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

Stem definitionDrug idCAS RN
463 58-08-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • anhydrous caffeine
  • peyona
  • caffeine
  • 1,3,7-trimethyl-2,6-dioxopurine
  • 7-methyltheophylline
  • cafalgine
  • cafeina
  • durvitan
  • guaranine
  • thein
  • caffeine citrate
  • caffeine, citrated
  • nymusa
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.
  • Molecular weight: 194.19
  • Formula: C8H10N4O2
  • CLOGP: -0.04
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 58.44
  • ALOGS: -1.25
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O
0.40 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 21.50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 51.77 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 98 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.63 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.64 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 26, 1948 FDA NOVARTIS

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
Completed suicide 2541.84 9.41 3482 244269 142438 46295873
Toxicity to various agents 1987.59 9.41 3816 243935 207950 46230361
Infusion related reaction 628.75 9.41 1547 246204 99661 46338650
Overdose 526.89 9.41 1455 246296 100524 46337787
Acute hepatic failure 380.04 9.41 429 247322 14292 46424019
Metabolic acidosis 373.08 9.41 708 247043 38072 46400239
Intentional product misuse 370.49 9.41 791 246960 46337 46391974
Blood pressure fluctuation 309.22 9.41 569 247182 29879 46408432
Hepatotoxicity 275.20 9.41 484 247267 24525 46413786
Sinusitis 259.86 9.41 1367 246384 128401 46309910
Exposure to toxic agent 241.23 9.41 144 247607 1870 46436441
Anion gap 236.35 9.41 115 247636 958 46437353
Product dose omission issue 200.09 9.41 368 247383 168152 46270159
Intentional overdose 162.09 9.41 729 247022 64215 46374096
Respiratory arrest 152.62 9.41 460 247291 33356 46404955
Coagulopathy 144.72 9.41 310 247441 18189 46420122
Depressed level of consciousness 144.45 9.41 567 247184 47002 46391309
Cardio-respiratory arrest 144.16 9.41 665 247086 59204 46379107
Psoriasis 135.74 9.41 130 247621 78474 46359837
Injection site pain 132.50 9.41 228 247523 106924 46331387
Diarrhoea 119.56 9.41 2172 245579 557430 45880881
Poisoning 115.85 9.41 240 247511 13754 46424557
Oxygen saturation decreased 109.03 9.41 684 247067 68480 46369831
Hepatic failure 107.74 9.41 406 247345 33010 46405301
Device expulsion 101.74 9.41 13 247738 27529 46410782
Heart rate decreased 101.10 9.41 384 247367 31339 46406972
Respiratory depression 100.82 9.41 203 247548 11397 46426914
Acute lung injury 100.53 9.41 70 247681 1201 46437110
Ergot poisoning 97.49 9.41 39 247712 190 46438121
Blood pressure increased 97.15 9.41 1064 246687 125602 46312709
Medication error 96.72 9.41 372 247379 30539 46407772
Blood pressure diastolic abnormal 92.62 9.41 139 247612 6155 46432156
Hepatic necrosis 87.18 9.41 127 247624 5474 46432837
Intentional product use issue 85.69 9.41 526 247225 52254 46386057
Pyroglutamate increased 82.71 9.41 42 247709 387 46437924
Body temperature increased 82.59 9.41 305 247446 24556 46413755
Drug ineffective 82.40 9.41 2860 244891 674978 45763333
Coma 82.17 9.41 561 247190 57788 46380523
Infusion site pain 80.93 9.41 171 247580 9936 46428375
Analgesic drug level increased 77.60 9.41 64 247687 1430 46436881
Suspected suicide 75.93 9.41 108 247643 4553 46433758
Heart rate increased 72.18 9.41 659 247092 74132 46364179
Blood pressure systolic abnormal 71.63 9.41 115 247636 5402 46432909
Disease progression 70.53 9.41 248 247503 91052 46347259
Infusion site swelling 70.20 9.41 116 247635 5583 46432728
Injection site erythema 68.99 9.41 186 247565 74241 46364070
Blood pressure diastolic decreased 68.57 9.41 198 247553 14013 46424298
Nasopharyngitis 68.41 9.41 1173 246578 152825 46285486
Exposure via ingestion 68.13 9.41 88 247663 3379 46434932
Blood pressure systolic increased 67.23 9.41 317 247434 28470 46409841
Injection site reaction 66.56 9.41 94 247657 47755 46390556
Dyspnoea 66.05 9.41 2160 245591 513388 45924923
Throat irritation 65.13 9.41 315 247436 28586 46409725
Suicide attempt 64.79 9.41 507 247244 54529 46383782
Cardiac failure congestive 64.51 9.41 259 247492 91491 46346820
Drug abuse 64.41 9.41 565 247186 62843 46375468
Liver injury 64.19 9.41 209 247542 15792 46422519
Hypotension 59.57 9.41 1636 246115 230953 46207358
Injection site pruritus 59.44 9.41 74 247677 39669 46398642
Infusion site erythema 58.55 9.41 127 247624 7515 46430796
Cardiac arrest 58.45 9.41 735 247016 89664 46348647
Joint swelling 57.63 9.41 1218 246533 164855 46273456
Hospitalisation 57.55 9.41 160 247591 63225 46375086
Accidental overdose 55.96 9.41 233 247518 19833 46418478
Hepatic enzyme increased 55.91 9.41 672 247079 81115 46357196
Migraine 54.45 9.41 590 247161 69436 46368875
Wrong technique in product usage process 54.29 9.41 131 247620 54291 46384020
No adverse event 54.12 9.41 61 247690 34170 46404141
Osteonecrosis of jaw 53.64 9.41 62 247689 34340 46403971
Alopecia 52.31 9.41 580 247171 161834 46276477
Muscle injury 52.00 9.41 93 247658 4773 46433538
Drug resistance 51.80 9.41 14 247737 17354 46420957
Sedation complication 51.51 9.41 79 247672 3566 46434745
International normalised ratio increased 51.43 9.41 425 247326 46458 46391853
Mucosal inflammation 50.88 9.41 80 247671 38896 46399415
Myocardial infarction 50.31 9.41 307 247444 97221 46341090
Anaemia 50.25 9.41 1006 246745 254773 46183538
Psoriatic arthropathy 50.07 9.41 72 247679 36307 46402004
Anion gap abnormal 50.05 9.41 28 247723 319 46437992
Headache 49.29 9.41 3052 244699 475300 45963011
Ear pain 49.21 9.41 240 247511 21852 46416459
Substance abuse 48.90 9.41 83 247668 4084 46434227
Alanine aminotransferase increased 48.85 9.41 699 247052 87752 46350559
Soft tissue disorder 48.63 9.41 83 247668 4103 46434208
Heart rate irregular 48.09 9.41 211 247540 18380 46419931
Product quality issue 47.65 9.41 72 247679 35576 46402735
Crystal urine present 47.52 9.41 45 247706 1214 46437097
Folliculitis 47.42 9.41 103 247648 6100 46432211
Electric shock 47.41 9.41 39 247712 868 46437443
Death 46.68 9.41 2202 245549 333346 46104965
Drug hypersensitivity 46.10 9.41 965 246786 242860 46195451
Neutropenia 45.87 9.41 512 247239 142692 46295619
Infusion site extravasation 45.70 9.41 92 247659 5164 46433147
Infusion site pruritus 44.33 9.41 68 247683 3070 46435241
Neonatal hypoxia 43.98 9.41 29 247722 453 46437858
Therapy cessation 43.70 9.41 46 247705 26583 46411728
Sopor 42.89 9.41 26 247725 19802 46418509
