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Details

Stereochemistry ACHIRAL
Molecular Formula C7H10NO7P2.Na
Molecular Weight 305.0941
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RISEDRONATE SODIUM

SMILES

[Na+].OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)([O-])=O

InChI

InChIKey=DRFDPXKCEWYIAW-UHFFFAOYSA-M
InChI=1S/C7H11NO7P2.Na/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6;/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15);/q;+1/p-1

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including: https://www.drugs.com/mtm/risedronate.html http://www.wikidoc.org/index.php/Risedronate http://www.rxlist.com/actonel-drug.htm

Risedronic acid is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism. The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. It is FDA approved for the treatment of postmenopausal osteoporosis, osteoporosis in men, glucocorticoid-induced osteoporosis and Paget’s disease. Calcium, antacids, or oral medications containing divalent cations interfere with the absorption of Risedronic acid. Common adverse reactions include rash, abdominal pain, constipation, diarrhea, indigestion, nausea, backache, urinary tract infectious disease and influenza-like illness.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ACTONEL

Approved Use

ACTONEL is indicated for the treatment and prevention of osteoporosis and Paget’s disease of bone in men and women.

Launch Date

1998
Primary
ACTONEL

Approved Use

ACTONEL is indicated for the treatment and prevention of glucocorticoid-induced osteoporosis in men and women who are either initiating or continuing systemic glucocorticoid treatment (daily dosage of ≥ 7.5 mg prednisone or equivalent) for chronic diseases.

Launch Date

1998
Primary
ACTONEL

Approved Use

ACTONEL is indicated for treatment of Paget’s disease of bone in men and women.

Launch Date

1998
Primary
ACTONEL

Approved Use

ACTONEL is indicated for treatment to increase bone mass in men with osteoporosis.

Launch Date

1998
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.05 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RISEDRONATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6.49 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RISEDRONATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.61 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RISEDRONATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.362
unhealthy, 41.6±15.7
n = 60
Health Status: unhealthy
Condition: Glucocorticoid-induced bone mineral density loss prevention
Age Group: 41.6±15.7
Sex: M+F
Population Size: 60
Sources: Page: p.362
Disc. AE: Skin rash, Gastrointestinal upset...
AEs leading to
discontinuation/dose reduction:
Skin rash (1.7%)
Gastrointestinal upset (1.7%)
Sources: Page: p.362
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 613
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 613
Sources: Page: p.9
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (0.3%)
Sources: Page: p.9
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 616
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 616
Sources: Page: p.9
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.2%)
Sources: Page: p.9
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 616
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 616
Sources: Page: p.9
Disc. AE: Vomiting, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Vomiting (1%)
Diarrhea (1%)
Sources: Page: p.9
150 mg 1 times / month multiple, oral
Recommended
Dose: 150 mg, 1 times / month
Route: oral
Route: multiple
Dose: 150 mg, 1 times / month
Sources: Page: p.10
unhealthy, 50 - 88
n = 650
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 650
Sources: Page: p.10
Disc. AE: Abdominal pain upper, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Abdominal pain upper (2.5%)
Diarrhea (0.8%)
Vomiting (0.3%)
Sources: Page: p.10
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.10
unhealthy, 50 - 88
n = 642
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 642
Sources: Page: p.10
Disc. AE: Abdominal pain upper, Vomiting...
AEs leading to
discontinuation/dose reduction:
Abdominal pain upper (1.4%)
Vomiting (0.3%)
Sources: Page: p.10
AEs

