Absorption, Distribution and Excretion
Following oral administration of 5 mg 14C-tolterodine solution to healthy volunteers, 77% of the radioactive material was recovered in urine and 17% in feces within 7 days.
113 ± 26.7 L
Metabolism/Metabolites Known metabolites of tolterodine include 5-hydroxymethyltolterodine and N-desalkyltolterodine.
Biological Half-Life 1.9–3.7 hours

Hepatotoxicity
In multiple randomized controlled trials of tolterodine for patients with overactive bladder, elevated serum transaminases and alkaline phosphatase levels were uncommon, with an incidence of less than 1% in both the treatment and placebo groups. No clinically significant liver injury or jaundice was reported in these clinical trials. Since tolterodine was approved and widely used in 1998 (with over 1 million prescriptions annually in the US), only one published case report has shown liver injury symptoms and jaundice after tolterodine use (Case 1). Therefore, acute symptomatic liver injury caused by tolterodine, even if it occurs, is certainly very rare. Probability Score: D (Possibly, but extremely rare, a cause of clinically significant liver injury). Pregnancy and Lactation Effects ◉ Overview of Use During Lactation There is currently no information on the use of tolterodine during lactation. Long-term use of tolterodine may reduce milk production or the milk ejection reflex. During long-term use, signs of decreased lactation (e.g., dissatisfaction, poor weight gain) should be observed.
◉ Effects on breastfed infants
As of the revision date, no relevant published information was found.
◉ Effects on lactation and breast milk
Anticholinergic drugs can inhibit lactation in animals, possibly by suppressing the secretion of growth hormone and oxytocin. Anticholinergic drugs can also lower serum prolactin levels in non-lactating women. Prolactin levels in established lactating mothers may not affect their ability to breastfeed.

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Protein binding
Approximately 96.3%.

[1]. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7.

[2]. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26(6):528-35.

[3]. Tolterodine does not affect memory assessed by passive-avoidance response test in mice. Eur J Pharmacol. 2008 Jan 28;579(1-3):225-8.

Tolterodine is a tertiary amine. It acts as a muscarinic receptor antagonist, muscle relaxant, and antispasmodic. Its function is similar to that of p-cresol. Tolterodine is an antimuscarinic drug used to treat urinary incontinence. Tolterodine acts on the M2 and M3 subtypes of muscarinic receptors. Tolterodine is a cholinergic muscarinic receptor antagonist. The mechanism of action of tolterodine is as a cholinergic muscarinic receptor antagonist. Tolterodine is an anticholinergic drug used to treat urinary incontinence and overactive bladder. No association has been found between tolterodine treatment and elevated liver enzymes; only one case of clinically significant acute liver injury has been reported, attributed to tolterodine use. Tolterodine tartrate is the tartrate salt form of tolterodine, a diphenylmethyl compound that is also a muscarinic receptor antagonist with antimuscarinic and antispasmodic effects. Tolterodine and its active metabolite, 5-hydroxymethyltolterodine, both competitively block muscarinic receptors, thereby inhibiting the binding of acetylcholine receptors. This antagonistic effect leads to increased residual urine volume, reflecting incomplete bladder emptying, and reduces detrusor pressure, indicating an antimuscarinic effect on the lower urinary tract. The 5-hydroxymethyl metabolite appears to contribute significantly to the therapeutic effect. Tolterodine is a diphenylmethyl compound and a muscarinic receptor antagonist with antimuscarinic and antispasmodic effects. Tolterodine and its active metabolite, 5-hydroxymethyltolterodine, both competitively block muscarinic receptors, thereby inhibiting the binding of acetylcholine. This antagonistic effect leads to increased residual urine volume, reflecting incomplete bladder emptying, and reduces detrusor pressure, indicating an antimuscarinic effect on the lower urinary tract. The 5-hydroxymethyl metabolite appears to contribute significantly to the therapeutic effect.
An antimuscarinic drug that selectively acts on bladder muscarinic receptors for the treatment of urinary incontinence and urge incontinence.
See also: Tolterodine tartrate (in saline form).
Drug Indications

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
FDA Label
Mechanism of Action

Tolterodine and its active metabolite 5-hydroxymethyltolterodine both act as competitive antagonists of muscarinic receptors. This antagonism results in inhibition of bladder contraction, decreased detrusor pressure, and incomplete bladder emptying.
Pharmacodynamics

Tolterodine is a competitive muscarinic receptor antagonist. Bladder contraction and salivation are mediated by cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver to produce a 5-hydroxymethyl derivative, which is the primary pharmacologically active metabolite. The 5-hydroxymethyl metabolite possesses antimuscarinic activity similar to tolterodine and significantly contributes to therapeutic efficacy. Both tolterodine and its 5-hydroxymethyl metabolite exhibit high specificity for muscarinic receptors, as their activity or affinity for other neurotransmitter receptors and other potential cellular targets (such as calcium channels) is negligible. Tolterodine has a significant effect on bladder function. Its primary action is to increase residual urine volume, reflecting incomplete bladder emptying, and to decrease detrusor pressure, consistent with its anticholinergic effects on the lower urinary tract.

C22H31NO

325.48764

325.24

C, 81.18; H, 9.60; N, 4.30; O, 4.92

124937-51-5

Tolterodine tartrate; 124937-52-6; Tolterodine-d14 hydrochloride; 1217645-16-3

443879

Colorless to light yellow solid powder

1.0±0.1 g/cm3

442.2±45.0 °C at 760 mmHg

192.1±27.4 °C

0.0±1.1 mmHg at 25°C

1.548

5.77

23.47

1

2

7

24

340

1

CC(C)N(C(C)C)CC[C@H](C1=CC=CC=C1)C2=C(O)C=CC(C)=C2

OOGJQPCLVADCPB-HXUWFJFHSA-N

InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1

2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol

Detrusitol; Tolterodine; Detrol; PHA-686464B

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Ethanol: ~120 mg/mL (~368.7 mM)
DMSO: ~100 mg/mL (~307.2 mM)

配方 1 中的溶解度: ≥ 2.08 mg/mL (6.39 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (6.39 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (6.39 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。