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

Stem definitionDrug idCAS RN
antihypertensive substances, prazosin derivatives 954 74191-85-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • doxazosin
  • doxazosin mesylate
  • doxazosine
  • doxazosin mesilate
A prazosin-related compound that is a selective alpha-1-adrenergic blocker.
  • Molecular weight: 451.48
  • Formula: C23H25N5O5
  • CLOGP: 3.58
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 1
  • TPSA: 112.27
  • ALOGS: -2.76
  • ROTB: 4

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.59 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 1.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.60 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 2, 1990 FDA PFIZER

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
Hyperkalaemia 153.16 13.61 125 15986 47964 50541049
Hypotension 123.40 13.61 247 15864 235222 50353791
Hypertensive crisis 114.81 13.61 64 16047 13090 50575923
Syncope 105.23 13.61 146 15965 102856 50486157
Drug interaction 94.58 13.61 201 15910 199420 50389593
Hyponatraemia 84.61 13.61 127 15984 96012 50493001
Acute kidney injury 81.99 13.61 206 15905 227852 50361161
Orthostatic hypotension 55.28 13.61 57 16054 29424 50559589
Bladder prolapse 54.98 13.61 21 16090 1800 50587213
Renal impairment 54.18 13.61 91 16020 75570 50513443
Rectal prolapse 52.19 13.61 20 16091 1729 50587284
Blood pressure increased 46.42 13.61 119 15992 133013 50456000
Hypoglycaemia 45.98 13.61 70 16041 53511 50535502
Bradycardia 45.47 13.61 77 16034 64349 50524664
Gallbladder polyp 43.79 13.61 14 16097 707 50588306
Drug intolerance 42.44 13.61 9 16102 219095 50369918
Dizziness 37.83 13.61 213 15898 346156 50242857
Injection site inflammation 37.59 13.61 19 16092 3186 50585827
Tubulointerstitial nephritis 37.13 13.61 34 16077 15177 50573836
Angioedema 36.32 13.61 52 16059 37624 50551389
Sinus bradycardia 35.21 13.61 31 16080 13152 50575861
Urinary incontinence 34.94 13.61 44 16067 28164 50560849
Sopor 34.69 13.61 37 16074 19842 50569171
Treatment failure 32.83 13.61 3 16108 137634 50451379
Thermal burn 32.82 13.61 20 16091 4821 50584192
Renal artery stenosis 32.31 13.61 14 16097 1658 50587355
Arthropathy 31.58 13.61 6 16105 157900 50431113
Presyncope 30.38 13.61 38 16073 24160 50564853
Maternal exposure during pregnancy 30.05 13.61 7 16104 159771 50429242
Therapeutic product effect decreased 29.83 13.61 4 16107 136046 50452967
Blood pressure inadequately controlled 29.45 13.61 18 16093 4362 50584651
Vitamin D decreased 29.16 13.61 23 16088 8383 50580630
Alopecia 28.26 13.61 22 16089 245025 50343988
Oedema peripheral 28.09 13.61 112 15999 157849 50431164
Blood pressure diastolic decreased 27.13 13.61 30 16081 16751 50572262
Confusional state 27.02 13.61 124 15987 185804 50403209
Drug ineffective 26.59 13.61 153 15958 819180 49769833
Abdominal discomfort 25.22 13.61 22 16089 231619 50357394
Systemic lupus erythematosus 24.82 13.61 7 16104 140615 50448398
Cardiac failure 24.46 13.61 66 16045 75974 50513039
Blood pressure systolic abnormal 24.43 13.61 20 16091 7686 50581327
Blood creatinine increased 24.39 13.61 66 16045 76094 50512919
Renal failure 24.33 13.61 82 16029 106551 50482462
Eye infarction 24.29 13.61 5 16106 40 50588973
Mucosal membrane hyperplasia 23.97 13.61 5 16106 43 50588970
Glossodynia 23.95 13.61 4 16107 115565 50473448
Product use issue 23.65 13.61 9 16102 149466 50439547
Blood pressure diastolic abnormal 22.99 13.61 21 16090 9340 50579673
Loss of consciousness 22.72 13.61 79 16032 104274 50484739
Renin increased 22.70 13.61 6 16105 153 50588860
Clonus 22.69 13.61 15 16096 4160 50584853
Glomerular filtration rate decreased 22.69 13.61 23 16088 11629 50577384
Daydreaming 22.65 13.61 7 16104 316 50588697
Lactic acidosis 22.38 13.61 39 16072 33316 50555697
Off label use 22.33 13.61 77 16034 474349 50114664
Atrial fibrillation 22.13 13.61 77 16034 101668 50487345
Feeling cold 21.89 13.61 29 16082 19502 50569511
Blood urea increased 20.48 13.61 31 16080 23554 50565459
Anaemia 20.47 13.61 144 15967 252312 50336701
Post cardiac arrest syndrome 20.44 13.61 4 16107 24 50588989
Pain 20.43 13.61 105 16006 578798 50010215
Cardiac failure congestive 20.24 13.61 66 16045 84316 50504697
Sinusitis 20.05 13.61 15 16096 170543 50418470
Hyperreflexia 19.93 13.61 15 16096 5103 50583910
Blood potassium increased 19.39 13.61 25 16086 16373 50572640
