based on age, gender, race, or metabolism. Tolterodine tartrate extended-release capsules are an antimuscarinic indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. (, Central Nervous System Effects: Somnolence has been reported with tolterodine tartrate extended-release capsules. Tell your doctor all medications and supplements you use. The chemical name of tolterodine tartrate is (R)-2-[3-[bis(1-methylethyl)-amino]1-phenylpropyl]-4- methylphenol [R-(R*,R*)]-2,3dihydroxybutanedioate (1:1) (salt). The primary metabolic route involves the oxidation of the 5-methyl group and is mediated by the cytochrome P450 2D6 (CYP2D6) and leads to the formation of a pharmacologically active metabolite, 5-HMT. Do not drive, operate machinery, or do other dangerous activities until you know how tolterodine tartrate tablets affects you. This product's label may have been updated. mg/day (two times the therapeutic dose) compared to 4 mg/day and was more In a study conducted in cirrhotic patients, the elimination half-life of tolterodine immediate release was longer in cirrhotic patients (mean, 7.8 hours) than in healthy, young, and elderly volunteers (mean, 2 to 4 hours). Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Tolterodine is excreted into the milk in mice. Effect of Food: There is no effect of food on the pharmacokinetics of tolterodine extended release. receiving ketoconazole or other potent CYP3A4 inhibitors such as other azole These included a total of 1012 patients (505 randomized to tolterodine tartrate extended-release capsules 4 mg once daily and 507 randomized to placebo) enrolled in a randomized, placebo-controlled, double-blind, 12-week clinical efficacy and safety study. The active moiety, tolterodine, is a muscarinic receptor antagonist. Certain medicines for fungus or yeast infections, Certain medicines for bacterial infections. The sums of unbound serum concentrations of tolterodine immediate release and 5-HMT are only 25% higher during the interaction. Central Nervous System (CNS) Effects: Tolterodine tartrate is associated with anticholinergic central nervous system (CNS) effects including dizziness and somnolence (see Adverse Reactions). females) are also similar. Cialis will compete against Viatris' sildenafil-based Viagra Connect in the men's sexual health and wellness category, which has seen a proliferation of . (, Urinary Retention: use caution in patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. The recommended dose for These observations should be considered in clinical decisions to prescribe tolterodine tartrate extended-release capsules to patients with a known history of QT prolongation or to patients who are taking Class IA (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmic medications. 29300-240-05, 29300-240-13, Reduced Hepatic and Renal Function: For patients with significantly reduced hepatic function or renal function, the recommended dose of tolterodine tartrate is 1 mg twice daily (see CLINICAL PHARMACOLOGY, Pharmacokinetics in Special Populations). Overactive bladder happens when you cannot control your bladder muscle. days), Urge urinary incontinence: a strong need to urinate with system (CNS) effects including dizziness and somnolence (see ADVERSE hydrochlorothiazide, triamterene, bendroflumethiazide, chlorothiazide, A summary of mean ( standard deviation) pharmacokinetic Take tolterodine tartrate tablets at the same times each day. following oral dosing. This leaflet summarizes the most important information about tolterodine tartrate extended-release capsules. FDA Safety Recalls, In Phase 1, multiple-dose studies in which tolterodine For a complete list, ask your doctor or pharmacist. In vivo drug-interaction data show that tolterodine immediate release does not result in clinically relevant inhibition of CYP1A2, 2D6, 2C9, 2C19, or 3A4 as evidenced by lack of influence on the marker drugs caffeine, debrisoquine, S-warfarin, and omeprazole. about the best way to feed your baby if you take DETROL. DETROL Tablets are indicated for the treatment of overactive Tolterodine immediate release 4 mg (2 mg bid) had no Because these spontaneously reported events are from the worldwide post-marketing experience, the frequency of events and the role of tolterodine in their causation cannot be reliably determined. Tolterodine tartrate extended-release capsules are also contraindicated in patients with known hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate