Tolterodine Uses, Dosage, Side Effects, Food Interaction and all others data.

Tolterodine is a competitive, specific muscarinic receptor antagonist which exhibits a selectivity for the urinary bladder over salivary glands, which have been demonstrated in non clinical pharmacological in vivo studies. Tolterodine has a high specificity for muscarinic receptors. A major active metabolite (5-hydroxymethyl derivative) of tolterodine exhibits a pharmacological profile which is similar to that of the parent compound. In extensive metabolisers this metabolite contributes significantly to the therapeutic effect of tolterodine. The effect of treatment can be expected within 4 weeks.

Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.

Trade Name Tolterodine
Availability Prescription only
Generic Tolterodine
Tolterodine Other Names Tolterodina, Tolterodine, Tolterodinum
Related Drugs oxybutynin, Myrbetriq, solifenacin, mirabegron, Ditropan, Detrol, VESIcare, trospium
Weight 2mg, 4mg, 1mg, 2mg
Type Oral capsule, extended release, oral tablet
Formula C22H31NO
Weight Average: 325.4876
Monoisotopic: 325.240564619
Protein binding

Approximately 96.3%.

Groups Approved, Investigational
Therapeutic Class BPH/ Urinary retention/ Urinary incontinence
Available Country United States
Last Updated: September 19, 2023 at 7:00 am


Tolterodine Tartrate is used for the treatment of overactive bladder with symptoms of urinary urgency, frequency, and/or urge incontinence.

Tolterodine is also used to associated treatment for these conditions: Urinary Bladder, Overactive

How Tolterodine works

Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.


Tolterodine dosage

The recommended dose for tolterodine is 2 mg twice daily. In case of troublesome side effects the dose may be reduced from 2 mg to 1 mg twice daily. 

The recommended total daily dose of tolterodine is 2 mg (1 mg b.i.d.) for patients with impaired renal function, impaired liver function, or receiving concomitant medication with potent CYP3A inhibitors, such as macrolide antibiotics (e.g. erythromycin and clarithromycin) or azole antifungal agents (e.g. ketoconazole, itraconazole and miconazole). After six months the need for further treatment should be considered.

Side Effects

Tolterodine may cause mild to moderate antimuscarinic effects, like dryness of mouth, dyspepsia and/or reduced lacrimation.


Tolterodine should be used with caution in the following patients:

  • at risk for urinary retention
  • at risk for decreased gastrointestinal motility
  • with impaired renal function
  • with impaired hepatic function

Organic reasons for urge and frequency should be considered before treatment.


Pharmacokinetic interactions are possible with other drugs metabolised by or inhibiting cytochrome P450 2D6 (CYP2D6) or CYP3A4. Concomitant treatment with fluoxetine does not result in a clinically significant interaction.

Ketoconazole, a potent inhibitor of CYP3A, significantly increased plasma concentrations of tolterodine when coadministered to poor metabolisers (i.e. persons devoid of CYP2D6 metabolic pathway).

Clinical studies have shown no interactions with warfarin or combined oral contraceptives (ethinyloestradiol or levonorgestrel).

Food Interaction

  • Take with food.

Tolterodine Alcohol interaction


Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.

In addition, the potential for abuse may be increased with the combination.

The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.

No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.

However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.

Alcohol should generally be avoided during therapy with anticholinergic agents.

Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.

Volume of Distribution

  • 113 ± 26.7 L

Half Life

1.9-3.7 hours

Elimination Route

Following administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days.

Pregnancy & Breastfeeding use

There are no studies in pregnant women. Therefore, tolterodine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Use of tolterodine during lactation should be avoided since no data on excretion of the drug into breast milk in humans is available.


Tolterodine is contraindicated in those patients with urinary retention, uncontrolled narrow angle glaucoma, known hypersensitivity to tolterodine or any other component of the drug.

Special Warning

Pediatric use: Safety and effectiveness of tolterodine in children have not been established.

Geriatric use: No overall differences in safety were observed between the older and younger patients treated with Tolterodine.

Acute Overdose

Overdosage with Tolterodine Tartrate capsules can potentially result in severe central anticholinergic effects and should be treated accordingly. ECG monitoring is recommended in the event of overdosage.

Storage Condition

Store in a cool and dry place. Protect from light. Keep out of the reach of children.

Innovators Monograph

You find simplified version here Tolterodine

Tolterodine contains Tolterodine see full prescribing information from innovator Tolterodine Monograph, Tolterodine MSDS, Tolterodine FDA label


What is Tolterodine used for?

