Product Name

Terfenadine

CAS Number

50679-08-08

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Product Name:
Terfenadine
CAS Number:
50679-08-08
Indication:
For the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
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.

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.

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)

IUPAC:
1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol
ATC:
R06AX12
PubChem:
5405
DrugBank:
DB00342 (APRD00606)
Formula:
C52H74N16O15S2
Molecular Mass:
471.6734
Synonyms:
Ternadin
SMILES:
CC(C)(C)C1=CC=C(C=C1)C(O)CCCN1CCC(CC1)C(O)(C1=CC=CC=C1)C1=CC=CC=C1
InChi:
GUGOEEXESWIERI-UHFFFAOYSA-N

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