Description

Simple

A medication used to treat overactive bladder, associated with various conditions such as the sudden urge to urinate.

Clinical

An antimuscarinic agent used in the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

Overview

Fesoterodine is an antimuscarinic prodrug for the treatment of overactive bladder syndrome.

Pharmacology

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Pharmacodynamic

In-vivo the fesoteridine prodrug is broken down into its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), by plasma esterases. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic rec... Read more

Mechanism of action

Fesoterodine, once converted to its active metabolite, 5-hydroxymethyltolterodine, acts as a competitive antagonists at muscarinic receptors. This results in the inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Absorption

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine.
AUC (0,∞)= 49.5 ng·h/ ml
Bioavailability, 5-HMT = 52%

Protein binding

5-HMT: 50% to albumin and alpha1-acid glycoprotein

Volume of distribution

IV, 5-HMT: 169 L

Clearance

5-HMT, healthy subjects: 14.4 L/h5-HMT is also secreted into the nephron.

Half life

7-8 hours for the active metabolite 5-hydroxymethyl tolterodine

Route of elimination

Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite
Fecal: 7%
Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4

Toxicity

Rat, Oral, LD50: ~ 681 mg/kg
Mouse, Oral, LD50: ~ 316 mg/kg
Rat, Intravenous, NOAEL: 10 mg/kg
Mouse, Intravenous, NOAEL: 10 mg/kg

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Urinary Retention
      • Drugbank Id: DBCOND0001412
  • Regions: US
  • Patient Conditions:
      • Name: Gastric Retention
      • Drugbank Id: DBCOND0088112
  • Regions: US
  • Patient Conditions:
      • Name: Uncontrolled narrow-angle glaucoma
      • Drugbank Id: DBCOND0107497

Food Interactions

  • Take with or without food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Fesoterodine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1,10-Phenanthroline
The therapeutic efficacy of Fesoterodine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of Tachycardia can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Fesoterodine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
4-Methoxyamphetamine
4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
7-Nitroindazole
7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
Abacavir
Abacavir may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Abatacept
The metabolism of Fesoterodine can be increased when combined with Abatacept.
Abediterol
The risk or severity of Tachycardia can be increased when Fesoterodine is combined with Abediterol.
Abiraterone
The metabolism of Fesoterodine can be decreased when combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Acebutolol
The metabolism of Fesoterodine can be decreased when combined with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Acepromazine
Acepromazine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
Aceprometazine
Aceprometazine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.
Acetaminophen
Acetaminophen may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
2 References
  1. 1 . Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x.PubMed: 21545485
  2. 2 . Malhotra B, Gandelman K, Sachse R, Wood N, Michel MC: The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9.PubMed: 19835561