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Tolterodine

  • Prescription medicine
  • Prescription only
  • Identity checked
  • Sources last checked 2026-09-04

This page shows what was measured, who it was measured in, and what that does not settle.

What Tolterodine does in the body

Tolterodine blocks the receptors that acetylcholine uses to tell the bladder wall to contract, so the involuntary squeeze while the bladder is filling is weakened.

The twist is that in most people the drug you swallow is not the drug that does the work: an enzyme in the liver converts it into a compound called 5-hydroxymethyl tolterodine, which blocks the same receptors and is present in larger quantity. About seven people in a hundred of European ancestry lack a working version of that enzyme, and they end up with almost none of the metabolite and much more of the parent drug. Both block the same receptor, so the drug still works — but what is circulating in one person is not what is circulating in another.

Why people take it. An overactive bladder — sudden urgency, going too often, and leaking before you reach the toilet

What happened in people

Incontinence episodes fell 11.8 per week on tolterodine ER against 6.9 on placebo, and micturitions 1.8 per day against 1.2, on the US label

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The recorded finding that sits closest to something a person would notice. Written into the record, not signed off, and it carries no population or interval.

The limit that matters most

That an active-control arm missing against placebo reflects a failed trial — assay sensitivity was demonstrated in the same trial by the experimental arm

Where it acts
Detrusor smooth muscle of the bladder wall, and the salivary glands where the same receptor sits
Kind of result
The kind of result is not recorded
Supervision
RNAWiki has not recorded a supervision or regulatory status for this substance.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · 5T619TQR3R · read 2026-08-29

Where each sentence above came from

A person wrote this explanation into the record, with the studies named in the path below.

The recorded use, written for a reader without medical training. Not signed off.

A limit recorded against this substance. Not signed off as a reviewed claim.

The four opening statements run to 168 words.

Words this page uses

Four words worth knowing first

Chosen from what this page shows, with each one explained before the word it depends on.

Comparator

A comparator is whatever the treatment was measured against.

A picture of it, and where the picture fails

It is like the other runner in a race.

Where that stops being true. A race has one winner. A study can show both arms improved.

What people get wrong. Results are read without asking what the other group got. Beating nothing is not beating a treatment.

The control condition against which the experimental intervention is assessed.

Randomisation

Randomisation means chance decides who gets which treatment.

A picture of it, and where the picture fails

It is like a coin toss deciding the groups.

Where that stops being true. A coin toss is fair once. Fairness here comes from doing it for everyone.

What people get wrong. It is thought to make groups identical. It makes them similar on average, including on things nobody measured.

Allocation of participants to arms by a chance process, so that unmeasured factors are balanced in expectation.

Absolute difference

An absolute difference is how many more people in a hundred were affected.

A picture of it, and where the picture fails

It is like counting heads in two rooms of a hundred.

Where that stops being true. Heads are easy to count. Study results carry a margin of error too.

What people get wrong. It is confused with a percentage change, which can look far larger.

The arithmetic difference in event rates between arms.

Confidence interval

A confidence interval is the range the true answer is likely to sit in.

A picture of it, and where the picture fails

It is like a weather forecast giving a range rather than one number.

Where that stops being true. A forecast range covers tomorrow. This one covers what the study could resolve.

What people get wrong. The middle number is read as the answer. A range crossing zero means no change is still possible.

An interval estimate that would contain the true parameter in a stated proportion of repeated studies.

What happened in peopleRead from sources, not yet reviewed

What happened in people

Each card is one study: the exact question it asked, who was in it, and whether it showed what it set out to show.

Change from baseline to week 12 in mean incontinence episodes and mean micturitions per 24 hours

The study did not show it

Who was studied
SCORPIO (NCT00689104) — tolterodine SR 4 mg as active control
How many people
2336
Study design
Phase 3 randomised double-blind placebo- and active-controlled, 12 weeks
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Tolterodine SR 4 mg: incontinence -1.27 versus placebo -1.17, p=0.11 (95% CI -0.42 to 0.21); micturitions -1.59 versus -1.34, p=0.11 (95% CI -0.55 to 0.06)
Repeated elsewhere
Failed to Replicate

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. Assay sensitivity was demonstrated in the same trial by the mirabegron arms clearing both endpoints at p=0.003 and p<0.001, which removes the usual excuse for an active control missing.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral extended-release capsule once daily, and immediate-release tablet twice daily

Interval reported. 95% CI -0

Written into the record, not signed off as a reviewed claim.

Change from baseline at week 12 in average micturitions per 24 hours, and in urge urinary incontinence episodes in the wet subgroup

The study did not show it

Who was studied
EMPOWUR (NCT03492281) — tolterodine ER 4 mg as active control
How many people
1530
Study design
Phase 3 randomised double-blind placebo- and active-controlled, 12 weeks
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Tolterodine versus placebo: micturitions difference -0.3, p=0.0988 (descriptive); urge incontinence difference -0.4, p=0.0123 (descriptive). Vibegron reached p<0.001 and p<0.0001 in the same trial.
Repeated elsewhere
Failed to Replicate

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. A different sponsor, a different experimental drug and seven years later, with the same outcome for the tolterodine arm on the first co-primary endpoint.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral extended-release capsule once daily, and immediate-release tablet twice daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Change from baseline in mean urgency urinary incontinence episodes per 24 hours at week 12

