clonidine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihypertensives, clonidine derivatives 704 4205-90-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • clonidine
  • clonidine hydrochloride
  • clonidine HCl
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
  • Molecular weight: 230.09
  • Formula: C9H9Cl2N3
  • CLOGP: 1.73
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 36.42
  • ALOGS: -2.68
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.45 mg O
0.45 mg P
0.10 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.17 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
EoM (Fraction excreted unchanged in urine) 62 % Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 95 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.56 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 7.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 3, 1974 FDA BOEHRINGER INGELHEIM

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
Temperature regulation disorder 298.64 10.15 126 56865 4081 53287994
Hypertension 267.35 10.15 679 56312 224752 53067323
Completed suicide 238.11 10.15 483 56508 137718 53154357
Food allergy 221.22 10.15 127 56864 8091 53283984
Coeliac disease 216.64 10.15 128 56863 8607 53283468
Bursitis 171.36 10.15 162 56829 22330 53269745
Cardiac failure congestive 153.48 10.15 319 56672 92438 53199637
Immunodeficiency 152.28 10.15 127 56864 14840 53277235
Drug withdrawal syndrome 145.03 10.15 164 56827 27858 53264217
Hypertensive crisis 129.08 10.15 114 56877 14392 53277683
Mental status changes 126.14 10.15 182 56809 39389 53252686
Blood pressure increased 122.65 10.15 379 56612 140100 53151975
Bradycardia 120.60 10.15 247 56744 70809 53221266
Hyperhidrosis 117.99 10.15 295 56696 96498 53195577
Blood pressure inadequately controlled 111.50 10.15 68 56923 4843 53287232
Application site rash 89.94 10.15 48 56943 2648 53289427
Rash erythematous 87.85 10.15 150 56841 37473 53254602
Application site pruritus 85.46 10.15 54 56937 4095 53287980
Overdose 84.27 10.15 280 56711 107456 53184619
Synovitis 83.41 10.15 9 56982 107884 53184191
Nephrogenic systemic fibrosis 80.99 10.15 55 56936 4712 53287363
Sinus bradycardia 79.90 10.15 88 56903 14513 53277562
Poisoning 78.45 10.15 85 56906 13765 53278310
Drug intolerance 78.09 10.15 63 56928 205430 53086645
Fluid retention 77.26 10.15 176 56815 54225 53237850
Cerebrovascular accident 74.95 10.15 265 56726 104909 53187166
Joint swelling 73.98 10.15 85 56906 234553 53057522
Maternal exposure during pregnancy 72.32 10.15 38 56953 155601 53136474
Product adhesion issue 71.71 10.15 54 56937 5443 53286632
Glossodynia 71.18 10.15 11 56980 100280 53191795
Hypertensive encephalopathy 70.82 10.15 27 56964 667 53291408
Infusion related reaction 68.26 10.15 41 56950 155916 53136159
Hypotension 65.46 10.15 480 56511 253596 53038479
Systemic lupus erythematosus 65.45 10.15 26 56965 125388 53166687
Sedation 63.66 10.15 114 56877 29561 53262514
Withdrawal hypertension 62.46 10.15 17 56974 133 53291942
Application site erythema 61.98 10.15 48 56943 5043 53287032
Alopecia 61.74 10.15 97 56894 234486 53057589
Arthropathy 60.77 10.15 38 56953 141415 53150660
Upper respiratory tract infection 60.75 10.15 187 56804 68910 53223165
Body tinea 59.61 10.15 28 56963 1173 53290902
Pericarditis 56.44 10.15 3 56988 64403 53227672
Application site irritation 56.10 10.15 31 56960 1833 53290242
Rash 51.31 10.15 274 56717 445917 52846158
Chronic kidney disease 50.52 10.15 130 56861 43240 53248835
Constipation 49.44 10.15 372 56619 198040 53094035
Neovascularisation 48.00 10.15 20 56971 627 53291448
Accidental exposure to product by child 44.55 10.15 23 56968 1185 53290890
Acute motor-sensory axonal neuropathy 44.26 10.15 16 56975 339 53291736
Malignant hypertension 43.52 10.15 22 56969 1084 53290991
Inhibitory drug interaction 42.71 10.15 28 56963 2262 53289813
Neutropenia 42.64 10.15 65 56926 159120 53132955
Intestinal angioedema 41.59 10.15 18 56973 621 53291454
Wound 41.56 10.15 23 56968 91534 53200541
Abdominal discomfort 40.74 10.15 112 56879 220950 53071125
Infection susceptibility increased 40.10 10.15 28 56963 2509 53289566
Skin induration 39.17 10.15 30 56961 3100 53288975
