cilostazol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 74 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class EIF2AK3,GRK2,PDK1,PDK2,PDK4 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 92.32 18.20 39 4730 26557 90597121
Ventricular fibrillation 50.07 18.20 21 4748 14023 90609655
Gastrointestinal haemorrhage 39.76 18.20 35 4734 90213 90533465
Nikolsky's sign 36.36 18.20 6 4763 92 90623586
Acinetobacter test positive 36.18 18.20 6 4763 95 90623583
Cardiac failure 34.00 18.20 35 4734 109461 90514217
Anaemia 33.99 18.20 64 4705 352738 90270940
Urticaria vesiculosa 29.87 18.20 4 4765 12 90623666
Cerebral haemorrhage 29.83 18.20 20 4749 34502 90589176
Cardiac failure congestive 29.65 18.20 31 4738 98663 90525015
Pyogenic granuloma 29.15 18.20 6 4763 321 90623357
Kounis syndrome 28.98 18.20 9 4760 2544 90621134
Myocardial infarction 26.12 18.20 30 4739 105942 90517736
Torsade de pointes 24.08 18.20 13 4756 15169 90608509
Peripheral arterial occlusive disease 23.75 18.20 9 4760 4612 90619066
Miosis 23.53 18.20 11 4758 9473 90614205
Parotid gland enlargement 22.82 18.20 6 4763 937 90622741
Subarachnoid haemorrhage 22.08 18.20 13 4756 17891 90605787
Blood pressure decreased 21.55 18.20 23 4746 74872 90548806
Acute leukaemia 21.41 18.20 6 4763 1190 90622488
Shock 20.93 18.20 15 4754 28763 90594915
Fall 20.77 18.20 64 4705 481746 90141932
Ventricular tachycardia 20.59 18.20 14 4755 24694 90598984
Upper respiratory tract inflammation 20.50 18.20 7 4762 2665 90621013
Interstitial lung disease 19.45 18.20 22 4747 76383 90547295
Disorientation 19.19 18.20 17 4752 44097 90579581
Colonic haematoma 18.72 18.20 3 4766 38 90623640
Enterobacter test positive 18.67 18.20 4 4765 260 90623418
Hepatic function abnormal 18.49 18.20 17 4752 46271 90577407
Melaena 18.40 18.20 15 4754 34782 90588896
Infectious mononucleosis 18.31 18.20 6 4763 2015 90621663

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 83.18 16.21 58 7627 31111 42582539
Interstitial lung disease 51.53 16.21 67 7618 78395 42535255
Hepatic function abnormal 41.84 16.21 49 7636 51518 42562132
Cerebral hyperperfusion syndrome 35.04 16.21 7 7678 89 42613561
Sprue-like enteropathy 34.63 16.21 10 7675 637 42613013
Pemphigoid 34.51 16.21 23 7662 11444 42602206
Lacunar infarction 34.19 16.21 15 7670 3245 42610405
Renal impairment 29.68 16.21 63 7622 110165 42503485
Decreased appetite 29.53 16.21 89 7596 193048 42420602
Cardiac vein perforation 29.15 16.21 5 7680 25 42613625
Therapeutic drug monitoring analysis incorrectly performed 26.54 16.21 7 7678 318 42613332
Peripheral arterial occlusive disease 26.26 16.21 16 7669 6822 42606828
Gastrointestinal haemorrhage 25.32 16.21 55 7630 97671 42515979
Vascular stent thrombosis 24.86 16.21 12 7673 3230 42610420
Pneumonia 22.32 16.21 141 7544 422008 42191642
Thrombosis in device 22.19 16.21 11 7674 3135 42610515
Cerebral haemorrhage 22.08 16.21 31 7654 38935 42574715
Intermittent claudication 21.39 16.21 10 7675 2505 42611145
Diarrhoea 20.80 16.21 148 7537 460701 42152949
Contrast encephalopathy 20.53 16.21 5 7680 164 42613486
Basal ganglia haematoma 20.01 16.21 4 7681 51 42613599
Foot amputation 19.85 16.21 7 7678 850 42612800
Haemobilia 19.76 16.21 6 7679 455 42613195
Hemiplegia 19.46 16.21 14 7671 7865 42605785
Renal haemorrhage 18.78 16.21 8 7677 1611 42612039
Cardiac failure 17.98 16.21 51 7634 106805 42506845
Peripheral artery occlusion 17.86 16.21 8 7677 1818 42611832
Peripheral artery restenosis 17.84 16.21 3 7682 13 42613637
Altered state of consciousness 17.66 16.21 24 7661 29235 42584415
Haematochezia 17.59 16.21 35 7650 58401 42555249
Photosensitivity reaction 17.41 16.21 16 7669 12686 42600964
Intestinal ischaemia 17.28 16.21 14 7671 9374 42604276
Gastric cancer 16.45 16.21 12 7673 6891 42606759

