Tolterodine Tart ER 4mg Capsules
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Anticholinergic; Muscarinic Receptor Antagonist
Pregnancy Category
C
FDA Approved
Sep 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Tolterodine ER is a medication used to treat an overactive bladder. It helps to relax the bladder muscles, which can reduce the sudden urge to urinate, the need to urinate frequently, and accidental urine leakage (incontinence). It's taken once a day.
How to Use This Medicine
Taking Your Medication Correctly
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 better.
Important Administration Instructions
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
Store your medication at room temperature, away from light and moisture.
Keep your medication in a dry place, such as a closet or drawer.
Do not store your medication in the bathroom.
Keep all medications in a safe and secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time.
* Do not take two doses at the same time or take extra doses to make up for a 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 better.
Important Administration Instructions
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
Store your medication at room temperature, away from light and moisture.
Keep your medication in a dry place, such as a closet or drawer.
Do not store your medication in the bathroom.
Keep all medications in a safe and secure location, out of the reach of children and pets.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take the capsule whole; do not chew, crush, or break it.
- Can be taken with or without food.
- Maintain adequate hydration to prevent constipation and dry mouth.
- Avoid or limit bladder irritants like caffeine, alcohol, carbonated drinks, and spicy foods.
- Practice timed voiding or bladder training techniques as advised by your doctor.
- Be aware of potential for dizziness or blurred vision, especially when driving or operating machinery.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
4 mg orally once daily
Dose Range:
2 - 4 mg
Condition-Specific Dosing:
initial_dose_for_some_patients:
2 mg orally once daily (e.g., those sensitive to anticholinergic side effects)
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (CrCl >30 mL/min)
Moderate:
2 mg orally once daily (CrCl 10-30 mL/min)
Severe:
2 mg orally once daily (CrCl <10 mL/min)
Dialysis:
2 mg orally once daily (limited data, use with caution)
Hepatic Impairment:
Mild:
No adjustment needed (Child-Pugh A)
Moderate:
2 mg orally once daily (Child-Pugh B)
Severe:
2 mg orally once daily (Child-Pugh C)
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It acts on muscarinic receptors in the bladder, inhibiting detrusor muscle contraction, thereby reducing symptoms of overactive bladder such as urinary urgency, frequency, and urge incontinence. It exhibits selectivity for the bladder over salivary glands in vivo.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive metabolizers), 65% (poor metabolizers)
Tmax:
2-4 hours (for ER capsule)
FoodEffect:
Negligible effect on absorption of ER capsule
Distribution:
Vd:
113 L
ProteinBinding:
Approximately 96% (primarily to alpha-1 acid glycoprotein)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 7 hours (extensive metabolizers), 10 hours (poor metabolizers)
Clearance:
Not available (variable due to metabolism)
ExcretionRoute:
Urine (77%), Feces (17%)
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Clinical benefit typically seen within 4-6 weeks of therapy
DurationOfAction:
24 hours (with ER formulation)
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, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact 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, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact 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 inability to have a bowel movement
- Inability to urinate or feeling of incomplete bladder emptying
- Severe eye pain or sudden vision changes (e.g., blurred vision, halos around lights)
- Signs of allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
- Confusion or hallucinations (especially in older adults)
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
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
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 reactions or judgment.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential 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 reactions or judgment.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe anticholinergic effects: severe dry mouth, blurred vision, dilated pupils, urinary retention, constipation, tachycardia (fast heart rate), fever, flushing, restlessness, confusion, hallucinations, seizures, respiratory depression.
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Physostigmine may be used in severe cases of central anticholinergic effects.
Drug Interactions
Contraindicated Interactions
- Not typically listed as contraindicated with specific drugs, but caution with strong CYP3A4 inhibitors in poor CYP2D6 metabolizers.
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir) in patients who are poor CYP2D6 metabolizers (increased exposure to tolterodine and active metabolite, potentially leading to increased anticholinergic side effects).
- Other anticholinergic agents (e.g., tricyclic antidepressants, phenothiazines, antipsychotics, antiarrhythmics, other antimuscarinics) - additive anticholinergic effects.
- Drugs that prolong QT interval (e.g., quinidine, sotalol, procainamide, amiodarone, pimozide, thioridazine) - theoretical risk of additive QT prolongation, though clinical significance is low with tolterodine.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., erythromycin, fluconazole) - may increase tolterodine exposure.
