varenicline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
nicotinic acetylcholine receptor partial agonists/agonists 2808 249296-44-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • varenicline
  • champix
  • chantix
  • varenicline tartrate
  • CP-526,555-18
A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.
  • Molecular weight: 211.27
  • Formula: C13H13N3
  • CLOGP: 0.90
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 37.81
  • ALOGS: -3.38
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 72 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 92 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.14 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 87 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.607 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.143 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 10.864 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 5.129 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 76.060 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 84.060 % High 1
herg hERG pIC50 4.375 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 5.636 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.251 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 78.560 % High 1
kinase-safety-class AAK1,ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK5,CDK7,CDK9,CHEK1,CLK2,CLK4,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK1,GRK2,GSK3B,HASPIN,IKBKB,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK12,MAPK7,MAPK9,MARK4,MELK,MET,MKNK2,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIM2,PRKCD,PRKDC,ROCK1,SGK1,SIK2,SIK3,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2 79
kinase-selectivity-class AURKB,AXL,BRAF,CAMK2D,CDK9,DYRK1B,EIF2AK3,FLT3,IRAK1,MAP3K11,MAP3K21,MARK4,SIK2,STK33,SYK,TTK 16
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 1.531 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 2.588 High 1
mh-clint Mouse hepatocyte intrinsic clearance 119.674 High 1
mppb Mouse plasma protein binding (% unbound) 81.640 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.199 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 80.250 % High 1
rat-kpuu-brain Rat brain Kpuu 0.040 % High 1
rh-clint Rat hepatocyte intrinsic clearance 76.033 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 92.750 % High 1
rppb Rat plasma protein binding (% unbound) 74.690 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 935.406 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 10, 2006 FDA PFIZER INC

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
Abnormal dreams 3017.00 17.01 746 38594 10511 90578596
Suicidal ideation 1409.98 17.01 672 38668 73183 90515924
Nausea 1237.07 17.01 1916 37424 1108400 89480707
Depression 1199.41 17.01 1011 38329 299590 90289517
Nightmare 907.73 17.01 345 38995 21380 90567727
Feeling abnormal 676.25 17.01 568 38772 166667 90422440
Anger 672.33 17.01 245 39095 13475 90575632
Anxiety 573.54 17.01 688 38652 309084 90280023
Crying 478.24 17.01 230 39110 25415 90563692
Irritability 475.65 17.01 255 39085 35407 90553700
Insomnia 459.21 17.01 640 38700 332834 90256273
Tobacco user 451.51 17.01 97 39243 689 90588418
Agitation 450.89 17.01 309 39031 66789 90522318
Aggression 439.96 17.01 220 39120 26448 90562659
Mood swings 327.40 17.01 166 39174 20536 90568571
Mood altered 323.35 17.01 155 39185 16989 90572118
Abnormal behaviour 321.99 17.01 169 39171 22459 90566648
Depressed mood 303.95 17.01 217 39123 50005 90539102
Nervousness 270.12 17.01 174 39166 33882 90555225
Dysgeusia 266.13 17.01 204 39136 52356 90536751
Flatulence 239.44 17.01 174 39166 41193 90547914
Paranoia 232.21 17.01 113 39227 12795 90576312
Thinking abnormal 217.97 17.01 105 39235 11627 90577480
Off label use 214.49 17.01 106 39234 1102146 89486961
Homicidal ideation 201.95 17.01 60 39280 1720 90587387
Panic attack 199.96 17.01 131 39209 26234 90562873
Emotional disorder 199.19 17.01 107 39233 14890 90574217
Tearfulness 174.92 17.01 69 39271 4711 90584396
Mental disorder 162.59 17.01 125 39215 32193 90556914
Disturbance in attention 153.82 17.01 142 39198 46967 90542140
Mania 149.99 17.01 87 39253 14037 90575070
Psychotic disorder 144.57 17.01 115 39225 31115 90557992
Infusion related reaction 117.20 17.01 20 39320 416760 90172347
Suicidal behaviour 114.49 17.01 44 39296 2800 90586307
Drug hypersensitivity 111.74 17.01 447 38893 463162 90125945
Systemic lupus erythematosus 109.50 17.01 14 39326 361882 90227225
Personality change 107.89 17.01 56 39284 7265 90581842
Treatment failure 107.59 17.01 6 39334 303922 90285185
Hallucination 106.25 17.01 137 39203 65822 90523285
Suicide attempt 102.23 17.01 144 39196 75255 90513852
Vomiting 100.89 17.01 635 38705 787658 89801449
General physical health deterioration 99.91 17.01 17 39323 355098 90234009
Bipolar disorder 99.81 17.01 57 39283 8928 90580179
Dizziness 97.84 17.01 509 38831 588775 90000332
Tobacco withdrawal symptoms 94.10 17.01 15 39325 9 90589098
Stress 89.61 17.01 141 39199 81254 90507853
Self-injurious ideation 89.11 17.01 38 39302 3165 90585942
Alopecia 88.04 17.01 53 39287 495018 90094089
Fear 87.35 17.01 66 39274 16556 90572551
Rheumatoid arthritis 86.63 17.01 25 39315 362589 90226518
Arthropathy 84.33 17.01 27 39313 366215 90222892
Chronic obstructive pulmonary disease 82.81 17.01 129 39211 73700 90515407
Pyrexia 80.77 17.01 101 39239 660384 89928723
Hostility 80.33 17.01 32 39308 2241 90586866
