This page shows what was measured, who it was measured in, and what that does not settle.
What Loperamide does in the body
Turning those down slows the gut, so there is more time to reabsorb water and stools become firmer and less frequent.
Loperamide is a genuine opioid, chemically related to the strong painkillers, and it works on opioid receptors on the nerves that control how fast the bowel pushes food along. The reason it is not a narcotic is a pump at the border of the brain called P-glycoprotein, which grabs the drug as it tries to cross and throws it back into the blood. That pump is the whole safety design of the drug. If another medicine disables it, or if someone takes a dose big enough to swamp it, the opioid gets into the brain — and at those doses the same molecule also blocks the electrical channels that keep the heart beating in rhythm.
Why people take it. Diarrhoea — slowing the bowel down so stools become less frequent and more solid
What happened in people
Respiratory depression from 16 mg loperamide with a P-glycoprotein inhibitor and none without it, at plasma concentrations that did not differ (P<0.001)
✎ 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.
On the WHO Model List of Essential Medicines, and not recommended by the WHO or the American Academy of Pediatrics in young children
Where it acts
Myenteric plexus — the nerve network running between the two muscle layers of the bowel wall, which sets how fast the gut pushes its contents along
Kind of result
A number that stands in for health
Supervision
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.
What the registries record it as
The substance registry classes this as chemical.
FDA substance registry · 6X9OC3H4II · 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 172 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.
Stand-in result
A stand-in result is a number measured because the real result takes too long.
A picture of it, and where the picture fails
It is like judging a journey by the speedometer rather than by arriving.
Where that stops being true. Speed does predict arrival. Many stand-in results do not predict the real one.
What people get wrong. A stand-in result is often reported as the result itself.
A surrogate endpoint substituted for a clinical endpoint, valid only where the substitution has been shown to hold.
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.
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.
Pathway
A pathway is a chain of steps inside a cell, each one setting off the next.
A picture of it, and where the picture fails
A pathway is like a row of dominoes.
Where that stops being true. Dominoes fall one way. Pathways loop back and can switch themselves off.
What people get wrong. Changing one step is read as changing the outcome. Other steps often absorb it.
An ordered series of molecular interactions producing a defined cellular change.
What happened in people◇Read from sources, not yet reviewed
What was measured, goal by goal
One row for each goal a registered study measured something for. One column for each kind of thing that could be measured.
Registered studies list 30 outcome measures that RNAWiki could read. A registered study says what someone planned to measure. It does not say what they found. 0 of the matched studies tested this substance, and 0 posted a result.
There is no single score. A strong test result and a weak life result are different facts.
Goals down the side, kinds of measurement across the top. Each cell says what kind of thing was registered, not what was found.
Goal
Life outcome
What a body can do
How a person feels
A test result
A step in the body
Harms
How long
Who was studied
Pain
∅Nothing in the sources checkedNo registered study lists a life outcome for this goal.
∅Nothing in the sources checkedNo registered study lists a performance measure for this goal.
…Waiting for a reviewer2 registered symptom measure.
∅Nothing in the sources checkedNo registered study lists a test result for this goal.
∅Nothing in the sources checkedNo registered study lists a body-step measure for this goal.
—Not recordedHarms were not a registered measure for this goal.
—Not recordedNo finished study window is recorded.
…Waiting for a reviewerWho was studied is listed further down the page.
Which registered measures put each goal on this table
Pain
reduction in daily genital pain; pain numeric rating scale
Sorted by fixed word lists, version v1. A name the rules do not recognise stays unsorted rather than moving to the nearest column.
What each mark on this table means
∅ Nothing in the sources checked
No registered study lists a life outcome for this goal.
… Waiting for a reviewer
2 registered symptom measure.
— Not recorded
Harms were not a registered measure for this goal.
What happened in people◇Read 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.
Respiratory response to carbon dioxide rebreathing after 16 mg loperamide with 600 mg quinidine against placebo
✓ The study showed what it set out to show
Who was studied
Loperamide with and without quinidine in healthy volunteers
How many people
8
Study design
Mechanistic crossover study in healthy male volunteers
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
No respiratory depression with loperamide alone; significant respiratory depression with loperamide plus quinidine, P<0.001, not explained by plasma loperamide concentrations
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. Eight participants, all male, all healthy. The finding is mechanistically decisive and the sample is small, and one P-glycoprotein inhibitor was tested rather than the class.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
Drugs@FDA: IMODIUM (loperamide hydrochloride) capsules, NDA 017694, J&J Consumer — original approval 28 December 1976 (https://www.accessdata.fda.gov/scripts… · a recorded source, not a stored snapshot
Duration and severity of acute diarrhoea in children under 12, and serious adverse events
✓ The study showed what it set out to show
Who was studied
Loperamide for acute diarrhoea in children — pooled randomised evidence
How many people
1691
Study design
Systematic review and meta-analysis of randomised placebo-controlled trials
Compared against
A dummy treatment
Kind of result
A number that stands in for health
What was found
Still diarrhoeal at 24 hours, prevalence ratio 0.66 (95% CI 0.57 to 0.78); duration shorter by 0.8 days (95% CI 0.7 to 0.9); stool count ratio 0.84 (95% CI 0.77 to 0.92)
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. Serious adverse events — ileus, lethargy or death — in 8 of 927 on loperamide (0.9%) against 0 of 764 on placebo, and every one of them in a child under three years old.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt
Interval reported. 95% CI 0
Written into the record, not signed off as a reviewed claim.
