Pronunciation: FES-oh-TER-oh-deen FUE-ma-rate
- Tablets, ER 4 mg
- Tablets, ER 8 mg
Contracts urinary bladder smooth muscles.
Well absorbed following oral administration. Rapidly and extensively metabolized to its active metabolite, which is 52% bioavailable. T max reached in approximately 5 h. C max ranges from 1.89 to 3.98 ng/mL in extensive metabolizers and 3.45 to 6.9 ng/mL in poor metabolizers.
Protein binding of the active metabolite is approximately 50%, primarily bound to albumin and alpha-1 acid glycoprotein. Mean steady-state Vd of the active metabolite is 169 L.
Rapidly and extensively metabolized to its active metabolite. The active metabolite is metabolized in the liver by CYP2D6 and CYP3A4 isozymes to metabolites that do not have muscarinic activity.
Approximately 70% of the administered dose is recovered in the urine as the active metabolite and smaller amounts are recovered in the feces. The terminal half-life of the active metabolite is approximately 4 h following IV administration and 7 h following oral administration.
Special PopulationsRenal Function Impairment
Plasma concentrations of the active metabolite are increased in patients with renal impairment. No dosage adjustment is recommended in patients with mild or moderate renal insufficiency. Doses greater than 4 mg are not recommended in patients with severe renal insufficiency (CrCl less than 30 mL/min).Hepatic Function Impairment
Plasma concentrations of the active metabolite are increased in patients with hepatic impairment. No dosage adjustment is recommended in patients with mild or moderate hepatic impairment. There are no data for patients with severe hepatic impairment; therefore, administration is not recommended.
Indications and Usage
Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.
Urinary retention; gastric retention; uncontrolled narrow-angle glaucoma; hypersensitivity to any component of the product.
Dosage and AdministrationAdults
PO Start with 4 mg once daily. Based upon response and tolerability, the dose may be increased to 8 mg once daily.Dosage Modification
PO Patients with severe renal insufficiency (CrCl less than 30 mL/min) or those taking potent CYP3A4 inhibitors (eg, clarithromycin, itraconazole, ketoconazole) should not receive more than 4 mg daily. Administration is not recommended in patients with severe hepatic impairment.
- May be administered without regard to meals.
- The ER tablets should be swallowed whole and not broken, crushed, or chewed.
Store at 59° to 86°F. Protect from moisture.
Drug InteractionsAnticholinergic agents
Frequency and severity of adverse reactions may be increased.CYP2D6 inhibitors
Plasma concentrations of the active metabolite of fesoterodine may be increased in poor metabolizers for CYP2D6.CYP3A4 inducers (eg, rifampin)
Plasma concentrations of the active metabolite of fesoterodine may be reduced, decreasing the clinical effect.Potent CYP3A4 inhibitors (clarithromycin, itraconazole, ketoconazole)
Plasma concentrations of the active metabolite of fesoterodine may be elevated, increasing the pharmacologic effects and adverse reactions.
Laboratory Test Interactions
None well documented.
Dry eyes (4%); dry throat (2%).
Dry mouth (35%); constipation (6%); dyspepsia, nausea (2%); upper abdominal pain (1%); diverticulitis, irritable bowel syndrome.
UTI (4%); dysuria (2%); urinary retention (1%).
Increased ALT, increased gamma-glutamyltransferase (1%).
Back pain (2%).
Upper respiratory tract infection (3%); cough (2%).
Peripheral edema (1%).
Category C .
Safety and efficacy not established.
No overall differences is safety and efficacy were found in patients 65 yr of age and older compared with younger patients.
Dosages greater than 4 mg once daily are not recommended in patients with severe renal insufficiency.
Administration is not recommended in patients with severe hepatic impairment.
Bladder outlet obstruction
Administer with caution in patients with clinically important bladder outlet obstruction because of risk of urinary retention.
Special risk patients
Use with caution in patients with decreased GI motility (eg, severe constipation), controlled narrow-angle glaucoma, or myasthenia gravis.
Severe anticholinergic effects.
- Instruct patients that product may be administered without regard to meals.
- Instruct patients to swallow the medication whole and not divide, crush, or chew the tablets.
- Inform patients that blurred vision may occur and to exercise caution until the effects of the drug on the patient have been determined.
- Inform patients that heat prostration due to decreased sweating can occur when patients are exposed to a hot environment.
- Instruct patients to avoid alcohol because the risk of drowsiness may be increased.
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