Joint swelling 79.97 17.01 61 39279 503239 90085868
Impaired healing 78.80 17.01 6 39334 234193 90354914
Hepatic necrosis 77.36 17.01 43 39297 6395 90582712
Glossodynia 77.19 17.01 22 39318 321757 90267350
Palpitations 75.93 17.01 177 39163 136551 90452556
Headache 75.67 17.01 635 38705 862111 89726996
Hepatic enzyme increased 75.58 17.01 31 39309 360705 90228402
Acute kidney injury 74.86 17.01 23 39317 320364 90268743
Impaired driving ability 74.59 17.01 39 39301 5134 90583973
Infection 74.45 17.01 32 39308 362062 90227045
Tremor 74.09 17.01 188 39152 152985 90436122
Psoriatic arthropathy 73.67 17.01 7 39333 228328 90360779
Wound 72.15 17.01 21 39319 302959 90286148
Impaired work ability 70.44 17.01 62 39278 19264 90569843
Anaemia 69.68 17.01 33 39307 352769 90236338
Product use in unapproved indication 68.66 17.01 30 39310 336206 90252901
Somnolence 68.45 17.01 223 39117 208861 90380246
Drug interaction 67.61 17.01 268 39072 276185 90312922
Malaise 67.44 17.01 460 38880 585526 90003581
Violence-related symptom 66.73 17.01 20 39320 591 90588516
Peripheral swelling 65.68 17.01 50 39290 413056 90176051
Feeling jittery 65.62 17.01 54 39286 15317 90573790
Somnambulism 65.16 17.01 38 39302 6190 90582917
Hypersomnia 64.70 17.01 62 39278 21469 90567638
Euphoric mood 64.64 17.01 36 39304 5373 90583734
Hallucination, auditory 63.80 17.01 54 39286 15921 90573186
Panic reaction 63.59 17.01 34 39306 4683 90584424
Death 63.21 17.01 63 39277 456488 90132619
Constipation 63.16 17.01 265 39075 280130 90308977
Apathy 62.85 17.01 46 39294 10994 90578113
Thrombocytopenia 60.91 17.01 9 39331 208716 90380391
Product use issue 60.47 17.01 34 39306 329885 90259222
Therapeutic response unexpected 60.13 17.01 60 39280 21820 90567287
Exposure during pregnancy 57.72 17.01 16 39324 238394 90350713
Poor quality sleep 57.57 17.01 62 39278 24631 90564476
Withdrawal syndrome 56.86 17.01 59 39281 22465 90566642
Lower respiratory tract infection 56.75 17.01 19 39321 250640 90338467
Neutropenia 56.53 17.01 14 39326 224890 90364217
Vision blurred 53.96 17.01 136 39204 110157 90478950
Sleep disorder 53.33 17.01 198 39142 197832 90391275
Amnesia 53.30 17.01 134 39206 108371 90480736
Nicotine dependence 52.33 17.01 19 39321 1031 90588076
Decreased interest 51.76 17.01 29 39311 4378 90584729
Weight increased 50.96 17.01 333 39007 417594 90171513
Therapeutic product effect incomplete 50.85 17.01 11 39329 193885 90395222
Liver injury 50.59 17.01 7 39333 170560 90418547
Hepatic encephalopathy 49.82 17.01 44 39296 13728 90575379
Sinusitis 49.02 17.01 46 39294 343042 90246065
Type 2 diabetes mellitus 48.52 17.01 14 39326 203230 90385877
Pre-existing condition improved 47.27 17.01 36 39304 9133 90579974
Social avoidant behaviour 47.13 17.01 25 39315 3388 90585719
Drug withdrawal syndrome 46.77 17.01 60 39280 28663 90560444
Parosmia 46.11 17.01 32 39308 7037 90582070
Mobility decreased 45.70 17.01 26 39314 250708 90338399
Screaming 44.93 17.01 25 39315 3725 90585382
Swelling 44.27 17.01 71 39269 418987 90170120
Psychiatric symptom 43.58 17.01 31 39309 7087 90582020
C-reactive protein increased 42.38 17.01 13 39327 181376 90407731
Impatience 41.63 17.01 13 39327 442 90588665
Joint range of motion decreased 41.59 17.01 5 39335 135638 90453469
Therapeutic product effect decreased 41.09 17.01 36 39304 277535 90311572
Hot flush 40.95 17.01 84 39256 59404 90529703
Musculoskeletal stiffness 40.91 17.01 41 39299 296491 90292616
Condition aggravated 40.76 17.01 128 39212 595417 89993690
Osteoarthritis 40.67 17.01 17 39323 195713 90393394
Impulsive behaviour 39.94 17.01 18 39322 1712 90587395
Inflammation 39.61 17.01 14 39326 178578 90410529
Nasopharyngitis 39.32 17.01 73 39267 407031 90182076
Irritable bowel syndrome 37.10 17.01 22 39318 207426 90381681
Alcohol use 36.91 17.01 17 39323 1700 90587407
Arthralgia 36.53 17.01 194 39146 778328 89810779
Seizure 36.49 17.01 147 39193 152482 90436625
Delusion 36.28 17.01 37 39303 13803 90575304
Drug intolerance 35.95 17.01 89 39251 447502 90141605
Disease progression 35.21 17.01 12 39328 156603 90432504
Energy increased 35.15 17.01 20 39320 3110 90585997
Ageusia 35.10 17.01 39 39301 16037 90573070
Psychomotor hyperactivity 34.95 17.01 35 39305 12778 90576329
Feelings of worthlessness 34.87 17.01 11 39329 387 90588720
Oedema mouth 34.43 17.01 18 39322 2368 90586739
Hyperphagia 34.34 17.01 19 39321 2799 90586308
Depression suicidal 34.05 17.01 17 39323 2032 90587075
Sepsis 33.69 17.01 18 39322 179796 90409311
Increased appetite 33.69 17.01 33 39307 11732 90577375
Physical assault 33.15 17.01 13 39327 873 90588234
Toxicity to various agents 33.06 17.01 46 39294 287800 90301307
Restlessness 32.73 17.01 57 39283 35663 90553444
Affective disorder 32.47 17.01 27 39313 7766 90581341
Stomatitis 32.46 17.01 43 39297 274655 90314452
Dissociation 31.65 17.01 25 39315 6690 90582417
Therapy non-responder 31.56 17.01 10 39330 136694 90452413
Hyperhidrosis 31.56 17.01 130 39210 136175 90452932
Incorrect dose administered 31.22 17.01 90 39250 78840 90510267
Bipolar I disorder 30.89 17.01 16 39324 2066 90587041
Tachyphrenia 30.87 17.01 15 39325 1691 90587416
Gastrointestinal disorder 30.51 17.01 40 39300 256647 90332460
Negative thoughts 30.47 17.01 13 39327 1084 90588023
Sciatica 30.44 17.01 4 39336 101378 90487729
Lip dry 30.27 17.01 4 39336 100951 90488156
Bursitis 29.75 17.01 10 39330 131644 90457463
Formication 29.64 17.01 21 39319 4770 90584337
