cilostazol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
644 73963-72-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • OPC 13013
  • cilostazol
  • cilostazole
  • pletal
  • OPC-13013
A quinoline and tetrazole derivative that acts as a phosphodiesterase type 3 inhibitor, with anti-platelet and vasodilating activity. It is used in the treatment of PERIPHERAL VASCULAR DISEASES; ISCHEMIC HEART DISEASE; and in the prevention of stroke.
  • Molecular weight: 369.47
  • Formula: C20H27N5O2
  • CLOGP: 3.67
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 81.93
  • ALOGS: -4.06
  • ROTB: 7

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 7.73 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 15, 1999 FDA OTSUKA

FDA Adverse Event Reporting System (Female)

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
Cerebral infarction 78.94 16.54 36 4081 23857 63461048
Ventricular fibrillation 45.97 16.54 20 4097 11847 63473058
Acinetobacter test positive 36.04 16.54 6 4111 78 63484827
Nikolsky's sign 34.70 16.54 6 4111 99 63484806
Gastrointestinal haemorrhage 31.11 16.54 32 4085 81144 63403761
Urticaria vesiculosa 29.03 16.54 4 4113 12 63484893
Cardiac failure 28.62 16.54 32 4085 89110 63395795
Pyogenic granuloma 28.14 16.54 6 4111 308 63484597
Cerebral haemorrhage 25.87 16.54 19 4098 30710 63454195
Anaemia 24.74 16.54 57 4060 293373 63191532
Subarachnoid haemorrhage 22.29 16.54 13 4104 14270 63470635
Parotid gland enlargement 22.14 16.54 6 4111 852 63484053
Cardiac failure congestive 21.21 16.54 28 4089 92405 63392500
Acute leukaemia 20.49 16.54 6 4111 1128 63483777
Torsade de pointes 20.43 16.54 12 4105 13339 63471566
Myocardial infarction 19.52 16.54 28 4089 99865 63385040
Upper respiratory tract inflammation 19.46 16.54 7 4110 2516 63482389
Peripheral arterial occlusive disease 19.32 16.54 8 4109 4193 63480712
Shock 18.61 16.54 14 4103 23449 63461456
Colonic haematoma 18.16 16.54 3 4114 37 63484868
Enterobacter test positive 18.00 16.54 4 4113 249 63484656
Kounis syndrome 17.99 16.54 6 4111 1724 63483181
Infectious mononucleosis 17.32 16.54 6 4111 1933 63482972

FDA Adverse Event Reporting System (Male)

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
Cerebral infarction 72.73 16.09 52 6621 27403 34922855
Interstitial lung disease 43.81 16.09 58 6615 65224 34885034
Hepatic function abnormal 38.73 16.09 45 6628 44318 34905940
Cerebral hyperperfusion syndrome 34.57 16.09 7 6666 90 34950168
Sprue-like enteropathy 31.79 16.09 9 6664 504 34949754
Cardiac vein perforation 28.87 16.09 5 6668 25 34950233
Renal impairment 27.89 16.09 58 6615 94455 34855803
Lacunar infarction 27.81 16.09 13 6660 3077 34947181
Peripheral arterial occlusive disease 27.67 16.09 16 6657 5858 34944400
Therapeutic drug monitoring analysis incorrectly performed 26.08 16.09 7 6666 321 34949937
Decreased appetite 24.91 16.09 79 6594 166313 34783945
Contrast encephalopathy 24.16 16.09 5 6668 72 34950186
Gastrointestinal haemorrhage 23.46 16.09 52 6621 88425 34861833
Intermittent claudication 21.73 16.09 10 6663 2284 34947974
Thrombosis in device 21.02 16.09 11 6662 3314 34946944
Cerebral haemorrhage 20.33 16.09 29 6644 34908 34915350
Hemiplegia 20.29 16.09 14 6659 6958 34943300
Foot amputation 20.27 16.09 7 6666 754 34949504
Haemobilia 20.21 16.09 6 6667 398 34949860
Diarrhoea 20.09 16.09 135 6538 389777 34560481
Basal ganglia haematoma 19.93 16.09 4 6669 49 34950209
Haematochezia 19.24 16.09 33 6640 46501 34903757
Renal haemorrhage 19.16 16.09 8 6665 1449 34948809
Altered state of consciousness 17.95 16.09 22 6651 22871 34927387
Peripheral artery occlusion 17.91 16.09 8 6665 1704 34948554
Toxicity to various agents 17.80 16.09 8 6665 200354 34749904
Peripheral artery restenosis 17.67 16.09 3 6670 13 34950245
Vascular stent thrombosis 16.56 16.09 9 6664 2926 34947332
Gastric cancer 16.53 16.09 12 6661 6457 34943801
Chronic pigmented purpura 16.51 16.09 4 6669 121 34950137
Thrombotic cerebral infarction 16.24 16.09 5 6668 375 34949883
Labelled drug-drug interaction medication error 16.22 16.09 17 6656 14922 34935336

