Details of the Drug

General Information of Drug (ID: DMH61ZB)

Drug Name
Cimetidine
Synonyms
Acibilin; Acinil; Altramet; Brumetidina; Cimal; Cimetadine; Cimetag; Cimetidina; Cimetidinum; Cimetum; Dyspamet; Edalene; Eureceptor; Evicer; Gastrobitan; Gastromet; Histodil; Magicul; Metracin; Peptol; Sigmetadine; Tagamet; Tametin; Tratul; Ulcedin; Ulcedine; Ulcestop; Ulcimet; Ulcofalk; Ulcomedina; Ulcomet; Ulhys; Valmagen; Venopex; Ci metum; Cimetidine Hcl; Tagamet Hb; Biomet400; C 4522; FPF 1002; SKF 92334; Tagamet Hb 200; CIMETIDINE A/AB; Cimetidina [INN-Spanish]; Cimetidinum [INN-Latin]; DRG-0150; SKF-92334; Tagamet (TN); Tagamet HB (TN); Tagamet HB200 (TN); SK&F-92334; Cimetidine (JP15/USP/INN); Cimetidine [USAN:INN:BAN:JAN]; Tagamet, SKF-92334, Tratul, Tametin, Dyspamet, Acinil, Cimetidine; N-Cyano-N'-methyl-[2-[[[5-methyl-1H-imidazol-4-yl]methyl]thio]ethyl]guanidine; N''-Cyano-N-methyl-N'-[2-[(5-methyl-1H-imidazol-4-yl)methylthio]ethyl]guanidine; N''-cyano-N-methyl-N'-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine; N-cyano-N'-methyl-N''-(2-([(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl)ethyl)guanidine; N-cyano-N'-methyl-N''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine; N-Cyano-N'-Methyl-N''-(2-(((5-Methyl-1H-Imidazol-4-YL)Methyl)Thio)Ethyl) Guanidine; N-Cyano-N'-methyl-N''-(2-(((5-methyl-1 H-imidazol-4-yl) methyl)thio)ethyl)guanidine; N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)guanidine; N''-cyano-N-methyl-N'-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)-ethyl)guanidine; 1-Cyano-2-methyl-3-(2-(((5-methyl-4-imidazolyl)methyl)thio)ethyl)guanidine; 1-Cyano-2-methyl-3-[2-[[(5-methylimidazol-4-yl)methyl]thio]ethyl]guanidine; 1-cyano-2-methyl-3-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine; 2-Cyano-1-methyl-3-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)guanidine; 2-Cyano-1-methyl-3-[2-(5-methyl-1H-imidazol-4-yl-methylthio)ethyl]guanidine; 2-cyano-1-methyl-3-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine; 2-cyano-1-methyl-3-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine
Indication
Disease Entry ICD 11 Status REF
Acid-reflux disorder DA22 Approved [1], [2]
Therapeutic Class
Antiulcer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 252.34
Topological Polar Surface Area (xlogp) 0.4
Rotatable Bond Count (rotbonds) 7
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 6-12 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
Bioavailability
The bioavailability of drug is 64-90% [3]
Clearance
The sytemic clearance of drug is 500-600 mL/min [5]
Elimination
62% of drug is excreted from urine in the unchanged form [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 2 hours [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 158.51427 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.78% [8]
Vd
The volume of distribution (Vd) of drug is 1 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 6.2 mg/mL [4]
Chemical Identifiers
Formula
C10H16N6S
IUPAC Name
1-cyano-2-methyl-3-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
Canonical SMILES
CC1=C(N=CN1)CSCCNC(=NC)NC#N
InChI
InChI=1S/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)
InChIKey
AQIXAKUUQRKLND-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
2756
ChEBI ID
CHEBI:3699
CAS Number
51481-61-9
DrugBank ID
DB00501
TTD ID
D02DPA
VARIDT ID
DR00037
INTEDE ID
DR2272
ACDINA ID
D00130

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H2 receptor (H2R) TTQHJ1K HRH2_HUMAN Antagonist [9], [10], [11]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [12]
Multidrug and toxin extrusion protein 2 (SLC47A2) DT3TX4H S47A2_HUMAN Substrate [13]
Multidrug and toxin extrusion protein 1 (SLC47A1) DTZGT0P S47A1_HUMAN Substrate [13]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [14]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Substrate [15]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [16]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [17]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Cimetidine
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Cisapride DMY7PED Major Decreased metabolism of Cimetidine caused by Cisapride mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [74]
Coadministration of a Drug Treating the Disease Different from Cimetidine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Sodium bicarbonate. Acidosis [5C73] [75]
Cefuroxime DMSIMD8 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Cefuroxime. Acute bronchitis [CA42] [76]
Repaglinide DM5SXUV Moderate Decreased metabolism of Cimetidine caused by Repaglinide mediated inhibition of CYP450 enzyme. Acute diabete complication [5A2Y] [77]
Glibenclamide DM8JXPZ Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Glibenclamide. Acute diabete complication [5A2Y] [78]
Tolazamide DMIHRNA Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Tolazamide. Acute diabete complication [5A2Y] [78]
Glipizide DMZA5PQ Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Glipizide. Acute diabete complication [5A2Y] [78]
Midostaurin DMI6E0R Moderate Decreased metabolism of Cimetidine caused by Midostaurin mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [79]
Gilteritinib DMWQ4MZ Moderate Decreased metabolism of Cimetidine caused by Gilteritinib mediated inhibition of CYP450 enzyme. Acute myeloid leukaemia [2A60] [80]
Galantamine DMEO794 Moderate Antagonize the effect of Cimetidine when combined with Galantamine. Alzheimer disease [8A20] [81]
Rivastigmine DMG629M Moderate Antagonize the effect of Cimetidine when combined with Rivastigmine. Alzheimer disease [8A20] [81]
Donepezil DMIYG7Z Moderate Antagonize the effect of Cimetidine when combined with Donepezil. Alzheimer disease [8A20] [81]
Metronidazole DMTIVEN Minor Decreased metabolism of Cimetidine caused by Metronidazole mediated inhibition of CYP450 enzyme. Amoebiasis [1A36] [82]
Ivabradine DM0L594 Moderate Decreased metabolism of Cimetidine caused by Ivabradine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [80]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Cimetidine caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [83]
Nifedipine DMSVOZT Moderate Decreased metabolism of Cimetidine caused by Nifedipine mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [84]
Clorazepate DMC3JST Moderate Decreased metabolism of Cimetidine caused by Clorazepate mediated inhibition of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [85]
Methylphenobarbital DMDSWAG Minor Altered absorption of Cimetidine caused by Methylphenobarbital. Anxiety disorder [6B00-6B0Z] [86]
Hydroxyzine DMF8Y74 Minor Decreased metabolism of Cimetidine caused by Hydroxyzine mediated inhibition of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [87]
Halazepam DMPFWO6 Moderate Decreased metabolism of Cimetidine caused by Halazepam mediated inhibition of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [88]
Cilostazol DMZMSCT Moderate Decreased metabolism of Cimetidine caused by Cilostazol mediated inhibition of CYP450 enzyme. Arterial occlusive disease [BD40] [89]
Aminophylline DML2NIB Moderate Decreased metabolism of Cimetidine caused by Aminophylline mediated inhibition of CYP450 enzyme. Asthma [CA23] [90]
