Tolterodine Tartrate 2mg Tablets
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodics; Antimuscarinics
Pharmacologic Class
Muscarinic Receptor Antagonists
Pregnancy Category
Category C
FDA Approved
Jun 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Tolterodine is a medication used to treat overactive bladder (OAB) symptoms like needing to urinate very often, having a sudden urge to urinate, and leaking urine. It works by relaxing the bladder muscle, which helps your bladder hold more urine and reduces the urge to go.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Ensure that all medications are kept in a safe location, out of reach of children and pets.
Missing a Dose
If you miss a dose, skip it 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 one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Ensure that all medications are kept in a safe location, out of reach of children and pets.
Missing a Dose
If you miss a dose, skip it 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 one.
Lifestyle & Tips
- Practice bladder training techniques (e.g., timed voiding, delaying urination).
- Perform pelvic floor exercises (Kegel exercises) to strengthen bladder control.
- Manage fluid intake, avoiding excessive caffeine and alcohol, which can irritate the bladder.
- Maintain a healthy weight and manage constipation, as these can worsen OAB symptoms.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
2 mg orally twice daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
initial_dose_hepatic_renal_impairment_or_strong_CYP3A4_inhibitors:
1 mg orally twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (CrCl >50 mL/min)
Moderate:
1 mg orally twice daily (CrCl 10-50 mL/min)
Severe:
1 mg orally twice daily (CrCl <10 mL/min)
Dialysis:
1 mg orally twice daily (no specific data for dialysis, but severe impairment dose applies)
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
1 mg orally twice daily
Severe:
1 mg orally twice daily
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It acts on muscarinic receptors in the bladder, inhibiting detrusor muscle contraction, thereby increasing bladder capacity and decreasing the frequency of involuntary detrusor contractions characteristic of overactive bladder.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive metabolizers), 77% (poor metabolizers)
Tmax:
1-2 hours (tolterodine), 2-4 hours (5-hydroxymethyl metabolite)
FoodEffect:
No significant effect on absorption
Distribution:
Vd:
113 L (tolterodine), 134 L (5-hydroxymethyl metabolite)
ProteinBinding:
96% (tolterodine), 63% (5-hydroxymethyl metabolite)
CnssPenetration:
Limited, but can cause CNS effects
Elimination:
HalfLife:
2-4 hours (tolterodine), 3-10 hours (5-hydroxymethyl metabolite)
Clearance:
Not available (highly variable due to metabolism)
ExcretionRoute:
77% urine, 17% feces
Unchanged:
<1% (tolterodine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Full clinical effect may take 4-6 weeks
DurationOfAction:
Approximately 12 hours (for IR formulation)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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 may be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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 may be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
If you experience any of these symptoms, seek medical help immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Feeling dizzy or sleepy
Headache
Stomach pain
Constipation
Dry mouth
Dry eyes
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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 inability to have a bowel movement
- Inability to urinate (urinary retention)
- Severe eye pain or sudden vision changes (especially if you have glaucoma)
- Signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
- Confusion, hallucinations, or significant memory problems
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 dose 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 dose 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 drug 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.
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 drug 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.
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, flushing, tachycardia (fast heart rate), urinary retention, dilated pupils, CNS excitation (e.g., restlessness, confusion, hallucinations, seizures), or severe drowsiness/stupor.
What to Do:
Seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is symptomatic and supportive. Gastric lavage, activated charcoal, and physostigmine (for severe CNS effects) may be considered by medical professionals.
Drug Interactions
Contraindicated Interactions
- Uncontrolled narrow-angle glaucoma
- Urinary retention
- Gastric retention
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) in patients who are poor CYP2D6 metabolizers (significant increase in tolterodine exposure)
- Other anticholinergic agents (e.g., tricyclic antidepressants, phenothiazines, antipsychotics, antihistamines) due to additive anticholinergic effects
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., erythromycin, fluconazole)
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine) in extensive metabolizers (can increase tolterodine levels and decrease active metabolite levels)
- Metoclopramide (antagonistic effect on GI motility)
Minor Interactions
- Not many clinically significant minor interactions specifically noted beyond additive anticholinergic effects with other agents.