The study showed what it set out to show

Who was studied
Fesoterodine versus tolterodine ER, A0221046 (NCT00611026)
How many people
2417
Study design
Phase 3 randomised double-blind double-dummy placebo-controlled, 12 weeks
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Placebo -1.62 ± 0.07 (n=448), tolterodine ER -1.74 ± 0.06 (n=926, p=0.0228 versus placebo), fesoterodine -1.95 ± 0.05 (n=908, p<0.0001 versus placebo and p=0.0072 versus tolterodine)
Repeated elsewhere
Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. The comparison was fesoterodine escalated to 8 mg against tolterodine ER 4 mg, not a matched-exposure comparison of the same active moiety by two routes.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral extended-release capsule once daily, and immediate-release tablet twice daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Change from baseline in mean urgency urinary incontinence episodes per 24 hours at week 12

The study showed what it set out to show

Who was studied
Fesoterodine versus tolterodine ER (NCT00444925)
How many people
1712
Study design
Phase 3 randomised double-blind double-dummy placebo-controlled, 12 weeks
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Placebo -1.46 (n=307), tolterodine ER -1.61 (n=626, p=0.0107 versus placebo), fesoterodine -1.72 (n=619, p<0.0001 versus placebo and p=0.0172 versus tolterodine)
Repeated elsewhere
Replicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. The tolterodine margin over placebo here is 0.15 incontinence episodes per 24 hours. It is statistically significant and it is fifteen hundredths of an episode.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral extended-release capsule once daily, and immediate-release tablet twice daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

Number and severity of treatment-emergent adverse events over 12 months, mirabegron versus tolterodine ER 4 mg

The study showed what it set out to show

Who was studied
TAURUS (NCT00688688) — tolterodine ER 4 mg as active control
How many people
2792
Study design
Phase 3 randomised double-blind active-controlled long-term safety, 12 months
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
A safety endpoint with no efficacy hypothesis test and no placebo arm; the trial establishes 12-month tolerability, not 12-month effect
Repeated elsewhere
Unreplicated

What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.

The limits of this study, and where it came from

Main limit. This is the longest randomised exposure to tolterodine in the public record, and it carries no placebo arm.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral extended-release capsule once daily, and immediate-release tablet twice daily

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

What we know
RNAWiki holds 5 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.

What it changes in the bodyRead from sources, not yet reviewed

The path through the body

From what a person takes to what changes. A solid line is a step measured in people. A dashed line is a step nobody has measured that way.

  1. Start

    Tolterodine

    What a person takes: Oral extended-release capsule once daily, and immediate-release tablet twice daily.

    The measurement behind this step

    The extended-release capsule exists for the same reason oxybutynin's does: to smooth the concentration peak that drives the anticholinergic side effects, without changing the molecule. Dose is reduced in significant hepatic or renal impairment and in the presence of strong CYP3A4 inhibitors, and the extended-release form is not recommended in severe renal impairment.

  2. Getting in

    Swallowed, then converted into the compound that does most of the work

    The capsule releases the drug slowly. On the way through the liver, an enzyme turns most of it into a second compound that blocks the same receptors. In most people, that second compound is what reaches the bladder in quantity.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Extended-release capsule, once daily. CYP2D6 hydroxylates the 5-methyl group to 5-hydroxymethyl tolterodine, an equally active antimuscarinic. In poor metabolisers, roughly 7% of Caucasians, that pathway is unavailable and CYP3A4 dealkylation dominates instead, giving significantly higher parent concentrations and negligible metabolite.

  3. Reaching the cell

    Both compounds reach the receptor from outside the cell

    The target sits on the outer surface of the bladder muscle cell. Neither the drug nor its metabolite needs to get inside anything — they arrive from the bloodstream and sit down.

    Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.

    The measurement behind this step

    Muscarinic receptors are plasma-membrane G-protein-coupled receptors with an outward-facing orthosteric pocket, so no transporter step exists. Tolterodine is a tertiary amine and lipophilic, and the hydroxymethyl metabolite is more polar than the parent — a difference that matters for tissue distribution but not for reaching a surface receptor.

  4. What it acts on

    It competes with acetylcholine at every muscarinic receptor

    The nerve chemical that tells the bladder to squeeze finds its seat taken. The same thing happens in the salivary gland, which is where the dry mouth comes from.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    The label describes competitive antagonism at postganglionic muscarinic receptors, with no subtype selectivity claimed. Competition is surmountable, so a large enough acetylcholine release still produces a contraction. The free phenol on the aromatic ring is the hydrogen-bond donor the binding pocket uses, and the methyl group next to it is the site CYP2D6 attacks.

  5. The change it makes

    Calcium release falls and the bladder holds more

    The internal calcium burst that drives a contraction is weakened, so the bladder tolerates more filling before it demands emptying. Each void is larger as a result.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Reduced M3-Gq/11 coupling lowers phospholipase C activity, inositol trisphosphate and sarcoplasmic reticulum calcium release, and myosin light-chain phosphorylation falls. The label captures the functional consequence directly: volume passed per void rose 34 mL against 14 mL on placebo.

  6. What that does for a person

    Five fewer leaks a week than placebo, or none at all depending on the trial

    On its own label, about five fewer leaks a week than placebo. In two large trials run by other companies, no measurable difference from placebo at all.

    Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.