Roflumilast DMPGHY8 Moderate Decreased metabolism of Cimetidine caused by Roflumilast mediated inhibition of CYP450 enzyme. Asthma [CA23] [80]
Desipramine DMT2FDC Moderate Decreased metabolism of Cimetidine caused by Desipramine mediated inhibition of CYP450 enzyme. Attention deficit hyperactivity disorder [6A05] [91]
Tindamax DM3OWT4 Minor Decreased metabolism of Cimetidine caused by Tindamax mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [82]
Cefpodoxime DMJUNY5 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Cefpodoxime. Bacterial infection [1A00-1C4Z] [76]
Bacampicillin DMP54C7 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Bacampicillin. Bacterial infection [1A00-1C4Z] [76]
Cefditoren DMSUVM1 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Cefditoren. Bacterial infection [1A00-1C4Z] [92]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Cimetidine caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [93]
Vismodegib DM5IXKQ Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Vismodegib. Basal cell carcinoma [2C32] [93]
Pexidartinib DMS2J0Z Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [94]
Loperamide DMOJZQ9 Major Decreased clearance of Cimetidine due to the transporter inhibition by Loperamide. Bowel habit change [ME05] [95]
Ixabepilone DM2OZ3G Moderate Decreased metabolism of Cimetidine caused by Ixabepilone mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [96]
Lapatinib DM3BH1Y Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Lapatinib. Breast cancer [2C60-2C6Y] [80]
HKI-272 DM6QOVN Major Decreased absorption of Cimetidine due to altered gastric pH caused by HKI-272. Breast cancer [2C60-2C6Y] [93]
Esterified estrogens DM9KZDO Minor Decreased metabolism of Cimetidine caused by Esterified estrogens. Breast cancer [2C60-2C6Y] [97]
Palbociclib DMD7L94 Moderate Decreased metabolism of Cimetidine caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [80]
Quinestrol DMJ6H1Z Minor Decreased metabolism of Cimetidine caused by Quinestrol. Breast cancer [2C60-2C6Y] [97]
Tamoxifen DMLB0EZ Major Decreased metabolism of Cimetidine caused by Tamoxifen mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [98]
Toremifene DMQYUWG Moderate Decreased metabolism of Cimetidine caused by Toremifene mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [99]
Bosutinib DMTI8YE Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Bosutinib. Breast cancer [2C60-2C6Y] [80]
Estradiol DMUNTE3 Minor Decreased metabolism of Cimetidine caused by Estradiol. Breast cancer [2C60-2C6Y] [97]
Moricizine DMOMBJW Moderate Decreased metabolism of Cimetidine caused by Moricizine mediated inhibition of CYP450 enzyme. Cardiac arrhythmia [BC9Z] [100]
Atorvastatin DMF28YC Moderate Decreased metabolism of Cimetidine caused by Atorvastatin mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [101]
Macitentan DMP79A1 Moderate Decreased metabolism of Cimetidine caused by Macitentan mediated inhibition of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [102]
PF-04449913 DMSB068 Moderate Decreased metabolism of Cimetidine caused by PF-04449913 mediated inhibition of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [103]
Anisindione DM2C48U Moderate Decreased metabolism of Cimetidine caused by Anisindione mediated inhibition of CYP450 enzyme. Coagulation defect [3B10] [104]
Irinotecan DMP6SC2 Moderate Decreased metabolism of Cimetidine caused by Irinotecan mediated inhibition of CYP450 enzyme. Colorectal cancer [2B91] [105]
Mestranol DMG3F94 Minor Decreased metabolism of Cimetidine caused by Mestranol. Contraceptive management [QA21] [97]
Levobupivacaine DM783CH Moderate Decreased metabolism of Cimetidine caused by Levobupivacaine mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [80]
Thiopental DMGP8AX Minor Altered absorption of Cimetidine caused by Thiopental. Corneal disease [9A76-9A78] [86]
Alfentanil DMVO0UB Moderate Decreased metabolism of Cimetidine caused by Alfentanil mediated inhibition of CYP450 enzyme. Corneal disease [9A76-9A78] [106]
Oxtriphylline DMLHSE3 Moderate Decreased metabolism of Cimetidine caused by Oxtriphylline mediated inhibition of CYP450 enzyme. Cough [MD12] [90]
Dextromethorphan DMUDJZM Moderate Decreased metabolism of Cimetidine caused by Dextromethorphan mediated inhibition of CYP450 enzyme. Cough [MD12] [93]
Mifepristone DMGZQEF Moderate Decreased metabolism of Cimetidine caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [107]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Cimetidine caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [80]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Cimetidine caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [108]
Ethanol DMDRQZU Minor Decreased metabolism of Cimetidine caused by Ethanol mediated inhibition of non-CYP450 enzyme. Cystitis [GC00] [109]
Rivaroxaban DMQMBZ1 Moderate Decreased metabolism of Cimetidine caused by Rivaroxaban mediated inhibition of CYP450 enzyme. Deep vein thrombosis [BD71] [110]
Nortriptyline DM4KDYJ Moderate Decreased metabolism of Cimetidine caused by Nortriptyline mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [91]
Paroxetine DM5PVQE Moderate Decreased metabolism of Cimetidine caused by Paroxetine. Depression [6A70-6A7Z] [111]
Escitalopram DMFK9HG Moderate Decreased metabolism of Cimetidine caused by Escitalopram mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [105]
Desvenlafaxine DMHD4PE Minor Decreased metabolism of Cimetidine caused by Desvenlafaxine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [112]
OPC-34712 DMHG57U Major Decreased metabolism of Cimetidine caused by OPC-34712 mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [113]
Clomipramine DMINRKW Moderate Decreased metabolism of Cimetidine caused by Clomipramine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [91]
Amoxapine DMKITQE Moderate Decreased metabolism of Cimetidine caused by Amoxapine mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [91]
Doxepin DMPI98T Moderate Decreased metabolism of Cimetidine caused by Doxepin mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [91]
Polatuzumab vedotin DMF6Y0L Moderate Decreased metabolism of Cimetidine caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme. Diffuse large B-cell lymphoma [2A81] [114]
[3H]estrone-3-sulphate DMGPF0N Minor Decreased metabolism of Cimetidine caused by [3H]estrone-3-sulphate. Discovery agent [N.A.] [97]
PMID28870136-Compound-49 DMTUC9E Moderate Decreased metabolism of Cimetidine caused by PMID28870136-Compound-49 mediated inhibition of CYP450 enzyme. Discovery agent [N.A.] [115]
Diazepam DM08E9O Moderate Decreased metabolism of Cimetidine caused by Diazepam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [88]
Zonisamide DM0DTF7 Moderate Decreased metabolism of Cimetidine caused by Zonisamide mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [116]
Primidone DM0WX6I Minor Altered absorption of Cimetidine caused by Primidone. Epilepsy/seizure [8A61-8A6Z] [86]
Stiripentol DMMSDOY Moderate Decreased metabolism of Cimetidine caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [80]
Fosphenytoin DMOX3LB Major Decreased metabolism of Cimetidine caused by Fosphenytoin mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [117]
