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

Stem definitionDrug idCAS RN
726 64-86-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • colchicine
  • colchisol
  • colcin
A major alkaloid from Colchicum autumnale L. and found also in other Colchicum species. Its primary therapeutic use is in the treatment of gout, but it has been used also in the therapy of familial Mediterranean fever (PERIODIC DISEASE). Potential to limit COVID-19-related myocardial damage has been hypothesized based on the drug’s mechanisms of action and promising results of ongoing research on colchicine in various cardiac conditions. However, the drug's safety and efficacy for treatment of COVID-19 is not yet established.
  • Molecular weight: 399.44
  • Formula: C22H25NO6
  • CLOGP: 1.20
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 83.09
  • ALOGS: -4.16
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
1 mg O
1 mg P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.29 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
S (Water solubility) 45 mg/mL Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 6.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.61 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 58 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 27, 1961 FDA MERCK

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
Gout 292.88 12.82 130 21444 11226 46653262
Panniculitis 124.00 12.82 58 21516 5646 46658842
Enthesopathy 121.87 12.82 54 21520 4636 46659852
Tenosynovitis 106.03 12.82 57 21517 7458 46657030
Blood parathyroid hormone decreased 96.63 12.82 45 21529 4336 46660152
Red blood cell sedimentation rate 89.80 12.82 33 21541 1740 46662748
Granuloma skin 87.10 12.82 39 21535 3431 46661057
Acute kidney injury 80.00 12.82 265 21309 235590 46428898
Drug interaction 78.75 12.82 239 21335 202855 46461633
Tongue disorder 78.13 12.82 46 21528 7164 46657324
Skin necrosis 78.09 12.82 49 21525 8555 46655933
Drug reaction with eosinophilia and systemic symptoms 76.97 12.82 81 21493 29467 46635021
Urticarial vasculitis 75.95 12.82 21 21553 433 46664055
Rheumatoid nodule 73.51 12.82 48 21526 8972 46655516
Diarrhoea 70.46 12.82 470 21104 559132 46105356
Toxicity to various agents 67.42 12.82 233 21341 211533 46452955
Tendonitis 66.17 12.82 54 21520 14223 46650265
Hypersensitivity vasculitis 62.31 12.82 33 21541 4188 46660300
Ulcer 56.95 12.82 54 21520 17338 46647150
Rhabdomyolysis 52.93 12.82 80 21494 41829 46622659
Hypercalcaemia 51.81 12.82 56 21518 20990 46643498
Loss of employment 51.38 12.82 20 21554 1236 46663252
Drug resistance 45.91 12.82 48 21526 17320 46647168
Familial mediterranean fever 45.46 12.82 9 21565 37 46664451
Drug eruption 44.38 12.82 52 21522 21277 46643211
Gouty tophus 43.06 12.82 11 21563 165 46664323
Skin ulcer 42.47 12.82 63 21511 32395 46632093
Psoriatic arthropathy 41.13 12.82 66 21508 36313 46628175
C-reactive protein abnormal 39.58 12.82 49 21525 21221 46643267
Basal cell carcinoma 39.42 12.82 48 21526 20439 46644049
Pericarditis 38.06 12.82 51 21523 23876 46640612
Aspartate aminotransferase increased 35.60 12.82 98 21476 78602 46585886
Chronic kidney disease 34.27 12.82 65 21509 40806 46623682
Pericardial effusion 34.02 12.82 50 21524 25493 46638995
Multiple organ dysfunction syndrome 33.60 12.82 74 21500 51636 46612852
Enterococcal sepsis 33.43 12.82 15 21559 1325 46663163
Alanine aminotransferase increased 33.16 12.82 103 21471 88348 46576140
Pancytopenia 32.77 12.82 100 21474 84958 46579530