Drugs@FDA: IMODIUM (loperamide hydrochloride) capsules, NDA 017694, J&J Consumer — original approval 28 December 1976 (https://www.accessdata.fda.gov/scripts… · a recorded source, not a stored snapshot
Cardiac conduction abnormality and death in association with significantly elevated loperamide concentrations
✓ The study showed what it set out to show
Who was studied
Loperamide abuse and cardiac dysrhythmia — published case series
How many people
2
Study design
Case reports and postmarketing surveillance, not a trial
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
What was found
Not applicable — two fatalities with measured elevated loperamide concentrations, reported alongside a documented rise in oral loperamide misuse
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. Case reports establish that a harm occurs and cannot establish how often. They are included because the regulatory response — package size limits and blister packaging — followed from them rather than from a trial.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
Drugs@FDA: IMODIUM (loperamide hydrochloride) capsules, NDA 017694, J&J Consumer — original approval 28 December 1976 (https://www.accessdata.fda.gov/scripts… · a recorded source, not a stored snapshot
What we know
RNAWiki holds 3 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 happened in people◇Read from sources, not yet reviewed
How close this is to real life
The top step is something a person would feel or care about. The bottom is a guess from software. Filled steps are where evidence exists for this substance.
□Living longer, or avoiding a major eventNo evidence recorded. Death, a heart attack, a stroke, a hospital stay.No registered study measures this.
□What a body can do day to dayNo evidence recorded. Walking, dressing, breathing, recovering.No registered study measures this.
□Measured performanceNo evidence recorded. How much was lifted, how far was run, how fast.No registered study measures this.
■Symptoms and quality of lifeEvidence recorded. Pain, tiredness, mood, sleep, as the person rated it.2 registered measures of this kind.
■A number that stands in for healthEvidence recorded. Cholesterol, blood sugar, bone density. A stand-in, not the thing itself.7 registered measures of this kind.
■A step measured inside a personEvidence recorded. Something measured in human tissue or human cells.A human record sits on the stored organism ladder.
■AnimalsEvidence recorded. Mice, rats, dogs. Useful for ideas, not proof about people.Stored records in Rat. A result in animals says what to test next. It does not say what happens in people.
■Cells in a dishEvidence recorded. Cells or chemistry on a bench, far from a whole body.Stored mechanism abstracts describe steps measured in cells or tissue.
□A guess from softwareNo evidence recorded. Nobody measured it. RNAWiki never publishes one as a finding.RNAWiki stores no prediction for this record. Software can suggest a link. RNAWiki does not publish one as a finding.
Higher on these steps means closer to something a person would feel. It does not mean better done.
What it changes in the body◇Read 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.
Start
Loperamide
What a person takes: Oral capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt.
The measurement behind this step
Every form is oral and the drug is meant to work in the gut it is passing through. Under 1% reaches the systemic circulation, the combined result of poor absorption, intestinal P-glycoprotein efflux and extensive first-pass metabolism — so the formulation problem here is the opposite of the proton pump inhibitors’, which have to be protected on the way through.
Getting in
Swallowed, and mostly never absorbed
Very little of the dose reaches the bloodstream. Most of it stays in the gut, which is the only place it is meant to work.
╌╌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
Oral bioavailability is under 1%, the result of poor absorption combined with extensive first-pass metabolism by CYP3A4 and CYP2C8 and by intestinal P-glycoprotein efflux returning absorbed drug to the lumen. The pharmacokinetics are those of a locally acting drug that happens to be a systemic opioid on paper.
It finds opioid receptors in the wall of the bowel
The gut has its own nervous system, and it carries the same opioid receptors as the brain. Loperamide acts on those.
╌╌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
Full agonism at mu-opioid receptors on neurons of the myenteric plexus, the network between the circular and longitudinal muscle layers that generates propulsive peristalsis. Receptor affinity is comparable to that of the strong analgesic opioids; the difference in effect is entirely one of where the drug is allowed to go.
Peristalsis weakens, contents move more slowly, and the colon has longer to reabsorb water. Stools become firmer and less frequent. The anal sphincter also tightens, which is why it helps urgency.
╌╌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
Inhibition of acetylcholine and prostaglandin release from myenteric neurons reduces propulsive peristalsis and lengthens transit time, increasing water and electrolyte absorption. Anal sphincter tone increases, reducing urgency and incontinence — the mechanism behind the ileostomy-output indication as much as the diarrhoea one.
The molecule is fatty enough to cross into the brain easily. It does not, because a transporter at the blood-brain barrier catches it and pushes it back into the blood, over and over. That single pump is why this is sold in a supermarket and morphine is not.
──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
Loperamide is a high-affinity P-glycoprotein substrate. At the blood-brain barrier the ABCB1 transporter effluxes it back to the luminal side faster than passive diffusion delivers it, holding brain concentrations near zero despite a logP around 5.5. Mdr1a-knockout mice show dramatically increased brain penetration of loperamide, and the human demonstration is the quinidine crossover.
Block that transporter with another drug, or take enough loperamide to overwhelm it, and the opioid reaches the brain. In volunteers given a transporter blocker, 16 mg depressed breathing — at blood levels that were no higher than without it.
