Fesoterodine

Therapeutic Class
 Anticholinergic Agent
Indications

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

Overactive bladder:

Oral: 4 mg once daily.
Doses in Renal impairment

Mild-to-moderate renal impairment (Clcr 30-80 mL/minute): No dose adjustment is recommended.

Severe renal impairment (Clcr <30 mL/minute): Maximum dose: 4 mg.
Doses in Hepatic impairment

Moderate hepatic impairment (Child-Pugh class B): No dose adjustment is recommended.

Severe hepatic impairment (Child-Pugh class C): Use is not recommended; not studied in severe impairment.
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.
Warnings / Precautions

Angioedema, Heat prostration, Bladder flow obstruction, Gastrointestinal obstructive disorders, Glaucoma, Hepatic impairment, Myasthenia gravis, Renal impairment, potent CYP3A4 inhibitors concurrent drug therapy.
Anticholinergics may cause drowsiness 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).
Adverse Reactions

Gastrointestinal: Xerostomia, Constipation, dyspepsia, nausea, abdominal pain
Central nervous system: Insomnia
Dermatological: Rash
Genitourinary: Urinary tract infection, dysuria, urinary retention
Hepatic: ALT increased, GGT increased
Neuromuscular & skeletal: Back pain
Ocular: Dry eyes
Respiratory: Upper respiratory tract infection, cough, dry throat
Miscellaneous: Peripheral edema

Very Rare: Angina, angioedema, blurred vision, chest pain, diverticulitis, gastroenteritis, heart rate increased, heat prostration, irritable bowel syndrome, QTc prolongation
Food Interactions

Ethanol: Adverse effects may be potentiated
Mechanism of Actions

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.
Pharmacodynamics

Absorption: Well absorbed

Distribution: I.V.: 5-HMT: Vd: 169 L

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

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.

Bioavailability: 5-HMT: 52%

Half-life elimination: ~7 hours

Time to peak, plasma: 5-HMT: ~5 hours; Cmax higher in poor CYP2D6 metabolizers

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

May be administered with or without food.

Swallow whole, do not chew, crush, or divide.
Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Lactation

Excretion in breast milk unknown/not recommended.
ATC Classification
 G04BD11
GenericPedia Classification
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