Fesoterodine

412.58500

411.58

621G617227

DTXSID80182853

C74138

G04BD11|G - Genito urinary system and sex hormones

49.77000

5.48800

1.043g/cm3

518.9ºC

267.6ºC

Highly soluble

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

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

Like most anticholinergic agents, fesoterodine has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. Fesoterodine is metabolized in the liver via the cytochrome P450 system (CYP 2D6 and 3A4). Its relative safety may relate to its relatively low daily dose.

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

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).|FDA Label|Treatment of the symptoms (increased urinary frequency and / or urgency and / or urgency incontinence) that may occur in patients with overactive-bladder syndrome.

Fesoterodine is an anticholinergic and antispasmotic agent used to treat urinary incontinence and overactive bladder syndrome. Fesoterodine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Anticholinergic Agents

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 receptors. Therefore, acting as a competitive muscarinic receptor antagonist, fesoterodine ultimately acts to decrease the detrusor pressure by its muscarinic antagonism, thereby decreasing bladder contraction and consequently, the urge to urinate.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system. (See all compounds classified as Muscarinic Antagonists.)|Drugs used in the treatment of urogenital conditions and diseases such as URINARY INCONTINENCE; PROSTATIC HYPERPLASIA; and ERECTILE DYSFUNCTION. (See all compounds classified as Urological Agents.)

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,∞)= 49.5 ng·h/ ml Bioavailability, 5-HMT = 52%|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|IV, 5-HMT: 169 L|5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.

Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites

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

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.

fesoterodine

Human drugs -> Toviaz -> EMA Drug Category|Urologicals -> Human pharmacotherapeutic group