Clonazepam DMTO13J Moderate Decreased metabolism of Cimetidine caused by Clonazepam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [88]
Phenobarbital DMXZOCG Minor Altered absorption of Cimetidine caused by Phenobarbital. Epilepsy/seizure [8A61-8A6Z] [86]
Carbamazepine DMZOLBI Moderate Decreased metabolism of Cimetidine caused by Carbamazepine mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [118]
Nicardipine DMCDYW7 Moderate Decreased metabolism of Cimetidine caused by Nicardipine mediated inhibition of CYP450 enzyme. Essential hypertension [BA00] [84]
Nadolol DMW6GVL Moderate Decreased metabolism of Cimetidine caused by Nadolol mediated inhibition of CYP450 enzyme. Essential hypertension [BA00] [119]
Tazemetostat DMWP1BH Moderate Decreased metabolism of Cimetidine caused by Tazemetostat mediated inhibition of CYP450 enzyme. Follicular lymphoma [2A80] [120]
Solifenacin DMG592Q Moderate Decreased metabolism of Cimetidine caused by Solifenacin mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [121]
Mirabegron DMS1GYT Minor Decreased metabolism of Cimetidine caused by Mirabegron mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [122]
Tolterodine DMSHPW8 Moderate Decreased metabolism of Cimetidine caused by Tolterodine mediated inhibition of CYP450 enzyme. Functional bladder disorder [GC50] [123]
Itraconazole DMCR1MV Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Itraconazole. Fungal infection [1F29-1F2F] [124]
Terbinafine DMI6HUW Minor Decreased metabolism of Cimetidine caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [125]
Ketoconazole DMPZI3Q Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Ketoconazole. Fungal infection [1F29-1F2F] [126]
Ripretinib DM958QB Moderate Decreased metabolism of Cimetidine caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [93]
Avapritinib DMK2GZX Moderate Decreased metabolism of Cimetidine caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [80]
Carteolol DMFMDOB Moderate Decreased metabolism of Cimetidine caused by Carteolol mediated inhibition of CYP450 enzyme. Glaucoma [9C61] [119]
Colchicine DM2POTE Moderate Decreased metabolism of Cimetidine caused by Colchicine mediated inhibition of CYP450 enzyme. Gout [FA25] [127]
Ergotamine DMKR3C5 Moderate Decreased metabolism of Cimetidine caused by Ergotamine mediated inhibition of CYP450 enzyme. Headache [8A80-8A84] [128]
Carvedilol DMHTEAO Moderate Decreased metabolism of Cimetidine caused by Carvedilol mediated inhibition of CYP450 enzyme. Heart failure [BD10-BD1Z] [119]
MK-1439 DM215WE Minor Decreased metabolism of Cimetidine caused by MK-1439 mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [129]
Delavirdine DM3NF5G Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Delavirdine. Human immunodeficiency virus disease [1C60-1C62] [130]
Fosamprenavir DM4W9B3 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Fosamprenavir. Human immunodeficiency virus disease [1C60-1C62] [131]
Dolutegravir DMCZGRE Minor Decreased metabolism of Cimetidine caused by Dolutegravir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [132]
Etravirine DMGV8QU Moderate Decreased metabolism of Cimetidine caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [133]
Lopinavir DMITQS0 Minor Decreased metabolism of Cimetidine caused by Lopinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [80]
Rilpivirine DMJ0QOW Major Decreased absorption of Cimetidine due to altered gastric pH caused by Rilpivirine. Human immunodeficiency virus disease [1C60-1C62] [134]
Amprenavir DMLMXE0 Minor Decreased metabolism of Cimetidine caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [135]
Atazanavir DMSYRBX Major Decreased absorption of Cimetidine due to altered gastric pH caused by Atazanavir. Human immunodeficiency virus disease [1C60-1C62] [80]
Maraviroc DMTL94F Moderate Decreased clearance of Cimetidine due to the transporter inhibition by Maraviroc. Human immunodeficiency virus disease [1C60-1C62] [136]
Raltegravir DMYURI6 Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Raltegravir. Human immunodeficiency virus disease [1C60-1C62] [137]
Simvastatin DM30SGU Moderate Decreased metabolism of Cimetidine caused by Simvastatin mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [101]
BMS-201038 DMQTAGO Moderate Decreased metabolism of Cimetidine caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [138]
Acebutolol DM0TI4U Moderate Decreased metabolism of Cimetidine caused by Acebutolol mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [119]
Bisoprolol DM3UZ95 Moderate Decreased metabolism of Cimetidine caused by Bisoprolol mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [119]
Penbutolol DM4ES8F Moderate Decreased metabolism of Cimetidine caused by Penbutolol mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [119]
Verapamil DMA7PEW Moderate Decreased metabolism of Cimetidine caused by Verapamil mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [84]
Pindolol DMD2NV7 Moderate Decreased metabolism of Cimetidine caused by Pindolol mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [119]
Labetalol DMK8U72 Moderate Decreased metabolism of Cimetidine caused by Labetalol mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [119]
Felodipine DMOSW35 Moderate Decreased metabolism of Cimetidine caused by Felodipine mediated inhibition of CYP450 enzyme. Hypertension [BA00-BA04] [84]
Pirfenidone DM6VZFQ Moderate Decreased metabolism of Cimetidine caused by Pirfenidone mediated inhibition of CYP450 enzyme. Idiopathic interstitial pneumonitis [CB03] [80]
Retapamulin DM9JXB7 Minor Decreased metabolism of Cimetidine caused by Retapamulin mediated inhibition of CYP450 enzyme. Impetigo [1B72] [139]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Cimetidine caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [93]
Amobarbital DM0GQ8N Minor Altered absorption of Cimetidine caused by Amobarbital. Insomnia [7A00-7A0Z] [86]
Ramelteon DM7IW9J Moderate Decreased metabolism of Cimetidine caused by Ramelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [140]
Flurazepam DMAL4G0 Moderate Decreased metabolism of Cimetidine caused by Flurazepam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [88]
Triazolam DMETYK5 Moderate Decreased metabolism of Cimetidine caused by Triazolam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [88]
Zaleplon DMGFWSM Moderate Decreased metabolism of Cimetidine caused by Zaleplon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [141]
Melatonin DMKWFBT Minor Decreased metabolism of Cimetidine caused by Melatonin mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [93]
Tasimelteon DMLOQ1V Moderate Decreased metabolism of Cimetidine caused by Tasimelteon mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [142]
ITI-007 DMUQ1DO Moderate Decreased metabolism of Cimetidine caused by ITI-007 mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [143]
Quazepam DMY4D87 Moderate Decreased metabolism of Cimetidine caused by Quazepam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [88]
Estazolam DMZGXUM Moderate Decreased metabolism of Cimetidine caused by Estazolam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [88]
