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Bupivacaine

  • 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 Bupivacaine does in the body

Numbing an area of the body for hours rather than for an hour, for surgery, childbirth or a nerve block

Bupivacaine blocks the same sodium gates in nerves that lidocaine blocks, and it blocks them the same way — from the inside of the nerve, in the mouth of the pore. The difference is that it is far greasier and it clings. Once it is on the channel it takes about ten times longer to fall off, so the numbness lasts hours instead of an hour. That same clinginess is the problem when the drug reaches the heart, because heart muscle cells also depend on those gates, and a drug that will not let go between beats accumulates block with every beat.

What happened in people

A 1.0 cm.h improvement in 24-to-72-hour pain AUC from the liposomal formulation, against a pre-specified clinical importance threshold of 2.0 cm.h

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 liposomal bupivacaine gives clinically better analgesia than plain bupivacaine in a nerve block — nine trials say the difference is half of what a patient would notice, and none once one industry trial is removed

Where it acts
Inner pore of the sodium channel, in peripheral nerve axons and — when it reaches the bloodstream — in cardiac ventricular myocytes
Kind of result
Symptoms and quality of life
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 · Y8335394RO · read 2026-08-29

Where each sentence above came from

No recorded sentence describes the change this makes in a way that stands on its own. The page opens with what it is taken for instead, and the recorded explanation follows below.

Shown as the opening line on this page.

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

The four opening statements run to 148 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.

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.

Formulation

A formulation is the exact made-up form a substance comes in.

A picture of it, and where the picture fails

It is like the difference between a whole bean and instant coffee.

Where that stops being true. Coffee tastes different. A formulation can change how much reaches the blood.

What people get wrong. Two products with the same name are assumed to behave the same. They often do not.

The specific composition and physical form of a product, including salt, excipients and release profile.

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.

Area under the curve of pooled 24-to-72-hour rest pain severity scores, against a pre-specified minimal clinically important difference of 2.0 cm.h

The study did not show it

Who was studied
Hussain meta-analysis of perineural liposomal bupivacaine versus non-liposomal local anaesthetic
How many people
619
Study design
Systematic review and meta-analysis of 9 randomised trials
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Improvement of 1.0 cm.h (95% CI 0.5 to 1.6; P=0.003), half the pre-specified threshold for clinical importance; 0.7 cm.h (95% CI -0.1 to 1.5; P=0.100) after excluding one industry-sponsored trial
Repeated elsewhere
Replicated

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. No liposomal bupivacaine side effects were reported in any included trial, which the authors note rather than treat as reassurance: nine trials of 619 patients cannot exclude an uncommon harm.

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

Form and route. Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

Interval reported. 95% CI 0

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

Cumulative pain intensity over 72 hours following surgery

The study did not show it

Who was studied
Hamilton Cochrane review of liposomal bupivacaine infiltration at the surgical site
How many people
1377
Study design
Systematic review of 9 studies
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
No meta-analysis was performed. The review judged there were insufficient data to ensure a clinically meaningful answer and reported narratively instead.
Repeated elsewhere
Unreplicated

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. Four Phase II trials presented only pooled data that could not be used; two studies were at high risk of selective reporting bias; four had fewer than 50 participants per arm.

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

Form and route. Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

Interval reported. Not recorded in this summary

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

Maximum tolerated dose and unbound plasma concentration for central nervous system symptoms, with echocardiographic and electrophysiological change

The study showed what it set out to show

Who was studied
Knudsen volunteer crossover of intravenous ropivacaine, bupivacaine and placebo
How many people
12
Study design
Randomised double-blind three-way crossover in volunteers
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Maximum tolerated unbound plasma concentration twice as high for ropivacaine (P<0.001); bupivacaine widened QRS versus placebo (P<0.001) and versus ropivacaine (P<0.01)
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. Twelve healthy young men infused to the point of definite symptoms. The design deliberately stops short of the cardiac events it is used to reason about, so the cardiotoxicity comparison is an extrapolation from sub-toxic endpoints.

