varenicline Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: ONP

  • 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) 0.20 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 92 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.14 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 87 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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 2599.17 16.84 749 39010 9530 46636773
Suicidal ideation 1349.08 16.84 744 39015 55638 46590665
Depression 1348.43 16.84 1130 38629 168974 46477329
Nausea 1020.64 16.84 1962 37797 685492 45960811
Nightmare 840.65 16.84 366 39393 16232 46630071
Anger 598.82 16.84 261 39498 11591 46634712
Feeling abnormal 566.09 16.84 611 39148 124449 46521854
Anxiety 559.01 16.84 729 39030 181228 46465075
Insomnia 555.85 16.84 692 39067 164232 46482071
Crying 466.39 16.84 265 39494 20876 46625427
Irritability 421.00 16.84 278 39481 28668 46617635
Depressed mood 420.31 16.84 293 39466 33026 46613277
Tobacco user 418.10 16.84 103 39656 671 46645632
Aggression 399.26 16.84 246 39513 22498 46623805
Agitation 385.63 16.84 343 39416 55072 46591231
Mood swings 321.92 16.84 190 39569 16062 46630241
Abnormal behaviour 291.06 16.84 196 39563 20862 46625441
Mood altered 283.96 16.84 162 39597 12845 46633458
Tearfulness 248.36 16.84 103 39656 4032 46642271
Paranoia 242.15 16.84 136 39623 10461 46635842
Nervousness 213.45 16.84 184 39575 28291 46618012
Dysgeusia 209.72 16.84 213 39546 40278 46606025
Flatulence 205.18 16.84 181 39578 28697 46617606
Panic attack 200.70 16.84 154 39605 20088 46626215
Thinking abnormal 200.27 16.84 117 39642 9697 46636606
Sleep disorder 196.12 16.84 220 39539 46575 46599728
Homicidal ideation 191.39 16.84 68 39691 1734 46644569
Emotional disorder 173.34 16.84 116 39643 12208 46634095
Off label use 166.69 16.84 58 39701 379783 46266520
Disturbance in attention 161.54 16.84 165 39594 31395 46614908
Psychotic disorder 161.11 16.84 142 39617 22479 46623824
Mental disorder 142.45 16.84 132 39627 22293 46624010
Rheumatoid arthritis 140.85 16.84 19 39740 240196 46406107
Death 139.16 16.84 56 39703 335492 46310811
Acute kidney injury 137.47 16.84 19 39740 235836 46410467
Mania 131.10 16.84 93 39666 10753 46635550
Anaemia 130.80 16.84 29 39730 255750 46390553
Personality change 124.24 16.84 69 39690 5189 46641114
Self-injurious ideation 120.50 16.84 52 39707 2248 46644055
Suicidal behaviour 110.98 16.84 50 39709 2398 46643905
Weight increased 104.78 16.84 343 39416 164130 46482173
Amnesia 100.54 16.84 149 39610 41482 46604821
Tobacco withdrawal symptoms 94.11 16.84 17 39742 12 46646291
Suicide attempt 93.52 16.84 168 39591 54868 46591435
Pyrexia 91.99 16.84 97 39662 348705 46297598
Violence-related symptom 90.30 16.84 27 39732 390 46645913
Drug hypersensitivity 88.37 16.84 426 39333 243399 46402904
Toxicity to various agents 85.00 16.84 37 39722 211729 46434574
Vomiting 83.45 16.84 664 39095 452130 46194173
Hostility 82.03 16.84 34 39725 1328 46644975
Bipolar disorder 80.92 16.84 59 39700 7118 46639185
Malaise 79.00 16.84 517 39242 330715 46315588
Panic reaction 77.95 16.84 45 39714 3644 46642659
Dizziness 77.38 16.84 525 39234 339889 46306414
Thrombocytopenia 76.58 16.84 9 39750 126572 46519731
Nicotine dependence 72.14 16.84 24 39735 499 46645804
Hallucination 70.63 16.84 141 39618 49810 46596493
Euphoric mood 69.34 16.84 44 39715 4228 46642075
