InAADR

Drug Information

Drug Name: Terfenadine (50679-08-8)
PubChem ID: 5405
SMILES: CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O
InchiKey: GUGOEEXESWIERI-UHFFFAOYSA-N
Therapeutic Category: Histamine Agents, Histamine Antagonists, Histamine H1 Antagonists, Neurotransmitter Agents

Computed Drug Properties

Molecular Weight (dalton): 471.685
LogP: 6.4458
Ring Count: 3
Hydrogen Bond Acceptor Count: 3
Hydrogen Bond Donor Count: 2
Total Polar Surface Area: 43.7

This panel provides information on interacting drugs and their ADRs along with references

Interacting drug Toxicity Interaction Type Mechanism Reference
Acetaminophen (103-90-2) Torsade De Pointes Synergistic overdosage with paracetamol produced large amounts of a metabolite (N-acetyl-p-benzoquinoneimine). This metabolite could have inhibited the metabolism of the terfenadine by the cytochrome P450 isoenzyme CYP3A4, Torsades de pointes ventricular tachycardia associated with terfenadine and paracetamol self medication
Erythromycin (114-07-8) Torsade De Pointes Synergistic macrolides ( erythromycin ) appear to reduce the metabolism of terfenadine by inhibition of the cytochrome P450 isoenzyme CYP3A Oxidation of the antihistaminic drug terfenadine in human liver microsomes Role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation
Fluoxetine (54910-89-3) Cardiotoxicity Synergistic Not understood Potential terfenadine-fluoxetine interaction
Itraconazole (84625-61-6) Torsade De Pointes Synergistic itraconazole reduce the metabolism of terfenadine by inhibition of the cytochrome P450 isoenzyme CYP3A Torsades de pointes after terfenadine-itraconazole interaction
Nefazodone (83366-66-9) Prolongs The Qt Interval Synergistic Nefazodone inhibits the metabolism of terfenadine Loratadine and terfenadine interaction with nefazodone: Both antihistamines are associated with QTc prolongation
Saquinavir (127779-20-8) Torsade De Pointes Synergistic saquinavir was a potent inhibitor of the metabolism of terfenadine Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small-intestinal cytochrome P4503A4: potential contribution to high first-pass metabolism
Sparfloxacin (110871-86-8) Torsade De Pointes Additives Additive effect of drug The effect of terfenadine on the cardiac pharmacodynamics of sparfloxacin

This panel provides drug-protein interaction and their ADRs along with references

Toxicity Interacting Protein Mechanism Reference
Arrhythmias Potassium voltage-gated channel subfamily H member 2 (Q12809) Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development
Hyperhidrosis Inward rectifier potassium channel 2 (P63252) Not Available Large-scale prediction and testing of drug activity on side-effect targets
Hyperhidrosis Potassium voltage-gated channel subfamily E member 2 (Q9Y6J6) Not Available Large-scale prediction and testing of drug activity on side-effect targets
Hyperhidrosis Sodium-dependent serotonin transporter (P31645) Not Available Large-scale prediction and testing of drug activity on side-effect targets
Palpitations Potassium voltage-gated channel subfamily E member 1 (P15382) Not Available Large-scale prediction and testing of drug activity on side-effect targets
Palpitations Potassium voltage-gated channel subfamily KQT member 1 (P51787) Not Available Large-scale prediction and testing of drug activity on side-effect targets
Sudden Cardiac Death Potassium voltage-gated channel subfamily H member 2 (Q12809) Sudden cardiac death due to long-QT syndrome [ ADR Type 2 ] Genetic and molecular basis of cardiac arrhythmias: impact on clinical management parts I and II
Sudden Cardiac Death Potassium voltage-gated channel subfamily KQT member 1 (P51787) Sudden cardiac death due to long-QT syndrome [ ADR Type 2 ] Genetic and molecular basis of cardiac arrhythmias: impact on clinical management parts I and II
Sudden Cardiac Death Sodium channel protein type 5 subunit alpha (Q14524) Sudden cardiac death due to long-QT syndrome [ ADR Type 2 ] Genetic and molecular basis of cardiac arrhythmias: impact on clinical management parts I and II
Torsade De Pointes Misshapen-like kinase(Mink) (Q8N4C8) Increased risk of drug-induced torsade de pointes. [ ADR Type 2 ] MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia
Torsade De Pointes Potassium voltage-gated channel subfamily E member 2 (MiRP1) (P00044) Increased risk of drug-induced torsade de pointes. [ ADR Type 2 ] MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia
Torsade De Pointes Potassium voltage-gated channel subfamily H member 2 (Q12809) Increased risk of drug-induced torsade de pointes [ ADR Type 2 ] MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia
Torsade De Pointes Potassium voltage-gated channel subfamily KQT member 1 (P51787) Increased risk of drug-induced torsade de pointes [ ADR Type 2 ] MiRP1 forms IKr potassium channels with HERG and is associated with cardiac arrhythmia

This panel provides information on metabolites and their ADRs along with references

Metabolite Toxicity Place of Metabolism Mechanism Reference

InAADR: Drug-Protein-ADRs database