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

Form and route. Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

Interval reported. Not recorded in this summary

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

Median effective local analgesic concentration in 20 mL for first-stage labour epidural analgesia

The study showed what it set out to show

Who was studied
Polley minimum local analgesic concentration study of epidural ropivacaine versus bupivacaine in labour
How many people
73
Study design
Randomised double-blind up-down sequential allocation study
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Ropivacaine 0.111% (95% CI 0.100 to 0.122) versus bupivacaine 0.067% (95% CI 0.052 to 0.082); potency ratio 0.6 (95% CI 0.49 to 0.74)
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 method measures potency for first-stage labour analgesia in a 20 mL epidural volume. Extending the ratio to surgical anaesthesia, to other blocks or to toxicity is an extrapolation the study does not make.

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

Form and route. Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

Interval reported. 95% CI 0

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

What we know
RNAWiki holds 4 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

    Bupivacaine

    What a person takes: Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block.

    The measurement behind this step

    Every presentation is the same molecule and the route decides what it does. Preservative-free formulations exist because methylparaben is not acceptable in the intrathecal or epidural space. Hyperbaric presentations add dextrose so that the solution sinks in cerebrospinal fluid and the block can be positioned by patient posture. Epinephrine-containing presentations slow systemic absorption and also act as an intravascular test: a sudden rise in heart rate after a test dose suggests the needle is in a vessel. The liposomal suspension is a multivesicular lipid particle that releases bupivacaine over roughly 72 hours, and it is a different product with a different price and its own evidence base.

  2. Getting in

    Deposited next to the nerve and left there

    The injection is placed around a nerve, into the epidural space or into the spinal fluid. From there it has to reach the nerve fibres by diffusion alone.

    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

    Very high lipid solubility means a large fraction partitions into local fat and myelin rather than being carried away in blood, which is why the block outlasts the plasma half-life by hours. Systemic absorption is fastest from intercostal and interpleural sites and slowest from subcutaneous infiltration, and the resulting peak plasma concentration for a fixed dose can differ several-fold by site.

  3. Reaching the cell

    It crosses into the axon and protonates

    Only the uncharged form gets through the nerve membrane. Inside, it picks up a proton, and the charged form is the one that blocks the gate.

    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 piperidine nitrogen has a pKa near 8.1, so a smaller uncharged fraction is available at physiological pH than for lidocaine, which contributes to a slower onset. The butyl chain raises the octanol-water partition coefficient about thirtyfold over mepivacaine, and lipid solubility is the property that tracks both potency and duration across this class.

  4. What it acts on

    It binds the inner pore and does not let go

    The blocking site is the same inner mouth of the channel that lidocaine uses. The difference is entirely in how long the drug stays there once it arrives.

    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

    Binding is strongly state-dependent, with a dissociation constant of 9 x 10^-7 M for the inactivated cardiac channel and much weaker affinity for the rested and activated states. Bound channels do not conduct and their inactivation curve shifts about 33 mV negative, so at any given membrane potential a larger fraction of the population sits unavailable.

  5. The change it makes

    In a heart, the block accumulates beat by beat

    Between heartbeats the drug is supposed to fall off. Bupivacaine falls off so slowly that at a normal heart rate the next beat arrives before it has cleared, and the block deepens with every beat.

    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

    Diastolic recovery has a time constant of 1,557 +/- 304 ms, longer than the diastolic interval at any rate between 60 and 150 beats per minute, so block accumulates rather than resetting. Reducing heart rate, hyperpolarising the membrane and shortening the action potential all reduce block, but Clarkson and Hondeghem found that varying them across clinically achievable ranges did not markedly change the effect.

  6. What that does for a person

    In a nerve, the same stickiness is the benefit

    A nerve is not firing eighty times a minute waiting for the drug to clear. The same slow release that is dangerous in the heart is exactly what gives six to twelve hours of numbness from one injection.

    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

    Conduction fails first in small unmyelinated C and small myelinated A-delta fibres, then in larger A-beta and A-alpha fibres, producing the labelled sequence of pain, then temperature, then touch, then proprioception, then skeletal muscle tone. Differential block is more pronounced at low concentrations, which is the pharmacological basis for a labour epidural that abolishes pain while leaving some motor function.

  7. What that does for a person

    It washes out, and if it has reached the heart that takes longer than it should

    A nerve block simply wears off. A cardiac arrest caused by this drug is different: the heart has to unbind it, and that is the part that has historically been hard.