Hepatocellular injury 32.61 12.82 53 21521 29469 46635019
Myopathy 31.82 12.82 29 21545 8852 46655636
Neuromyopathy 31.22 12.82 11 21563 513 46663975
Metabolic acidosis 30.47 12.82 60 21514 38720 46625768
Alanine aminotransferase abnormal 29.70 12.82 17 21557 2510 46661978
Rash pruritic 29.55 12.82 64 21510 44151 46620337
Drug intolerance 29.27 12.82 140 21434 146909 46517579
Acute febrile neutrophilic dermatosis 28.74 12.82 17 21557 2668 46661820
International normalised ratio increased 28.12 12.82 65 21509 46818 46617670
Behcet's syndrome 27.79 12.82 7 21567 99 46664389
C-reactive protein increased 27.53 12.82 74 21500 58516 46605972
Fear of injection 26.51 12.82 19 21555 4128 46660360
Gouty arthritis 24.07 12.82 9 21565 498 46663990
Parotid gland enlargement 23.42 12.82 10 21564 784 46663704
Hypertriglyceridaemia 23.17 12.82 20 21554 5684 46658804
Blood creatine phosphokinase increased 23.12 12.82 44 21530 27680 46636808
Appetite disorder 22.53 12.82 19 21555 5235 46659253
Red blood cell sedimentation rate increased 22.49 12.82 39 21535 22850 46641638
Leukopenia 22.37 12.82 76 21498 68267 46596221
Disseminated intravascular coagulation 20.82 12.82 34 21540 18971 46645517
Seizure 20.61 12.82 16 21558 123038 46541450
Iodine allergy 19.77 12.82 8 21566 548 46663940
Inflammation 19.39 12.82 58 21516 48723 46615765
Loss of personal independence in daily activities 19.07 12.82 64 21510 57119 46607369
Hyperferritinaemia 19.04 12.82 5 21569 84 46664404
Amegakaryocytic thrombocytopenia 18.95 12.82 4 21570 24 46664464
Natural killer cell count 18.95 12.82 4 21570 24 46664464
Maternal exposure during pregnancy 18.94 12.82 12 21562 102537 46561951
Bone marrow failure 18.75 12.82 42 21532 29627 46634861
Macrophages increased 18.54 12.82 4 21570 27 46664461
Chondrocalcinosis pyrophosphate 18.35 12.82 9 21565 972 46663516
Rash maculo-papular 18.22 12.82 40 21534 27834 46636654
Allergy to metals 17.95 12.82 7 21567 435 46664053
Acarodermatitis 17.77 12.82 8 21566 712 46663776
Axial spondyloarthritis 17.61 12.82 5 21569 114 46664374
Myopathy toxic 17.15 12.82 6 21568 274 46664214
Cutaneous tuberculosis 16.53 12.82 5 21569 143 46664345
Malignant neoplasm progression 16.06 12.82 5 21569 64921 46599567
Meningocele 15.89 12.82 3 21571 9 46664479
Polyarteritis nodosa 15.84 12.82 6 21568 344 46664144
Autoinflammatory disease 15.66 12.82 4 21570 60 46664428
Therapy non-responder 15.48 12.82 48 21526 41104 46623384
Drug abuse 15.47 12.82 5 21569 63403 46601085
Joint injury 15.42 12.82 30 21544 19179 46645309
Drug hypersensitivity 15.26 12.82 176 21398 243649 46420839
Myalgia 15.09 12.82 103 21471 122985 46541503
Synovitis 15.04 12.82 62 21512 61013 46603475
Cardiac tamponade 14.90 12.82 14 21560 4440 46660048
White blood cell count decreased 14.84 12.82 18 21556 112213 46552275
Toxic epidermal necrolysis 14.60 12.82 32 21542 22246 46642242
Memory impairment 14.34 12.82 9 21565 77328 46587160
Vasculitis 14.31 12.82 24 21550 13687 46650801
Product use issue 13.95 12.82 83 21491 94561 46569927
White blood cells urine positive 13.93 12.82 13 21561 4087 46660401
Febrile neutropenia 13.80 12.82 14 21560 94613 46569875
Mesenteric vein thrombosis 13.73 12.82 7 21567 821 46663667
Angiopathy 13.50 12.82 13 21561 4250 46660238
Acute lung injury 13.48 12.82 8 21566 1263 46663225
Neutrophilia 13.25 12.82 11 21563 2966 46661522
Drug tolerance decreased 12.99 12.82 11 21563 3048 46661440
Left ventricular dilatation 12.95 12.82 5 21569 302 46664186

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
