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Identification
NameRisedronate
Accession NumberDB00884  (APRD00410, DB02782)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget’s disease of bone.

Structure
Thumb
Synonyms
Acide risédroniqe
Acido risedronico
Acidum risedronicum
Ridron
Risedronate
Risedronic acid
Risedronsäure
External Identifiers
  • NE-58095
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Actoneltablet5 mgoralWarner Chilcott Canada Co2000-07-25Not applicableCanada
Actoneltablet, film coated30 mg/1oralWarner Chilcott Pharmaceuticals Inc.1998-03-27Not applicableUs
Actoneltablet150 mgoralWarner Chilcott Canada Co2008-12-01Not applicableCanada
Actoneltablet30 mgoralWarner Chilcott Canada Co1999-09-07Not applicableCanada
Actoneltablet, film coated150 mg/1oralPhysicians Total Care, Inc.2009-10-05Not applicableUs
Actoneltablet, film coated35 mg/1oralPhysicians Total Care, Inc.2002-09-16Not applicableUs
Actoneltablet, film coated5 mg/1oralPhysicians Total Care, Inc.2002-03-15Not applicableUs
Actoneltablet, film coated150 mg/1oralWarner Chilcott Pharmaceuticals Inc.2008-04-22Not applicableUs
Actoneltablet75 mgoralWarner Chilcott Canada Co2007-08-13Not applicableCanada
Actoneltablet, film coated35 mg/1oralWarner Chilcott Pharmaceuticals Inc.2002-05-17Not applicableUs
Actoneltablet35 mgoralWarner Chilcott Canada Co2002-12-10Not applicableCanada
Actoneltablet, film coated5 mg/1oralWarner Chilcott Pharmaceuticals Inc.2000-04-14Not applicableUs
Actonel Drtablet (delayed-release)35 mgoralWarner Chilcott Canada Co2011-08-10Not applicableCanada
Auro-risedronatetablet150 mgoralAuro Pharma Inc2016-04-13Not applicableCanada
Auro-risedronatetablet30 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-risedronatetablet5 mgoralAuro Pharma IncNot applicableNot applicableCanada
Auro-risedronatetablet35 mgoralAuro Pharma Inc2013-07-08Not applicableCanada
Dom-risedronatetablet35 mgoralDominion Pharmacal2011-04-19Not applicableCanada
Jamp-risedronatetablet35 mgoralJamp Pharma Corporation2011-10-04Not applicableCanada
Mylan-risedronatetablet150 mgoralMylan Pharmaceuticals Ulc2013-09-30Not applicableCanada
Mylan-risedronatetablet35 mgoralMylan Pharmaceuticals Ulc2011-06-16Not applicableCanada
Ntp-risedronatetablet35 mgoralNt Pharma Canada LtdNot applicableNot applicableCanada
Ntp-risedronatetablet30 mgoralNt Pharma Canada LtdNot applicableNot applicableCanada
Ntp-risedronatetablet5 mgoralNt Pharma Canada LtdNot applicableNot applicableCanada
Pendo-risedronatetablet35 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
PHL-risedronatetablet35 mgoralPharmel IncNot applicableNot applicableCanada
PMS-risedronatetablet150 mgoralPharmascience Inc2014-05-28Not applicableCanada
PMS-risedronatetablet35 mgoralPharmascience Inc2010-07-27Not applicableCanada
Q-risedronatetablet35 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Ratio-risedronatetablet35 mgoralRatiopharm Inc Division Of Teva Canada Limited2010-07-272015-10-26Canada
Risedronatetablet30 mgoralSanis Health IncNot applicableNot applicableCanada
Risedronatetablet5 mgoralSanis Health IncNot applicableNot applicableCanada
Risedronatetablet35 mgoralSanis Health Inc2011-10-18Not applicableCanada
Risedronatetablet35 mgoralSivem Pharmaceuticals Ulc2011-04-08Not applicableCanada
Risedronatetablet35 mgoralPro Doc Limitee2010-10-15Not applicableCanada
Risedronate-35tablet35 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Riva-risedronatetablet35 mgoralLaboratoire Riva Inc2010-07-28Not applicableCanada
Sandoz Risedronatetablet35 mgoralSandoz Canada Incorporated2010-07-28Not applicableCanada
Teva-risedronatetablet35 mgoralTeva Canada Limited2010-01-27Not applicableCanada