    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

    Elimination is hepatic, principally by CYP3A4 N-dealkylation to pipecolylxylidide, with an elimination half-life around 2.7 hours in adults and considerably longer in neonates. Recovery of cardiac conduction after a toxic exposure is governed by unbinding rather than by clearance, which is the pharmacological rationale for intravenous lipid emulsion as a rescue: it is proposed to act as a circulating lipid sink, and that proposal is a mechanistic inference supported by animal work and human case reports rather than by a randomised trial in people.

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 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.

  • Anyone having an epidural in labour, a spinal for a caesarean section or a joint replacement, a nerve block for shoulder or knee surgery, or local infiltration at the end of an operation. It is on the WHO Model List of Essential Medicines.

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: “Safety and effectiveness of bupivacaine liposome injectable suspension have not been established to produce postsurgical: Local analgesia via infiltration in pediatric patients aged less than 6 years old.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • On older people, the label states: “Of the total number of patients in the bupivacaine liposome injectable suspension local infiltration clinical studies (N=823), 171 patients were greater than or equal to 65 years of age and 47 patients were greater than or equal to 75 years of age.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary There are no studies conducted with bupivacaine liposome injectable suspension in pregnant women.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • On people who are breastfeeding, the label states: “Risk Summary Limited published literature reports that bupivacaine and its metabolite, pipecoloxylidide, are present in human milk at low levels.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • On people with reduced liver function, the label states: “Amide-type local anesthetics, such as bupivacaine, are metabolized by the liver.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • On people with reduced kidney function, the label states: “Bupivacaine is known to be substantially excreted by the kidney, and the risk of adverse reactions to bupivacaine liposome injectable suspension may be greater in patients with renal impairment than in patients with normal renal function.”

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

Where the result stopped carrying

  • The 0.75% concentration was removed from obstetric use in the United States after reports of cardiac arrest occurring simultaneously with, rather than after, neurological toxicity
  • Perineural liposomal bupivacaine failed to reach its pre-specified minimal clinically important difference across nine randomised trials, and lost statistical significance entirely when one industry-sponsored trial was excluded
  • Every secondary outcome of that meta-analysis — analgesic consumption, time to first request, opioid side effects, satisfaction, length of stay, functional recovery — was negative
  • 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.

A different form was studied

The studied form is not the form on the shelf.

On this record: This record is linked to 1 related forms. Evidence does not carry across all of them.

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)
It was studied for a different goal
The studies measured something else entirely. 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

Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

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 presentation is the same molecule and the route decides what it does. Preservative-free formulations exist because methylparaben is not acceptable in the intrathecal or epidural space. Hyperbaric presentations add dextrose so that the solution sinks in cerebrospinal fluid and the block can be positioned by patient posture. Epinephrine-containing presentations slow systemic absorption and also act as an intravascular test: a sudden rise in heart rate after a test dose suggests the needle is in a vessel. The liposomal suspension is a multivesicular lipid particle that releases bupivacaine over roughly 72 hours, and it is a different product with a different price and its own evidence base.

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

The defining risk is systemic toxicity from inadvertent intravascular injection, and it is more dangerous with this molecule than with any other in routine use because cardiovascular collapse can occur without the usual neurological warning and because the resulting conduction block is slow to reverse. Intravenous lipid emulsion is stocked wherever large-volume blocks are performed for this reason. The 0.75% concentration is not used for obstetric anaesthesia in the United States. Bupivacaine is not for intravenous regional anaesthesia. As with the whole class, the label carries a methaemoglobinaemia warning. None of this is dosing guidance and no dosing guidance appears anywhere on this page.

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

Sterile injection for infiltration, peripheral nerve block, epidural and caudal use; preservative-free presentations for intrathecal use, some with dextrose for hyperbaric spinal anaesthesia; some presentations co-formulated with epinephrine; a separate patented liposomal suspension for infiltration and interscalene block

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

Preservative-free formulations exist because methylparaben is not acceptable in the intrathecal or epidural space. Hyperbaric presentations add dextrose so that the solution sinks in cerebrospinal fluid and the block can be positioned by patient posture. Epinephrine-containing presentations slow systemic absorption and also act as an intravascular test: a sudden rise in heart rate after a test dose suggests the needle is in a vessel. The liposomal suspension is a multivesicular lipid particle that releases bupivacaine over roughly 72 hours, and it is a different product with a different price and its own evidence base.

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

  • 173 products list this as an active ingredient in the United States drug directory. 144 of them contain it and nothing else.