Gout 697.11 11.70 326 25413 16989 29909750
Enthesopathy 155.98 11.70 67 25672 2839 29923900
Neuromyopathy 151.40 11.70 49 25690 923 29925816
Tenosynovitis 146.86 11.70 68 25671 3447 29923292
Drug interaction 141.81 11.70 434 25305 199134 29727605
Myopathy 130.11 11.70 92 25647 10494 29916245
Rhabdomyolysis 126.50 11.70 209 25530 63371 29863368
Acute kidney injury 124.42 11.70 514 25225 273328 29653411
Tongue disorder 116.31 11.70 62 25677 4260 29922479
Diarrhoea 113.80 11.70 576 25163 333527 29593212
Toxicity to various agents 104.64 11.70 362 25377 176821 29749918
C-reactive protein abnormal 103.99 11.70 63 25676 5530 29921209
Synovitis 88.97 11.70 71 25668 9712 29917027
Alanine aminotransferase abnormal 86.13 11.70 43 25696 2576 29924163
Familial mediterranean fever 79.56 11.70 15 25724 17 29926722
Pericarditis 68.90 11.70 58 25681 8548 29918191
Drug reaction with eosinophilia and systemic symptoms 66.74 11.70 101 25638 28387 29898352
Tendonitis 66.08 11.70 55 25684 7981 29918758
Drug abuse 58.14 11.70 3 25736 82069 29844670
Loss of personal independence in daily activities 52.79 11.70 78 25661 21457 29905282
Myopathy toxic 52.57 11.70 18 25721 406 29926333
Type 2 lepra reaction 50.22 11.70 17 25722 370 29926369
Blood uric acid increased 49.05 11.70 41 25698 5982 29920757
Aspartate aminotransferase increased 41.17 11.70 134 25605 63288 29863451
Behcet's syndrome 40.64 11.70 10 25729 64 29926675
Metabolic acidosis 40.08 11.70 95 25644 37366 29889373
Psoriatic arthropathy 39.94 11.70 58 25681 15703 29911036
Drug intolerance 37.22 11.70 104 25635 45187 29881552
Treatment failure 37.15 11.70 88 25651 34591 29892148
Therapeutic response decreased 35.50 11.70 70 25669 24279 29902460
Oligoasthenozoospermia 35.44 11.70 7 25732 12 29926727
Alanine aminotransferase increased 33.91 11.70 140 25599 74136 29852603
Gouty arthritis 33.74 11.70 17 25722 1038 29925701
Renal failure 31.47 11.70 204 25535 128762 29797977
Death 31.23 11.70 180 25559 357103 29569636
Spermatozoa progressive motility decreased 30.02 11.70 9 25730 130 29926609
Malignant neoplasm progression 27.30 11.70 14 25725 72273 29854466
Gouty tophus 25.81 11.70 8 25731 130 29926609
Myalgia 25.70 11.70 132 25607 76535 29850204
Herbal interaction 25.45 11.70 10 25729 336 29926403
Erythema 25.03 11.70 132 25607 77319 29849420
Hypertrophic osteoarthropathy 24.62 11.70 7 25732 83 29926656
Myositis 24.58 11.70 37 25702 10340 29916399
Agranulocytosis 22.76 11.70 55 25684 21887 29904852
Scrotal erythema 22.27 11.70 5 25734 20 29926719
Cholestasis 22.19 11.70 59 25680 24891 29901848
Pericardial effusion 21.93 11.70 53 25686 21091 29905648
Drug hypersensitivity 21.60 11.70 116 25623 68403 29858336
Insulin autoimmune syndrome 21.54 11.70 8 25731 230 29926509
Multiple organ dysfunction syndrome 21.06 11.70 109 25630 63378 29863361
Overdose 20.91 11.70 134 25605 84203 29842536
Bradycardia foetal 20.88 11.70 8 25731 251 29926488
Chondrocalcinosis 20.59 11.70 8 25731 261 29926478
Leukocytosis 20.30 11.70 52 25687 21450 29905289
Seizure 19.67 11.70 34 25705 98441 29828298
Disease progression 19.46 11.70 24 25715 79850 29846889
Serum amyloid A protein increased 18.71 11.70 4 25735 12 29926727
Mixed dementia 18.63 11.70 7 25732 208 29926531
Sinus arrhythmia 18.34 11.70 10 25729 718 29926021
Biopsy muscle abnormal 18.18 11.70 3 25736 0 29926739
Pneumonia 18.09 11.70 192 25547 334114 29592625
Hepatitis acute 17.85 11.70 26 25713 7057 29919682
Aggression 17.49 11.70 5 25734 36902 29889837
Genital ulceration 16.47 11.70 6 25733 163 29926576
