Overview
11 DESCRIPTION Fesoterodine fumarate extended-release tablets contain fesoterodine fumarate. Fesoterodine is rapidly de-esterified to its active metabolite (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol, or 5-hydroxymethyl tolterodine, which is a muscarinic receptor antagonist.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Fesoterodine is a competitive muscarinic receptor antagonist. After oral administration, fesoterodine is rapidly and extensively hydrolyzed by nonspecific esterases to its active metabolite, 5-hydroxymethyl tolterodine, which is responsible for the antimuscarinic activity of fesoterodine. Muscarinic receptors play a role in contractions of urinary bladder smooth muscle. Inhibition of these receptors in the bladder is presumed to be the mechanism by which fesoterodine produces its effects. 12.2 Pharmacodynamics In a urodynamic study involving patients with involuntary detrusor contractions, the effects after the administration of fesoterodine on the volume at first detrusor contraction and bladder capacity were assessed.
Indications
- 1 INDICATIONS AND USAGE Fesoterodine fumarate extended-release tablets are indicated for the treatment of: Overactive bladder (OAB) in adults with symptoms of urge urinary incontinence, urgency, and frequency. ( 1.1 ) 1.1 Adult Overactive Bladder Fesoterodine fumarate extended-release tablets are indicated for the treatment of overactive bladder (OAB) in adults with symptoms of urge urinary incontinence, urgency, and frequency. Pediatric use information is approved for Pfizer Inc.’s TOVIAZ ® (fesoterodine fumarate) extended-release tablets. However, due to Pfizer Inc.
Common Doses
- 4 mg
- 8 mg
- 89 mL
- 29 mL
Dosage
2 DOSAGE AND ADMINISTRATION OAB in Adults : The recommended starting dosage is 4 mg orally once daily. Based upon individual response and tolerability, increase to the maximum dosage of 8 mg once daily. ( 2.1 ) Adult Patients with Renal Impairment : Refer to the full prescribing information for recommended dosage. ( 2.3 ) Dosage Modifications Due to Strong CYP3A4 Inhibitors : Refer to the full prescribing information for recommended dosage. ( 2.5 ) Administration : Swallow whole with liquid. Do not chew, divide, or crush. Take with or without food. ( 2.6 ) 2.
Contraindications
- 4 CONTRAINDICATIONS Fesoterodine fumarate extended-release tablets are contraindicated in patients with any of the following: known or suspected hypersensitivity to fesoterodine fumarate extended-release tablets or any of its ingredients, or to tolterodine tartrate tablets or tolterodine tartrate extended-release capsules [see Clinical Pharmacology (12.1) ] . Reactions have included angioedema [see Warnings and Precautions (5.1) ] . urinary retention [see Warnings and Precautions (5.2) ] gastric retention [see Warnings and Precautions (5.
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in labeling: Angioedema [see Warnings and Precautions (5.1) ] Urinary Retention [see Warnings and Precautions (5.2) ] Decreased Gastrointestinal Motility [see Warnings and Precautions (5.3) ] Most frequently reported adverse events with fesoterodine fumarate in adult patients with OAB (≥4%) were: dry mouth (placebo, 7%; fesoterodine fumarate 4 mg, 19%; fesoterodine fumarate 8 mg, 35%) and constipation (placebo, 2%; fesoterodine fumarate 4 mg, 4%; fesoterodine fumarate 8 mg, 6%). (6.
Interactions
- 7 DRUG INTERACTIONS 7.1 Antimuscarinic Drugs Co-administration of fesoterodine fumarate with other antimuscarinic agents that produce dry mouth, constipation, urinary retention, and other anticholinergic pharmacological effects may increase the frequency and/or severity of such effects. Anticholinergic agents may potentially alter the absorption of some concomitantly administered drugs due to anticholinergic effects on gastrointestinal motility. 7.