ALENDRONATE SODIUM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ALENDRONATE SODIUM (UNII: 2UY4M2U3RA) (ALENDRONIC ACID - UNII:X1J18R4W8P)

Available from:

Actavis Pharma, Inc.

INN (International Name):

ALENDRONATE SODIUM

Composition:

ALENDRONIC ACID 5 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ALENDRONATE SODIUM- ALENDRONATE SODIUM TABLET
ACTAVIS PHARMA, INC.
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ALENDRONATE SODIUM TABLETS, USP
ALENDRONATE SODIUM TABLETS, USP
Revised: April 2011
RX ONLY
DESCRIPTION
Alendronate sodium is a bisphosphonate that acts as a specific
inhibitor of osteoclast-mediated bone
resorption. Bisphosphonates are synthetic analogs of pyrophosphate
that bind to the hydroxyapatite
found in bone.
Alendronate sodium is chemically described as
(4-amino-1-hydroxybutylidene) bisphosphonic acid
monosodium salt trihydrate.
The empirical formula of alendronate sodium is C H NNaO P •3H O and
its formula weight is
325.12. The structural formula is:
Alendronate sodium is a white, crystalline, nonhygroscopic powder. It
is soluble in water, very slightly
soluble in alcohol, and practically insoluble in chloroform.
Each tablet, for oral administration contains: 6.53, 13.05, 45.68.
52.21 or 91.37 mg of alendronate
monosodium salt trihydrate, which is the molar equivalent of 5, 10,
35, 40 and 70 mg, respectively, of
free acid, and the following inactive ingredients: magnesium stearate,
mannitol, microcrystalline
cellulose, sodium starch glycolate and starch.
CLINICAL PHARMACOLOGY
_MECHANISM OF ACTION_
Animal studies have indicated the following mode of action. At the
cellular level, alendronate shows
preferential localization to sites of bone resorption, specifically
under osteoclasts. The osteoclasts
adhere normally to the bone surface but lack the ruffled border that
is indicative of active resorption.
Alendronate does not interfere with osteoclast recruitment or
attachment, but it does inhibit osteoclast
activity. Studies in mice on the localization of radioactive
[3H]alendronate in bone showed about 10-
fold higher uptake on osteoclast surfaces than on osteoblast surfaces.
Bones examined 6 and 49 days
after [3H]alendronate administration in rats and mice, respectively,
showed that normal bone was formed
on top of the alendronate, which was incorporated inside the matrix.
While incorporated in bone matrix,
4
21
7
2
2
alendron