    The measurement behind this step

    Label figures: incontinence episodes -11.8 per week against -6.9 on placebo, micturitions -1.8 per day against -1.2, volume per void +34 mL against +14 mL. Against that, the tolterodine arm missed both co-primary endpoints in SCORPIO (p=0.11) and missed on micturitions in EMPOWUR (p=0.0988). Dry mouth 23% against 8%. A measured QT effect of 11.84 msec at twice the therapeutic dose.

No suggested links are held for this record, so nothing is hidden from this path.

What we know
The record describes 5 steps from taking it to an effect in a person.
How we know it
Each step names the study behind it in the technical detail beside it.
What this does not prove
A change inside the body is a reason to look. It is not a result in a person.
Why it matters
A reader can see exactly where the chain stops being measured in people.
What we still do not know
No reviewed claim binds any of these steps to a named population.

What is missing or unclearRead from sources, not yet reviewed

Were people like you studied?

RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.

Who was studied

People similar to this profile were included.

  • Adults with overactive bladder, and — in a much larger number — trial participants randomised to it as the yardstick against which a newer drug is being measured.

Who is missing from the studies

  • Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What the label states about particular groups

  • On pediatric, the label states: “The effectiveness of tolterodine tartrate extended-release capsules has not been established in pediatric patients.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • On older people, the label states: “No overall differences in safety were observed between the older and younger patients treated with tolterodine.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary There are no available data with tolterodine tartrate extended-release capsules use in pregnant women to inform drug-associated risks.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • On people who are breastfeeding, the label states: “Risk Summary There is no information on the presence of tolterodine or its 5-HMT metabolite in human milk, the effects on the breastfed infant, or the effects on milk production.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • On people with reduced liver function, the label states: “Liver impairment can significantly alter the disposition of tolterodine immediate release.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • On people with reduced kidney function, the label states: “can significantly alter the disposition of tolterodine immediate release and its metabolites.”

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

Where the result stopped carrying

  • The active-control arm in SCORPIO, which missed both co-primary endpoints against placebo in 475 patients
  • The active-control arm in EMPOWUR seven years later, under a different sponsor, on the first co-primary endpoint
  • The head-to-head against solifenacin in STAR, which tolterodine ER lost on most efficacy variables
  • The head-to-head against its own active metabolite, which tolterodine lost twice
  • This is a scope explorer, not a diagnosis engine.
  • It shows who was studied so you can see whether people similar to you were included.

RNAWiki cannot tell whether a study fits you. It can show who was in it.

What it would be like to takeRead from sources, not yet reviewed

Why it might seem to do nothing

A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.

It was studied in different people

The people in the studies were not much like the reader.

On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

The evidence may simply be wrong

Small early studies often do not hold up.

On this record: RNAWiki has not yet published a reviewed conclusion for this use.

Other reasons RNAWiki checked and found nothing for (11)
It was studied for a different goal
The studies measured something else entirely. Nothing in this record points to this reason.
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.

None of these is a reason to take more. Taking more is not a step this page ever suggests.

What it would be like to takeRead from sources, not yet reviewed

What taking it involves

The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.

How it is supplied

Prescription only

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Read from the recorded approval status.

No source is stored against this line.

Form and route

Oral extended-release capsule once daily, and immediate-release tablet twice daily

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form and route recorded on this substance.

No source is stored against this line.

Who oversees it

RNAWiki has not recorded a supervision or regulatory status for this substance.

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

No register row and no identity class settled the question.

No source is stored against this line.

What is in the pack

The extended-release capsule exists for the same reason oxybutynin's does: to smooth the concentration peak that drives the anticholinergic side effects, without changing the molecule. Dose is reduced in significant hepatic or renal impairment and in the presence of strong CYP3A4 inhibitors, and the extended-release form is not recommended in severe renal impairment.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on how this is sold and what that means for what is in the pack.

No source is stored against this line.

Where it is registered

Regulatory records are listed in the technical disclosure at the foot of this page.

Counted from records

Where this came from

A count of rows RNAWiki holds. It describes our records, not your body.

Register entries are stored per jurisdiction and shown with their dates.

No source is stored against this line.

Why people stop

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No record of why people stopped taking it is stored for this substance.

No source is stored against this line.

What it would be like to takeRead from sources, not yet reviewed

What can go wrong

Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.

Worth asking a clinician aboutWritten into the record from the studies named on this page

Dry mouth is the dominant effect at 23% against 8% on placebo, with constipation and headache barely separating. The label carries warnings for angioedema, urinary retention, gastric retention, narrow-angle glaucoma and central nervous system effects including somnolence, and reports a measured QT prolongation of 11.84 msec at twice the therapeutic dose with confidence intervals overlapping the positive control. The pharmacokinetic profile depends on CYP2D6 status, and in poor metabolisers CYP3A4 becomes the only remaining clearance route.

Nobody counted how many people took this and were fine, so this cannot be turned into a rate.

Where this came from

Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.

Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What is missing or unclearRead from sources, not yet reviewed

Does the exact form matter?

Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.

The form that was studied

Oral extended-release capsule once daily, and immediate-release tablet twice daily

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form used in the studies cited on this page.

No source is stored against this line.

What is sold

Dose is reduced in significant hepatic or renal impairment and in the presence of strong CYP3A4 inhibitors, and the extended-release form is not recommended in severe renal impairment.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on which forms are sold and how they compare.

No source is stored against this line.