Teva-risedronatetablet30 mgoralTeva Canada Limited2010-01-27Not applicableCanada
Teva-risedronatetablet5 mgoralTeva Canada Limited2010-01-27Not applicableCanada
Teva-risedronatetablet150 mgoralTeva Canada Limited2013-10-10Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-risedronatetablet150 mgoralApotex Inc2012-05-17Not applicableCanada
Apo-risedronatetablet35 mgoralApotex Inc2010-11-10Not applicableCanada
Risedronate Sodiumtablet, film coated75 mg/1oralMylan Pharmaceuticals Inc.2014-06-102016-01-07Us
Risedronate Sodiumtablet, film coated35 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Risedronate Sodiumtablet, film coated30 mg/1oralAurobindo Pharma Limited2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated5 mg/1oralAurobindo Pharma Limited2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated150 mg/1oralSun Pharma Global FZE2014-06-11Not applicableUs
Risedronate Sodiumtablet, film coated35 mg/1oralMylan Pharmaceuticals Inc.2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated35 mg/1oralApotex Corp.2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated75 mg/1oralSun Pharma Global FZE2014-06-11Not applicableUs
Risedronate Sodiumtablet, film coated150 mg/1oralMylan Pharmaceuticals Inc.2014-06-10Not applicableUs
Risedronate Sodiumtablet, film coated150 mg/1oralApotex Corp.2014-06-11Not applicableUs
Risedronate Sodiumtablet, film coated35 mg/1oralSun Pharma Global FZE2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated30 mg/1oralMylan Pharmaceuticals Inc.2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated75 mg/1oralApotex Corp.2014-06-11Not applicableUs
Risedronate Sodiumtablet, film coated30 mg/1oralSun Pharma Global FZE2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated5 mg/1oralMylan Pharmaceuticals Inc.2015-11-30Not applicableUs
Risedronate Sodiumtablet, film coated5 mg/1oralSun Pharma Global FZE2015-11-30Not applicableUs
Risedronate Sodiumtablet, delayed release35 mg/1oralTeva Pharmaceuticals USA Inc2015-05-18Not applicableUs
Risedronate Sodiumtablet, film coated30 mg/1oralMacleods Pharmaceuticals Limited2015-12-09Not applicableUs
Risedronate Sodiumtablet, film coated30 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Risedronate Sodiumtablet, film coated5 mg/1oralMacleods Pharmaceuticals Limited2015-12-09Not applicableUs
Risedronate Sodiumtablet, film coated5 mg/1oralTeva Pharmaceuticals USA Inc2015-06-01Not applicableUs
Risedronate Sodiumtablet, film coated35 mg/1oralAurobindo Pharma Limited2015-11-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BenetTakeda
Brand mixtures
NameLabellerIngredients
ActonelWarner Chilcott (US), LLC
Actonel Plus CalciumWarner Chilcott Canada Co
Actonel Sachet KitWarner Chilcott Canada Co
AtelviaWarner Chilcott (US), LLC
PMS-risedronate Plus CalciumPharmascience Inc
Risedronate SodiumActavis Pharma, Inc.
Salts
Name/CASStructureProperties
Risedronate sodium
Thumb
  • InChI Key: DRFDPXKCEWYIAW-UHFFFAOYNA-M
  • Monoisotopic Mass: 304.983019378
  • Average Mass: 305.0941
DBSALT000494
Risedronate sodium hemi-pentahydrate
ThumbNot applicableDBSALT001515
Risedronate sodium monohydrate
ThumbNot applicableDBSALT001516
Categories
UNIIKM2Z91756Z
CAS number105462-24-6
WeightAverage: 283.1123
Monoisotopic: 283.001074735
Chemical FormulaC7H11NO7P2
InChI KeyInChIKey=IIDJRNMFWXDHID-UHFFFAOYSA-N
InChI
InChI=1S/C7H11NO7P2/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)
IUPAC Name
[1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid
SMILES
OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as bisphosphonates. These are organic compounds containing two phosphonate groups linked together through a carbon atoms.