Sepsis 68.29 16.84 16 39743 135998 46510305
Fear 65.93 16.84 75 39684 16097 46630206
Apathy 64.89 16.84 52 39707 7216 46639087
Impaired driving ability 64.83 16.84 42 39717 4182 46642121
Headache 63.26 16.84 653 39106 477699 46168604
Stress 61.78 16.84 136 39623 51415 46594888
Hypersomnia 60.24 16.84 70 39689 15369 46630934
Pneumonia 60.08 16.84 146 39613 376174 46270129
Dissociation 59.57 16.84 30 39729 1847 46644456
General physical health deterioration 59.35 16.84 13 39746 115756 46530547
Impaired work ability 57.37 16.84 62 39697 12574 46633729
Memory impairment 57.20 16.84 170 39589 77167 46569136
Urinary tract infection 57.14 16.84 62 39697 220204 46426099
White blood cell count decreased 54.77 16.84 14 39745 112217 46534086
Somnambulism 53.61 16.84 40 39719 4997 46641306
Psychiatric symptom 53.05 16.84 38 39721 4459 46641844
Palpitations 52.12 16.84 189 39570 95070 46551233
Feeling jittery 51.71 16.84 55 39704 10953 46635350
Negative thoughts 51.06 16.84 21 39738 804 46645499
Infusion related reaction 50.60 16.84 12 39747 101196 46545107
Affect lability 48.59 16.84 46 39713 7974 46638329
Decreased interest 47.54 16.84 31 39728 3121 46643182
Pleural effusion 47.51 16.84 7 39752 82945 46563358
Hallucination, auditory 47.48 16.84 52 39707 10704 46635599
Haemoglobin decreased 46.45 16.84 26 39733 128923 46517380
Hypotension 45.72 16.84 80 39679 232509 46413794
Social avoidant behaviour 45.48 16.84 29 39730 2810 46643493
Disease progression 45.30 16.84 11 39748 91289 46555014
Infection 45.22 16.84 29 39730 133563 46512740
Cardiac failure 45.21 16.84 7 39752 79941 46566362
Peripheral swelling 44.98 16.84 41 39718 158030 46488273
Hypokalaemia 44.87 16.84 10 39749 88014 46558289
Exposure during pregnancy 44.83 16.84 18 39741 108194 46538109
Depression suicidal 44.34 16.84 23 39736 1507 46644796
Chronic obstructive pulmonary disease 43.85 16.84 128 39631 57505 46588798
Renal failure 43.73 16.84 21 39738 113573 46532730
Withdrawal syndrome 42.46 16.84 64 39695 18070 46628233
Poor quality sleep 41.80 16.84 58 39701 15195 46631108
Therapeutic product effect incomplete 41.65 16.84 8 39751 78145 46568158
Leukopenia 40.97 16.84 5 39754 68338 46577965
Respiratory failure 40.55 16.84 15 39744 94801 46551502
Impatience 40.55 16.84 14 39745 327 46645976
Blood creatinine increased 40.34 16.84 8 39751 76395 46569908
Parosmia 40.09 16.84 31 39728 4085 46642218
Cardio-respiratory arrest 39.52 16.84 3 39756 59866 46586437
Platelet count decreased 39.26 16.84 18 39741 100006 46546297
Feeling of despair 38.09 16.84 22 39737 1783 46644520
Screaming 37.72 16.84 27 39732 3164 46643139
Hyperphagia 37.71 16.84 21 39738 1587 46644716
Alopecia 37.54 16.84 50 39709 162364 46483939
Constipation 37.33 16.84 265 39494 173832 46472471
Impulsive behaviour 36.11 16.84 20 39739 1495 46644808
Affective disorder 35.82 16.84 31 39728 4784 46641519
Septic shock 35.28 16.84 4 39755 57889 46588414
Dehydration 34.99 16.84 51 39708 159489 46486814
Hospitalisation 34.83 16.84 6 39753 63379 46582924
Product use in unapproved indication 34.27 16.84 17 39742 90256 46556047
Therapeutic response unexpected 33.60 16.84 53 39706 15563 46630740
Depressive symptom 33.53 16.84 24 39735 2812 46643491
Tremor 33.45 16.84 190 39569 115449 46530854
Renal impairment 33.12 16.84 11 39748 74361 46571942
Completed suicide 32.63 16.84 46 39713 145874 46500429