What is recorded as being sold

  • 53 products list this as an active ingredient in the United States drug directory. 53 of them contain it and nothing else.

    FDA National Drug Code directory · 0093-7164 · read 2026-08-29

  • They are sold as capsule, capsule, extended release, powder, tablet and tablet, film coated, taken oral.

    FDA National Drug Code directory · 0093-7164 · read 2026-08-29

  • The regulator's established pharmacologic class for it is cholinergic muscarinic antagonist [epc] and cholinergic muscarinic antagonists [moa].

    FDA National Drug Code directory · 0093-7164 · read 2026-08-29

  • 19 published labels name it as an active ingredient. 19 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · d27e25b5-5d02-419f-b098-41fb162c5872 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · d27e25b5-5d02-419f-b098-41fb162c5872 · read 2026-08-29

  • Tolterodine Tartrate is oral at 3 DOSAGE FORMS AND STRENGTHS The 2 mg capsules are light green with “7163” imprinted on the body and “TEVA” imprinted on the cap., recorded as fda label in effect 2026-01-09 in the United States.

    US prescribing information · fd6c8b3d-a52a-4418-aa9c-0297db6c0807 · read 2026-08-30

  • Recorded price in US: 0.21281–0.24829 USD per one unit as the pricing file counts it — a tablet, capsule, patch or single item, across 16 priced products whose strengths and pack forms differ, as of 2026-08-26, paid by retail pharmacies buying the product, as surveyed by the Centers for Medicare & Medicaid Services. It is not a list price, an insurance price, or what anyone pays at a counter..

    Recorded source · 2026-08-26 · read 2026-08-28

Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.

What it would be like to takeRead from sources, not yet reviewed

What you could measure

This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.

RNAWiki could not confidently classify this substance, so no self-experiment plan is offered.

Questions worth asking

  • Which of the trials of Tolterodine studied people like me?
  • What was measured, and for how long?
  • Was the result a laboratory value or a health outcome?
  • What would we watch for, and when would we stop?

Tracking can show whether something changed for you. It cannot show what caused it.

RNAWiki records evidence. It does not say whether this substance is right for you.

What is missing or unclearRead from sources, not yet reviewed

Claims that go past the evidence

Things said about this substance that sound reasonable, and the exact step that is missing between the evidence and the claim.

Goes past the evidence

That an active-control arm missing against placebo reflects a failed trial — assay sensitivity was demonstrated in the same trial by the experimental arm

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That fesoterodine is a different mechanism from tolterodine — both labels name 5-hydroxymethyl tolterodine as the active moiety

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That the label's efficacy figures apply equally to poor and extensive CYP2D6 metabolisers — no trial stratified on genotype

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

Goes past the evidence

That tolterodine specifically raises dementia risk — the observational evidence is class-level and does not identify this molecule

Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.

The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.

What would change this

A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.

RNAWiki has not yet published a reviewed conclusion for this use.

What is missing or unclearRead from sources, not yet reviewed

What nobody knows yet

Open questions, each with why it is open and what would close it.

Missing populations

Which groups were under-represented in the studies has not been recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing long-term data

No completed tested study window is recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

No reviewed conclusion

RNAWiki has not yet published a reviewed conclusion for this use.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing interaction studies

No interaction was found in the registers checked. Not finding one is not the same as showing there is none.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Formulation uncertainty

Several salts, forms or products of Tolterodine are recorded. Results from one form may not transfer to another.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Mechanism not reviewed

No reviewed mechanism story exists for this substance.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

What happened in peopleRead from sources, not yet reviewed

Check any of this yourself

Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.

Every line above can be traced to the study named beside it. Follow the link and read it.