KingdomOrganic compounds
Super ClassOrganophosphorus compounds
ClassOrganic phosphonic acids and derivatives
Sub ClassBisphosphonates
Direct ParentBisphosphonates
Alternative Parents
Substituents
  • Bisphosphonate
  • Pyridine
  • Heteroaromatic compound
  • Organophosphonic acid
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis
PharmacodynamicsRisedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women.
Mechanism of actionThe 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. 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.
Related Articles
AbsorptionRapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract
Volume of distribution
  • 13.8 L/kg
Protein binding~24%
Metabolism

No evidence found for metabolization of risedronate in humans or mammals

Route of eliminationRisedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats.
Half life1.5 hours
Clearance
  • 122 mL/min
  • 73 mL/min [osteopenic postmenopausal women]
ToxicitySide effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Risedronate Action PathwayDrug actionSMP00112
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9357
Blood Brain Barrier+0.9172
Caco-2 permeable-0.6795
P-glycoprotein substrateNon-substrate0.6846
P-glycoprotein inhibitor INon-inhibitor0.9582
P-glycoprotein inhibitor IINon-inhibitor1.0
Renal organic cation transporterNon-inhibitor0.9542
CYP450 2C9 substrateNon-substrate0.8452
CYP450 2D6 substrateNon-substrate0.8162
CYP450 3A4 substrateNon-substrate0.7208
CYP450 1A2 substrateNon-inhibitor0.8778
CYP450 2C9 inhibitorNon-inhibitor0.8792
CYP450 2D6 inhibitorNon-inhibitor0.9062
CYP450 2C19 inhibitorNon-inhibitor0.8777
CYP450 3A4 inhibitorNon-inhibitor0.9068
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.989
Ames testNon AMES toxic0.7663
CarcinogenicityNon-carcinogens0.8386
BiodegradationNot ready biodegradable0.5058
Rat acute toxicity2.1053 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9095
hERG inhibition (predictor II)Non-inhibitor0.9303
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Warner chilcott co llc
  • Teva pharmaceuticals usa
  • Procter & Gamble
Packagers
Dosage forms
FormRouteStrength
Tabletoral150 mg
Tabletoral30 mg
Tabletoral35 mg
Tabletoral5 mg
Tabletoral75 mg
Tablet, film coatedoral150 mg/1
Tablet (delayed-release)oral35 mg
Granules (effervescents); kit; tabletoral
Tablet, delayed releaseoral
Tabletoral
Tablet, delayed releaseoral35 mg/1
Tablet, film coatedoral
Tablet, film coatedoral30 mg/1
Tablet, film coatedoral35 mg/1
Tablet, film coatedoral5 mg/1
Tablet, film coatedoral75 mg/1
Prices
Unit descriptionCostUnit
Actonel 150 mg tablet125.1USD tablet
Actonel 4 35 mg tablet Disp Pack119.43USD disp
Actonel 75 mg tablet54.83USD tablet
Actonel 30 mg tablet29.32USD tablet
Actonel 35 mg tablet28.75USD tablet
Actonel 5 mg tablet4.13USD tablet
Actonel with calcium tablet3.92USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2294595 No2001-08-212018-07-17Canada
CA2399976 No2007-03-272021-02-01Canada
US5994329 Yes1999-01-172019-01-17Us
US6015801 Yes1999-01-172019-01-17Us
US6096342 No1994-11-222011-11-22Us
US6165513 Yes1998-12-102018-12-10Us
US6432932 Yes1999-01-172019-01-17Us
US6465443 Yes1999-02-142019-02-14Us
US7192938 Yes2003-11-062023-11-06Us
US7645459 No2008-01-092028-01-09Us
US7645460 No2008-01-092028-01-09Us
US7718634 Yes2003-11-062023-11-06Us
US8246989 No2006-01-162026-01-16Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP-3.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility10.4 mg/mLALOGPS
logP-0.75ALOGPS
logP-3.3ChemAxon
logS-1.4ALOGPS
pKa (Strongest Acidic)0.68ChemAxon
pKa (Strongest Basic)4.91ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area148.18 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity57.12 m3·mol-1ChemAxon
Polarizability21.91 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Srinivasa Rao V.N Divvela, Lenin Racha, Sivakumaran Meenakshisunderam, Ramesh Dandala, “Process for the preparation of risedronate sodium hemi-pentahydrate.” U.S. Patent US20070173484, issued July 26, 2007.

