Tolterodine Tart 2mg ER Capsules
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Muscarinic Receptor Antagonist
Pregnancy Category
Category C
FDA Approved
Feb 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Tolterodine extended-release is a medication used to treat symptoms of an overactive bladder, such as a strong, sudden urge to urinate, needing to urinate often, and leaking urine (urge incontinence). It works by relaxing the bladder muscles.
How to Use This Medicine
Taking Your Medication
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start feeling well.
Swallow your medication whole; do not chew, open, or crush it.
Take your medication with a full glass of water.
Storing and Disposing of Your Medication
To ensure the quality and safety of your medication:
Store your medication at room temperature, away from light.
Keep your medication in a dry place.
Do not store your medication in the bathroom.
Keep all medications in a safe and secure location.
Make sure to keep all medications out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Skip the missed dose and resume your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for the missed dose.
To get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food.
Take your medication at the same time every day to establish a routine.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start feeling well.
Swallow your medication whole; do not chew, open, or crush it.
Take your medication with a full glass of water.
Storing and Disposing of Your Medication
To ensure the quality and safety of your medication:
Store your medication at room temperature, away from light.
Keep your medication in a dry place.
Do not store your medication in the bathroom.
Keep all medications in a safe and secure location.
Make sure to keep all medications out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Skip the missed dose and resume your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Avoid activities requiring mental alertness (e.g., driving, operating machinery) until you know how this medication affects you, as it may cause dizziness or blurred vision.
- Stay hydrated to help with dry mouth, but avoid excessive fluid intake if it worsens bladder symptoms.
- Manage constipation by increasing fiber intake, drinking plenty of water, and engaging in regular physical activity.
- Avoid alcohol, as it can worsen dizziness and other side effects.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
2 mg extended-release capsule orally once daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
Overactive Bladder (OAB):
2 mg extended-release capsule orally once daily. May be reduced to 1 mg extended-release capsule once daily based on individual response and tolerability.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
1 mg extended-release capsule orally once daily
Severe:
1 mg extended-release capsule orally once daily
Dialysis:
Not studied, caution advised. Consider 1 mg extended-release capsule once daily.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
1 mg extended-release capsule orally once daily
Severe:
1 mg extended-release capsule orally once daily
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It exerts its effect by blocking muscarinic receptors, primarily M2 and M3 subtypes, in the bladder, thereby inhibiting involuntary bladder contractions and increasing bladder capacity. This leads to a reduction in symptoms of overactive bladder such as urinary urgency, frequency, and urge incontinence.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive metabolizers), 65% (poor metabolizers)
Tmax:
2-4 hours (extended-release)
FoodEffect:
Food does not significantly affect the absorption of tolterodine extended-release capsules.
Distribution:
Vd:
113 L (extensive metabolizers), 211 L (poor metabolizers)
ProteinBinding:
96% (tolterodine), 63% (5-hydroxymethyl metabolite)
CnssPenetration:
Limited
Elimination:
HalfLife:
6-10 hours (tolterodine), 15-20 hours (5-hydroxymethyl metabolite)
Clearance:
Not available
ExcretionRoute:
Urine (77%), Feces (17%)
Unchanged:
Less than 1% (tolterodine), 5-14% (5-hydroxymethyl metabolite)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
Within 4 weeks
DurationOfAction:
24 hours (due to extended-release formulation and active metabolite)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Changes in eyesight
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Changes in eyesight
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe constipation or abdominal pain
- Difficulty urinating or inability to urinate (urinary retention)
- Severe blurred vision or eye pain
- Signs of an allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Fast or irregular heartbeat
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Urinary retention (trouble passing urine)
+ Glaucoma
+ Gastrointestinal issues, such as slow stomach emptying
Pre-existing kidney disease or liver disease
Additionally, to ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems
It is crucial to verify that this medication is safe to take with all your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Urinary retention (trouble passing urine)
+ Glaucoma
+ Gastrointestinal issues, such as slow stomach emptying
Pre-existing kidney disease or liver disease
Additionally, to ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Your complete medical history, including any health problems
It is crucial to verify that this medication is safe to take with all your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Consult your doctor before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter medications that may impair your reaction time or alertness.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss this with your doctor. You and your doctor will need to weigh the benefits and risks of this medication to both you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Consult your doctor before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter medications that may impair your reaction time or alertness.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss this with your doctor. You and your doctor will need to weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe anticholinergic effects (e.g., severe dry mouth, dilated pupils, hot and dry skin, rapid heart rate, urinary retention, constipation)
- Central nervous system excitation (e.g., restlessness, confusion, hallucinations, seizures)
- Respiratory depression
What to Do:
Seek immediate medical attention or call 911. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic. Gastric lavage may be considered. Physostigmine may be used for severe central anticholinergic effects.
