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Fesoterodine

Pronunciation

(fes oh TER oh deen)

Index Terms

  • FESO
  • Fesoterodine Fumarate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Extended Release 24 Hour, Oral, as fumarate:

Toviaz: 4 mg, 8 mg [contains fd&c blue #2 aluminum lake, soybean lecithin]

Brand Names: U.S.

  • Toviaz

Pharmacologic Category

  • Anticholinergic Agent

Pharmacology

Fesoterodine acts as a prodrug and is converted to an active metabolite, 5-hydroxymethyl tolterodine (5-HMT); 5-HMT is responsible for fesoterodine’s antimuscarinic activity and acts as a competitive antagonist of muscarinic receptors.

Urinary bladder contractions are mediated by muscarinic receptors; fesoterodine inhibits the receptors in the bladder preventing symptoms of urgency and frequency.

Absorption

Well absorbed

Distribution

IV: 5-HMT: Vd: 169 L

Metabolism

Fesoterodine is rapidly and extensively metabolized to its active metabolite (5-hydroxymethyl tolterodine; 5-HMT) by nonspecific esterases; 5-HMT is further metabolized via CYP2D6 and CYP3A4 to inactive metabolites.

Excretion

Urine (~70%; 16% as 5-HMT, ~53% as inactive metabolites); feces (7%)

Time to Peak

Plasma: 5-HMT: ~5 hours; Cmax higher in poor CYP2D6 metabolizers

Half-Life Elimination

~7 hours

Protein Binding

5-HMT: ~50% (primarily to albumin and alpha1-acid glycoprotein)

Special Populations: Renal Function Impairment

Plasma concentrations of the active metabolite are increased in patients with renal impairment.

Special Populations: Hepatic Function Impairment

Plasma concentrations of the active metabolite are increased in patients with hepatic impairment.

Use: Labeled Indications

Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence.

Contraindications

Hypersensitivity to fesoterodine or tolterodine (both are metabolized to 5-hydroxymethyl tolterodine) or any component of the formulation; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma

Dosing: Adult

Overactive bladder: Oral: 4 mg once daily; may be increased to 8 mg once daily based on individual response and tolerability

Dosing adjustment for concomitant strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin): 4 mg once daily; maximum dose: 4 mg once daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute: 4 mg once daily; maximum dose: 4 mg once daily

Dosing: Hepatic Impairment

Mild-to-moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Use is not recommended; has not been studied.

Administration

May be administered with or without food. Swallow whole; do not chew, crush, or divide.

Dietary Considerations

May be taken with or without food.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Protect from moisture.

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Alcohol (Ethyl): May enhance the CNS depressant effect of Fesoterodine. Monitor therapy

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP2D6 Inhibitors: May increase serum concentrations of the active metabolite(s) of Fesoterodine. Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase serum concentrations of the active metabolite(s) of Fesoterodine. Management: Avoid fesoterodine doses greater than 4 mg daily in adult patients who are also receiving strong CYP3A4 inhibitors. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Adverse Reactions

>10%: Gastrointestinal: Xerostomia (19% to 35%; dose-related)

1% to 10%:

Cardiovascular: Peripheral edema (1%)

Central nervous system: Insomnia (1%)

Dermatological: Skin rash (1%)

Endocrine & metabolic: Increased gamma-glutamyl transferase (1%)

Gastrointestinal: Constipation (4% to 6%), dyspepsia (2%), nausea (1% to 2%), abdominal pain (1%)

Genitourinary: Urinary tract infection (3% to 4%), dysuria (1% to 2%), urinary retention (1%)

Hepatic: Increased serum ALT (1%)

Neuromuscular & skeletal: Back pain (1% to 2%)

Ophthalmic: Dry eye syndrome (1% to 4%)

Respiratory: Upper respiratory tract infection (2% to 3%), cough (1% to 2%), dry throat (1% to 2%)

<1% (Limited to important or life-threatening): Angina pectoris, angioedema, diverticulitis, gastroenteritis, heat exhaustion, hypersensitivity reaction, irritable bowel syndrome, prolonged Q-T interval on ECG

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema: Cases of angioedema involving the face, lips, tongue, and/or larynx have been reported. Discontinue immediately if tongue, hypopharynx, or larynx are involved.

• CNS effects: Anticholinergics may cause drowsiness, dizziness, headache, and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Dose reduction or discontinuation should be considered if CNS effects occur.

• Heat prostration: May occur in the presence of increased environmental temperature; use caution in hot weather and/or exercise.

Disease-related concerns:

• Bladder flow obstruction: Use with caution in patients with bladder flow obstruction; may increase the risk of urinary retention.

• Gastrointestinal obstructive disorders: Use with caution in patients with decreased GI motility or gastrointestinal obstructive disorders (ie, pyloric stenosis); may increase the risk of gastric retention.

• Glaucoma: Use with caution in patients with controlled (treated) narrow-angle glaucoma.

• Hepatic impairment: No dosing adjustments recommended for patients with mild-or-moderate hepatic impairment. No studies have been performed in patients with severe hepatic impairment (Child-Pugh class C); use is not recommended in this population.

• Myasthenia gravis: Use with caution in patients with myasthenia gravis.

• Renal impairment: Use with caution in patients with renal impairment. Dose adjustment recommended in patients with severe renal impairment (Clcr <30 mL/minute). There are no dosing adjustments for patients with mild-to-moderate renal impairment.

Concurrent drug therapy issues:

• High potential for interactions: Doses >4 mg are not recommended in patients receiving strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, clarithromycin). No dosing adjustments are recommended in patients receiving moderate CYP3A4 inhibitors (eg, erythromycin, fluconazole, diltiazem, verapamil, grapefruit juice).

• Sedatives: CNS effects may be potentiated when used with other sedative drugs or ethanol.

Special populations:

• Elderly: Risk of adverse effects may be increased in elderly patients.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse effects have been observed in some animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dry mouth or constipation. Have patient report immediately to prescriber lack of sweat, difficult urination, blurred vision, or swelling of arms or legs (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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