Fesoterodine Fumarate
Indications
Fesoterodine Fumarate is used for:
Overactive bladder with symptoms of urge urinary incontinence, urgency & frequency
Adult Dose
Overactive Bladder
Indicated for overactive bladder with urge incontinence, urgency, and frequency
Adult & elderly Recommended dose: 4 mg once daily, may be increased to 8 mg once daily.
Max: 8 mg once daily. Duration of treatment: 2-8 wk.
Hepatic impairment
Mild-to-moderate (Child Pugh A to B): No dosage adjustment necessary
Severe (Child Pugh C): Not recommended
Child Dose
Pediatric Neurogenic Detrusor Overactivity
Indicated for treatment of neurogenic detrusor overactivity (NDO)
<6 years: Not established
>6 years ?25 kg: Not established
>6 years >25-35 kg: 4 mg PO qDay; may increase dose to 8 mg PO qDay if needed
>6 years >35 kg: 4 mg PO qDay, initially; increase to 8 mg PO qDay after one week
Renal Dose
Renal impairment
Mild-to-moderate (CrCl >30 mL/min): No dosage adjustment necessary
Severe (CrCl <30 mL/min): Not to exceed 4 mg PO once a Day
Administration
May be taken with or without food
Contra Indications
Hypersensitivity to peanut or soya. Urinary &/or gastric retention; uncontrolled narrow angle glaucoma; myasthenia gravis; severe ulcerative colitis; toxic megacolon. Concomitant use of potent CYP3A4 inhibitors in moderate to severe hepatic or renal impairment. Severe hepatic impairment (Child-Pugh C).
Precautions
Discontinue use if angioedema occurs. Risk of urinary retention & decreased GI motility; controlled narrow-angle glaucoma; myasthenia gravis; autonomic neuropathy; GI obstructive disorders eg, pyloric stenosis; GERD &/or taking drugs that cause or exacerbate oesophagitis eg, oral bisphosphanates; UTI;
Risk for QT-prolongation & preexisting cardiac diseases. Monitor for signs of anticholinergic effects. Concomitant use w/ CYP3A4 inhibitors, potent CYP3A4 inducers & CYP2D6 inhibitors. Galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.
Not recommended in severe hepatic impairment. Severe renal impairment. May affect ability to drive or operate machinery. Pregnancy. Not recommended during lactation.
Pregnancy-Lactation
Pregnancy
There are no data with fesoterodine use in pregnant women to inform a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes
In animal reproduction studies, oral administration of fesoterodine to pregnant mice and rabbits during organogenesis resulted in fetotoxicity at maternal exposures that were 6 and 3 times, respectively, the maximum recommended human dose (MRHD) of 8 mg/day based on AUC
Lactation
There is no information on the presence of fesoterodine in human milk, the effects on the breastfed child, or the effects on milk production
Interactions
Increased frequency &/or severity of AR & other anticholinergic effects w/ antimuscarinic agents.
Altered absorption w/ anticholinergic agents. Increased Cmax & AUC w/ CYP3A4 inhibitors eg, ketoconazole, itraconazole, miconazole & clarithromycin & CYP2D6 metabolizers.
Side Effects
Side effects of Fesoterodine Fumarate :
>10%
Adult overactive bladder
Dry mouth (18.8-34.6%)
Pediatric neurogenic detrusor overactivity
Diarrhea (7.1-11.9%)
1-10%
Adult overactive bladder
Constipation (4.2-6%)
Dyspepsia (1.6-2.3%)
Urinary tract infection (3.2-4.2%)
Xerophthalmia (1.4-3.7%)
Upper respiratory tract infection (1.8-2.5%)
Dysuria (1.3-1.6%)
Urinary retention (1.1-1.4%)
Dry throat (0.9-2.3%)
Insomnia (0.4-1.3%)
Back pain (0.9-2%)
Nausea (0.7-1.9%)
ncreased ALT (0.5-1.2%)
Increased GGT (0.4-1.2%)
Peripheral edema (0.7-1.2%)
Upper abdominal pain (0.5-1.1%)
Rash (0.7-1.1%)
Pediatric neurogenic detrusor overactivity
Urinary tract infection (2.4-9.5%)
Dry mouth (7.1-9.5%)
Constipation (7.1-7.1%)
Abdominal pain (4.8-2.4%)
Weight increased (0-4.8%)
Headache (4.8-7.1%)
Ophthalmological reactions (6.1%)
Increased heart rate compared to baseline (8.1-12.2%, week 4; 7.6-11.4%, week 12; 3.3-2.7% week 24)
Mode of Action
Competitive muscarinic receptor antagonist; inhibition of receptors in the bladder prevent symptoms of urgency and frequency.