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Terfenadine
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DRUG INFO Terfenadine
Drug Name:
Terfenadine
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 depression is minimal.
Drug Category: Antiarrhythmic Agents; Anti-allergic Agents; Antihistamines; ATC:R06AX12
Brand Names/Synonyms: Aldaban; Allerplus; Cyater; MDL-9918; Nebralin; RMI 9918; Seldane; Teldane; Teldanex; Terdin; Terfenadine; Terfex; Ternadin; Triludan
Dosage Forms: Oral tablets
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%
Interactions:
DrugBank: Interactions for Terfenadine
Interactions for Terfenadine:
Ketoconazole
Spontaneous adverse reaction reports of patients taking concomitant ketoconazole with recommended doses of
terfenadine demonstrate QT interval prolongation and rare serious cardiac events, e.g. death, cardiac arrest, and
ventricular arrhythmia including torsades de pointes. Pharmacokinetic data indicate that ketoconazole markedly
inhibits the metabolism of terfenadine, resulting in elevated plasma terfenadine levels. Presence of unchanged
terfenadine is associated with statistically significant prolongation of the QT and QTc intervals.Concomitant
administration of ketoconazole and terfenadine is contraindicated.
Itraconazole
Torsades de pointes and elevated parent terfenadine levels have been reported during concomitant use of
terfenadine and itraconazole in clinical trials of itraconazole and from foreign post-marketing sources. One death
has also been reported from foreign post- marketing sources. Concomitant administration of itraconazole and
terfenadine is contraindicated.
Due to the chemical similarity of other azole-type antifungal agents (including fluconazole, metronidazole, and
miconazole) to ketoconazole, and itraconazole, concomitant use of these products with terfenadine is not recommended
pending full examination of potential interactions.
Macrolides
Clinical drug interaction studies indicate that erythromycin and clarithromycin can exert an effect on terfenadine
metabolism by a mechanism which may be similar to that of ketoconazole, but to a lesser extent. Although erythromycin
measurably decreases the clearance of the terfenadine acid metabolite, its influence on terfenadine plasma levels is
still under investigation. A few spontaneous accounts of QT interval prolongation with ventricular arrhythmia
including torsades de pointes, have been reported in patients receiving erythromycin or troleandomycin.
Concomitant administration of terfenadine with clarithromycin, erythromycin, or troleandomycin is
contraindicated: Pending full characterization of potential interactions, concomitant administration of
terfenadine with other macrolide antibiotics, including azithromycin, is not recommended. Studies to evaluate
potential interactions of terfenadine with azithromycin are in progress.
Chemical IUPAC Name: 4-[4-(hydroxy-diphenyl-methyl)-1-piperidyl]-1-(4-tert-butylphenyl)-butan-1-ol
Chemical Formula: C32H41NO2
Half Life: 3.5 hours
Drug Type: Approved Drug
# Accession No: APRD00606
CAS Registry Number: 50679-08-8
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Terfenadine News (When available)
Expert works to fix drug development Jan 14, 2006 Arizona Republic, ...effectiveness of drugs. In the 1990s, he uncovered the toxicity of the antihistamine Seldane, which led to a ban on the product. At the ...
FDA Approves EMEND® (aprepitant), in Combination with Other ... Jan 11, 2006 Biotech Intelligence (press release), Patients should not take EMEND with ORAP® (pimozide), SELDANE® (terfenadine), HISMANAL® (astemizole) or PROPULSID® (cisapride) as EMEND may cause serious ...
FDA Approves EMEND(R) (aprepitant), in Combination with Other ... Jan 11, 2006 Business Wire (press release), Patients should not take EMEND with ORAP(R) (pimozide), SELDANE(R) (terfenadine), HISMANAL(R) (astemizole) or PROPULSID(R) (cisapride) as EMEND may cause ...
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