Hypokalaemia 29.55 17.01 10 39330 131106 90458001
White blood cell count decreased 29.49 17.01 18 39322 167091 90422016
Feeling of despair 29.48 17.01 18 39322 3186 90585921
Feeling guilty 29.29 17.01 11 39329 657 90588450
Cardiac failure 29.13 17.01 6 39334 109490 90479617
Disorientation 28.85 17.01 61 39279 44053 90545054
Intentional product use issue 28.76 17.01 31 39309 216861 90372246
Hospitalisation 28.48 17.01 10 39330 128090 90461017
Discomfort 28.46 17.01 47 39293 274288 90314819
Affect lability 28.26 17.01 37 39303 18026 90571081
Pneumonia 28.26 17.01 162 39178 637897 89951210
Leukopenia 27.89 17.01 5 39335 100705 90488402
Weaning failure 27.88 17.01 10 39330 524 90588583
Liver disorder 27.77 17.01 9 39331 121260 90467847
Memory impairment 27.64 17.01 163 39177 197081 90392026
Obesity 27.62 17.01 6 39334 105501 90483606
Renal impairment 27.59 17.01 6 39334 105415 90483692
Alcohol interaction 27.53 17.01 14 39326 1740 90587367
Emphysema 27.42 17.01 30 39310 12125 90576982
Recalled product administered 27.16 17.01 11 39329 804 90588303
Blister 27.09 17.01 43 39297 254955 90334152
Vertigo 27.03 17.01 79 39261 69732 90519375
Nasal discomfort 26.89 17.01 21 39319 5527 90583580
Fibromyalgia 26.78 17.01 30 39310 206239 90382868
Restless legs syndrome 26.21 17.01 40 39300 22430 90566677
Malignant neoplasm progression 26.17 17.01 7 39333 106863 90482244
Frustration tolerance decreased 26.14 17.01 24 39316 7872 90581235
Mental impairment 25.77 17.01 34 39306 16686 90572421
Middle insomnia 25.72 17.01 34 39306 16717 90572390
Flight of ideas 25.29 17.01 9 39331 461 90588646
Grip strength decreased 24.78 17.01 5 39335 92571 90496536
Tobacco abuse 24.73 17.01 10 39330 728 90588379
Intentional self-injury 24.56 17.01 45 39295 29289 90559818
Abdominal distension 24.51 17.01 117 39223 130484 90458623
Pleural effusion 24.45 17.01 9 39331 111982 90477125
Gingival bleeding 24.05 17.01 31 39309 14872 90574235
Liver function test increased 23.97 17.01 4 39336 84851 90504256
Urinary tract infection 23.57 17.01 62 39278 305570 90283537
Musculoskeletal pain 23.24 17.01 24 39316 171227 90417880
Autoimmune disorder 23.10 17.01 3 39337 76741 90512366
Major depression 23.04 17.01 25 39315 10010 90579097
Gait inability 22.89 17.01 18 39322 146438 90442669
Pulmonary fibrosis 22.87 17.01 9 39331 107494 90481613
Pharyngeal oedema 22.78 17.01 29 39311 13742 90575365
Large intestine polyp 22.64 17.01 24 39316 9362 90579745
Product dispensing error 22.15 17.01 27 39313 12246 90576861
Flat affect 22.13 17.01 12 39328 1699 90587408
Psychotic behaviour 22.10 17.01 9 39331 667 90588440
Oedema 22.01 17.01 33 39307 200262 90388845
Respiratory failure 21.97 17.01 12 39328 118406 90470701
Lower limb fracture 21.92 17.01 5 39335 85008 90504099
Hepatotoxicity 21.86 17.01 56 39284 45786 90543321
Obsessive-compulsive disorder 21.73 17.01 17 39323 4487 90584620
Laziness 21.57 17.01 9 39331 710 90588397
Knee arthroplasty 21.24 17.01 5 39335 83177 90505930
Morbid thoughts 21.16 17.01 9 39331 745 90588362
Neutrophil count decreased 21.05 17.01 3 39337 71529 90517578
Red blood cell sedimentation rate increased 21.02 17.01 5 39335 82590 90506517
Pain 20.83 17.01 306 39034 996035 89593072
Blood creatinine increased 20.74 17.01 9 39331 101377 90487730
Interstitial lung disease 20.72 17.01 4 39336 76401 90512706
Haemoglobin decreased 20.54 17.01 24 39316 161932 90427175
Lethargy 20.32 17.01 67 39273 63072 90526035
Menstruation irregular 20.14 17.01 21 39319 8039 90581068
Platelet count decreased 19.97 17.01 18 39322 136951 90452156
Obsessive thoughts 19.56 17.01 8 39332 600 90588507
Depressive symptom 19.35 17.01 17 39323 5268 90583839
Contusion 19.33 17.01 51 39289 251165 90337942
Unevaluable event 19.28 17.01 60 39280 54788 90534319
Nocturia 19.23 17.01 23 39317 10232 90578875
Speech disorder 19.02 17.01 53 39287 45532 90543575
Tobacco poisoning 18.93 17.01 5 39335 92 90589015
Muscle twitching 18.85 17.01 36 39304 24166 90564941
Hypotension 18.83 17.01 75 39265 325322 90263785
Delusional perception 18.38 17.01 6 39334 236 90588871
Oropharyngeal blistering 18.36 17.01 9 39331 1034 90588073
Loss of employment 18.27 17.01 13 39327 2974 90586133
Derealisation 18.06 17.01 10 39330 1475 90587632
Exercise test abnormal 18.04 17.01 5 39335 111 90588996
Chest pain 17.99 17.01 215 39125 319430 90269677
Food craving 17.97 17.01 11 39329 1956 90587151
Sleep talking 17.66 17.01 9 39331 1124 90587983
Dependence 17.33 17.01 11 39329 2084 90587023
Increased bronchial secretion 17.06 17.01 11 39329 2142 90586965

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
Abnormal dreams 2070.93 19.07 545 23034 7726 42590030
Depression 1311.41 19.07 795 22784 110568 42487188
Suicidal ideation 1242.98 19.07 581 22998 47580 42550176
Nightmare 888.92 19.07 378 23201 24634 42573122
Anger 606.35 19.07 239 23340 12779 42584977
Insomnia 494.17 19.07 454 23125 117799 42479957
Aggression 485.99 19.07 303 23276 43860 42553896
Irritability 483.33 19.07 258 23321 27870 42569886
Agitation 458.20 19.07 337 23242 63977 42533779
Mood swings 438.98 19.07 170 23409 8656 42589100
Nausea 435.23 19.07 780 22799 396019 42201737
Anxiety 394.85 19.07 402 23177 118158 42479598
Feeling abnormal 386.46 19.07 315 23264 69471 42528285
Abnormal behaviour 279.43 19.07 177 23402 26274 42571482
Tobacco user 254.36 19.07 60 23519 519 42597237
Mood altered 229.19 19.07 114 23465 10604 42587152
Off label use 217.47 19.07 45 23534 638290 41959466