Nodal rhythm 39.01 10.15 24 56967 1736 53290339
Swelling 38.93 10.15 92 56899 191013 53101062
Myocardial infarction 38.85 10.15 209 56782 99145 53192930
Unresponsive to stimuli 36.68 10.15 98 56893 33328 53258747
Paradoxical drug reaction 33.37 10.15 28 56963 3297 53288778
Abortion spontaneous 33.34 10.15 5 56986 46630 53245445
Hypothermia 33.06 10.15 54 56937 13002 53279073
Therapeutic product effect decreased 32.98 10.15 52 56939 125603 53166472
Febrile neutropenia 31.97 10.15 39 56952 104897 53187178
Product substitution issue 31.56 10.15 59 56932 15807 53276268
Left ventricular hypertrophy 31.24 10.15 33 56958 5190 53286885
Lower respiratory tract infection 30.81 10.15 31 56960 90950 53201125
Glucose tolerance impaired 30.74 10.15 33 56958 5287 53286788
Skin hypertrophy 30.18 10.15 26 56965 3173 53288902
Coronary artery disease 29.85 10.15 91 56900 33346 53258729
Malignant neoplasm progression 29.64 10.15 20 56971 71521 53220554
Arthralgia 29.50 10.15 314 56677 439469 52852606
Cardiac arrest 29.44 10.15 186 56805 93481 53198594
Somnolence 28.92 10.15 290 56701 167444 53124631
Lethargy 28.91 10.15 124 56867 53636 53238439
Helicobacter infection 28.37 10.15 4 56987 39065 53253010
Anti-neutrophil cytoplasmic antibody positive vasculitis 28.26 10.15 22 56969 2329 53289746
C-reactive protein increased 28.10 10.15 19 56972 67867 53224208
Toxicity to various agents 28.05 10.15 358 56633 219240 53072835
Impaired quality of life 27.77 10.15 30 56961 4841 53287234
Duodenal ulcer perforation 27.01 10.15 3 56988 35180 53256895
Medical device site pain 26.65 10.15 10 56981 236 53291839
Infection 26.25 10.15 95 56896 172110 53119965
Nasopharyngitis 26.18 10.15 111 56880 192184 53099891
Respiratory arrest 26.03 10.15 87 56904 33453 53258622
Withdrawal syndrome 25.80 10.15 61 56930 19240 53272835
Discomfort 25.53 10.15 39 56952 95433 53196642
Agitation 25.45 10.15 127 56864 58499 53233576
Miosis 24.97 10.15 34 56957 6968 53285107
Interstitial lung disease 24.81 10.15 16 56975 58606 53233469
Drug ineffective 24.73 10.15 675 56316 816570 52475505
Retrograde amnesia 24.25 10.15 11 56980 425 53291650
Anaesthesia 24.03 10.15 11 56980 434 53291641
Drug dependence 23.60 10.15 63 56928 21409 53270666
Cardio-respiratory arrest 23.22 10.15 124 56867 58634 53233441
Diarrhoea 23.18 10.15 501 56490 625045 52667030
Urinary incontinence 23.09 10.15 79 56912 30742 53261333
Acute myocardial infarction 23.01 10.15 83 56908 33152 53258923
Basal ganglion degeneration 22.89 10.15 11 56980 485 53291590
Hypertensive emergency 22.65 10.15 17 56974 1704 53290371
Contraindicated product administered 22.59 10.15 72 56919 135557 53156518
Condition aggravated 22.47 10.15 206 56785 296928 52995147
Pyrexia 22.01 10.15 301 56690 402892 52889183
Apnoea 21.98 10.15 34 56957 7819 53284256
Blood aldosterone increased 21.76 10.15 8 56983 178 53291897
Accidental overdose 21.60 10.15 61 56930 21418 53270657
Injection site erythema 21.19 10.15 31 56960 77218 53214857
Renin decreased 21.07 10.15 7 56984 114 53291961
Back pain 20.91 10.15 359 56632 233888 53058187
Pulse absent 20.82 10.15 27 56964 5279 53286796
Leukopenia 20.63 10.15 29 56962 73434 53218641
Asthma 20.53 10.15 192 56799 108780 53183295
Impaired healing 20.48 10.15 23 56968 64182 53227893
Medication error 20.42 10.15 85 56906 36280 53255795
Respiratory moniliasis 20.28 10.15 8 56983 217 53291858
Tissue infiltration 20.28 10.15 11 56980 627 53291448
Gastrointestinal disorder 20.23 10.15 41 56950 89963 53202112
Primary hyperaldosteronism 20.22 10.15 6 56985 66 53292009
Norepinephrine increased 19.82 10.15 6 56985 71 53292004
Osteonecrosis of jaw 19.67 10.15 7 56984 36139 53255936
Implant site extravasation 19.26 10.15 10 56981 521 53291554
Encephalomalacia 19.25 10.15 10 56981 522 53291553
Atrioventricular block second degree 18.60 10.15 22 56969 3917 53288158
Sinusitis 18.49 10.15 105 56886 168459 53123616
Peritonitis bacterial 18.47 10.15 35 56956 9470 53282605
Off label use 18.39 10.15 375 56616 471837 52820238
Hyperlipidaemia 18.25 10.15 54 56937 19461 53272614
Implant site infection 18.13 10.15 12 56979 985 53291090
Device infusion issue 17.99 10.15 13 56978 1230 53290845