Metabolic acidosis 19.36 13.61 40 16071 38785 50550228
Hypertensive encephalopathy 18.59 13.61 7 16104 577 50588436
Blood pressure decreased 18.45 13.61 49 16062 55860 50533153
Oral discharge 17.89 13.61 5 16106 158 50588855
Hepatic enzyme increased 17.59 13.61 11 16100 137369 50451644
Malignant hypertension 17.57 13.61 8 16103 1066 50587947
Angiosclerosis 17.00 13.61 3 16108 9 50589004
Circulatory collapse 16.96 13.61 26 16085 19974 50569039
Familial periodic paralysis 16.96 13.61 4 16107 63 50588950
Dyspnoea 16.90 13.61 256 15855 547352 50041661
Duodenal ulcer 16.25 13.61 15 16096 6760 50582253
Swollen tongue 16.08 13.61 31 16080 28599 50560414
Product dose omission issue 16.05 13.61 21 16090 183817 50405196
Vision blurred 15.79 13.61 58 16053 78589 50510424
Bradyphrenia 15.50 13.61 14 16097 6138 50582875
Simple partial seizures 15.41 13.61 6 16105 541 50588472
Therapeutic product effect incomplete 15.34 13.61 5 16106 91510 50497503
Hypokalaemia 15.31 13.61 62 16049 87930 50501083
Fasting 15.05 13.61 3 16108 20 50588993
Discomfort 14.83 13.61 8 16103 108372 50480641
Injection site erythema 14.65 13.61 3 16108 74933 50514080
Gingival bleeding 14.52 13.61 18 16093 11335 50577678
Muscle twitching 14.43 13.61 21 16090 15410 50573603
Chronic kidney disease 14.30 13.61 36 16075 39735 50549278
Heart rate decreased 14.14 13.61 34 16077 36463 50552550
Nephrogenic anaemia 14.07 13.61 8 16103 1697 50587316
Rheumatoid arthritis 14.02 13.61 27 16084 202523 50386490
Pemphigoid 14.02 13.61 13 16098 5894 50583119
Periorbital oedema 13.81 13.61 12 16099 5000 50584013

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
Syncope 132.64 11.26 281 31900 81090 29461256
Orthostatic hypotension 90.10 11.26 117 32064 22512 29519834
Off label use 75.13 11.26 133 32048 300667 29241679
Hypertensive crisis 73.49 11.26 64 32117 7784 29534562
Blood pressure inadequately controlled 61.27 11.26 36 32145 2350 29539996
Middle insomnia 58.45 11.26 49 32132 5659 29536687
Mycotic allergy 56.77 11.26 18 32163 246 29542100
Febrile neutropenia 54.52 11.26 27 32154 112213 29430133
Carotid arteriosclerosis 54.34 11.26 28 32153 1410 29540936
Mite allergy 53.54 11.26 18 32163 299 29542047
Asthma 52.86 11.26 115 32066 33734 29508612
Full blood count abnormal 51.18 11.26 72 32109 14941 29527405
Hypotension 51.12 11.26 374 31807 193980 29348366
Conjunctivitis allergic 50.92 11.26 21 32160 629 29541717
Spirometry abnormal 50.48 11.26 18 32163 359 29541987
Dust allergy 49.47 11.26 19 32162 470 29541876
Presyncope 48.79 11.26 73 32108 16016 29526330
Drug interaction 48.05 11.26 373 31808 197012 29345334
Drug abuse 45.65 11.26 15 32166 79868 29462478
Left ventricular hypertrophy 44.20 11.26 45 32136 6658 29535688
Hyperkalaemia 44.09 11.26 157 32024 61235 29481111
Renal cyst haemorrhage 41.92 11.26 16 32165 389 29541957
Bradycardia 40.61 11.26 160 32021 65469 29476877
Productive cough 39.78 11.26 98 32083 31161 29511185
Neutropenia 39.76 11.26 51 32130 131660 29410686
Tricuspid valve incompetence 37.52 11.26 46 32135 8348 29533998
Oedema peripheral 36.75 11.26 215 31966 103342 29439004
Dizziness 35.88 11.26 339 31842 189345 29353001
Blood creatinine increased 35.76 11.26 185 31996 84917 29457429
Gastrointestinal tract mucosal pigmentation 35.62 11.26 14 32167 369 29541977
Ventricular hyperkinesia 35.49 11.26 12 32169 203 29542143
Loss of consciousness 34.67 11.26 166 32015 73890 29468456
Hypertensive heart disease 34.66 11.26 24 32157 2083 29540263
Right atrial enlargement 34.24 11.26 12 32169 227 29542119
Atrial fibrillation 32.85 11.26 212 31969 105434 29436912
Rectal prolapse 32.77 11.26 12 32169 259 29542087
Mitral valve thickening 32.48 11.26 13 32168 360 29541986
Aortic valve incompetence 31.87 11.26 33 32148 4980 29537366
Renal artery stenosis 31.47 11.26 22 32159 1939 29540407
Hypochromasia 31.24 11.26 12 32169 297 29542049
SARS-CoV-2 antibody test positive 30.73 11.26 11 32170 222 29542124
Mean platelet volume increased 30.37 11.26 13 32168 428 29541918
Drug ineffective 30.12 11.26 252 31929 362918 29179428
Nephrectomy 29.91 11.26 15 32166 713 29541633
Death 29.91 11.26 234 31947 341850 29200496
Mycobacterium test positive 28.56 11.26 12 32169 377 29541969
Left ventricular enlargement 28.46 11.26 14 32167 638 29541708
Subacute hepatic failure 28.06 11.26 8 32173 74 29542272
Floppy iris syndrome 27.77 11.26 11 32170 296 29542050