Skin hyperpigmentation 15.82 11.70 16 25723 2978 29923761
Chondrocalcinosis pyrophosphate 15.26 11.70 9 25730 751 29925988
Thrombocytopenic purpura 14.72 11.70 10 25729 1068 29925671
Chronic kidney disease 14.71 11.70 68 25671 37770 29888969
Pancytopenia 14.69 11.70 124 25615 84928 29841811
Hepatosplenomegaly neonatal 14.68 11.70 4 25735 40 29926699
Somnolence 14.66 11.70 39 25700 96724 29830015
Thrombocytopenia 14.64 11.70 181 25558 136863 29789876
Angioedema 14.27 11.70 63 25676 34321 29892418
Blood creatine phosphokinase increased 13.65 11.70 74 25665 43774 29882965
Gastrointestinal disorder 13.59 11.70 54 25685 28083 29898656
Sperm concentration decreased 13.49 11.70 5 25734 143 29926596
Narcolepsy 13.46 11.70 7 25732 457 29926282
Cellulitis 13.27 11.70 77 25662 46707 29880032
Necrotising colitis 13.20 11.70 9 25730 967 29925772
Skin plaque 13.17 11.70 16 25723 3646 29923093
Stomatitis 12.95 11.70 8 25731 37271 29889468
Completed suicide 12.68 11.70 136 25603 99356 29827383
Quadriparesis 12.67 11.70 9 25730 1032 29925707
Thrombocytosis 12.42 11.70 15 25724 3398 29923341
Hepatocellular injury 12.39 11.70 49 25690 25422 29901317
Brain hypoxia 12.29 11.70 6 25733 342 29926397
Arthralgia 12.27 11.70 174 25565 135617 29791122

Pharmacologic Action:

SourceCodeDescription
ATC M04AC01 MUSCULO-SKELETAL SYSTEM
ANTIGOUT PREPARATIONS
ANTIGOUT PREPARATIONS
Preparations with no effect on uric acid metabolism
FDA MoA N0000000239 P-Glycoprotein Interactions
MeSH PA D050256 Antimitotic Agents
MeSH PA D018501 Antirheumatic Agents
MeSH PA D006074 Gout Suppressants
MeSH PA D050257 Tubulin Modulators
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
CHEBI has role CHEBI:25435 mutagens
CHEBI has role CHEBI:35845 gout suppressants
CHEBI has role CHEBI:67079 antiinflammatory agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Familial Mediterranean fever indication 12579009 DOID:2987
Chronic gouty arthritis indication 68451005
Gout indication 90560007 DOID:13189
Gout Prevention indication
Peptic ulcer contraindication 13200003 DOID:750
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Diarrhea contraindication 62315008
Leukopenia contraindication 84828003 DOID:615
Anemia due to enzyme deficiency contraindication 111577008
Disorder of muscle contraindication 129565002 DOID:423
Disease of blood AND/OR blood-forming organ contraindication 191124002 DOID:74
Impaired renal function disorder contraindication 197663003
Rhabdomyolysis contraindication 240131006
Renal dialysis contraindication 265764009
Uric acid renal calculus contraindication 274401005
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Aplastic anemia contraindication 306058006 DOID:12449
Bone marrow depression contraindication 307762000
Granulocytopenic disorder contraindication 417672002
Vomiting contraindication 422400008
Uric Acid Nephropathy Gout contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.19 acidic

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
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
Glycine receptor subunit alpha-2 Ion channel IC50 4.19 WOMBAT-PK
Tubulin beta-4B chain Structural Ki 5.24 WOMBAT-PK
Glycine receptor subunit alpha-1 Ion channel IC50 3.49 WOMBAT-PK
Multidrug resistance protein 1 Transporter Kd 3.80 WOMBAT-PK
Cytochrome P450 3A4 Enzyme Ki 4.19 WOMBAT-PK
Tubulin beta chain Structural INHIBITOR Ki 5.24 WOMBAT-PK
Tubulin Structural Ki 5.24 CHEMBL
Tubulin alpha-1A chain Structural Ki 5.60 CHEMBL
Tubulin beta-2B chain Structural Ki 6.11 CHEMBL
