Drug intelligence / Profile preview

tolterodine

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Tolterodine is a small molecule antimuscarinic drug used to treat symptoms of overactive bladder, including urinary incontinence, urgency, and frequency. It acts as a competitive antagonist at muscarinic acetylcholine receptors—primarily the M2 and M3 subtypes—on the bladder detrusor muscle. By blocking these receptors, tolterodine reduces involuntary contractions of the bladder muscle and increases bladder capacity. Its main pharmacologically active metabolite is 5-hydroxymethyl-tolterodine, which also exhibits antimuscarinic activity. Tolterodine was developed for oral administration in both immediate-release tablet and extended-release capsule forms[1][2][4][7].

Brand names
DetrolDetrol LADetrusitol
Other names
tolterodine hydrogen tartrateUrotol
02

Targets

CHRM2 (M2)CHRM3 (M3)CHRM5 (M5)

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