Depressed mood 199.57 19.07 137 23442 23247 42574509
Paranoia 173.89 19.07 104 23475 13922 42583834
Personality change 168.88 19.07 76 23503 5643 42592113
Homicidal ideation 168.51 19.07 62 23517 2732 42595024
Vomiting 165.27 19.07 439 23140 289284 42308472
Thinking abnormal 152.58 19.07 76 23503 7085 42590671
Hallucination 137.14 19.07 164 23415 57343 42540413
Nervousness 131.57 19.07 86 23493 13446 42584310
Amnesia 123.76 19.07 112 23467 28325 42569431
Suicide attempt 122.47 19.07 139 23440 45961 42551795
Violence-related symptom 122.46 19.07 33 23546 509 42597247
Acute kidney injury 114.56 19.07 31 23548 367306 42230450
Death 100.74 19.07 69 23510 471116 42126640
Panic attack 99.64 19.07 67 23512 10978 42586778
Emotional disorder 97.41 19.07 54 23525 6260 42591496
Hostility 96.48 19.07 30 23549 783 42596973
Pyrexia 96.46 19.07 49 23530 393993 42203763
Drug hypersensitivity 92.38 19.07 183 23396 99206 42498550
Suicidal behaviour 92.09 19.07 34 23545 1512 42596244
Mania 90.43 19.07 62 23517 10485 42587271
Pneumonia 87.31 19.07 64 23515 422085 42175671
Alcohol use 84.56 19.07 38 23541 2810 42594946
Psychotic disorder 82.56 19.07 91 23488 29117 42568639
Crying 78.16 19.07 47 23532 6347 42591409
Febrile neutropenia 77.13 19.07 7 23572 185696 42412060
Neutropenia 76.54 19.07 10 23569 199421 42398335
Toxicity to various agents 75.86 19.07 17 23562 229119 42368637
Sepsis 74.13 19.07 11 23568 199323 42398433
Physical assault 72.67 19.07 26 23553 1056 42596700
Disturbance in attention 67.59 19.07 83 23496 29783 42567973
Mental disorder 66.88 19.07 65 23514 17964 42579792
Anaemia 66.79 19.07 36 23543 280242 42317514
Thrombocytopenia 65.26 19.07 13 23566 190266 42407490
Memory impairment 62.51 19.07 105 23474 50117 42547639
Product use in unapproved indication 62.43 19.07 13 23566 184443 42413313
Apathy 59.56 19.07 44 23535 8362 42589394
Sleep disorder 56.49 19.07 98 23481 47997 42549759
Impaired driving ability 56.05 19.07 29 23550 2926 42594830
Self-injurious ideation 55.70 19.07 25 23554 1843 42595913
Bipolar disorder 53.63 19.07 31 23548 3891 42593865
Asthma-chronic obstructive pulmonary disease overlap syndrome 53.39 19.07 23 23556 1536 42596220
Dizziness 53.13 19.07 275 23304 248979 42348777
Headache 52.34 19.07 266 23313 239103 42358653
Flatulence 50.72 19.07 66 23513 25086 42572670
Hypotension 50.66 19.07 41 23538 257590 42340166
Disease progression 48.85 19.07 10 23569 143646 42454110
Bronchial hyperreactivity 48.70 19.07 23 23556 1906 42595850
Malignant neoplasm progression 48.05 19.07 3 23576 108397 42489359
Pancytopenia 47.38 19.07 5 23574 117738 42480018
Somnambulism 46.71 19.07 27 23552 3388 42594368
Verbal abuse 46.46 19.07 13 23566 232 42597524
Platelet count decreased 46.39 19.07 10 23569 138571 42459185
White blood cell count decreased 46.24 19.07 4 23575 110392 42487364
Pulmonary function test abnormal 44.20 19.07 24 23555 2670 42595086
Negative thoughts 43.45 19.07 16 23563 706 42597050
Screaming 42.46 19.07 21 23558 1926 42595830
Multiple organ dysfunction syndrome 42.08 19.07 3 23576 97032 42500724
Road traffic accident 41.48 19.07 52 23527 19041 42578715
General physical health deterioration 41.30 19.07 16 23563 151230 42446526
Completed suicide 40.14 19.07 131 23448 96334 42501422
Affective disorder 39.56 19.07 30 23549 5930 42591826
Morbid thoughts 39.38 19.07 11 23568 195 42597561
Stress 39.33 19.07 80 23499 44132 42553624
Post-traumatic stress disorder 39.29 19.07 21 23558 2264 42595492
Intentional self-injury 38.91 19.07 45 23534 15157 42582599
Urinary tract infection 38.00 19.07 5 23574 99279 42498477
Social avoidant behaviour 36.70 19.07 23 23556 3341 42594415
COVID-19 35.62 19.07 10 23569 115938 42481818
Major depression 35.45 19.07 27 23552 5371 42592385
Dysgeusia 35.45 19.07 66 23513 34123 42563633
Needle track marks 35.15 19.07 8 23571 58 42597698
Renal failure 34.85 19.07 18 23561 143708 42454048
Impaired work ability 34.72 19.07 38 23541 12053 42585703
Haemoglobin decreased 34.56 19.07 15 23564 132456 42465300
Septic shock 34.18 19.07 5 23574 91667 42506089
Withdrawal syndrome 33.32 19.07 41 23538 14734 42583022
Tobacco withdrawal symptoms 32.50 19.07 5 23574 0 42597756
Gun shot wound 31.30 19.07 14 23565 1023 42596733
Respiratory failure 31.13 19.07 16 23563 128116 42469640
Abdominal discomfort 31.11 19.07 102 23477 75153 42522603
Blood creatinine increased 31.09 19.07 11 23568 109992 42487764
Leukopenia 30.51 19.07 3 23576 74743 42523013
Libido decreased 30.22 19.07 24 23555 5074 42592682
Disorientation 30.20 19.07 64 23515 36325 42561431
Frustration tolerance decreased 29.79 19.07 20 23559 3266 42594490
Drug withdrawal syndrome 29.42 19.07 47 23532 21502 42576254
Food craving 29.15 19.07 11 23568 520 42597236
Fear 28.98 19.07 33 23546 10932 42586824
Feeling jittery 28.44 19.07 22 23557 4476 42593280
Psychiatric symptom 27.38 19.07 21 23558 4220 42593536
Panic reaction 27.24 19.07 15 23564 1715 42596041
Erectile dysfunction 26.96 19.07 49 23530 24864 42572892
Alcohol interaction 26.88 19.07 16 23563 2119 42595637
Palpitations 26.77 19.07 75 23504 50722 42547034
Drug screen false positive 26.66 19.07 12 23567 890 42596866
Pharyngeal oedema 26.58 19.07 24 23555 6044 42591712
Renal impairment 26.43 19.07 14 23565 110214 42487542
Seizure 26.28 19.07 134 23445 120427 42477329
Loss of employment 25.87 19.07 10 23569 505 42597251
Infection 25.76 19.07 15 23564 112053 42485703
Hospitalisation 25.61 19.07 5 23574 74325 42523431