──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
Efflux is saturable and competitively inhibitable. With 600 mg quinidine, 16 mg loperamide produced significant respiratory depression on carbon dioxide rebreathing (P<0.001) where the same dose alone produced none, and plasma concentrations did not account for the difference. The safety of the drug is a transport phenomenon, not a pharmacodynamic one.
And above that dose it stops being an opioid problem
At the very high doses people use to get past the barrier, the same molecule blocks the electrical channels that control the heartbeat. That is what has killed people — not the opioid effect, but the rhythm.
──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
At supratherapeutic plasma concentrations loperamide blocks the hERG potassium channel, prolonging repolarisation and the QT interval, and blocks cardiac sodium channels, widening the QRS complex. The reported presentation is ventricular dysrhythmia including torsades de pointes and Brugada-pattern conduction, with fatalities documented at significantly elevated loperamide concentrations. The cardiac liability sits entirely above the concentration range the blood-brain barrier normally enforces, which is why thirty years of use did not reveal it.
No suggested links are held for this record, so nothing is hidden from this path.
What we know
The record describes 6 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 it would be like to take◇Read from sources, not yet reviewed
Felt, measured, or meaningful
Three different things that get called the same word. Registered studies measured all three, and mixing them is how a blood test becomes a health claim.
Felt
Things a person could notice without a test.
reduction in daily genital pain
pain numeric rating scale
Measured
Things only a test, a scale or a device shows.
maximum concentration at steady state
minimum concentration at steady state
average concentration of administration interval
time of maximum concentration
area under the concentrations time curve
maximum concentration
maximum observed concentration
Meaningful
Things that change how a life goes, not only a number.
No registered study measured anything of this kind.
A registered study says what someone planned to measure. It does not say what they found. A number moving is not the same as a life going better. The two are shown apart here.
Felt, but not shown to help. A person notices a change. No study showed it leads anywhere good.
Measured, but not felt. A number moves. The person notices nothing. Both can be true.
Measured, but not shown to matter. A number moves in the good direction. Nobody showed that lives went better.
Matters, but takes years. The result that counts may take longer than anyone would keep watching.
Names that fit none of the three (21)
response rate
pharmacokinetic parameters
whole gut transit time
renal clearance
area under the curve of administration window
oro cecal transit time
average whole gut transit time
renal clearances
terminal half life
residence time
distribution volume at steady state
total body clearance
one or more drug related adverse events
grade 3 or higher diarrhea according to nci ctcae v4 0
phase i number of dose limiting toxicities
dose escalation phase maximum tolerated dose of lmp744
treatment related adverse events
objective response rate
maximum tolerated dose of selinexor
fecal incontinence
These are harms, study-process measures, or names the rules did not recognise. They are shown rather than dropped.
What it would be like to take◇Read from sources, not yet reviewed
How long anything takes
Nine different lengths of time that get confused with each other. None of them is worked out from another.
Before anything is noticed.RNAWiki does not store this separately, and never works it out from another figure on this page.
Before a test result moves.RNAWiki does not store this separately, and never works it out from another figure on this page.
Before performance moves.RNAWiki does not store this separately, and never works it out from another figure on this page.
How long the result was watched.No finished study window is recorded for a study that tested this substance.
How long people took it.How long people actually took it is not stored. The study window is not the same thing.
How long people were followed.Follow-up length is not stored separately. It is never read off the study window, which would be a different thing.
How fast the body clears it. 10.8 hours hours
Read from the label, which states: “Elimination The apparent elimination half-life of loperamide is 10.8 hours with a range of 9.1 to 14.4 hours.”
How long effects linger.RNAWiki does not store this separately, and never works it out from another figure on this page.
Beyond the studies. Nothing is recorded about the long term.
The longest finished study sets the edge of what anyone measured.
A study window is not how long people took it, and neither is how long they were followed. Where RNAWiki holds only one of the three, it shows one.
What is missing or unclear◇Read 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.
Almost anyone with acute diarrhoea, bought without a prescription, and a smaller group with chronic diarrhoea, ileostomy output or inflammatory bowel disease. Since around 2010 a further group has used it in very large doses as an opioid substitute, and some of them have died.
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: “Although loperamide hydrochloride capsules have been studied in a limited number of pediatric patients with chronic diarrhea; the therapeutic dose for the treatment of chronic diarrhea in a pediatric population has not been established.”
US prescribing information · 8b0ac05b-90c1-476b-b001-5801dd21701d · read 2026-08-30
On people who are pregnant, the label states: “These studies have revealed no evidence of impaired fertility or harm to the fetus at doses up to 10 mg/kg/day in rats (5 times the human dose based on body surface area comparison) and 40 mg/kg/day in rabbits (43 times the human dose based on body surface area comparison).”
US prescribing information · 8b0ac05b-90c1-476b-b001-5801dd21701d · read 2026-08-30
On people who are breastfeeding, the label states: “Small amounts of loperamide may appear in human breast milk.”
US prescribing information · 8b0ac05b-90c1-476b-b001-5801dd21701d · read 2026-08-30
Where the result stopped carrying
The design assumption that a peripherally restricted opioid could not be misused, defeated once people found the dose that saturates the transporter
Ileus, lethargy and death in children under three, at doses at or below 0.25 mg/kg/day
A cardiac liability that thirty years of therapeutic-dose use never revealed, because it lives above the concentration range the barrier enforces
Contraindication in dysentery, invasive enterocolitis and Clostridioides difficile, where slowing the bowel prolongs toxin contact
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 take◇Read 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 for a different goal
The studies measured something else entirely.