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 173.34 14.34 93 11977 51745 110525484
Interstitial lung disease 74.96 14.34 84 11986 139250 110437979
Gastrointestinal haemorrhage 63.34 14.34 84 11986 165434 110411795
Hepatic function abnormal 60.73 14.34 61 12009 89234 110487995
Cardiac failure 55.21 14.34 84 11986 187542 110389687
Peripheral arterial occlusive disease 53.00 14.34 24 12046 9256 110567973
Lacunar infarction 48.15 14.34 20 12050 6266 110570963
Cerebral haemorrhage 47.17 14.34 46 12024 64922 110512307
Renal impairment 44.03 14.34 76 11994 188369 110388860
Pemphigoid 43.49 14.34 27 12043 19680 110557549
Anaemia 41.89 14.34 143 11927 546943 110030286
Joint swelling 37.08 14.34 3 12067 442842 110134387
Cardiac failure congestive 36.71 14.34 62 12008 150938 110426291
Cerebral hyperperfusion syndrome 36.48 14.34 7 12063 122 110577107
Peripheral artery occlusion 35.60 14.34 13 12057 2892 110574337
Blood pressure decreased 33.08 14.34 51 12019 115040 110462189
Pneumonia aspiration 32.24 14.34 42 12028 81191 110496038
Cardiac vein perforation 31.66 14.34 5 12065 25 110577204
Subarachnoid haemorrhage 31.40 14.34 26 12044 29676 110547553
Ventricular fibrillation 31.39 14.34 30 12040 41283 110535946
Vascular stent thrombosis 31.07 14.34 13 12057 4148 110573081
Pneumonia 31.01 14.34 182 11888 876532 109700697
Melaena 29.57 14.34 37 12033 68720 110508509
Decreased appetite 29.32 14.34 116 11954 475730 110101499
Drug intolerance 28.52 14.34 5 12065 406507 110170722
Upper gastrointestinal haemorrhage 28.28 14.34 31 12039 50065 110527164
Altered state of consciousness 28.02 14.34 33 12037 57593 110519636
Nikolsky's sign 27.78 14.34 6 12064 192 110577037
Haemorrhage subcutaneous 27.50 14.34 13 12057 5526 110571703
Peripheral artery restenosis 27.21 14.34 4 12066 11 110577218
Urticaria vesiculosa 26.95 14.34 4 12066 12 110577217
Subdural haematoma 26.81 14.34 26 12044 36428 110540801
Sprue-like enteropathy 26.15 14.34 9 12061 1687 110575542
Atrial fibrillation 26.02 14.34 69 12001 229573 110347656
Foot amputation 25.52 14.34 8 12062 1120 110576109
Acinetobacter test positive 25.44 14.34 6 12064 287 110576942
Therapeutic drug monitoring analysis incorrectly performed 24.59 14.34 7 12063 705 110576524
Alopecia 24.49 14.34 5 12065 364748 110212481
Acute myocardial infarction 23.90 14.34 37 12033 83740 110493489
Contrast encephalopathy 23.86 14.34 6 12064 376 110576853
Drug ineffective 23.69 14.34 86 11984 1520454 109056775
Haematoma 22.84 14.34 30 12040 58446 110518783
Aortic dissection 22.73 14.34 11 12059 4922 110572307
Thrombosis in device 21.93 14.34 11 12059 5316 110571913
Pyogenic granuloma 21.77 14.34 6 12064 537 110576692
Labelled drug-drug interaction medication error 21.73 14.34 21 12049 29281 110547948
Gastric cancer 21.59 14.34 14 12056 10994 110566235
Peripheral ischaemia 21.53 14.34 14 12056 11044 110566185
Parotid gland enlargement 21.19 14.34 7 12063 1158 110576071
Thalamus haemorrhage 21.17 14.34 8 12062 1956 110575273
Intestinal ischaemia 21.04 14.34 16 12054 16163 110561066
Basal ganglia haematoma 20.99 14.34 4 12066 67 110577162
Haemobilia 20.67 14.34 6 12064 647 110576582
Drug interaction 20.39 14.34 108 11962 500075 110077154
Loss of consciousness 20.25 14.34 57 12013 196249 110380980
Gastric ulcer haemorrhage 20.19 14.34 13 12057 10081 110567148
Shock 20.17 14.34 27 12043 53561 110523668
Colonic haematoma 19.96 14.34 4 12066 88 110577141
Blood alkaline phosphatase increased 19.77 14.34 31 12039 70904 110506325
Intermittent claudication 19.34 14.34 9 12061 3692 110573537
Renal haemorrhage 19.22 14.34 8 12062 2517 110574712
Infusion related reaction 18.87 14.34 9 12061 381153 110196076
Haematochezia 18.82 14.34 40 12030 115484 110461745
Hypoglycaemia 18.68 14.34 40 12030 116064 110461165
Angina unstable 18.66 14.34 15 12055 16417 110560812
Peripheral artery thrombosis 18.62 14.34 9 12061 4015 110573214
Fall 18.58 14.34 121 11949 603361 109973868
Hemiplegia 18.18 14.34 17 12053 22765 110554464
Maternal exposure during pregnancy 18.16 14.34 3 12067 254880 110322349
Dehydration 17.88 14.34 69 12001 279442 110297787
Cardio-respiratory arrest 17.60 14.34 39 12031 115797 110461432
Fatigue 17.46 14.34 71 11999 1215887 109361342
Arthropathy 17.23 14.34 5 12065 287517 110289712
Putamen haemorrhage 17.22 14.34 5 12065 540 110576689
Drug eruption 17.16 14.34 25 12045 53634 110523595
Lower respiratory tract infection 17.02 14.34 3 12067 243103 110334126
Gastric haemorrhage 16.96 14.34 14 12056 15901 110561328
Haematemesis 16.71 14.34 26 12044 59082 110518147
Blood urea increased 16.70 14.34 25 12045 54932 110522297
Muscle haemorrhage 16.66 14.34 10 12060 6859 110570370
Rheumatoid arthritis 16.56 14.34 6 12064 299607 110277622
Musculoskeletal stiffness 16.52 14.34 5 12065 279817 110297412
Sinus node dysfunction 16.51 14.34 11 12059 9036 110568193
Photosensitivity reaction 16.51 14.34 17 12053 25572 110551657
Scleroderma associated digital ulcer 16.39 14.34 3 12067 40 110577189
Systemic lupus erythematosus 16.03 14.34 4 12066 254334 110322895
Disseminated intravascular coagulation 15.84 14.34 21 12049 41265 110535964
Arteriovenous fistula 15.83 14.34 6 12064 1479 110575750
Abdominal discomfort 15.72 14.34 12 12058 393846 110183383
Rhabdomyolysis 15.52 14.34 38 12032 120363 110456866
Arterial restenosis 15.39 14.34 3 12067 57 110577172
Thrombotic cerebral infarction 15.36 14.34 5 12065 789 110576440
Kounis syndrome 15.35 14.34 9 12061 5916 110571313
Chronic pigmented purpura 15.34 14.34 4 12066 290 110576939
Weight increased 15.25 14.34 14 12056 419630 110157599
Post procedural haemorrhage 15.20 14.34 13 12057 15499 110561730
Upper respiratory tract inflammation 15.04 14.34 8 12062 4363 110572866
Arthralgia 14.98 14.34 40 12030 779592 109797637
Pericarditis 14.71 14.34 3 12067 219111 110358118
Subcutaneous haematoma 14.69 14.34 7 12063 3029 110574200
Hypophagia 14.67 14.34 23 12047 52603 110524626
Small intestinal haemorrhage 14.62 14.34 8 12062 4610 110572619
Gangrene 14.61 14.34 13 12057 16328 110560901
Acute leukaemia 14.56 14.34 6 12064 1843 110575386