Monitoring
Baseline Monitoring
Bladder diary
Rationale: To assess baseline symptoms of urgency, frequency, and incontinence episodes.
Timing: Before initiation
Urinalysis
Rationale: To rule out urinary tract infection or other causes of OAB symptoms.
Timing: Before initiation
Assessment for contraindications
Rationale: To ensure patient does not have uncontrolled narrow-angle glaucoma, urinary retention, or gastric retention.
Timing: Before initiation
Routine Monitoring
Efficacy (OAB symptoms)
Frequency: 2-4 weeks after initiation/dose change, then periodically (e.g., every 3-6 months)
Target: Reduction in urgency, frequency, and incontinence episodes
Action Threshold: Lack of improvement or worsening of symptoms may indicate need for dose adjustment or alternative therapy.
Adverse effects (e.g., dry mouth, constipation, blurred vision, urinary retention, cognitive changes)
Frequency: At each follow-up visit (e.g., 2-4 weeks after initiation, then periodically)
Target: Tolerable side effect profile
Action Threshold: Intolerable side effects may require 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: Significant increase in PVR (>200-300 mL) may indicate urinary retention and necessitate discontinuation.
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Difficulty urinating or feeling of incomplete bladder emptying (urinary retention)
- Abdominal pain
- Headache
- Dizziness
- Cognitive changes (e.g., confusion, memory impairment, drowsiness)
Special Patient Groups
Pregnancy
Category C. Animal studies have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for developmental abnormalities based on animal data; human data limited.
Second Trimester:
Limited human data; potential for anticholinergic effects on fetus (e.g., decreased fetal movement, decreased amniotic fluid).
Third Trimester:
Limited human data; potential for anticholinergic effects on fetus/neonate (e.g., urinary retention, decreased GI motility).
Lactation
L3 (Moderately Safe). Tolterodine and its active metabolite are excreted into breast milk. Potential for anticholinergic effects in the breastfed infant (e.g., constipation, dry mouth, sedation). Use with caution; monitor infant for adverse effects.
Infant Risk:
Low to moderate risk of anticholinergic effects.
Pediatric Use
Safety and efficacy have not been established for the treatment of overactive bladder in pediatric patients. Not recommended for this population.
Geriatric Use
Use with caution due to increased susceptibility to anticholinergic side effects (e.g., dry mouth, constipation, urinary retention, cognitive impairment, blurred vision). Consider starting with a lower dose (1 mg twice daily) in frail elderly patients or those on other anticholinergic medications.
Clinical Information
Clinical Pearls
- Tolterodine IR (immediate-release) is dosed twice daily, while the ER (extended-release) formulation is once daily.
- Full therapeutic effect may not be observed for several weeks (up to 4-6 weeks), so patients should be advised to continue treatment even if immediate improvement is not seen.
- Patients should be screened for conditions that could be worsened by anticholinergic effects, such as uncontrolled narrow-angle glaucoma, urinary retention, or severe gastrointestinal motility disorders.
- Dry mouth is a common side effect; advise patients on strategies like sugar-free candy/gum or frequent sips of water.
- Monitor for signs of urinary retention, especially in men with benign prostatic hyperplasia (BPH).
Alternative Therapies
- Other antimuscarinics (e.g., oxybutynin, solifenacin, darifenacin, fesoterodine, trospium)
- Beta-3 adrenergic agonists (e.g., mirabegron, vibegron)
- OnabotulinumtoxinA (Botox) injections into the detrusor muscle
- Sacral neuromodulation
- Percutaneous tibial nerve stimulation (PTNS)
- Behavioral therapies (e.g., bladder training, timed voiding, fluid management, pelvic floor muscle training)
Cost & Coverage
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.