On this record: Some registered studies measured things that match no goal on this page.
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 (10)
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 take◇Read 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 capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt
✎ 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
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.
❝ Quoted from a source
Where this came from
Copied from a source RNAWiki stored, with the source named.
Suppression classes recorded: S6.
No source is stored against this line.
What is in the pack
Every form is oral and the drug is meant to work in the gut it is passing through.
✎ 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. The rest of the recorded wording: Under 1% reaches the systemic circulation, the combined result of poor absorption, intestinal P-glycoprotein efflux and extensive first-pass metabolism — so the formulation problem here is the opposite of the proton pump inhibitors’, which have to be protected on the way through.
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 take◇Read 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
Contraindicated in acute dysentery with blood in the stool and high fever, in acute ulcerative colitis, in bacterial enterocolitis caused by invasive organisms, and in antibiotic-associated pseudomembranous colitis; discontinue at the first sign of abdominal distension. Ileus, abdominal distension and toxic megacolon have been reported. The labels warn of serious cardiac events including QT interval prolongation, torsades de pointes and cardiac arrest with doses higher than recommended — the reason over-the-counter package sizes were limited and blister packaging introduced. Concomitant P-glycoprotein inhibitors increase central nervous system exposure without necessarily raising plasma concentrations. Not recommended in children under two years, and the pooled paediatric randomised evidence places the harm threshold at three.
Nobody counted how many people took this and were fine, so this cannot be turned into a rate.
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.
Loperamide appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1751 reaction mentions were counted. One report can name several reactions.
open-targets-adr · recorded 2026-06-24 · a recorded source, not a stored snapshot
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 unclear◇Read 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 capsule, tablet, orally disintegrating tablet and oral solution, all of the hydrochloride salt
✎ 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
A recorded note compares this form with the others that are sold. It is kept below, word for word.
§ A fixed RNAWiki sentence
Where this came from
Wording RNAWiki always uses, not a finding about this substance.
The recorded note, unchanged: Under 1% reaches the systemic circulation, the combined result of poor absorption, intestinal P-glycoprotein efflux and extensive first-pass metabolism — so the formulation problem here is the opposite of the proton pump inhibitors’, which have to be protected on the way through.
No source is stored against this line.
What is recorded as being sold
258 products list this as an active ingredient in the United States drug directory. 216 of them contain it and nothing else.
FDA National Drug Code directory · 75907-097 · read 2026-08-29
They are sold as capsule, capsule, liquid filled, powder, solution, suspension and tablet, taken oral.
FDA National Drug Code directory · 75907-097 · read 2026-08-29
The regulator's established pharmacologic class for it is opioid agonist [epc] and opioid agonists [moa].
FDA National Drug Code directory · 75907-097 · read 2026-08-29
232 published labels name it as an active ingredient. 194 of them describe this substance alone, which is where its own label text on this page comes from.
US prescribing information · 59e1c4cf-17cc-13c9-e063-6294a90af61c · read 2026-08-29
Those labels are classed as human otc drug and human prescription drug.
US prescribing information · 59e1c4cf-17cc-13c9-e063-6294a90af61c · read 2026-08-29
1 marketed supplement label lists this ingredient, classed as fiber and other nutrients.
Those labels carry all other, nutrient and structure/function claims. A claim of that kind is written by the manufacturer and is not assessed by any regulator, so its presence says nothing about whether it is true.
Loperamide Hydrochloride is oral at HOW SUPPLIED Loperamide Hydrochloride Capsules, USP are available containing 2 mg of loperamide hydrochloride, USP., recorded as fda label in effect 2026-03-19 in the United States.
US prescribing information · 8b0ac05b-90c1-476b-b001-5801dd21701d · read 2026-08-30
Recorded price in US: 0.02645 USD per one millilitre, across 2 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
Recorded price in US: 0.05649 USD per one unit as the pricing file counts it — a tablet, capsule, patch or single item, across 23 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 take◇Read 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.
Self-experiment planning is not offered for a prescription or clinician-supervised medicine. The questions below are for a clinician or pharmacist.
Questions worth asking
Which of the trials of Loperamide 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 unclear◇Read 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 exclusion from the brain at label doses means safety at any dose; the efflux is saturable and the cardiac harm sits above it
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 every P-glycoprotein inhibitor produces the effect quinidine produced — mechanistically sound and tested for one drug only
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 reducing stool frequency treats diarrhoeal illness, when what harms people is fluid and electrolyte loss
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 an antimotility drug is neutral in infective diarrhoea, when the label contraindicates it and toxic megacolon has followed
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 unclear◇Read 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 Loperamide 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 people◇Read 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.
Disable one transporter and the antidiarrhoeal becomes a respiratory depressant, at the same blood level
In plain words
Eight healthy men took 16 mg of loperamide alone, and again with a drug that blocks the pump guarding the brain. Alone, it caused no breathing depression at all. With the blocker, it did — and the amount of drug in their blood was no higher. The barrier, not the dose, is what makes this drug safe.