Iron DMAP8MV Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Iron. Iron deficiency anaemia [3A00] [144]
Alosetron DML2A03 Moderate Decreased metabolism of Cimetidine caused by Alosetron mediated inhibition of CYP450 enzyme. Irritable bowel syndrome [DD91] [145]
Naloxegol DML0B41 Minor Decreased metabolism of Cimetidine caused by Naloxegol mediated inhibition of CYP450 enzyme. Large intestine motility disorder [DB32] [146]
Physostigmine DM2N0TO Moderate Antagonize the effect of Cimetidine when combined with Physostigmine. Lips/oral mucosa miscellaneous disorder [DA02] [81]
Pemigatinib DM819JF Moderate Decreased metabolism of Cimetidine caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [80]
Ceritinib DMB920Z Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Ceritinib. Lung cancer [2C25] [147]
Erlotinib DMCMBHA Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Erlotinib. Lung cancer [2C25] [93]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Cimetidine caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [148]
PF-06463922 DMKM7EW Moderate Decreased metabolism of Cimetidine caused by PF-06463922 mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [149]
Dacomitinib DMOH8VY Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Dacomitinib. Lung cancer [2C25] [80]
Osimertinib DMRJLAT Moderate Decreased metabolism of Cimetidine caused by Osimertinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [150]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Cimetidine caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [151]
Selpercatinib DMZR15V Major Decreased absorption of Cimetidine due to altered gastric pH caused by Selpercatinib. Lung cancer [2C25] [80]
Halofantrine DMOMK1V Major Decreased metabolism of Cimetidine caused by Halofantrine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [152]
Chloroquine DMSI5CB Moderate Decreased metabolism of Cimetidine caused by Chloroquine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [80]
Hydroxychloroquine DMSIVND Moderate Decreased metabolism of Cimetidine caused by Hydroxychloroquine mediated inhibition of CYP450 enzyme. Malaria [1F40-1F45] [80]
GDC-0199 DMH0QKA Moderate Decreased metabolism of Cimetidine caused by GDC-0199 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [93]
IPI-145 DMWA24P Moderate Decreased metabolism of Cimetidine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [153]
Ibrutinib DMHZCPO Moderate Decreased metabolism of Cimetidine caused by Ibrutinib mediated inhibition of CYP450 enzyme. Mature B-cell lymphoma [2A85] [154]
Ponatinib DMYGJQO Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Ponatinib. Mature B-cell lymphoma [2A85] [93]
Selumetinib DMC7W6R Moderate Decreased metabolism of Cimetidine caused by Selumetinib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [155]
Dabrafenib DMX6OE3 Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Dabrafenib. Melanoma [2C30] [93]
Estrone DM5T6US Minor Decreased metabolism of Cimetidine caused by Estrone. Menopausal disorder [GA30] [97]
Dienestrol DMBSXI0 Minor Decreased metabolism of Cimetidine caused by Dienestrol. Menopausal disorder [GA30] [97]
Ethinyl estradiol DMODJ40 Minor Decreased metabolism of Cimetidine caused by Ethinyl estradiol. Menopausal disorder [GA30] [97]
Ubrogepant DM749I3 Moderate Decreased metabolism of Cimetidine caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [156]
Propranolol DM79NTF Moderate Decreased metabolism of Cimetidine caused by Propranolol mediated inhibition of CYP450 enzyme. Migraine [8A80] [119]
Flibanserin DM70DTN Moderate Decreased metabolism of Cimetidine caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [157]
Midazolam DMXOELT Moderate Decreased metabolism of Cimetidine caused by Midazolam mediated inhibition of CYP450 enzyme. Mood/affect symptom [MB24] [88]
Panobinostat DM58WKG Moderate Decreased metabolism of Cimetidine caused by Panobinostat mediated inhibition of CYP450 enzyme. Multiple myeloma [2A83] [158]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Cimetidine and Thalidomide. Multiple myeloma [2A83] [93]
Siponimod DM2R86O Major Increased risk of atrioventricular block by the combination of Cimetidine and Siponimod. Multiple sclerosis [8A40] [93]
Fingolimod DM5JVAN Moderate Increased risk of bradycardia by the combination of Cimetidine and Fingolimod. Multiple sclerosis [8A40] [159]
Ozanimod DMT6AM2 Moderate Increased risk of atrioventricular block by the combination of Cimetidine and Ozanimod. Multiple sclerosis [8A40] [160]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Cimetidine caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [80]
Nilotinib DM7HXWT Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Nilotinib. Myeloproliferative neoplasm [2A20] [93]
Ruxolitinib DM7Q98D Minor Decreased metabolism of Cimetidine caused by Ruxolitinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [80]
Imatinib DM7RJXL Moderate Decreased metabolism of Cimetidine caused by Imatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [161]
Dasatinib DMJV2EK Major Decreased absorption of Cimetidine due to altered gastric pH caused by Dasatinib. Myeloproliferative neoplasm [2A20] [162]
Prasugrel DM7MT6E Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Prasugrel. Myocardial infarction [BA41-BA43] [163]
Modafinil DMYILBE Minor Decreased metabolism of Cimetidine caused by Modafinil mediated inhibition of CYP450 enzyme. Narcolepsy [7A20] [93]
Dolasetron DMMG26Z Minor Decreased metabolism of Cimetidine caused by Dolasetron mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [164]
Entrectinib DMMPTLH Moderate Decreased metabolism of Cimetidine caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [165]
Sibutramine DMFJTDI Minor Decreased metabolism of Cimetidine caused by Sibutramine mediated inhibition of CYP450 enzyme. Obesity [5B80-5B81] [166]
Levomethadyl Acetate DM06HG5 Major Decreased metabolism of Cimetidine caused by Levomethadyl Acetate mediated inhibition of CYP450 enzyme. Opioid use disorder [6C43] [167]
Valdecoxib DMAY7H4 Moderate Decreased metabolism of Cimetidine caused by Valdecoxib mediated inhibition of CYP450 enzyme. Osteoarthritis [FA00-FA05] [168]
Olaparib DM8QB1D Moderate Decreased metabolism of Cimetidine caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [169]
Buprenorphine DMPRI8G Moderate Decreased metabolism of Cimetidine caused by Buprenorphine mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [170]
Hydrocodone DMQ2JO5 Major Decreased metabolism of Cimetidine caused by Hydrocodone mediated inhibition of CYP450 enzyme. Pain [MG30-MG3Z] [171]
Mebendazole DMO14SG Minor Decreased metabolism of Cimetidine caused by Mebendazole mediated inhibition of CYP450 enzyme. Parasitic worm infestation [1F90] [172]
Istradefylline DM20VSK Moderate Decreased metabolism of Cimetidine caused by Istradefylline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [173]
Rasagiline DM3WKQ4 Moderate Decreased metabolism of Cimetidine caused by Rasagiline mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [93]
Pimavanserin DMR7IVC Moderate Decreased metabolism of Cimetidine caused by Pimavanserin mediated inhibition of CYP450 enzyme. Parkinsonism [8A00] [174]
