73152-027-05, In female mice treated for 2 weeks before mating and during gestation with 20 mg/kg/day (corresponding to AUC value of about 500 µg∙h/L), neither effects on reproductive performance or fertility were seen. The effect of tolterodine 8 mg/day was not as large as that observed after four days of therapeutic dosing with the active control moxifloxacin. The active moiety, tolterodine, is a muscarinic receptor antagonist. Beatty
The blood to serum ratio of tolterodine and the 5-hydroxymethyl metabolite averages 0.6 and 0.8, respectively, indicating that these compounds do not distribute extensively into erythrocytes. et al Cognitive markers preceding Alzheimer's dementia in the healthy oldest old.
“The recent publication of the paper “Anticholinergic drugs and risk of dementia: case control study” identified an association … Further metabolism leads to formation of the 5-carboxylic acid and N-dealkylated 5-carboxylic acid metabolites, which account for 51% ± 14% and 29% ± 6.3% of the metabolites recovered in the urine, respectively.A subset (about 7%) of the population is devoid of CYP2D6, the enzyme responsible for the formation of the 5-hydroxymethyl metabolite of tolterodine. NJanowsky
Pahlman
In clinical trials of normal volunteers and patients, QT interval prolongation was observed with tolterodine immediate release at doses up to 8 mg (4 mg bid) and higher doses were not evaluated (see Effects on urodynamic parameters before and 1 and 5 hours after a single 6.4 mg dose of tolterodine immediate release were determined in healthy volunteers. The clearance of orally administered tolterodine was substantially lower in cirrhotic patients (1.0 ± 1.7 L/h/kg) than in the healthy volunteers (5.7 ± 3.8 L/h/kg). Nevertheless, in the absence of tolterodine therapy, results from the patient's memory testing were normal and any underlying diagnosis remained obscure in the absence of objective deficits. PDR Drug Summaries are concise point-of-care prescribing, dosing and administering information to help phsyicans more efficiently and accurately prescribe in their practice PDR's drug summaries are … Martin
Hasselmo
SH
Symptoms of a serious allergic reaction may include swelling of the face, lips, throat or tongue. Patients should be monitored for signs of anticholinergic CNS effects, particularly after beginning treatment or increasing the dose. et al Identification of medications that cause cognitive impairment in older people: the case of oxybutynin chloride. Keep a list of them with you to show your doctor or pharmacist each time you get a new medicine.Medicines like tolterodine tartrate can cause blurred vision, dizziness, and drowsiness. Both Fridericia's (QTcF) and a population-specific (QTcP) method were used to correct QT interval for heart rate. In addition to raising suspicions about the safety profile of tolterodine, this case also illustrates the use of detailed mental status testing. Van Kerrebroeck
SD
The patient's memory impairment began prior to the initiation of tolterodine therapy suggesting that her memory deficit could not be solely due to this medication. It is not known whether tolterodine is excreted in human milk; therefore, tolterodine tartrate should not be administered during nursing. ACamicioli
LDierks
PCox
Based on AUC values, the systemic exposure was about 15-fold higher in animals than in humans. Alternatively, our patient may have had aberrant metabolism of this drug or an increased sensitivity as a result of incipient Alzheimer disease.© 2020 American Medical Association. AC drugs are often prescribed to elderly patients with overactive bladder (OAB) or incontinence complaints. Long-term use of a particular anticholinergic drug may increase subsequent risk for developing dementia. PJ Recall and recognition memory in patients with Alzheimer's and Parkinson's diseases. KJonas
Patients should be informed that antimuscarinic agents such as tolterodine tartrate may produce the following effects: blurred vision, dizziness, or drowsiness. L Tolterodine in the treatment of overactive bladder: analysis of the pooled phase II efficacy and safety data. DeKosky
The Phase 2 and 3 clinical trial program for tolterodine tartrate tablets included 3071 patients who were treated with tolterodine tartrate (N=2133) or placebo (N=938). LAndersson
PRatcliff
The initial recommended dose of tolterodine tartrate tablets is 2 mg twice daily. At the maximum tolerated dose in mice (30 mg/kg/day), female rats (20 mg/kg/day), and male rats (30 mg/kg/day), AUC values obtained for tolterodine were 355, 291, and 462 µg∙h/L, respectively. Study subjects [approximately equal representation of CYP2D6 extensive metabolizers (EMs) and poor metabolizers (PMs)] completed sequential 4-day periods of dosing with moxifloxacin 400 mg QD, tolterodine 2 mg BID, tolterodine 4 mg BID, and placebo.