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QuickView for Terfenadine (compound)
PubChem
| Name: | Terfenadine |
|---|---|
| PubChem Compound ID: | 5405 |
| Description: | A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. |
| Molecular formula: | C32H41NO2 |
| Molecular weight: | 471.673 g/mol |
| Synonyms: |
RMI-9918; Seldane (TN); MDL 9918; Triludan; DivK1c_001011; alpha-(p-tert-Butylphenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Terfenadine (JAN/USAN); alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; NSC665802; Nebralin.
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DrugBank
Identification
| Name: | Terfenadine |
|---|---|
| Name (isomeric): | DB00342 |
| Drug Type: | small molecule |
| Description: | A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. |
| Synonyms: |
Ternadin
|
| Brand: | Allerplus, Terdin, Teldanex, Cyater, Seldane, Aldaban, Terfex, Teldane, Triludan |
| Category: | Antihistamines, Antiarrhythmic Agents, Anti-Allergic Agents, Histamine H1 Antagonists, Non-Sedating |
| CAS number: | 50679-08-8 |
Pharmacology
| Indication: | For the treatment of allergic rhinitis, hay fever, and allergic skin disorders. |
|---|---|
| Pharmacology: | Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. The active metabolite of terfenadine is fexofenadine. |
| Mechanism 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 dep...
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| Absorption: | On the basis of a mass balance study using 14C labeled terfenadine the oral absorption of terfenadine was estimated to be at least 70% |
| Protein binding: | 70% |
| Biotransformation: | Hepatic |
| Half Life: | 3.5 hours |
| 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) |
| Affected organisms: | Humans and other mammals |
Interactions
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Targets
Enzymes
Transporters
