Detrol 2mg Tablets
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Muscarinic Receptor Antagonist
Pregnancy Category
Category C
FDA Approved
Dec 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Tolterodine is a medication used to treat overactive bladder. It helps to reduce the sudden urge to urinate, frequent urination, and accidental leakage by relaxing the bladder muscles.
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 try to take it 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. Avoid storing it in a 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 once 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 try to take it 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. Avoid storing it in a 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 once or take extra doses to make up for the missed one.
Lifestyle & Tips
- Maintain adequate hydration, but avoid excessive fluid intake, especially before bedtime.
- Limit caffeine and alcohol intake, as these can irritate the bladder.
- Practice bladder training techniques (e.g., gradually increasing time between urinations).
- Perform pelvic floor exercises (Kegel exercises) to strengthen bladder control.
- Manage constipation, as it can worsen OAB symptoms.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
2 mg twice daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
initial_dose_hepatic_renal_impairment_or_strong_CYP3A4_inhibitors:
1 mg 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 >30 mL/min)
Moderate:
No adjustment needed (CrCl >30 mL/min)
Severe:
Reduce dose to 1 mg twice daily (CrCl <30 mL/min)
Dialysis:
Not specifically studied, but likely requires dose reduction similar to severe impairment due to renal excretion of metabolites.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
Reduce dose to 1 mg twice daily
Severe:
Reduce dose to 1 mg twice daily
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It acts on muscarinic receptors in the bladder, inhibiting the cholinergic stimulation of detrusor muscle contraction, thereby reducing symptoms of overactive bladder such as urinary urgency, frequency, and urge incontinence.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive first-pass metabolism in extensive metabolizers), 65% (poor metabolizers)
Tmax:
1-2 hours (tolterodine), 2-4 hours (5-hydroxymethyl metabolite)
FoodEffect:
Food increases bioavailability by approximately 20% but does not significantly alter Cmax or Tmax.
Distribution:
Vd:
113 L (tolterodine), 134 L (5-hydroxymethyl metabolite)
ProteinBinding:
Approximately 96% (tolterodine), 85% (5-hydroxymethyl metabolite)
CnssPenetration:
Limited
Elimination:
HalfLife:
2-3 hours (tolterodine), 3-4 hours (5-hydroxymethyl metabolite)
Clearance:
Not available
ExcretionRoute:
Urine (approximately 77%), Feces (approximately 17%)
Unchanged:
<1% (tolterodine), ~5-10% (5-hydroxymethyl metabolite)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Full therapeutic effect may take 4-8 weeks
DurationOfAction:
Approximately 12 hours (for immediate release formulation)
Note:
Clinical benefit is typically assessed after several weeks of treatment.
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 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
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
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.
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 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
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
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 or significant difficulty emptying the bladder
- Eye pain or sudden vision changes (e.g., blurred vision, halos around lights)
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
- Confusion or hallucinations
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
Existing kidney disease or liver disease
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Natural products and vitamins you are using
Any health problems you have
Before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any medication, consult with your doctor to confirm it is safe for you to do so.
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
Existing kidney disease or liver disease
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Natural products and vitamins you are using
Any health problems you have
Before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any medication, consult with your doctor to confirm it is safe for you to do so.
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: severe dry mouth, dilated pupils, blurred vision, hot and dry skin, fever, flushing, tachycardia, hypertension, urinary retention, constipation.
- Central nervous system excitation: restlessness, confusion, hallucinations, delirium, convulsions.
What to Do:
Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is symptomatic and supportive. Physostigmine may be considered for severe central anticholinergic effects.
Drug Interactions
Major Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir) in patients who are poor CYP2D6 metabolizers (due to significantly increased exposure to tolterodine and its active metabolite).
- Drugs that prolong the QT interval (e.g., quinidine, procainamide, sotalol, amiodarone, cisapride, pimozide, thioridazine) - potential for additive QT prolongation.
Moderate Interactions
- Other anticholinergic agents (e.g., oxybutynin, tricyclic antidepressants, phenothiazines) - potential for additive anticholinergic effects (dry mouth, constipation, urinary retention, blurred vision).
- Metoclopramide (decreased effect of metoclopramide due to anticholinergic action).