Hypertrichosis 17.88 10.15 12 56979 1008 53291067
Rheumatoid arthritis 17.80 10.15 233 56758 314298 52977777
Application site discolouration 17.80 10.15 11 56980 802 53291273
Psoriasis 17.66 10.15 42 56949 87047 53205028
Medical device site discharge 17.56 10.15 5 56986 47 53292028
Application site pain 17.54 10.15 22 56969 4161 53287914
Gastrointestinal tract mucosal pigmentation 17.51 10.15 10 56981 630 53291445
Cerebral ischaemia 17.46 10.15 28 56963 6637 53285438
Gamma-glutamyltransferase increased 17.42 10.15 7 56984 33548 53258527
Blood pressure abnormal 17.36 10.15 42 56949 13441 53278634
Renal transplant failure 16.65 10.15 10 56981 692 53291383
Sleep disorder due to general medical condition, insomnia type 16.54 10.15 3 56988 24346 53267729
Dialysis 16.41 10.15 35 56956 10307 53281768
Pernicious anaemia 16.36 10.15 10 56981 715 53291360
Posterior reversible encephalopathy syndrome 16.35 10.15 46 56945 16114 53275961
Drug ineffective for unapproved indication 16.30 10.15 54 56937 20666 53271409
White blood cell count decreased 16.23 10.15 73 56918 124402 53167673
Skin disorder 16.16 10.15 61 56930 24897 53267178
Application site papules 16.09 10.15 5 56986 65 53292010
Hyperlactacidaemia 15.91 10.15 17 56974 2708 53289367
Renal failure 15.91 10.15 195 56796 118257 53173818
Application site vesicles 15.86 10.15 13 56978 1481 53290594
Aggression 15.82 10.15 58 56933 23345 53268730
Hyperaesthesia 15.67 10.15 31 56960 8658 53283417
Focal segmental glomerulosclerosis 15.63 10.15 13 56978 1512 53290563
Tachyphylaxis 15.54 10.15 7 56984 266 53291809
Drug abuser 15.54 10.15 18 56973 3135 53288940
Cardiac hypertrophy 15.23 10.15 11 56980 1040 53291035
Seizure 15.21 10.15 208 56783 129301 53162774
Blister 15.16 10.15 39 56952 78714 53213361
Blood glucose increased 14.92 10.15 137 56854 77224 53214851
Inguinal hernia 14.82 10.15 14 56977 1926 53290149
Irritable bowel syndrome 14.61 10.15 15 56976 43617 53248458
Anhedonia 14.53 10.15 34 56957 10653 53281422
Dry mouth 14.43 10.15 111 56880 59439 53232636
Hepatic function abnormal 14.39 10.15 11 56980 36888 53255187
Medical device site erythema 14.30 10.15 4 56987 35 53292040
Anuria 14.18 10.15 37 56954 12403 53279672
Neutrophil count decreased 14.17 10.15 19 56972 49079 53242996
Delirium 14.10 10.15 84 56907 41345 53250730
Enthesopathy 13.94 10.15 25 56966 6486 53285589
Systolic dysfunction 13.86 10.15 12 56979 1475 53290600
Trichoglossia 13.81 10.15 6 56985 209 53291866
Erythema 13.78 10.15 240 56751 156729 53135346
Uterine enlargement 13.66 10.15 11 56980 1223 53290852
Fibrosis 13.66 10.15 19 56972 3973 53288102
Human ehrlichiosis 13.60 10.15 6 56985 217 53291858
Tremor 13.58 10.15 199 56792 125537 53166538
Sinus arrhythmia 13.58 10.15 12 56979 1515 53290560
Poor quality sleep 13.50 10.15 45 56946 17278 53274797
Hypertensive heart disease 13.20 10.15 15 56976 2558 53289517
Patent ductus arteriosus 13.20 10.15 19 56972 4099 53287976
Disease progression 13.15 10.15 60 56931 101860 53190215
Bone marrow failure 13.04 10.15 8 56983 30107 53261968
Pulmonary renal syndrome 12.97 10.15 7 56984 395 53291680
Neoplasm progression 12.89 10.15 8 56983 29911 53262164
SJS-TEN overlap 12.83 10.15 6 56985 249 53291826
Glomerulonephritis rapidly progressive 12.79 10.15 9 56982 816 53291259
Normochromic normocytic anaemia 12.77 10.15 20 56971 4646 53287429
Injection site abscess 12.74 10.15 10 56981 1071 53291004
Bone density decreased 12.71 10.15 33 56958 11031 53281044
Kidney fibrosis 12.63 10.15 12 56979 1663 53290412
Psoriatic arthropathy 12.58 10.15 20 56971 48170 53243905
Drug reaction with eosinophilia and systemic symptoms 12.51 10.15 10 56981 32790 53259285
Pain in jaw 12.50 10.15 15 56976 40654 53251421
Arthritis 12.11 10.15 50 56941 87248 53204827
Injection site pruritus 12.10 10.15 16 56975 41573 53250502
Purpura 12.09 10.15 32 56959 10821 53281254
Vascular stenosis 12.07 10.15 6 56985 285 53291790
Fanconi syndrome 11.83 10.15 10 56981 1190 53290885
Spinal pain 11.75 10.15 33 56958 11547 53280528
Skin fibrosis 11.75 10.15 9 56982 930 53291145
Femur fracture 11.75 10.15 15 56976 39570 53252505
Blood pressure systolic decreased 11.74 10.15 22 56969 5902 53286173