Somnolence 32.25 16.84 236 39523 156285 46490018
Systemic lupus erythematosus 32.04 16.84 8 39751 65172 46581131
Alcohol interaction 31.96 16.84 22 39737 2423 46643880
Atrial fibrillation 31.75 16.84 25 39734 103565 46542738
Abdominal distension 31.57 16.84 135 39624 73216 46573087
Injection site erythema 31.45 16.84 12 39747 74415 46571888
Injection site pain 31.43 16.84 27 39732 107125 46539178
Oedema mouth 31.19 16.84 22 39737 2519 46643784
Feelings of worthlessness 30.64 16.84 11 39748 289 46646014
Formication 30.51 16.84 26 39733 3930 46642373
Sinusitis 29.93 16.84 40 39719 129728 46516575
Interstitial lung disease 29.88 16.84 5 39754 53944 46592359
Alcohol use 29.64 16.84 21 39738 2421 46643882
Abdominal pain upper 29.30 16.84 218 39541 145087 46501216
Energy increased 29.29 16.84 20 39739 2174 46644129
Drug withdrawal syndrome 29.20 16.84 69 39690 27315 46618988
Gastrointestinal haemorrhage 28.73 16.84 15 39744 77358 46568945
Psychomotor hyperactivity 28.53 16.84 38 39721 9575 46636728
Multiple organ dysfunction syndrome 28.18 16.84 5 39754 51705 46594598
Ageusia 27.59 16.84 41 39718 11431 46634872
Product use issue 27.57 16.84 24 39735 94620 46551683
Joint swelling 27.56 16.84 63 39696 166010 46480293
Cardiac failure congestive 27.05 16.84 23 39736 91727 46554576
Hyponatraemia 26.82 16.84 28 39731 101304 46544999
Physical assault 26.00 16.84 14 39745 990 46645313
Pre-existing condition improved 25.83 16.84 30 39729 6582 46639721
Major depression 25.54 16.84 30 39729 6660 46639643
Drug abuse 25.52 16.84 11 39748 63397 46582906
Delusion 25.50 16.84 39 39720 11149 46635154
Hyperkalaemia 25.36 16.84 6 39753 50703 46595600
Feeling guilty 25.35 16.84 11 39748 482 46645821
Neuropathy peripheral 25.34 16.84 24 39735 90869 46555434
Bipolar I disorder 25.28 16.84 16 39743 1530 46644773
Tachyphrenia 25.27 16.84 15 39744 1279 46645024
Arthropathy 25.25 16.84 21 39738 84679 46561624
Diarrhoea 25.19 16.84 331 39428 559271 46087032
Cardiac arrest 25.05 16.84 24 39735 90375 46555928
Arthralgia 24.96 16.84 195 39564 364408 46281895
Oxygen saturation decreased 24.81 16.84 14 39745 69150 46577153
Restlessness 24.74 16.84 62 39697 25462 46620841
Morbid thoughts 24.34 16.84 11 39748 531 46645772
Middle insomnia 24.32 16.84 35 39724 9480 46636823
Nasopharyngitis 24.29 16.84 60 39699 153938 46492365
Increased appetite 24.23 16.84 33 39726 8494 46637809
Derealisation 23.06 16.84 12 39747 791 46645512
Cellulitis 22.77 16.84 16 39743 70272 46576031
Flat affect 22.65 16.84 14 39745 1284 46645019
Herpes zoster 22.59 16.84 15 39744 67857 46578446
Tobacco abuse 22.15 16.84 11 39748 657 46645646
Abdominal discomfort 22.08 16.84 211 39548 150954 46495349
Flight of ideas 22.02 16.84 9 39750 339 46645964
Drug interaction 22 16.84 267 39492 202827 46443476
Hot flush 21.82 16.84 84 39675 43433 46602870
Injection site swelling 21.76 16.84 4 39755 40323 46605980
Frustration tolerance decreased 20.78 16.84 24 39735 5233 46641070
Fall 20.69 16.84 180 39579 328917 46317386
Intentional self-injury 20.65 16.84 56 39703 24110 46622193
Loss of employment 20.54 16.84 13 39746 1243 46645060
Incorrect dose administered 20.50 16.84 85 39674 45465 46600838
Vision blurred 20.48 16.84 127 39632 79581 46566722
Condition aggravated 20.23 16.84 124 39635 244928 46401375
Panic disorder 20.09 16.84 17 39742 2544 46643759
Chest pain 20.06 16.84 234 39525 176090 46470213