Interstitial lung disease 25.56 19.07 6 23573 78456 42519300
Ischaemic cardiomyopathy 25.09 19.07 24 23555 6498 42591258
Marital problem 25.02 19.07 6 23573 56 42597700
Cardiac failure 24.99 19.07 14 23565 106842 42490914
C-reactive protein increased 24.80 19.07 3 23576 63557 42534199
Loss of consciousness 24.76 19.07 109 23470 92245 42505511
Hypomania 24.51 19.07 16 23563 2492 42595264
Mental impairment 24.32 19.07 32 23547 12285 42585471
Poor quality sleep 24.25 19.07 28 23551 9412 42588344
Confusional state 24.10 19.07 167 23412 167430 42430326
Tearfulness 24.08 19.07 18 23561 3482 42594274
Affect lability 23.89 19.07 19 23560 4025 42593731
Pleural effusion 23.80 19.07 12 23567 97154 42500602
Personality disorder 23.76 19.07 12 23567 1151 42596605
Infusion related reaction 23.41 19.07 3 23576 60803 42536953
Bradycardia 23.39 19.07 9 23570 85475 42512281
Decreased interest 23.20 19.07 16 23563 2729 42595027
Restlessness 22.61 19.07 50 23529 29199 42568557
Chest pain 22.45 19.07 143 23436 139387 42458369
Hypokalaemia 22.37 19.07 6 23573 71715 42526041
Diarrhoea 22.04 19.07 157 23422 460692 42137064
Flight of ideas 22.01 19.07 8 23571 340 42597416
Ascites 21.33 19.07 3 23576 56675 42541081
Hyperkalaemia 21.15 19.07 9 23570 80449 42517307
Loss of personal independence in daily activities 21.01 19.07 68 23511 49748 42548008
Tinnitus 20.74 19.07 48 23531 28890 42568866
Anti-cyclic citrullinated peptide antibody positive 20.68 19.07 13 23566 1899 42595857
Feeling of despair 20.48 19.07 11 23568 1197 42596559
Imprisonment 20.42 19.07 9 23570 635 42597121
Feeding disorder 19.85 19.07 24 23555 8467 42589289
Vision blurred 19.74 19.07 70 23509 53629 42544127
Hallucination, auditory 19.72 19.07 32 23547 14832 42582924
Adjustment disorder with mixed anxiety and depressed mood 19.50 19.07 3 23576 0 42597756
Cellulitis 19.49 19.07 5 23574 61580 42536176
Blood triglycerides increased 19.45 19.07 33 23546 15863 42581893
Drug screen positive 19.40 19.07 17 23562 4114 42593642

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Abnormal dreams 1986.51 15.11 511 33339 12269 110543180
Suicidal ideation 1599.07 15.11 709 33141 93228 110462221
Depression 1410.42 15.11 987 32863 316348 110239101
Nightmare 1084.14 15.11 418 33432 38445 110517004
Anger 659.36 15.11 240 33610 18767 110536682
Nausea 530.85 15.11 1163 32687 1234527 109320922
Irritability 495.00 15.11 257 33593 47552 110507897
Agitation 493.65 15.11 349 33501 112702 110442747
Aggression 486.53 15.11 273 33577 58937 110496512
Anxiety 456.13 15.11 544 33306 344534 110210915
Feeling abnormal 401.47 15.11 376 33474 180335 110375114
Mood swings 389.70 15.11 173 33677 22639 110532810
Abnormal behaviour 376.00 15.11 200 33650 38839 110516610
Drug hypersensitivity 364.82 15.11 562 33288 453528 110101921
Depressed mood 360.01 15.11 227 33623 60582 110494867
Insomnia 346.89 15.11 486 33364 360104 110195345
Mood altered 292.61 15.11 139 33711 21236 110534213
Crying 291.93 15.11 147 33703 25481 110529968
Paranoia 256.79 15.11 129 33721 22245 110533204
Tobacco user 222.98 15.11 51 33799 727 110554722
Thinking abnormal 193.68 15.11 94 33756 15046 110540403
Suicide attempt 180.77 15.11 189 33661 103205 110452244
Off label use 174.53 15.11 124 33726 1500061 109055388
Tearfulness 158.92 15.11 66 33784 7329 110548120
Panic attack 151.36 15.11 100 33750 28840 110526609
Vomiting 150.50 15.11 613 33237 910062 109645387
Psychotic disorder 148.89 15.11 124 33726 50813 110504636
Mania 141.76 15.11 85 33765 20711 110534738
Homicidal ideation 141.52 15.11 50 33800 3577 110551872
Personality change 136.79 15.11 67 33783 10935 110544514
Mental disorder 125.08 15.11 100 33750 38691 110516758
Emotional disorder 117.85 15.11 69 33781 16091 110539358
Hallucination 103.60 15.11 141 33709 101291 110454158
Alcohol use 96.10 15.11 39 33811 4083 110551366
Suicidal behaviour 95.18 15.11 37 33813 3460 110551989
Nervousness 88.07 15.11 80 33770 36771 110518678
Self-injurious ideation 87.39 15.11 37 33813 4309 110551140
Acute kidney injury 83.96 15.11 45 33805 635385 109920064
Pyrexia 82.72 15.11 92 33758 898173 109657276
Violence-related symptom 81.99 15.11 24 33826 935 110554514
Anaemia 79.51 15.11 34 33816 547052 110008397
Hostility 75.06 15.11 29 33821 2667 110552782
Hepatic necrosis 74.03 15.11 43 33807 9879 110545570
Apathy 72.75 15.11 51 33799 16188 110539261
Amnesia 72.65 15.11 122 33728 105286 110450163
Impaired work ability 72.42 15.11 62 33788 26357 110529092
Disturbance in attention 72.29 15.11 92 33758 61903 110493546
Febrile neutropenia 69.12 15.11 8 33842 316759 110238690
Bipolar disorder 67.11 15.11 39 33811 8968 110546481
Negative thoughts 65.40 15.11 23 33827 1623 110553826
General physical health deterioration 64.09 15.11 25 33825 425270 110130179
Infusion related reaction 63.33 15.11 19 33831 381143 110174306
Thrombocytopenia 62.47 15.11 15 33835 348870 110206579
Bronchial hyperreactivity 60.89 15.11 27 33823 3517 110551932
Somnambulism 59.34 15.11 32 33818 6373 110549076
Social avoidant behaviour 58.79 15.11 30 33820 5339 110550110
Stress 58.55 15.11 111 33739 105237 110450212
Neutropenia 58.15 15.11 21 33829 374599 110180850
Physical assault 58.07 15.11 21 33829 1607 110553842
Treatment failure 58.05 15.11 8 33842 277226 110278223
Withdrawal syndrome 57.74 15.11 59 33791 31321 110524128
Chronic obstructive pulmonary disease 56.98 15.11 112 33738 109046 110446403
Major depression 56.25 15.11 37 33813 10584 110544865
