Approved October 31, 2008

FESOTERODINE FUMARATE
(FDA Category 1S)

TOVIAZ (Pfizer Labs) is a competitive muscarinic receptor antagonist. The presumed mechanism of action is inhibition of muscarinic receptors in the bladder by fesoterodine's active metabolite.

DOSING INFORMATION: The recommended starting dose is 4 mg orally once daily. The dose may be increased to 8 mg once daily based on patient response and tolerability.

PHARMACOKINETICS: Fesoterodine cannot be detected in the plasma and is rapidly and extensively hydrolyzed to its active metabolite, 5-hydroxymethyl tolterodine. The absolute bioavailability of 5-hydroxymethyl tolterodine after oral administration is 52%. Maximum plasma concentrations of 5-hydroxymethyl tolterodine are reached approximately 5 hours after oral dosing. The Vd of 5-hydroxymethyl tolterodine following intravenous administration is 169 L and 5-hydroxymethyl tolterodine is approximately 50% bound to plasma proteins. 5-hydroxymethyl tolterodine is eliminated by renal excretion (70%) and in the feces (7%). The elimination half-life of 5-hydroxymethyl tolterodine after oral administration is approximately 7 hours.

CAUTIONS: Contraindications to fesoterodine include urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Use with caution in patients with bladder outlet obstruction, decreased gastrointestinal motility, controlled narrow-angle glaucoma, reduced hepatic function, myasthenia gravis, reduced renal function and in patients receiving concomitant CYP3A4 inhibitors. The most commonly reported adverse effects include dry mouth and constipation.

FDA APPROVED INDICATIONS: Indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.