Drug ineffective 20.02 16.84 433 39326 677405 45968898
Mental impairment 19.84 16.84 37 39722 12419 46633884
Psychotic behaviour 19.79 16.84 10 39749 620 46645683
Injection site reaction 19.74 16.84 8 39751 47841 46598462
Osteonecrosis of jaw 19.47 16.84 3 39756 34399 46611904
Pain 19.33 16.84 288 39471 476660 46169643
Blood bilirubin increased 19.30 16.84 3 39756 34181 46612122
Weaning failure 19.19 16.84 8 39751 317 46645986
Hyperhidrosis 19.14 16.84 136 39623 89172 46557131
Gingival bleeding 19.08 16.84 35 39724 11604 46634699
Plasma cell myeloma 19.07 16.84 7 39752 44471 46601832
Hepatic enzyme increased 19.06 16.84 25 39734 81762 46564541
Electrocardiogram QT prolonged 18.97 16.84 10 39749 51315 46594988
Osteoarthritis 18.96 16.84 15 39744 62010 46584293
Encephalopathy 18.85 16.84 3 39756 33586 46612717
Hepatic failure 18.72 16.84 3 39756 33413 46612890
Laziness 18.50 16.84 9 39750 514 46645789
Road traffic accident 18.38 16.84 53 39706 23638 46622665
Pulmonary embolism 18.16 16.84 41 39718 108544 46537759
Bradycardia 17.90 16.84 18 39741 66280 46580023
Agitated depression 17.85 16.84 6 39753 129 46646174
Pain in extremity 17.84 16.84 138 39621 258542 46387761
Rhabdomyolysis 17.30 16.84 7 39752 41902 46604401
Oropharyngeal blistering 17.18 16.84 10 39749 822 46645481
Postmenopausal haemorrhage 17.12 16.84 14 39745 1999 46644304

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 1882.06 18.24 551 24604 7564 29919759
Depression 1374.77 18.24 884 24271 89553 29837770
Suicidal ideation 1315.65 18.24 629 24526 35485 29891838
Nightmare 1079.41 18.24 399 24756 11677 29915646
Anger 592.22 18.24 253 24902 10867 29916456
Aggression 533.90 18.24 351 24804 36556 29890767
Irritability 478.09 18.24 276 24879 22774 29904549
Insomnia 465.97 18.24 477 24678 92859 29834464
Agitation 449.46 18.24 368 24787 53705 29873618
Mood swings 440.89 18.24 184 24971 7442 29919881
Nausea 426.66 18.24 832 24323 296125 29631198
Anxiety 417.40 18.24 442 24713 89429 29837894
Feeling abnormal 361.67 18.24 332 24823 56424 29870899
Abnormal behaviour 292.93 18.24 211 24944 25412 29901911
Tobacco user 273.49 18.24 68 25087 470 29926853
Depressed mood 265.61 18.24 170 24985 16859 29910464
Mood altered 249.60 18.24 127 25028 8123 29919200
Personality change 219.69 18.24 97 25058 4503 29922820
Paranoia 195.19 18.24 116 25039 10072 29917251
Homicidal ideation 168.17 18.24 67 25088 2396 29924927
Thinking abnormal 146.91 18.24 77 25078 5234 29922089
Acute kidney injury 143.84 18.24 28 25127 273814 29653509
Vomiting 141.51 18.24 455 24700 219363 29707960
Violence-related symptom 139.16 18.24 40 25115 507 29926816
Amnesia 136.86 18.24 133 25022 24188 29903135
Pneumonia 124.57 18.24 63 25092 334243 29593080
Death 123.49 18.24 74 25081 357209 29570114
Off label use 121.72 18.24 30 25125 249260 29678063
Suicide attempt 116.89 18.24 149 25006 36548 29890775
Nervousness 116.48 18.24 89 25066 11699 29915624
Hallucination 111.06 18.24 169 24986 48890 29878433
Emotional disorder 110.79 18.24 63 25092 5031 29922292
Pyrexia 98.85 18.24 63 25092 294426 29632897
Disturbance in attention 97.29 18.24 106 25049 22023 29905300
Suicidal behaviour 96.29 18.24 38 25117 1324 29925999
Physical assault 93.38 18.24 36 25119 1177 29926146
Toxicity to various agents 93.13 18.24 18 25137 177165 29750158
Panic attack 91.20 18.24 68 25087 8613 29918710