- Warfarin (potential for increased INR, monitor closely).
Minor Interactions
- Not specifically categorized as minor, but general caution with drugs that may cause dizziness or drowsiness.
Monitoring
Baseline Monitoring
Bladder diary/symptom assessment
Rationale: To establish baseline severity of OAB symptoms (urgency, frequency, incontinence episodes) and track treatment efficacy.
Timing: Prior to initiation of therapy
Renal function (CrCl)
Rationale: To identify patients requiring dose adjustment due to severe renal impairment.
Timing: Prior to initiation, if renal impairment is suspected or known
Hepatic function (LFTs)
Rationale: To identify patients requiring dose adjustment due to moderate to severe hepatic impairment.
Timing: Prior to initiation, if hepatic impairment is suspected or known
Routine Monitoring
Efficacy assessment (symptom improvement)
Frequency: Periodically, typically after 4-8 weeks of treatment and then as clinically indicated
Target: Reduction in urgency, frequency, and incontinence episodes
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Adverse effects (e.g., dry mouth, constipation, blurred vision, urinary retention)
Frequency: Regularly, especially during initial weeks of therapy and with dose changes
Target: Tolerable side effect profile
Action Threshold: Intolerable side effects may require dose reduction or discontinuation.
Post-void residual (PVR) volume
Frequency: Periodically, especially in patients at risk for urinary retention (e.g., BPH)
Target: <100-150 mL
Action Threshold: Significant increase in PVR (e.g., >200 mL) may indicate urinary retention and necessitate discontinuation.
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Dizziness
- Headache
- Urinary retention (difficulty urinating, feeling of incomplete bladder emptying)
- Abdominal pain
- Somnolence
Special Patient Groups
Pregnancy
Category C. Animal studies have shown adverse effects on the fetus at doses higher than human therapeutic doses. 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, though human data are limited.
Second Trimester:
Potential for developmental abnormalities, though human data are limited.
Third Trimester:
Potential for developmental abnormalities, though human data are limited.
Lactation
L3 (Moderately Safe). Tolterodine and its active metabolite are excreted into breast milk in animals. It is unknown if they are excreted in human milk. Potential for anticholinergic effects in the infant (e.g., dry mouth, constipation, urinary retention, tachycardia). Weigh the developmental and health benefits of breastfeeding against the mother's clinical need for tolterodine and any potential adverse effects on the breastfed infant.
Infant Risk:
Potential for anticholinergic effects (e.g., dry mouth, constipation, urinary retention, tachycardia, drowsiness).
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 greater sensitivity of some older individuals cannot be ruled out. Dose adjustment is not routinely required based on age alone, but consider lower initial doses (1 mg BID) in patients with renal or hepatic impairment, which is more common in the elderly. Elderly patients may be more susceptible to anticholinergic side effects (e.g., dry mouth, constipation, cognitive impairment, urinary retention).
Clinical Information
Clinical Pearls
- Tolterodine is available in both immediate-release (Detrol) and extended-release (Detrol LA) formulations. Detrol is dosed twice daily, while Detrol LA is once daily.
- The active metabolite, 5-hydroxymethyl tolterodine, contributes significantly to the pharmacological effect.
- Patients who are poor CYP2D6 metabolizers will have higher exposure to unchanged tolterodine and may require dose adjustment, especially if also taking strong CYP3A4 inhibitors.
- Common anticholinergic side effects (dry mouth, constipation, blurred vision) are generally mild to moderate and may decrease over time.
- Monitor for signs of urinary retention, especially in men with benign prostatic hyperplasia (BPH).
Alternative Therapies
- Other antimuscarinics: Oxybutynin (Ditropan), Solifenacin (Vesicare), Darifenacin (Enablex), Fesoterodine (Toviaz), Trospium (Sanctura)
- Beta-3 adrenergic agonists: Mirabegron (Myrbetriq), Vibegron (Gemtesa)
- OnabotulinumtoxinA (Botox) bladder injections (for refractory OAB)
- Neuromodulation (e.g., sacral neuromodulation, percutaneous tibial nerve stimulation)
- Behavioral therapies (e.g., bladder training, pelvic floor muscle training, fluid management)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 for generic per 30 tablets
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 is 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 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.