Neuropathy peripheral 42.37 9.41 295 247456 90598 46347713
White blood cells urine positive 40.82 9.41 76 247675 4024 46434287
Duodenal ulcer perforation 39.62 9.41 117 247634 8385 46429926
Cardiac failure 39.50 9.41 255 247496 79693 46358618
Injection site bruising 39.46 9.41 81 247670 35555 46402756
Administration site swelling 39.02 9.41 39 247712 1126 46437185
Palmar-plantar erythrodysaesthesia syndrome 38.70 9.41 31 247720 20420 46417891
Anti-cyclic citrullinated peptide antibody positive 38.44 9.41 202 247549 18943 46419368
Aspartate aminotransferase increased 38.05 9.41 608 247143 78092 46360219
Injection site swelling 37.95 9.41 100 247651 40227 46398084
Ill-defined disorder 37.20 9.41 257 247494 26570 46411741
Urinary sediment present 37.03 9.41 47 247704 1773 46436538
Creatinine renal clearance decreased 36.91 9.41 100 247651 6820 46431491
Muscle spasticity 36.87 9.41 139 247612 11301 46427010
Decreased appetite 36.66 9.41 767 246984 193069 46245242
Product use in unapproved indication 36.41 9.41 305 247446 89968 46348343
Interstitial lung disease 36.22 9.41 155 247596 53794 46384517
Off label use 35.46 9.41 1651 246100 378190 46060121
Body temperature fluctuation 35.26 9.41 46 247705 1784 46436527
Administration site pain 35.16 9.41 29 247722 648 46437663
Product substitution issue 34.98 9.41 18 247733 15013 46423298
Bone marrow failure 34.96 9.41 65 247686 29604 46408707
Lower respiratory tract infection 34.78 9.41 446 247305 54643 46383668
Body temperature decreased 34.54 9.41 152 247599 13257 46425054
Respiratory rate increased 34.46 9.41 136 247615 11297 46427014
Injection site warmth 34.34 9.41 15 247736 13757 46424554
Helicobacter infection 34.09 9.41 138 247613 11598 46426713
Acidosis 33.74 9.41 133 247618 11041 46427270
Lymphocyte count decreased 33.64 9.41 242 247509 25347 46412964
Hypothermia 33.61 9.41 141 247610 12042 46426269
Malignant neoplasm progression 33.15 9.41 205 247546 64721 46373590
Infusion site nodule 32.78 9.41 33 247718 961 46437350
Blood pressure diastolic increased 32.54 9.41 87 247664 5887 46432424
Jaundice cholestatic 31.28 9.41 77 247674 4952 46433359
Maternal exposure during pregnancy 31.13 9.41 371 247380 102178 46336133
Urine abnormality 31.01 9.41 82 247669 5512 46432799
Cerebrovascular accident 30.87 9.41 365 247386 100674 46337637
Red blood cells urine positive 30.69 9.41 52 247699 2555 46435756
Infusion site bruising 30.41 9.41 39 247712 1487 46436824
Product prescribing error 30.32 9.41 37 247714 20010 46418301
Brain death 30.22 9.41 54 247697 2769 46435542
Cognitive disorder 30.17 9.41 314 247437 36569 46401742
Surgery 28.93 9.41 69 247682 28716 46409595
Posterior reversible encephalopathy syndrome 28.59 9.41 23 247728 15118 46423193
Liver transplant 28.17 9.41 48 247703 2369 46435942
Therapy interrupted 28.12 9.41 11 247740 10780 46427531
Brain oedema 28.11 9.41 136 247615 12342 46425969
Prothrombin time prolonged 28.00 9.41 113 247638 9483 46428828
Drug screen positive 27.93 9.41 63 247688 3828 46434483
Haemolysis 27.87 9.41 83 247668 5976 46432335
Paraesthesia 27.72 9.41 447 247304 116990 46321321
Red cell distribution width increased 27.70 9.41 97 247654 7607 46430704
Ear pruritus 27.26 9.41 44 247707 2076 46436235
Blood calcium decreased 27.21 9.41 159 247592 15514 46422797
Neutrophil percentage increased 26.99 9.41 50 247701 2637 46435674
Lymphocyte percentage decreased 26.83 9.41 50 247701 2649 46435662
Intervertebral discitis 26.46 9.41 48 247703 2491 46435820
Anion gap increased 26.46 9.41 36 247715 1455 46436856
Analgesic drug level above therapeutic 26.29 9.41 15 247736 178 46438133
Product storage error 26.16 9.41 15 247736 11777 46426534
Dyspnoea exertional 26.08 9.41 158 247593 50131 46388180
Hypomania 26.05 9.41 66 247685 4322 46433989
Somnolence 25.88 9.41 1046 246705 155475 46282836
Hypertensive crisis 25.31 9.41 21 247730 13594 46424717
Blood pH decreased 25.29 9.41 48 247703 2579 46435732
Pericarditis 25.22 9.41 215 247536 23712 46414599
Injection site rash 25.19 9.41 28 247723 15785 46422526
Irritable bowel syndrome 25.18 9.41 162 247589 16353 46421958
Foetal exposure during pregnancy 24.76 9.41 82 247669 30665 46407646
Red blood cell sedimentation rate abnormal 24.22 9.41 22 247729 13627 46424684
Ventricular arrhythmia 24.12 9.41 55 247696 3366 46434945
Pain 24.06 9.41 2886 244865 474062 45964249
Bradypnoea 23.85 9.41 51 247700 2988 46435323
Medication overuse headache 23.69 9.41 20 247731 462 46437849
Poor venous access 23.58 9.41 97 247654 8211 46430100
Unevaluable event 23.46 9.41 146 247605 46029 46392282
Cholecystitis chronic 23.34 9.41 114 247637 10385 46427926
Sleep disorder due to general medical condition, insomnia type 23.29 9.41 71 247680 5178 46433133
Unresponsive to stimuli 23.14 9.41 267 247484 31907 46406404
Neoplasm progression 23.01 9.41 69 247682 26614 46411697
Encephalopathy 22.94 9.41 276 247475 33313 46404998
Ductus arteriosus premature closure 22.94 9.41 17 247734 323 46437988
Precancerous cells present 22.73 9.41 30 247721 1177 46437134
Myelodysplastic syndrome 22.72 9.41 30 247721 15681 46422630
Pancytopenia 22.39 9.41 317 247434 84741 46353570
Administration site erythema 22.22 9.41 21 247730 565 46437746
Electrocardiogram QRS complex abnormal 21.32 9.41 14 247737 217 46438094
Oedema peripheral 21.31 9.41 665 247086 159041 46279270
Asthma 21.08 9.41 350 247401 91192 46347119
Hand deformity 21.01 9.41 278 247473 34296 46404015
Bone erosion 20.96 9.41 12 247739 9431 46428880
Bacterial test 20.54 9.41 29 247722 1214 46437097
Injection site mass 20.46 9.41 30 247721 15010 46423301
Urine leukocyte esterase positive 20.42 9.41 43 247708 2492 46435819
Epistaxis 20.14 9.41 231 247520 64074 46374237
Hyponatraemia 20.01 9.41 398 247353 100934 46337377
Pyroglutamic acidosis 19.97 9.41 14 247737 243 46438068
Plasma cell myeloma 19.92 9.41 146 247605 44332 46393979
Hyperkalaemia 19.69 9.41 173 247578 50536 46387775
Dysgeusia 19.56 9.41 130 247621 40361 46397950
Drug interaction 19.45 9.41 880 246871 202214 46236097
Muscle spasms 19.37 9.41 501 247250 122612 46315699
Diabetes mellitus 19.35 9.41 171 247580 49894 46388417
Injection site urticaria 19.27 9.41 21 247730 11946 46426365
Pneumocystis jirovecii pneumonia 19.24 9.41 32 247719 15216 46423095
Night sweats 19.09 9.41 225 247526 27025 46411286
Renal impairment 18.93 9.41 279 247472 74093 46364218
Specific gravity urine decreased 18.92 9.41 17 247734 428 46437883
Osmolar gap 18.91 9.41 10 247741 101 46438210
Therapeutic product effect decreased 18.61 9.41 572 247179 82029 46356282