US20070173484
General ReferencesNot Available
External Links
ATC CodesM05BA07M05BB02M05BB04M05BB07
AHFS Codes
  • 92:00.00
PDB Entries
FDA labelDownload (1.52 MB)
MSDSDownload (57 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Risedronate can be increased when combined with Acetaminophen.
Aluminum hydroxideThe serum concentration of Risedronate can be decreased when it is combined with Aluminum hydroxide.
AmikacinAmikacin may increase the activities of Risedronate.
AmobarbitalThe metabolism of Risedronate can be increased when combined with Amobarbital.
ArbekacinArbekacin may increase the activities of Risedronate.
Atracurium besylateRisedronate may increase the neuromuscular blocking activities of Atracurium besylate.
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Risedronate.
ButabarbitalThe metabolism of Risedronate can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Risedronate can be increased when combined with Butalbital.
CaffeineThe metabolism of Risedronate can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Risedronate can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Risedronate can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Risedronate can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Risedronate can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Risedronate can be decreased when used in combination with Calcium gluconate.
CimetidineThe serum concentration of Risedronate can be increased when it is combined with Cimetidine.
Cisatracurium besylateRisedronate may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe metabolism of Risedronate can be decreased when combined with Clarithromycin.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Risedronate.
DeferasiroxThe risk or severity of adverse effects can be increased when Risedronate is combined with Deferasirox.
DoxazosinDoxazosin may increase the hypotensive activities of Risedronate.
EfavirenzThe serum concentration of Risedronate can be decreased when it is combined with Efavirenz.
ErythromycinThe metabolism of Risedronate can be decreased when combined with Erythromycin.
EsomeprazoleThe therapeutic efficacy of Risedronate can be decreased when used in combination with Esomeprazole.
FamotidineThe serum concentration of Risedronate can be increased when it is combined with Famotidine.
FluconazoleThe serum concentration of Risedronate can be increased when it is combined with Fluconazole.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Risedronate.
FramycetinFramycetin may increase the activities of Risedronate.
GentamicinGentamicin may increase the activities of Risedronate.
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Risedronate.
Iron DextranThe serum concentration of Risedronate can be decreased when it is combined with Iron Dextran.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Risedronate.
KanamycinKanamycin may increase the activities of Risedronate.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Risedronate.
LansoprazoleThe therapeutic efficacy of Risedronate can be decreased when used in combination with Lansoprazole.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Risedronate is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Risedronate is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Risedronate is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Risedronate can be decreased when it is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Risedronate is combined with Magnesium salicylate.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Risedronate is combined with Magnesium Sulfate.
MethohexitalThe metabolism of Risedronate can be increased when combined with Methohexital.
NafcillinThe metabolism of Risedronate can be increased when combined with Nafcillin.
NeomycinNeomycin may increase the activities of Risedronate.
NetilmicinNetilmicin may increase the activities of Risedronate.
NitroprussideRisedronate may increase the hypotensive activities of Nitroprusside.
NizatidineThe serum concentration of Risedronate can be increased when it is combined with Nizatidine.
OmeprazoleThe therapeutic efficacy of Risedronate can be decreased when used in combination with Omeprazole.
PancuroniumRisedronate may increase the neuromuscular blocking activities of Pancuronium.
PantoprazoleThe therapeutic efficacy of Risedronate can be decreased when used in combination with Pantoprazole.
PentobarbitalThe metabolism of Risedronate can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Risedronate can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Risedronate.
PhentolaminePhentolamine may increase the hypotensive activities of Risedronate.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Risedronate.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Risedronate.
