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Roliten - Roliten is an antimuscarinic drug that is used to treat urinary incontinence. Roliten acts on M2 and M3 subtypes of muscarinic receptors.
Indication: For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
Roliten is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, Roliten is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both Roliten and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Roliten has a pronounced effect on bladder function. The main effects of Roliten are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.
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