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Terfenadine



Terfenadine
Systematic (IUPAC) name
4-[4-(hydroxy-diphenyl-methyl)-1-piperidyl]-
1-(4-tert-butylphenyl)-butan-1-ol
Identifiers
CAS number 50679-08-8
ATC code R06AX12
PubChem 5405
DrugBank APRD00606
Chemical data
Formula C32H41NO2 
Mol. mass 471.673 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 70%
Metabolism  ?
Half life 3.5 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was marketed under various brand names including Seldane in the United States, Triludan in the United Kingdom, and Teldane in Australia. It was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation.

Additional recommended knowledge

Terfenadine is a prodrug, generally completely metabolised to the active form fexofenadine by intestinal CYP3A4. Terfenadine itself, however, has a cardiotoxic effect and may be absorbed and reach myocytes if the patient is concurrently taking a CYP3A4 inhibitor (e.g. erythromycin, grapefruit juice).

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Terfenadine". A list of authors is available in Wikipedia.
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