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 D001993 Bronchodilator Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D014665 Vasodilator Agents
MeSH PA D018696 Neuroprotective Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D020011 Protective Agents
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
FDA EPC N0000175598 Phosphodiesterase 3 Inhibitor
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35523 bronchodilator agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:48676 fibrin modulating drug
CHEBI has role CHEBI:50249 anticoagulant
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:50568 EC 3.1.4.17 (3,5-cyclic-nucleotide phosphodiesterase) inhibitor
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:73336 vulnerary
CHEBI has role CHEBI:145947 antiatherosclerotic agent

Related Drugs by ATC class:

B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
abciximabacetylsalicylic acidaloxiprinberaprostcangrelorcarbasalate calciumclopidogrelcloricromendipyridamoleditazoleepoprostenoleptifibatide show all 24 →

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




🐶 Veterinary Drug Use

None

🐶 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
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
4021153 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2064 TABLET 100 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 0093-2065 TABLET 50 mg ORAL ANDA 27 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 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 62135-983 TABLET 50 mg ORAL ANDA 19 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 62135-986 TABLET 100 mg ORAL ANDA 19 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8795 TABLET 100 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 63629-8796 TABLET 50 mg ORAL ANDA 27 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 68151-3844 TABLET 50 mg ORAL ANDA 26 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 68151-4123 TABLET 100 mg ORAL ANDA 26 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 70436-156 TABLET 50 mg ORAL ANDA 28 sections
Cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 70436-157 TABLET 100 mg ORAL ANDA 28 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 71610-813 TABLET 100 mg ORAL ANDA 20 sections
cilostazol HUMAN PRESCRIPTION DRUG LABEL 1 71610-822 TABLET 100 mg ORAL ANDA 20 sections
CILOSTAZOL HUMAN PRESCRIPTION DRUG LABEL 1 72189-116 TABLET 50 mg ORAL ANDA 16 sections