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Details

Stereochemistry ACHIRAL
Molecular Formula C7H10NO7P2.Na.H2O
Molecular Weight 323.1094
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RISEDRONATE SODIUM MONOHYDRATE

SMILES

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

InChI

InChIKey=KLQNARDFMJRXSF-UHFFFAOYSA-M
InChI=1S/C7H11NO7P2.Na.H2O/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);;1H2/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
Osteoporosis in children and adolescent girls: case report of idiopathic juvenile osteoporosis and review of the literature.
2001 Aug
Risedronate for the prevention and treatment of postmenopausal osteoporosis: results from recent clinical trials.
2001 Dec
Risedronate pharmacokinetics and intra- and inter-subject variability upon single-dose intravenous and oral administration.
2001 Feb
Nitrogen-bisphosphonates block retinoblastoma phosphorylation and cell growth by inhibiting the cholesterol biosynthetic pathway in a keratinocyte model for esophageal irritation.
2001 Feb
Effect of risedronate on the risk of hip fracture in elderly women. Hip Intervention Program Study Group.
2001 Feb 1
Risedronate: a clinical review.
2001 Feb 12
Effect of high doses of oral risedronate (20 mg/day) on serum parathyroid hormone levels and urinary collagen cross-link excretion in postmenopausal women with spinal osteoporosis.
2001 Jan
(31)P NMR of apicomplexans and the effects of risedronate on Cryptosporidium parvum growth.
2001 Jun 15
Evidence-based medicine: putting theory into practice.
2001 Mar
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
2001 Mar 15
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
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
Alendronate for the treatment of osteoporosis in men.
2001 Oct
Maintenance of cancellous bone in ovariectomized, human parathyroid hormone [hPTH(1-84)]-treated rats by estrogen, risedronate, or reduced hPTH.
2001 Oct
Bisphosphonates for osteoporosis.
2001 Sep
Vgamma2Vdelta2 T-cell receptor-mediated recognition of aminobisphosphonates.
2001 Sep 1
Direct effects of bisphosphonates on breast cancer cells.
2002
[When osteoporosis first manifests itself. Without therapy the next fracture threatens].
2002 Apr 4
The efficacy and tolerability of risedronate once a week for the treatment of postmenopausal osteoporosis.
2002 Aug
Risedronate preserves trabecular architecture and increases bone strength in vertebra of ovariectomized minipigs as measured by three-dimensional microcomputed tomography.
2002 Jul
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
2002 Jul 4
Treatment of postmenopausal osteoporosis.
2002 Jun 8
Gateways to clinical trials.
2002 May
Risedronate: a new oral bisphosphonate.
2002 May
The potential of parathyroid hormone as a therapy for osteoporosis.
2002 May-Jun
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 MONOHYDRATE
Common Name English
RISEDRONIC ACID MONOSODIUM SALT MONOHYDRATE
Common Name English
PHOSPHONIC ACID, P,P'-(1-HYDROXY-2-(3-PYRIDINYL)ETHYLIDENE)BIS-, SODIUM SALT, HYDRATE (1:1:1)
Common Name English
Risedronate sodium monohydrate [WHO-DD]
Common Name English
Code System Code Type Description
PUBCHEM
23709605
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY
FDA UNII
F67L43UT5C
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY
DRUG BANK
DBSALT001516
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY
RXCUI
1356128
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY RxNorm
CAS
353228-19-0
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY
DAILYMED
F67L43UT5C
Created by admin on Sat Dec 16 03:14:01 GMT 2023 , Edited by admin on Sat Dec 16 03:14:01 GMT 2023
PRIMARY