Fracture 18.61 9.41 37 247714 16434 46421877
Blood creatine increased 18.45 9.41 60 247691 4530 46433781
Blood urine present 18.43 9.41 120 247631 12162 46426149
Weight increased 18.07 9.41 1056 246695 163417 46274894
Coronary artery disease 18.05 9.41 105 247646 33647 46404664
Neurotoxicity 18.05 9.41 28 247723 13689 46424622
Dizziness 17.76 9.41 1560 246191 338854 46099457
Coma hepatic 17.71 9.41 19 247732 597 46437714
Drug abuser 17.52 9.41 47 247704 3186 46435125
Toxicologic test abnormal 17.41 9.41 20 247731 679 46437632
PCO2 decreased 17.24 9.41 27 247724 1241 46437070
Smear cervix abnormal 17.24 9.41 40 247711 2476 46435835
Ejection fraction decreased 17.24 9.41 44 247707 17893 46420418
Pneumonia viral 16.99 9.41 75 247676 6549 46431762
Device dislocation 16.97 9.41 59 247692 21743 46416568
Blood bilirubin increased 16.85 9.41 265 247486 33919 46404392
Drug-induced liver injury 16.69 9.41 207 247544 25161 46413150
Cystitis 16.69 9.41 316 247435 41925 46396386
Band neutrophil count increased 16.42 9.41 14 247737 328 46437983
Infusion site urticaria 16.38 9.41 20 247731 725 46437586
Anaphylactic shock 16.37 9.41 54 247697 20220 46418091
Tachycardia 16.27 9.41 665 247086 98957 46339354
Pneumonia 16.21 9.41 1749 246002 374571 46063740
Pathogen resistance 16.09 9.41 6 247745 6054 46432257
Polyneuropathy 16.06 9.41 23 247728 11621 46426690
Osteonecrosis 16.05 9.41 76 247675 25668 46412643
Traumatic liver injury 16.05 9.41 13 247738 283 46438028
Intentional self-injury 15.87 9.41 70 247681 24096 46414215
Therapeutic response shortened 15.79 9.41 62 247689 5137 46433174
Disease recurrence 15.76 9.41 48 247703 18423 46419888
Antidepressant drug level above therapeutic 15.63 9.41 14 247737 351 46437960
Renal papillary necrosis 15.54 9.41 12 247739 243 46438068
Feeling abnormal 15.42 9.41 526 247225 124534 46313777
Adverse event 15.41 9.41 112 247639 34072 46404239
Infusion site haemorrhage 15.38 9.41 35 247716 2139 46436172
Transplant rejection 15.28 9.41 17 247734 9579 46428732
Administration site pruritus 15.27 9.41 13 247738 304 46438007
Hypokalaemia 15.27 9.41 353 247398 87671 46350640
Second primary malignancy 15.15 9.41 8 247743 6576 46431735
Synovitis 15.13 9.41 428 247323 60647 46377664
Drug use disorder 15.07 9.41 40 247711 2695 46435616
Device issue 14.93 9.41 55 247696 19925 46418386
Femur fracture 14.91 9.41 125 247626 36872 46401439
Memory impairment 14.89 9.41 305 247446 77032 46361279
Cytomegalovirus infection 14.88 9.41 48 247703 18096 46420215
Mean cell haemoglobin concentration increased 14.87 9.41 15 247736 438 46437873
Lactic acidosis 14.85 9.41 112 247639 33797 46404514
Haemoglobin urine present 14.84 9.41 18 247733 648 46437663
Abortion spontaneous 14.78 9.41 154 247597 43492 46394819
Inflammation 14.75 9.41 351 247400 48430 46389881
Post-traumatic stress disorder 14.58 9.41 51 247700 3997 46434314
Vitamin K deficiency 14.57 9.41 15 247736 449 46437862
Ageusia 14.54 9.41 24 247727 11448 46426863
Self-medication 14.52 9.41 34 247717 2118 46436193
Underdose 14.51 9.41 54 247697 19504 46418807
Angioedema 14.50 9.41 136 247615 39206 46399105
Haematocrit decreased 14.45 9.41 264 247487 34793 46403518
Transaminases increased 14.37 9.41 217 247534 27544 46410767
Respiratory disorder 14.37 9.41 214 247537 27086 46411225
Therapeutic product effect incomplete 14.24 9.41 311 247440 77842 46360469
Injection site haemorrhage 14.20 9.41 59 247692 20650 46417661
Dry skin 14.18 9.41 144 247607 40872 46397439
Chills 14.11 9.41 634 247117 95398 46342913
Blood parathyroid hormone decreased 14.11 9.41 3 247748 4378 46433933
Breast cancer 14.06 9.41 164 247587 45354 46392957
Activated partial thromboplastin time prolonged 14.04 9.41 73 247678 6816 46431495
Administration site extravasation 13.99 9.41 17 247734 613 46437698
Ear infection 13.97 9.41 185 247566 22828 46415483
Transfusion-related acute lung injury 13.94 9.41 8 247743 96 46438215
Wound 13.88 9.41 311 247440 42491 46395820
Gastrointestinal toxicity 13.88 9.41 3 247748 4328 46433983
Myelocyte count increased 13.87 9.41 13 247738 346 46437965
White blood cell count decreased 13.84 9.41 472 247279 111759 46326552
Derailment 13.83 9.41 7 247744 64 46438247
Oral discomfort 13.77 9.41 13 247738 7905 46430406
Haematotoxicity 13.77 9.41 10 247741 6923 46431388
Diabetic ketoacidosis 13.69 9.41 50 247701 18160 46420151
Orthostatic hypotension 13.65 9.41 195 247556 24463 46413848
Musculoskeletal disorder 13.54 9.41 40 247711 15505 46422806
Transplant dysfunction 13.54 9.41 4 247747 4678 46433633
Device use error 13.54 9.41 5 247746 5076 46433235
Accidental death 13.49 9.41 30 247721 1805 46436506
Cholelithiasis 13.48 9.41 284 247467 38397 46399914
Asphyxia 13.43 9.41 60 247691 5266 46433045
Blood creatinine decreased 13.41 9.41 55 247696 4649 46433662
Infective pulmonary exacerbation of cystic fibrosis 13.34 9.41 23 247728 10784 46427527
Culture urine positive 13.34 9.41 44 247707 3347 46434964
Arthralgia 13.28 9.41 2165 245586 362438 46075873
Duodenal stenosis 13.19 9.41 16 247735 576 46437735
Flushing 13.13 9.41 442 247309 64172 46374139
Magnesium deficiency 13.10 9.41 14 247737 438 46437873
Cells in urine 13.05 9.41 9 247742 152 46438159
Procedural anxiety 13.02 9.41 15 247736 511 46437800
Blood count abnormal 12.85 9.41 50 247701 17828 46420483
Nail bed inflammation 12.79 9.41 13 247738 383 46437928
Parkinsonism 12.74 9.41 14 247737 7934 46430377
Sinus tachycardia 12.71 9.41 173 247578 21476 46416835
Anticholinergic syndrome 12.69 9.41 29 247722 1777 46436534
Pulmonary arterial hypertension 12.65 9.41 83 247668 25845 46412466
Joint stiffness 12.61 9.41 88 247663 27020 46411291
Epilepsy 12.61 9.41 74 247677 23664 46414647
Renal failure 12.59 9.41 484 247267 113110 46325201
Congestive hepatopathy 12.59 9.41 35 247716 2423 46435888
Autonomic dysreflexia 12.57 9.41 10 247741 212 46438099
Device related thrombosis 12.54 9.41 23 247728 1204 46437107
Drug dependence 12.50 9.41 161 247590 19740 46418571
Full blood count decreased 12.47 9.41 68 247683 22143 46416168
Diaphragmatic rupture 12.41 9.41 10 247741 216 46438095
Labelled drug-drug interaction medication error 12.40 9.41 18 247733 9043 46429268
Gestational diabetes 12.38 9.41 12 247739 7207 46431104
Genital haemorrhage 12.36 9.41 10 247741 6556 46431755
Sepsis 12.28 9.41 593 247158 135421 46302890
Febrile bone marrow aplasia 12.25 9.41 11 247740 6851 46431460
Oesophageal mucosal dissection 12.24 9.41 5 247746 26 46438285
Administration site reaction 12.22 9.41 10 247741 221 46438090
Gastrooesophageal reflux disease 12.10 9.41 301 247450 74043 46364268