Vena cava injury 27.65 11.26 10 32171 208 29542138
Wheezing 27.35 11.26 89 32092 33151 29509195
Intraductal papillary mucinous neoplasm 26.69 11.26 11 32170 329 29542017
Renal impairment 26.38 11.26 165 32016 81168 29461178
Hyperparathyroidism 26.20 11.26 16 32165 1121 29541225
Haemodialysis 25.77 11.26 42 32139 9912 29532434
Myopathy 25.33 11.26 43 32138 10490 29531856
Normochromic normocytic anaemia 24.93 11.26 25 32156 3633 29538713
Primary hyperaldosteronism 24.92 11.26 7 32174 61 29542285
Electrocardiogram T wave inversion 24.38 11.26 19 32162 1978 29540368
Lung diffusion test decreased 23.84 11.26 12 32169 575 29541771
Blood urea increased 23.79 11.26 76 32105 28036 29514310
Left atrial enlargement 23.76 11.26 13 32168 740 29541606
Septic shock 23.61 11.26 20 32161 62540 29479806
Angioedema 23.22 11.26 82 32099 31833 29510513
Vertigo 23.16 11.26 64 32117 21797 29520549
Acute kidney injury 23.13 11.26 411 31770 264856 29277490
Mitral valve incompetence 22.87 11.26 47 32134 13246 29529100
Aortic dilatation 22.87 11.26 14 32167 985 29541361
Tooth avulsion 22.46 11.26 5 32176 14 29542332
Completed suicide 22.33 11.26 40 32141 90206 29452140
Arteriosclerosis 22.24 11.26 40 32141 10216 29532130
Bundle branch block left 22.11 11.26 28 32153 5249 29537097
Orthopnoea 22.03 11.26 26 32155 4534 29537812
Mucosal inflammation 21.79 11.26 4 32177 31591 29510755
Nocturia 21.26 11.26 35 32146 8327 29534019
Product use issue 21.25 11.26 15 32166 51429 29490917
Treatment failure 20.98 11.26 7 32174 36932 29505414
Cardiac autonomic neuropathy 20.45 11.26 6 32175 62 29542284
Obstructive airways disorder 20.20 11.26 40 32141 10976 29531370
Thrombocytopenia 20.15 11.26 77 32104 134746 29407600
Hyperparathyroidism secondary 19.75 11.26 14 32167 1261 29541085
Metabolic acidosis 19.51 11.26 87 32094 37575 29504771
Urine flow decreased 19.16 11.26 13 32168 1091 29541255
Hypertension 18.90 11.26 202 31979 116412 29425934
Atrioventricular block first degree 18.86 11.26 26 32155 5293 29537053
Atrioventricular block 18.81 11.26 30 32151 6952 29535394
Shock hypoglycaemic 18.05 11.26 6 32175 96 29542250
Scrotal oedema 18.02 11.26 14 32167 1450 29540896
Sprue-like enteropathy 17.88 11.26 9 32172 431 29541915
High density lipoprotein decreased 17.85 11.26 19 32162 2960 29539386
Arteriosclerosis coronary artery 17.66 11.26 37 32144 10568 29531778
Chronic kidney disease 17.29 11.26 82 32099 36334 29506012
Angina pectoris 17.29 11.26 68 32113 27782 29514564
Blood pressure ambulatory increased 17.19 11.26 5 32176 50 29542296
Inappropriate schedule of product administration 17.05 11.26 14 32167 44458 29497888
Human polyomavirus infection 16.63 11.26 10 32171 681 29541665
Delayed graft function 16.61 11.26 15 32166 1912 29540434
Haematuria 16.51 11.26 93 32088 44046 29498300
Chronic obstructive pulmonary disease 16.47 11.26 88 32093 40867 29501479
Psychotic symptom 16.28 11.26 13 32168 1401 29540945
Benign prostatic hyperplasia 16.27 11.26 38 32143 11672 29530674
Large intestine polyp 16.22 11.26 27 32154 6482 29535864
Palpitations 15.90 11.26 74 32107 32530 29509816
Abdominal wall haemorrhage 15.85 11.26 7 32174 249 29542097
Drug monitoring procedure not performed 15.74 11.26 7 32174 253 29542093
Xanthopsia 15.71 11.26 6 32175 146 29542200
Hypoglycaemia 15.61 11.26 98 32083 48248 29494098
Myocardial infarction 15.57 11.26 186 31995 110110 29432236
Genital swelling 15.45 11.26 6 32175 153 29542193
Crystalluria 15.45 11.26 8 32173 407 29541939
Dilatation ventricular 15.40 11.26 16 32165 2424 29539922
Diastolic dysfunction 15.38 11.26 23 32158 5041 29537305
Spinal osteoarthritis 15.35 11.26 26 32155 6330 29536016
Sepsis 15.18 11.26 92 32089 142590 29399756
Product dose omission issue 15.07 11.26 54 32127 96329 29446017
Pyrexia 14.86 11.26 222 31959 287400 29254946
Renal cyst 14.85 11.26 29 32152 7878 29534468
Dermatosis 14.81 11.26 7 32174 292 29542054
Product use in unapproved indication 14.72 11.26 47 32134 86828 29455518
Obstruction 14.69 11.26 14 32167 1912 29540434
Spermatozoa progressive motility abnormal 14.66 11.26 4 32177 31 29542315
Toxicity to various agents 14.55 11.26 120 32061 173541 29368805
Supine hypertension 14.52 11.26 7 32174 305 29542041
Electrocardiogram ST segment elevation 14.51 11.26 21 32160 4471 29537875
Microalbuminuria 14.37 11.26 9 32172 659 29541687
Infusion related reaction 14.27 11.26 16 32165 43870 29498476