Sleep disorder 88.56 18.24 106 25049 24373 29902950
Mental disorder 88.00 18.24 80 25075 13369 29913954
Psychotic disorder 87.59 18.24 99 25056 21416 29905907
Crying 87.39 18.24 56 25099 5553 29921770
Mania 85.82 18.24 67 25088 9087 29918236
Drug hypersensitivity 85.42 18.24 182 24973 68337 29858986
Memory impairment 82.60 18.24 127 25028 37047 29890276
Anaemia 82.20 18.24 36 25119 207956 29719367
Hostility 81.24 18.24 30 25125 869 29926454
Sepsis 80.98 18.24 13 25142 146382 29780941
Impaired driving ability 79.74 18.24 40 25115 2478 29924845
Affective disorder 77.33 18.24 42 25113 3066 29924257
Apathy 77.31 18.24 54 25101 6178 29921145
Neutropenia 74.35 18.24 10 25145 128530 29798793
Thrombocytopenia 71.80 18.24 14 25141 137030 29790293
Alcohol use 67.35 18.24 41 25114 3714 29923609
Hypotension 64.35 18.24 45 25110 200520 29726803
Febrile neutropenia 62.41 18.24 8 25147 106685 29820638
Bipolar disorder 62.07 18.24 39 25116 3737 29923586
Impaired work ability 61.06 18.24 45 25110 5598 29921725
Negative thoughts 58.56 18.24 22 25133 669 29926654
Tearfulness 58.45 18.24 28 25127 1568 29925755
Self-injurious ideation 58.24 18.24 28 25127 1581 29925742
Verbal abuse 57.64 18.24 16 25139 177 29927146
Platelet count decreased 57.38 18.24 10 25145 106119 29821204
Pancytopenia 55.99 18.24 4 25151 85048 29842275
White blood cell count decreased 55.11 18.24 4 25151 83943 29843380
Headache 53.98 18.24 298 24857 182008 29745315
Morbid thoughts 52.87 18.24 16 25139 245 29927078
Flatulence 52.07 18.24 70 25085 18059 29909264
Stress 51.93 18.24 74 25081 20161 29907162
Dizziness 51.44 18.24 309 24846 194600 29732723
Renal failure 49.82 18.24 23 25132 128943 29798380
General physical health deterioration 48.70 18.24 12 25143 99932 29827391
Somnambulism 47.39 18.24 31 25124 3183 29924140
Social avoidant behaviour 45.63 18.24 29 25126 2834 29924489
Haemoglobin decreased 44.60 18.24 20 25135 114078 29813245
Product use in unapproved indication 44.37 18.24 5 25150 73688 29853635
Dysgeusia 43.26 18.24 76 25079 24725 29902598
Blood creatinine increased 42.56 18.24 12 25143 91363 29835960
Septic shock 41.83 18.24 3 25152 63604 29863719
Multiple organ dysfunction syndrome 41.74 18.24 3 25152 63484 29863839
Road traffic accident 41.71 18.24 61 25094 17010 29910313
Post-traumatic stress disorder 40.66 18.24 22 25133 1593 29925730
Respiratory failure 40.35 18.24 17 25138 100625 29826698
Tobacco withdrawal symptoms 40.09 18.24 7 25148 3 29927320
Disease progression 40.07 18.24 9 25146 79865 29847458
Intentional self-injury 40.01 18.24 53 25102 13479 29913844
Frustration tolerance decreased 39.20 18.24 23 25132 1947 29925376
Major depression 38.91 18.24 30 25125 3992 29923331
Screaming 38.81 18.24 20 25135 1311 29926012
Palpitations 38.17 18.24 86 25069 33487 29893836
Loss of personal independence in daily activities 37.57 18.24 66 25089 21469 29905854
Alcohol interaction 36.93 18.24 25 25130 2717 29924606
Leukopenia 35.94 18.24 3 25152 56156 29871167
Cardiac failure 35.23 18.24 13 25142 83405 29843918
Panic reaction 34.76 18.24 19 25136 1404 29925919
Interstitial lung disease 34.03 18.24 5 25150 60192 29867131
Withdrawal syndrome 33.16 18.24 44 25111 11206 29916117
Dissociation 32.91 18.24 17 25138 1120 29926203
Pleural effusion 32.20 18.24 11 25144 74055 29853268
Abdominal discomfort 31.16 18.24 101 25054 48690 29878633
Disorientation 30.84 18.24 76 25079 31342 29895981