AEs

AESignificanceDosePopulation
Gastrointestinal upset 1.7%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.362
unhealthy, 41.6±15.7
n = 60
Health Status: unhealthy
Condition: Glucocorticoid-induced bone mineral density loss prevention
Age Group: 41.6±15.7
Sex: M+F
Population Size: 60
Sources: Page: p.362
Skin rash 1.7%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.362
unhealthy, 41.6±15.7
n = 60
Health Status: unhealthy
Condition: Glucocorticoid-induced bone mineral density loss prevention
Age Group: 41.6±15.7
Sex: M+F
Population Size: 60
Sources: Page: p.362
Diarrhea 0.3%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 613
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 613
Sources: Page: p.9
Vomiting 0.2%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 616
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 616
Sources: Page: p.9
Diarrhea 1%
Disc. AE
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 616
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 616
Sources: Page: p.9
Vomiting 1%
Disc. AE
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources: Page: p.9
unhealthy, 50 - 86
n = 616
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 86
Sex: F
Population Size: 616
Sources: Page: p.9
Vomiting 0.3%
Disc. AE
150 mg 1 times / month multiple, oral
Recommended
Dose: 150 mg, 1 times / month
Route: oral
Route: multiple
Dose: 150 mg, 1 times / month
Sources: Page: p.10
unhealthy, 50 - 88
n = 650
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 650
Sources: Page: p.10
Diarrhea 0.8%
Disc. AE
150 mg 1 times / month multiple, oral
Recommended
Dose: 150 mg, 1 times / month
Route: oral
Route: multiple
Dose: 150 mg, 1 times / month
Sources: Page: p.10
unhealthy, 50 - 88
n = 650
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 650
Sources: Page: p.10
Abdominal pain upper 2.5%
Disc. AE
150 mg 1 times / month multiple, oral
Recommended
Dose: 150 mg, 1 times / month
Route: oral
Route: multiple
Dose: 150 mg, 1 times / month
Sources: Page: p.10
unhealthy, 50 - 88
n = 650
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 650
Sources: Page: p.10
Vomiting 0.3%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.10
unhealthy, 50 - 88
n = 642
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 642
Sources: Page: p.10
Abdominal pain upper 1.4%
Disc. AE
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources: Page: p.10
unhealthy, 50 - 88
n = 642
Health Status: unhealthy
Condition: Postmenopausal osteoporosis
Age Group: 50 - 88
Sex: F
Population Size: 642
Sources: Page: p.10
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Hormone replacement therapy and prevention of vertebral fractures: a meta-analysis of randomised trials.
2001
Risedronate: a review of its pharmacological properties and clinical use in resorptive bone disease.
2001
Anabolic agents for treating postmenopausal osteoporosis.
2001 Dec
Inhibition of bone resorption by alendronate and risedronate does not require osteoclast apoptosis.
2001 Dec
[Therapy of osteoporosis. Risk factors alone are not an indication].
2001 Dec 6
Risedronate pharmacokinetics and intra- and inter-subject variability upon single-dose intravenous and oral administration.
2001 Feb
[Fluorides and bisphosphonates in the treatment of osteoporosis].
2001 Jul
Role of bisphosphonates and calcitonin in the prevention and treatment of osteoporosis.
2001 Jul
[Bisphosphonate treatment prevents hip fractures in 70-79 year old women with osteoporotic vertebral fractures].
2001 Jul 14
Ocular adverse effects of alendronic acid.
2001 Jun
(31)P NMR of apicomplexans and the effects of risedronate on Cryptosporidium parvum growth.
2001 Jun 15
Risedronate: clinical usage.
2001 May
[Therapy of osteoporosis from the viewpoint of evidence-based medicine].
2001 May 15
Absolute vs. relative numbers in evaluating drug therapy.
2001 May 15
[Bisphosphonates in osteoporosis. Significantly reduces risk of fracture].
2001 May 3
The effect of risedronate on the risk of hip fracture in elderly women.
2001 May 31
The effect of risedronate on the risk of hip fracture in elderly women.
2001 May 31
The effect of risedronate on the risk of hip fracture in elderly women.
2001 May 31
[Alternatives to hormonal treatment for the prevention of postmenopausal osteoporosis: the bisphosphonates].
2001 Nov
Bisphosphonate treatment suppresses not only stochastic remodeling but also the targeted repair of microdamage.
2001 Nov
The role of serial bone mineral density testing for osteoporosis.
2001 Nov
Role of alendronate and risedronate in preventing and treating osteoporosis.
2001 Nov
A method to assess the proportion of treatment effect explained by a surrogate endpoint.
2001 Nov 15
[Economic aspects of osteoporosis therapy. What does a prevented fracture cost?].
2001 Nov 22
Risedronate treatment and extended fracture protection in postmenopausal women.
2001 Nov-Dec
Risedronate increases bone density and reduces vertebral fracture risk within one year in men on corticosteroid therapy.
2001 Oct
Alendronate for the treatment of osteoporosis in men.
2001 Oct
Paget's disease of the spine and its management.
2001 Oct
Maintenance of cancellous bone in ovariectomized, human parathyroid hormone [hPTH(1-84)]-treated rats by estrogen, risedronate, or reduced hPTH.
2001 Oct
Nitrogen-containing bisphosphonates induce apoptosis of Caco-2 cells in vitro by inhibiting the mevalonate pathway: a model of bisphosphonate-induced gastrointestinal toxicity.
2001 Oct
[Osteoporosis. Fracture as alarm signal].
2001 Oct 11
Pharmacologic therapy for the treatment and prevention of osteoporosis.
2001 Sep
Vgamma2Vdelta2 T-cell receptor-mediated recognition of aminobisphosphonates.
2001 Sep 1
Evaluation and treatment of postmenopausal osteoporosis.
2001 Sep 25
Risedronate reduces the risk of first vertebral fracture in osteoporotic women.
2002
The underuse of therapy in the secondary prevention of hip fractures.
2002
Development of bisphosphonates.
2002
Direct effects of bisphosphonates on breast cancer cells.
2002
[Osteoporosis - Evidence based therapy].
2002 Apr
Risedronate for the prevention of fractures in postmenopausal osteoporosis.
2002 Apr
Therapies to improve bone mineral density and reduce the risk of fracture: clinical trial results.
2002 Jan
Risedronate preserves trabecular architecture and increases bone strength in vertebra of ovariectomized minipigs as measured by three-dimensional microcomputed tomography.
2002 Jul
Sequential treatment with basic fibroblast growth factor and PTH is more efficacious than treatment with PTH alone for increasing vertebral bone mass and strength in osteopenic ovariectomized rats.
2002 Jul
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
2002 Jul 4
[Risedronate: clinical usage].
2002 Mar
Risedronate for the prevention and treatment of corticosteroid-induced osteoporosis.
2002 Mar
Upper gastrointestinal tract safety of risedronate: a pooled analysis of 9 clinical trials.
2002 Mar
[Risedronate, a new diphosphonate in osteoporosis and Paget's disease].
2002 Mar 2
The cost utility of bisphosphonate treatment in established osteoporosis.
2002 May
Do bisphosphonates reduce the risk of osteoporotic fractures? An evaluation of the evidence to date.
2002 May 28
Patents