Tolterodine is used treat overactive bladder a condition in which the bladder muscles contract uncontrollably and cause frequent urination, urgent need to urinate, and inability to control urination.

How safe is Tolterodine?

Tolterodine is safe and shows efficacy, particularly at a dosage of 2 mg bid, in the treatment of older patients with urinary symptoms attributable to overactive bladder.

What are the common side effects of Tolterodine?

The common side effects are include:

  • dry mouth
  • headache
  • feeling dizzy, sleepy, or a spinning sensation (vertigo)
  • diarrhoea or being sick (vomiting)
  • constipation
  • farting and burping (wind)
  • stomach pain
  • dry eyes
  • blurred vision
  • problems or pain when peeing, and not being able to empty your bladder

Is Tolterodine safe during pregnancy?

Tolterodine is not usually recommended in pregnancy because there's not enough information available to say it's safe for you and your baby.
If you're trying to get pregnant or you're already pregnant, talk to your doctor about whether taking tolterodine is right for you.

Is Tolterodine safe during breastfeeding?

Tolterodine is not usually recommended while breastfeeding. However, some breastfeeding mothers may still need it.
It is not known how much Tolterodine gets into breast milk, but this is likely to be small.

How long does Tolterodine take to work?

Tolterodine begins to work within 3 to 8 hours but it may take up to 4 weeks before it takes full effect. If the symptoms do not improve after 1 to 2 weeks, talk to your doctor.

How long will I take Tolterodine?

Usually, you'll need to take Tolterodine for a long time.
After 4 weeks your doctor will check that Tolterodine is helping your symptoms. They'll also do a review every 6 to 12 months after that to check it's still working for you.
Take Tolterodine until your doctor tells you to stop. Do not stop taking it just because you feel better.

Is Tolterodine safe to take for a long time?

Do not take Tolterodine for longer than you need to. Your doctor will check every 6 to 12 months that your treatment is still needed.

Is Tolterodine safe to take with painkillers?

It's safe to take Tolterodine with everyday painkillers like paracetamol and ibuprofen.

Can I drink alcohol with Tolterodine?

Avoid drinking alcohol when you first start taking Tolterodine, or if your dose is increased, to see how you feel.Tolterodine combined with alcohol can make you feel very sleepy.
Drinking alcohol may make you more likely to need to get up in the night to pee.

Is there any food or drink I need to avoid?

You can eat normally while taking Tolterodine. If you have urinary incontinence, cut down on alcohol and drinks containing caffeine, such as tea, coffee and cola.

Will I gain or lose weight?

You may gain weight when you take Tolterodine tablets. If you start to have problems with your weight while taking Tolterodine, talk to your pharmacist or doctor.

Will Tolterodine affect my contraception?

Tolterodine does not stop contraceptive pills working, including the combined pill or emergency contraception.

Will Tolterodine affect my fertility?

There's no clear evidence to suggest that taking tolterodine will reduce fertility in either men or women.
However, speak to a pharmacist or your doctor before taking it if you're trying to get pregnant.

Can I drive after taking Tolterodine?

Do not drive a car, ride a bike, use tools or operate machinery if tolterodine makes you sleepy, gives you blurred vision, or makes you feel dizzy.

Can I stop taking Tolterodine?

If you want to stop taking Tolterodine, talk to your doctor first.
If you've been taking it for at least 6 months, your doctor may suggest at your review that you can stop taking it for up to 4 weeks to see how your symptoms change without it.
Some people find that the improvement in their symptoms continues after they've stopped taking the medicine.

What happen if I take too much Tolterodine?

Taking 1 extra dose of Tolterodine is unlikely to harm you.
However, you may get more side effects, such as a dry mouth or headache.
The amount of tolterodine that can lead to an overdose varies from person to person, and too much Tolterodine can be dangerous.

What happen if I forget to take Tolterodine?

If you forget to take a dose, take it as soon as you remember, unless it's nearly time for your next dose. In this case, just skip the missed dose and take your next dose as normal.
Never take 2 doses at the same time. Never take an extra dose to make up for a forgotten one.

Who can and can't take Tolterodine?

Tolterodine can be taken by most adults. It can also be taken by children aged 2 years and over, on the advice of their specialist.

Does Tolterodine affect liver?

Tolterodine may causes liver problems also anyother symtom.
*** Taking medicines without doctor's advice can cause long-term problems.