Cerebral atrophy 11.74 10.15 20 56971 4984 53287091
Intentional product use issue 11.70 10.15 39 56952 72455 53219620
Alanine aminotransferase increased 11.67 10.15 57 56934 95038 53197037
Klebsiella infection 11.64 10.15 26 56965 7900 53284175
Medical device site infection 11.56 10.15 5 56986 172 53291903
Product complaint 11.54 10.15 34 56957 12223 53279852
Labile blood pressure 11.49 10.15 12 56979 1862 53290213
Device expulsion 11.48 10.15 9 56982 29804 53262271
Hypernatraemia 11.47 10.15 24 56967 6973 53285102
Parosmia 11.46 10.15 19 56972 4631 53287444
Medical device site swelling 11.44 10.15 3 56988 20 53292055
Heart rate decreased 11.37 10.15 73 56918 36874 53255201
Application site haematoma 11.31 10.15 3 56988 21 53292054
Extrapyramidal disorder 11.30 10.15 34 56957 12368 53279707
Hepatotoxicity 11.27 10.15 8 56983 27872 53264203
Transient ischaemic attack 11.25 10.15 71 56920 35654 53256421
Implant site haematoma 11.19 10.15 4 56987 82 53291993
Left atrial dilatation 11.12 10.15 12 56979 1933 53290142
End stage renal disease 11.11 10.15 22 56969 6149 53285926
Daydreaming 10.98 10.15 6 56985 347 53291728
Loss of personal independence in daily activities 10.97 10.15 38 56953 69777 53222298
Suspected suicide 10.97 10.15 18 56973 4350 53287725
Melaena 10.96 10.15 9 56982 29120 53262955
COVID-19 10.92 10.15 14 56977 36874 53255201
Glomerulonephritis 10.79 10.15 11 56980 1660 53290415
Infusion site mass 10.72 10.15 9 56982 1060 53291015
Drug detoxification 10.72 10.15 5 56986 206 53291869
Injection site pain 10.68 10.15 74 56917 113317 53178758
Drug dependence, antepartum 10.65 10.15 3 56988 27 53292048
Tic 10.61 10.15 10 56981 1372 53290703
Skin tightness 10.59 10.15 17 56974 4034 53288041
Exposure via ingestion 10.41 10.15 15 56976 3240 53288835
Psychogenic seizure 10.39 10.15 11 56980 1734 53290341
Mobility decreased 10.38 10.15 44 56947 76227 53215848
Pregnancy 10.31 10.15 11 56980 31430 53260645
Anxiety 10.26 10.15 279 56712 196425 53095650
Rash maculo-papular 10.22 10.15 10 56981 29739 53262336
Joint contracture 10.19 10.15 11 56980 1773 53290302
Laboratory test interference 10.15 10.15 7 56984 615 53291460

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
Completed suicide 217.58 11.42 394 38557 92123 32382452
Drug withdrawal syndrome 172.14 11.42 163 38788 20068 32454507
Hypertension 148.79 11.42 419 38532 131331 32343244
Aggression 126.31 11.42 193 38758 39196 32435379
Withdrawal hypertension 125.41 11.42 28 38923 70 32474505
Bradycardia 123.62 11.42 268 38683 71294 32403281
Hypertensive crisis 94.63 11.42 81 38870 8736 32465839
Oppositional defiant disorder 78.72 11.42 28 38923 501 32474074
Decreased eye contact 72.69 11.42 26 38925 473 32474102
Application site rash 69.35 11.42 29 38922 815 32473760
Drug dependence 68.21 11.42 110 38841 23374 32451201
Febrile neutropenia 68.09 11.42 29 38922 119537 32355038
Respiratory depression 67.13 11.42 81 38870 13130 32461445
Choreoathetosis 66.39 11.42 30 38921 1021 32473554
Blood pressure inadequately controlled 66.07 11.42 41 38910 2681 32471894
Blood pressure increased 65.87 11.42 227 38724 79127 32395448
Sedation 65.40 11.42 95 38856 18431 32456144
Victim of child abuse 64.66 11.42 27 38924 756 32473819
Miosis 60.78 11.42 63 38888 8641 32465934
Sinus bradycardia 60.38 11.42 76 38875 12862 32461713
Cardiac failure congestive 59.67 11.42 230 38721 84622 32389953
Anxiety 59.35 11.42 250 38701 95755 32378820
Product substitution issue 58.02 11.42 67 38884 10369 32464206
Agitation 57.68 11.42 175 38776 57061 32417514
Withdrawal syndrome 56.24 11.42 71 38880 12051 32462524
Accidental exposure to product by child 51.52 11.42 29 38922 1582 32472993
Dystonia 50.53 11.42 63 38888 10560 32464015
Mental status changes 49.21 11.42 128 38823 38209 32436366
Crying 49.16 11.42 47 38904 5849 32468726
Hypotension 48.47 11.42 432 38519 215678 32258897
Trismus 48.08 11.42 33 38918 2562 32472013
Bruxism 47.94 11.42 28 38923 1639 32472936
Homicidal ideation 47.11 11.42 33 38918 2647 32471928
Product adhesion issue 47.00 11.42 27 38924 1532 32473043
Pyrexia 44.95 11.42 214 38737 319754 32154821
Tic 44.50 11.42 29 38922 2065 32472510
Somnolence 43.66 11.42 242 38709 103555 32371020