FDA Adverse Event Reporting System (Geriatric)

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
Cerebral infarction 144.16 14.18 84 10366 45592 79688346
Interstitial lung disease 58.63 14.18 73 10377 112527 79621411
Gastrointestinal haemorrhage 51.63 14.18 79 10371 147640 79586298
Hepatic function abnormal 49.06 14.18 54 10396 73053 79660885
Peripheral arterial occlusive disease 48.41 14.18 23 10427 8235 79725703
Cerebral haemorrhage 41.13 14.18 44 10406 57629 79676309
Renal impairment 36.16 14.18 70 10380 157713 79576225
Cardiac failure 35.86 14.18 69 10381 154773 79579165
Cerebral hyperperfusion syndrome 35.04 14.18 7 10443 125 79733813
Anaemia 33.59 14.18 131 10319 444884 79289054
Lacunar infarction 33.12 14.18 16 10434 5941 79727997
Ventricular fibrillation 31.36 14.18 29 10421 31897 79702041
Peripheral artery occlusion 31.28 14.18 12 10438 2545 79731393
Cardiac vein perforation 30.75 14.18 5 10445 25 79733913
Subarachnoid haemorrhage 29.58 14.18 25 10425 24440 79709498
Pneumonia aspiration 29.50 14.18 40 10410 66927 79667011
Joint swelling 27.28 14.18 3 10447 288643 79445295
Altered state of consciousness 27.04 14.18 31 10419 43791 79690147
Contrast encephalopathy 27.00 14.18 6 10444 182 79733756
Decreased appetite 26.79 14.18 102 10348 342316 79391622
Upper gastrointestinal haemorrhage 26.77 14.18 30 10420 41350 79692588
Peripheral artery restenosis 26.48 14.18 4 10446 11 79733927
Urticaria vesiculosa 26.22 14.18 4 10446 12 79733926
Cardiac failure congestive 25.38 14.18 57 10393 142345 79591593
Foot amputation 25.28 14.18 8 10442 960 79732978
Nikolsky's sign 25.13 14.18 6 10444 251 79733687
Acinetobacter test positive 24.99 14.18 6 10444 257 79733681
Haemorrhage subcutaneous 24.00 14.18 12 10438 4797 79729141
Blood pressure decreased 23.84 14.18 45 10405 99421 79634517
Melaena 23.30 14.18 34 10416 60856 79673082
Therapeutic drug monitoring analysis incorrectly performed 23.28 14.18 7 10443 709 79733229
Drug ineffective 23.28 14.18 69 10381 1080844 78653094
Sprue-like enteropathy 22.86 14.18 8 10442 1310 79732628
Aortic dissection 22.56 14.18 11 10439 4164 79729774
Hemiplegia 21.71 14.18 17 10433 14922 79719016
Labelled drug-drug interaction medication error 21.32 14.18 22 10428 27628 79706310
Haematoma 21.22 14.18 30 10420 52165 79681773
Pyogenic granuloma 21.00 14.18 6 10444 509 79733429
Parotid gland enlargement 20.99 14.18 7 10443 991 79732947
Pneumonia 20.95 14.18 153 10297 660093 79073845
Haemobilia 20.85 14.18 6 10444 522 79733416
Vascular stent thrombosis 20.73 14.18 10 10440 3700 79730238
Basal ganglia haematoma 20.68 14.18 4 10446 60 79733878
Gastric cancer 20.26 14.18 14 10436 10165 79723773
Drug intolerance 19.98 14.18 5 10445 264114 79469824
Thrombosis in device 19.81 14.18 11 10439 5431 79728507
Subdural haematoma 18.99 14.18 22 10428 31412 79702526
Peripheral ischaemia 18.80 14.18 13 10437 9444 79724494
Renal haemorrhage 18.68 14.18 8 10442 2248 79731690
Acute myocardial infarction 18.64 14.18 35 10415 77001 79656937
Intermittent claudication 18.32 14.18 9 10441 3462 79730476
Muscle haemorrhage 18.32 14.18 11 10439 6289 79727649
Shock 17.66 14.18 25 10425 43523 79690415
Liver disorder 17.64 14.18 33 10417 72384 79661554
Fatigue 17.45 14.18 63 10387 929664 78804274
Drug interaction 17.26 14.18 103 10347 415080 79318858
Atrial fibrillation 17.17 14.18 61 10389 197825 79536113
Toxicity to various agents 17.12 14.18 18 10432 421522 79312416
Gangrene 17.07 14.18 12 10438 8952 79724986
Gastric ulcer haemorrhage 16.99 14.18 12 10438 9015 79724923
Blood alkaline phosphatase increased 16.76 14.18 30 10420 63634 79670304
Haematochezia 16.64 14.18 36 10414 87609 79646329
Putamen haemorrhage 16.58 14.18 5 10445 512 79733426
Loss of consciousness 16.53 14.18 54 10396 167889 79566049
Alopecia 16.34 14.18 5 10445 231350 79502588
Sinus node dysfunction 16.29 14.18 11 10439 7690 79726248
Angina unstable 16.20 14.18 15 10435 16512 79717426
Thrombotic cerebral infarction 16.08 14.18 5 10445 567 79733371
Chronic pigmented purpura 15.38 14.18 4 10446 238 79733700
Arteriovenous fistula 15.31 14.18 6 10444 1348 79732590
Pemphigoid 15.21 14.18 14 10436 15301 79718637
Rhabdomyolysis 14.83 14.18 38 10412 103093 79630845
Post procedural haemorrhage 14.50 14.18 13 10437 13731 79720207
Cardiac tamponade 14.45 14.18 11 10439 9265 79724673
Upper respiratory tract inflammation 14.27 14.18 8 10442 4027 79729911