Personality disorder 29.82 18.24 16 25139 1139 29926184
Decreased interest 29.53 18.24 20 25135 2175 29925148
Feeling jittery 29.39 18.24 25 25130 3823 29923500
Dehydration 28.69 18.24 37 25118 123502 29803821
Hyperkalaemia 28.35 18.24 10 25145 66000 29861323
Restlessness 28.07 18.24 60 25095 22539 29904784
Cardio-respiratory arrest 27.67 18.24 7 25148 57299 29870024
Libido decreased 27.61 18.24 26 25129 4540 29922783
Anti-cyclic citrullinated peptide antibody positive 27.19 18.24 13 25142 725 29926598
Nicotine dependence 27.16 18.24 10 25145 287 29927036
Urinary tract infection 27.11 18.24 14 25141 73645 29853678
Depressive symptom 27.06 18.24 17 25138 1628 29925695
Infection 27.05 18.24 16 25139 78058 29849265
Renal impairment 26.79 18.24 19 25136 84165 29843158
Hypokalaemia 26.52 18.24 5 25150 50187 29877136
Bradycardia 26.36 18.24 11 25144 65515 29861808
Drug withdrawal syndrome 26.24 18.24 54 25101 19755 29907568
Diarrhoea 26.16 18.24 169 24986 333934 29593389
C-reactive protein increased 26.04 18.24 3 25152 43470 29883853
Psychiatric symptom 25.90 18.24 22 25133 3357 29923966
Depression suicidal 25.66 18.24 15 25140 1261 29926062
Cardiac failure congestive 25.63 18.24 20 25135 84387 29842936
Drug abuse 25.49 18.24 19 25136 82053 29845270
Loss of employment 25.20 18.24 11 25144 496 29926827
Plasma cell myeloma 24.92 18.24 7 25148 53455 29873868
Blood carbon monoxide increased 24.33 18.24 4 25151 0 29927323
Hospitalisation 24.32 18.24 4 25151 44315 29883008
Loss of consciousness 24.24 18.24 131 25024 79244 29848079
Drug screen false positive 24.17 18.24 12 25143 727 29926596
Sleep terror 24.11 18.24 12 25143 731 29926592
Cellulitis 24.01 18.24 5 25150 46779 29880544
Poor quality sleep 23.97 18.24 30 25125 7211 29920112
Tinnitus 23.89 18.24 46 25109 16042 29911281
Pharyngeal oedema 23.35 18.24 28 25127 6443 29920880
Mental impairment 22.44 18.24 33 25122 9244 29918079
Erectile dysfunction 22.41 18.24 48 25107 18054 29909269
Hypomania 22.20 18.24 17 25138 2239 29925084
Hypoglycaemia 21.42 18.24 8 25147 50973 29876350
Gun shot wound 21.27 18.24 13 25142 1185 29926138
Marital problem 21.25 18.24 6 25149 71 29927252
Confusional state 21.17 18.24 189 24966 134645 29792678
Hallucination, auditory 21.10 18.24 33 25122 9756 29917567
Somnolence 20.89 18.24 146 25009 96617 29830706
Peripheral swelling 20.48 18.24 13 25142 61061 29866262
Ascites 20.26 18.24 3 25152 35918 29891405
Fear 19.95 18.24 34 25121 10791 29916532
Atrial fibrillation 19.76 18.24 38 25117 108086 29819237
Oxygen saturation decreased 19.67 18.24 6 25149 43434 29883889
Narcolepsy 19.65 18.24 9 25146 455 29926868
Imprisonment 19.04 18.24 9 25146 489 29926834
Feeding disorder 18.92 18.24 24 25131 5847 29921476
Feeling of despair 18.77 18.24 11 25144 929 29926394
Vision blurred 18.61 18.24 77 25078 41739 29885584
Flight of ideas 18.57 18.24 8 25147 349 29926974
Adjustment disorder with mixed anxiety and depressed mood 18.25 18.24 3 25152 0 29927323
Spousal abuse 18.25 18.24 3 25152 0 29927323
Cough 18.24 18.24 50 25105 125592 29801731

Pharmacologic Action:

SourceCodeDescription
ATC N07BA03 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
DRUGS USED IN ADDICTIVE DISORDERS
Drugs used in nicotine dependence
FDA MoA N0000175702 Partial Cholinergic Nicotinic Agonists
FDA EPC N0000175705 Partial Cholinergic Nicotinic Agonist
MeSH PA D018678 Cholinergic Agents