Aplasia pure red cell 13.98 11.26 23 32158 5468 29536878
Asthenia 13.88 11.26 319 31862 214931 29327415
Rhabdomyolysis 13.68 11.26 113 32068 60695 29481651
Hospitalisation 13.65 11.26 18 32163 45970 29496376
Ischaemic cardiomyopathy 13.53 11.26 23 32158 5615 29536731
Duplicate therapy error 13.48 11.26 5 32176 112 29542234
Blood phosphorus increased 13.42 11.26 16 32165 2821 29539525
Melaena 13.23 11.26 68 32113 31108 29511238
Malignant neoplasm progression 13.20 11.26 39 32142 73820 29468526
Leukopenia 13.17 11.26 25 32156 55178 29487168
Blood uric acid increased 13.15 11.26 23 32158 5745 29536601
Multiple organ dysfunction syndrome 13.04 11.26 31 32150 63085 29479261
Vitamin D decreased 13.02 11.26 16 32165 2909 29539437
Renal failure 13.00 11.26 191 31990 118408 29423938
Blood pressure increased 12.96 11.26 130 32051 73673 29468673
Glomerular filtration rate decreased 12.95 11.26 34 32147 11232 29531114
Respiratory failure 12.92 11.26 58 32123 97073 29445273
Cardio-respiratory arrest 12.90 11.26 22 32159 50579 29491767
Sinus node dysfunction 12.86 11.26 18 32163 3716 29538630
Myalgia 12.82 11.26 130 32051 73889 29468457
Spermatozoa progressive motility decreased 12.75 11.26 5 32176 131 29542215
Disease progression 12.74 11.26 46 32135 81870 29460476
Sinus rhythm 12.50 11.26 6 32175 259 29542087
Toxic neuropathy 12.48 11.26 7 32174 418 29541928
Blood pressure systolic decreased 12.46 11.26 18 32163 3826 29538520
Blood chloride increased 12.36 11.26 15 32166 2694 29539652
Aortic arteriosclerosis 12.34 11.26 18 32163 3858 29538488
Myopathy toxic 12.30 11.26 7 32174 430 29541916
Post transplant distal limb syndrome 12.03 11.26 6 32175 282 29542064
Jaundice hepatocellular 11.98 11.26 4 32177 65 29542281
Chronic fatigue syndrome 11.89 11.26 6 32175 289 29542057
Pneumonia 11.84 11.26 262 31919 319910 29222436
Blood potassium increased 11.84 11.26 39 32142 14612 29527734
Haemoglobinaemia 11.79 11.26 5 32176 161 29542185
Mean cell volume increased 11.71 11.26 14 32167 2475 29539871
Cerebral haemorrhage 11.61 11.26 66 32115 31360 29510986
Vascular compression 11.59 11.26 5 32176 168 29542178
Agitation 11.58 11.26 24 32157 51280 29491066
Diverticulum intestinal 11.54 11.26 16 32165 3274 29539072
Tongue haemorrhage 11.48 11.26 7 32174 489 29541857
Mouth breathing 11.45 11.26 4 32177 75 29542271
Breath sounds 11.38 11.26 3 32178 20 29542326
Eosinophilia 11.33 11.26 51 32130 22110 29520236

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
Syncope 229.43 11.03 388 41923 157247 64299174
Hypertensive crisis 185.07 11.03 127 42184 18121 64438300
Hyperkalaemia 180.05 11.03 273 42038 100856 64355565
Drug interaction 144.61 11.03 543 41768 361540 64094881
Hypotension 142.06 11.03 559 41752 380415 64076006
Orthostatic hypotension 140.21 11.03 163 42148 46575 64409846
Acute kidney injury 99.63 11.03 567 41744 448673 64007748
Bradycardia 86.14 11.03 219 42092 118000 64338421
Off label use 85.37 11.03 180 42131 632626 63823795
Renal impairment 80.22 11.03 232 42079 134785 64321636
Rectal prolapse 76.07 11.03 32 42279 1694 64454727
Presyncope 69.98 11.03 100 42211 34989 64421432
Blood pressure inadequately controlled 68.02 11.03 43 42268 5341 64451080
Carotid arteriosclerosis 64.10 11.03 30 42281 2049 64454372
Renal artery stenosis 59.53 11.03 32 42279 2937 64453484
Atrial fibrillation 58.71 11.03 245 42066 170844 64285577
Blood creatinine increased 58.50 11.03 209 42102 135573 64320848
Middle insomnia 58.40 11.03 56 42255 12821 64443600
Dizziness 57.10 11.03 479 41832 429684 64026737
Drug ineffective 55.66 11.03 324 41987 839923 63616498
Angioedema 54.11 11.03 123 42188 61698 64394723
Alopecia 53.26 11.03 21 42290 165669 64290752
Hyponatraemia 52.91 11.03 215 42096 148124 64308297
Febrile neutropenia 52.28 11.03 29 42282 187628 64268793
Loss of consciousness 51.31 11.03 213 42098 148152 64308269
Hypoglycaemia 51.00 11.03 152 42159 89740 64366681
Oedema peripheral 50.81 11.03 272 42039 210045 64246376
Left ventricular hypertrophy 50.19 11.03 45 42266 9461 64446960
Conjunctivitis allergic 48.44 11.03 20 42291 1010 64455411
Treatment failure 48.41 11.03 9 42302 116807 64339614
Spirometry abnormal 48.09 11.03 17 42294 559 64455862
Renal cyst haemorrhage 47.77 11.03 16 42295 446 64455975
Contraindicated product administered 47.59 11.03 7 42304 107822 64348599
Product use issue 47.51 11.03 20 42291 151695 64304726