Lefamulin DME6G97 Moderate Decreased clearance of Cimetidine due to the transporter inhibition by Lefamulin. Pneumonia [CA40] [175]
Bromfenac DMKB79O Minor Decreased renal excretion of Cimetidine caused by Bromfenac. Postoperative inflammation [1A00-CA43] [176]
Ergonovine DM0VEC1 Moderate Decreased metabolism of Cimetidine caused by Ergonovine mediated inhibition of CYP450 enzyme. Postpartum haemorrhage [JA43] [177]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Cimetidine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [178]
Darolutamide DMV7YFT Minor Decreased metabolism of Cimetidine caused by Darolutamide mediated inhibition of CYP450 enzyme. Prostate cancer [2C82] [179]
Tamsulosin DM5QF9V Moderate Decreased metabolism of Cimetidine caused by Tamsulosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [180]
Silodosin DMJSBT6 Moderate Decreased metabolism of Cimetidine caused by Silodosin mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [181]
Dutasteride DMQ4TJK Moderate Decreased metabolism of Cimetidine caused by Dutasteride mediated inhibition of CYP450 enzyme. Prostate hyperplasia [GA90] [182]
Bosentan DMIOGBU Moderate Decreased metabolism of Cimetidine caused by Bosentan mediated inhibition of CYP450 enzyme. Pulmonary hypertension [BB01] [183]
Everolimus DM8X2EH Moderate Decreased clearance of Cimetidine due to the transporter inhibition by Everolimus. Renal cell carcinoma [2C90] [184]
Axitinib DMGVH6N Minor Decreased absorption of Cimetidine due to altered gastric pH caused by Axitinib. Renal cell carcinoma [2C90] [185]
Temsirolimus DMS104F Moderate Decreased metabolism of Cimetidine caused by Temsirolimus mediated inhibition of CYP450 enzyme. Renal cell carcinoma [2C90] [186]
Upadacitinib DM32B5U Moderate Decreased metabolism of Cimetidine caused by Upadacitinib mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [187]
Thioridazine DM35M8J Major Decreased metabolism of Cimetidine caused by Thioridazine mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [188]
Asenapine DMSQZE2 Moderate Decreased metabolism of Cimetidine caused by Asenapine mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [189]
Pimozide DMW83TP Major Decreased metabolism of Cimetidine caused by Pimozide mediated inhibition of CYP450 enzyme. Schizophrenia [6A20] [105]
Tadalafil DMJZHT1 Moderate Decreased metabolism of Cimetidine caused by Tadalafil mediated inhibition of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [190]
LDE225 DMM9F25 Moderate Decreased metabolism of Cimetidine caused by LDE225 mediated inhibition of CYP450 enzyme. Skin cancer [2C30-2C37] [191]
Larotrectinib DM26CQR Moderate Decreased metabolism of Cimetidine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [93]
Docetaxel DMDI269 Moderate Decreased metabolism of Cimetidine caused by Docetaxel mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [192]
Trabectedin DMG3Y89 Moderate Decreased metabolism of Cimetidine caused by Trabectedin mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [80]
Armodafinil DMGB035 Minor Decreased metabolism of Cimetidine caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [93]
LEE011 DMMX75K Moderate Decreased metabolism of Cimetidine caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [93]
Taxol DMUOT9V Moderate Decreased metabolism of Cimetidine caused by Taxol mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [193]
Pitolisant DM8RFNJ Moderate Decreased metabolism of Cimetidine caused by Pitolisant mediated inhibition of CYP450 enzyme. Somnolence [MG42] [80]
Warfarin DMJYCVW Moderate Decreased metabolism of Cimetidine caused by Warfarin mediated inhibition of CYP450 enzyme. Supraventricular tachyarrhythmia [BC81] [104]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Cimetidine caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [194]
Clopidogrel DMOL54H Moderate Decreased metabolism of Cimetidine caused by Clopidogrel mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [195]
Tizanidine DMR2IQ4 Major Decreased metabolism of Cimetidine caused by Tizanidine mediated inhibition of CYP450 enzyme. Tonus and reflex abnormality [MB47] [196]
Trimetrexate DMDEA85 Minor Decreased metabolism of Cimetidine caused by Trimetrexate mediated inhibition of CYP450 enzyme. Toxoplasmosis [1F57] [197]
Sirolimus DMGW1ID Moderate Decreased metabolism of Cimetidine caused by Sirolimus mediated inhibition of CYP450 enzyme. Transplant rejection [NE84] [93]
Tacrolimus DMZ7XNQ Moderate Decreased metabolism of Cimetidine caused by Tacrolimus mediated inhibition of CYP450 enzyme. Transplant rejection [NE84] [93]
Saxagliptin DMGXENV Moderate Decreased metabolism of Cimetidine caused by Saxagliptin mediated inhibition of CYP450 enzyme. Type 2 diabetes mellitus [5A11] [80]
Chlorpropamide DMPHZQE Moderate Decreased absorption of Cimetidine due to altered gastric pH caused by Chlorpropamide. Type 2 diabetes mellitus [5A11] [78]
Elagolix DMB2C0E Moderate Decreased metabolism of Cimetidine caused by Elagolix mediated inhibition of CYP450 enzyme. Uterine fibroid [2E86] [198]
Astemizole DM2HN6Q Major Decreased metabolism of Cimetidine caused by Astemizole mediated inhibition of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [199]
Procainamide DMNMXR8 Moderate Decreased elimination of Cimetidine caused by Procainamide mediated competitive inhibition of renal tubular secretion. Ventricular tachyarrhythmia [BC71] [200]
Propafenone DMPIBJK Moderate Decreased metabolism of Cimetidine caused by Propafenone mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [201]
Flecainide DMSQDLE Moderate Decreased metabolism of Cimetidine caused by Flecainide mediated inhibition of CYP450 enzyme. Ventricular tachyarrhythmia [BC71] [202]
⏷ Show the Full List of 217 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Vanillin E00049 1183 Flavoring agent
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Hypromellose E00634 Not Available Coating agent
Magnesium stearate E00208 11177 lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Sodium alginate E00671 Not Available Binding agent; Disintegrant; Suspending agent; Viscosity-controlling agent
Soybean lecithin E00637 Not Available Other agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Triethyl citrate E00128 6506 Plasticizing agent; Solvent
⏷ Show the Full List of 17 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Cimetidine 400 mg tablet 400 mg Oral Tablet Oral
Cimetidine 200 mg tablet 200 mg Oral Tablet Oral
Cimetidine 800 mg tablet 800 mg Oral Tablet Oral
Cimetidine 300 mg tablet 300 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1231).
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074151.
3 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
4 BDDCS applied to over 900 drugs
5 Somogyi A, Gugler R: Clinical pharmacokinetics of cimetidine. Clin Pharmacokinet. 1983 Nov-Dec;8(6):463-95. doi: 10.2165/00003088-198308060-00001.
6 DPD Approved Drug Products: Cimetidine (200, 300, 400, 600, 800 mg)
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
9 Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. J Invest Dermatol. 2001 Feb;116(2):261-5.
10 Characterization and modulation of antigen-induced effects in isolated rat heart. J Cardiovasc Pharmacol. 1991 Oct;18(4):556-65.