Delusion 55.64 15.11 51 33799 23704 110531745
Dizziness 55.18 15.11 384 33466 697809 109857640
Affective disorder 54.34 15.11 37 33813 11204 110544245
Pre-existing condition improved 53.29 15.11 30 33820 6496 110548953
Pericarditis 51.85 15.11 4 33846 219110 110336339
Recalled product administered 51.26 15.11 18 33832 1264 110554185
Joint swelling 50.65 15.11 37 33813 442808 110112641
Alcohol interaction 50.46 15.11 24 33826 3670 110551779
Product use in unapproved indication 50.37 15.11 38 33812 447339 110108110
Depression suicidal 50.06 15.11 26 33824 4798 110550651
Pulmonary function test abnormal 49.19 15.11 26 33824 4974 110550475
Pancytopenia 49.11 15.11 4 33846 209609 110345840
Seizure 48.94 15.11 164 33686 221021 110334428
Therapeutic response unexpected 47.86 15.11 47 33803 23796 110531653
Intentional self-injury 47.56 15.11 58 33792 37371 110518078
Glossodynia 47.45 15.11 6 33844 221998 110333451
Hepatic enzyme increased 46.48 15.11 20 33830 320872 110234577
Infection 45.83 15.11 27 33823 362173 110193276
Contraindicated product administered 45.78 15.11 10 33840 248257 110307192
Product availability issue 45.51 15.11 29 33821 7861 110547588
Impaired healing 45.41 15.11 4 33846 196713 110358736
Systemic lupus erythematosus 45.39 15.11 11 33839 254327 110301122
Verbal abuse 45.29 15.11 12 33838 322 110555127
Fear 45.22 15.11 45 33805 23148 110532301
Flatulence 45.11 15.11 67 33783 52082 110503367
Panic reaction 44.91 15.11 25 33825 5297 110550152
Toxicity to various agents 43.28 15.11 50 33800 480505 110074944
Death 42.83 15.11 94 33756 698775 109856674
Duodenal ulcer perforation 42.74 15.11 3 33847 177697 110377752
Dysgeusia 41.71 15.11 76 33774 69909 110485540
Screaming 41.38 15.11 23 33827 4858 110550591
Asthma-chronic obstructive pulmonary disease overlap syndrome 40.83 15.11 25 33825 6319 110549130
Palpitations 40.62 15.11 124 33726 159088 110396361
Ischaemic cardiomyopathy 40.23 15.11 27 33823 7984 110547465
Alopecia 39.75 15.11 32 33818 364721 110190728
Hallucination, auditory 38.67 15.11 44 33806 26353 110529096
Affect lability 37.90 15.11 37 33813 18600 110536849
Hepatic encephalopathy 37.88 15.11 45 33805 28211 110527238
Sepsis 37.87 15.11 27 33823 327319 110228130
Arthropathy 36.98 15.11 21 33829 287501 110267948
Needle track marks 36.97 15.11 8 33842 87 110555362
Hypotension 36.79 15.11 65 33785 523784 110031665
Post-traumatic stress disorder 34.98 15.11 23 33827 6573 110548876
Blood creatinine increased 34.46 15.11 7 33843 182882 110372567
Decreased interest 33.28 15.11 20 33830 4888 110550561
Impaired driving ability 33.27 15.11 22 33828 6348 110549101
Headache 32.80 15.11 413 33437 881964 109673485
Feeling of despair 32.48 15.11 18 33832 3780 110551669
Impulsive behaviour 31.94 15.11 17 33833 3298 110552151
Loss of employment 31.80 15.11 17 33833 3327 110552122
Urinary tract infection 31.52 15.11 32 33818 326250 110229199
Tachyphrenia 31.25 15.11 15 33835 2341 110553108
C-reactive protein increased 30.89 15.11 14 33836 217905 110337544
Disorientation 30.41 15.11 67 33783 70604 110484845
Exposure during pregnancy 30.34 15.11 7 33843 167417 110388032
Drug withdrawal syndrome 30.23 15.11 47 33803 38007 110517442
Disease progression 29.73 15.11 19 33831 244015 110311434
Inflammation 29.68 15.11 11 33839 193227 110362222
Leukopenia 29.52 15.11 5 33845 148786 110406663
Haemoglobin decreased 29.44 15.11 20 33830 248707 110306742
Platelet count decreased 29.39 15.11 17 33833 230426 110325023
White blood cell count decreased 29.14 15.11 17 33833 229373 110326076
Psoriatic arthropathy 28.90 15.11 12 33838 196749 110358700
Memory impairment 28.73 15.11 128 33722 196816 110358633
Pharyngeal oedema 28.62 15.11 30 33820 16398 110539051
Malignant neoplasm progression 28.43 15.11 9 33841 174558 110380891
Mobility decreased 28.23 15.11 19 33831 237403 110318046
Loss of consciousness 28.20 15.11 127 33723 196179 110359270
Multiple organ dysfunction syndrome 28.18 15.11 6 33844 151704 110403745
Flat affect 27.43 15.11 14 33836 2491 110552958
Flight of ideas 27.15 15.11 10 33840 806 110554643
Frustration tolerance decreased 27.06 15.11 22 33828 8709 110546740
Hypokalaemia 27.00 15.11 11 33839 182437 110373012
Weaning failure 26.91 15.11 10 33840 826 110554623
Tobacco withdrawal symptoms 26.13 15.11 4 33846 3 110555446
Hypomania 26.04 15.11 23 33827 10187 110545262
Psychiatric symptom 26.02 15.11 22 33828 9191 110546258
Cardiac disorder 25.96 15.11 66 33784 76214 110479235
Liver injury 25.88 15.11 7 33843 150406 110405043
Nasopharyngitis 25.84 15.11 51 33799 394310 110161139
Marital problem 25.80 15.11 7 33843 206 110555243
Lower respiratory tract infection 25.64 15.11 22 33828 243084 110312365
Anti-cyclic citrullinated peptide antibody positive 25.31 15.11 12 33838 181972 110373477
Arthralgia 25.21 15.11 138 33712 779494 109775955
Wound 24.99 15.11 21 33829 234416 110321033
Hepatotoxicity 24.93 15.11 58 33792 63342 110492107
Agoraphobia 24.66 15.11 9 33841 707 110554742
Sinusitis 24.46 15.11 33 33817 296655 110258794
Food craving 24.31 15.11 12 33838 1991 110553458
Musculoskeletal stiffness 24.22 15.11 30 33820 279792 110275657
Hypersomnia 24.19 15.11 36 33814 28025 110527424
Irritable bowel syndrome 24.14 15.11 10 33840 164205 110391244
Therapy non-responder 24.08 15.11 9 33841 157298 110398151
Osteoarthritis 23.96 15.11 13 33837 182610 110372839
Hospitalisation 23.83 15.11 7 33843 142486 110412963