Full blood count abnormal 46.86 11.03 76 42235 29681 64426740
Blood urea increased 46.86 11.03 95 42216 44058 64412363
Bladder prolapse 46.46 11.03 20 42291 1121 64455300
Drug intolerance 45.61 11.03 34 42277 187958 64268463
Maternal exposure during pregnancy 45.28 11.03 5 42306 95879 64360542
Pain 44.75 11.03 199 42112 553312 63903109
Mite allergy 44.32 11.03 17 42294 706 64455715
Metabolic acidosis 43.14 11.03 123 42188 70835 64385586
Renal failure 42.53 11.03 233 42078 181455 64274966
Dust allergy 41.38 11.03 18 42293 1035 64455386
Mycotic allergy 39.02 11.03 17 42294 981 64455440
Ventricular hyperkinesia 38.64 11.03 12 42299 261 64456160
Sinusitis 38.59 11.03 24 42287 145904 64310517
Mitral valve thickening 37.97 11.03 13 42298 388 64456033
Vitamin D decreased 37.86 11.03 35 42276 7652 64448769
Neutropenia 37.62 11.03 62 42249 239562 64216859
Glomerular filtration rate decreased 36.43 11.03 54 42257 19518 64436903
Right atrial enlargement 36.22 11.03 12 42299 323 64456098
Tricuspid valve incompetence 36.18 11.03 50 42261 16953 64439468
Aortic valve incompetence 35.58 11.03 35 42276 8266 64448155
SARS-CoV-2 antibody test positive 35.47 11.03 11 42300 238 64456183
Hypertensive heart disease 35.11 11.03 25 42286 3779 64452642
Therapeutic product effect decreased 34.85 11.03 16 42295 115335 64341086
Left ventricular enlargement 34.62 11.03 14 42297 670 64455751
Productive cough 34.38 11.03 116 42195 73087 64383334
Arteriosclerosis 34.25 11.03 47 42264 15830 64440591
Mycobacterium test positive 33.73 11.03 12 42299 402 64456019
Mitral valve incompetence 33.32 11.03 60 42251 25478 64430943
Cardiac failure 33.17 11.03 173 42138 132200 64324221
Benign prostatic hyperplasia 32.68 11.03 35 42276 9130 64447291
Hepatic enzyme increased 32.16 11.03 23 42288 129920 64326501
Systemic lupus erythematosus 32.11 11.03 6 42305 77606 64378815
Vena cava injury 32.09 11.03 10 42301 220 64456201
Rheumatoid arthritis 31.28 11.03 37 42274 164257 64292164
Gastrointestinal tract mucosal pigmentation 30.52 11.03 14 42297 913 64455508
Nephrectomy 30.41 11.03 16 42295 1406 64455015
Sopor 29.33 11.03 62 42249 29599 64426822
Chronic kidney disease 29.18 11.03 94 42217 57825 64398596
Arthropathy 29.17 11.03 22 42289 120945 64335476
Completed suicide 29.16 11.03 65 42246 224349 64232072
Product dose omission issue 29.08 11.03 52 42259 194695 64261726
Hypochromasia 28.30 11.03 12 42299 648 64455773
Primary hyperaldosteronism 28.00 11.03 8 42303 129 64456292
Melaena 27.98 11.03 88 42223 53460 64402961
Blood pressure increased 27.70 11.03 201 42110 172351 64284070
Gallbladder polyp 27.62 11.03 13 42298 899 64455522
Scrotal oedema 27.01 11.03 14 42297 1193 64455228
Mean platelet volume increased 26.76 11.03 13 42298 965 64455456
Pemphigus 26.64 11.03 4 42307 60697 64395724
Rhabdomyolysis 26.61 11.03 125 42186 91601 64364820
Blood potassium increased 26.50 11.03 55 42256 25925 64430496
Sinus bradycardia 26.39 11.03 51 42260 22842 64433579
Circulatory collapse 26.12 11.03 64 42247 33668 64422753
Intraductal papillary mucinous neoplasm 26.08 11.03 11 42300 586 64455835
Cardiac failure congestive 25.69 11.03 160 42151 130420 64326001
Nocturia 25.53 11.03 34 42277 11131 64445290
Abdominal discomfort 25.19 11.03 51 42260 182271 64274150
Asthenia 25.06 11.03 407 41904 427637 64028784
Injection site inflammation 24.85 11.03 19 42292 3202 64453219
Infusion related reaction 24.47 11.03 44 42267 164423 64291998
Subacute hepatic failure 24.45 11.03 8 42303 207 64456214
Angina pectoris 24.39 11.03 75 42236 45006 64411415
Floppy iris syndrome 24.38 11.03 9 42302 336 64456085
Ischaemic cardiomyopathy 24.18 11.03 26 42285 6812 64449609
Nasopharyngitis 23.70 11.03 59 42252 196014 64260407
Blood uric acid increased 23.68 11.03 28 42283 8135 64448286
Haemodialysis 23.41 11.03 41 42270 17036 64439385
Urine flow decreased 23.34 11.03 12 42299 1005 64455416
Left atrial enlargement 23.18 11.03 12 42299 1020 64455401
Wheezing 22.78 11.03 109 42202 80470 64375951
Orthopnoea 22.73 11.03 29 42282 9105 64447316
Injection site erythema 22.69 11.03 9 42302 70791 64385630
Arteriosclerosis coronary artery 22.22 11.03 38 42273 15491 64440930
Haematuria 21.81 11.03 88 42223 60383 64396038
Swollen tongue 21.63 11.03 61 42250 34893 64421528
Lung diffusion test decreased 21.52 11.03 12 42299 1184 64455237
Hypertension 21.39 11.03 262 42049 258999 64197422
