Detrol 1mg 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 symptoms of an overactive bladder, such as needing to urinate frequently, having a sudden strong urge to urinate, or leaking urine. It works by relaxing the bladder muscles.
How to Use This Medicine
Taking Your Medication
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best 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 feeling well.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature, away from light and moisture. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion.
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 the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely. You can take this medication with or without food, and it's best 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 feeling well.
Storing and Disposing of Your Medication
To keep your medication effective and safe, store it at room temperature, away from light and moisture. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion.
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 the missed one.
Lifestyle & Tips
- Take the tablet whole with water, with or without food.
- Do not crush, chew, or split the tablet.
- Maintain adequate fluid intake to prevent constipation, but avoid excessive intake that could worsen bladder symptoms.
- Limit intake of bladder irritants like caffeine, alcohol, and spicy foods.
- Practice bladder training techniques as advised by your doctor (e.g., timed voiding, urge suppression strategies).
- Be aware that this medication may cause dry mouth; sugar-free candies or gum may help.
- Be cautious when driving or operating machinery until you know how this medication affects you, as it may cause dizziness or blurred vision.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
1 mg twice daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
normal_renal_hepatic:
1 mg twice daily
renal_impairment_moderate_severe:
Reduce to 1 mg once daily
hepatic_impairment_moderate_severe:
Reduce to 1 mg once daily
concomitant_strong_CYP3A4_inhibitors:
Reduce to 1 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
Reduce to 1 mg once daily (CrCl 10-30 mL/min)
Severe:
Reduce to 1 mg once daily (CrCl <10 mL/min)
Dialysis:
Use with caution; consider 1 mg once daily
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
Reduce to 1 mg once daily (Child-Pugh Class B)
Severe:
Reduce to 1 mg once daily (Child-Pugh Class C)
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It exhibits selectivity for the urinary bladder over salivary glands in vivo. This antagonism results in inhibition of bladder contraction, leading to a decrease in detrusor activity and an increase in bladder capacity, thereby reducing symptoms of overactive bladder such as urinary frequency, urgency, and urge incontinence.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive metabolizers), 65% (poor metabolizers)
Tmax:
1-2 hours (IR), 2-6 hours (ER)
FoodEffect:
Food increases bioavailability by approximately 20% but does not significantly alter Cmax or Tmax for IR tablets. Can be taken with or without food.
Distribution:
Vd:
113 L (tolterodine), 211 L (5-hydroxymethyl metabolite)
ProteinBinding:
96% (tolterodine), 70% (5-hydroxymethyl metabolite)
CnssPenetration:
Limited (due to P-glycoprotein efflux), but can cause CNS side effects at higher doses or in susceptible individuals.
Elimination:
HalfLife:
2-4 hours (tolterodine), 3-10 hours (5-HMT)
Clearance:
Not available
ExcretionRoute:
Urine (77%), Feces (17%)
Unchanged:
Less than 1% (tolterodine), 5-14% (5-HMT)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Within 4-8 weeks for maximal clinical benefit
DurationOfAction:
12 hours (with twice daily dosing)
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
If you experience any of these symptoms, get medical help right away.
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. Contact your doctor or seek medical help if you experience any of the following side effects or 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.
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
If you experience any of these symptoms, get medical help right away.
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. Contact your doctor or seek medical help if you experience any of the following side effects or 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:
- Difficulty urinating or inability to urinate (urinary retention)
- Severe constipation or abdominal pain
- Eye pain or vision changes (especially if you have glaucoma)
- Severe dizziness or fainting
- Rapid or irregular heartbeat
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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
Natural products and vitamins you are using
Any health problems you have
It is crucial to verify that it is safe to take this medication with your existing 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
Natural products and vitamins you are using
Any health problems you have
It is crucial to verify that it is safe to take this medication with your existing 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 (OTC) medications that may cause drowsiness or impair your reactions.
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 (OTC) medications that may cause drowsiness or impair your reactions.