Nephrogenic systemic fibrosis 42.71 11.42 38 38913 4314 32470261
Neutropenia 41.89 11.42 66 38885 142109 32332466
Interstitial lung disease 41.65 11.42 13 38938 64988 32409587
Lethargy 41.47 11.42 126 38825 41102 32433473
Irritability 40.98 11.42 91 38860 24563 32450012
Catatonia 38.25 11.42 37 38914 4671 32469904
Cerebrovascular accident 38.14 11.42 204 38747 86116 32388459
Suicidal ideation 37.94 11.42 116 38835 37967 32436608
Pneumonia 36.83 11.42 262 38689 354990 32119585
Hepatic function abnormal 34.60 11.42 6 38945 44834 32429741
Psychomotor hyperactivity 34.32 11.42 48 38903 8991 32465584
Hypertensive emergency 33.89 11.42 18 38933 875 32473700
Malignant catatonia 33.77 11.42 12 38939 214 32474361
Thrombocytopenia 33.16 11.42 81 38870 148218 32326357
Overweight 32.74 11.42 22 38929 1649 32472926
Dyskinesia 32.56 11.42 81 38870 23522 32451053
Pancytopenia 32.29 11.42 37 38914 91198 32383377
Neuroleptic malignant syndrome 31.85 11.42 67 38884 17428 32457147
Application site pruritus 31.35 11.42 20 38931 1373 32473202
Blood prolactin increased 31.13 11.42 21 38930 1584 32472991
Hyperaesthesia 30.72 11.42 30 38921 3832 32470743
Unresponsive to stimuli 30.25 11.42 87 38864 27522 32447053
Rheumatoid arthritis 30.21 11.42 8 38943 44536 32430039
Obesity 29.97 11.42 48 38903 10134 32464441
Respiratory arrest 29.67 11.42 89 38862 28819 32445756
Hypotonia 29.45 11.42 41 38910 7646 32466929
Cardiac arrest 29.04 11.42 207 38744 96569 32378006
Device failure 29.00 11.42 23 38928 2228 32472347
Application site erythema 28.19 11.42 23 38928 2320 32472255
Affect lability 27.87 11.42 28 38923 3700 32470875
Malignant neoplasm progression 25.50 11.42 34 38917 78462 32396113
Child abuse 25.09 11.42 11 38940 348 32474227
Accelerated hypertension 25.04 11.42 10 38941 249 32474326
Emotional distress 24.67 11.42 58 38893 16248 32458327
Epidural lipomatosis 24.25 11.42 13 38938 644 32473931
Accidental overdose 24.22 11.42 64 38887 19275 32455300
Inadequate analgesia 24.20 11.42 23 38928 2840 32471735
Serotonin syndrome 23.67 11.42 63 38888 19054 32455521
Application site irritation 23.34 11.42 13 38938 695 32473880
Toxicity to various agents 23.25 11.42 320 38631 177721 32296854
Overdose 23.14 11.42 181 38770 86896 32387679
Poisoning 23.00 11.42 45 38906 11113 32463462
Autonomic nervous system imbalance 22.47 11.42 21 38930 2539 32472036
Suspected suicide 21.29 11.42 22 38929 3006 32471569
Corneal reflex decreased 21.17 11.42 8 38943 171 32474404
Anger 20.98 11.42 45 38906 11859 32462716
Kidney transplant rejection 20.72 11.42 35 38916 7720 32466855
Insomnia 20.59 11.42 197 38754 100151 32374424
Pain 20.53 11.42 327 38624 187229 32287346
Drug tolerance 20.30 11.42 19 38932 2302 32472273
Product compounding quality issue 19.71 11.42 5 38946 25 32474550
Abnormal behaviour 19.61 11.42 73 38878 26393 32448182
Axillary pain 19.55 11.42 9 38942 320 32474255
Platelet count decreased 19.52 11.42 71 38880 114520 32360055
Coordination abnormal 19.43 11.42 34 38917 7714 32466861
Speech disorder 19.11 11.42 72 38879 26181 32448394
Metabolic alkalosis 19.04 11.42 15 38936 1439 32473136
Fibrosis 18.74 11.42 19 38932 2538 32472037
Injury 18.74 11.42 64 38887 22181 32452394
Labile hypertension 18.70 11.42 6 38945 77 32474498
Mood altered 18.47 11.42 36 38915 8868 32465707
Drug screen positive 18.35 11.42 24 38927 4217 32470358
Tourette's disorder 18.29 11.42 6 38945 83 32474492
Aplastic anaemia 18.03 11.42 32 38919 7341 32467234
Medical device site pain 17.60 11.42 6 38945 94 32474481
Tardive dyskinesia 17.56 11.42 27 38924 5504 32469071
General physical health deterioration 17.36 11.42 75 38876 115184 32359391
Product administered to patient of inappropriate age 17.27 11.42 19 38932 2787 32471788
Attention deficit hyperactivity disorder 17.25 11.42 17 38934 2195 32472380
Reaction to excipient 16.88 11.42 9 38942 441 32474134
Streptococcal infection 16.86 11.42 25 38926 4937 32469638
Implant site extravasation 16.84 11.42 9 38942 443 32474132
Hyperkinesia 16.80 11.42 17 38934 2265 32472310
Neutrophil count decreased 16.79 11.42 19 38932 47120 32427455
Atrioventricular block first degree 16.59 11.42 27 38924 5776 32468799