11 Effect of the H2 histamine receptor antagonist on oxygen metabolism in some morphotic blood elements in patients with ulcer disease. Hepatogastroenterology. 1998 Jan-Feb;45(19):276-80.
12 Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
13 Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71.
14 Progesterone acts via progesterone receptors A and B to regulate breast cancer resistance protein expression. Mol Pharmacol. 2008 Mar;73(3):613-5.
15 Elevated systemic elimination of cimetidine in rats with acute biliary obstruction: the role of renal organic cation transporter OCT2. Drug Metab Pharmacokinet. 2010;25(4):328-34.
16 Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther. 2007 May;321(2):673-83.
17 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
18 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
19 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
20 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
21 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
22 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
23 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
24 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
25 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
26 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
27 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
28 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
29 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
30 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
31 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
32 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
33 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
34 Cisplatin nephrotoxicity is critically mediated via the human organic cation transporter 2. Am J Pathol. 2005 Dec;167(6):1477-84.
35 Relevance of copper transporter 1 and organic cation transporters 1-3 for oxaliplatin uptake and drug resistance in colorectal cancer cells. Metallomics. 2018 Mar 1;10(3):414-425.
36 Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81.
37 Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
38 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
39 The organic cation transporters (OCT1, OCT2, EMT) and the plasma membrane monoamine transporter (PMAT) show differential distribution and cyclic expression pattern in human endometrium and early pregnancy decidua. Mol Reprod Dev. 2007 Oct;74(10):1303-11.
40 Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. Drug Metab Pharmacokinet. 2005 Oct;20(5):379-86.
41 A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther. 2005 Oct;315(1):337-45.
42 Human multidrug and toxin extrusion 1 (MATE1/SLC47A1) transporter: functional characterization, interaction with OCT2 (SLC22A2), and single nucleotide polymorphisms. Am J Physiol Renal Physiol. 2010 Apr;298(4):F997-F1005.
43 Molecular mechanism of renal tubular secretion of the antimalarial drug chloroquine. Antimicrob Agents Chemother. 2011 Jul;55(7):3091-8.
44 Reduced renal clearance of a zwitterionic substrate cephalexin in MATE1-deficient mice. J Pharmacol Exp Ther. 2010 Aug;334(2):651-6.
45 Abemaciclib Inhibits Renal Tubular Secretion Without Changing Glomerular Filtration Rate. Clin Pharmacol Ther. 2019 May;105(5):1187-1195.
46 FDA Drug Development and Drug Interactions
47 Expression of Organic Anion Transporter 1 or 3 in Human Kidney Proximal Tubule Cells Reduces Cisplatin Sensitivity. Drug Metab Dispos. 2018 May;46(5):592-599.
48 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
49 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
50 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
51 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
52 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
53 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
54 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
55 Methotrexate-loxoprofen interaction: involvement of human organic anion transporters hOAT1 and hOAT3. Drug Metab Pharmacokinet. 2004 Oct;19(5):369-74.
56 Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol Exp Ther. 2002 Apr;301(1):293-8.
57 Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24.
58 Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86.
59 Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos. 2011 Jun;39(6):1031-8.
60 Murine renal organic anion transporters mOAT1 and mOAT3 facilitate the transport of neuroactive tryptophan metabolites. Am J Physiol Cell Physiol. 2005 Nov;289(5):C1075-84.
61 Organic anion transporter 3 is involved in the brain-to-blood efflux transport of thiopurine nucleobase analogs. J Neurochem. 2004 Aug;90(4):931-41.
62 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
63 The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7.
64 Aspirin and probenecid inhibit organic anion transporter 3-mediated renal uptake of cilostazol and probenecid induces metabolism of cilostazol in the rat. Drug Metab Dispos. 2014 Jun;42(6):996-1007.
65 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
66 Does the use of nizatidine, as a pro-kinetic agent, improve gastric emptying in patients post-oesophagectomy J Gastrointest Surg. 2009 Mar;13(3):432-7.
67 Effect of nizatidine and cimetidine on betazole-stimulated gastric secretion of normal subjects: comparison of effects on acid, water, and pepsin. Am J Gastroenterol. 1988 Jan;83(1):32-6.
68 Histamine H2-receptor antagonist action of ebrotidine. Effects on gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat. Arzneimittelforschung. 1997 Apr;47(4A):439-46.
69 Comparative pharmacology of epibatidine: a potent agonist for neuronal nicotinic acetylcholine receptors. Mol Pharmacol. 1995 Oct;48(4):774-82.
70 Effects of osutidine (T-593) and its enantiomers on gastric mucosal hemodynamics and mucosal integrity in anesthetized rats. Arzneimittelforschung. 2001 Jan;51(1):46-50.
71 Pharmacological profiles of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy] propyl] urea. Arzneimittelforschung. 1993 Feb;43(2):129-33.
72 New and Future Drug Development for Gastroesophageal Reflux Disease. J Neurogastroenterol Motil. 2014 January; 20(1): 6-16.
73 Effects of IGN-2098, a new histamine H2-receptor antagonist, on gastric secretion and gastric and duodenal lesions induced in rats. Comparison with roxatidine. Nihon Yakurigaku Zasshi. 1992 Mar;99(3):167-80.
74 Bedford TA, Rowbotham DJ "Cisapride: drug interactions of clinical significance." Drug Saf 15 (1996): 167-75. [PMID: 8879971]
75 Albin H, Vincon G, Begaud B, Bistue C, Perez P "Effect of aluminum phosphate on the bioavailability of ranitidine." Eur J Clin Pharmacol 32 (1987): 97-9. [PMID: 3582475]
76 Honig PK, Gillespie BK "Clinical significance of pharmacokinetic drug interactions with over-the-counter (OTC) drugs." Clin Pharmacokinet 35 (1998): 167-71. [PMID: 9784931]
77 Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT "CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide." Br J Clin Pharmacol 56 (2003): 305-14. [PMID: 12919179]
78 Dey NG, Castleden CM, Ward J, et al "The effect of cimetidine on tolbutamide kinetics." Br J Clin Pharmacol 16 (1983): 438-40. [PMID: 6626438]
79 Dutreix C, Munarini F, Lorenzo S, Roesel J, Wang Y "Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers." Cancer Chemother Pharmacol 72 (2013): 1223-34. [PMID: 24085261]
80 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
81 Beers MH, Ouslander JG, Rollingher I, Reuben DB, Brooks J, Beck JC "Explicit criteria for determining inappropriate medication use in nursing home residents." Arch Intern Med 151 (1991): 1825-32. [PMID: 1888249]
82 Gugler R, Jensen JC "Interaction between cimetidine and metronidazole." N Engl J Med 309 (1983): 1518-9. [PMID: 6646177]