    FDA National Drug Code directory · 0409-7535 · read 2026-08-29

  • They are sold as injection, injection, solution, injection, suspension, liposomal, liquid, powder and solution, taken epidural, infiltration, intracaudal and perineural.

    FDA National Drug Code directory · 0409-7535 · read 2026-08-29

  • The regulator's established pharmacologic class for it is amide local anesthetic [epc], amides [cs] and local anesthesia [pe].

    FDA National Drug Code directory · 0409-7535 · read 2026-08-29

  • 66 published labels name it as an active ingredient. 52 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 0e6a55f0-5107-4ea9-9ee1-5c6c09bbe4a6 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 0e6a55f0-5107-4ea9-9ee1-5c6c09bbe4a6 · read 2026-08-29

  • Bupivacaine is infiltration at 3., recorded as fda label in effect 2024-07-09 in the United States.

    US prescribing information · 0af296bb-1599-4b35-b66b-994924d3e898 · read 2026-08-30

  • Recorded price in US: 0.04792–0.08596 USD per one millilitre, across 12 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.

Names and forms linked to this record

  • Stereoisomer of

    Levobupivacaine

    Evidence on this page does not automatically apply to this one.

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.

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 Bupivacaine 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 liposomal bupivacaine gives clinically better analgesia than plain bupivacaine in a nerve block — nine trials say the difference is half of what a patient would notice, and none once one industry trial is removed

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 wound infiltration with the liposomal formulation is evidence-based — Cochrane could not pool the data at all

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 local anaesthetic toxicity gives neurological warning before cardiac collapse, a rule inherited from lidocaine that Albright showed does not hold here

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 ropivacaine safety margin measured at equal milligram doses transfers to equal analgesic doses; the potency ratio of 0.6 says it does not transfer intact

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 lipid emulsion rescue is proven in humans — it rests on animal experiments and case reports, and no randomised human trial exists or is likely to

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 Bupivacaine 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.