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, blurred vision, hot and dry skin, fever, rapid heartbeat, urinary retention, constipation)
- CNS excitation (e.g., restlessness, confusion, hallucinations, seizures)
- Respiratory depression
What to Do:
Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is symptomatic and supportive. Gastric lavage may be performed. Physostigmine may be used to reverse severe central anticholinergic effects.
Drug Interactions
Contraindicated Interactions
- Not specifically contraindicated with other 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 (significant increase in tolterodine exposure).
- Other anticholinergic agents (e.g., oxybutynin, tricyclic antidepressants, phenothiazines, disopyramide) - additive anticholinergic effects.
Moderate Interactions
- Moderate CYP3A4 inhibitors (e.g., erythromycin, fluconazole).
- CYP2D6 inhibitors (e.g., quinidine, fluoxetine, paroxetine) - may increase exposure to tolterodine in extensive metabolizers.
- Drugs that prolong QT interval (e.g., quinidine, sotalol, procainamide, amiodarone, pimozide, thioridazine) - theoretical risk of additive QT prolongation.
Minor Interactions
- Metoclopramide (decreased prokinetic effect).
- Warfarin (minor effect on INR).
Monitoring
Baseline Monitoring
Renal function (CrCl)
Rationale: To determine appropriate dosing in patients with renal impairment.
Timing: Prior to initiation of therapy.
Hepatic function (LFTs)
Rationale: To determine appropriate dosing in patients with hepatic impairment.
Timing: Prior to initiation of therapy.
Post-void residual (PVR) volume
Rationale: To assess for urinary retention, especially in patients with bladder outlet obstruction.
Timing: Prior to initiation of therapy.
Routine Monitoring
Symptom improvement (frequency, urgency, incontinence episodes)
Frequency: Regularly, at follow-up visits (e.g., 4-8 weeks after initiation, then every 3-6 months)
Target: Patient-specific reduction in symptoms
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Side effects (dry mouth, constipation, blurred vision, urinary retention)
Frequency: Regularly, at follow-up visits
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
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity based on animal data.
Second Trimester:
Limited human data, animal data suggest potential risk.
Third Trimester:
Limited human data, animal data suggest potential risk.
Lactation
It is not known whether tolterodine or its metabolites are excreted in human milk. Due to the potential for serious adverse reactions in nursing 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 (Moderate risk - no human data, but 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, but greater sensitivity of some older individuals cannot be ruled out. Dose adjustment may be necessary in elderly patients with renal or hepatic impairment, or those taking strong CYP3A4 inhibitors.
Clinical Information
Clinical Pearls
- Tolterodine IR (Detrol) is typically dosed twice daily, while the extended-release formulation (Detrol LA) is once daily.
- Patients who are poor CYP2D6 metabolizers will have higher exposure to tolterodine and may require a lower dose, especially if also taking strong CYP3A4 inhibitors.
- Dry mouth is a common anticholinergic side effect; advise patients on strategies like sugar-free gum/candies, artificial saliva, or frequent sips of water.
- Monitor for signs of urinary retention, especially in men with benign prostatic hyperplasia (BPH).
- Clinical benefit may take several weeks to become apparent; encourage patients to continue therapy as prescribed.
Alternative Therapies
- Other antimuscarinics: Oxybutynin (Ditropan), Solifenacin (Vesicare), Darifenacin (Enablex), Fesoterodine (Toviaz)
- Beta-3 adrenergic agonists: Mirabegron (Myrbetriq), Vibegron (Gemtesa)
- OnabotulinumtoxinA (Botox) intravesical injection
- Neuromodulation (e.g., sacral neuromodulation, percutaneous tibial nerve stimulation)
- Behavioral therapies (e.g., bladder training, pelvic floor muscle exercises, fluid management)
Cost & Coverage
Average Cost:
Varies, typically $10-$50 per 30 tablets (generic 1mg IR)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic tolterodine)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. 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 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 details about the overdose, including the medication taken, the amount, and the time it occurred.