83 Product Information. Multaq (dronedarone). sanofi-aventis , Bridgewater, NJ.
84 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
85 Greenblatt DJ, Abernethy DR, Morse DS, Harmatz JS, Shader RI "Clinical importance of the interaction of diazepam and cimetidine." N Engl J Med 310 (1984): 1639-43. [PMID: 6427609]
86 Somogyi A, Thielscher S, Gugler R "Influence of phenobarbital treatment on cimetidine kinetics." Eur J Clin Pharmacol 19 (1981): 343-7. [PMID: 7238562]
87 Simons FE, Sussman GL, Simons KJ "Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria." J Allergy Clin Immunol 95 (1995): 685-93. [PMID: 7897151]
88 Abernethy DR, Greenblatt DJ, Divoll M, Moschitto LJ, Harmatz JS, Shader RI "Interaction of cimetidine with the triazolobenzodiazepines alprazolam and triazolam." Psychopharmacology (Berl) 80 (1983): 275-8. [PMID: 6137021]
89 Hedaya MA, El-Afify DR, El-Maghraby GM "The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers." Biopharm Drug Dispos 27 (2006): 103-10. [PMID: 16372380]
90 Anderson JR, Poklis A, Slavin RG "A fatal case of theophylline intoxication." Arch Intern Med 143 (1983): 559-60. [PMID: 6830388]
91 Abernethy DR, Greenblatt DJ, Shader RI "Imipramine-cimetidine interaction: impairment of clearance and enhanced absolute bioavailability." J Pharmacol Exp Ther 229 (1984): 702-5. [PMID: 6726654]
92 Product Information. Spectracef (cefditoren). TAP Pharmaceuticals Inc, Deerfield, IL.
93 Cerner Multum, Inc. "Australian Product Information.".
94 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
95 Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
96 Product Information. Ixempra (ixabepilone). Bristol-Myers Squibb, Princeton, NJ.
97 Galbraith RA, Michnovicz JJ "The effects of cimetidine on the oxidative metabolism of estradiol." N Engl J Med 321 (1989): 269-74. [PMID: 2747769]
98 Amchin J, Ereshefsky L, Zarycranski W, Taylor K, Albano D, Klockowski PM "Effect of venlafaxine versus fluoxetine on metabolism of dextromethorphan, a CYP2D6 probe." J Clin Pharmacol 41 (2001): 443-51. [PMID: 11304901]
99 Product Information. Fareston (toremifene). Schering Laboratories, Kenilworth, NJ.
100 Clyne CA, Estes NA, Wang PJ "Moricizine." N Engl J Med 327 (1992): 255-60. [PMID: 1614466]
101 Agbin NE, Brater DC, Hall SD "Interaction of diltiazem with lovastatin and pravastatin." Clin Pharmacol Ther 61 (1997): 201. [PMID: 9797793]
102 Product Information. Opsumit (macitentan). Actelion Pharmaceuticals US Inc, South San Francisco, CA.
103 Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
104 Breckenridge AM, Challiner M, Mossman S, et al "Cimetidine increases the action of warfarin in man." Br J Clin Pharmacol 8 (1979): p392-3. [PMID: 508530]
105 Canadian Pharmacists Association.
106 Bartkowski RR, Goldberg ME, Larijani GE, Boerner T "Inhibition of alfentanil metabolism by erythromycin." Clin Pharmacol Ther 46 (1989): 99-102. [PMID: 2501060]
107 Product Information. Korlym (mifepristone). Corcept Therapeutics Incorporated, Menlo Park, CA.
108 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
109 Feely J, Wood AJ "Effects of cimetidine on the elimination and actions of ethanol." JAMA 247 (1982): 2819-21. [PMID: 7043008]
110 Product Information. Xarelto (rivaroxaban). Bayer Inc, Toronto, IA.
111 Bannister SJ, Houser VP, Hulse JD, Kisicki JC, Rasmussen JG "Evaluation of the potential for interactions of paroxetine with diazepam, cimetidine, warfarin, and digoxin." Acta Psychiatr Scand Suppl 350 (1989): 102-6. [PMID: 2530759]
112 Product Information. Effexor (venlafaxine). Wyeth-Ayerst Laboratories, Philadelphia, PA.
113 Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
114 Product Information. Polivy (polatuzumab vedotin). Genentech, South San Francisco, CA.
115 Mauro VF, Mauro LS, Hageman JH "Alteration of pentoxifylline pharmacokinetics by cimetidine." J Clin Pharmacol 28 (1988): 649-54. [PMID: 3216031]
116 Nakasa H, Nakamura H, Ono S, Tsutsui M, Kiuchi M, Ohmori S, Kitada M "Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data." Eur J Clin Pharmacol 54 (1998): 177-83. [PMID: 9626925]
117 Algozzine GJ, Stewart RB, Springer PK "Decreased clearance of phenytoin with cimetidine." Ann Intern Med 95 (1981): 244-5. [PMID: 7258891]
118 Dalton MJ, Powell JR, Messenheimer JA Jr, Clark J "Cimetidine and carbamazepine: a complex drug interaction." Epilepsia 27 (1986): 553-8. [PMID: 3757941]
119 Asgharnejad M, Powell R, Donn K, Danis M "The effect of cimetidine dose timing on oral propranolol kinetics in adults." Clin Pharmacol Ther 41 (1987): 203. [PMID: 3392231]
120 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
121 Product Information. VESIcare (solifenacin). GlaxoSmithKline, Research Triangle Park, NC.
122 Product Information. Myrbetriq (mirabegron). Astellas Pharma US, Inc, Deerfield, IL.
123 Brynne N, Forslund C, Hallen B, Gustafsson LL, Bertilsson L "Ketoconazole inhibits the metabolism of tolterodine in subjects with deficient CYP2D6 activity." Br J Clin Pharmacol 48 (1999): 564-72. [PMID: 10583027]
124 Blum RA, D'Andrea DT, Florentino BM, et al "Increased gastric pH and the bioavailability of fluconazole and ketoconazole." Ann Intern Med 114 (1991): 755-7. [PMID: 2012358]
125 Long CC, Hill SA, Thomas RC, Johnston A, Smith SG, Kendall F, Finlay AY "Effect of terbinafine on the pharmacokinetics of cyclosporin in humans." J Invest Dermatol 102 (1994): 740-3. [PMID: 8176256]
126 Adachi M, Hinatsu Y, et.al "Improved dissolution and absorption of ketoconazole in the presence of organic acids as pH-modifiers." Eur J Pharm Sci 76 (2015): 225-30. [PMID: 25988287]
127 Leighton JA, Bay MK, Maldonado AL, et al "The effect of liver dysfunction on colchicine pharmacokinetics in the rat." Hepatology 11 (1990): 210-5. [PMID: 2307399]
128 Ausband SC, Goodman PE "An unusual case of clarithromycin associated ergotism." J Emerg Med 4 (2001): 411-3. [PMID: 11728770]