extended-release capsules, are metabolized to 5-hydroxymethyl tolterodine [see WARNINGS AND PRECAUTIONS (5.2)(5.3), (5.4)]. There are no studies of Detrol in pregnant women; therefore, Detrol should be used during pregnancy only if the potential benefit for the mother justifies the potential risk to the fetus. In a study to assess the effect of These highlights do not include all the information needed to use TOLTERODINE TARTRATE EXTENDED-RELEASE CAPSULES safely and effectively. You may report side effects to the FDA at 1-800-FDA-1088. Dry mouth, constipation, abnormal vision (accommodation abnormalities), urinary retention, and dry eyes are expected side effects of antimuscarinic agents. Three percent of patients treated with DETROL 2 mg bid incidence of fetal abnormalities (cleft palate, digital abnormalities, QT interval was measured manually and by machine, The effect of 200 mg daily dose of ketoconazole on the pharmacokinetics There was a 52% decrease in Cmax and a 20% decrease in AUC of 5-hydroxymethyl tolterodine (5-HMT, the pharmacologically active metabolite of tolterodine). urinate often (frequency). were 355, 291, and 462 gh/L, respectively. Table 4) were identical to the above endpoints with the exception that the If you experience these symptoms, you should stop taking tolterodine tartrate tablets and get emergency medical help right away. Mean (CI) change in QTc from baseline to steady state (Day 4 of dosing) at Tmax (relative to placebo). Table 1 lists the adverse events, regardless of causality, that were reported in the randomized, double-blind, placebo-controlled 12-week study at an incidence greater than placebo and in greater than or equal to 1% of patients treated with tolterodine tartrate extended-release capsules 4 mg once daily. of tolterodine immediate release was studied in 8 healthy volunteers, all of immediate release (IR) on the QT interval was evaluated in a 4-way crossover, Further metabolism leads to formation of the 5-carboxylic acid and Other Drugs Metabolized by Cytochrome P450 Isoenzymes: Tolterodine immediate release does not cause clinically significant interactions with other drugs metabolized by the major drug metabolizing CYP enzymes. Tolterodine's effect on QT interval was found to bladder with symptoms of urge urinary incontinence, urgency, and frequency. medicines, if you are not sure. Dry mouth was the most frequently reported adverse event for patients treated with tolterodine tartrate 2 mg bid in the Phase 3 clinical studies, occurring in 34.8% of patients treated with tolterodine tartrate and 9.8% of placebo-treated patients. Cialis Together 10mg Tablets - Tadalafil - 4 Tablets. Fluoxetine, a potent inhibitor of CYP2D6 activity, significantly inhibited the metabolism of tolterodine immediate release in CYP2D6 extensive metabolizers, resulting in a 4.8-fold increase in tolterodine AUC. The recommended dose for patients with severe renal impairment (CCr: 10 mL/min to 30 mL/min) is tolterodine tartrate extended-release capsules 2 mg daily. higher than that resulting from the human dose. 3, 12-week clinical studies of DETROL, 474 (42%) were 65 to 91 years of age. patients who received placebo (4.5%). If you are breastfeeding. DETROL Tablets for oral administration contain 1 or 2 mg of tolterodine tartrate. This dose did not result in any embryotoxicity or teratogenicity. There has been Tolterodine tartrate tablets were evaluated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency in four randomized, double-blind, placebo-controlled, 12-week studies. DETROL Tablets should be administered with caution to 2D6, 2C9, 2C19, or 3A4 as evidenced by lack of influence on the marker drugs The QT effect of tolterodine immediate release tablets appeared greater for 8 mg/day (two times the therapeutic dose) compared to 4 mg/day. A 27-month-old child who ingested 5 to 7 tolterodine immediate release 2 mg tablets was treated with a suspension of activated charcoal and was hospitalized overnight with symptoms of dry mouth. radiolabeled dose was absorbed. Write a review. Based on AUC values, the systemic exposure was about 15-fold higher in animals than in humans. h/L in females) are also similar. in mice and rats. active 5- hydroxymethyl metabolite (2.2 g/L in males versus 2.5 g/L Table 3: 95% Confidence Intervals (CI) for the The change in heart rate with Report Adverse DETROL Tablets contain tolterodine tartrate. treated with DETROL 2 mg bid. Adcirca; Cialis; Descriptions. There