Fast-in, slow-out: the off-rate from the cardiac channel is ten times lidocaine's
In plain words
Both drugs block the sodium gate during a heartbeat. Lidocaine falls off again in about a sixth of a second; bupivacaine takes about a second and a half. At a normal heart rate there is not enough time between beats for it to clear, so block builds up.
What was measured
Time constant of diastolic recovery from sodium channel block, and dissociation constant for the inactivated state
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Clarkson and Hondeghem compared bupivacaine and lidocaine on guinea pig ventricular muscle under single sucrose-gap voltage clamp, using maximum upstroke velocity as an index of peak sodium current. Bupivacaine had low affinity for rested and activated channels but bound the inactivated channel with a dissociation constant of 9 x 10^-7 M, and shifted the voltage dependence of inactivation about 33 mV negative. Above 0.2 micrograms per mL a substantial fraction of channels blocked during the action potential, while diastolic recovery proceeded with a time constant of 1,557 +/- 304 ms (n=8). Lidocaine at 5 to 10 micrograms per mL blocked a comparable fraction during the action potential but recovered with a time constant of 153.8 +/- 51.2 ms (n=4). Bupivacaine therefore accumulates block across the range of 60 to 150 beats per minute and lidocaine does not, which the authors offered as the mechanistic explanation for why bupivacaine cardiac arrest is both severe and hard to reverse.
Source
Clarkson CW, Hondeghem LM. Anesthesiology 1985;62:396-405 (PMID 2580463)
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 0.75% concentration was withdrawn from obstetric use after Albright's editorial
In plain words
In 1979 an anaesthetist published six cases in which patients given a long-acting local anaesthetic had cardiac arrest almost at the same moment as the seizure, rather than afterwards. The strongest concentration was withdrawn from use in childbirth.
What was measured
That local anaesthetic systemic toxicity always announces itself neurologically before it becomes cardiac — true for lidocaine, false for bupivacaine, and believed for both until 1979
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Albright described cardiac arrest following regional anaesthesia with etidocaine or bupivacaine, in which cardiovascular collapse occurred simultaneously with, rather than following, central nervous system toxicity — breaking the assumption inherited from lidocaine that seizures give warning before the heart is affected. The FDA subsequently removed the 0.75% concentration from obstetric use. This is a genuine change of mind rather than a refinement: the class-wide safety model, in which local anaesthetic toxicity progresses through predictable neurological stages, was correct for lidocaine and wrong for bupivacaine, and it was wrong because of the off-rate measured six years later by Clarkson and Hondeghem.
Source
Albright GA. Cardiac arrest following regional anesthesia with etidocaine or bupivacaine. Anesthesiology 1979;51:285-287
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
Liposomal bupivacaine in nerve blocks: statistically significant, clinically not
In plain words
The slow-release version is sold as lasting longer in a nerve block. Pooling nine randomised trials, it beat ordinary bupivacaine by half of what the researchers had defined in advance as the smallest difference a patient would notice — and once one industry-funded trial was removed, it did not beat it at all.
What was measured
Difference in area under the curve of 24-to-72-hour rest pain scores against a pre-specified minimal clinically important difference of 2.0 cm.h
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
Hussain and colleagues pooled nine randomised trials with 619 patients comparing perineural liposomal bupivacaine with non-liposomal local anaesthetic for peripheral nerve block. The primary outcome was the area under the curve of 24-to-72-hour rest pain scores, interpreted against a pre-specified minimal clinically important difference of 2.0 cm.h. Pooled AUC pain scores were 7.6 +/- 4.9 cm.h for non-liposomal and 6.6 +/- 4.6 cm.h for liposomal, an improvement of 1.0 cm.h (95% CI 0.5 to 1.6; P=0.003) — half the threshold for clinical importance. Excluding a single industry-sponsored trial rendered the difference non-significant at 0.7 cm.h (95% CI -0.1 to 1.5; P=0.100). No secondary outcome favoured the liposomal product: not analgesic consumption, not time to first analgesic request, not opioid side effects, not patient satisfaction, not length of stay, not functional recovery. The authors concluded that high-quality evidence does not support its use over plain bupivacaine for peripheral nerve blocks.
Source
Hussain N, Brull R, Sheehy B, et al. Anesthesiology 2021;134:147-164
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 infiltration evidence was too thin for Cochrane to pool at all
In plain words
Injected into the wound rather than around a nerve, the slow-release version has been studied nine times. Cochrane could not combine the results into a meaningful answer, and four of the trials were too small to trust.
What was measured
That wound infiltration with liposomal bupivacaine is an evidence-based alternative to plain bupivacaine — an inference the systematic review could not evaluate, let alone support
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Hamilton and colleagues identified nine studies with 1,377 participants of liposomal bupivacaine infiltrated at the surgical site. Four were Phase II dose-escalating or de-escalating trials whose pooled data could not be used. Of the five remaining parallel-arm studies with 965 participants, two were placebo-controlled and three used bupivacaine hydrochloride as the control. The review planned a meta-analysis and a summary-of-findings table and abandoned both, stating there were insufficient data to ensure a clinically meaningful answer and presenting narrative summaries instead. Two studies were at high risk of selective reporting bias and four at high risk of bias from size, with fewer than 50 participants per arm. Where a difference against placebo was reported for cumulative 72-hour pain, it came from a single study graded very low quality.
Source
Hamilton TW, Athanassoglou V, Mellon S, et al. Cochrane Database Syst Rev 2017;2:CD011419
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
Ropivacaine tolerates twice the free plasma concentration before symptoms appear
In plain words
Twelve volunteers were infused with both drugs on separate days and asked to say when they felt the first definite symptoms. They could tolerate about twice as much unbound ropivacaine in the blood as unbound bupivacaine, and only bupivacaine widened the electrical complex on their ECG.
What was measured
Maximum tolerated unbound arterial plasma concentration, QRS width and left ventricular function during controlled intravenous infusion
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Knudsen and colleagues ran a randomised double-blind crossover in 12 volunteers already familiar with the central nervous system effects of lignocaine, infusing ropivacaine, bupivacaine or placebo at 10 mg per minute to the point of definite symptoms. The maximum tolerated dose was higher for ropivacaine in nine of the 12 subjects, with 95% confidence limits on the mean difference of -30 to 7 mg. The maximum tolerated unbound arterial plasma concentration was twice as high for ropivacaine (P<0.001), with an apparent CNS toxicity threshold near 0.6 mg/L free ropivacaine against 0.3 mg/L free bupivacaine. Muscular twitching was more frequent after bupivacaine (P<0.05) and symptoms resolved faster after ropivacaine (P<0.05). Bupivacaine widened the QRS complex against both placebo (P<0.001) and ropivacaine (P<0.01), and depressed both systolic and diastolic left ventricular function, where ropivacaine depressed systolic function only. This is a direct human measurement of the safety margin, in volunteers, at the concentrations that matter.
Source
Knudsen K, Beckman Suurkula M, Blomberg S, Sjovall J, Edvardsson N. Br J Anaesth 1997;78:507-514
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
Part of ropivacaine's safety margin is that it is a weaker drug
In plain words
Comparing the two by the milligram makes the newer one look safer. Measured properly, it takes about 1.7 times as much ropivacaine to produce the same pain relief, so a milligram-for-milligram safety comparison is not a fair one.
What was measured
That ropivacaine is safer than bupivacaine by the ratio seen in equal-milligram toxicity studies — an inference that ignores a measured potency ratio of 0.6
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
Polley and colleagues determined minimum local analgesic concentration by up-down sequential allocation in 73 labouring women at 7 cm dilation or less, giving 20 mL of epidural test solution and defining effectiveness as a visual analogue score of 10 mm or less within 30 minutes. The minimum local analgesic concentration was 0.111% weight/volume for ropivacaine (95% CI 0.100 to 0.122) and 0.067% for bupivacaine (95% CI 0.052 to 0.082), a potency ratio of 0.6 (95% CI 0.49 to 0.74). No difference in motor effects was seen. The toxicity comparisons that established ropivacaine's reputation, including Scott 1989 and Knudsen 1997, infused equal milligram doses of the two drugs. This audit is not a claim that ropivacaine has no safety advantage — Knudsen measured a real one in unbound plasma concentration — but that the size of the advantage quoted from equal-milligram studies is inflated by roughly the potency ratio, and the therapeutic index is the number that should be compared.
Source
Polley LS, Columb MO, Naughton NN, Wagner DS, van de Ven CJ. Anesthesiology 1999;90:944-950
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