In SCORPIO, 475 patients on this drug could not be told apart from placebo
In plain words
Mirabegron's registration trial included a tolterodine arm as the yardstick. On both main endpoints the yardstick missed. Mirabegron cleared placebo comfortably in the same trial, on the same days, in the same patients.
What was measured
Tolterodine SR 4 mg versus placebo on both co-primary endpoints, in a 2,336-patient trial
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
SCORPIO (NCT00689104) randomised 2,336 patients to placebo (480), mirabegron 50 mg (473), mirabegron 100 mg (478) or tolterodine SR 4 mg (475). Incontinence episodes per 24 hours fell 1.17 on placebo and 1.27 on tolterodine, p=0.11 (95% CI -0.42 to 0.21). Micturitions fell 1.34 and 1.59, p=0.11 (95% CI -0.55 to 0.06). Mirabegron 50 mg in the same trial reached p=0.003 and p<0.001. An active-control arm that misses is usually written off as a failure of assay sensitivity — but assay sensitivity was demonstrated in the same trial by the experimental drug clearing both endpoints. The remaining explanation is that the tolterodine effect is small enough that a 475-patient arm can miss it.
Source
ClinicalTrials.gov results record, SCORPIO NCT00689104; Khullar V et al., Eur Urol 2013;63:283-295
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
It happened again in EMPOWUR, seven years later, with a different sponsor
In plain words
Vibegron's registration trial also used tolterodine as the comparator. Tolterodine again failed to beat placebo on the number of daily toilet trips.
What was measured
Tolterodine ER 4 mg versus placebo on micturitions and urge incontinence episodes per 24 hours
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
EMPOWUR (NCT03492281) randomised 1,530 patients to placebo (475), vibegron 75 mg (492) or tolterodine ER 4 mg (378). On the first co-primary endpoint, micturitions per 24 hours, vibegron beat placebo by 0.5 (p<0.001) while tolterodine reached only a 0.3 difference at p=0.0988, reported as descriptive. On urge urinary incontinence episodes in the wet subgroup, vibegron beat placebo by 0.6 (p<0.0001) and tolterodine by 0.4 (p=0.0123, descriptive). Two independent sponsors, seven years apart, using different beta-3 agonists, produced the same result for the tolterodine arm. Two replications of a null is not a coincidence about trial conduct.
Source
ClinicalTrials.gov results record, EMPOWUR NCT03492281
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
Where it did beat placebo, the margin was about a tenth of an episode a day
In plain words
Two large trials run by tolterodine's own manufacturer did show it beating placebo. The size of the win was 0.12 and 0.15 fewer leaks a day.
What was measured
Change from baseline in urgency incontinence episodes per 24 hours, tolterodine ER versus placebo, in two trials
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Pfizer ran two 12-week double-blind, double-dummy, placebo-controlled trials of fesoterodine against tolterodine ER 4 mg. In the larger (NCT00611026, n=2,417), urgency incontinence episodes per 24 hours fell 1.62 ± 0.07 on placebo (n=448) and 1.74 ± 0.06 on tolterodine (n=926), p=0.0228 — a difference of 0.12 episodes a day. In the second (NCT00444925, n=1,712), placebo fell 1.46 (n=307) and tolterodine 1.61 (n=626), p=0.0107 — a difference of 0.15. The label reports the same order of magnitude in different units: 11.8 against 6.9 weekly incontinence episodes, 1.8 against 1.2 daily micturitions, and 34 mL against 14 mL added to the volume passed each time. These are positive results with defensible p-values and effect sizes measured in tenths of an episode.
Source
ClinicalTrials.gov results records NCT00611026 and NCT00444925; US prescribing information for tolterodine tartrate extended-release capsules, Clinical Studies section
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
The manufacturer developed this drug's own metabolite and beat it with it
In plain words
Fesoterodine, sold as a separate newer drug, is a delivery vehicle for the exact compound tolterodine turns into inside the body. Pfizer tested it against tolterodine twice and won both times.
What was measured
Fesoterodine 8 mg versus tolterodine ER 4 mg on urgency incontinence episodes per 24 hours, in two trials totalling 4,129 patients
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The fesoterodine label states that after oral administration fesoterodine is rapidly and extensively hydrolysed by nonspecific esterases to 5-hydroxymethyl tolterodine, "which is responsible for the antimuscarinic activity of fesoterodine," and names the compound explicitly. The tolterodine label states that tolterodine is metabolised by CYP2D6 to the same 5-hydroxymethyl metabolite. So the two products deliver the same active moiety by different routes — one requiring a polymorphic liver enzyme, one requiring only ubiquitous esterases. In the head-to-heads, fesoterodine escalated to 8 mg beat tolterodine ER 4 mg on urgency incontinence episodes: -1.95 against -1.74 (p=0.0072) and -1.72 against -1.61 (p=0.0172). A fair reading is that the newer drug is a real pharmacokinetic improvement over the older one whose clinical size is about a tenth of an episode a day, and that the dose comparison was 8 mg against 4 mg rather than a like-for-like exposure.
Source
US prescribing information for fesoterodine fumarate extended-release tablets, Mechanism of Action and Clinical Pharmacology; US prescribing information for tolterodine tartrate extended-release capsules, Clinical Pharmacology; ClinicalTrials.gov results records NCT00611026 and NCT00444925
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
About seven Caucasians in a hundred get a different drug from the same capsule
In plain words
The enzyme that converts tolterodine into its active form is missing or non-functional in roughly 7% of people of European ancestry. Those people end up with almost none of the metabolite and much more of the parent drug.
What was measured
Proportion of poor metabolisers and their relative parent-drug and metabolite concentrations
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The US label states that poor metabolisers, approximately 7% of Caucasians, cannot efficiently form 5-hydroxymethyl tolterodine via CYP2D6, and that dealkylation via CYP3A4 becomes the primary route instead, "resulting in significantly higher serum concentrations of tolterodine and negligible concentrations of 5-HMT". Both compounds are antimuscarinic, so the therapeutic effect does not vanish; what changes is the identity, exposure and clearance route of the circulating active species. It also removes the redundancy: in a poor metaboliser, CYP3A4 is the only clearance pathway left, which is why the label handles strong CYP3A4 inhibitors differently in that group. Trials of this drug did not stratify on CYP2D6 status, so every efficacy figure quoted for tolterodine is an average over two pharmacologically distinct populations.
Source
US prescribing information for tolterodine tartrate extended-release capsules, Clinical Pharmacology section (openFDA drug label endpoint)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
A measured 11.84 msec QT effect at twice the therapeutic dose
In plain words
At double the normal daily dose, tolterodine lengthened an electrical interval in the heart by about 12 milliseconds. The label compares it with a known QT-prolonging antibiotic and notes the confidence intervals overlapped.
What was measured
Mean QT interval change at twice the therapeutic dose, with 95% confidence interval, against a moxifloxacin positive control
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The US label reports a dedicated QT study. At tolterodine 4 mg twice daily — twice the therapeutic 4 mg once-daily extended-release exposure — the mean QT interval change by manual measurement was 11.84 msec (7.11, 16.58). The label states the effect at 8 mg/day "was not as large as that observed after four days of therapeutic dosing with moxifloxacin. However, the confidence intervals overlapped." That last sentence is doing real work: overlapping confidence intervals with the positive control is not the same as a clean negative, and the label chose to say so rather than to summarise. The mechanism is hERG channel block, which is unrelated to the muscarinic receptor the drug was designed for.
Source
US prescribing information for tolterodine tartrate extended-release capsules, Clinical Pharmacology section (openFDA drug label endpoint)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
caution
Review state
Written into the record, not signed off as a reviewed claim
Dry mouth in 23% against 8% on placebo, and it is the same receptor
In plain words
Nearly one in four patients gets a dry mouth, against one in twelve on placebo. As with every drug in this class, that is the identical receptor block happening in the salivary gland.
What was measured
Incidence of dry mouth, constipation and headache against placebo
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The US label for the extended-release capsule reports dry mouth in 23% against 8% on placebo, constipation 6% against 4%, and headache 6% against 5%. Only the dry mouth separates convincingly. In patients aged 65 and over, dry mouth occurred with roughly six times the incidence on tolterodine ER 4 mg as on mirabegron over 12 weeks, and three times the incidence over a year. The extended-release capsule was itself developed to reduce this: it is the same molecule as the immediate-release tablet, released more slowly, on the same logic that produced oxybutynin's extended-release form.
Source
US prescribing information for tolterodine tartrate extended-release capsules, Adverse Reactions section; Wagg A et al., Curr Med Res Opin 2016;32:621-638 (PMID 26828974)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
verified
Review state
Written into the record, not signed off as a reviewed claim
The class dementia association applies here and has never been tested in a trial
In plain words
Large database studies associate bladder antimuscarinics as a group with later dementia. Tolterodine is one of them. No randomised trial in this indication has ever measured cognition as an endpoint.
What was measured
That tolterodine specifically raises dementia risk — the evidence is class-level and observational, and this drug is not separately identified in it
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Coupland and colleagues, in 58,769 dementia cases and 225,574 controls, reported an adjusted odds ratio of 1.65 (95% CI 1.56 to 1.75) for bladder antimuscarinic drugs as a class, and a rise from 1.06 (1.03 to 1.09) to 1.49 (1.44 to 1.54) across cumulative anticholinergic exposure bands. Gray and colleagues, following 3,434 people aged 65 and over for a mean 7.3 years, reported an adjusted hazard ratio of 1.54 (1.21 to 1.96) above 1,095 total standardised daily doses. Neither study can attribute risk to tolterodine specifically, and neither randomised anyone. What makes the inference harder rather than easier here is that most patients discontinue within months: the cumulative-exposure bands that carry the signal are populated by the minority who stayed on treatment, who differ from everyone else in ways no adjustment fully captures.
Source
Coupland CAC et al., JAMA Intern Med 2019;179:1084-1093 (PMID 31233095); Gray SL et al., JAMA Intern Med 2015;175:401-407 (PMID 25621434)
Role in the trial
Not matched to a registered study
Identity check
no open identity hold
Audit mark
contested
Review state
Written into the record, not signed off as a reviewed claim

