Details of the Drug

General Information of Drug (ID: DM72JXH)

Drug Name
Losartan
Synonyms
Cozaar; Cozaar (TN); DUP 89; DuP 753; DuP-753; Hyzaar; JMS50MPO89; LOSARTAN POTASSIUM; Lortaan; Losartan (INN); 114798-26-4; C22H23ClN6O; CHEBI:6541; CL23623; Losartan [INN:BAN]; Losartan monopotassium salt; Losartic; Losartic (TN); MK-954; MK954; UNII-JMS50MPO89; [3H]losartan
Indication
Disease Entry ICD 11 Status REF
Diabetic kidney disease GB61.Z Approved [1]
Hypertension BA00-BA04 Approved [2]
Prediabetes syndrome N.A. Approved [1]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [3]
Therapeutic Class
Antihypertensive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 422.9
Logarithm of the Partition Coefficient (xlogp) 4.3
Rotatable Bond Count (rotbonds) 8
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 8.2 mL/min/kg [5]
Elimination
12% 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 1.8 hours [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 3.94873 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.01% [5]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.37 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 0.048 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Capillary fragility increased Not Available IL1A OTPSGILV [7]
Metabolic disorder Not Available CYP2C9 OTGLBN29 [7]
Chemical Identifiers
Formula
C22H23ClN6O
IUPAC Name
[2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol
Canonical SMILES
CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CO)Cl
InChI
InChI=1S/C22H23ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,30H,2-3,8,13-14H2,1H3,(H,25,26,27,28)
InChIKey
PSIFNNKUMBGKDQ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3961
ChEBI ID
CHEBI:6541
CAS Number
114798-26-4
DrugBank ID
DB00678
TTD ID
D0DD0K
VARIDT ID
DR00429
INTEDE ID
DR0984
ACDINA ID
D00153
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Angiotensin II receptor type-1 (AGTR1) TT8DBY3 AGTR1_HUMAN Antagonist [8]
HUMAN type-1 angiotensin II receptor (AGTR1) TTPKMXQ AGTR1_HUMAN Blocker [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Peptide transporter 1 (SLC15A1) DT9G7XN S15A1_HUMAN Substrate [10]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [11]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [12]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [13]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [14]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [12]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [15]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [13]
UDP-glucuronosyltransferase 1A10 (UGT1A10) DEL5N6Y UD110_HUMAN Substrate [13]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate [13]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 2C9 (CYP2C9) OTGLBN29 CP2C9_HUMAN Drug Response [7]
Interleukin-1 alpha (IL1A) OTPSGILV IL1A_HUMAN Drug Response [7]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Diabetic kidney disease
ICD Disease Classification GB61.Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Angiotensin II receptor type-1 (AGTR1) DTT AGTR1 8.95E-01 1.34E-02 0.07
P-glycoprotein 1 (ABCB1) DTP P-GP 9.39E-02 1.07E-01 2.80E-01
Peptide transporter 1 (SLC15A1) DTP PEPT1 4.57E-01 2.15E-02 1.72E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 1.10E-01 -5.91E-02 -3.60E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.82E-04 -1.35E-01 -5.84E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.96E-01 -3.17E-03 -1.84E-02
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.90E-01 -9.81E-03 -5.96E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Losartan
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Aliskiren DM1BV7W Major Increased risk of hyperkalemia by the combination of Losartan and Aliskiren. Hypertension [BA00-BA04] [16]
Moexipril DM26E4B Major Increased risk of hyperkalemia by the combination of Losartan and Moexipril. Hypertension [BA00-BA04] [17]
Captopril DM458UM Major Increased risk of hyperkalemia by the combination of Losartan and Captopril. Hypertension [BA00-BA04] [17]
Perindopril DMOPZDT Major Increased risk of hyperkalemia by the combination of Losartan and Perindopril. Hypertension [BA00-BA04] [17]
Quinapril DMR8H31 Major Increased risk of hyperkalemia by the combination of Losartan and Quinapril. Hypertension [BA00-BA04] [17]
Lisinopril DMUOK4C Major Increased risk of hyperkalemia by the combination of Losartan and Lisinopril. Hypertension [BA00-BA04] [17]
⏷ Show the Full List of 6 DDI Information of This Drug
Coadministration of a Drug Treating the Disease Different from Losartan (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Nateglinide DMLK2QH Moderate Decreased metabolism of Losartan caused by Nateglinide mediated inhibition of CYP450 enzyme. Acute diabete complication [5A2Y] [18]
Insulin-aspart DMX7V28 Moderate Increased risk of hypoglycemia by the combination of Losartan and Insulin-aspart. Acute diabete complication [5A2Y] [19]