Urinary casts 12.05 9.41 14 247737 481 46437830
Monocyte count increased 11.99 9.41 56 247695 5008 46433303
Renal failure neonatal 11.97 9.41 8 247743 128 46438183
Device malfunction 11.95 9.41 34 247717 13340 46424971
Urine analysis abnormal 11.95 9.41 49 247702 4141 46434170
Immunodeficiency 11.89 9.41 114 247637 12992 46425319
Gallbladder injury 11.88 9.41 24 247727 1350 46436961
Mean cell haemoglobin concentration decreased 11.88 9.41 35 247716 2505 46435806
Treatment failure 11.83 9.41 390 247361 92697 46345614
Sedation 11.83 9.41 179 247572 22731 46415580
Adverse drug reaction 11.78 9.41 165 247586 44197 46394114
Infusion site discomfort 11.72 9.41 16 247735 649 46437662
Immune reconstitution inflammatory syndrome 11.71 9.41 8 247743 5717 46432594
Cardiovascular disorder 11.63 9.41 30 247721 12157 46426154
Hepatic encephalopathy 11.63 9.41 93 247658 10064 46428247
Atypical femur fracture 11.60 9.41 6 247745 4991 46433320
Postmortem blood drug level increased 11.54 9.41 13 247738 432 46437879
Syncope 11.52 9.41 447 247304 104356 46333955
Upper respiratory tract infection 11.49 9.41 429 247322 63127 46375184
Galactorrhoea 11.44 9.41 3 247748 3794 46434517
Hyperlipidaemia 11.40 9.41 55 247696 18484 46419827
Hypomagnesaemia 11.40 9.41 70 247681 22140 46416171
Gastric infection 11.40 9.41 37 247714 2791 46435520
Angina unstable 11.34 9.41 14 247737 7534 46430777
Ataxia 11.32 9.41 37 247714 13893 46424418
Hepatic cirrhosis 11.31 9.41 44 247707 15688 46422623
Renal disorder 11.28 9.41 89 247662 26597 46411714
Diffuse large B-cell lymphoma 11.23 9.41 9 247742 5929 46432382
Urine oxalate increased 11.22 9.41 9 247742 193 46438118
Rash pruritic 11.20 9.41 166 247585 44049 46394262
Visual acuity reduced 11.19 9.41 70 247681 22043 46416268
Injection site induration 11.10 9.41 16 247735 8063 46430248
Systemic inflammatory response syndrome 11.01 9.41 57 247694 5314 46432997
Cystic fibrosis 10.95 9.41 3 247748 3685 46434626
Malaise 10.94 9.41 1566 246185 329666 46108645
Band neutrophil percentage increased 10.92 9.41 9 247742 201 46438110
Anoxia 10.89 9.41 10 247741 259 46438052
Treatment noncompliance 10.86 9.41 103 247648 29628 46408683
Vein collapse 10.81 9.41 14 247737 539 46437772
Osmolar gap abnormal 10.78 9.41 5 247746 37 46438274
Blood methaemoglobin present 10.75 9.41 6 247745 68 46438243
Opiates positive 10.71 9.41 10 247741 265 46438046
Administration site bruise 10.71 9.41 10 247741 265 46438046
Acute graft versus host disease 10.68 9.41 4 247747 4026 46434285
Obstructive airways disorder 10.64 9.41 36 247715 13376 46424935
Lupus vulgaris 10.62 9.41 4 247747 16 46438295
Rheumatoid factor positive 10.62 9.41 160 247591 20301 46418010
General physical health deterioration 10.59 9.41 504 247247 115265 46323046
Extrapyramidal disorder 10.55 9.41 28 247723 11240 46427071
Spinal cord abscess 10.53 9.41 8 247743 158 46438153
Metastases to liver 10.43 9.41 61 247690 19524 46418787
Gait inability 10.43 9.41 128 247623 35075 46403236
Pericardial effusion 10.43 9.41 86 247665 25457 46412854
Infusion site mass 10.40 9.41 18 247733 900 46437411
Peripheral swelling 10.38 9.41 974 246777 157097 46281214
Haemorrhage 10.38 9.41 217 247534 54652 46383659
Septic shock 10.36 9.41 231 247520 57662 46380649
Nightmare 10.35 9.41 49 247702 16549 46421762
Head banging 10.34 9.41 12 247739 412 46437899
Transient ischaemic attack 10.30 9.41 127 247624 34776 46403535
Myelocyte percentage increased 10.28 9.41 8 247743 164 46438147
Acute myocardial infarction 10.26 9.41 114 247637 31810 46406501
Bursitis 10.23 9.41 155 247596 19687 46418624
Glycosylated haemoglobin increased 10.21 9.41 27 247724 10849 46427462
Temperature regulation disorder 10.15 9.41 40 247711 3320 46434991
Infusion site irritation 10.13 9.41 13 247738 496 46437815
Hypocalcaemia 10.12 9.41 92 247659 26693 46411618
Mood swings 10.12 9.41 48 247703 16204 46422107
Nose deformity 10.11 9.41 7 247744 119 46438192
Metastases to bone 10.09 9.41 53 247698 17423 46420888
Haemophagocytic lymphohistiocytosis 10.07 9.41 18 247733 8324 46429987
Amenorrhoea 10.03 9.41 20 247731 8875 46429436
Lower limb fracture 10.03 9.41 33 247718 12365 46425946
Oedema 10.00 9.41 275 247476 66796 46371515
Pharyngitis streptococcal 9.95 9.41 78 247673 8390 46429921
C-reactive protein abnormal 9.92 9.41 69 247682 21201 46417110
Bone pain 9.92 9.41 182 247569 46708 46391603
Device difficult to use 9.91 9.41 17 247734 7987 46430324
Akathisia 9.91 9.41 16 247735 7698 46430613
Hypersensitivity vasculitis 9.90 9.41 5 247746 4216 46434095
Hallucination, auditory 9.87 9.41 27 247724 10729 46427582
Pulmonary mass 9.84 9.41 55 247696 17802 46420509
Invasive ductal breast carcinoma 9.74 9.41 11 247740 6157 46432154
Atrial fibrillation 9.67 9.41 450 247301 103140 46335171
Eye infection 9.63 9.41 82 247669 9041 46429270
Pregnancy with contraceptive device 9.61 9.41 6 247745 4497 46433814
Administration site nodule 9.58 9.41 5 247746 49 46438262
Electrolyte imbalance 9.53 9.41 53 247698 17173 46421138
Abdominal discomfort 9.52 9.41 682 247069 150483 46287828
Carnitine deficiency 9.44 9.41 7 247744 133 46438178
Blood chloride increased 9.44 9.41 33 247718 2586 46435725

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 1118.14 9.98 1666 118706 97826 29734280
Toxicity to various agents 973.57 9.98 2174 118198 175009 29657097
Infusion related reaction 374.81 9.98 622 119750 39942 29792164
Overdose 345.07 9.98 926 119446 83411 29748695
Blood pressure fluctuation 261.63 9.98 337 120035 17166 29814940
Intentional product misuse 225.62 9.98 457 119915 34210 29797896
Acute hepatic failure 206.11 9.98 246 120126 11581 29820525
Intentional overdose 180.11 9.98 466 119906 41015 29791091
Drug ineffective 149.52 9.98 783 119589 339604 29492502
Exposure to toxic agent 131.83 9.98 72 120300 1053 29831053
Product dose omission issue 103.12 9.98 130 120242 91501 29740605
Neonatal hypoxia 98.17 9.98 37 120335 208 29831898
Hepatotoxicity 98.17 9.98 222 120150 17923 29814183
Coagulopathy 96.49 9.98 223 120149 18264 29813842
Anion gap 94.63 9.98 48 120324 598 29831508
Cardio-respiratory arrest 89.46 9.98 461 119911 56845 29775261
Heart rate decreased 84.12 9.98 229 120143 20765 29811341
Respiratory arrest 83.26 9.98 283 120089 28975 29803131
Oxygen saturation decreased 81.16 9.98 368 120004 43072 29789034
Metabolic acidosis 80.46 9.98 331 120041 37130 29794976
Blood pressure increased 75.21 9.98 521 119851 71407 29760699
Myocardial infarction 73.91 9.98 258 120114 125367 29706739
Diarrhoea 73.36 9.98 926 119446 333177 29498929