What was measured
Respiratory response to carbon dioxide rebreathing after 16 mg loperamide with and without 600 mg quinidine, in a crossover of eight healthy volunteers
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
On the basis of in vitro evidence that loperamide is a P-glycoprotein substrate, eight healthy male volunteers received 16 mg of loperamide with either 600 mg of quinidine, a known P-glycoprotein inhibitor, or placebo. Central nervous system effect was measured as the respiratory response to carbon dioxide rebreathing, a standard index of opioid-induced respiratory depression. Loperamide alone produced no respiratory depression. Loperamide with quinidine did (P<0.001). The changes were not explained by increased plasma loperamide concentrations. The study demonstrated a new class of drug interaction — transporter inhibition rather than metabolic inhibition — and demonstrated that the entire clinical distinction between this drug and a narcotic rests on one efflux pump.
Written into the record, not signed off as a reviewed claim
In children under three it caused ileus, lethargy or death in 8 of 927, against none of 764 on placebo
In plain words
Pooling the randomised trials in children, loperamide did shorten diarrhoea — by about a fifth of a day at 24 hours, and 0.8 days overall. It also caused serious harm in nine children in a thousand, and every one of those cases was in a child under three years old. Nothing comparable happened on placebo.
What was measured
Duration and severity of acute diarrhoea, and serious adverse events, in randomised trials of children under 12
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
A systematic review and meta-analysis of randomised placebo-controlled trials in children under 12 with acute diarrhoea found that loperamide reduced the likelihood of still having diarrhoea at 24 hours (prevalence ratio 0.66, 95% CI 0.57 to 0.78), shortened duration by 0.8 days (95% CI 0.7 to 0.9) and reduced stool count at 24 hours (ratio 0.84, 95% CI 0.77 to 0.92). Serious adverse events, defined as ileus, lethargy or death, occurred in 8 of 927 children allocated to loperamide (0.9%, 95% CI 0.4% to 1.7%) and in 0 of 764 allocated to placebo (0%, 95% CI 0% to 0.5%). Every serious adverse event on loperamide occurred in a child younger than three. The authors concluded that in children under three, malnourished, moderately or severely dehydrated, systemically ill, or with bloody diarrhoea, adverse events outweigh benefits even at doses at or below 0.25 mg/kg/day; and that above three years with minimal dehydration it may be a useful adjunct to rehydration and early refeeding.
Written into the record, not signed off as a reviewed claim
An over-the-counter antidiarrhoeal turned out to be a lethal cardiac drug at the doses people were taking it in
In plain words
From around 2010, people trying to manage opioid withdrawal began taking loperamide in enormous quantities to get past the brain barrier. It worked, and it also stopped hearts. Published cases describe abnormal rhythms and deaths, and the packaging was changed as a result.
What was measured
That a drug excluded from the brain at label doses is therefore safe at any dose — an inference the mechanism does not support, because the exclusion is saturable and the cardiac liability sits above it
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Loperamide is a mu-opioid agonist that produces no central effects at therapeutic oral doses because of poor bioavailability and P-glycoprotein-mediated exclusion from the central nervous system. At supratherapeutic oral doses, central opioid effects do occur, and reports of ventricular dysrhythmia with prolongation of the QRS duration and the QTc interval followed the rise in oral loperamide misuse as an opioid substitute among people attempting to self-treat opioid addiction. The 2017 case report describes two fatalities with significantly elevated loperamide concentrations. The mechanism is dual channel blockade — hERG potassium channel block giving QT prolongation, cardiac sodium channel block giving QRS widening — appearing only at concentrations the barrier normally prevents. The regulatory response was to the packaging rather than to the availability: over-the-counter package quantities were limited and unit-dose blister packaging introduced, so that acquiring a supratherapeutic quantity takes deliberate effort. A drug can be safe for thirty years and become lethal without changing, if the way people use it changes.
Written into the record, not signed off as a reviewed claim
Slowing the bowel is exactly wrong when the bowel is clearing an infection
In plain words
In dysentery, in Clostridioides difficile and in any diarrhoea with blood or high fever, keeping the contents inside for longer keeps the toxin in contact with the lining. The label contraindicates the drug in those situations, and toxic megacolon has followed when it was used anyway.
What was measured
Not recorded
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
The United States labels contraindicate loperamide in patients with acute dysentery, characterised by blood in the stool and high fever; in acute ulcerative colitis; in bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella and Campylobacter; and in pseudomembranous colitis associated with broad-spectrum antibiotics. Abdominal distension, toxic megacolon and ileus have been reported, particularly in acute ulcerative colitis and in Clostridioides difficile-associated diarrhoea, and the label directs discontinuation at the first sign of abdominal distension. The mechanism is the drug working as designed: an antimotility agent prolongs contact between luminal toxin and mucosa. The paediatric meta-analysis places bloody diarrhoea in the same category, among the conditions in which harms outweigh benefits at any dose tested.
Source
IMODIUM and IMODIUM A-D (loperamide hydrochloride) United States prescribing information and Drug Facts labelling, Contraindications and Warnings (NDA 017694 and NDA 019487)
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
What it actually does for adults is shorten an illness, not treat one
In plain words
The endpoint this drug is licensed against is symptom control: fewer stools, firmer stools, a shorter episode. It does not kill an organism, does not replace lost fluid, and does not change whether someone gets better.
