%)

1% to 10%:

Cardiovascular: Peripheral edema (8%)

Central nervous system: Chest pain (7%), dizziness (7%)

Gastrointestinal: Nausea (10%), constipation (7%), belching (3%), colitis (3%, placebo 3%)

Neuromuscular & skeletal: Weakness (5%), bone pain (5%, placebo 5%), leg cramps (3%, placebo 3%), myasthenia (3%)

Ocular: Amblyopia (3%, placebo 3%), dry eye (3%)

Otic: Tinnitus (3%, placebo 3%)

Respiratory: Sinusitis (5%), bronchitis (3%, placebo 5%) <1%: Acute iritis

Miscellaneous: Neoplasm (3%)

Seen in patient taking 5 mg/day for osteoporosis (events similar to those seen with placebo)

>10%:

Central nervous system: Pain (14%)

Gastrointestinal: Abdominal pain (12%), diarrhea (11%), nausea (11%)

Genitourinary: Urinary tract infection (11%)

Neuromuscular & skeletal: Back pain (26%), arthralgia (24%)

1% to 10%:

Cardiovascular: Hypertension (10%), chest pain (5%), cardiovascular disorder (2%), angina (2%)

Central nervous system: Depression (7%), dizziness (6%), insomnia (5%), anxiety (4%), vertigo (3%)

Dermatologic: Rash (8%), bruising (4%), pruritus (3%), skin carcinoma (2%)

Gastrointestinal: Flatulence (5), gastritis (2%), gastrointestinal disorder (2%), rectal disorder (2%), tooth disorder (2%)

Genitourinary: Cystitis (4%)

Hematologic: Anemia (2%)

Neuromuscular & skeletal: Joint disorder (7%), myalgia (7%), neck pain (5%), asthenia (5%), bone pain (5%), bone disorder (4%), neuralgia (4%), leg cramps (4%), bursitis (3%), tendon disorder (3%), hypertonia (2%), paresthesia (2%)

Ocular: Cataract (6%), conjunctivitis (3%)

Otic: Otitis media (2%)

Respiratory: Pharyngitis (6%), rhinitis (6%), dyspnea (4%), pneumonia (3%)

Miscellaneous: Neoplasm(3%), hernia (3%)

Additional effects observed in either patient group noted above: <1%: Duodenitis, glossitis, iritis, liver function test abnormality, osteonecrosis

Overdosage/Toxicology

Symptoms of overdose include hypocalcemia, hypophosphatemia, and upper GI adverse events (upset stomach, heartburn, esophagitis, gastritis, or ulcer). Gastric lavage may remove unabsorbed drug. Treat with milk or antacids to bind risedronate; dialysis would not be beneficial.

Drug Interactions

Antacids: Interfere with the absorption of risedronate; take at a different time of the day.

Calcium supplements: Interfere with the absorption of risedronate; take at a different time of the day.

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase risk of osteoporosis).

Food: Food may reduce absorption (similar to other bisphosphonates); mean oral bioavailability is decreased when given with food.

Stability

Store at room temperature of 20°C to 25°C (68°F to 77°F).

Mechanism of Action

A bisphosphonate which inhibits bone resorption via actions on osteoclasts or on osteoclast precursors; decreases the rate of bone resorption, leading to an indirect increase in bone mineral density. In Paget's disease, characterized by disordered resorption and formation of bone, inhibition of resorption leads to an indirect decrease in bone formation; but the newly-formed bone has a more normal architecture.

Pharmacodynamics/Kinetics

Onset of action: May require weeks

Absorption: Rapid

Distribution: Vd: 6.3 L/kg

Protein binding: ~24%

Metabolism: None

Bioavailability: Poor, ~0.54% to 0.75%

Half-life elimination: Terminal: 480 hours

Excretion: Urine (up to 80%); feces (as unabsorbed drug)

Dosage

Risedronate should be taken at least 30 minutes before the first food or drink of the day other than water. Oral:

Adults (patients should receive supplemental calcium and vitamin D if dietary intake is inadequate):

Paget's disease of bone: 30 mg once daily for 2 months

Retreatment may be considered (following post-treatment observation of at least 2 months) if relapse occurs, or if treatment fails to normalize serum alkaline phosphatase. For retreatment, the dose and duration of therapy are the same as for initial treatment. No data are available on more than one course of retreatment.