How many documents were read

  • 19 documents were read for this substance.

    RNAWiki source record

  • 8 of them state the same bioavailability, and they agree.

    RNAWiki source record

Where else this substance is registered

FDA substance identifier (UNII)
5T619TQR3R
RxNorm concept
855182

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

    The opening statement carries the origin: Written into the record, not signed off.

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Not passed

    Safety mode resolved

    No register row and no identity class settled the question.

  • Passed

    Canonical metadata present

    slug and display name present

What is missing or unclearRead from sources, not yet reviewed

How this medicine reached us

Kept near the foot of the page. A historical event moves up only when it changes something about this substance today.

What the approval register records

  • 20 approved applications cover products containing this substance. The earliest was NDA020771, approved 19980325 to UPJOHN.

    Drugs@FDA application register · NDA020771 · read 2026-08-29

  • Marketing status on the register: discontinued, none (tentative approval) and prescription.

    Drugs@FDA application register · NDA020771 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 19980325.

    FDA National Drug Code directory · 0093-7164 · read 2026-08-29

What is missing or unclearRead from sources, not yet reviewed

What to learn next

Ordered by what would most change how you read this page, starting with what is easiest to misunderstand.

This order is fixed in code and does not count clicks or time on the page.

What is not here

7 questions this page could not answer

These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.

  • What was measured, goal by goal — found nothing in the sources checked.
  • How close this is to real life — found nothing in the sources checked.
  • Felt, measured, or meaningful — found nothing in the sources checked.
  • How long anything takes — found nothing in the sources checked.
  • What it may clash with — found nothing in the sources checked.
  • Other ways to the same goal — found nothing in the sources checked.
  • What changed on this page — found nothing in the sources checked.

The record as stored

The full record, for auditing

Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.

The older medicine-wide conclusion held in this record

Written for a clinical reader, and about the medicine as a whole rather than about one indication, population and set of trials. RNAWiki does not treat it as a programme conclusion and no reviewer has signed it off in that form. It is here word for word because it is what the record holds.