Accidental overdose 70.89 9.98 197 120175 18078 29814028
Hepatic necrosis 66.71 9.98 80 120292 3783 29828323
Substance abuse 63.65 9.98 107 120265 6933 29825173
Psoriasis 61.95 9.98 48 120324 42458 29789648
Cardiac failure congestive 60.63 9.98 158 120214 84249 29747857
Alanine aminotransferase increased 56.07 9.98 499 119873 73777 29758329
Hypotension 54.88 9.98 1120 119252 199445 29632661
Sinusitis 51.83 9.98 268 120104 33077 29799029
Drug resistance 50.02 9.98 10 120362 20123 29811983
Respiratory depression 48.62 9.98 128 120244 11375 29820731
Cardiac failure 46.59 9.98 175 120197 83243 29748863
Aspartate aminotransferase increased 45.27 9.98 421 119951 63001 29769105
Heart rate irregular 44.47 9.98 129 120243 12130 29819976
Product use in unapproved indication 42.86 9.98 152 120220 73541 29758565
Blood pressure diastolic increased 42.60 9.98 54 120318 2704 29829402
Treatment failure 42.41 9.98 46 120326 34633 29797473
Poisoning 41.50 9.98 120 120252 11262 29820844
Chills 41.01 9.98 458 119914 71880 29760226
Liver injury 40.74 9.98 126 120246 12274 29819832
Suicide attempt 40.22 9.98 269 120103 36428 29795678
Blood pressure diastolic abnormal 39.02 9.98 36 120336 1251 29830855
Medication error 37.18 9.98 175 120197 20797 29811309
Exposure via ingestion 37.01 9.98 49 120323 2562 29829544
Blood pressure systolic increased 36.86 9.98 139 120233 14971 29817135
Drug abuse 36.31 9.98 496 119876 81576 29750530
Cardiac arrest 35.49 9.98 547 119825 92303 29739803
Depressed level of consciousness 34.83 9.98 268 120104 37954 29794152
Analgesic drug level increased 33.96 9.98 24 120348 565 29831541
Heart rate increased 33.36 9.98 268 120104 38453 29793653
Blood pressure systolic abnormal 32.46 9.98 35 120337 1472 29830634
Coronary artery disease 32.02 9.98 98 120274 49614 29782492
Coma 31.14 9.98 273 120099 40176 29791930
Hepatic failure 30.63 9.98 238 120134 33805 29798301
Tachycardia 29.95 9.98 439 119933 73300 29758806
Contraindicated product administered 29.82 9.98 16 120356 17215 29814891
Interstitial lung disease 28.81 9.98 134 120238 60063 29772043
Suspected suicide 28.52 9.98 48 120324 3113 29828993
Infusion site extravasation 27.96 9.98 42 120330 2471 29829635
Blood pH decreased 27.91 9.98 40 120332 2255 29829851
Blood pressure diastolic decreased 27.01 9.98 70 120302 6161 29825945
Neutrophil percentage increased 26.45 9.98 35 120337 1829 29830277
Acute lung injury 26.14 9.98 27 120345 1080 29831026
Anaemia 25.96 9.98 637 119735 207355 29624751
Pyrexia 25.87 9.98 1438 118934 293051 29539055
Toxic epidermal necrolysis 25.69 9.98 141 120231 17799 29814307
International normalised ratio increased 25.57 9.98 299 120073 47440 29784666
Neuropathy peripheral 25.49 9.98 172 120200 70303 29761803
Methaemoglobinaemia 25.20 9.98 40 120332 2470 29829636
Body temperature fluctuation 24.79 9.98 28 120344 1241 29830865
Prothrombin time prolonged 24.73 9.98 88 120284 9215 29822891
Urine sodium decreased 24.49 9.98 13 120359 179 29831927
Stevens-Johnson syndrome 23.83 9.98 136 120236 17420 29814686
Body temperature decreased 23.70 9.98 89 120283 9566 29822540
Ergot poisoning 23.67 9.98 10 120362 79 29832027
Fatigue 23.44 9.98 1052 119320 319621 29512485
Unresponsive to stimuli 23.37 9.98 184 120188 26235 29805871
Product prescribing error 23.00 9.98 20 120352 16713 29815393
Oxygen saturation abnormal 22.66 9.98 25 120347 1079 29831027
Infusion site pruritus 22.58 9.98 19 120353 583 29831523
Brain death 22.54 9.98 38 120334 2468 29829638
Infusion site pain 22.28 9.98 39 120333 2611 29829495
Acidosis 22.08 9.98 91 120281 10210 29821896
Lymphocyte percentage decreased 21.99 9.98 34 120338 2052 29830054
Cerebrovascular accident 21.87 9.98 222 120150 83255 29748851
Intentional product use issue 21.68 9.98 233 120139 36207 29795899
Nasopharyngitis 21.44 9.98 344 120028 58505 29773601
Depression 21.10 9.98 247 120125 90190 29741916
Hospitalisation 20.99 9.98 99 120273 44220 29787886
Infusion site swelling 20.89 9.98 29 120343 1587 29830519
No adverse event 20.32 9.98 24 120348 17395 29814711
Asthenia 20.25 9.98 707 119665 220583 29611523
Apparent life threatening event 20.23 9.98 12 120360 207 29831899
Drug interaction 20.05 9.98 630 119742 198938 29633168
Hepatocellular carcinoma 19.67 9.98 7 120365 9603 29822503
Progressive multifocal leukoencephalopathy 19.44 9.98 6 120366 9007 29823099
Fluid retention 19.33 9.98 45 120327 24953 29807153
Mental status changes 19.31 9.98 231 120141 36848 29795258
Respiratory rate increased 19.30 9.98 79 120293 8836 29823270
Anion gap abnormal 19.21 9.98 10 120362 132 29831974
Apnoea 19.10 9.98 62 120310 6196 29825910
Migraine 18.98 9.98 102 120270 12772 29819334
Transaminases increased 18.93 9.98 160 120212 23297 29808809
Injection site pain 18.64 9.98 61 120311 30249 29801857
Renal papillary necrosis 18.51 9.98 10 120362 143 29831963
Osteonecrosis of jaw 18.34 9.98 29 120343 18589 29813517
Plasma cell myeloma 18.09 9.98 133 120239 53329 29778777
Psoriatic arthropathy 18.08 9.98 22 120350 15739 29816367
Dizziness 17.76 9.98 623 119749 194286 29637820
Bone marrow failure 17.59 9.98 61 120311 29724 29802382
Decreased appetite 17.37 9.98 464 119908 149446 29682660
Body temperature increased 17.19 9.98 110 120262 14670 29817436
Dyspnoea 17.14 9.98 1132 119240 332163 29499943
Angina pectoris 17.07 9.98 61 120311 29457 29802649
Asthma 17.02 9.98 81 120291 36093 29796013
Off label use 16.75 9.98 825 119547 248465 29583641
Blood triglycerides increased 16.69 9.98 19 120353 13998 29818108
Maternal exposure before pregnancy 16.61 9.98 13 120359 359 29831747
Administration site pain 16.54 9.98 10 120362 179 29831927
Immune reconstitution inflammatory syndrome 16.42 9.98 8 120364 9093 29823013
Therapeutic product effect incomplete 16.37 9.98 75 120297 33759 29798347
Wrong technique in product usage process 16.33 9.98 67 120305 31088 29801018
Diabetes mellitus 16.24 9.98 100 120272 41765 29790341
Corneal abscess 16.18 9.98 6 120366 32 29832074
Therapeutic response shortened 16.18 9.98 41 120331 3559 29828547
Glycosylated haemoglobin increased 16.15 9.98 9 120363 9482 29822624
Brain oedema 16.14 9.98 95 120277 12303 29819803
Granulomatosis with polyangiitis 16.12 9.98 19 120353 882 29831224
Chronic gastrointestinal bleeding 15.98 9.98 11 120361 248 29831858
Hypertension neonatal 15.86 9.98 4 120368 3 29832103
Vital functions abnormal 15.82 9.98 8 120364 99 29832007
Anion gap increased 15.80 9.98 26 120346 1655 29830451
Disease progression 15.73 9.98 226 120146 79648 29752458
Feeling abnormal 15.67 9.98 149 120223 56607 29775499