Drug Interactions
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir): Increased tolterodine exposure, especially in poor CYP2D6 metabolizers. Reduce tolterodine dose to 1 mg ER daily.
- Other anticholinergic agents (e.g., oxybutynin, solifenacin, tricyclic antidepressants): Additive anticholinergic effects, increasing risk of dry mouth, constipation, urinary retention, and blurred vision.
Moderate Interactions
- Drugs that prolong QT interval (e.g., quinidine, sotalol, procainamide, amiodarone, pimozide, thioridazine): Theoretical risk of additive QT prolongation, though tolterodine's effect on QT is generally small at therapeutic doses.
- Metoclopramide, cisapride: May antagonize the prokinetic effects of these drugs due to anticholinergic activity.
Minor Interactions
- Warfarin: No significant interaction reported, but monitor INR if co-administered.
- Digoxin: No significant interaction reported.
Monitoring
Baseline Monitoring
Renal function (e.g., serum creatinine, eGFR)
Rationale: To determine appropriate dosing in patients with renal impairment.
Timing: Prior to initiation, especially if renal impairment is suspected or known.
Hepatic function (e.g., ALT, AST, bilirubin)
Rationale: To determine appropriate dosing in patients with hepatic impairment.
Timing: Prior to initiation, especially if hepatic impairment is suspected or known.
Baseline symptoms of OAB (e.g., voiding diary)
Rationale: To assess treatment efficacy and patient response.
Timing: Prior to initiation.
Routine Monitoring
Efficacy (reduction in urgency, frequency, incontinence episodes)
Frequency: Periodically, typically within 4-8 weeks of initiation and then as clinically indicated.
Target: Patient-reported improvement in OAB symptoms.
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Anticholinergic side effects (e.g., dry mouth, constipation, blurred vision, urinary retention)
Frequency: Regularly, especially during initial weeks of therapy and after dose adjustments.
Target: Tolerable level of side effects.
Action Threshold: Severe or intolerable side effects may require dose reduction or discontinuation.
Post-void residual (PVR) volume
Frequency: If concerns about urinary retention arise, or in patients with pre-existing bladder outlet obstruction.
Target: < 100-150 mL (generally)
Action Threshold: Significant increase in PVR or symptoms of urinary retention (e.g., difficulty voiding, feeling of incomplete emptying) may require discontinuation.
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Urinary retention (difficulty urinating, feeling of incomplete bladder emptying)
- Dizziness
- Headache
- Somnolence
- Abdominal pain
Special Patient Groups
Pregnancy
Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high doses, but there are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data; avoid if possible.
Second Trimester:
Limited human data; use with caution.
Third Trimester:
Limited human data; use with caution.
Lactation
It is not known whether tolterodine or its active metabolite are excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk L3 (Moderate concern - no human data, potential for anticholinergic effects in infant).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Not recommended for use in children.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients. However, elderly patients may be more susceptible to anticholinergic side effects (e.g., dry mouth, constipation, cognitive impairment, urinary retention). Use with caution and monitor closely.
Clinical Information
Clinical Pearls
- Tolterodine ER is generally preferred over immediate-release due to once-daily dosing and potentially fewer anticholinergic side effects.
- Patients should be advised that full therapeutic effect may take several weeks (up to 4-8 weeks) to be observed.
- Ensure patients understand the importance of reporting urinary retention symptoms, as this is a contraindication.
- For patients experiencing bothersome dry mouth, suggest sugar-free candies, chewing gum, or artificial saliva products.
- Consider a lower dose (1 mg ER) for patients with moderate to severe renal or hepatic impairment, or those taking strong CYP3A4 inhibitors.
Alternative Therapies
- Other anticholinergic agents (e.g., oxybutynin, solifenacin, darifenacin, fesoterodine)
- Beta-3 adrenergic agonists (e.g., mirabegron, vibegron)
- OnabotulinumtoxinA (Botox) injections into the bladder
- Percutaneous tibial nerve stimulation (PTNS)
- Sacral neuromodulation (SNS)
- Behavioral therapies (e.g., bladder training, pelvic floor muscle exercises)
Cost & Coverage
Average Cost:
$100 - $300 per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 or Non-Formulary (for brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.