What was measured
Prevalence of continuing diarrhoea at 24 hours, duration in days and stool count, against placebo
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The registered indications are control and symptomatic relief of acute non-specific diarrhoea and of chronic diarrhoea associated with inflammatory bowel disease, and reduction of the volume of ileostomy discharge. In the paediatric randomised literature — the largest pooled dataset with a placebo comparator — the measured effects were a prevalence ratio of 0.66 for still having diarrhoea at 24 hours, a reduction in duration of 0.8 days, and a stool-count ratio of 0.84. The authors framed the drug as a possible adjunct to oral rehydration and early refeeding rather than as a treatment, which is the correct reading of an antimotility agent: what causes death in diarrhoeal illness is fluid and electrolyte loss, and this drug does not address it.
Written into the record, not signed off as a reviewed claim
The transporter interaction is documented for quinidine and assumed for everything else that inhibits it
In plain words
Only one drug has actually been tested for the interaction that lets loperamide into the brain. A number of common medicines block the same pump, and the interaction is expected to apply to them too — but that is reasoning from the mechanism rather than from a trial.
What was measured
That every P-glycoprotein inhibitor produces the central opioid effect quinidine produced — mechanistically sound, tested for one drug and assumed for the rest
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
The volunteer study that established the interaction used quinidine, a strong P-glycoprotein inhibitor, and measured a hard physiological endpoint. Many other agents inhibit P-glycoprotein to varying degrees — verapamil, ritonavir, ketoconazole, itraconazole, clarithromycin, ciclosporin among them — and the labels advise caution accordingly. No comparable volunteer study measuring respiratory depression has been published for any of them, so the extrapolation is from transporter chemistry rather than from measurement. The extrapolation is likely correct and is stated here as an inference because it has not been demonstrated. The same logic runs the other way for CYP3A4 and CYP2C8 inhibitors, which raise plasma loperamide by slowing its metabolism rather than by opening the barrier, and which the label also flags.
This order is fixed in code and does not count clicks or time on the page.
What is not here
3 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 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 full mu-opioid agonist that acts only on the nerves of the bowel wall because a transporter at the blood-brain barrier pumps it straight back out — proved when 16 mg with a P-glycoprotein inhibitor produced respiratory depression in healthy volunteers that 16 mg alone did not, at plasma concentrations that were no higher: it shortens acute diarrhoea in children by 0.8 days, caused ileus, lethargy or death in 8 of 927 children under 3 against 0 of 764 on placebo, and at the doses used to defeat the barrier deliberately it blocks cardiac ion channels and kills.
Recorded evidence blocks (13)
Q2
What did Loperamide's largest trial (563 people) and its longest (14 years) measure?
563 people in Loperamide's largest registered study, 14 years in its longest registered window, measuring maximum concentration at steady state (Css max). ClinicalTrials.gov · 2026-09-01
19 phase2, 17 phase1, 13 phase3, 8 phase4, 6 na, 1 early phase1; NCT01391962; 2026-01-16; no ageing endpoint recorded. Last human test completed 2026, NCT01391962.
Interpretation These counts include studies where Loperamide was a comparison treatment, a background treatment or an exposure in an observational study, and the longest window may be a planned end date. Trial roles have not yet been classified for this record.
Show the evidence
phase2
19
phase1
17
phase3
13
phase4
8
na
6
early phase1
1
1 more recorded row
Last recorded human testNCT01391962
2026-01-16
recorded 2026-09-01 · last checked 2026-09-04
Q3
From rat to human: where has Loperamide shown biomarker?
Interpretation maximum concentration at steady state (Css max) — the recorded outcome words.
Show the evidence
rat
mechanism-only
humanNCT01596764
biomarker; maximum concentration at steady state (Css max); 57
recorded 2026-09-01 · last checked 2026-09-04
Q4
8 of Loperamide's trials stopped: safety, futility/efficacy, accrual/recruitment, other?
safety (2), futility/efficacy (1), accrual/recruitment (2) and other (3): Loperamide's stop wording, clustered. ClinicalTrials.gov · 2026-09-01
"Lack of personnel to complete trial"; 8 of 57 registered studies
Show the evidence
Trial
NCT00591357
suspended; "Lack of personnel to complete trial"
NCT00650637
terminated; "The study was prematurely discontinued due to administrative reasons on August 18, 2003. There were no safety concerns that led to the decision to terminate."
NCT01717456
terminated; "Low enrollment led sponsor to terminate study early."
NCT02217982
terminated; "Study did not meet required enrollment numbers"
NCT02263365
terminated; "Unable to meet study requirements"
NCT02266849
terminated; "Insuficcient recruiting"
2 further recorded trials
NCT04172597
terminated; "Strategic business decision (unrelated to safety)"
NCT06865677
terminated; "This protocol was terminated prematurely because the prior principal investigator departed the Institute without treating any participants."
recorded 2026-09-01 · last checked 2026-09-04
Q5
Human studies of Loperamide used Loperamide 2mg — over how long?
Loperamide's half-life is 10.8 hours — which schedules were studied?
