W. Jeal et al., ALENDRONATE - A REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC EFFICACY IN POSTMENOPAUSAL OSTEOPOROSIS, Drugs, 53(3), 1997, pp. 415-434
Alendronate is an aminobisphosphonate which appears to attenuate, rath
er than completely inhibiting bone turnover by suppressing the activit
y of osteoclasts. Clinical trials have established that 10 mg/day oral
ly administered alendronate is the optimum dosage. Despite its poor bi
oavailability after oral administration, alendronate is highly effecti
ve at preventing bone loss associated with the absence of endogenous e
strogen. A sustained increase in bone mass was observed during alendro
nate therapy without accelerated loss after withdrawal of the drug. In
creased bone mass was associated with a reduction in the risk and rate
of occurrence of vertebral fractures. A recent study demonstrated a 4
7% reduction in the risk of developing new radiographic vertebral frac
tures over 3 years in women with low bone mass and pre-existing verteb
ral fractures. There have been few direct comparisons in clinical tria
ls. However; when compared with calcium or low dosages of salmon calci
tonin (salcatonin) therapy in women with postmenopausal osteoporosis,
alendronate induced a sustained increase in bone mass during therapy t
hat was not seen with the comparator: In clinical trials alendronate w
as generally well tolerated when taken as recommended. Adverse events
tended to be transient and usually associated with the upper gastroint
estinal tract; the most common events included abdominal pain, nausea,
dyspepsia, constipation and diarrhoea, which are also common with oth
er bisphosphonates. Of potential concern are the small number of repor
ts of patients developing oesophageal ulceration; however this adverse
event was attributed to noncompliance with rite manufacturer's recomm
endations for administration of the drug. In addition, alendronate has
nor been associated with osteomalacia. Studies are still required to
establish the long term efficacy of alendronate, particularly with reg
ard to other available therapies. Although estrogen replacement therap
y is generally considered the treatment of choice for the management o
f postmenopausal osteoporosis, many women are unable or unwilling to r
eceive estrogens on a long term basis. Thus, alendronate, with its dem
onstrated beneficial effects and its good, tolerability profile (when
taken as recommended), is a promising alternative treatment option for
the management of postmenopausal osteoporosis.