A non-selective muscarinic antagonist that is mostly a delivery vehicle for its own metabolite: its US label reports 11.8 fewer weekly incontinence episodes against 6.9 on placebo and 1.8 fewer daily voids against 1.2, yet as the active control in other companies' trials it failed to separate from placebo in SCORPIO (p=0.11 on both endpoints, n=2,336) and missed on micturitions in EMPOWUR (p=0.0988, n=1,530).

Recorded evidence blocks (9)

On the Tolterodine label: indicated for what?


"Tolterodine Tartrate Extended-Release Capsules are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency [see CLINICAL STUDIES (14) ] . Tolterodine Tartrate Extended-Release Capsules are an antimuscarinic indicated for the treatment of overactive bladder…": indications and usage on Tolterodine's label. DailyMed label · bbbee85a-e5e2-24ec-e053-2995a90acfd8 · 2026-08-05

69 registered trials of Tolterodine — at which phases?


Registered studies posting no result
44 of 69

69 registered studies of Tolterodine: 18 phase3, 18 phase4, 13 phase2, 9 phase1, 8 na, 7 na or unstated. CLINICALTRIALS_SNAPSHOT · 2026-09-01

297 with a PubMed record

Show the evidence
  • phase3
    18
  • phase4
    18
  • phase2
    13
  • phase1
    9
  • na
    8
  • na or unstated
    7
6 more recorded rows
  • completed
    57
  • unknown
    5
  • terminated
    4
  • active not recruiting
    1
  • not yet recruiting
    1
  • withdrawn
    1

recorded 2026-09-01 · last checked 2026-09-04

5 of Tolterodine's trials stopped: accrual/recruitment, other?


accrual/recruitment (1) and other (4): Tolterodine's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"New department chairman instructed PI to discontinue study."; 5 of 69 registered studies

Show the evidence

Trial

  • NCT00323635
    terminated; "New department chairman instructed PI to discontinue study."
  • NCT00439192
    terminated; "side effect profile did not match expectations"
  • NCT00523068
    withdrawn; "it stopped at a regulatory stage"
  • NCT00852696
    terminated; "Investigator left Cleveland Clinic and absolutely no data is available."
  • NCT01500382
    terminated; "This study was terminated early due to insufficient recruitment."

recorded 2026-09-01 · last checked 2026-09-04

Human studies of Tolterodine used Tolterodine 4 mg — over how long?


Human studies of Tolterodine used "Tolterodine 4 mg". ClinicalTrials.gov · 2026-09-01

7 recorded entries; human; tablet; also "arm 2: Tolterodine 4 mg + local oestrogens once daily for 12 weeks", "Detrusitol ER 4mg", "Tolterodine ER 4mg"

Show the evidence

human

  • NCT00648310
    Tolterodine 4 mg
  • NCT00648310
    arm 2: Tolterodine 4 mg + local oestrogens once daily for 12 weeks
  • NCT00730535
    Detrusitol ER 4mg
  • NCT00939120
    Tolterodine ER 4mg
  • NCT02485067
    tablet; Detrusitol 2mg tablet
  • NCT02485067
    tablet; Placebo(For Detrusitol 2mg tablet)
1 more recorded row
  • human NCT05250245
    Tolterodine Tartrate 4 MG

recorded 2026-09-01 · last checked 2026-09-04

Which 32 trials of Tolterodine posted no result?


Posted no result
32 of 32 completed trials
Registrations
NCT00802373, NCT01604928, NCT00174798, NCT00746681, NCT00282932 and NCT00332137, and 26 more
Completion dates
oldest 2004-10; newest 2022-01-01
Show the evidence

Trial

  • NCT00802373
    2004-10
  • NCT01604928
    2005-01-25
  • NCT00174798
    2006-05
  • NCT00746681
    2006-11
  • NCT00282932
    2007-05-14
  • NCT00332137
    2007-08
14 further recorded trials
  • NCT00413790
    2007-09
  • NCT00648310
    2007-12
  • NCT00553657
    2008-01
  • NCT00368706
    2008-03
  • NCT01181505
    2008-06
  • NCT00703703
    2008-10
  • NCT00481728
    2008-12
  • NCT00564226
    2009-02
  • NCT00730535
    2009-07
  • NCT00966004
    2010-02-15
  • NCT01036035
    2010-04
  • NCT01011036
    2010-06
  • NCT01291316
    2011-11
  • NCT01521767
    2011-11

At the median, Tolterodine's trials enrolled 156 people — anything larger?


Median enrolment
156
Largest enrolment
11157
Registered trials counted
68

What do 298 spontaneous reports say about Tolterodine — and not say?


These are reports people sent to a regulator. They do not show the medicine caused the reaction. Nobody counted how many people took the medicine and reported nothing. The same event can be reported more than once, and many reports are incomplete. News coverage, lawsuits and new warnings change how often people report. A count is not a rate and not a risk.

