alendronic acid indications/contra

Stem definitionDrug idCAS RN
calcium metabolism regulator, pharmaceutical aid 112 66376-36-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alendronate monosodium salt trihydrate
  • alendronate sodium trihydrate
  • alendronate sodium hydrate
  • alendronate
  • alendronic acid
  • alendronate sodium
  • aminohydroxybutane bisphosphonate
  • MK-217
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.
  • Molecular weight: 249.10
  • Formula: C4H13NO7P2
  • CLOGP: -5.64
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 6
  • TPSA: 161.31
  • ALOGS: -1.17
  • ROTB: 5

Drug dosage:

DoseUnitRoute
10 mg O
10 mg O
10 mg O
10 mg O

Approvals:

DateAgencyCompanyOrphan
Sept. 29, 1995 FDA MERCK AND CO INC

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Femur fracture 22421.10 29.17 3838 10751 3550 3367720
Osteonecrosis 11340.02 29.17 2319 12270 8580 3362690
Osteoarthritis 8691.29 29.17 1762 12827 6008 3365262
Fall 8299.60 29.17 2514 12075 56369 3314901
Low turnover osteopathy 7565.51 29.17 1192 13397 57 3371213
Osteonecrosis of jaw 6942.98 29.17 1545 13044 8951 3362319
Gastrooesophageal reflux disease 5546.25 29.17 1315 13274 10376 3360894
Osteomyelitis 5010.55 29.17 1041 13548 3999 3367271
Impaired healing 4865.96 29.17 1075 13514 5873 3365397
Intramedullary rod insertion 4718.76 29.17 743 13846 20 3371250
Tooth disorder 4706.89 29.17 974 13615 3640 3367630
Hypertension 4464.83 29.17 1429 13160 37037 3334233
Stress fracture 4464.67 29.17 769 13820 595 3370675
Osteoporosis 4195.43 29.17 891 13698 3874 3367396
Arthralgia 4188.40 29.17 1527 13062 59334 3311936
Hyperlipidaemia 4077.56 29.17 866 13723 3762 3367508
Depression 4049.79 29.17 1339 13250 38431 3332839
Dental caries 3976.64 29.17 760 13829 1633 3369637
Anxiety 3688.67 29.17 1248 13341 38381 3332889
Pain in extremity 3647.58 29.17 1307 13282 47905 3323365
Osteopenia 3600.16 29.17 688 13901 1472 3369798
Spinal osteoarthritis 3550.76 29.17 685 13904 1574 3369696
Back pain 3405.20 29.17 1164 13425 36841 3334429
Foot fracture 3167.65 29.17 650 13939 2272 3368998
Fracture nonunion 3046.08 29.17 498 14091 143 3371127
Bursitis 3043.93 29.17 598 13991 1561 3369709
Vitamin D deficiency 3039.38 29.17 579 14010 1202 3370068
Bone disorder 2913.52 29.17 649 13940 3640 3367630
Intervertebral disc degeneration 2910.32 29.17 573 14016 1517 3369753
Arthropathy 2789.34 29.17 701 13888 7050 3364220

Pharmacologic Action:

