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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].
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