Drug Interaction:
Drug interactions -summary-
CYP2A4 inhibitors (eg rifampin) + Fesotetrodune -
Co admin decreased festerodine Cmax and AUC . No dosing adjustments are recommended
CYP3A4 inhibitors (eg clarithromycin ,erythromycin , itraconazole, ketoconazole ) + Fesotrodine-
Coadmin of potent CYP3A4 increase the Cmax and AUC of active metabolite of festerodine
doses of festerodine more than 4mg are not recommended
Fesoterodine + Anticholinergic agents/ Anticholinergic agents + fesoterodine-
concomittant use may increase frequency and and severity of antichilnergic effects eg. dry mouth,urinary retention. Anicholinergic agents may alter the absorption of some co-administred drugs
Indication:
Overactive Bladder
Adverse Reaction:
Adverse reactions-
GI - abdominal pain 1% constipation 2% dry mouth 6% nausea 1%
GU - urinary tract infection 3%
Lab test abnormalities- ALT increased 0.9%
Respiratory - cough 0.5% dry throat 0.5% upper respiratory tract infection 2%
Miscellaneous- back pain 0.4% edema peripheral 0.6% insomnia 0.5% rash 0.5%
Contra-Indications:
Urinary retention, gastric irritation
Special Precautions-
Bladder outlet obstruction- administer festerodine with caution on patients with clinically
significant bladder outlet obstruction
GI motility- use with caution in patients with decreased gastric motility such as those with severe
constipation
Myasthenia gravis- use fesoterodine with caution in patients with myasthenia gravis
Controlled narrow -angle glaucoma - use fesoteridine with caution in patients treated for narrow
angle glaucoma
Renal function impairment- doses of fesoterodine more than 4mg are not recommended
Hepatic function impairment- not recommended for use in this population
Pregnancy-use fesoteridine during pregnancy only if needed
Lactation- do ot administer during breast feeding unless the potential benefit outweighs
the potential risk to the fetus.
Children- safety and effectiveness in children have not been established
Elderly- increase in urinary tract infection was higher in patients over 75 years of age than
as compared to younger patients
Dosages/ Overdosage Etc:
Indication-
Overactive Bladder
Dosage-
8mg once daily based on indivudual response and tolerability
Initial dosage- 4mg once daily
Concomittant treatment- the daily dose should not exceed 4mg in patients taking potent CYP3A4
inhibitors eg. clarithromycin, itraconazole, ketaconazole
Renal function impairment - doses more than 4mg are not recommended
Hepatic function impairment- fesoterodine is not recommended for use in with severe hepatic
function impairment
Patient Information:
1. Inform patients that fesoterdine like other antimuscarnic agents may produce clinically
significant reactions to antimuscranic pharmacological acitivity including constipation
and urinary retention
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts and Comparisons (2010)
Pharmacology-
Fesoterodine is a competitive muscarinic receptor antagonist. After Oral administration
fesotterodine is rapidly and extensively hydrolysed by nonspecific esterases to its active
metobolite, -hydroxymethyl tolerodine , which is responsible for the antimuscaranic
activity of fesoteridine.
Muscarinic receptors play a role in contractions of urinary bladder smooth muscle and
stimulation of salivary secretion. Inhibition of these receptors in the bladder is presumed
to be the mechanism by which festerodine produces its effects
Pharmacokinetics-
After oral administration festerodine is well absorbed. Because of rapid and extensive
hydrolysis by nonspecific esterases to its active metabolite, festerodine cannot be
deteced in plasma.
Bioavailability of the active metabolite is 52%. Maximum plasma concentrations of the
active metabolite is reached after approximately 5 hours.
A summary of pharmacokinetic parameters for the active metaboliteafter a single dose
of fesoterodine 4 and 8mg in extensive and poor metabolizers of CYP2D6 is indicated-
Fesoterodine Summary of Mean CV pharmacokinetic Parameters for
Fesoterodine4 and 8mg in Extensive and Poor CYP2D6 Metabolizers
Fesoterodine 4mg Fesoteridine 8mg
EM (n=16) PM (n=8) EM (n=16) PM (n=8)
Cmax (ng/mL) 1.89 (43%) 3.45 (54%) 3.98 (28%) 6.90(39%)
AUC 0-x (ng*h/mL) 21.2(38%) 40.5(31%) 45.3(32%) 88.7(36%)
Tmax (h) 5(2 to 6) 5 (5 to 6) 5(3 to 6) 5(5 to6)
t 1/2 (h) 7.31(27%) 7.31(30%) 8.59(41%) 7.66(21%)
Pregnancy and lactation:
Pregnancy-
Use fesoteridine during pregnancy only if needed
Lactation-
Do ot administer during breast feeding unless the potential benefit outweighs
the potential risk to the fetus.
Children-
Safety and effectiveness in children have not been established
Elderly-
Increase in urinary tract infection was higher in patients over 75 years of age than
as compared to younger patients
Manufacturer Details