Terfenadine

What is Terfenadine

NOTE: This drug is discontinued in the U.S.

Terfenadine was a non-sedating antihistamine (H1-blocker) that is similar in structure to astemizole. Terfenadine, however, had a much shorter duration of action.

Both agents were structurally similar to haloperidol, a butyrophenone antipsychotic. Interestingly, all 3 agents have been associated with torsade de pointes (TdP).

Unlike other first-generation antihistamines, therapeutic doses of terfenadine produce insignificant anticholinergic activity or sedation, perhaps due to poor penetration of the drug into the CNS.

Terfenadine was originally approved by the FDA in May 1985 but was subsequently withdrawn in February 1998 due to its risk of causing cardiac arrhythmias.

Indications

  • allergic rhinitis

For symptomatic relief of seasonal allergic rhinitis

Side Effects

  1. anxiety
  2. dizziness
  3. drowsiness
  4. headache
  5. hypotension
  6. insomnia
  7. nausea
  8. QT prolongation
  9. restlessness
  10. torsade de pointes
  11. ventricular tachycardia
  12. vomiting
  13. xerostomia

Monitoring Parameters

  • ECG
  • LFTs

Contraindications

  • asthma
  • breast-feeding
  • cardiac disease
  • children
  • driving or operating machinery
  • geriatric
  • hepatic disease
  • infants
  • neonates
  • pregnancy
  • QT prolongation
  • renal disease
  • renal impairment
  • torsade de pointes

Interactions

  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amprenavir
  • Atazanavir
  • Atazanavir; Cobicistat
  • Cisapride
  • Clomipramine
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Desipramine
  • Dextromethorphan; Quinidine
  • Disopyramide
  • Doxepin
  • Fosamprenavir
  • Heparin
  • Imipramine
  • Indinavir
  • Lanreotide
  • Levomethadyl
  • Lopinavir; Ritonavir
  • Nelfinavir
  • Nortriptyline
  • Ombitasvir; Paritaprevir; Ritonavir
  • Pentamidine
  • Perphenazine; Amitriptyline
  • Procainamide
  • Protease inhibitors
  • Protriptyline
  • Quinidine
  • Quinine
  • Ritonavir
  • Rufinamide
  • Saquinavir
  • Sparfloxacin
  • Telaprevir
  • Telithromycin
  • Thioridazine
  • Tipranavir
  • Tricyclic antidepressants
  • Trimipramine
  • Voriconazole
  • Zileuton
  • Ziprasidone
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