Labelled drug-drug interaction issue 16.29 11.42 6 38945 119 32474456
Brief psychotic disorder with marked stressors 16.22 11.42 7 38944 213 32474362
Skin tightness 16.20 11.42 16 38935 2071 32472504
Device infusion issue 16.18 11.42 10 38941 649 32473926
Poor quality sleep 15.97 11.42 32 38919 8042 32466533
Diarrhoea 15.94 11.42 325 38626 364477 32110098
Oromandibular dystonia 15.87 11.42 9 38942 498 32474077
Loss of consciousness 15.81 11.42 160 38791 82547 32392028
Gastrointestinal tract mucosal pigmentation 15.67 11.42 8 38943 358 32474217
Respiratory rate decreased 15.55 11.42 15 38936 1887 32472688
Device power source issue 15.45 11.42 8 38943 369 32474206
Renal artery stenosis 15.34 11.42 15 38936 1918 32472657
Double inlet left ventricle 15.16 11.42 4 38947 24 32474551
Galactorrhoea 15.13 11.42 8 38943 385 32474190
Metastases to eye 14.99 11.42 5 38946 73 32474502
Mast cell degranulation present 14.99 11.42 5 38946 73 32474502
Accidental poisoning 14.94 11.42 9 38942 558 32474017
Anhedonia 14.92 11.42 32 38919 8432 32466143
Myocardial infarction 14.83 11.42 222 38729 125454 32349121
Drooling 14.80 11.42 19 38932 3278 32471297
Cardio-respiratory arrest 14.65 11.42 116 38835 55873 32418702
Autoimmune enteropathy 14.63 11.42 4 38947 28 32474547
Hypoxic-ischaemic encephalopathy 14.45 11.42 23 38928 4831 32469744
Juvenile idiopathic arthritis 14.39 11.42 13 38938 1505 32473070
Peritonitis bacterial 14.29 11.42 40 38911 12456 32462119
Infection 14.09 11.42 53 38898 84662 32389913
Therapeutic response decreased 14.08 11.42 65 38886 25855 32448720
Drug withdrawal maintenance therapy 13.98 11.42 5 38946 91 32474484
Renal transplant 13.90 11.42 14 38937 1855 32472720
Post transplant distal limb syndrome 13.88 11.42 7 38944 305 32474270
Inflammation 13.83 11.42 6 38945 24487 32450088
Lower respiratory tract infection 13.81 11.42 9 38942 29234 32445341
Impulsive behaviour 13.78 11.42 15 38936 2174 32472401
Hyperhidrosis 13.75 11.42 138 38813 71030 32403545
Univentricular heart 13.65 11.42 4 38947 37 32474538
Transcription medication error 13.59 11.42 6 38945 193 32474382
Cardiac failure 13.58 11.42 60 38891 91613 32382962
Skin induration 13.57 11.42 15 38936 2213 32472362
Pneumocystis jirovecii pneumonia 13.55 11.42 3 38948 18867 32455708
Intentional self-injury 13.52 11.42 42 38909 13858 32460717
Product prescribing error 13.47 11.42 53 38898 19664 32454911
Sprue-like enteropathy 13.44 11.42 8 38943 485 32474090
Disease progression 13.39 11.42 56 38895 86806 32387769
Hydrocele male infected 13.37 11.42 4 38947 40 32474535
Skin hypertrophy 13.25 11.42 16 38935 2595 32471980
Tremor 13.10 11.42 152 38799 81125 32393450
Harlequin syndrome 13.04 11.42 3 38948 9 32474566
Product prescribing issue 13.03 11.42 11 38940 1164 32473411
Toxic epidermal necrolysis 12.98 11.42 54 38897 20539 32454036
Incision site pain 12.90 11.42 14 38937 2023 32472552
Rash 12.89 11.42 175 38776 209158 32265417
Agranulocytosis 12.86 11.42 6 38945 23471 32451104
Sepsis 12.81 11.42 125 38826 158709 32315866
Rash maculo-papular 12.73 11.42 9 38942 28013 32446562
Infusion site mass 12.64 11.42 6 38945 229 32474346
C-reactive protein increased 12.62 11.42 24 38927 48078 32426497
End stage renal disease 12.61 11.42 29 38922 8008 32466567
Product preparation issue 12.59 11.42 6 38945 231 32474344
Cardiomyopathy 12.56 11.42 45 38906 15968 32458607
Electrocardiogram PR prolongation 12.49 11.42 9 38942 755 32473820
Hyperbilirubinaemia 12.37 11.42 3 38948 17727 32456848
Chronic kidney disease 12.26 11.42 86 38865 39889 32434686
Septic shock 12.24 11.42 42 38909 68947 32405628
White blood cell count decreased 12.16 11.42 62 38889 91136 32383439
Osteonecrosis of jaw 11.98 11.42 4 38947 19162 32455413
Productive cough 11.88 11.42 14 38937 34102 32440473
Hypervolaemia 11.82 11.42 15 38936 2559 32472016
Cytomegalovirus infection 11.80 11.42 8 38943 25456 32449119
Joint contracture 11.69 11.42 13 38938 1930 32472645
Stomatitis 11.52 11.42 19 38932 40210 32434365
Nervousness 11.49 11.42 37 38914 12442 32462133
Muscle spasticity 11.47 11.42 23 38928 5782 32468793

Pharmacologic Action:

SourceCodeDescription
ATC C02AC01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIADRENERGIC AGENTS, CENTRALLY ACTING