10.8 hours, the half-life Loperamide's label states. openfda-label · 59e1c4cf-17cc-13c9-e063-6294a90af61c · 2026-08-30
Show the evidence
half life
10.8 hours hours; Elimination The apparent elimination half-life of loperamide is 10.8 hours with a range of 9.1 to 14.4 hours.
metabolism
Metabolism In vitro loperamide is metabolized mainly by cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, to form- N-demethyl loperamide.
recorded 2026-08-30 · last checked 2026-09-04
Q7
Which of area under the concentrations time curve, area under the curve of administration window and average concentration of administration interval did Loperamide's trials measure?
area under the concentrations time curve, area under the curve of administration window and average concentration of administration interval lead 30 outcome terms across Loperamide's trials. ClinicalTrials.gov · 2026-09-01
Interpretation renal clearance, area under the curve of administration window, maximum concentration at steady state, minimum concentration at steady state, average concentration of administration interval and time of maximum concentration follow.
Show the evidence
response rate
1
pharmacokinetic parameters
1
whole gut transit time
1
renal clearance
1
area under the curve of administration window
1
maximum concentration at steady state
1
14 more recorded rows
minimum concentration at steady state
1
average concentration of administration interval
1
time of maximum concentration
1
oro cecal transit time
1
average whole gut transit time
1
renal clearances
1
area under the concentrations time curve
1
maximum concentration
1
terminal half life
1
residence time
1
distribution volume at steady state
1
total body clearance
1
one or more drug related adverse events
1
reduction in daily genital pain
1
recorded 2026-09-01 · last checked 2026-09-04
Q8
Which of Loperamide's 12 ongoing trials reports first?
Number of Participants with One or More Drug-Related Adverse Events; Incidence of fecal microbiota transplantation (FMT)-related adverse events; latest 2030-01
Show the evidence
Trial
NCT02057133
"A Study of LY2835219 (Abemaciclib) in Combination With Therapies for Breast Cancer That Has Spread"; n 198; "Number of Participants with One or More Drug-Related Adverse Events"; 2026-12
NCT04038619
"Fecal Microbiota Transplantation in Treating Immune-Checkpoint Inhibitor Induced-Diarrhea or Colitis in Genitourinary Cancer Patients"; n 40; "Incidence of fecal microbiota transplantation (FMT)-related adverse events"; 2027-12-31
NCT04216329
"Selinexor (KPT-330) in Combination With Temozolomide and Radiation Therapy in Patients With Newly Diagnosed Glioblastoma"; n 11; "Maximum Tolerated Dose (MTD) of Selinexor"; 2028-07-30
NCT05252988
"Three Antidiarrheal Strategies in HER2+/HR+ Early Breast Cancer Patients Treated With Extended Adjuvant Neratinib"; n 177; "The incidence of neratinib discontinuations due to diarrhoea at the end of 3 cycles (1 cycle= 28 days) of neratinib treatment."; 2030-01
NCT05528848
"Multi-System Analysis of Opioid Receptor Binding"; n 25; "MOR BPND measurement - [11C]carfentanil"; 2027-09
NCT05677282
"Single Dose Antibiotic Treatment of Acute Watery Diarrhea, Rifaximin Versus Azithromycin, With Loperamide Adjunct"; n 150; "Therapeutic efficacy of single-dose rifaximin (550 mg) with loperamide in treating acute watery diarrhea compared to single-dose azithromycin (500 mg) with loperamide."; 2025-12
6 further recorded trials
NCT06148025
"Antibiotics and Vaccine Immune Responses Study"; n 348; "Sub-study 1 BCG re-challenge"; 2028-10-01
NCT06424522
"A Bowel Management Program (Retrograde Rectal Enema) for the Treatment of Low Anterior Resection Syndrome in Rectal Cancer Patients"; n 80; "Fecal incontinence"; 2028-12-31
NCT06892093
"Probiotics for Prevention of Neratinib-Induced Diarrhea in Breast Cancer Patients"; n 308; "Incidence of Grade ≥3 Diarrhea"; 2027-12
NCT07016737
"Immunochemotherapy ± Salvage Chemoradiation for Local Recurrence of Esophageal Squamous Cell Carcinoma After Definitive Chemoradiotherapy"; n 79; "2-year ARS rate"; 2029-09-01
NCT07426822
"Rash & Diarrhea Prophylaxis With Capivasertib"; n 108; "Number of patients who experience grade 2 or greater diarrhea as assessed by Common Terminology Criteria for Adverse Events (CTCAE) v4.0"; 2029-04
NCT07756359
"Tirzepatide for Ileal Pouch-anal Anastomosis (IPAA) and Chronic High Bowel Frequency (I8F-NS-X008)"; n 20; "Proportion of patients achieving a decrease of the average daily bowel frequency by 30% at week 12 (Week 16 if applicable)"; 2027-09
recorded 2026-09-01 · last checked 2026-09-04
Q9
Which 15 trials of Loperamide posted no result?
Posted no result
15 of 15 completed trials
Registrations
NCT00359970, NCT02340481, NCT00685607, NCT00806299, NCT00954304 and NCT01596777, and 9 more
Completion dates
oldest 2003-08; newest 2024-04-30
Show the evidence
Trial
NCT00359970
2003-08
NCT02340481
2006-05
NCT00685607
2008-10
NCT00806299
2008-11
NCT00954304
2009-09
NCT01596777
2010-05
9 further recorded trials
NCT00401388
2011-10
NCT01596764
2012-01
NCT01350570
2014-09
NCT04186936
2019-12-26
NCT04315116
2020-09-01
NCT04225078
2022-01-12
NCT03501498
2022-03-01
NCT05252546
2022-08-02
NCT04823065
2024-04-30
Q10
At the median, Loperamide's trials enrolled 40 people — anything larger?
