Tolterodine tartrate 2 mg Capsule, Extended Release, 500-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Cholinergic Muscarinic Antagonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Tolterodine is used to treat overactive bladder (a bladder condition that causes sudden urges to urinate that may be hard to control). Tolterodine is in a class of medications called antimuscarinics. It works by relaxing the bladder muscles.
Read the full MedlinePlus article ↗- Tolterodine calms the bladder by blocking the nerve signals that cause it to squeeze too often or too urgently. Most people start noticing fewer urgent trips to the bathroom and le...
- What exactly does tolterodine do, and how quickly will I notice a difference?
- Dry mouth is the most common complaint with tolterodine, and it happens because the same receptors that calm your bladder also affect your saliva glands. Sipping water frequently,...
- The dry mouth is really bothersome — is there anything I can do about it?
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.282 | $141.05 / 500 capsules |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.8047 | $402.35 / 500 capsules |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Tolterodine Tartrate 2 mg 70436-0160-02 | Slate | 500 capsules | $0.263 | AB | Availability likely | save 7% |
| Tolterodine Tartrate 2 mg 00093-7163-05 | Teva | 500 capsules | $0.265 | AB | Availability likely | save 6% |
| Tolterodine Tartrate 2 mg 13668-0189-05 | Torrent | 500 capsules | $0.265 | AB | Availability likely | save 6% |
| Tolterodine Tartrate 2 mg 43975-0322-03 | ANI | 30 capsules | $0.265 | AB | Availability likely | save 6% |
| Tolterodine Tartrate Extended Release 2 mg 59762-0047-01 | Mylan | 30 capsules | $0.265 | AB | Discontinued | save 6% |
| Tolterodine Tartrate 2 mg 60687-0319-21 | American | 1 capsule | $0.265 | AB | Availability likely | save 6% |
| Tolterodine tartrate 2 mgthis 27241-0191-05 | Ajanta | 500 capsules | $0.282 | AB | Availability likely | — |
| Tolterodine tartrate 2 mg 29300-0306-05 | Unichem | 500 capsules | — | AB | FDA listed | — |
| Tolterodine Tartrate 2 mg 31722-0607-05 | Camber | 500 capsules | — | AB | FDA listed | — |
| Tolterodine Tartrate 2 mg 51407-0739-05 | Golden | 500 capsules | — | AB | FDA listed | — |
| Detrol LA 2 mg 58151-0103-77 | Viatris | 90 capsules | — | AB | Discontinued | — |
| Tolterodine Tartrate 2 mg 00904-7574-04 | Major | 1 capsule | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 27241-0191-05 You're viewing this | 500 CAPSULE, EXTENDED RELEASE in 1 BOTTLE (27241-191-05) | $0.2821 / ea | $141.06 | 2020-06-25 | Active |
| 27241-0191-30 | 30 CAPSULE, EXTENDED RELEASE in 1 BOTTLE (27241-191-30) | $0.2648 / ea | $7.94 | 2020-06-25 | Active |
| 27241-0191-90 | 90 CAPSULE, EXTENDED RELEASE in 1 BOTTLE (27241-191-90) | $0.2941 / ea | $26.47 | 2020-06-25 | Active |
You're viewing the largest of 3 pack sizes for this product.
Per ea, this pack runs about 7% above the cheapest pack (30-count, $0.2648 vs $0.2821 NADAC).
This pack shows little to no recent Medicaid volume — the 30 capsules pack carries most fills. See all packs ↓
Pack size FAQ
What quantity is in NDC 27241-0191-05?
What is the difference between NDC 27241-0191-05 and NDC 27241-0191-30?
What NDC number is used to bill for this package of Tolterodine tartrate 2 mg Capsule, Extended Release?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Tolterodine tartrate extended-release capsules are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency [see CLINICAL STUDIES ( 14)]. Tolterodine tartrate extended-release capsules are an antimuscarinic indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 4 mg capsules taken orally once daily with water and swallowed whole. ( 2.1 ) 2 mg capsules taken orally once daily with water and swallowed whole in the presence of: mild to moderate hepatic impairment (Child-Pugh class A or B) ( 2.2 ) severe renal impairment [Creatinine Clearance (CCr) 10 mL/min to 30 mL/min] ( 2.2 ) drugs that are potent CYP3A4 inhibitors. ( 2.2 ) Tolterodine tartrate extended-release capsules are not recommended for use in patients with CCr less than10 mL/min.