Methylphenobarbital DMDSWAG Minor Increased metabolism of Losartan caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [20]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Losartan caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [21]
Troleandomycin DMUZNIG Minor Decreased metabolism of Losartan caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [22]
Cariprazine DMJYDVK Moderate Additive hypotensive effects by the combination of Losartan and Cariprazine. Bipolar disorder [6A60] [23]
Alpelisib DMEXMYK Moderate Increased metabolism of Losartan caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [24]
Olopatadine DMKMWQG Moderate Additive CNS depression effects by the combination of Losartan and Olopatadine. Conjunctiva disorder [9A60] [25]
Drospirenone DM1A9W3 Moderate Increased risk of hyperkalemia by the combination of Losartan and Drospirenone. Contraceptive management [QA21] [26]
Ardeparin DMYRX8B Moderate Increased risk of hyperkalemia by the combination of Losartan and Ardeparin. Coronary thrombosis [BA43] [17]
Mifepristone DMGZQEF Moderate Decreased metabolism of Losartan caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [27]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Losartan caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [28]
MK-8228 DMOB58Q Moderate Increased metabolism of Losartan caused by MK-8228 mediated induction of CYP450 enzyme. Cytomegaloviral disease [1D82] [29]
Selegiline DM6034S Moderate Additive hypotensive effects by the combination of Losartan and Selegiline. Depression [6A70-6A7Z] [30]
Isocarboxazid DMAF1NB Moderate Additive hypotensive effects by the combination of Losartan and Isocarboxazid. Depression [6A70-6A7Z] [30]
Tranylcypromine DMGB5RE Moderate Additive hypotensive effects by the combination of Losartan and Tranylcypromine. Depression [6A70-6A7Z] [30]
OPC-34712 DMHG57U Moderate Additive hypotensive effects by the combination of Losartan and OPC-34712. Depression [6A70-6A7Z] [23]
Phenelzine DMHIDUE Moderate Additive hypotensive effects by the combination of Losartan and Phenelzine. Depression [6A70-6A7Z] [30]
Primidone DM0WX6I Minor Increased metabolism of Losartan caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [20]
Phenobarbital DMXZOCG Minor Increased metabolism of Losartan caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [20]
Itraconazole DMCR1MV Moderate Decreased metabolism of Losartan caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [31]
Ketoconazole DMPZI3Q Minor Decreased metabolism of Losartan caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [22]
Eplerenone DMF0NQR Moderate Increased risk of hyperkalemia by the combination of Losartan and Eplerenone. Heart failure [BD10-BD1Z] [32]
Rifampin DMA8J1G Moderate Increased metabolism of Losartan caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [33]
Rifapentine DMCHV4I Moderate Increased metabolism of Losartan caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [34]
Procarbazine DMIK367 Moderate Additive hypotensive effects by the combination of Losartan and Procarbazine. Hodgkin lymphoma [2B30] [30]
Etravirine DMGV8QU Moderate Decreased metabolism of Losartan caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [35]
Fenofibrate DMFKXDY Moderate Decreased metabolism of Losartan caused by Fenofibrate mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [36]
Potassium chloride DMMTAJC Major Increased risk of hyperkalemia by the combination of Losartan and Potassium chloride. Hypo-kalaemia [5C77] [37]
Tolvaptan DMIWFRL Moderate Increased risk of hyperkalemia by the combination of Losartan and Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [38]
Amobarbital DM0GQ8N Minor Increased metabolism of Losartan caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [20]
Propiomazine DMKY8V1 Moderate Additive hypotensive effects by the combination of Losartan and Propiomazine. Insomnia [7A00-7A0Z] [23]
ITI-007 DMUQ1DO Moderate Additive hypotensive effects by the combination of Losartan and ITI-007. Insomnia [7A00-7A0Z] [23]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Losartan and Porfimer Sodium. Lung cancer [2C25] [39]
PF-06463922 DMKM7EW Moderate Increased metabolism of Losartan caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [36]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Losartan caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [40]
Ozanimod DMT6AM2 Moderate Additive hypotensive effects by the combination of Losartan and Ozanimod. Multiple sclerosis [8A40] [30]
Promethazine DM6I5GR Moderate Additive hypotensive effects by the combination of Losartan and Promethazine. Nausea/vomiting [MD90] [23]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Losartan caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [41]
Safinamide DM0YWJC Moderate Additive hypotensive effects by the combination of Losartan and Safinamide. Parkinsonism [8A00] [30]
Rasagiline DM3WKQ4 Moderate Additive hypotensive effects by the combination of Losartan and Rasagiline. Parkinsonism [8A00] [30]