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SourceCodeDescription
ATC M05BA04 MUSCULO-SKELETAL SYSTEM
DRUGS FOR TREATMENT OF BONE DISEASES
DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
Bisphosphonates
ATC M05BB03 MUSCULO-SKELETAL SYSTEM
DRUGS FOR TREATMENT OF BONE DISEASES
DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
Bisphosphonates, combinations
ATC M05BB05 MUSCULO-SKELETAL SYSTEM
DRUGS FOR TREATMENT OF BONE DISEASES
DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
Bisphosphonates, combinations
ATC M05BB06 MUSCULO-SKELETAL SYSTEM
DRUGS FOR TREATMENT OF BONE DISEASES
DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION
Bisphosphonates, combinations
FDA EPC N0000175579 Bisphosphonate
FDA Chemical/Ingredient N0000007707 Diphosphonates
CHEBI has role CHEBI:50646 bone density conservation agent
MeSH PA D050071 Bone Density Conservation Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Osteitis deformans indication 2089002 DOID:5408
Postmenopausal osteoporosis indication 102447009
Prevention of Glucocorticoid-Induced Osteoporosis indication
Glucocorticoid Induced Osteoporosis indication
Hypogonadal Osteoporosis in Males indication
Gastritis contraindication 4556007 DOID:4029
Hypocalcemia contraindication 5291005
Esophagitis contraindication 16761005 DOID:11963
Hyperphosphatemia contraindication 20165001 DOID:0050459
Hypervitaminosis D contraindication 27712000 DOID:9971
Ulcer of esophagus contraindication 30811009
Sarcoidosis contraindication 31541009 DOID:13404
Vitamin D deficiency contraindication 34713006
Dysphagia contraindication 40739000
Achalasia of esophagus contraindication 45564002 DOID:9164
Atrial fibrillation contraindication 49436004 DOID:0060224
Joint pain contraindication 57676002
Acute nephropathy contraindication 58574008
Stricture of esophagus contraindication 63305008
Hypercalcemia contraindication 66931009 DOID:12678
Fracture of femur contraindication 71620000
Duodenitis contraindication 72007001 DOID:8643
Kidney disease contraindication 90708001 DOID:2527
Kidney stone contraindication 95570007
Bed-ridden contraindication 160685001
Acute peptic ulcer contraindication 196682000
Esophageal dysmotility contraindication 266434009 DOID:9192
Arteriosclerosis obliterans contraindication 361133006 DOID:5160
Aseptic necrosis of bone of jaw contraindication 441809006
Esophageal Obstruction contraindication
High Grade Dysplasia associated with Barrett's Esophagus contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.27 acidic
pKa2 5.34 acidic
pKa3 6.32 acidic
pKa4 10.39 acidic
pKa5 12.82 acidic
pKa6 10.98 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 70MG BASE FOSAMAX PLUS D MERCK N021762 April 7, 2005 RX TABLET ORAL 5994329 July 17, 2018 TREATMENT OF OSTEOPOROSIS IN POST MENOPAUSAL WOMEN AND/OR THE TREATMENT TO INCREASE BONE MASS IN MEN WITH OSTEOPOROSIS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Farnesyl pyrophosphate synthase Enzyme INHIBITOR Ki 7.35 CHEMBL CHEMBL
Protein farnesyltransferase subunit beta Enzyme IC50 7.30 WOMBAT-PK
Farnesyl pyrophosphate synthase Enzyme Ki 7.02 CHEMBL

External reference:

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IDSource
4020932 VUID
N0000148414 NUI
C0102118 UMLSCUI
3141 IUPHAR_LIGAND_ID
D00939 KEGG_DRUG
CHEMBL675 ChEMBL_ID
2UY4M2U3RA UNII
121268-17-5 SECONDARY_CAS_RN
DB00630 DRUGBANK_ID
CHEMBL870 ChEMBL_ID
2088 PUBCHEM_CID
236083 RXNORM
421552005 SNOMEDCT_US
391730008 SNOMEDCT_US
005056 NDDF
CHEBI:2567 CHEBI
6462 INN_ID
D019386 MESH_DESCRIPTOR_UI
212 PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
FOSAMAX HUMAN PRESCRIPTION DRUG LABEL 1 0006-0031 TABLET 70 mg ORAL NDA 18 sections
FOSAMAX PLUS D HUMAN PRESCRIPTION DRUG LABEL 2 0006-0270 TABLET 70 mg ORAL NDA 18 sections
FOSAMAX PLUS D HUMAN PRESCRIPTION DRUG LABEL 2 0006-0710 TABLET 70 mg ORAL NDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-5140 TABLET 5 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-5141 TABLET 10 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-5142 TABLET 40 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-5171 TABLET 70 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-5172 TABLET 35 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-1676 TABLET 5 mg ORAL ANDA 19 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-1678 TABLET 10 mg ORAL ANDA 19 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-1679 TABLET 35 mg ORAL ANDA 19 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-1680 TABLET 40 mg ORAL ANDA 19 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-1681 TABLET 70 mg ORAL ANDA 19 sections
Binosto HUMAN PRESCRIPTION DRUG LABEL 1 0178-0101 TABLET, EFFERVESCENT 70 mg ORAL NDA 17 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-3566 TABLET 5 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-3567 TABLET 10 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-3568 TABLET 35 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-3569 TABLET 70 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0591-3169 TABLET 5 mg ORAL ANDA 13 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0591-3170 TABLET 10 mg ORAL ANDA 13 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0591-3171 TABLET 35 mg ORAL ANDA 13 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0591-3172 TABLET 40 mg ORAL ANDA 13 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0591-3173 TABLET 70 mg ORAL ANDA 13 sections
alendronate sodium HUMAN PRESCRIPTION DRUG LABEL 1 16252-599 TABLET 35 mg ORAL ANDA 18 sections
alendronate sodium HUMAN PRESCRIPTION DRUG LABEL 1 16252-601 TABLET 70 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 16714-631 TABLET 10 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 16714-632 TABLET 35 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 16714-633 TABLET 70 mg ORAL ANDA 18 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-901 TABLET 35 mg ORAL ANDA 13 sections
Alendronate Sodium HUMAN PRESCRIPTION DRUG LABEL 1 21695-902 TABLET 70 mg ORAL ANDA 13 sections