Fesoterodinefumarate

Chemical properties

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The Uses of Fesoterodinefumarate

Fesoterodine fumarate (Toviaz) is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist. Fesoterodine fumarate (Toviaz) is used to treat the symptoms of overactiv

The Uses of Fesoterodinefumarate

(R)-Fesoterodine Fumarate is a muscarinic receptor antagonist for the treatment of Lower Urininary Tract Symptoms (LUTS). It is very similar to Tolterodine (T535800).

What are the applications of Application

(R)-Fesoterodine Fumarate is a mAChR M antagonist that blocks acetylcholine binding

Clinical Use

Antimuscarinic:
Symptomatic treatment of urinary incontinence, frequency or urgency

Drug interactions

Potentially hazardous interactions with other drugs
 Anti-arrhythmics: increased risk of antimuscarinic side effects with disopyramide.
 Antifungals: dose reduction advised with itraconazole and ketoconazole.
 Antivirals: dose reduction advised with atazanavir, indinavir, ritonavir and saquinavir.
 Induction of CYP3A4 may lead to subtherapeutic plasma levels. Concomitant use with CYP3A4 inducers (e.g. carbamazepine, rifampicin, phenobarbital, phenytoin, St John's Wort) is not recommended.
 Co-administration of a potent CYP2D6 inhibitor may result in increased exposure and adverse events. A dose reduction to 4 mg may be needed' 

Metabolism

Rapidly and extensively hydrolysed to its active metabolite. The active metabolite is further metabolised in the liver to its carboxy, carboxy-N-desisopropyl, and N-desisopropyl metabolites via two major pathways involving CYP2D6 and CYP3A4. None of these metabolites contribute significantly to the antimuscarinic activity of fesoterodine. Approximately 70% of an oral dose of fesoterodine is recovered in the urine as metabolites, and a smaller amount in the faeces.