Tubulin Structural IC50 6.10 CHEMBL
Tubulin polymerization-promoting protein Unclassified EC50 6.12 CHEMBL

External reference:

IDSource
4020930 VUID
N0000148412 NUI
D00570 KEGG_DRUG
4017416 VANDF
4020930 VANDF
C0009262 UMLSCUI
CHEBI:27882 CHEBI
LOC PDB_CHEM_ID
CHEMBL107 ChEMBL_ID
DB01394 DRUGBANK_ID
D003078 MESH_DESCRIPTOR_UI
6167 PUBCHEM_CID
2367 IUPHAR_LIGAND_ID
SML2Y3J35T UNII
2683 RXNORM
4493 MMSL
581 MMSL
d00150 MMSL
002372 NDDF
387413002 SNOMEDCT_US
73133000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0143-3018 CAPSULE 0.60 mg ORAL NDA 27 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0254-2008 TABLET, FILM COATED 0.60 mg ORAL NDA AUTHORIZED GENERIC 32 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0378-1086 TABLET, FILM COATED 0.60 mg ORAL ANDA 28 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0591-2562 TABLET, FILM COATED 0.60 mg ORAL ANDA 27 sections
Probenecid and Colchicine HUMAN PRESCRIPTION DRUG LABEL 2 0591-5325 TABLET 0.50 mg ORAL ANDA 13 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0904-6732 CAPSULE 0.60 mg ORAL NDA 27 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 0904-7120 TABLET, FILM COATED 0.60 mg ORAL ANDA 27 sections
Colcrys HUMAN PRESCRIPTION DRUG LABEL 1 13310-119 TABLET, FILM COATED 0.60 mg ORAL NDA 29 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 42292-054 TABLET, FILM COATED 0.60 mg ORAL ANDA 27 sections
Colcrys HUMAN PRESCRIPTION DRUG LABEL 1 43353-854 TABLET, FILM COATED 0.60 mg ORAL NDA 28 sections
colchicine HUMAN PRESCRIPTION DRUG LABEL 1 43598-372 TABLET 0.60 mg ORAL ANDA 28 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 50090-3465 CAPSULE 0.60 mg ORAL NDA 27 sections
Probenecid and Colchicine Human Prescription Drug Label 2 50742-263 TABLET 0.50 mg ORAL ANDA 13 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 51407-082 TABLET, FILM COATED 0.60 mg ORAL ANDA 27 sections
Colcrys HUMAN PRESCRIPTION DRUG LABEL 1 54868-6256 TABLET, FILM COATED 0.60 mg ORAL NDA 29 sections
MITIGARE HUMAN PRESCRIPTION DRUG LABEL 1 59467-318 CAPSULE 0.60 mg ORAL NDA 28 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 60687-358 CAPSULE 0.60 mg ORAL NDA 27 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 60687-389 TABLET, FILM COATED 0.60 mg ORAL NDA authorized generic 28 sections
Colcrys HUMAN PRESCRIPTION DRUG LABEL 1 63187-292 TABLET, FILM COATED 0.60 mg ORAL NDA 29 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 63629-2166 TABLET, FILM COATED 0.60 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 63629-2167 TABLET, FILM COATED 0.60 mg ORAL NDA AUTHORIZED GENERIC 31 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 63629-7422 CAPSULE 0.60 mg ORAL NDA 27 sections
colchicine HUMAN PRESCRIPTION DRUG LABEL 1 63629-8362 TABLET 0.60 mg ORAL ANDA 26 sections
Colcrys HUMAN PRESCRIPTION DRUG LABEL 1 64764-119 TABLET, FILM COATED 0.60 mg ORAL NDA 30 sections
Probenecid and Colchicine Human Prescription Drug Label 2 64980-149 TABLET 0.50 mg ORAL ANDA 13 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 65162-710 TABLET 0.60 mg ORAL ANDA 19 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 67296-1708 TABLET, FILM COATED 0.60 mg ORAL NDA authorized generic 28 sections
colchicine Human Prescription Drug Label 1 67877-589 TABLET 0.60 mg ORAL ANDA 26 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 70010-002 TABLET, FILM COATED 0.60 mg ORAL ANDA 27 sections
Colchicine HUMAN PRESCRIPTION DRUG LABEL 1 71205-310 TABLET, FILM COATED 0.60 mg ORAL NDA authorized generic 28 sections