Hepatitis C 15.61 9.98 18 120354 13187 29818919
Cytokine release syndrome 15.54 9.98 80 120292 9853 29822253
Graft versus host disease 15.38 9.98 11 120361 10139 29821967
Pemphigus 15.37 9.98 22 120350 1239 29830867
Visual acuity reduced 15.31 9.98 25 120347 15821 29816285
Poor venous access 15.30 9.98 32 120340 2448 29829658
Malaise 15.12 9.98 534 119838 166428 29665678
Mucosal inflammation 15.11 9.98 67 120305 30427 29801679
Flushing 15.03 9.98 183 120189 29309 29802797
Venoocclusive liver disease 15.00 9.98 4 120368 6609 29825497
Renal impairment 14.94 9.98 243 120129 83941 29748165
Anti-erythrocyte antibody positive 14.94 9.98 6 120366 41 29832065
Ear infection 14.92 9.98 64 120308 7310 29824796
Haemolysis 14.81 9.98 63 120309 7168 29824938
Environmental exposure 14.69 9.98 11 120361 284 29831822
Pulmonary oedema 14.52 9.98 253 120119 43722 29788384
Administration site erythema 14.18 9.98 7 120365 82 29832024
Cerebral haemorrhage 14.13 9.98 76 120296 32811 29799295
Memory impairment 13.80 9.98 90 120282 37084 29795022
Malignant neoplasm progression 13.72 9.98 206 120166 72081 29760025
Blood count abnormal 13.65 9.98 16 120356 11636 29820470
Cerebral infarction 13.64 9.98 57 120315 26316 29805790
Electrocardiogram QRS complex prolonged 13.62 9.98 43 120329 4234 29827872
Lung neoplasm malignant 13.60 9.98 25 120347 15107 29816999
Haematotoxicity 13.50 9.98 4 120368 6166 29825940
Oedema peripheral 13.48 9.98 323 120049 105509 29726597
Throat tightness 13.47 9.98 61 120311 7131 29824975
Bilirubin urine present 13.08 9.98 7 120365 98 29832008
Endocardial fibrosis 13.00 9.98 5 120367 30 29832076
Myopathy 12.99 9.98 14 120358 10572 29821534
Sopor 12.97 9.98 15 120357 10976 29821130
Peritonitis bacterial 12.93 9.98 16 120356 11362 29820744
Ammonia increased 12.93 9.98 42 120330 4199 29827907
Pulmonary congestion 12.82 9.98 89 120283 12198 29819908
Crystal urine present 12.81 9.98 10 120362 275 29831831
Balance disorder 12.72 9.98 90 120282 36403 29795703
Febrile neutropenia 12.68 9.98 537 119835 106156 29725950
Blood ethanol increased 12.53 9.98 11 120361 358 29831748
Osteonecrosis 12.51 9.98 29 120343 16106 29816000
Leukopenia 12.47 9.98 155 120217 56004 29776102
Vitello-intestinal duct remnant 12.43 9.98 7 120365 109 29831997
Cardiac disorder 12.21 9.98 102 120270 39791 29792315
Acute myocardial infarction 12.18 9.98 145 120227 52794 29779312
Infusion site bruising 12.13 9.98 9 120363 229 29831877
Infusion site rash 12.13 9.98 10 120362 298 29831808
Chronic obstructive pulmonary disease 11.94 9.98 123 120249 46003 29786103
Analgesic drug level above therapeutic 11.90 9.98 9 120363 236 29831870
Labelled drug-drug interaction medication error 11.78 9.98 15 120357 10523 29821583
Hepatic haematoma 11.70 9.98 12 120360 476 29831630
Infusion site nodule 11.67 9.98 6 120366 77 29832029
Drug ineffective for unapproved indication 11.64 9.98 16 120356 10864 29821242
Hyperlipidaemia 11.61 9.98 24 120348 13883 29818223
Agitation 11.60 9.98 292 120080 53781 29778325
Stomatitis 11.55 9.98 95 120277 37184 29794922
Rheumatoid arthritis 11.52 9.98 231 120141 40966 29791140
Monocyte percentage increased 11.41 9.98 16 120356 884 29831222
Ultrasound liver abnormal 11.40 9.98 7 120365 129 29831977
Adrenergic syndrome 11.21 9.98 6 120366 84 29832022
Vessel puncture site bruise 11.18 9.98 5 120367 46 29832060
Urticaria 11.16 9.98 293 120079 54313 29777793
Drug screen positive 11.13 9.98 41 120331 4366 29827740
Anti-thyroid antibody positive 11.08 9.98 5 120367 47 29832059
Infusion site erythema 11.05 9.98 22 120350 1624 29830482
Prescribed overdose 10.86 9.98 11 120361 8550 29823556
Urobilinogen urine increased 10.71 9.98 10 120362 353 29831753
Liver transplant 10.66 9.98 30 120342 2772 29829334
Medication overuse headache 10.65 9.98 5 120367 52 29832054
Post transplant lymphoproliferative disorder 10.63 9.98 4 120368 5302 29826804
General physical health deterioration 10.63 9.98 313 120059 99631 29732475
Pathogen resistance 10.45 9.98 11 120361 8399 29823707
Antineutrophil cytoplasmic antibody positive 10.29 9.98 11 120361 458 29831648
Necrotising enterocolitis neonatal 10.14 9.98 6 120366 103 29832003
Bacterial test 10.08 9.98 7 120365 160 29831946
Therapeutic response decreased 10.06 9.98 57 120315 24292 29807814
Ureteric obstruction 10.04 9.98 18 120354 1228 29830878
Cytomegalovirus infection 10.01 9.98 55 120317 23619 29808487

Pharmacologic Action:

SourceCodeDescription
ATC D11AX26 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC N06BC01 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Xanthine derivatives
ATC V04CG30 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Tests for gastric secretion
FDA CS M0023046 Xanthines
FDA PE N0000175729 Central Nervous System Stimulation
FDA EPC N0000175739 Central Nervous System Stimulant
FDA EPC N0000175790 Methylxanthine
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058915 Purinergic P1 Receptor Antagonists
CHEBI has role CHEBI:25435 mutagens
CHEBI has role CHEBI:35337 analeptic drug
CHEBI has role CHEBI:35471 psychopharmaceuticals
CHEBI has role CHEBI:35498 diuretics
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:50218 phosphodiesterase inhibitors
CHEBI has role CHEBI:50925 serine/threonine protein kinase inhibitors
CHEBI has role CHEBI:53121 adenosine a2a receptor antagonists
CHEBI has role CHEBI:60809 adjuvants
CHEBI has role CHEBI:64047 food additives
CHEBI has role CHEBI:67114 ryrs activator
CHEBI has role CHEBI:71232 adenosine receptor antagonists
CHEBI has role CHEBI:75771 mus musculus metabolite
CHEBI has role CHEBI:76924 plant metabolites
CHEBI has role CHEBI:76946 fungal metabolites
CHEBI has role CHEBI:78298 environmental contaminants
CHEBI has role CHEBI:85234 human blood serum metabolites

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Sinus headache indication 4969004
Apnea in the newborn indication 13094009
Pain indication 22253000
Migraine indication 37796009 DOID:6364
Joint pain indication 57676002
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Common cold indication 82272006 DOID:10459
Vascular headache indication 128187005
Backache indication 161891005
Cluster headache syndrome indication 193031009
Spasticity indication 221360009
Headache disorder indication 230461009
Dysmenorrhea indication 266599000
Influenza-like symptoms indication 315642008
Tension-type headache indication 398057008
Cluster Headache Prevention indication
Fatigue off-label use 84229001
Urinary incontinence off-label use 165232002
Obesity off-label use 414916001 DOID:9970