Tolterodine appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 298 reaction mentions were counted: urinary retention 53; fall 39; confusional state 33; drug hypersensitivity 30. FAERS via Open Targets · CHEMBL1382 · 2026-06-24

Show the evidence
  • urinary retention
    53
  • fall
    39
  • confusional state
    33
  • drug hypersensitivity
    30
  • palpitations
    30
  • dry mouth
    29
4 more recorded rows
  • drug interaction
    28
  • hyponatraemia
    20
  • dysphagia
    18
  • general physical health deterioration
    18

recorded 2026-06-24 · last checked 2026-09-04

Which 10 reactions does Tolterodine's label not list?


confusional state, drug hypersensitivity and drug interaction and 7 more reported for Tolterodine, absent from its label. FAERS via Open Targets · CHEMBL1382 · 2026-06-24

2 label terms; 10 reported and unlisted; bbbee85a-e5e2-24ec-e053-2995a90acfd8

Show the evidence
  • confusional state
    count not stated
  • drug hypersensitivity
    count not stated
  • drug interaction
    count not stated
  • dry mouth
    count not stated
  • dysphagia
    count not stated
  • fall
    count not stated
4 more recorded rows
  • general physical health deterioration
    count not stated
  • hyponatraemia
    count not stated
  • palpitations
    count not stated
  • urinary retention
    count not stated

recorded 2026-06-24 · last checked 2026-09-04

Tolterodine and CYP2D6, CYP3A4 and CYTOCHROME P450: shared by which compounds?


CYP2D6, CYP3A4 and CYTOCHROME P450 appear in Tolterodine's recorded interaction sentences, 8 in all. DailyMed label · bbbee85a-e5e2-24ec-e053-2995a90acfd8 · 2026-08-05

CYP1A2, CYP2D6, CYP2D6, CYP3A4, CYP3A4; 5 shared nodes; drug_interactions, pharmacokinetics

Show the evidence

Interaction statement

  • drug_interactions
    Potent CYP3A4 Inhibitors: Coadministration may increase systemic exposure to tolterodine tartrate extended-release capsules.
  • drug_interactions
    ( 7.6 ) 7.1 Potent CYP2D6 Inhibitors Fluoxetine, a potent inhibitor of CYP2D6 activity, significantly inhibited the metabolism of tolterodine immediate release in CYP2D6 extensive metabolizers, resulting in a 4.8-fold increase in tolterodine AUC.
  • drug_interactions
    7.2 Potent CYP3A4 Inhibitors Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers.
  • drug_interactions
    For patients receiving ketoconazole or other potent CYP3A4 inhibitors such as itraconazole, clarithromycin, or ritonavir, the recommended dose of tolterodine tartrate extended-release capsules is 2 mg once daily [see DOSAGE AND ADMINISTRATION (2.2) and CLINICAL PHARMACOLOGY (12.3) ] .
  • drug_interactions
    7.4 Other Drugs Metabolized by Cytochrome P450 Isoenzymes In vivo drug-interaction data show that tolterodine immediate release does not result in clinically relevant inhibition of CYP1A2, 2D6, 2C9, 2C19, or 3A4 as evidenced by lack of influence on the marker drugs caffeine, debrisoquine, S-warfarin, and omeprazole [see CLINICAL PHARMACOLOGY (12.3) ].
  • pharmacokinetics
    The primary metabolic route involves the oxidation of the 5-methyl group and is mediated by the cytochrome P450 2D6 (CYP2D6) and leads to the formation of a pharmacologically active metabolite, 5-HMT.
2 more recorded rows
  • Interaction statement pharmacokinetics
    Variability in Metabolism A subset of individuals (approximately 7% of Caucasians and approximately 2% of African Americans) are poor metabolizers for CYP2D6, the enzyme responsible for the formation of 5-HMT from tolterodine.
  • Interaction statement pharmacokinetics
    The identified pathway of metabolism for these individuals (“poor metabolizers”) is dealkylation via cytochrome P450 3A4 (CYP3A4) to N -dealkylated tolterodine.
  • CYP1A2
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole

CYP2D6

  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Fluoxetine
  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Fluoxetine

CYP3A4

  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium
  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium

recorded 2026-08-05 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL1382
PubChem CID
60774
CAS number
124937-53-7
RxCUI
221174
InChIKey
OOGJQPCLVADCPB-HXUWFJFHSA-N
Trade name
Blerone xl, Detrusitol, Detrusitol xl, Efflosomyl xl, Inconex xl, Mariosea xl, Neditol xl, Preblacon xl, Santizor xl, Detrol, Detrol la
Development code
KABI 2234, PNU-200583E
Also called
Tolterodina, long acting tolterodine, tolterodine er, TOLTERODINE TARTRATE, (+)-(R)-2-(I-(2-(DIISOPROPYLAMINO)ETHYL)BENZYL)-P-CRESOL L-TARTRATE (1:1) (SALT), (R)-2-(3-(BIS(1-METHYLETHYL)AMINO)-1-PHENYLPROPYL)-4-METHYLPHENOL (R-(R*,R*))-2,3-DIHYDROXYBUTANEDIOATE (1:1) (SALT), TOLTERODINE TARTRATE [EP MONOGRAPH], TOLTERODINE TARTRATE [JAN], TOLTERODINE TARTRATE [MART.], TOLTERODINE TARTRATE [MI], TOLTERODINE TARTRATE [ORANGE BOOK]
Salt form
Tolterodine l-tartrate
Sources (6)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported · ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · Open Targets 26.06 — CC0 · mixed register set; per-register licences in docs/specs/corpus-20k-sources.md · openFDA / DailyMed — US Government work

How these records are assembled · Which registers were checked

Index-quality checks
  • identity passed: no open identity hold
  • required summary fields resolved: 4 required field(s) not terminal: Why people use it, Best-supported result, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 6 source rows
  • no critical contamination: no quarantine open
  • canonical metadata passed: slug and display name present
  • no raw internal fields: enforced by the copy-contract test over the rendered page

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