Cardiac failure 23.70 15.11 14 33836 187612 110367837
Vision blurred 23.66 15.11 90 33760 128932 110426517
Tremor 23.41 15.11 123 33727 202109 110353340
Peripheral swelling 23.37 15.11 56 33794 403978 110151471
Pneumonia 22.78 15.11 166 33684 876548 109678901
Therapeutic product effect incomplete 22.71 15.11 21 33829 223784 110331665
Obsessive thoughts 22.59 15.11 10 33840 1297 110554152
Morbid thoughts 22.47 15.11 9 33841 910 110554539
Sleep disorder due to general medical condition, insomnia type 22.22 15.11 3 33847 105640 110449809
Rheumatoid arthritis 22.09 15.11 36 33814 299577 110255872
Neutrophil count decreased 22.02 15.11 5 33845 120936 110434513
Formication 21.34 15.11 16 33834 5632 110549817
Ageusia 21.09 15.11 28 33822 19617 110535832
Dissociation 20.88 15.11 20 33830 9822 110545627
Euphoric mood 20.77 15.11 19 33831 8808 110546641
Flashback 20.76 15.11 7 33843 435 110555014
Lip dry 20.68 15.11 3 33847 100080 110455369
Libido decreased 20.63 15.11 16 33834 5919 110549530
Restlessness 20.53 15.11 50 33800 56209 110499240
Therapeutic product effect decreased 20.31 15.11 27 33823 244289 110311160
Large intestine polyp 20.14 15.11 24 33826 15093 110540356
Bipolar I disorder 20.02 15.11 11 33839 2272 110553177
Type 2 diabetes mellitus 19.99 15.11 15 33835 177217 110378232
Energy increased 19.95 15.11 13 33837 3661 110551788
Emotional distress 19.84 15.11 43 33807 44804 110510645
Anhedonia 19.75 15.11 24 33826 15404 110540045
Oedema mouth 19.29 15.11 12 33838 3118 110552331
Sleep disorder 19.14 15.11 115 33735 198529 110356920
Renal failure 18.87 15.11 25 33825 226549 110328900
Pleural effusion 18.84 15.11 16 33834 177693 110377756
Agitated depression 18.82 15.11 7 33843 580 110554869
Hyperkalaemia 18.81 15.11 9 33841 135787 110419662
Feelings of worthlessness 18.78 15.11 7 33843 583 110554866
Renal impairment 18.74 15.11 18 33832 188427 110367022
Oedema 18.71 15.11 22 33828 209954 110345495
Alcohol abuse 18.70 15.11 14 33836 4915 110550534
Lactic acidosis 18.67 15.11 3 33847 92808 110462641
Poor quality sleep 18.67 15.11 32 33818 28045 110527404
Dependence 18.19 15.11 11 33839 2718 110552731
Panic disorder 18.19 15.11 12 33838 3449 110552000
Obesity 18.18 15.11 6 33844 113345 110442104
Tinnitus 18.18 15.11 50 33800 60490 110494959
Interstitial lung disease 18.16 15.11 10 33840 139324 110416125
Hypercholesterolaemia 18.13 15.11 3 33847 90834 110464615
Swelling 17.75 15.11 52 33798 350989 110204460
Speech disorder 17.65 15.11 50 33800 61519 110493930
Gun shot wound 17.60 15.11 8 33842 1104 110554345
Bursitis 17.41 15.11 9 33841 129909 110425540
Prescribed overdose 17.25 15.11 3 33847 87578 110467871
Impatience 16.60 15.11 7 33843 807 110554642
Emphysema 16.54 15.11 25 33825 19731 110535718
Sciatica 16.47 15.11 4 33846 92395 110463054
Economic problem 16.27 15.11 12 33838 4119 110551330
Nicotine dependence 16.23 15.11 8 33842 1323 110554126
Pressure of speech 16.22 15.11 8 33842 1324 110554125
Malaise 16.14 15.11 292 33558 671527 109883922
Stomatitis 15.98 15.11 37 33813 270205 110285244
Feeling jittery 15.83 15.11 21 33829 14701 110540748
Drug reaction with eosinophilia and systemic symptoms 15.76 15.11 3 33847 82092 110473357
Hepatic cirrhosis 15.70 15.11 51 33799 67575 110487874
Feeling guilty 15.59 15.11 7 33843 939 110554510
Cardio-respiratory arrest 15.56 15.11 8 33842 115828 110439621
Pneumonia aspiration 15.53 15.11 3 33847 81230 110474219
Somnolence 15.49 15.11 149 33701 297300 110258149
Dysphoria 15.44 15.11 14 33836 6414 110549035
Amyotrophic lateral sclerosis 15.43 15.11 9 33841 2082 110553367
Contusion 15.43 15.11 30 33820 233331 110322118
Fibromyalgia 15.13 15.11 18 33832 170891 110384558

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07BA03 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in nicotine dependence
ATC S01XA28 SENSORY ORGANS
OPHTHALMOLOGICALS
OTHER OPHTHALMOLOGICALS
Other ophthalmologicals
FDA MoA N0000175369 Cholinergic Agonists
MeSH PA D000077444 Smoking Cessation Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018679 Cholinergic Agonists
MeSH PA D018722 Nicotinic Agonists
FDA MoA N0000175702 Partial Cholinergic Nicotinic Agonists
FDA EPC N0000175705 Partial Cholinergic Nicotinic Agonist
FDA EPC N0000175884 Cholinergic Receptor Agonist
CHEBI has role CHEBI:35941 serotonergic agonist
CHEBI has role CHEBI:47958 nicotinic acetylcholine receptor agonist

Related Drugs by ATC class:

N07BA Drugs used in nicotine dependence 1 drug
nicotine
S01XA Other ophthalmologicals 24 drugs
acetylcysteinealteplasealumascorbic acidavacincaptad pegolcenegerminciclosporindexpanthenoldiquafosolethylmorphineguaiazulenheparin show all 24 →

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

DiseaseRelationSNOMED_IDDOID
Smoking cessation assistance indication 384742004
Suicidal thoughts contraindication 6471006
Alcoholism contraindication 7200002
Bipolar disorder contraindication 13746004 DOID:3312
Mood swings contraindication 18963009
Feeling agitated contraindication 24199005
Alcohol intoxication contraindication 25702006
Depressive disorder contraindication 35489007
Schizophrenia contraindication 58214004 DOID:5419
Acute nephropathy contraindication 58574008
Aggressive behavior contraindication 61372001
Aortocoronary artery bypass graft contraindication 67166004
Hostile behavior contraindication 79351003
Angina pectoris contraindication 194828000
Acute coronary syndrome contraindication 394659003