Imidazoline receptor agonists
ATC N02CX02 NERVOUS SYSTEM
ANALGESICS
ANTIMIGRAINE PREPARATIONS
Other antimigraine preparations
ATC S01EA04 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Sympathomimetics in glaucoma therapy
ATC C02LC01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
Imidazoline receptor agonists in combination with diuretics
ATC C02LC51 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
Imidazoline receptor agonists in combination with diuretics
FDA MoA N0000009918 Adrenergic alpha2-Agonists
FDA EPC N0000175554 Central alpha-2 Adrenergic Agonist
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D000700 Analgesics
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D013565 Sympatholytics
CHEBI has role CHEBI:35569 alpha-adrenergic receptor agonist
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:66991 sympatholytics

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Severe pain indication 76948002
Open-angle glaucoma indication 84494001 DOID:1067
Attention deficit hyperactivity disorder indication 406506008
Increased Intraocular Pressure after Ocular Procedure indication
Ocular hypertension off-label use 4210003 DOID:9282
Gilles de la Tourette's syndrome off-label use 5158005 DOID:11119
Pain off-label use 22253000
Diarrhea off-label use 62315008
Opioid withdrawal off-label use 87132004
Menopausal flushing off-label use 198436008
Smoking cessation assistance off-label use 384742004
Nicotine Withdrawal Symptoms off-label use
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Myocardial infarction contraindication 22298006 DOID:5844
Depressive disorder contraindication 35489007
Hyperuricemia contraindication 35885006 DOID:1920
Hypokalemia contraindication 43339004
Diabetes mellitus type 2 contraindication 44054006 DOID:9352
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Tear film insufficiency contraindication 46152009
End stage renal disease contraindication 46177005 DOID:784
Diabetes mellitus type 1 contraindication 46635009 DOID:9744
Bradycardia contraindication 48867003
Sinus bradycardia contraindication 49710005
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Cerebrovascular disease contraindication 62914000 DOID:6713
Blood coagulation disorder contraindication 64779008 DOID:1247
Hypercalcemia contraindication 66931009 DOID:12678
Hypochloremic alkalosis contraindication 70134007
Decreased respiratory function contraindication 80954004
Oliguria contraindication 83128009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Magnetic resonance imaging contraindication 113091000
Perioperative care contraindication 133897009
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Atrioventricular block contraindication 233917008 DOID:0050820
Labor pain contraindication 247412007
Raynaud's phenomenon contraindication 266261006
Syncope contraindication 271594007
Surgical procedure contraindication 387713003
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Myocardial ischemia contraindication 414795007 DOID:3393
Inflammatory dermatosis contraindication 703938007
Vagal Reflex Bradycardia contraindication
Severe Cardiopulmonary Disease contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.5 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-2C adrenergic receptor GPCR AGONIST EC50 6.70 WOMBAT-PK CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST Ki 8.42 CHEMBL CHEMBL
Alpha-2B adrenergic receptor GPCR AGONIST Ki 7.50 CHEMBL CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 6.22 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 6.50 PDSP
Solute carrier family 22 member 1 Transporter IC50 4.65 CHEMBL
Solute carrier family 22 member 2 Transporter IC50 4.80 WOMBAT-PK
Multidrug and toxin extrusion protein 1 Transporter IC50 4.48 CHEMBL
Nischarin Membrane receptor Ki 8.05 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.49 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 6.50 PDSP
Alpha-1B adrenergic receptor GPCR Ki 5.99 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR Kd 6.59 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 8.08 CHEMBL
Alpha-1D adrenergic receptor GPCR AGONIST Ki 6.90 IUPHAR