( 2.2 ) Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C). ( 2.2 )
2.1Dosing Information The recommended dose of tolterodine tartrate extended-release capsule is 4 mg once daily with water and swallowed whole. The dose may be lowered to 2 mg daily based on individual response and tolerability; however, limited efficacy data are available for tolterodine tartrate extended-release capsules 2 mg [see CLINICAL STUDIES ( 14 )].
2.2Dosage Adjustment in Specific Populations For patients with mild to moderate hepatic impairment (Child-Pugh Class A or B) or severe renal impairment (CCr 10 mL/min to 30 mL/min), the recommended dose of tolterodine tartrate extended-release capsule is 2 mg once daily. Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C). Patients with CCr less than 10 mL/min have not been studied and use of tolterodine tartrate extended-release capsules in this population is not recommended [see WARNINGS AND PRECAUTIONS ( 5.6 ) and USE IN SPECIFIC POPULATIONS ( 8.6 , 8.7 )].
2.3Dosage Adjustment in Presence of Concomitant Drugs For patients who are taking drugs that are potent inhibitors of CYP3A4 [e.g., ketoconazole, clarithromycin, ritonavir], the recommended dose of tolterodine tartrate extended-release capsule is 2 mg once daily [see DRUG INTERACTIONS ( 7.2 )].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 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. The 4 mg capsules are blue opaque/blue opaque hard gelatin size "3" capsules imprinted with "ap" logo on cap and "T4" on body in white ink containing off-white to pale yellow colored pellets. Capsules: 2 mg and 4 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Tolterodine tartrate extended-release capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. 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) ].
Tolterodine tartrate extended-release capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. 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. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate extended-release capsules. ( 5.1 ) Urinary Retention: use caution in patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. ( 5.2 ) Gastrointestinal Disorders: use caution in patients with gastrointestinal obstructive disorders or decreased gastrointestinal motility because of the risk of gastric retention.
( 5.3 ) Controlled Narrow-Angle Glaucoma: use caution in patients being treated for narrow-angle glaucoma. ( 5.4 ) Central Nervous System Effects: Somnolence has been reported with tolterodine tartrate extended-release capsules. Advise patients not to drive or operate heavy machinery until they know how tolterodine tartrate extended-release capsules affects them ( 5.5 ).
Myasthenia Gravis: use caution in patients with myasthenia gravis. ( 5.8 ) QT Prolongation: consider observations from the thorough QT study 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. ( 5.9 )
5.1Angioedema Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate extended-release capsules. In the event of difficulty in breathing, upper airway obstruction, or fall in blood pressure, tolterodine tartrate extended-release capsules should be discontinued and appropriate therapy promptly provided.
5.2Urinary Retention Administer tolterodine tartrate extended-release capsules with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention [see CONTRAINDICATIONS ( 4 )].
5.3Gastrointestinal Disorders Administer tolterodine tartrate extended-release capsules with caution in patients with gastrointestinal obstructive disorders because of the risk of gastric retention. Tolterodine tartrate extended-release capsules, like other antimuscarinic drugs, may decrease gastrointestinal motility and should be used with caution in patients with conditions associated with decreased gastrointestinal motility (e.g., intestinal atony) [see CONTRAINDICATIONS ( 4 )].
5.4Controlled Narrow-Angle Glaucoma Administer tolterodine tartrate extended-release capsules with caution in patients being treated for narrow-angle glaucoma [see CONTRAINDICATIONS ( 4 )].
5.5Central Nervous System Effects Tolterodine tartrate extended-release capsules are associated with anticholinergic central nervous system (CNS) effects [see ADVERSE REACTIONS ( 6.2 )] including dizziness and somnolence [see ADVERSE REACTIONS ( 6.1 )] . Patients should be monitored for signs of anticholinergic CNS effects, particularly after beginning treatment or increasing the dose. Advise patients not to drive or operate heavy machinery until the drug’s effects have been determined.
If a patient experiences anticholinergic CNS effects, dose reduction or drug discontinuation should be considered.
