Detrol LA 2mg Capsules
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Antimuscarinic; Anticholinergic
Pregnancy Category
Category C
FDA Approved
Feb 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Detrol LA is a medication used to treat overactive bladder (OAB) symptoms like frequent urination, urgent need to urinate, and leaking urine. It works by relaxing the bladder muscle, helping it hold more urine and reducing the sudden urges to go.
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 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 direct light.
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.
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 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 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 direct light.
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.
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 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 the missed dose.
Lifestyle & Tips
- Take the capsule whole; do not chew, crush, or divide it.
- Can be taken with or without food.
- Manage dry mouth by sipping water, chewing sugar-free gum, or using saliva substitutes.
- Prevent constipation by increasing fiber intake, drinking plenty of fluids, and engaging in regular physical activity.
- 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.
- Limit alcohol consumption, as it may worsen dizziness or drowsiness.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
2 mg extended-release capsule orally once daily
Dose Range:
1 - 4 mg
Condition-Specific Dosing:
initial_dose:
2 mg extended-release capsule orally once daily
maximum_dose:
4 mg extended-release capsule orally once daily (if 2 mg is well tolerated and further symptom reduction is desired)
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
1 mg extended-release capsule orally once daily (CrCl <30 mL/min)
Dialysis:
Use with caution; consider 1 mg once daily. No specific data for dialysis patients.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
1 mg extended-release capsule orally once daily (Child-Pugh Class B)
Severe:
1 mg extended-release capsule orally once daily (Child-Pugh Class C)
Confidence:
High
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It exhibits selectivity for the urinary bladder over salivary glands in vivo. The M3 muscarinic receptor subtype is primarily responsible for bladder smooth muscle contraction. By blocking muscarinic receptors, tolterodine reduces detrusor muscle activity, thereby decreasing urinary frequency, urgency, and urge incontinence associated with overactive bladder.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 17% (poor CYP2D6 metabolizers) to 77% (extensive CYP2D6 metabolizers) for immediate release; extended-release formulation provides sustained release.
Tmax:
2 to 6 hours (for tolterodine and its active 5-hydroxymethyl metabolite)
FoodEffect:
Food increases Cmax and AUC of tolterodine by approximately 20% and 30% respectively, but this is not considered clinically significant, and Detrol LA can be taken with or without food.
Distribution:
Vd:
Approximately 113 L (tolterodine)
ProteinBinding:
Approximately 96% (tolterodine) and 85% (5-hydroxymethyl metabolite) to alpha-1 acid glycoprotein and albumin.
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 7 hours (tolterodine) and 3.5 hours (5-hydroxymethyl metabolite) in extensive metabolizers; significantly longer in poor CYP2D6 metabolizers.
Clearance:
Not available
ExcretionRoute:
Urine (approximately 77%), Feces (approximately 17%)
Unchanged:
Less than 1% (tolterodine)
Pharmacodynamics
OnsetOfAction:
Within 1 week
PeakEffect:
Within 4 weeks
DurationOfAction:
24 hours (due to extended-release 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 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 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
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 for medical advice. 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 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
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 for medical advice. 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:
- Inability to urinate (urinary retention)
- Severe constipation
- Severe abdominal pain
- Eye pain or vision changes (especially if you have glaucoma)
- Signs of an allergic reaction (rash, itching, swelling, 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 allergic reaction you experienced, including any symptoms that occurred.
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, it is crucial to disclose all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
Your doctor and pharmacist need this information to assess potential interactions between this medication and your other treatments or health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm it is safe 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 allergic reaction you experienced, including any symptoms that occurred.
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, it is crucial to disclose all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
Your doctor and pharmacist need this information to assess potential interactions between this medication and your other treatments or health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor to confirm it is safe 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 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 (e.g., severe dry mouth, blurred vision, dilated pupils, hot/dry skin, fever)
- Urinary retention
- Severe constipation
- Central nervous system excitation (e.g., restlessness, confusion, hallucinations, seizures)
- Tachycardia
- Respiratory depression
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Gastric lavage may be performed. Physostigmine may be considered for severe central anticholinergic effects.