Cardiovascular event risk contraindication 395112001
Peripheral vascular disease contraindication 400047006
Nausea contraindication 422587007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.83 Basic
pKa2 1.25 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 10456396 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 11224598 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 11903941 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 11903943 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 11911380 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 12576080 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 9504644 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 9532944 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)
EQ 0.03MG BASE/SPRAY TYRVAYA OYSTER POINT PHARMA N213978 Oct. 15, 2021 RX SPRAY NASAL 9597284 Oct. 19, 2035 TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel AGONIST Ki 9.40 WOMBAT-PK CHEMBL
Neuronal acetylcholine receptor; alpha3/beta4 Ion channel Ki 7.07 WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel Ki 6.96 CHEMBL
Acetylcholine receptor; alpha1/beta1/delta/gamma Ion channel Ki 5.09 CHEMBL
Neuronal acetylcholine receptor subunit alpha-7 Ion channel Ki 6.90 CHEMBL
Neuronal acetylcholine receptor subunit alpha-7 Ion channel Ki 7.49 CHEMBL
Neuronal acetylcholine receptor; alpha2/beta2 Ion channel Ki 9.66 CHEMBL
Neuronal acetylcholine receptor; alpha3/beta2 Ion channel Ki 8.72 CHEMBL
Neuronal acetylcholine receptor; alpha3/beta4 Ion channel Ki 7.07 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel Ki 10.30 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel Ki 7.82 CHEMBL
Neuronal acetylcholine receptor; alpha2/beta4 Ion channel Ki 7.15 CHEMBL
Acetylcholine receptor Ion channel Ki 5.45 CHEMBL

External reference:

IDSource
4025278 VUID
N0000179790 NUI
D06282 KEGG_DRUG
375815-87-5 SECONDARY_CAS_RN
4025278 VANDF
4025594 VANDF
C1569608 UMLSCUI
CHEBI:84500 CHEBI
QMR PDB_CHEM_ID
CHEMBL1076903 ChEMBL_ID
DB01273 DRUGBANK_ID
CHEMBL6067972 ChEMBL_ID
D000068580 MESH_DESCRIPTOR_UI
5310966 PUBCHEM_CID
5459 IUPHAR_LIGAND_ID
8366 INN_ID
W6HS99O8ZO UNII
591622 RXNORM
21404 MMSL
348368 MMSL
82173 MMSL
d05807 MMSL
011508 NDDF
011509 NDDF
420507002 SNOMEDCT_US
421772003 SNOMEDCT_US
428382005 SNOMEDCT_US
W6HS99O8ZO INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 0069-0468 TABLET, FILM COATED 0.50 mg ORAL NDA 32 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 0069-0469 TABLET, FILM COATED 1 mg ORAL NDA 32 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 0378-5089 TABLET, FILM COATED 0.50 mg ORAL ANDA 31 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 0378-5090 TABLET, FILM COATED 1 mg ORAL ANDA 31 sections
varenicline Human Prescription Drug Label 1 0904-7413 TABLET, FILM COATED 0.50 mg ORAL ANDA 26 sections
varenicline Human Prescription Drug Label 1 0904-7414 TABLET, FILM COATED 1 mg ORAL ANDA 26 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 10135-808 TABLET, FILM COATED 0.50 mg ORAL ANDA 28 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 10135-809 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
Varenicline tartrate Human Prescription Drug Label 1 14445-153 TABLET, FILM COATED 0.50 mg ORAL ANDA 26 sections
Varenicline tartrate Human Prescription Drug Label 1 14445-154 TABLET, FILM COATED 1 mg ORAL ANDA 26 sections
Chantix HUMAN PRESCRIPTION DRUG LABEL 1 21695-633 TABLET, FILM COATED 0.50 mg ORAL NDA 31 sections
Chantix HUMAN PRESCRIPTION DRUG LABEL 1 21695-946 TABLET, FILM COATED 1 mg ORAL NDA 31 sections
Varenicline Human Prescription Drug Label 1 27241-173 TABLET, FILM COATED 0.50 mg ORAL ANDA 28 sections
Varenicline Human Prescription Drug Label 1 27241-174 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 31722-678 TABLET, FILM COATED 0.50 mg ORAL ANDA 27 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 31722-679 TABLET, FILM COATED 1 mg ORAL ANDA 27 sections
Varenicline Human Prescription Drug Label 1 33342-489 TABLET, FILM COATED 0.50 mg ORAL ANDA 29 sections
Varenicline Human Prescription Drug Label 1 33342-490 TABLET, FILM COATED 1 mg ORAL ANDA 29 sections
varenicline HUMAN PRESCRIPTION DRUG LABEL 1 42291-927 TABLET, FILM COATED 0.50 mg ORAL ANDA 26 sections
varenicline HUMAN PRESCRIPTION DRUG LABEL 1 42291-928 TABLET, FILM COATED 1 mg ORAL ANDA 26 sections
varenicline tartrate HUMAN PRESCRIPTION DRUG LABEL 1 42571-459 TABLET, FILM COATED 0.50 mg ORAL ANDA 26 sections
varenicline tartrate HUMAN PRESCRIPTION DRUG LABEL 1 42571-460 TABLET, FILM COATED 1 mg ORAL ANDA 26 sections
VARENICLINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 42858-563 TABLET, FILM COATED 1 mg ORAL ANDA 32 sections
VARENICLINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 42858-564 TABLET, FILM COATED 0.50 mg ORAL ANDA 32 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 43353-899 TABLET, FILM COATED 1 mg ORAL NDA 30 sections
varenicline tartrate HUMAN PRESCRIPTION DRUG LABEL 1 43598-907 TABLET, FILM COATED 0.50 mg ORAL ANDA 28 sections
varenicline tartrate HUMAN PRESCRIPTION DRUG LABEL 1 43598-908 TABLET, FILM COATED 1 mg ORAL ANDA 28 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 49884-155 TABLET, FILM COATED 0.50 mg ORAL ANDA 26 sections
Varenicline HUMAN PRESCRIPTION DRUG LABEL 1 49884-156 TABLET, FILM COATED 1 mg ORAL ANDA 26 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 50090-0995 TABLET, FILM COATED 1 mg ORAL NDA 29 sections