Obstructive airways disorder 21.25 11.03 47 42264 23138 64433283
Normochromic normocytic anaemia 21.17 11.03 24 42287 6666 64449755
End stage renal disease 21.09 11.03 30 42281 10445 64445976
Coronary artery disease 21.05 11.03 87 42224 60346 64396075
Dermatosis 21.03 11.03 9 42302 497 64455924
Death 20.96 11.03 209 42102 482496 63973925
Sinus node dysfunction 20.77 11.03 24 42287 6804 64449617
Chronic obstructive pulmonary disease 20.73 11.03 97 42214 70951 64385470
Atrioventricular block 20.73 11.03 32 42279 11983 64444438
Angiosclerosis 20.61 11.03 4 42307 9 64456412
Bundle branch block left 20.59 11.03 29 42282 10005 64446416
Myocardial infarction 20.52 11.03 182 42129 165639 64290782
Discomfort 20.42 11.03 14 42297 80864 64375557
Mucosal membrane hyperplasia 20.27 11.03 5 42306 44 64456377
Exposure during pregnancy 20.21 11.03 13 42298 77662 64378759
Hyperparathyroidism 20.21 11.03 16 42295 2836 64453585
Tubulointerstitial nephritis 20.17 11.03 55 42256 30854 64425567
Product use in unapproved indication 19.93 11.03 55 42256 176563 64279858
Myopathy 19.90 11.03 39 42272 17641 64438780
Infection 19.81 11.03 59 42252 184821 64271600
Cerebral haemorrhage 19.76 11.03 76 42235 51014 64405407
Drug monitoring procedure not performed 19.74 11.03 10 42301 812 64455609
Aortic dilatation 19.74 11.03 12 42299 1391 64455030
Blood pressure ambulatory increased 19.60 11.03 5 42306 51 64456370
Cardiac autonomic neuropathy 19.60 11.03 5 42306 51 64456370
High density lipoprotein decreased 19.50 11.03 18 42293 3928 64452493
Glossodynia 19.50 11.03 9 42302 64687 64391734
Dyspnoea 19.37 11.03 612 41699 718062 63738359
Abdominal wall haemorrhage 19.13 11.03 8 42303 417 64456004
Hypokalaemia 18.98 11.03 141 42170 121762 64334659
Large intestine polyp 18.89 11.03 29 42282 10808 64445613
Kidney transplant rejection 18.80 11.03 27 42284 9484 64446937
Thermal burn 18.37 11.03 21 42290 5885 64450536
Renal cyst 18.30 11.03 31 42280 12539 64443882
Nausea 17.74 11.03 387 41924 785413 63671008
Urinary incontinence 17.60 11.03 58 42253 36093 64420328
Post cardiac arrest syndrome 17.55 11.03 4 42307 24 64456397
Psychotic symptom 17.35 11.03 13 42298 2125 64454296
Delayed graft function 17.28 11.03 15 42296 3021 64453400
Rectal haemorrhage 17.02 11.03 83 42228 61734 64394687
Rash 16.92 11.03 206 42105 458343 63998078
Flushing 16.88 11.03 16 42295 78632 64377789
Acute myocardial infarction 16.68 11.03 90 42221 69628 64386793
Spermatozoa progressive motility abnormal 16.66 11.03 4 42307 31 64456390
Stomatitis 16.59 11.03 29 42282 109576 64346845
Blood chloride increased 16.52 11.03 18 42293 4785 64451636
Cerebrovascular accident 16.50 11.03 150 42161 137433 64318988
Electrocardiogram ST segment elevation 16.43 11.03 22 42289 7237 64449184
Renin increased 16.40 11.03 6 42305 218 64456203
Hyperparathyroidism secondary 16.36 11.03 13 42298 2317 64454104
Muscular dystrophy 16.35 11.03 5 42306 103 64456318
Electrocardiogram T wave inversion 16.24 11.03 18 42293 4876 64451545
Fasting 16.23 11.03 4 42307 35 64456386
Nephrogenic anaemia 16.11 11.03 15 42296 3310 64453111
Haemoglobin decreased 16.02 11.03 197 42114 194866 64261555
Drug abuse 15.86 11.03 40 42271 132334 64324087
Joint swelling 15.83 11.03 80 42231 215302 64241119
Shock hypoglycaemic 15.76 11.03 6 42305 244 64456177
Priapism 15.65 11.03 16 42295 3954 64452467
Simple partial seizures 15.64 11.03 8 42303 663 64455758
Erectile dysfunction 15.63 11.03 29 42282 12598 64443823
Injection site pruritus 15.48 11.03 3 42308 37823 64418598
Vertigo 15.38 11.03 78 42233 58933 64397488
Human polyomavirus infection 15.07 11.03 9 42302 1010 64455411
Eosinophilia 15.02 11.03 57 42254 38019 64418402
Atrioventricular block first degree 15.01 11.03 26 42285 10708 64445713
Sprue-like enteropathy 14.99 11.03 9 42302 1020 64455401
Prostatic haemorrhage 14.77 11.03 5 42306 144 64456277
Asthma 14.74 11.03 110 42201 95115 64361306
Anuria 14.70 11.03 36 42275 18928 64437493
Clonus 14.68 11.03 19 42292 6048 64450373
Obstruction 14.49 11.03 14 42297 3234 64453187
Genital swelling 14.44 11.03 6 42305 308 64456113
Blood phosphorus increased 14.40 11.03 17 42294 4929 64451492
Gastrointestinal disorder 14.26 11.03 23 42288 89686 64366735
Spermatozoa progressive motility decreased 14.21 11.03 4 42307 61 64456360
Arthralgia 14.01 11.03 205 42106 442055 64014366
Crystalluria 13.97 11.03 8 42303 830 64455591