Brain damage contraindication 2470005
Necrotizing enterocolitis in fetus OR newborn contraindication 2707005
Ocular hypertension contraindication 4210003 DOID:9282
Gastritis contraindication 4556007 DOID:4029
Hypophosphatemia contraindication 4996001
Tachyarrhythmia contraindication 6285003
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Urinary tract obstruction contraindication 7163005 DOID:5200
Alcoholism contraindication 7200002
Alcohol withdrawal delirium contraindication 8635005
Hyperammonemia contraindication 9360008
Peptic ulcer contraindication 13200003 DOID:750
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Asthenia contraindication 13791008
Hepatic encephalopathy contraindication 13920009 DOID:13413
Hyperkalemia contraindication 14140009
Severe chronic ulcerative colitis contraindication 14311001
Constipation contraindication 14760008 DOID:2089
Chronic disease of respiratory system contraindication 17097001
Mood swings contraindication 18963009
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Inflammatory bowel disease contraindication 24526004 DOID:0050589
Ventricular tachycardia contraindication 25569003
Alcohol intoxication contraindication 25702006
Complete atrioventricular block contraindication 27885002
Shock contraindication 27942005
Toxic megacolon contraindication 28536002 DOID:1770
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Acute cerebrovascular insufficiency contraindication 29322000
Atony of colon contraindication 29479008
Hypercapnia contraindication 29596007
Dehydration contraindication 34095006
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Acute hepatitis contraindication 37871000
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Gastrointestinal ulcer contraindication 40845000
Hypothyroidism contraindication 40930008 DOID:1459
Complete trisomy 21 syndrome contraindication 41040004 DOID:14250
Hypokalemia contraindication 43339004
Body fluid retention contraindication 43498006
Hyperactive behavior contraindication 44548000
Fecal impaction contraindication 44635007
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Retroperitoneal fibrosis contraindication 49120005
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Acidosis contraindication 51387008
Fibrosis of lung contraindication 51615001 DOID:3770
Gastrointestinal perforation contraindication 51875005
Vitamin K deficiency contraindication 52675005 DOID:11249
Nasal polyp contraindication 52756005
Gastrectomy contraindication 53442002
Paralytic ileus contraindication 55525008 DOID:8442
Peptic reflux disease contraindication 57643001
Congenital myotonia, autosomal dominant form contraindication 57938005
Acute nephropathy contraindication 58574008
Leber's optic atrophy contraindication 58610003 DOID:705
Hepatic failure contraindication 59927004
Diarrhea contraindication 62315008
Thrombophlebitis contraindication 64156001 DOID:3875
Ulcerative colitis contraindication 64766004 DOID:8577
Blood coagulation disorder contraindication 64779008 DOID:1247
Arterial thrombosis contraindication 65198009
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Hypermagnesemia contraindication 66978005
Benign intracranial hypertension contraindication 68267002 DOID:11459
Hemorrhoids contraindication 70153002 DOID:9746
Poisoning by acetaminophen contraindication 70273001
Agoraphobia contraindication 70691001 DOID:593
Arteriosclerotic vascular disease contraindication 72092001
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Sleep apnea contraindication 73430006 DOID:0050847
Factor II deficiency contraindication 73975000
Reye's syndrome contraindication 74351001 DOID:14525
Gastrointestinal hemorrhage contraindication 74474003
Urethral stricture contraindication 76618002
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Spastic paralysis contraindication 78403003
Disturbance of salivary secretion contraindication 78948009
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Chronic idiopathic constipation contraindication 82934008
Cor pulmonale contraindication 83291003 DOID:8515
Hiatal hernia contraindication 84089009 DOID:12642
Atrophic gastritis contraindication 84568007 DOID:8929
Epilepsy contraindication 84757009 DOID:1826
Pulmonary emphysema contraindication 87433001
Gout contraindication 90560007 DOID:13189
Chronic renal failure syndrome contraindication 90688005
Kidney disease contraindication 90708001 DOID:557
Thyrotoxicosis contraindication 90739004 DOID:7997
Hemophilia contraindication 90935002
Myasthenia gravis contraindication 91637004 DOID:437
Obstruction of duodenum contraindication 95532008 DOID:3558
Disorder of biliary tract contraindication 105997008 DOID:9741
Anemia due to enzyme deficiency contraindication 111577008
Prolonged QT interval contraindication 111975006
Acute abdominal pain contraindication 116290004
Procedure on urinary system contraindication 118677009
Gastrointestinal obstruction contraindication 126765001
Neoplasm of brain contraindication 126952004 DOID:1319
von Willebrand disorder contraindication 128105004 DOID:12531
Seizure disorder contraindication 128613002
Autonomic dysreflexia contraindication 129618003
Bleeding contraindication 131148009
Prolonged PR interval contraindication 164947007
Drug-induced psychosis contraindication 191483003 DOID:1742
Obsessive-compulsive disorder contraindication 191736004 DOID:10933
Insomnia contraindication 193462001
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Coronary artery bypass graft contraindication 232717009
Myocardial dysfunction contraindication 233928007
Peripheral ischemia contraindication 233958001
Gastroesophageal reflux disease contraindication 235595009 DOID:8534
Gastroparesis contraindication 235675006
Disease of liver contraindication 235856003 DOID:409
Chronic diarrhea contraindication 236071009
Hyporeninemic hypoaldosteronism contraindication 236464008
Aluminum intoxication contraindication 236546003
Bladder outflow obstruction contraindication 236645006
Morbid obesity contraindication 238136002 DOID:11981
Sepsis syndrome contraindication 238150007
Pyloric obstruction contraindication 244815007
Sleep automatism contraindication 247962006
Raynaud's phenomenon contraindication 266261006
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Anemia contraindication 271737000 DOID:2355
Drowsy contraindication 271782001
Exacerbation of asthma contraindication 281239006
Cerebral ischemia contraindication 287731003
Pregnancy, function contraindication 289908002
Lesion of brain contraindication 301766008