Median enrolment
40
Largest enrolment
563
Registered trials counted
55
Q11
What do 1751 spontaneous reports say about Loperamide — 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.
Loperamide appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1751 reaction mentions were counted: diarrhoea 281; somnolence 244; coma 216; gastrooesophageal reflux disease 196. open-targets-adr · CHEMBL1707 · 2026-06-24
Show the evidence
diarrhoea
281
somnolence
244
coma
216
gastrooesophageal reflux disease
196
pneumonia aspiration
185
drug abuse
155
4 more recorded rows
constipation
128
vomiting
123
abdominal pain
113
electrocardiogram qt prolonged
110
recorded 2026-06-24 · last checked 2026-09-04
Q12
Loperamide and CYP2C8, CYP3A4 and P-GLYCOPROTEIN: shared by which compounds?
CYP2C8, CYP3A4 and P-GLYCOPROTEIN appear in Loperamide's recorded interaction sentences, 8 in all. openfda-label+europepmc · 2026-08-30
Interpretation pharmacokinetics
Show the evidence
CYP2B6pharmacokinetics
In addition, CYP2B6 and CYP2D6 appear to play a minor role in loperamide N-demethylation.
CYP2C8
pharmacokinetics
Metabolism In vitro loperamide is metabolized mainly by cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, to form- N-demethyl loperamide.
pharmacokinetics
In an in vitro study, quercetin (CYP2C8 inhibitor) and ketoconazole (CYP3A4 inhibitor) significantly inhibited the N-demethylation process by 40% and 90%, respectively.
pharmacokinetics
Concomitant use of loperamide hydrochloride capsules with inhibitors of CYP3A4 (e.g., itraconazole) or CYP2C8 (e.g., gemfibrozil) or inhibitors of P-glycoprotein (e.g., quinidine, ritonavir) can increase exposure to loperamide (see PRECAUTIONS: Drug Interactions ).
CYP2D6pharmacokinetics
In addition, CYP2B6 and CYP2D6 appear to play a minor role in loperamide N-demethylation.
CYP3A4
pharmacokinetics
Metabolism In vitro loperamide is metabolized mainly by cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, to form- N-demethyl loperamide.
pharmacokinetics
In an in vitro study, quercetin (CYP2C8 inhibitor) and ketoconazole (CYP3A4 inhibitor) significantly inhibited the N-demethylation process by 40% and 90%, respectively.
pharmacokinetics
Concomitant use of loperamide hydrochloride capsules with inhibitors of CYP3A4 (e.g., itraconazole) or CYP2C8 (e.g., gemfibrozil) or inhibitors of P-glycoprotein (e.g., quinidine, ritonavir) can increase exposure to loperamide (see PRECAUTIONS: Drug Interactions ).
recorded 2026-08-30 · last checked 2026-09-04
Q13
Was Loperamide studied with fasting?
fasting is named in Loperamide's label sentences: "Using a randomized, balanced, crossover design, each patient received the following three treatments under fasting conditions: didanosine as a single agent, didanosine 5 min after a single 10 mg intravenous dose of metoclopramide, and didanosine 1 h after the final of 4 doses, 4 mg each, of…" openfda-label+europepmc · 2026-08-30
1 recorded statement; fasting
Show the evidence
fasting
Using a randomized, balanced, crossover design, each patient received the following three treatments under fasting conditions: didanosine as a single agent, didanosine 5 min after a single 10 mg intravenous dose of metoclopramide, and didanosine 1 h after the final of 4 doses, 4 mg each, of loperamide.
recorded 2026-08-30 · last checked 2026-09-04
Q14
What is recorded about Loperamide and autophagy?
"Notably, ROS scavenger N-acetyl-L-cysteine (NAC) and JNK inhibitor SP600125 effectively attenuated the induction of autophagy and apoptosis triggered by loperamide." — where Loperamide and autophagy appear together. Europe PMC · pathway abstract search · 2025-01-02
autophagy, mTOR; PMID 37863323, 39744815
Show the evidence
autophagy
PMID 37863323
"Notably, ROS scavenger N-acetyl-L-cysteine (NAC) and JNK inhibitor SP600125 effectively attenuated the induction of autophagy and apoptosis triggered by loperamide."
PMID 37863323
"Overall, these findings demonstrated that loperamide induced autophagy and apoptosis through the ROS-mediated JNK pathway in bladder cancer cells."
PMID 37863323
"Our results suggest that the strategy of combining loperamide with autophagy inhibitor CQ may provide a therapeutic option for the treatment of bladder cancer."
mTORPMID 39744815
"Our results reveal novel functions of M1 poly-Ub during lysosomal homeostasis, LMP and degradation of damaged lysosomes, with important implications for NFKB signaling, inflammation and cell death.<b>Abbreviation</b>: ATG: autophagy related; BafA1: bafilomycin A<sub>1</sub>; CALCOCO2/NDP52: calcium binding and coiled-coil domain 2; CRISPR: clustered regularly interspaced short palindromic…"
recorded 2025-01-02 · last checked 2026-09-04
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