Electrocardiogram T wave peaked 13.93 11.03 8 42303 835 64455586
Herpes zoster 13.85 11.03 19 42292 79168 64377253
Aortic valve sclerosis 13.71 11.03 10 42301 1569 64454852
Tooth avulsion 13.64 11.03 4 42307 71 64456350
Supine hypertension 13.63 11.03 6 42305 355 64456066
Ventricular hypertrophy 13.62 11.03 19 42292 6497 64449924
Nephrogenic systemic fibrosis 13.56 11.03 18 42293 5874 64450547
Ill-defined disorder 13.47 11.03 6 42305 44046 64412375
Therapeutic product effect incomplete 13.40 11.03 30 42281 103452 64352969
Feeling cold 13.38 11.03 40 42271 23638 64432783
Septic shock 13.31 11.03 31 42280 105406 64351015
Injection site reaction 13.29 11.03 7 42304 46657 64409764
Chills 13.17 11.03 46 42265 137218 64319203
Hyperlipidaemia 13.16 11.03 39 42272 22937 64433484
Bronchiolitis 13.15 11.03 14 42297 3627 64452794
Duplicate therapy error 13.14 11.03 5 42306 203 64456218
Toxicity to various agents 13.14 11.03 164 42147 363349 64093072
Vascular anastomotic haemorrhage 13.01 11.03 4 42307 84 64456337
Myalgia 12.93 11.03 160 42151 158457 64297964
Perineal cyst 12.92 11.03 4 42307 86 64456335
Diabetic nephropathy 12.91 11.03 12 42299 2642 64453779
Fatigue 12.79 11.03 384 41927 748346 63708075
Oliguria 12.74 11.03 29 42282 14547 64441874
Angina unstable 12.67 11.03 30 42281 15437 64440984
Disease progression 12.60 11.03 49 42262 141631 64314790
Aplasia pure red cell 12.55 11.03 19 42292 6995 64449426
Shock 12.50 11.03 54 42257 38186 64418235
Condition aggravated 12.37 11.03 171 42140 372255 64084166
Blood glucose increased 12.30 11.03 108 42203 97965 64358456
Ventricular extrasystoles 12.26 11.03 32 42279 17497 64438924
Bundle branch block 12.23 11.03 9 42302 1431 64454990
Anaemia 12.21 11.03 330 41981 378350 64078071
Oral discharge 12.06 11.03 5 42306 255 64456166
Haemoglobinaemia 12.04 11.03 5 42306 256 64456165
Multiple sclerosis relapse 11.97 11.03 6 42305 41129 64415292
Vascular compression 11.77 11.03 5 42306 271 64456150
Duodenal ulcer perforation 11.77 11.03 4 42307 34621 64421800
Periorbital oedema 11.76 11.03 19 42292 7395 64449026
Tachyarrhythmia 11.75 11.03 17 42294 6009 64450412
Jaundice hepatocellular 11.70 11.03 4 42307 119 64456302
Toxic neuropathy 11.69 11.03 7 42304 789 64455632
Coronary artery stenosis 11.69 11.03 24 42287 11224 64445197
Ejaculation disorder 11.68 11.03 6 42305 502 64455919
Aortic arteriosclerosis 11.64 11.03 19 42292 7457 64448964
Optic neuropathy 11.63 11.03 12 42299 2999 64453422
Daydreaming 11.58 11.03 7 42304 803 64455618
Blood lactic acid abnormal 11.56 11.03 3 42308 33 64456388
Neuropathy peripheral 11.54 11.03 39 42272 117486 64338935
Cardiomegaly 11.53 11.03 38 42273 23646 64432775
Anti-erythropoietin antibody negative 11.49 11.03 5 42306 288 64456133
Post transplant distal limb syndrome 11.44 11.03 6 42305 524 64455897
Proteinuria 11.35 11.03 42 42269 27681 64428740
Mouth breathing 11.33 11.03 4 42307 131 64456290
Lactic acidosis 11.30 11.03 74 42237 61336 64395085
Phaeochromocytoma crisis 11.26 11.03 5 42306 302 64456119
Hepatocellular injury 11.19 11.03 8 42303 45227 64411194
Tongue haemorrhage 11.17 11.03 7 42304 856 64455565
Xanthopsia 11.17 11.03 5 42306 308 64456113
Sepsis 11.14 11.03 97 42214 230244 64226177
Haemorrhage subcutaneous 11.09 11.03 14 42297 4347 64452074
Folliculitis 11.08 11.03 3 42308 30074 64426347
Gravitational oedema 11.04 11.03 9 42302 1663 64454758

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02CA04 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING
Alpha-adrenoreceptor antagonists
FDA MoA N0000000099 Adrenergic alpha-Antagonists
FDA EPC N0000175553 alpha-Adrenergic Blocker
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:37890 alpha-adrenergic receptor blockaders
CHEBI has role CHEBI:59844 antihyperplasia drugs
MeSH PA D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents

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

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Benign prostatic hyperplasia indication 266569009
Priapism contraindication 6273006 DOID:9286
Stenosis of intestine contraindication 23065003
Orthostatic hypotension contraindication 28651003
Low blood pressure contraindication 45007003
Hepatic failure contraindication 59927004
Chronic idiopathic constipation contraindication 82934008
Cataract surgery contraindication 110473004
Disease of liver contraindication 235856003 DOID:409
