Fesoterodine Fumarate
Fesoterodine Fumarate Prescribing Information
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 Adult Overactive BladderFesoterodine 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.'s marketing exclusivity rights, this drug product is not labeled with that pediatric information.
- 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 Recommended Dosage for Adult Patients With OABThe recommended starting dosage of fesoterodine fumarate extended-release tablets in adults is 4 mg orally once daily. Based upon individual response and tolerability, increase to the maximum dosage of fesoterodine fumarate extended-release tablets 8 mg once daily. For administration instructions,
see Dosage and Administration . - Adult Patients with Renal Impairment: Refer to the full prescribing information for recommended dosage. ()
2.3 Recommended Dosage in Adult Patients with Renal ImpairmentThe recommended dosage of fesoterodine fumarate extended-release tablets in adult patients with renal impairment is described in Table 1
[see Use in Specific Populations ].For administration instructions,see Dosage and Administration.Table 1:Fesoterodine fumarate extended-release tablets Recommended Dose in Adult Patients With Renal Impairment (Administered Orally Once Daily)Estimated Creatinine Clearance1Recommended DoseCLcr 30 to 89 mL/min 8 mg CLcr 15 to 29 mL/min 4 mg CLcr <15 mL/min 4 mg 1Calculate CLcr using the Cockcroft-Gault formula
- Dosage Modifications Due to Strong CYP3A4 Inhibitors: Refer to the full prescribing information for recommended dosage. ()
2.5 Fesoterodine fumarate extended-release tablets Dosage Modifications Due to Strong CYP3A4 InhibitorsAdult Patients with OABThe maximum recommended dosage is fesoterodine fumarate extended-release tablet 4 mg orally once daily in adult patients taking strong CYP3A4 inhibitors
[see Drug Interactions (7.2) and Clinical Pharmacology (12.3)]. For administration instructions,see Dosage and Administration. - Administration: Swallow whole with liquid. Do not chew, divide, or crush. Take with or without food. ()
2.6 Administration InstructionsSwallow fesoterodine fumarate extended-release tablets whole with liquid. Do not chew, divide, or crush. Take with or without food
[see Clinical Pharmacology ].Pediatric use information is approved for Pfizer Inc.'s TOVIAZ®(fesoterodine fumarate) Extended-Release Tablets. However, due to Pfizer Inc.'s marketing exclusivity rights, this drug product is not labeled with that pediatric information.
Extended-release tablets:
- Fesoterodine fumarate extended-release tablets, 4 mg are light blue, oval, biconvex film-coated; debossed with ´´F4´´ on one side and plain on other side.
- Fesoterodine fumarate extended-release tablets, 8 mg are blue, oval, biconvex film-coated; debossed with ´´F8´´ on one side and plain on other side.
There are no available data with the use of fesoterodine fumarate extended-release tablets in pregnant women and adolescents to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of fesoterodine to pregnant mice and rabbits during organogenesis resulted in fetotoxicity at maternal exposures that were 6 and 3 times
No dose-related teratogenicity was observed in reproduction studies performed in mice and rabbits. In mice at 6 to 27 times the expected exposure at the maximum recommended human dose (MRHD)of 8 mg based on AUC (75 mg/kg/day, oral), increased resorptions and decreased live fetuses were observed. One fetus with cleft palate was observed at each dose (15, 45, and 75 mg/kg/day), at an incidence within the background historical range. In rabbits treated at 3 to 11 times the MRHD (27 mg/kg/day, oral), incompletely ossified sternebrae (retardation of bone development) and reduced survival were observed in fetuses. In rabbits at 9 to 11 times the MRHD (4.5 mg/kg/day, subcutaneous), maternal toxicity and incompletely ossified sternebrae were observed in fetuses (at an incidence within the background historical range). In rabbits at 3 times the MRHD (1.5 mg/kg/day, subcutaneous), decreased maternal food consumption in the absence of any fetal effects was observed. Oral administration of 30 mg/kg/day fesoterodine to mice in a pre- and post-natal development study resulted in decreased body weight of the dams and delayed ear opening of the pups. No effects were noted on mating and reproduction of the F1 dams or on the F2 offspring.
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 (. Reactions have included angioedema)]
12.1 Mechanism of ActionFesoterodine 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.
[see Warnings and Precautions ()]5.1 AngioedemaAngioedema of the face, lips, tongue, and/or larynx has been reported with fesoterodine. In some cases, angioedema occurred after the first dose; however, cases have been reported to occur hours after the first dose or after multiple doses. Angioedema associated with upper airway swelling may be life-threatening.
Fesoterodine fumarate extended-release tablets are contraindicated in patients with a known or suspected hypersensitivity to fesoterodine fumarate extended-release tablets or any of its ingredients
[see Contraindications ].If involvement of the tongue, hypopharynx, or larynx occurs, fesoterodine should be promptly discontinued and appropriate therapy and/or measures to ensure a patent airway should be promptly provided. - urinary retention [see Warnings and Precautions ()]
5.2 Urinary Retention in Adult Patients With Bladder Outlet ObstructionThe use of fesoterodine fumarate extended-release tablets, like other antimuscarinic drugs, in patients with clinically significant bladder outlet obstruction, including patients with urinary retention, may result in further urinary retention and kidney injury. The use of fesoterodine fumarate extended-release tablets are not recommended in patients with clinically significant bladder outlet obstruction, and is contraindicated in patients with urinary retention
[see Contraindications and Adverse Reactions ]. - gastric retention [see Warnings and Precautions ()]
5.3 Decreased Gastrointestinal MotilityFesoterodine fumarate extended-release tablets are associated with decreased gastric motility. Fesoterodine fumarate extended-release tablets are contraindicated in patients with gastric retention
[see Contraindications ].The use of fesoterodine fumarate extended-release tablets are not recommended in patients with decreased gastrointestinal motility, such as those with severe constipation. - uncontrolled narrow-angle glaucoma [see Warnings and Precautions ()]
5.4 Worsening of Narrow-Angle GlaucomaFesoterodine fumarate extended-release tablets can worsen controlled narrow-angle glaucoma. Fesoterodine fumarate extended-release tablets are contraindicated in patients with uncontrolled narrow-angle glaucoma
[see Contraindications ].Fesoterodine fumarate extended-release tablets should be used with caution in patients being treated for narrow-angle glaucoma.
- Angioedema: Promptly discontinue fesoterodine fumarate extended-release tablets and provide appropriate therapy. (5.1)
- Urinary Retention: Fesoterodine fumarate extended-release tablets are not recommended in patients with clinically significant bladder outlet obstruction because of the risk of urinary retention. (5.2)
- Decreased Gastrointestinal Motility: Fesoterodine fumarate extended-release tablets are not recommended for use in patients with decreased gastrointestinal motility, such as those with severe constipation. (5.3)
- Worsening of Narrow -Angle Glaucoma: Use fesoterodine fumarate extended-release tablets with caution in patients being treated for narrow-angle glaucoma. (5.4)
- Central Nervous System Effects: Somnolence has been reported with fesoterodine fumarate extended-release tablets. Advise patients not to drive or operate heavy machinery until they know how fesoterodine fumarate extended-release tablets affects them. (5.5)
- Worsening of Myasthenia Gravis Symptoms: Use fesoterodine fumarate extended-release tablets with caution in patients with myasthenia gravis. (5.6)