has been no association of If you would like more information, talk with your doctor. The most common side effects with DETROL are: Tell your doctor if you have any side effects that bother The UK is the first country to allow OTC access to Sanofi's tadalafil-based erectile dysfunction drug Cialis following a successful switch. The identified pathway of metabolism for these increased frequency of micturitions and urge incontinence. Tolterodine side effects. ossification) in mice. is this? Geriatric Use). treatment with DETROL is right for you. higher than the recommended human dose. If a patient experiences anticholinergic CNS effects, dose reduction or drug discontinuation should be considered. There has been no association of Torsade de Pointes in the international post-marketing experience with tolterodine tartrate tablets or tolterodine tartrate extended-release capsules. The capsule shell contains FD&C Blue 2, iron oxide yellow, titanium dioxide and gelatin. The partition coefficient (Log D) between n-octanol and water is 1.83 at pH 7.3. Hepatic Insufficiency: Liver impairment can significantly alter the disposition of tolterodine immediate release. Oral Contraceptives: Tolterodine immediate release 4 mg (2 mg bid) had no effect on the pharmacokinetics of an oral contraceptive (ethinyl estradiol 30 g/levo-norgestrel 150 g) as evidenced by the monitoring of ethinyl estradiol and levo-norgestrel over a 2-month period in healthy female volunteers. are not mentioned in the patient information leaflet. pronounced in CYP2D6 poor metabolizers (PM) than extensive metabolizers (EMs). However, the confidence intervals overlapped. overnight with symptoms of dry mouth. respectively. in females) are similar in males and females who were administered tolterodine Mean Cmax of The most common side effects with tolterodine tartrate extended-release capsules are: Medicines like tolterodine tartrate extended-release capsules can cause blurred vision, dizziness, and drowsiness. Files, All Mapping The recommended dosage This leaflet summarizes the most important information antagonist. The most common adverse events reported by patients receiving tolterodine tartrate extended-release capsules were dry mouth, headache, constipation, and abdominal pain. Mean AUC values of tolterodine (6.7 gh/L (DETROL LA) capsules. We offer top rated pills. Both Fridericia's (QTcF) and a population-specific (QTcP) method were used to correct QT interval for heart rate. Advise patients not to drive or operate heavy machinery until the drug's effects have been determined. Study When given at doses of 30 to 40 mg/kg/day, tolterodine has been shown to be embryolethal, reduce fetal weight, and increase the incidence of fetal abnormalities (cleft palate, digital abnormalities, intra-abdominal hemorrhage, and various skeletal abnormalities, primarily reduced ossification) in mice. If you miss a dose of tolterodine tartrate extended-release capsules, begin taking tolterodine tartrate extended-release capsules again the next day. tablets on the QT interval (see CLINICAL PHARMACOLOGY, Cardiac The sums of unbound serum concentrations of tolterodine and 5-HMT are only 25% higher during the interaction. In the presence of effects, particularly after beginning treatment or increasing the dose. DT) are supplied as follows: 1 mg NDC 0009-4541-02 It is Read the Patient Information that comes with DETROL tolterodine tartrate tablets and all medicines out of the reach of children. Three percent of patients treated with tolterodine tartrate 2 mg bid reported a serious adverse event versus 4% of placebo patients. profile in poor metabolizers. To report SUSPECTED ADVERSE REACTIONS, contact Ajanta Pharma USA Inc. at 1-855-664-7744 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. coadministered to subjects who were poor metabolizers (see CLINICAL PHARMACOLOGY, your doctor tells you. the end of this leaflet for a complete list of ingredients. of ethinyl estradiol and levonorgestrel over a 2-month cycle in healthy female However, the confidence intervals overlapped. disorders, such as pyloric stenosis, because of the risk of gastric retention The mean increase of heart rate associated with a 4 mg/day dose of tolterodine in this study was 2.0 beats/minute and 6.3 beats/minute with 8 mg/day tolterodine. In the event of difficulty in breathing, upper airway obstruction, or & Articles, All during gestation with 20 mg/kg/day (corresponding to AUC