MeSH PA D018679 Cholinergic Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018722 Nicotinic Agonists
MeSH PA D000077444 Smoking Cessation Agents
CHEBI has role CHEBI:35941 serotonergic agonists
CHEBI has role CHEBI:47958 muscarinic agonists

Drug Use (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

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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.5MG BASE CHANTIX PF PRISM CV N021928 May 10, 2006 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO LABELING TO DESCRIBE A STUDY TO EVALUATE THE SAFETY AND EFFICACY OF VARENICLINE FOR SMOKING CESSATION IN ADOLESCENT SMOKERS
EQ 1MG BASE CHANTIX PF PRISM CV N021928 May 10, 2006 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO LABELING TO DESCRIBE A STUDY TO EVALUATE THE SAFETY AND EFFICACY OF VARENICLINE FOR SMOKING CESSATION IN ADOLESCENT SMOKERS
EQ 0.5MG BASE CHANTIX PF PRISM CV N021928 May 10, 2006 RX TABLET ORAL Aug. 22, 2022 PEDIATRIC EXCLUSIVITY
EQ 1MG BASE CHANTIX PF PRISM CV N021928 May 10, 2006 RX TABLET ORAL Aug. 22, 2022 PEDIATRIC EXCLUSIVITY

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 subunit alpha-7 Ion channel Ki 6.90 CHEMBL
Acetylcholine receptor; alpha1/beta1/delta/gamma Ion channel Ki 5.09 CHEMBL
Neuronal acetylcholine receptor; alpha3/beta4 Ion channel Ki 7.07 WOMBAT-PK
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel Ki 6.96 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; alpha2/beta2 Ion channel Ki 9.66 CHEMBL
Neuronal acetylcholine receptor; alpha2/beta4 Ion channel Ki 7.15 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel Ki 7.82 CHEMBL
Neuronal acetylcholine receptor subunit alpha-7 Ion channel Ki 7.49 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel Ki 10.30 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
C1956439 UMLSCUI
CHEBI:84507 CHEBI
QMR PDB_CHEM_ID
CHEMBL2062259 ChEMBL_ID
CHEMBL1396 ChEMBL_ID
D000068580 MESH_DESCRIPTOR_UI
6918678 PUBCHEM_CID
8366 INN_ID
DB01273 DRUGBANK_ID
W6HS99O8ZO UNII
5459 IUPHAR_LIGAND_ID
591622 RXNORM
21404 MMSL
82173 MMSL
d05807 MMSL
011508 NDDF
011509 NDDF
420507002 SNOMEDCT_US
421772003 SNOMEDCT_US
428382005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 0069-0468 TABLET, FILM COATED 0.50 mg ORAL NDA 30 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 0069-0469 TABLET, FILM COATED 1 mg ORAL NDA 30 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
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 43353-899 TABLET, FILM COATED 1 mg ORAL NDA 30 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 50090-0995 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 50090-0995 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 50090-4481 TABLET, FILM COATED 0.50 mg ORAL NDA 30 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 50090-4482 TABLET, FILM COATED 1 mg ORAL NDA 30 sections
Chantix HUMAN PRESCRIPTION DRUG LABEL 1 54868-5674 TABLET, FILM COATED 1 mg ORAL NDA 31 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 68151-4952 TABLET, FILM COATED 1 mg ORAL NDA 31 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 68151-4953 TABLET, FILM COATED 0.50 mg ORAL NDA 31 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 69189-0492 TABLET, FILM COATED 0.50 mg ORAL NDA 30 sections
CHANTIX HUMAN PRESCRIPTION DRUG LABEL 1 71205-381 TABLET, FILM COATED 1 mg ORAL NDA 30 sections