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC23 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA MoA N0000175086 Phosphodiesterase 3 Inhibitors
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D018696 Neuroprotective Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D014665 Vasodilator Agents
FDA EPC N0000175598 Phosphodiesterase 3 Inhibitor
CHEBI has role CHEBI:35523 bronchodilator
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:48676 fibrin modulating agent
CHEBI has role CHEBI:50249 anticoagulants
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:50568 3,5-cyclic nucleoside monophosphate phosphodiesterase inhibitors
CHEBI has role CHEBI:63726 neuroprotective agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Intermittent claudication indication 63491006 DOID:3669
Chronic heart failure contraindication 48447003
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme INHIBITOR IC50 6.70 IUPHAR CHEMBL
Cytochrome P450 2C9 Enzyme IC50 5 DRUG MATRIX
cGMP-inhibited 3',5'-cyclic phosphodiesterase B Enzyme INHIBITOR IC50 6.42 IUPHAR

External reference:

IDSource
4021153 VUID
N0000148605 NUI
D01896 KEGG_DRUG
21107 RXNORM
4021153 VANDF
C0055729 UMLSCUI
CHEBI:31401 CHEBI
CHEMBL799 ChEMBL_ID
DB01166 DRUGBANK_ID
D000077407 MESH_DESCRIPTOR_UI
2754 PUBCHEM_CID
7148 IUPHAR_LIGAND_ID
5680 INN_ID
N7Z035406B UNII
14036 MMSL
60734 MMSL
7889 MMSL
d04382 MMSL
007339 NDDF
116087001 SNOMEDCT_US
395239000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0028 TABLET 50 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0028 TABLET 50 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0044 TABLET 100 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0054-0044 TABLET 100 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2064 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2064 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2064 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2064 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2065 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2065 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2065 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2065 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0185-0123 TABLET 50 mg ORAL ANDA 29 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0185-0223 TABLET 100 mg ORAL ANDA 29 sections
CILOSTAZOL HUMAN PRESCRIPTION DRUG LABEL 1 16590-285 TABLET 100 mg ORAL ANDA 22 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 42291-453 TABLET 100 mg ORAL ANDA 20 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 50090-5329 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 50090-5329 TABLET 50 mg ORAL ANDA 28 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 50268-176 TABLET 50 mg ORAL ANDA 20 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 50268-177 TABLET 100 mg ORAL ANDA 20 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 54868-5411 TABLET 100 mg ORAL ANDA 16 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 60505-2521 TABLET 50 mg ORAL ANDA 20 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 60505-2522 TABLET 100 mg ORAL ANDA 20 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8795 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8795 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8795 TABLET 100 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8796 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8796 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8796 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 68151-3844 TABLET 50 mg ORAL ANDA 26 sections