Tolterodine Tartrate 1mg Tablets
It is used to treat an overactive bladder.
Drug Class
Urinary Antispasmodic
Pharmacologic Class
Antimuscarinic; Muscarinic Receptor Antagonist
Pregnancy 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, feeling a sudden strong urge to urinate, and having accidents (leakage). It works 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 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 the 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 the 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
- Avoid overheating and dehydration, especially in hot weather or during exercise, as this medication can decrease sweating.
- Limit alcohol intake, as it can worsen dizziness or drowsiness.
- Maintain adequate fluid intake to prevent constipation and dry mouth.
- Practice bladder training techniques (e.g., scheduled voiding, urge suppression) as advised by your healthcare provider.
- Avoid driving or operating machinery until you know how this medication affects you, due to potential for dizziness or blurred vision.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
1 mg twice daily (immediate release), may be increased to 2 mg twice daily based on response and tolerability.
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
overactive_bladder:
Initial: 1 mg twice daily. Maintenance: 1 mg to 2 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
Moderate:
Maximum 1 mg twice daily
Severe:
Maximum 1 mg twice daily
Dialysis:
Maximum 1 mg twice daily (data limited, use with caution)
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
Maximum 1 mg twice daily
Severe:
Maximum 1 mg twice daily
Pharmacology
Mechanism of Action
Tolterodine is a competitive muscarinic receptor antagonist. It acts on muscarinic receptors in the bladder, inhibiting cholinergic stimulation, which reduces detrusor muscle activity and decreases symptoms of overactive bladder such as urinary frequency, urgency, and urge incontinence.
Pharmacokinetics
Absorption:
Bioavailability:
17% (extensive first-pass metabolism by CYP2D6 in extensive metabolizers); up to 60% in poor metabolizers.
Tmax:
1-2 hours (immediate release)
FoodEffect:
Food increases bioavailability by approximately 20% but does not significantly alter Cmax or Tmax.
Distribution:
Vd:
Approximately 113 L
ProteinBinding:
Approximately 96% (primarily to alpha-1 acid glycoprotein)
CnssPenetration:
Limited
Elimination:
HalfLife:
Tolterodine: 2-4 hours; 5-HMT: 3-10 hours
Clearance:
Not available
ExcretionRoute:
Renal (approximately 77% as metabolites), Fecal (approximately 17%)
Unchanged:
Less than 1% (tolterodine); approximately 5% (5-HMT)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Full therapeutic effect may take 4-6 weeks
DurationOfAction:
Approximately 12 hours (for immediate release formulation)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
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 help right away:
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. 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 help right away:
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. 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 abdominal pain
- Inability to urinate (urinary retention)
- Severe blurred vision or eye pain
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
- Confusion or hallucinations
- 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 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.
Remember, do not 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
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.
Remember, do not 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 medications that may cause drowsiness or 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 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 cause drowsiness or 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, dilated pupils, blurred vision, hot and dry skin, fever, rapid heart rate, urinary retention, constipation)
- Central nervous system effects (e.g., confusion, disorientation, hallucinations, seizures, severe drowsiness, stupor, coma)
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 considered in severe cases with central anticholinergic symptoms.
Drug Interactions
Contraindicated Interactions
- Not applicable (no absolute contraindications based on drug-drug interactions)
Major Interactions
- Strong CYP2D6 inhibitors (e.g., quinidine, fluoxetine, paroxetine, bupropion) in poor metabolizers of CYP2D6 (may significantly increase tolterodine exposure)
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, erythromycin, ritonavir) in patients who are extensive metabolizers of CYP2D6 (may significantly increase tolterodine exposure)
Moderate Interactions
- Other anticholinergic agents (additive anticholinergic effects, increased risk of dry mouth, constipation, urinary retention, blurred vision)
- Prokinetic agents (e.g., metoclopramide, cisapride - may antagonize effects of prokinetics)
- Drugs that prolong QT interval (theoretical risk, use with caution)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Assessment of OAB symptoms (frequency, urgency, incontinence episodes)
Rationale: To establish baseline severity and guide treatment.
Timing: Prior to initiation of therapy
Post-void residual (PVR) volume
Rationale: To assess for risk of urinary retention, especially in patients with bladder outlet obstruction.
Timing: Prior to initiation of therapy
Renal and hepatic function tests
Rationale: To determine need for dose adjustment in impaired patients.
Timing: Prior to initiation of therapy
Routine Monitoring
Efficacy of OAB symptom control
Frequency: Periodically (e.g., 4-8 weeks after initiation, then every 3-6 months)
Target: Reduction in urgency, frequency, and incontinence episodes
Action Threshold: Lack of improvement or worsening symptoms may require dose adjustment or alternative therapy.
Anticholinergic side effects (dry mouth, constipation, blurred vision, urinary retention)
Frequency: Regularly, especially during dose titration and initial weeks of therapy
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 (>200-250 mL) may indicate urinary retention and require intervention or 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 abnormalities based on animal data; human data lacking.
Second Trimester:
Human data lacking; theoretical risk of anticholinergic effects on fetal development.
Third Trimester:
Human data lacking; theoretical risk of anticholinergic effects on fetal development or labor.
Lactation
It is not known whether tolterodine or its active metabolite are excreted in human milk. Tolterodine is excreted in the milk of mice. 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:
Risk unknown; theoretical risk of anticholinergic effects in the infant (e.g., drowsiness, constipation, dry mouth).
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. However, elderly patients may be more susceptible to anticholinergic side effects (e.g., dry mouth, constipation, cognitive impairment, urinary retention). Use with caution and monitor closely.
Clinical Information
Clinical Pearls
- Tolterodine is available in both immediate-release (IR) and extended-release (ER) formulations. The 1mg tablet is an IR formulation.
- The active metabolite, 5-hydroxymethyl metabolite (5-HMT), contributes significantly to the pharmacological effect.
- Patients who are poor metabolizers of CYP2D6 will have higher exposure to tolterodine and lower exposure to 5-HMT, but the overall effect is similar due to the activity of the parent drug.
- Counsel patients on managing common anticholinergic side effects like dry mouth (sugar-free candy/gum, sips of water) and constipation (fiber, fluids).
- Always assess for bladder outlet obstruction or significant urinary retention before initiating therapy, as anticholinergics can worsen these conditions.
Alternative Therapies
- Other antimuscarinics: Oxybutynin (Ditropan), Solifenacin (Vesicare), Darifenacin (Enablex), Fesoterodine (Toviaz), Trospium (Sanctura)
- Beta-3 adrenergic agonists: Mirabegron (Myrbetriq), Vibegron (Gemtesa)
- OnabotulinumtoxinA (Botox) intravesical injection
- Sacral neuromodulation
- Percutaneous tibial nerve stimulation (PTNS)
- Behavioral therapies (e.g., bladder training, pelvic floor muscle exercises)
Cost & Coverage
Average Cost:
$10 - $50 per 30 tablets (generic)
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 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 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.