Overview
| Generic Names: | Acide Alendronique [INN-French]; Acido Alendronico [INN-Spanish]; Acidum Alendronicum [INN-Latin]; Alendronate Sodium; Alendronic acid |
|---|---|
| Trade Names: | Adronat; Alendros; Arendal; Fosamax; Onclast |
| PharmGKB Accession Id: | PA448082 |
Description
A nonhormonal medication for the treatment of postmenopausal osteoporosis in women. This drug builds healthy bone, restoring some of the bone loss as a result of osteoporosis. PubChem (source: Drug Bank)
Indication
For the treatment and prevention of osteoporosis in women and Paget's disease of bone in both men and women. (source: Drug Bank)
ATC Therapeutic Category
- M05BA:Bisphosphonates
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The action of Alendronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Alendronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. (source: Drug Bank)
Pharmacology
Alendronate, a second-generation bisphosphonate is the first member of a group of drugs which strengthens bone. Alendronate is used to reduce hypercalcemia in tumor-induced bone disease, to treat corticosteroid-induced osteoporosis and Paget's disease, and to prevent osteoporosis in postmenopausal women. (source: Drug Bank)
Food Interactions
Take with a full glass of water Take 30-60 minutes before breakfast. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
There is no evidence that alendronate is metabolized in humans or animals. (source: Drug Bank)
Protein Binding
78% (source: Drug Bank)
Absorption
Relative to an intravenous (IV) reference dose, the mean oral bioavailability of alendronate in women was 0.7% for doses ranging from 5 to 40 mg when administered after an overnight fast and two hours before a standardized breakfast. Oral bioavailability of the 10 mg tablet in men (0.59%) was similar to that in women (0.78%) when administered after an overnight fast and 2 hours before breakfast. (source: Drug Bank)
Toxicity
Alendronate can damage the esophagus both by toxicity from the medication itself and by nonspecific irritation secondary to contact between the pill and the esophageal mucosa, similar to other cases of "pill esophagitis." (source: Drug Bank)
Isomeric SMILES Code:
C(CC(O)(P(=O)(O)O)P(=O)(O)O)CN (source: Drug Bank)
Curated Annotations (
)
-
rs2297480
at chr1:153546106
in
FDPS,
PKLR
This variant impacted the response to long-term N-bisphosphonates treatment in a study of 234 Danish postmenopausal women. Patients with the homozygous CC genotype showed a decreased response of bone turnover markers to amino-bisphosphonate therapy.- Related Drugs:
- alendronate, ibandronate, pamidronate, risedronate, zoledronate
- Related Diseases:
- Osteoporosis, Osteoporosis, Postmenopausal
- Evidence:
-
PMID:18687167
-
rs1544411
at chr7:10786072
This variant is associated with alendronate response in Caucasian (Italian) postmenopausal women, with bb genotype associated with lower increase in bone mineral density (BMD) after bisphosphonate treatments. BsmI VDR genotypes influenced the efficacy of antiresorptive drugs particularly when used in combination.- Variant Name:
- VDR: BsmI
- Related Drugs:
- alendronate, calcium, raloxifene
- Related Diseases:
- Osteoporosis, Osteoporosis, Postmenopausal
- Evidence:
-
PMID:15739035
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ESR2 |
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Publications |
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FDFT1 |
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Publications |
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FDPS |
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Publications, Variants |
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PKLR |
|
Variants |
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VDR |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| FDPS |
|
(source: Drug Bank) |
| PTPN4 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Hypercalcemia |
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Publications |
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Osteogenesis Imperfecta |
|
Publications |
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Osteoporosis |
|
Publications, Variants |
|
|
Osteoporosis, Postmenopausal |
|
Publications, Variants |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
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Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.