Sample Use Guides

Treatment of Postmenopausal Osteoporosis: 5 mg daily, 35 mg once-a-week, 75 mg two consecutive days each month, 150 mg once-a-month. Prevention of Postmenopausal Osteoporosis: 5 mg daily, 35 mg once-a-week. Men with Osteoporosis: 35 mg once-a-week. Glucocorticoid-Induced Osteoporosis: 5 mg daily. Paget’s Disease: 30 mg daily for 2 month.
Route of Administration: Oral
The antimalarial activities of risedronate, one of the most potent bisphosphonates clinically used to treat bone resorption diseases, against blood stages of Plasmodium falciparum (50% inhibitory concentration [IC50] of 20.3±1.0 μM).
Name Type Language
RISEDRONATE SODIUM ANHYDROUS
Preferred Name English
RISEDRONATE SODIUM
MART.   ORANGE BOOK   USAN   USP   VANDF   WHO-DD  
USAN  
Official Name English
RISEDRONATE SODIUM [USP-RS]
Common Name English
Risedronate sodium [WHO-DD]
Common Name English
NSC-722598
Code English
NSC-759280
Code English
RISEDRONATE SODIUM [MART.]
Common Name English
NE-58095 ANHYDROUS
Code English
RISEDRONATE SODIUM [ORANGE BOOK]
Common Name English
PHOSPHONIC ACID, (1-HYDROXY-2-(3-PYRIDINYL)ETHYLIDENE)BIS-, MONOSODIUM SALT
Common Name English
RISEDRONATE SODIUM [VANDF]
Common Name English
RISEDRONATE MONOSODIUM
Common Name English
RISEDRONIC ACID MONOSODIUM SALT [MI]
Common Name English
RISEDRONATE SODIUM [USAN]
Common Name English
RISEDRONATE SODIUM [USP MONOGRAPH]
Common Name English
Sodium trihydrogen [1-hydroxy-2-(3-pyridyl)ethylidene]diphosphonate
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C443
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
NCI_THESAURUS C67439
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
FDA ORPHAN DRUG 229106
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
Code System Code Type Description
PUBCHEM
68739
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
ChEMBL
CHEMBL923
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
NCI_THESAURUS
C1528
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
NSC
722598
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
USAN
AA-96
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
EPA CompTox
DTXSID1046132
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
EVMPD
SUB04252MIG
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
SMS_ID
100000092051
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
EVMPD
SUB129792
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
DRUG BANK
DBSALT000494
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
RXCUI
60334
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY RxNorm
DAILYMED
OFG5EXG60L
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
FDA UNII
OFG5EXG60L
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
CAS
115436-72-1
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
NSC
759280
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
RS_ITEM_NUM
1604610
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY
MERCK INDEX
m9630
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
PRIMARY Merck Index
RXCUI
1926958
Created by admin on Fri Dec 15 15:55:18 GMT 2023 , Edited by admin on Fri Dec 15 15:55:18 GMT 2023
ALTERNATIVE