Product Name

Tolterodine

CAS Number

124937-51-5

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Product Name:
Tolterodine
CAS Number:
124937-51-5
Indication:
For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
Mode of Action:

Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Pharmacodynamics:

Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine 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 tolterodine 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. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine 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.

IUPAC:
2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
ATC:
G04BD07
DrugBank:
DB01036 (APRD00146)
Formula:
C16H20N4O3S
Molecular Mass:
325.4876
Synonyms:
Tolterodina [INN-Spanish] Tolterodine [INN] tolterodine extended release capsules Tolterodine L-Tartrate Tolterodine Tartrate Tolterodinum [INN-Latin] Tolterondine Tartrate
SMILES:
CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(O)C=CC(C)=C1)C(C)C
AHFS Code:
26:12.0
InChi:
OOGJQPCLVADCPB-HXUWFJFHSA-N

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