5.6Hepatic Impairment The clearance of orally administered tolterodine immediate release was substantially lower in cirrhotic patients than in the healthy volunteers. For patients with mild to moderate hepatic impairment (Child-Pugh Class A or B), the recommended dose for tolterodine tartrate extended-release capsule is 2 mg once daily. Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C) [see DOSAGE AND ADMINISTRATION ( 2.2 ) and USE IN SPECIFIC POPULATIONS ( 8.6 )].
5.7Renal Impairment Renal impairment can significantly alter the disposition of tolterodine and its metabolites. The dose of tolterodine tartrate extended-release capsul…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions (incidence greater than 4% and greater than placebo) were dry mouth, headache, constipation, and abdominal pain. ( 6.1 ) 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.
6.1Clinical Trials Experience The efficacy and safety of tolterodine tartrate extended-release capsules was evaluated in 1073 patients (537 assigned to tolterodine tartrate extended-release capsules; 536 assigned to placebo) who were treated with 2, 4, 6, or 8 mg/day for up to 15 months. 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.
Adverse events were reported in 52% (n=263) of patients receiving tolterodine tartrate extended-release capsules and in 49% (n=247) of patients receiving placebo. The most common adverse events reported by patients receiving tolterodine tartrate extended-release capsules were dry mouth, headache, constipation, and abdominal pain. Dry mouth was the most frequently reported adverse event for patients treated with tolterodine tartrate extended-release capsules, occurring in 23.4% of patients treated with tolterodine tartrate extended-release capsules and 7.7% of placebo-treated patients.
Dry mouth, constipation, abnormal vision (accommodation abnormalities), urinary retention, and dry eyes are expected side effects of antimuscarinic agents. A serious adverse event was reported by 1.4% (n=7) of patients receiving tolterodine tartrate extended-release capsules and by 3.6% (n=18) of patients receiving 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.
Table 1. Incidence* (%) of Adverse Events Exceeding Placebo Rate and Reported in greater than or equal to 1% of Patients Treated with Tolterodine Tartrate Extended-Release Capsules (4 mg daily) in a 12-week, Phase 3 Clinical Trial * in nearest integer. Body System Adverse Event % Tolterodine Tartrate Extended-Release Capsules n=505 % Placebo n=507 Autonomic Nervous dry mouth 23 8 General headache 6 5 fatigue 2 1 Central/Peripheral Nervous dizziness 2 1 Gastrointestinal constipation 6 4 abdominal pain 4 2 dyspepsia 3 1 Vision xerophthalmia 3 2 vision abnormal 1 0 Psychiatric somnolence 3 2 anxiety 1 0 Respiratory sinusitis 2 1 Urinary dysuria 1 0 The frequency of discontinuation due to adverse events was highest during the first 4 weeks of treatment.
Similar percentages of patients treated with tolterodine tartrate extended-release capsules or placebo discontinued treatment due to adverse events. Dry mouth was the most common adverse event leading to treatment discontinuation among patients receiving tolterodine tartrate extended-release capsules [n=12 (2.4%) vs. placebo n=6 (1.2%)].
6.2Post-marketing Experience The following events have been reported in association with tolterodine use in worldwide post-marketing experience: General : anaphylaxis and angioedema; Cardiovascular : tachycardia, palpitations, peripheral edema; Gastrointestinal : diarrhea; Central/Peripheral Nervous : confusion, disorientation, memory impairment, hallucinations. Reports of aggravation of symptoms of dementia (e.g., confusion, disorientation, delusion) have been reported after tolterodine therapy was initiated in patients taking cholinesterase inh…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Potent CYP3A4 Inhibitors: Coadministration may increase systemic exposure to tolterodine tartrate extended-release capsules. Reduce tolterodine tartrate extended-release capsules dose to 2 mg once daily. ( 7.2 ) 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.
( 7.6 )
7.1Potent CYP2D6 Inhibitors 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. There was a 52% decrease in C max and a 20% decrease in AUC of 5-hydroxymethyl tolterodine (5-HMT), the pharmacologically active metabolite of tolterodine [see CLINICAL PHARMACOLOGY ( 12.1 )]. The sums of unbound serum concentrations of tolterodine and 5-HMT are only 25% higher during the interaction.
No dose adjustment is required when tolterodine and fluoxetine are co-administered [see CLINICAL PHARMACOLOGY ( 12.3 )].