- Metoclopramide, cisapride (drugs affecting GI motility) - tolterodine may antagonize their effects.
Minor Interactions
- Not typically listed as minor interactions with specific drugs, but general caution with drugs that cause dry mouth or constipation.
Monitoring
Baseline Monitoring
Baseline urinary symptoms (frequency, urgency, incontinence episodes)
Rationale: To assess efficacy and establish treatment goals.
Timing: Prior to initiation of therapy
Renal and hepatic function (CrCl, LFTs)
Rationale: To determine appropriate dosing, especially in patients with suspected impairment.
Timing: Prior to initiation of therapy, if impairment is suspected
History of narrow-angle glaucoma, urinary retention, gastric retention
Rationale: Contraindications to therapy.
Timing: Prior to initiation of therapy
Routine Monitoring
Efficacy (improvement in OAB symptoms)
Frequency: Periodically (e.g., 4-6 weeks after initiation, then every 3-6 months)
Target: Patient-reported improvement in urgency, frequency, and incontinence episodes
Action Threshold: Lack of improvement or worsening symptoms may warrant dose adjustment or alternative therapy
Anticholinergic side effects (dry mouth, constipation, blurred vision, urinary retention, cognitive changes)
Frequency: Regularly, especially during initial weeks and with dose changes
Target: Tolerable level of side effects
Action Threshold: Intolerable side effects may warrant dose reduction or discontinuation
Post-void residual (PVR) volume
Frequency: Periodically, especially if symptoms of urinary retention develop or worsen
Target: <100-150 mL (generally)
Action Threshold: Significantly increased PVR (>200-300 mL) may indicate urinary retention and require discontinuation
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Urinary retention (difficulty urinating, feeling of incomplete emptying)
- Headache
- Dizziness
- Somnolence
- Abdominal pain
- Confusion (especially in elderly)
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Animal studies showed adverse effects at high doses. Human data is limited.
Second Trimester:
Limited human data, potential for fetal exposure.
Third Trimester:
Limited human data, potential for fetal exposure.
Lactation
L3 (Moderately Safe). Tolterodine and its active metabolite are excreted into breast milk in animals. It is not known if they are excreted in human milk. Weigh the potential benefits of breastfeeding against the potential risks to the infant (e.g., anticholinergic effects like dry mouth, constipation, sedation).
Infant Risk:
Potential for anticholinergic effects in the infant. Monitor for dry mouth, constipation, decreased feeding, or sedation.
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, but increased sensitivity to anticholinergic side effects (e.g., dry mouth, constipation, cognitive impairment) cannot be ruled out. Consider starting with a lower dose (2 mg ER once daily) in frail elderly patients or those with multiple comorbidities.
Clinical Information
Clinical Pearls
- Tolterodine ER offers once-daily dosing, which can improve patient adherence compared to immediate-release formulations.
- It is metabolized by both CYP2D6 and CYP3A4, making it important to consider potential drug interactions, especially with strong CYP3A4 inhibitors in patients who are poor CYP2D6 metabolizers.
- Patients should be advised about common anticholinergic side effects such as dry mouth, constipation, and blurred vision. Strategies to manage these (e.g., sugar-free candies, increased fiber, artificial tears) can be helpful.
- Monitor for signs of urinary retention, especially in patients with bladder outlet obstruction, as this is a contraindication.
- Cognitive impairment is a concern, particularly in the elderly. Assess for changes in mental status.
- Contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma.
Alternative Therapies
- Other Anticholinergics: Oxybutynin (Ditropan, Oxytrol), Solifenacin (Vesicare), Darifenacin (Enablex), Fesoterodine (Toviaz), Trospium (Sanctura)
- Beta-3 Adrenergic Agonists: Mirabegron (Myrbetriq), Vibegron (Gemtesa)
- OnabotulinumtoxinA (Botox) injections into the detrusor muscle
- Neuromodulation: Sacral neuromodulation (SNS), Percutaneous tibial nerve stimulation (PTNS)
- Behavioral therapies: Bladder training, timed voiding, pelvic floor muscle exercises
Cost & Coverage
Average Cost:
$30 - $150 per 30 capsules (generic)
Generic Available:
Yes
Insurance Coverage:
Generic formulations are typically covered as Tier 1 or Tier 2 by most insurance plans. Brand name may be Tier 3 or higher.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure 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 seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.