Osteoporosis (postmenopausal) prevention and treatment: 5 mg once daily; efficacy for use longer than 1 year has not been established; alternatively, a dose of 35 mg once weekly has been demonstrated to be effective

Osteoporosis (glucocorticoid-induced) prevention and treatment: 5 mg once daily

Elderly: Dosage adjustment is not necessary in patients with Clcr 30 mL/minute.

Dosage adjustment in renal impairment: Clcr<30 mL/minute: Not recommended for use

Administration

It is imperative to administer risedronate 30-60 minutes before the patient takes any food, drink, or other medications orally to avoid interference with absorption. The patient should take risedronate on an empty stomach with a full glass (8 oz) of plain water (not mineral water) and avoid lying down for 30 minutes after swallowing tablet to help delivery to stomach.

Monitoring Parameters

Alkaline phosphatase should be periodically measured; serum calcium, phosphorus, and possibly potassium due to its drug class; use of absorptiometry may assist in noting benefit in osteoporosis; monitor pain and fracture rate

Reference Range

Calcium (total): Adults: 9.0-11.0 mg/dL (2.05-2.54 mmol/L), may slightly decrease with aging; phosphorus: 2.5-4.5 mg/dL (0.81-1.45 mmol/L)

Dietary Considerations

Take

30 minutes before the first food or drink of the day other than water.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Avoid alcohol (ethanol may increase risk of osteoporosis). In order to be effective, this medication must be taken exactly as directed, with a full glass of water first thing in the morning, at least 30 minutes before the first food or beverage of the day. Wait at least 30 minutes after taking this medication before taking anything else. Stay in sitting or standing position for 30 minutes following administration and until after the first food of the day to reduce potential for esophageal irritation. Consult prescriber to determine necessity of lifestyle changes (eg, decreased smoking, decreased alcohol intake, dietary supplements of calcium, or increased dietary vitamin D). You may experience GI upset (eg, flatulence, bloating, nausea, acid regurgitation); small, frequent meals may help. Report unresolved muscle twitching or bone pain or leg cramps; acute abdominal pain; chest pain, palpitations, or swollen extremities; disturbed vision or excessively dry eyes; ringing in the ears; or persistent flu-like symptoms. Also notify prescriber at once if experiencing difficulty swallowing, pain when swallowing, or severe or persistent heartburn. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant or if you are breast-feeding.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause dizziness

Mental Health: Effects on Psychiatric Treatment

None reported

Dosage Forms

Tablet, as sodium: 5 mg, 30 mg, 35 mg

References

"Abstracts of the American College of Rheumatology 65th Meeting and the Association of Rheumatology Health Professionals 36th Meeting. November 10-15, 2001, San Francisco, California, USA," Arthritis Rheum , 2001, 44(9 Suppl):40-520.

French AE, Kaplan N, Lishner M, et al, "Taking Bisphosphonates During Pregnancy," Can Fam Physician , 2003, 49:1281-2.

Ruggiero SL, Mehrotra B, Rosenberg TJ, et al, "Osteonecrosis of the Jaws Associated With the Use of Bisphosphonates: A Review of 63 Cases," J Oral Maxillofac Surg , 2004, 62(5):527-34.

International Brand Names

Actonel® (AR, AT, AU, BE, BR, CA, CH, CO, CR, CZ, DE, DO, EC, ES, FR, GB, GT, HN, ID, IE, IL, IT, JP, MX, NZ, PA, PL, PT, RO, SG, SI, SV, TH, TR, ZA); Benet® (JP); Optinate® (FI, IT, NO, SE); Optinate®Septimum (SE); Ribastamin® (AR)

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