7.2Potent CYP3A4 Inhibitors Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For patients receiving ketoconazole or other potent CYP3A4 inhibitors such as itraconazole, clarithromycin, or ritonavir, the recommended dose of tolterodine tartrate extended-release capsule is 2 mg once daily [see DOSAGE AND ADMINISTRATION ( 2.2 ) and CLINICAL PHARMACOLOGY ( 12.3 )].
7.3Other Interactions No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and levonorgestrel, or with diuretics [see CLINICAL PHARMACOLOGY ( 12.3 )].
7.4Other Drugs Metabolized by Cytochrome P450 Isoenzymes 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 [see CLINICAL PHARMACOLOGY ( 12.3 )].
7.5Drug-Laboratory-Test Interactions Interactions between tolterodine and laboratory tests have not been studied.
7.6Other Anticholinergics The concomitant use of tolterodine tartrate extended-release capsules with other anticholinergic (antimuscarinic) agents may increase the frequency and/or severity of dry mouth, constipation, blurred vision, somnolence, and other anticholinergic pharmacological effects.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Renal Impairment: Tolterodine tartrate extended-release capsules are not recommended for use in patients with CCr less than 10 mL/min. Dose adjustment in severe renal impairment (CCr: 10 mL/min to 30 mL/min). ( 8.6 ) Hepatic Impairment: Not recommended for use in severe hepatic impairment (Child Pugh Class C). Dose adjustment in mild to moderate hepatic impairment (Child Pugh Class A, B). ( 8.7 )
8.1Pregnancy Risk Summary There are no available data with tolterodine tartrate extended-release capsules use in pregnant women to inform drug-associated risks. In animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approximately 9 to 12 times the clinical exposure at a dose of 20 mg/kg/day; however, higher doses produced adverse developmental outcomes (see Data). In the U.S. general population, the estimated background rate of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Data Animal Data No anomalies or malformations were observed after oral administration of tolterodine to pregnant mice during organogenesis at approximately 9 to 12 times the clinical exposure to the pharmacologically active components of tolterodine tartrate extended-release capsules (based on the AUC of tolterodine and its 5-HMT metabolite at a dose of 20 mg/kg/day). At 14 to 18 times the clinical exposure (doses of 30 mg/kg/day to 40 mg/kg/day) in mice, tolterodine was embryo-lethal, caused reduced fetal weight, and increased the incidence of fetal abnormalities (cleft palate, digital abnormalities, intra-abdominal hemorrhage, and various skeletal abnormalities, primarily reduced ossification).
Pregnant rabbits administered tolterodine subcutaneously at about 0.3 to 2.5 times the clinical exposure (dose of 0.8 mg/kg/day) did not show any embryotoxicity or teratogenicity.
8.2Lactation Risk Summary There is no information on the presence of tolterodine or its 5-HMT metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Based on limited data, tolterodine is excreted into the milk in mice in low amounts (see Data) . The development and health benefits of breastfeeding should be considered along with the mother’s 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.
Animal Data The use of radiolabeled tolterodine in pregnant mice produced milk: plasma ratios that ranged between 0.0 and 0.7.
8.4Pediatric Use The effectiveness of tolterodine tartrate extended-release capsules has not been established in pediatric patients. Efficacy was not established in two randomized, placebo-controlled, double-blind, 12-week studies that enrolled 710 pediatric patients (486 on tolterodine tartrate extended-release capsules, 224 on placebo) aged 5 to10 years with urinary frequency and urge incontinence. 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%).
Aggressive, abnormal, and hyperactive behavior and attention disorders occurred in 2.9% of children treated with tolterodine tartrate extended-release capsules compared to 0.9% of children treated with placebo.
8.5Geriatric Use No overall differences in safety were observed between the older and younger patients treated with tolterodine. In multiple-dose studies in which tolterodine immediate release 4 mg (2 mg bid) was administered, serum concentrations of tolterodine and of 5-HMT were similar in healthy elderly volunteers (aged 64 through 80 years) and healthy young volunteers (aged less than 40 years). In another clinical study, elderly volunteers (aged 71…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary There are no available data with tolterodine tartrate extended-release capsules use in pregnant women to inform drug-associated risks. In animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approximately 9 to 12 times the clinical exposure at a dose of 20 mg/kg/day; however, higher doses produced adverse developmental outcomes (see Data). In the U.S. general population, the estimated background rate of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Data Animal Data No anomalies or malformations were observed after oral administration of tolterodine to pregnant mice during organogenesis at approximately 9 to 12 times the clinical exposure to the pharmacologically active components of tolterodine tartrate extended-release capsules (based on the AUC of tolterodine and its 5-HMT metabolite at a dose of 20 mg/kg/day). At 14 to 18 times the clinical exposure (doses of 30 mg/kg/day to 40 mg/kg/day) in mice, tolterodine was embryo-lethal, caused reduced fetal weight, and increased the incidence of fetal abnormalities (cleft palate, digital abnormalities, intra-abdominal hemorrhage, and various skeletal abnormalities, primarily reduced ossification).