  • 46 documents were read for this substance.

    RNAWiki source record

  • 42 of them state the same halfLife, and they agree.

    RNAWiki source record

  • 44 of them state the same proteinBinding, and they agree.

    RNAWiki source record

Where else this substance is registered

FDA substance identifier (UNII)
Y8335394RO
RxNorm concept
1191508

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

  • Passed

    Safety mode resolved

    Suppression classes recorded: S6.

  • 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

  • 52 approved applications cover products containing this substance. The earliest was NDA016964, approved 19721003 to HOSPIRA.

    Drugs@FDA application register · NDA016964 · read 2026-08-29

  • Marketing status on the register: discontinued and prescription.

    Drugs@FDA application register · NDA016964 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 19790201.

    FDA National Drug Code directory · 0409-7535 · 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 long-acting sodium channel blocker whose defining measurement is not an analgesia score but an unbinding rate — it leaves the cardiac sodium channel with a time constant of 1,557 milliseconds against lidocaine's 154, which is why one injection numbs for hours and why an accidental intravascular dose can stop a heart that is then hard to restart.

Recorded evidence blocks (9)

On the Bupivacaine label: indicated for what?


"Bupivacaine hydrochloride injection is indicated in adults for the production of local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and for obstetrical procedures. Specific concentrations and presentations of bupivacaine hydrochloride…": indications and usage on Bupivacaine's label. DailyMed label · ee3b5bbe-4013-4682-b6ee-db86e7788077 · 2026-07-20

1144 registered trials of Bupivacaine — at which phases?


Registered studies posting no result
836 of 1144

1144 registered studies of Bupivacaine: 431 phase4, 340 na, 150 phase3, 146 phase2, 63 phase1, 33 na or unstated, 29 early phase1. CLINICALTRIALS_SNAPSHOT · 2026-09-01

5575 with a PubMed record

Show the evidence
  • phase4
    431
  • na
    340
  • phase3
    150
  • phase2
    146
  • phase1
    63
  • na or unstated
    33
10 more recorded rows
  • early phase1
    29
  • completed
    686
  • unknown
    173
  • terminated
    96
  • recruiting
    60
  • withdrawn
    60
  • not yet recruiting
    33
  • active not recruiting
    19
  • enrolling by invitation
    15
  • suspended
    2