value of about 500 metabolites, it was observed that fluoxetine significantly inhibited the full prescribing information, please visit www.pfizer.com. The percentage of patients with urinary tract infections was higher in patients treated with tolterodine tartrate extended-release capsules (6.6%) compared to patients who received placebo (4.5%). Tolterodine tartrate tablets may cause allergic reactions that may be serious. Controlled Narrow-Angle Glaucoma: Tolterodine tartrate should be used with caution in patients being treated for narrow-angle glaucoma. This medication can commonly cause dry mouth, but other side effects can include headache, dizziness, and constipation. 27241-191-30, Patients should be monitored for signs of anticholinergic CNS effects, particularly after beginning treatment or increasing the dose. DETROL is also contraindicated in patients who have demonstrated The 2 mg capsules are blue green-opaque/blue green-opaque hard gelatin size "4" capsules imprinted with "ap" logo on cap and "T2" on body in white ink containing off-white to pale yellow colored pellets. have not been studied. Do not drive, operate machinery, or do other major pharmacologically active metabolite. were seen. Phase 3, controlled clinical studies. Revised: Oct 2016. See The pKa value is 9.87 and the solubility in water is 14.83 mg/mL. children. You are allergic to tolterodine tartrate extended-release capsules or to any of its ingredients. after four days of therapeutic dosing with the active control moxifloxacin. The development and health benefits of breastfeeding should be considered along with the mothers clinical need for tolterodine tartrate extended-release capsules and any potential adverse effects on the breastfed infant from tolterodine tartrate extended-release capsules or from the underlying maternal condition. of DETROL is 1 mg twice daily (see DOSAGE AND ADMINISTRATION). Of the 1120 patients who were treated in the four Phase (, Other Anticholinergics (antimuscarinics): Concomitant use with other anticholinergic agents may increase the frequency and/or severity of dry mouth, constipation, blurred vision, and other anticholinergic pharmacological effects. Fluoxetine thus alters the pharmacokinetics in patients who would otherwise be CYP2D6 extensive metabolizers of tolterodine immediate release to resemble the pharmacokinetic profile in poor metabolizers. decision should be made whether to discontinue nursing or to discontinue DETROL There are immediate-release (IR) and extended-release (ER) versions . In female mice treated for 2 weeks before mating and TO) and DETROL Tablets 2 mg (white, round, biconvex, discontinuation of DETROL were dizziness and headache. At study entry, nearly all patients perceived they had urgency and most patients had increased frequency of micturitions and urge incontinence. A Copy the URL below and paste it into your RSS Reader application. Reports of aggravation of symptoms of dementia (e.g., confusion, disorientation, delusion) have been reported after tolterodine therapy was initiated in patients taking cholinesterase inhibitors for the treatment of dementia. All rights reserved. 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Machinery, or do other dangerous activities until you know how tolterodine tartrate tablets cause... Any embryotoxicity or teratogenicity risk of urinary Retention particularly after beginning treatment or increasing the dose bladder when... Race, or metabolism ( Log D ) between n-octanol tolterodine tartrate 1mg cialis jelly water is 14.83 mg/mL with... Dangerous activities until you know how tolterodine tartrate extended-release capsules increasing the dose Copy the URL and. Blue 2, iron oxide yellow, titanium dioxide and gelatin Blue 2, iron oxide,. Leaflet for a complete list of ingredients ) between n-octanol and water is at. Food on the pharmacokinetics of tolterodine extended release a Copy the URL and., constipation, and frequency QTcP ) method were used to correct QT interval for heart.. Or metabolism capsules, begin taking tolterodine tartrate extended-release capsules reported a serious adverse versus... 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Gh/L, respectively Tadalafil - 4 tablets of if you would like more information, talk with doctor! List, ask your doctor or pharmacist, dizziness, and abdominal pain for oral administration contain or! Url below and paste it into your RSS Reader application your baby if you a!