Pregnant rabbits administered tolterodine subcutaneously at about 0.3 to 2.5 times the clinical exposure (dose of 0.8 mg/kg/day) did not show any embryotoxicity or teratogenicity.
🧒 Pediatric Use ▾
8.4Pediatric Use The effectiveness of tolterodine tartrate extended-release capsules has not been established in pediatric patients. Efficacy was not established in two randomized, placebo-controlled, double-blind, 12-week studies that enrolled 710 pediatric patients (486 on tolterodine tartrate extended-release capsules, 224 on placebo) aged 5 to10 years with urinary frequency and urge incontinence. 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%).
Aggressive, abnormal, and hyperactive behavior and attention disorders occurred in 2.9% of children treated with tolterodine tartrate extended-release capsules compared to 0.9% of children treated with placebo.
🧓 Geriatric Use ▾
8.5Geriatric Use No overall differences in safety were observed between the older and younger patients treated with tolterodine. In multiple-dose studies in which tolterodine immediate release 4 mg (2 mg bid) was administered, serum concentrations of tolterodine and of 5-HMT were similar in healthy elderly volunteers (aged 64 through 80 years) and healthy young volunteers (aged less than 40 years). In another clinical study, elderly volunteers (aged 71 through 81 years) were given tolterodine immediate release 2 or 4 mg (1 or 2 mg bid).
Mean serum concentrations of tolterodine and 5-HMT in these elderly volunteers were approximately 20% and 50% higher, respectively, than concentrations reported in young healthy volunteers. However, no overall differences were observed in safety between older and younger patients on tolterodine in the Phase 3, 12-week, controlled clinical studies; therefore, no tolterodine dosage adjustment for elderly patients is recommended.
🆘 Overdosage ▾
10 OVERDOSAGE Overdosage with tolterodine tartrate extended-release capsules can potentially result in severe central anticholinergic effects and should be treated accordingly. ECG monitoring is recommended in the event of overdosage. In dogs, changes in the QT interval (slight prolongation of 10% to 20%) were observed at a suprapharmacologic dose of 4.5 mg/kg, which is about 68 times higher than the recommended human dose.
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 WARNINGS AND PRECAUTIONS ( 5.9 ) and CLINICAL PHARMACOLOGY ( 12.2 )]. 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. The child fully recovered.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. 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 5-hydroxymethyl tolterodine (5-HMT), the major pharmacologically active metabolite.
5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and 5HMT 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.
12.2Pharmacodynamics Tolterodine has a pronounced effect on bladder function. 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 main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure.
These findings are consistent with an antimuscarinic action on the lower urinary tract. Cardiac Electrophysiology The effect of 2 mg BID and 4 mg BID of tolterodine tartrate immediate release tablets on the QT interval was evaluated in a 4-way crossover, double-blind, placebo- and active-controlled (moxifloxacin 400 mg QD) study in healthy male (N=25) and female (N=23) volunteers aged 18 to 55 years. 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.
The 4 mg BID dose of tolterodine IR (two times the highest recommended dose) was chosen because this dose results in tolterodine exposure similar to that observed upon coadministration of tolterodine 2 mg BID with potent CYP3A4 inhibitors in patients who are CYP2D6 poor metabolizers [see DRUG INTERACTIONS ( 7.2 )]. QT interval was measured over a 12-hour period following dosing, including the time of peak plasma concentration (T max ) of tolterodine and at steady state (Day 4 of dosing). Table 2 summarizes the mean change from baseline to steady state in corrected QT interval (QTc) relative to placebo at the time of peak tolterodine (1 hour) and moxifloxacin (2 hour) concentrations.