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

148 of Bupivacaine's trials stopped: safety, futility/efficacy, accrual/recruitment, funding/business, sponsor decision unspecified, other?


safety (2), futility/efficacy (8), accrual/recruitment (52), funding/business (9), sponsor decision unspecified (2) and other (75): Bupivacaine's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"Bupivacaine has recently been shown to inhibit osteoclast formation in vitro."; 148 of 1144 registered studies

Show the evidence

Trial

  • NCT00314457
    terminated; "Bupivacaine has recently been shown to inhibit osteoclast formation in vitro."
  • NCT00519584
    terminated; "Collected study data was not usable due to process miscommunications"
  • NCT00557843
    withdrawn; "No patients enrolled"
  • NCT00801138
    terminated; "A strong primary outcome crosses the efficacy boundary at the interim analysis"
  • NCT00813111
    terminated; "Sponsor decision, unrelated to safety"
  • NCT00871442
    withdrawn; "would not substantially add to existing contributions in the literature"
14 further recorded trials
  • NCT00930072
    terminated; "Poor Enrollment"
  • NCT01005459
    terminated; "feasibility /drug availability issues - No study drug sources available"
  • NCT01219062
    terminated; "Surgeon team were not happy with the study protocol, the periarticular injection of local anesthetics"
  • NCT01294098
    terminated; "Patients were not willing to be randomized and therefore recruitment could not continue."
  • NCT01303107
    withdrawn; "The Sponsor has no interest in continuing the study."
  • NCT01308047
    withdrawn; "The Sponsor has no interest in continuing the study."
  • NCT01394523
    terminated; "Interim power analysis was prohibitive to continuing the study"
  • NCT01507233
    terminated; "Slow enrollment."
  • NCT01550302
    terminated; "Unable to continue enrollment due to lack of resources (research coordinator no longer available)."
  • NCT01565512
    withdrawn; "Lack of funding, PI left the institution, poor enrollment"
  • NCT01575028
    terminated; "The study was allowed to expire due to changes in standard care for the patient population within the NCH institution."
  • NCT01584947
    terminated; "Because of a very slow patient recruitment."
  • NCT01615939
    terminated; "The study has been terminiated due to minimal subject recruitment"
  • NCT01688362
    terminated; "Did not meet target enrollment deadlines."

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

Human studies of Bupivacaine used Marcaine 0.25% with epinephrine 1:200,000 — over how long?


studies of Bupivacaine used the recorded amount. ClinicalTrials.gov · 2026-09-01

20 recorded entries; human; intrathecal; also "Marcaine 0.25% with epinephrine 1:200,000", "Bupivacaine HCl (Marcaine 0.25% with epinephrine 1:200,000)", "Marcaine 0.5% with epinephrine"

Show the evidence

human

  • NCT00485433
    Marcaine 0.25% with epinephrine 1:200,000
  • NCT00485693
    Bupivacaine HCl (Marcaine 0.25% with epinephrine 1:200,000)
  • NCT00813111
    Marcaine 0.5% with epinephrine
  • NCT00895843
    Marcain 0.5% with 1 in 200,000 epinephrine
  • NCT00993746
    Bupivacaine 30 ml
  • NCT01126593
    0.5% bupivacaine
14 more recorded rows
  • human NCT01147146
    bupivacaine 8-10mg
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 6 mg with 100 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 7 mg with 100 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 8 mg with 100 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 9 mg with 100 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 10 mg with 100 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 11 mg with epinephrine 100 mcg
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 6 mg with 200 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 7 mg with 200 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 8 mg with 200 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 9 mg with 200 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 10 mg with 200 mcg of epinephrine
  • human NCT01264575
    intrathecal; intrathecal bupivacaine 11 mg with 200 mcg of epinephrine
  • human NCT01303731
    Marcaine Spinal 0.5% Heavy

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

Bupivacaine's half-life is 2.7 hours — which schedules were studied?


2.7 hours, the half-life Bupivacaine's label states: "Elimination The half-life of bupivacaine in adults is 2.7 hours." DailyMed label · ee3b5bbe-4013-4682-b6ee-db86e7788077 · 2026-07-20

Show the evidence
  • half life pharmacokinetics
    2.7 hours; Elimination The half-life of bupivacaine in adults is 2.7 hours.
  • metabolism pharmacokinetics
    Metabolism Amide-type local anesthetics such as bupivacaine are metabolized primarily in the liver via conjugation with glucuronic acid.

recorded 2026-07-20 · last checked 2026-09-04

Which 392 trials of Bupivacaine posted no result?


