fesoterodine

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

Therapeutic effects:

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

Pharmacokinetics ⬆ ⬇

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).

Time/Action Profile ⬆ ⬇

(plasma concentrations of active metabolite)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	5 hr	24 hr

Contraind./Precautions ⬆ ⬇

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.

Adv. Reactions/Side Effects ⬆ ⬇

CV: tachycardia (dose related)

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

GU: dysuria, urinary retention

MS: back pain

Neuro: dizziness, drowsiness, headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

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.

Route/Dosage ⬆ ⬇

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.

Renal Impairment

PO (Adults ): CCr <30 mL/min: 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.

Renal Impairment

PO (Children ≥6 yr and >35 kg): eGFR 15–29 mL/min/1.73 m²: Do not exceed 4 mg/day; eGFR <15 mL/min/1.73 m² or requiring dialysis: Use not recommended

Renal Impairment

PO (Children ≥6 yr and 25–35 kg): eGFR 30–89 mL/min/1.73 m²: Do not exceed 4 mg/day; eGFR <30 mL/min/1.73 m² or requiring dialysis: Use not recommended

Availability ⬆ ⬇

(Generic available)

Extended-release tablets: 4 mg; 8 mg

Assessment ⬆ ⬇

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.

Lab Test Considerations:

May cause ↑ ALT and GGT.

Implementation ⬆ ⬇

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

Patient/Family Teaching ⬆ ⬇

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.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