Alendronate

Bisphosphonates (BP) are today the first line treatment of benign and malignant bone diseases. As pyrophosphate analogues (Fig. 3), BP accumulate in bone and are taken up by osteoclasts. Once in the cell, the nitrogen-containing BP (N-BP) such as Alendronate, Risedronate, Ibandronate and Zoledronate effectively inhibit osteoclast resorption and induce cell... 

Bone Metabolism. Figure 3 Chemical structure of pyrophosphate (a) and the bisphosphonates etidronate (b), clodronate (c), pamidronate (d), ibandronate (e). alendronate (f), risedronate (g), zoledronate (h). 

Alendronate, etidronate, and risedronate act primarily on the bone by inhibiting normal and abnormal bone resorption. This results in increased bone mineral density, reversing the progression of osteoporosis. 

These dragp are contraindicated in patients who are hypersensitive to the bisphosphonates. Alendronate and risedronate are contraindicated in patients with hypocalcemia Alendronate is a pregnancy Category C drug and is contraindicated during pregnancy. These drugp are contraindicated in patients with renal impairment with serum creatinine less than 5 mg/dL. Concurrent use of these dm with hormone replacement therapy is not recommended. 

When administered with ranitidine, alendronate bioavailability is increased. When calcium supplements or antacids are administered with risedronate or alendronate, absorption of the bisphosphonates is decreased, hi addition, risedronate absorption is inhibited when the drug is administered with magnesium and aluminum. There is an increased risk of gastrointestinal... 

BISPHOSPHONATES. When administering alendronate or risedronate the nurse gives the drug orally in the morning before the first food or drink of the day. Risedronate and etidronate are administered once daily. Etidronate is not administered within 2 hours of food, vitamin and mineral supplements, or antacids. 

When alendronate and risedronate are administered, serum calcium levels are monitored before, during, and after therapy. 

Discuss the important points to include when educating a patient prescribed alendronate 35 mg once weekly. 

CH4O3S 75-75-2) see Alatrofloxacin mesilate Alendronate sodium Dolasetron mesilate Glaziovine Nelfinavir mesylate Tirilazad mesilate Trovafloxacin mesilate... 

H2NNa 7782-92-5) see Milnacipran hydrochloride sodium 5-(3-aminopropyl)-4,6-dihydroxy-l,3,2,4,6-di-oxatriphosphorinan-5-olate 2,4,6-trioxide (C4H NNa08P3) see Alendronate sodium sodium azide... 

Spicy foods Orange juice Medications Alendronate Aspirin Iron... 

Alendronate should be considered hrst-line treatment for primary osteoporosis in men owing to its proven benefit in reducing fractures and relative safety. 

In placebo-controlled clinical trials, alendronate, ibandronate, and risedronate increased bone mineral density by up to 5% to 8% in the lumbar spine and up to 3% to 5% in the hip.13-16 Additional data suggest that bone mineral density continues to increase with long-term therapy of 7 to 10 years.17,18... 

Large, well-designed trials have proven the benefits of bis-phosphonate therapy in preventing vertebral and nonvertebral fractures. Several studies have found decreases in vertebral fracture risk by as much as 40% to 50% with alendronate and risedronate.13,14,19-21 Data suggest a similar reduction with ibandronate on vertebral fractures.16,22 Alendronate and risedronate decrease the incidence of hip and nonvertebral fractures as well.14,19,23... 

Several studies have evaluated the long-term efficacy and safety of bisphosphonates in postmenopausal women. One study evaluated the use of alendronate over a 10-year period and found no difference in adverse effects between women who received alendronate for 10 years and women who discontinued alendronate after 5 years. Women who discontinued alendronate after 5 years continued to experience sustained increases in bone mineral density compared with baseline values and a reduction... 

Bisphosphonates Alendronate 5-, 1 0-, 35-, 70-mg Postmenopausal osteoporosis or Take after an overnight fast with 70 for 70-mg... 

Ibandronate 2.5-, 150-mg Treatment or prevention of Same as alendronate except administer 76 for 150-mg... 

Rised ronate 5-, 35-mg tablet Osteoporosis or glucocorticoid-induced Same as alendronate 68 for 35-mg... 

The combination of a bisphosphonate with anabolic therapy (teriparatide) should not be used because a well-controlled trial showed that women receiving the combination actually had smaller increases in bone mineral density than women receiving teriparatide alone.44 However, sequential therapy with these agents may be more promising. In one study, women who received alendronate for 1 year directly after receiving parathyroid hormone for 1 year had greater... 

Compared with postmenopausal osteoporosis, few clinical trials have been conducted evaluating therapies in men. Although alendronate and calcitonin have both been studied, only alendronate reduces fracture rates in men. Teriparatide also has been studied, but no data are available yet on fracture rates. At this time, alendronate and teriparatide are approved by the FDA for the treatment of osteoporosis in men. Owing to proven benefit in reducing fractures and relative safety, alendronate should be considered first-line treatment for primary osteoporosis in men. Teriparatide should be reserved as alternate therapy in this population. 

In other studies, bisphosphonate-pamidronate or alendronate were linked to the terminal carboxylic acid of the stabilized dipeptide Pro-Phe to improve the bioavailability of bisphosphonates by hPepTl-mediated absorption. In-situ single-pass perfused rat intestine studies revealed competitive inhibition of transport by Pro-Phe, suggesting carrier-mediated transport. Oral administration of the dipeptidyl prodrugs resulted in a 3-fold increase in drug absorption following oral administration to rats. The authors suggested that oral bioavailability of bisphosphonates may be improved by PepTl-mediated absorption when administered as peptidyl prodrugs [53]. Future mechanistic studies may prove if hPepTl is involved in the absorption process. 

US patent 6,696,601, Hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof [102], New hydrate forms of alendronate sodium, having a water content of about 1-12%, and processes for their manufacture, are disclosed. New crystalline forms of alendronate sodium, and processes for manufacturing these, are also disclosed. These new forms of alendronate sodium are suitable for incorporation into pharmaceutical compositions for combating bone resorption in bone diseases. 

Alendronate, risedronate, and oral ibandronate are FDA approved for prevention and treatment of postmenopausal osteoporosis. IV ibandronate and zoledronic acid are indicated only for treatment of postmenopausal women. Risedronate and alendronate are also approved for male and glucocorticoid-induced osteoporosis. 

Alendronate (Fosamax, 5 mg daily, 35 mg weekly (prevention) to zero with food or beverage... 

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