Posted no result
392 of 392 completed trials
Registrations
NCT00001088, NCT00358280, NCT00450099, NCT00485667, NCT00472134 and NCT00508976, and 386 more
Completion dates
oldest 2001-02; newest 2024-09-01
Show the evidence

Trial

  • NCT00001088
    2001-02
  • NCT00358280
    2006-09
  • NCT00450099
    2007-08
  • NCT00485667
    2007-08
  • NCT00472134
    2007-12
  • NCT00508976
    2008-04
14 further recorded trials
  • NCT00921102
    2008-05
  • NCT00500565
    2008-06
  • NCT02343432
    2008-09
  • NCT00405262
    2008-10
  • NCT00806806
    2009-02
  • NCT00795223
    2009-05
  • NCT00845962
    2009-07
  • NCT00808327
    2009-08
  • NCT00672347
    2009-09
  • NCT01090882
    2009-10
  • NCT01040234
    2010-01
  • NCT01528722
    2010-01
  • NCT00836134
    2010-06
  • NCT01377415
    2010-06

At the median, Bupivacaine's trials enrolled 64 people — anything larger?


Median enrolment
64
Largest enrolment
22435
Registered trials counted
1139

What do 1189 spontaneous reports say about Bupivacaine — 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.

Bupivacaine appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1189 reaction mentions were counted: hypotension 260; pain 249; hypoaesthesia 123; anaesthetic complication 94. FAERS via Open Targets · CHEMBL1098 · 2026-06-24

Show the evidence
  • hypotension
    260
  • pain
    249
  • hypoaesthesia
    123
  • anaesthetic complication
    94
  • drug withdrawal syndrome
    93
  • muscular weakness
    85
4 more recorded rows
  • bradycardia
    82
  • premature baby
    78
  • labelled drug-drug interaction medication error
    72
  • cardiac arrest
    53

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

Which 10 reactions does Bupivacaine's label not list?


anaesthetic complication, bradycardia and cardiac arrest and 7 more reported for Bupivacaine, absent from its label. FAERS via Open Targets · CHEMBL1098 · 2026-06-24

2 label terms; 10 reported and unlisted; ee3b5bbe-4013-4682-b6ee-db86e7788077

Show the evidence
  • anaesthetic complication
    count not stated
  • bradycardia
    count not stated
  • cardiac arrest
    count not stated
  • drug withdrawal syndrome
    count not stated
  • hypoaesthesia
    count not stated
  • hypotension
    count not stated
4 more recorded rows
  • labelled drug-drug interaction medication error
    count not stated
  • muscular weakness
    count not stated
  • pain
    count not stated
  • premature baby
    count not stated

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

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL1098
PubChem CID
117963
CAS number
27262-45-9
RxCUI
1191508
InChIKey
LEBVLXFERQHONN-UHFFFAOYSA-N

Relations

Trade name
Anekain, Bupivacaine component of zynrelef, Exparel, Exparel liposomal, Posimir, Marcain, Marcaine
Development code
BR-003, LIQ-865, LIQ865, SKY-0402, SKY0402, AH-2250, LAC-43
Also called
Bucaine, Bupivacaina, Bupivacaine liposome, Liposomal bupivacaine, bupivacain, bupivacaine liposomes, bupivacaine tts, bupivacaine-epinephrine, bupivicaine, bupivocaine, collarx bupivacaine implant, depofoam bupivacaine
Salt form
Ropivacaine hydrochloride impurity, bupivacaine-, bupivacaine liposome injectable suspension, bupivicaine hcl, hydrochloride bupivacaine, Bupivacaine hcl, Bupivacaine hydrochloride component of duocaine, Bupivacaine hydrochloride component of sensorcaine, Bupivacaine hydrochloride hydrate, Bupivacaine hydrochloride kit, Bupivacaine hydrochloride monohydrate, Bupivacaine hydrochloride preservative free, Bupivacaine hydrochloride rs
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

This is a record of evidence. It is not medical advice, and it does not say this substance suits you. Nothing here says any substance on RNAWiki is appropriate for a child.