Abametapir DM2RX0I Moderate Decreased metabolism of Losartan caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [42]
Lefamulin DME6G97 Moderate Decreased metabolism of Losartan caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [43]
Enzalutamide DMGL19D Moderate Increased metabolism of Losartan caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [44]
Levomepromazine DMIKFEL Moderate Additive hypotensive effects by the combination of Losartan and Levomepromazine. Psychotic disorder [6A20-6A25] [23]
Leflunomide DMR8ONJ Moderate Decreased metabolism of Losartan caused by Leflunomide mediated inhibition of CYP450 enzyme. Rheumatoid arthritis [FA20] [45]
Quetiapine DM1N62C Moderate Additive hypotensive effects by the combination of Losartan and Quetiapine. Schizophrenia [6A20] [23]
Mesoridazine DM2ZGAN Moderate Additive hypotensive effects by the combination of Losartan and Mesoridazine. Schizophrenia [6A20] [23]
Thioridazine DM35M8J Moderate Additive hypotensive effects by the combination of Losartan and Thioridazine. Schizophrenia [6A20] [23]
Aripiprazole DM3NUMH Moderate Additive hypotensive effects by the combination of Losartan and Aripiprazole. Schizophrenia [6A20] [23]
Iloperidone DM6AUFY Moderate Additive hypotensive effects by the combination of Losartan and Iloperidone. Schizophrenia [6A20] [23]
Paliperidone DM7NPJS Moderate Additive hypotensive effects by the combination of Losartan and Paliperidone. Schizophrenia [6A20] [23]
Molindone DMAH70G Moderate Additive hypotensive effects by the combination of Losartan and Molindone. Schizophrenia [6A20] [23]
Thiothixene DMDINC4 Moderate Additive hypotensive effects by the combination of Losartan and Thiothixene. Schizophrenia [6A20] [23]
Trifluoperazine DMKBYWI Moderate Additive hypotensive effects by the combination of Losartan and Trifluoperazine. Schizophrenia [6A20] [23]
Risperidone DMN6DXL Moderate Additive hypotensive effects by the combination of Losartan and Risperidone. Schizophrenia [6A20] [23]
Amisulpride DMSJVAM Moderate Additive hypotensive effects by the combination of Losartan and Amisulpride. Schizophrenia [6A20] [23]
Asenapine DMSQZE2 Moderate Additive hypotensive effects by the combination of Losartan and Asenapine. Schizophrenia [6A20] [23]
Larotrectinib DM26CQR Moderate Decreased metabolism of Losartan caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [36]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Losartan caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [46]
Insulin-detemir DMOA4VW Moderate Increased risk of hypoglycemia by the combination of Losartan and Insulin-detemir. Type-1/2 diabete [5A10-5A11] [47]
Insulin degludec DMPL395 Moderate Increased risk of hypoglycemia by the combination of Losartan and Insulin degludec. Type-1/2 diabete [5A10-5A11] [47]
Methdilazine DMAUHQX Moderate Additive hypotensive effects by the combination of Losartan and Methdilazine. Vasomotor/allergic rhinitis [CA08] [23]
Trimeprazine DMEMV9D Moderate Additive hypotensive effects by the combination of Losartan and Trimeprazine. Vasomotor/allergic rhinitis [CA08] [48]
⏷ Show the Full List of 64 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. 2 E00446 2723854 Colorant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Quinoline yellow WS E00309 24671 Colorant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Hydroxypropyl cellulose E00632 Not Available Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Methyl chloride E00114 6327 Other agent
Polyethylene glycol 3350 E00652 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling 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
Water E00035 962 Solvent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 29 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Losartan 100 mg tablet 100 mg Oral Tablet Oral
Losartan 25 mg tablet 25 mg Oral Tablet Oral
Losartan 50 mg tablet 50 mg Oral Tablet Oral
Losartan Potassium 25mg tablet 25mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Losartan FDA Label
2 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: 590).
3 ClinicalTrials.gov (NCT04343001) Coronavirus Response - Active Support for Hospitalised Covid-19 Patients. U.S. National Institutes of Health.
4 BDDCS applied to over 900 drugs
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 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
7 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
8 Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
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10 High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
11 Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco-2 cell monolayers. Br J Pharmacol. 2000 Mar;129(6):1235-43.
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14 The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan. Biochem Pharmacol. 2008 Sep 15;76(6):763-72.
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