Pyloric obstruction contraindication 244815007
Syncope contraindication 271594007
Intraoperative floppy iris syndrome contraindication 418801006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.22 Basic
pKa2 0.72 Basic

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
Alpha-1D adrenergic receptor GPCR ANTAGONIST Ki 8.85 WOMBAT-PK CHEMBL
Alpha-1B adrenergic receptor GPCR ANTAGONIST Ki 9.10 WOMBAT-PK CHEMBL
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 8.80 WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.23 WOMBAT-PK
Multidrug resistance protein 1 Transporter Ki 5 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter Ki 5.85 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.63 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.55 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.55 CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 6.83 DRUG MATRIX
Interstitial collagenase Enzyme IC50 5.24 DRUG MATRIX
HLA class I histocompatibility antigen, A-3 alpha chain Unclassified Kd 4.80 CHEMBL
Beta-2 adrenergic receptor GPCR Ki 5.72 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 6.14 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 9.38 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 8.81 CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 6.90 DRUG MATRIX

External reference:

IDSource
4019735 VUID
N0000147827 NUI
D00608 KEGG_DRUG
77883-43-3 SECONDARY_CAS_RN
4019565 VANDF
4019735 VANDF
C0114873 UMLSCUI
CHEBI:4708 CHEBI
CHEMBL707 ChEMBL_ID
CHEMBL1200561 ChEMBL_ID
D017292 MESH_DESCRIPTOR_UI
DB00590 DRUGBANK_ID
7170 IUPHAR_LIGAND_ID
5143 INN_ID
NW1291F1W8 UNII
3157 PUBCHEM_CID
39173 RXNORM
37806 MMSL
40546 MMSL
4637 MMSL
d00726 MMSL
003561 NDDF
004493 NDDF
108556006 SNOMEDCT_US
108557002 SNOMEDCT_US
372508002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2040 TABLET, MULTILAYER, EXTENDED RELEASE 4 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2040 TABLET, MULTILAYER, EXTENDED RELEASE 4 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2080 TABLET, MULTILAYER, EXTENDED RELEASE 8 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2080 TABLET, MULTILAYER, EXTENDED RELEASE 8 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2410 TABLET 1 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2512 TABLET 2 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2614 TABLET 4 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2710 TABLET, MULTILAYER, EXTENDED RELEASE 4 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2710 TABLET, MULTILAYER, EXTENDED RELEASE 4 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2716 TABLET 8 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2720 TABLET, MULTILAYER, EXTENDED RELEASE 8 mg ORAL NDA 28 sections
Cardura XL HUMAN PRESCRIPTION DRUG LABEL 1 0049-2720 TABLET, MULTILAYER, EXTENDED RELEASE 8 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2750 TABLET 1 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2760 TABLET 2 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2770 TABLET 4 mg ORAL NDA 28 sections
Cardura HUMAN PRESCRIPTION DRUG LABEL 1 0049-2780 TABLET 8 mg ORAL NDA 28 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2067 TABLET 8 mg ORAL ANDA 26 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2068 TABLET 4 mg ORAL ANDA 26 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2069 TABLET 2 mg ORAL ANDA 26 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0093-2070 TABLET 1 mg ORAL ANDA 26 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0832-0356 TABLET 1 mg ORAL ANDA 28 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0832-0357 TABLET 2 mg ORAL ANDA 28 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0832-1358 TABLET 4 mg ORAL ANDA 28 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0832-1359 TABLET 8 mg ORAL ANDA 28 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5522 TABLET 1 mg ORAL ANDA 18 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5523 TABLET 2 mg ORAL ANDA 18 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5524 TABLET 4 mg ORAL ANDA 18 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 10544-292 TABLET 4 mg ORAL ANDA 24 sections
Doxazosin Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 10544-629 TABLET 1 mg ORAL ANDA 24 sections
Doxazosin HUMAN PRESCRIPTION DRUG LABEL 1 16590-274 TABLET 4 mg ORAL ANDA 12 sections