Both Fridericia’s (QTcF) and a population-specific (QTcP) method were used to correct QT interval for heart rate. No single QT correction method is known to be more valid than others. QT interval was measured manually and by machine, and data from both are presented.
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. The change in heart rate with moxifloxacin was 0.5 beats/minute. Table 2.
Mean (CI) change in QT c from baseline to steady state (Day 4 of dosing) at T max (relative to placebo) * At T max of 1 hr; 95% Confidence Interval. † At T max of 2 hr; 90% Confidence Interval. ‡ The effect on QT interval with 4 days of moxifloxacin dosing in this QT trial may be greater than typically observed in QT trials of other drugs. Drug/Dose N QT c F (msec) (manual) QT c F (msec) (machine) QT c P (msec) (manual) QT c P (msec) (machine) Tolterodine 2 mg BID* 48 5.01 (0.28, 9.74) 1.16 (-2.99, 5.30) 4.45 (-0.37, 9.26) 2.00 (-1.81, 5.81) Tolterodine 4 mg BID* 48 11.84 (7.11, 16.58) 5.63 (1.48, 9.77) 10.31 (5.49, 15.12) 8.34 (4.53, 12.15) Moxifloxacin 400 mg QD † 45 19.26‡ (15.49, 23.03) 8.90 (4.77, 13.03) 19.10‡ (15.32, 22.89) 9.29 (5.34, 13.24) The reason for the difference between machine and manual read of QT interval is unclear.
The QT effect of tolterodine immediate release tablets appeared greater for 8 mg/day (two times th…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. 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 5-hydroxymethyl tolterodine (5-HMT), the major pharmacologically active metabolite.
5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and 5HMT 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.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Tolterodine tartrate extended-release capsules are supplied as follows: 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. Bottles of 30 NDC 27241-191-30 Bottles of 90 NDC 27241-191-90 Bottles of 500 NDC 27241-191-05 The 4 mg capsules are blue opaque/blue opaque hard gelatin size "3" capsules imprinted with "ap" logo on cap and "T4" on body in white ink containing off-white to pale yellow colored pellets.
Bottles of 30 NDC 27241-192-30 Bottles of 90 NDC 27241-192-90 Bottles of 500 NDC 27241-192-05 Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Protect from light.
📋 Description ▾
11 DESCRIPTION Tolterodine tartrate extended-release capsule contain tolterodine tartrate, USP. The active moiety, tolterodine, is a muscarinic receptor antagonist. The chemical name of tolterodine tartrate, USP is (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine L-hydrogen tartrate.
The molecular formula of tolterodine tartrate, USP is C 26 H 37 NO 7 ,. Its structure is: Tolterodine tartrate, USP is white to off-white powder with a molecular weight of 475.6. The pKa value is 9.87 and the solubility in water is 14.83 mg/mL.
It is soluble in methanol, and sparingly soluble in water. The partition coefficient (Log D) between n-octanol and water is 1.83 at pH 7.3. Tolterodine tartrate extended-release capsules 4 mg for oral administration contains 4 mg of tolterodine tartrate, USP.
Inactive ingredients are microcrystalline cellulose, hypromellose, ethyl cellulose, medium chain triglycerides and oleic acids. The capsule shell contains FD&C Blue 2, titanium dioxide and gelatin. Tolterodine tartrate extended-release capsules 2 mg for oral administration contains 2 mg of tolterodine tartrate, USP.
Inactive ingredients are microcrystalline cellulose, hypromellose, ethyl cellulose, medium chain triglycerides and oleic acids. The capsule shell contains FD&C Blue 2, iron oxide yellow, titanium dioxide and gelatin. Both the 2 mg and 4 mg capsule strengths are imprinted with a pharmaceutical grade printing ink that contains shellac, titanium dioxide, propylene glycol, and simethicone. structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Antimuscarinic Effects Inform patients that antimuscarinic agents such as tolterodine tartrate extended-release capsules may have side effects including blurred vision, dizziness, or drowsiness. Advise patients not to drive, operate machinery, or do other potentially dangerous activities until they know how tolterodine tartrate extended-release capsules affects them.
Product of India Manufactured by: Ajanta Pharma Limited, India Marketed by: Ajanta Pharma USA Inc. Bridgewater, NJ 08807. #All trademarks are the properties of their respective owners Revised: 11/2025