fes-oh-TER-o-deen

Therapeutic Classification: urinary tract antispasmodics

Pharmacologic Classification: anticholinergics

• Overactive bladder with symptoms of urinary frequency, urgency, and urge incontinence.
• Neurogenic detrusor overactivity.

• Acts as a competitive muscarinic receptor antagonist resulting in inhibition of cholinergically mediated bladder contraction.

• Decreased urinary frequency, urgency, and urge incontinence in overactive bladder.
• Increase in maximum cystometric bladder capacity in neurogenic detrusor overactivity.

Absorption: Rapidly absorbed following oral administration, but is rapidly converted to its active metabolite (bioavailability of metabolite 52%).

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP2D6 and CYP3A4 isoenzymes; the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers and may have significantly ↑ fesoterodine concentrations and an ↑ risk of adverse effects. 16% of active metabolite is excreted in urine, most of the remainder of inactive metabolites are renally excreted. 7% excreted in feces.

Half-life: 7 hr (following oral administration).

(plasma concentrations of active metabolite)

Contraindicated in:

• Hypersensitivity
• Urinary retention
• Significant bladder outlet obstruction (↑ risk of retention)
• Gastric retention
• ↓GI motility including severe constipation
• Severe hepatic impairment
• Uncontrolled narrow-angle glaucoma
• Pedi: eGFR <15 mL/min/1.73 m² or requiring dialysis (children 6 yr and >35 kg)
• Pedi: eGFR <30 mL/min/1.73 m² or requiring dialysis (children 6 yr and 25–35 kg).

Use Cautiously in:

• CCr <30 mL/min (dose adjustment required in adults)
• Treated narrow-angle glaucoma (use only if benefits outweigh risks)
• Myasthenia gravis
• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Safety and effectiveness not established in children <18 yr (overactive bladder) or <6 yr or <25 kg (neurogenic detrusor overactivity)
• Geri: ↑risk of anticholinergic side effects in patients >75 yr.

CV: tachycardia (dose related).

GI: dry mouth, constipation, nausea, upper abdominal pain.

GU: dysuria, urinary retention.

MS: back pain.

Neuro: dizziness, drowsiness, headache.
Misc: (INCLUDING ANGIOEDEMA)HYPERSENSITIVITY REACTIONS .

Drug-Drug:

• Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, and clarithromycin, ↑ levels and risk of toxicity; daily dose should not exceed 4 mg in adults and children 6 yr and >35 kg; avoid concurrent use in children 6 yr and 25–35 kg.
• Additive anticholinergic effects with other anticholinergic drugs, including antihistamines, phenothiazines, quinidine, disopyramide, and tricyclic antidepressants.
• May ↓ GI absorption of other drugs.

Overactive Bladder

• PO (Adults): 4 mg once daily initially; may ↑ to 8 mg/daily, if needed based on response and tolerability; Concurrent use of strong CYP3A4 inhibitors: Do not exceed 4 mg/day.

Neurogenic Detrusor Overactivity

• PO (Children 6 yr and >35 kg): 4 mg once daily, then ↑ to 8 mg once daily after 1 wk; Concurrent use of strong CYP3A4 inhibitors: Do not exceed 4 mg/day.
• PO (Children 6 yr and 25–35 kg): 4 mg once daily; ↑ to 8 mg once daily, if needed; Concurrent use of strong CYP3A4 inhibitors: Use not recommended.

(Generic available)

• Extended-release tablets: 4 mg; 8 mg;

• Assess for urinary urgency, frequency, and urge incontinence periodically during therapy.
• Monitor for signs and symptoms of angioedema (swelling of face, lips, tongue, and/or larynx). May occur with first or subsequent doses. Discontinue therapy and prove supportive therapy. Have epinephrine, corticosteroids, and resuscitation equipment available.

• May cause ↑ ALT and GGT.

• PO: Administer with liquid without regard to food.
  • DNC: Swallow extended-release tablets whole; do not break, crush, or chew.

• Instruct patient to take fesoterodine as directed. If a dose is missed, omit and begin taking again the next day; do not take 2 doses the same day. Advise patient to read the Patient Information sheet prior to initiation of therapy and with each Rx refill in case of changes.
• May cause drowsiness, dizziness, and blurred vision. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
• Advise patient to avoid alcohol; may increase drowsiness.
• Advise patient to use caution in hot environments; may cause decreased sweating and severe heat illness.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise patient to stop medication and notify health care professional if signs and symptoms of angioedema occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

• Decreased urinary frequency, urgency, and urge incontinence.
• Increase in maximum cystometric bladder capacity in neurogenic detrusor overactivity.

Toviaz