Drug Interactions
Major Interactions
- Potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir) in patients who are poor CYP2D6 metabolizers or in patients with renal/hepatic impairment (due to increased tolterodine exposure and risk of anticholinergic side effects).
- Other anticholinergic agents (additive effects, increased risk of urinary retention, severe constipation, blurred vision).
Moderate Interactions
- Potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir) in extensive CYP2D6 metabolizers (monitor for increased anticholinergic side effects).
- Drugs that prolong QT interval (e.g., quinidine, sotalol, procainamide, amiodarone, tricyclic antidepressants, phenothiazines) - theoretical risk of additive QT prolongation, use with caution.
- Metoclopramide, cisapride (may antagonize prokinetic effects).
Minor Interactions
- Warfarin (no clinically significant interaction reported, but monitor INR if co-administered).
Monitoring
Baseline Monitoring
Urinary symptoms (frequency, urgency, incontinence episodes)
Rationale: To establish baseline severity and assess treatment efficacy.
Timing: Prior to initiation of therapy
Post-void residual (PVR) volume
Rationale: To assess for baseline urinary retention, especially in patients with bladder outlet obstruction.
Timing: Prior to initiation of therapy
Renal and hepatic function tests (CrCl, LFTs)
Rationale: To determine appropriate dosing in patients with impairment.
Timing: Prior to initiation of therapy if impairment is suspected or known
Routine Monitoring
Urinary symptoms
Frequency: Periodically (e.g., 4-8 weeks after initiation, then every 3-6 months)
Target: Reduction in frequency, urgency, and incontinence episodes
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Anticholinergic side effects (dry mouth, constipation, blurred vision, urinary retention)
Frequency: Regularly, especially during initial weeks of therapy and with dose adjustments
Target: Tolerable level of side effects
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 mL) may indicate urinary retention and require discontinuation.
Symptom Monitoring
- Dry mouth
- Constipation
- Blurred vision
- Urinary retention (difficulty urinating, feeling of incomplete emptying)
- Dizziness
- Headache
- Somnolence
- Abdominal pain
- Dyspepsia
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at doses higher than clinical doses, but there are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity observed in animal studies at high doses.
Second Trimester:
No specific data, but generally considered similar risk to first trimester.
Third Trimester:
No specific data, but generally considered similar risk to first trimester.
Lactation
It is not known whether tolterodine is 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:
L3 (Moderately safe; potential for anticholinergic effects in infant, monitor for dry mouth, constipation, sedation, or irritability).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Not indicated 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. Use with caution and monitor for adverse effects.
Clinical Information
Clinical Pearls
- Detrol LA is an extended-release formulation, offering once-daily dosing, which may improve patient adherence compared to immediate-release formulations.
- Patients who are poor CYP2D6 metabolizers or those taking potent CYP3A4 inhibitors may have significantly increased tolterodine exposure, requiring a dose reduction to 1 mg daily.
- While generally well-tolerated, anticholinergic side effects like dry mouth and constipation are common. Advise patients on management strategies.
- Always assess for bladder outlet obstruction before initiating therapy, as antimuscarinics can precipitate urinary retention in these patients.
- Consider alternative therapies (e.g., beta-3 agonists like mirabegron) if anticholinergic side effects are intolerable or contraindicated.
Alternative Therapies
- Other antimuscarinics: Oxybutynin (Ditropan, Oxytrol), Solifenacin (Vesicare), Darifenacin (Enablex), Fesoterodine (Toviaz), Trospium (Sanctura)
- Beta-3 adrenergic agonists: Mirabegron (Myrbetriq), Vibegron (Gemtesa)
- OnabotulinumtoxinA (Botox) intravesical injection
- Percutaneous tibial nerve stimulation (PTNS)
- Sacral neuromodulation (SNS)
- Behavioral therapies (bladder training, pelvic floor muscle exercises)
Cost & Coverage
Average Cost:
$10 - $300+ per 30 capsules (generic to brand)
Generic Available:
Yes
Insurance Coverage:
Tier 1 (generic) or Tier 2/3 (brand), varies by plan
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 it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.