alendronate, Binosto, Fosamax

 Indications

Treatment and prevention of postmenopausal osteoporosis.

Treatment of osteoporosis in men. Treatment of

Paget’s disease of the bone. Treatment of corticosteroid-

induced osteoporosis in patients (men and

women) who are receiving 7.5 mg of prednisone/day

(or equivalent) with evidence of decreased bone mineral

density.

Action

Inhibits resorption of bone by inhibiting osteoclast activity.

Therapeutic Effects: Reversal of the progression

of osteoporosis with decreased fractures. Decreased

progression of Paget’s disease.

Pharmacokinetics

Absorption: Poorly absorbed (0.6–0.8%) after oral

administration.

Distribution: Transiently distributes to soft tissue,

then distributes to bone.

Metabolism and Excretion: Excreted in urine.

Half-life: 10 yr (reflects release of drug from skeleton).

TIME/ACTION PROFILE (inhibition of bone

resorption)

ROUTE ONSET PEAK DURATION

PO 1 mo 3–6 mo 3 wk–7 mo†

†After discontinuation of alendronate.

Contraindications/Precautions

Contraindicated in: Abnormalities of the esophagus

which delay esophageal emptying (i.e. strictures,

achalasia); Inability to stand/sit upright for at least 30

min; Renal insufficiency (CCr 35 mL/min); OB, Lactation:

Safety not established.

Use Cautiously in: History of upper GI disorders;

Pre-existing hypocalcemia or vitamin D deficiency; Invasive

dental procedures, cancer, receiving chemother apy, corticosteroids, or angiogenesis inhibitors, poor

oral hygiene, periodontal disease, dental disease, anemia,

coagulopathy, infection, or poorly-fitting dentures

(mayqrisk of jaw osteonecrosis).

Adverse Reactions/Side Effects

CNS: headache. EENT: blurred vision, conjunctivitis,

eye pain/inflammation. CV: atrial fibrillation. GI: abdominal

distention, abdominal pain, acid regurgitation,

constipation, diarrhea, dyspepsia, dysphagia, esophageal

cancer, esophageal ulcer, esophagitis, flatulence,

gastritis, nausea, taste perversion, vomiting. Derm:

erythema, photosensitivity, rash. MS: musculoskeletal

pain, femur fractures, osteonecrosis (primarily of jaw).

Resp: asthma exacerbation.

Interactions

Drug-Drug: Calcium supplements, antacids, and

levothyroxine maypthe absorption of alendronate.

Doses 10 mg/dayqrisk of adverse GI events when

used with NSAIDs. IV ranitidineqblood levels.

Drug-Food: Food significantlypabsorption. Caffeine

(coffee, tea, cola), mineral water, and orange

juice alsopabsorption.

Route/Dosage

PO (Adults): Treatment of osteoporosis—10 mg

once daily or 70 mg once weekly. Prevention of osteoporosis—

5 mg once daily or 35 mg once weekly.

Paget’s disease—40 mg once daily for 6 mo. Retreatment

may be considered for patients who relapse.

Treatment of corticosteroid-induced osteoporosis in

men and premenopausal women—5 mg once daily.

Treatment of corticosteroid-induced osteoporosis in

postmenopausal women not receiving estrogen—

10 mg once daily.

Availability (generic available)

Tablets: 5 mg, 10 mg, 35 mg, 40 mg, 70 mg. Cost: Generic—

10 mg $20.94/100, 35 mg $6.99/4, 70 mg

$8.22/4. Oral solution (raspberry flavor): 70 mg/

75 mL. Cost: Generic—$23.44/75 mL. Effervescent

tablets (strawberry flavor): 70 mg. Cost: $168.00/

4. In combination with: Cholecalciferol (Fosamax

plus D) See Appendix B.