Terfenadine

CAS No:
50679-08-8 Category:
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 50679-08-8
  • AHFC code:
  • Synonyms: Ternadin
  • ATC Code: R06AX12
  • Chemical Formula: C52H74N16O15S2
  • Molecular Weight: 471.6734
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00342 (APRD00606)
  • SMILES: CC(C)(C)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1
  • InChl: GUGOEEXESWIERI-UHFFFAOYSA-N
  • PubChem: 5405
  • IUPAC: 1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol

Additional Details

Indication:
For the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
Pharmacodynamics:
Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. The active metabolite of terfenadine is fexofenadine.
Mode of Action:
Terfenadine competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of terfenadine to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier, CNS depression is minimal.
Metabolism:
Hepatic
Toxicity:
Mild (e.g., headache, nausea, confusion), but adverse cardiac events including cardiac arrest, ventricular arrhythmias including torsades de pointes and QT prolongation have been reported. LD50=mg/kg (orally in mice)
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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