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Familial hyperkalemic periodic paralysis contraindication 304737009 DOID:14451
Panic disorder contraindication 371631005 DOID:594
Coma contraindication 371632003
Primary adrenocortical insufficiency contraindication 373662000
Operation on gastrointestinal tract contraindication 386621005
Hypoxia contraindication 389086002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Cardiovascular event risk contraindication 395112001
Pseudomembranous enterocolitis contraindication 397683000
Gastric ulcer contraindication 397825006 DOID:10808
Peripheral vascular disease contraindication 400047006
Respiratory insufficiency contraindication 409623005
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393
Myocardial infarction in recovery phase contraindication 418044006
Central nervous system depression contraindication 418072004
Porphyria contraindication 418470004
Ultrarapid metabolizer due to cytochrome p450 CYP2D6 variant contraindication 422681000
Dysfunction of sphincter of Oddi contraindication 430887001
Fibrosis of pleura contraindication 442110002
Congenital long QT syndrome contraindication 442917000
Hypertensive urgency contraindication 443482000
Acute erosive gastritis contraindication 444926003
Smokes tobacco daily contraindication 449868002
Severe dehydration contraindication 450316000
Acute exacerbation of asthma contraindication 708038006
Ergot Alkaloid Toxicity contraindication
Acute Thromboembolic Stroke contraindication
Organic Cardiac Disease contraindication
Severe Pruritus contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.86 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
Adenosine receptor A2b GPCR ANTAGONIST Ki 4.77 WOMBAT-PK CHEMBL
Adenosine receptor A1 GPCR ANTAGONIST Ki 4.97 IUPHAR CHEMBL
Adenosine receptor A2a GPCR ANTAGONIST Ki 5.61 CHEMBL CHEMBL
Acetylcholinesterase Enzyme IC50 5.14 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.31 CHEMBL
Adenosine receptor A3 GPCR ANTAGONIST Ki 4.33 WOMBAT-PK
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase IC50 4.12 CHEMBL
Guanine deaminase Enzyme Ki 4.99 CHEMBL
Adenosine receptor A1 GPCR Ki 4.54 CHEMBL
Adenosine receptor A1 GPCR Ki 4.77 CHEMBL
Adenosine A2a receptor Unclassified Ki 4.10 CHEMBL
Adenosine receptor A2a GPCR Ki 5.03 CHEMBL
Adenosine A2 receptor GPCR Ki 4.57 CHEMBL
Glycogen phosphorylase, muscle form Enzyme IC50 4.13 CHEMBL
Adenosine receptor A1 GPCR Ki 4 CHEMBL
Adenosine receptor GPCR Ki 4.22 CHEMBL
Adenosine receptor A2b Unclassified ANTAGONIST Ki 4.89 IUPHAR

External reference:

IDSource
4017537 VUID
N0000145919 NUI
D00528 KEGG_DRUG
69-22-7 SECONDARY_CAS_RN
4017537 VANDF
4018995 VANDF
C0006644 UMLSCUI
CHEBI:27732 CHEBI
CFF PDB_CHEM_ID
CHEMBL113 ChEMBL_ID
2519 PUBCHEM_CID
CHEMBL1200569 ChEMBL_ID
DB00201 DRUGBANK_ID
D002110 MESH_DESCRIPTOR_UI
C026189 MESH_SUPPLEMENTAL_RECORD_UI
407 IUPHAR_LIGAND_ID
3G6A5W338E UNII
1886 RXNORM
11623 MMSL
17093 MMSL
4318 MMSL
4319 MMSL
46084 MMSL
4939 MMSL
d00801 MMSL
000600 NDDF
000601 NDDF
23068001 SNOMEDCT_US
255641001 SNOMEDCT_US
91107009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fiorinal with Codeine HUMAN PRESCRIPTION DRUG LABEL 4 0023-6010 CAPSULE 40 mg ORAL NDA 36 sections
Fiorinal HUMAN PRESCRIPTION DRUG LABEL 3 0023-6146 CAPSULE 40 mg ORAL NDA 23 sections
ExcedrinExtra Strength Pain Reliever HUMAN OTC DRUG LABEL 3 0067-2000 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 13 sections
ExcedrinExtra Strength Pain Reliever HUMAN OTC DRUG LABEL 3 0067-2001 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 15 sections
ExcedrinExtra Strength Geltabs HUMAN OTC DRUG LABEL 3 0067-2021 TABLET, COATED 65 mg ORAL OTC monograph not final 14 sections
ExcedrinMigraine Geltabs HUMAN OTC DRUG LABEL 3 0067-2035 TABLET, COATED 65 mg ORAL NDA 14 sections
EXCEDRINMIGRAINE HUMAN OTC DRUG LABEL 3 0067-2039 TABLET, FILM COATED 65 mg ORAL NDA 15 sections
ExcedrinMigraine HUMAN OTC DRUG LABEL 3 0067-2040 TABLET, FILM COATED 65 mg ORAL NDA 16 sections
ExcedrinTension Headache HUMAN OTC DRUG LABEL 2 0067-8139 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 15 sections
EXCEDRINMIGRAINE HUMAN OTC DRUG LABEL 3 0067-8201 TABLET, FILM COATED 65 mg ORAL NDA 15 sections
ExcedrinExtra Strength Pain Reliever HUMAN OTC DRUG LABEL 3 0067-8202 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 15 sections
ExcedrinExtra Strength Pain Reliever HUMAN OTC DRUG LABEL 3 0067-8203 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 15 sections
good sense migraine formula HUMAN OTC DRUG LABEL 3 0113-0374 TABLET, FILM COATED 65 mg ORAL ANDA 15 sections
good sense stay awake HUMAN OTC DRUG LABEL 1 0113-0409 TABLET 200 mg ORAL OTC monograph final 14 sections
basic care migraine relief HUMAN OTC DRUG LABEL 3 0113-7374 TABLET, FILM COATED 65 mg ORAL ANDA 15 sections
PANULLDOLExtra HUMAN OTC DRUG LABEL 2 0135-0620 TABLET, FILM COATED 65 mg ORAL OTC monograph not final 16 sections
Butalbital, Acetaminophen, and Caffeine HUMAN PRESCRIPTION DRUG LABEL 3 0143-0170 CAPSULE 40 mg ORAL ANDA 26 sections
ERGOTAMINE HUMAN PRESCRIPTION DRUG LABEL 2 0143-2120 TABLET, FILM COATED 100 mg ORAL ANDA 22 sections
Bayer Headache HUMAN OTC DRUG LABEL 2 0280-0064 TABLET 32.50 mg ORAL OTC monograph not final 14 sections
Bayer Back and BodyExtra Strength HUMAN OTC DRUG LABEL 2 0280-2150 TABLET 35.50 mg ORAL OTC monograph not final 15 sections
Midol Complete HUMAN OTC DRUG LABEL 3 0280-8005 TABLET 60 mg ORAL OTC monograph not final 17 sections
Midol CompleteGelcaps HUMAN OTC DRUG LABEL 3 0280-8015 TABLET, COATED 60 mg ORAL OTC monograph not final 16 sections
Extra Strength Headache Relief HUMAN OTC DRUG LABEL 3 0363-0021 CAPSULE 65 mg ORAL OTC monograph not final 16 sections
Headache ReliefExtra Strength HUMAN OTC DRUG LABEL 3 0363-0159 TABLET, FILM COATED 65 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections
Stay AwakeMaximum Strength HUMAN OTC DRUG LABEL 1 0363-0226 TABLET 200 mg ORAL OTC MONOGRAPH FINULLL 13 sections
Menstrual ReliefMaximum Strength HUMAN OTC DRUG LABEL 3 0363-0252 TABLET 60 mg ORAL OTC MONOGRAPH NOT FINULLL 16 sections
migraine relief HUMAN OTC DRUG LABEL 3 0363-0374 TABLET, FILM COATED 65 mg ORAL ANDA 15 sections
Tension Headache Relief HUMAN OTC DRUG LABEL 2 0363-0428 TABLET, FILM COATED 65 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections
Extra Strength Back and Body HUMAN OTC DRUG LABEL 2 0363-0431 TABLET, FILM COATED 32.50 mg ORAL OTC monograph not final 15 sections
Headache ReliefExtra Strength HUMAN OTC DRUG LABEL 3 0363-0443 TABLET, FILM COATED 65 mg ORAL OTC MONOGRAPH NOT FINULLL 15 sections