5-hydroxytryptamine receptor 1A GPCR IC50 5.27 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 9.41 CHEMBL
Alpha-1A adrenergic receptor GPCR EC50 7.05 CHEMBL
Alpha-2A adrenergic receptor GPCR IC50 8.70 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 4.40 CHEMBL
Nischarin Unclassified Ki 6.95 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 Ion channel BLOCKER IC50 4.40 IUPHAR
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 Ion channel BLOCKER IC50 5.10 IUPHAR
Adrenergic receptor alpha-2 GPCR Ki 8.82 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel BLOCKER IC50 5 IUPHAR
Alpha-1B adrenergic receptor GPCR EC50 7.08 CHEMBL

External reference:

IDSource
4017850 VUID
N0000146207 NUI
D00281 KEGG_DRUG
4205-91-8 SECONDARY_CAS_RN
C0009014 UMLSCUI
CHEBI:46631 CHEBI
CLU PDB_CHEM_ID
CHEMBL134 ChEMBL_ID
DB00575 DRUGBANK_ID
CHEMBL1705 ChEMBL_ID
D003000 MESH_DESCRIPTOR_UI
2803 PUBCHEM_CID
2624 INN_ID
516 IUPHAR_LIGAND_ID
MN3L5RMN02 UNII
142432 RXNORM
27687 MMSL
381 MMSL
4478 MMSL
4479 MMSL
89106 MMSL
d00044 MMSL
000644 NDDF
004495 NDDF
372805007 SNOMEDCT_US
387121001 SNOMEDCT_US
62782004 SNOMEDCT_US
4017849 VANDF
4017850 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9723 INJECTION, SOLUTION 500 ug INTRAVENOUS ANDA 21 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9724 INJECTION, SOLUTION 100 ug INTRAVENOUS ANDA 21 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2127 TABLET 0.10 mg ORAL ANDA 12 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2128 TABLET 0.20 mg ORAL ANDA 12 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2129 TABLET 0.30 mg ORAL ANDA 12 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-4241 TABLET, EXTENDED RELEASE 0.10 mg ORAL ANDA 19 sections
Clonidine HUMAN PRESCRIPTION DRUG LABEL 1 0378-0871 PATCH 0.10 mg TRANSDERMAL ANDA 16 sections
Clonidine HUMAN PRESCRIPTION DRUG LABEL 1 0378-0872 PATCH 0.20 mg TRANSDERMAL ANDA 16 sections
Clonidine HUMAN PRESCRIPTION DRUG LABEL 1 0378-0873 PATCH 0.30 mg TRANSDERMAL ANDA 16 sections
Clonidine transdermal system HUMAN PRESCRIPTION DRUG LABEL 1 0591-3508 PATCH 0.10 mg TRANSDERMAL ANDA 21 sections
Clonidine transdermal system HUMAN PRESCRIPTION DRUG LABEL 1 0591-3509 PATCH 0.20 mg TRANSDERMAL ANDA 21 sections
Clonidine transdermal system HUMAN PRESCRIPTION DRUG LABEL 1 0591-3510 PATCH 0.30 mg TRANSDERMAL ANDA 21 sections
Catapres-TTS HUMAN PRESCRIPTION DRUG LABEL 1 0597-0031 PATCH 0.10 mg TRANSDERMAL NDA 23 sections
Catapres-TTS HUMAN PRESCRIPTION DRUG LABEL 1 0597-0032 PATCH 0.20 mg TRANSDERMAL NDA 23 sections
Catapres-TTS HUMAN PRESCRIPTION DRUG LABEL 1 0597-0033 PATCH 0.30 mg TRANSDERMAL NDA 23 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-2572 TABLET 0.10 mg ORAL ANDA 18 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-2574 TABLET 0.30 mg ORAL ANDA 18 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8272 TABLET 0.20 mg ORAL ANDA 12 sections
CLONIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10135-708 TABLET 0.10 mg ORAL ANDA 20 sections
CLONIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10135-709 TABLET 0.20 mg ORAL ANDA 20 sections
CLONIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10135-710 TABLET 0.30 mg ORAL ANDA 20 sections
Clonidine HydrochlorideExtended-Release HUMAN PRESCRIPTION DRUG LABEL 1 10370-257 TABLET, EXTENDED RELEASE 0.10 mg ORAL ANDA 26 sections
Clonidine HydrochlorideExtended-Release HUMAN PRESCRIPTION DRUG LABEL 1 10370-302 TABLET, EXTENDED RELEASE 0.20 mg ORAL ANDA 26 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-042 TABLET 0.30 mg ORAL ANDA 20 sections
CLONIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 10544-158 TABLET 0.20 mg ORAL ANDA 21 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-196 TABLET 0.10 mg ORAL ANDA 24 sections
Clonidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-199 TABLET 0.20 mg ORAL ANDA 24 sections
Clonidine HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 12634-465 TABLET 0.10 mg ORAL ANDA 14 sections
CLONIDINE HUMAN PRESCRIPTION DRUG LABEL 1 16590-266 TABLET 0.10 mg ORAL ANDA 10 sections
CLONIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 16590-267 TABLET 0.20 mg ORAL ANDA 11 sections