129 Product Information. Pifeltro (doravirine). Merck & Company Inc, Whitehouse Station, NJ.
130 Product Information. Rescriptor (delavirdine). Pharmacia and Upjohn, Kalamazoo, MI.
131 Product Information. Lexiva (fosamprenavir). GlaxoSmithKline, Research Triangle Park, NC.
132 Product Information. Tivicay (dolutegravir). ViiV Healthcare, Research Triangle Park, NC.
133 Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
134 Product Information. Edurant (rilpivirine). Tibotec Pharmaceuticals, Titusville, NJ.
135 Product Information. Agenerase (amprenavir). Glaxo Wellcome, Research Triangle Pk, NC.
136 Product Information. Selzentry (maraviroc). Pfizer U.S. Pharmaceuticals Group, New York, NY.
137 Product Information. Isentress (raltegravir). Merck & Company Inc, West Point, PA.
138 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
139 Product Information. Altabax (retapamulin topical). GlaxoSmithKline, Research Triangle Park, NC.
140 Product Information. Rozerem (ramelteon). Takeda Pharmaceuticals America, Lincolnshire, IL.
141 Product Information. Sonata (zaleplon) Wyeth-Ayerst Laboratories, Philadelphia, PA.
142 Product Information. Hetlioz (tasimelteon). Vanda Pharmaceuticals Inc, Rockville, MD.
143 Product Information. Caplyta (lumateperone). Intra-Cellular Therapies, Inc., New York, NY.
144 Bianchi FM, Cavassini GB, Leo P "Iron protein succynilate in the treatment of iron deficiency: potential interaction with H2-receptor antagonists." Int J Clin Pharmacol Ther Toxicol 31 (1993): 209-17. [PMID: 8100220]
145 Product Information. Lotronex (alosetron). Glaxo Wellcome, Research Triangle Park, NC.
146 Product Information. Movantik (naloxegol). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
147 Product Information. Zykadia (ceritinib). Novartis Pharmaceuticals, East Hanover, NJ.
148 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
149 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
150 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
151 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
152 Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
153 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
154 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
155 Product Information. Koselugo (selumetinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
156 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
157 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
158 Hamberg P, Woo MM, Chen LC, et al. "Effect of ketoconazole-mediated CYP3A4 inhibition on clinical pharmacokinetics of panobinostat (LBH589), an orally active histone deacetylase inhibitor." Cancer Chemother Pharmacol 68 (2011): 805-13. [PMID: 21706316]
159 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
160 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
161 Product Information. Gleevec (imatinib mesylate). Novartis Pharmaceuticals, East Hanover, NJ.
162 Product Information. Sprycel (dasatinib). Bristol-Myers Squibb, Princeton, NJ.
163 Product Information. Effient (prasugrel). Lilly, Eli and Company, Indianapolis, IN.
164 Product Information. Anzemet (dolasetron). Hoechst Marion-Roussel Inc, Kansas City, MO.
165 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
166 Product Information. Meridia (sibutramine). Knoll Pharmaceutical Company, Whippany, NJ.
167 Product Information. Orlaam (levomethadyl acetate) Roxanne Laboratories Inc, Columbus, OH.
168 Product Information. Bextra (valdecoxib). Pharmacia Corporation, Peapack, NJ.
169 Product Information. Lynparza (olaparib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
170 Product Information. Buprenex (buprenorphine). Reckitt and Colman Pharmaceutical, Richmond, VA.
171 Hutchinson MR, Menelaou A, Foster DJ, Coller JK, Somogyi AA "CYP2D6 and CYP3A4 involvement in the primary oxidative metabolism of hydrocodone by human liver microsomes." Br J Clin Pharmacol 57 (2004): 287-97. [PMID: 14998425]
172 Bekhti A, Pirotte J "Cimetidine increases serum mebendazole concentrations: implications for treatment of hepatic hydatid cysts." Br J Clin Pharmacol 24 (1987): 390-2. [PMID: 3663452]
173 Product Information. Nourianz (istradefylline). Kyowa Kirin, Inc, Bedminster, NJ.
174 Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
175 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
176 Product Information. Duract (bromfenac). Wyeth-Ayerst Laboratories, Philadelphia, PA.
177 Francis H, Tyndall A, Webb J "Severe vascular spasm due to erythromycin-ergotamine interaction." Clin Rheumatol 3 (1984): 243-6. [PMID: 6236021]
178 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
179 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
180 Franco-Salinas G, de la Rosette JJ, Michel MC "Pharmacokinetics and pharmacodynamics of tamsulosin in its modified-release and oral controlled absorption system formulations." Clin Pharmacokinet 49 (2010): 177-88. [PMID: 20170206]
181 Product Information. Rapaflo (silodosin). Watson Pharmaceuticals, Corona, CA.
182 Product Information. Duagen (dutasteride). GlaxoSmithKline Healthcare, Pittsburgh, PA.
183 Product Information. Tracleer (bosentan). Acetelion Pharmaceuticals US, Inc, South San Francisco, CA.
184 Product Information. Afinitor (everolimus). Novartis Pharmaceuticals, East Hanover, NJ.
185 Product Information. Inlyta (axitinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
186 Product Information. Torisel (temsirolimus). Wyeth-Ayerst Laboratories, Philadelphia, PA.
187 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
188 Abernethy DR, Greenblatt DJ, Steel K, Shader RI "Impairment of hepatic drug oxidation by propoxyphene." Ann Intern Med 97 (1982): 223-4. [PMID: 7103282]
189 Product Information. Saphris (asenapine). Schering-Plough Corporation, Kenilworth, NJ.
190 Product Information. Cialis (tadalafil). Lilly, Eli and Company, Indianapolis, IN.
191 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
192 Aronson JK, Grahame-Smith DG "Clinical pharmacology: adverse drug interactions." Br Med J 282 (1981): 288-91. [PMID: 6779990]
193 Bergmann TK, Filppula AM, Launiainen T, Nielsen F, Backman J, Brosen K "Neurotoxicity and low paclitaxel clearance associated with concomitant clopidogrel therapy in a 60 year old Caucasian woman with ovarian carcinoma." Br J Clin Pharmacol (2015):. [PMID: 26446447]
194 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
195 Collet JP, Hulot JS, Pena A, et al. "Cytochrome P450 2C19 polymorphism in young patients treated with clopidogrel after myocardial infarction: a cohort study." Lancet 373 (2009): 309-17. [PMID: 19108880]
196 Granfors MT, Backman JT, Laitila J, Neuvonen PJ "Tizanidine is mainly metabolized by cytochrome P450 1A2 in vitro." Br J Clin Pharmacol 57 (2004): 349-53. [PMID: 14998432]
197 Product Information. Neutrexin (trimetrexate). US Bioscience, West Conshohocken, PA.
198 Product Information. Orilissa (elagolix). AbbVie US LLC, North Chicago, IL.
199 Hey JA, Delprado M, Egan RW, Kreutner W "Terfenadine, astemizole, and ebastine produce QTc interval prolongation in an experimental model predictive of adverse clinical ECG effects." Ann Allergy Asthma Immunol 76 (1996): 476. [PMID: 8630724]
200 Bauer LA, Black D, Gensler A "Procainamide-cimetidine drug interaction in elderly male patients." J Am Geriatr Soc 38 (1990): 467-9. [PMID: 2329253]
201 Pritchett EL, Smith WM, Kirsten EB "Pharmacokinetic and pharmacodynamic interactions of propafenone and cimetidine." J Clin Pharmacol 28 (1988): 619-24. [PMID: 3063727]
202 Tjandra-Maga TB, Van Hecken A, Van Melle P, Verbesselt R, de Schepper PJ "Altered pharmacokinetics of oral flecainide by cimetidine." Br J Clin Pharmacol 22 (1986): 108-10. [PMID: 3741720]