PrazosinPrazosin may increase the hypotensive activities of Risedronate.
RabeprazoleThe therapeutic efficacy of Risedronate can be decreased when used in combination with Rabeprazole.
RanitidineThe serum concentration of Risedronate can be increased when it is combined with Ranitidine.
RibostamycinRibostamycin may increase the activities of Risedronate.
RifabutinThe serum concentration of Risedronate can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Risedronate can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Risedronate can be decreased when it is combined with Rifapentine.
RocuroniumRisedronate may increase the neuromuscular blocking activities of Rocuronium.
SecobarbitalThe metabolism of Risedronate can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Risedronate.
SpectinomycinSpectinomycin may increase the activities of Risedronate.
StreptomycinStreptomycin may increase the activities of Risedronate.
SulfisoxazoleThe metabolism of Risedronate can be decreased when combined with Sulfisoxazole.
TamsulosinTamsulosin may increase the hypotensive activities of Risedronate.
TelithromycinThe metabolism of Risedronate can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Risedronate.
TobramycinTobramycin may increase the activities of Risedronate.
VecuroniumRisedronate may increase the neuromuscular blocking activities of Vecuronium.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Risedronate.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Poly(a) rna binding
Specific Function:
Key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate (FPP), a precursor for several classes of essential metabolites including sterols, dolichols, carotenoids, and ubiquinones. FPP also serves as substrate for protein farnesylation and geranylgeranylation. Catalyzes the sequential condensation of isopentenyl pyrophosphate with the allylic pyrophosphates, d...
Gene Name:
FDPS
Uniprot ID:
P14324
Molecular Weight:
48275.03 Da
References
  1. Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G: Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [PubMed:10620343 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Coxon FP, Ebetino FH, Mules EH, Seabra MC, McKenna CE, Rogers MJ: Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo. Bone. 2005 Sep;37(3):349-58. [PubMed:16006204 ]
  4. Dunford JE, Thompson K, Coxon FP, Luckman SP, Hahn FM, Poulter CD, Ebetino FH, Rogers MJ: Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42. [PubMed:11160603 ]
  5. Ortiz-Gomez A, Jimenez C, Estevez AM, Carrero-Lerida J, Ruiz-Perez LM, Gonzalez-Pacanowska D: Farnesyl diphosphate synthase is a cytosolic enzyme in Leishmania major promastigotes and its overexpression confers resistance to risedronate. Eukaryot Cell. 2006 Jul;5(7):1057-64. [PubMed:16835450 ]
  6. Russell RG, Xia Z, Dunford JE, Oppermann U, Kwaasi A, Hulley PA, Kavanagh KL, Triffitt JT, Lundy MW, Phipps RJ, Barnett BL, Coxon FP, Rogers MJ, Watts NB, Ebetino FH: Bisphosphonates: an update on mechanisms of action and how these relate to clinical efficacy. Ann N Y Acad Sci. 2007 Nov;1117:209-57. [PubMed:18056045 ]
Kind
Small molecule
Organism
Human
Pharmacological action
yes
Actions
antagonist
References
  1. Jahnke W, Henry C: An in vitro assay to measure targeted drug delivery to bone mineral. ChemMedChem. 2010 May 3;5(5):770-6. doi: 10.1002/cmdc.201000016. [PubMed:20209564 ]
  2. Nancollas GH, Tang R, Phipps RJ, Henneman Z, Gulde S, Wu W, Mangood A, Russell RG, Ebetino FH: Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite. Bone. 2006 May;38(5):617-27. Epub 2005 Jul 20. [PubMed:16046206 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Valenti MT, Giannini S, Donatelli L, Zanatta M, Bertoldo F, Sella S, Vilei MT, Ossi E, Realdi G, Lo Cascio V, Dalle Carbonare L: The effect of risedronate on osteogenic lineage is mediated by cyclooxygenase-2 gene upregulation. Arthritis Res Ther. 2010;12(4):R163. doi: 10.1186/ar3122. Epub 2010 Aug 25. [PubMed:20738860 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on June 27, 2016 03:07