Carbenoxolone

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Carbenoxolone

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Carbenoxolone

Property Description
Active ingredient Carbenoxolone (or Carbenoxolone disodium)
Form Tablets, capsules, oral gels, and mouthwash
Pharmacological class Triterpenoid derivative, Anti-Ulcer Agent
Common use Supporting the healing of digestive tract linings
Origin Synthetic derivative of glycyrrhetinic acid

What Type of Medicine is Carbenoxolone?

Carbenoxolone is a pharmaceutical substance classified as a Triterpenoid derivative and an Anti-Ulcer Agent, derived synthetically from glycyrrhetinic acid. The drug’s active ingredient is Carbenoxolone, which is structurally related to glycyrrhizin, the principal compound found in natural liquorice root, but is a purified and standardized synthetic derivative. Carbenoxolone is recognized as having a specific action of modulating aldosterone metabolism, differentiating it from simple antacids by targeting mucosal integrity.

Composition, Forms, and General Purpose

The general purpose of Carbenoxolone is to provide mucosal protection and support the integrity of compromised tissue linings in the digestive tract. It promotes the production of protective mucus while simultaneously providing a localized anti-inflammatory effect. The use of the compound in supporting the healing of gastric ulcers is a basis for its clinical relevance. For application, Carbenoxolone is available in forms suitable for oral administration, such as tablets and capsules, and for topical administration as specialized oral gels or mouthwash preparations, allowing targeted delivery to mucosal surfaces throughout the alimentary canal.

Regulatory References

  1. National Library of Medicine, MeSH: Carbenoxolone

What side effects are possible with Carbenoxolone?

Possible Side Effects and Safety Information

This section outlines the adverse reactions and safety restrictions for Carbenoxolone as documented in official government regulatory sources.

Documented Adverse Reactions

The most commonly reported side effects are directly related to the medicine’s impact on fluid and electrolyte balance, specifically mimicking the effects of mineralocorticoids. Safety information is typically classified by how often an effect occurs or which body system is involved.

Classification Examples of Adverse Reactions
Common Sodium and water retention (leading to oedema/swelling), Hypertension (high blood pressure), Hypokalaemia (low potassium levels), Headache, Muscle weakness (secondary to hypokalaemia).
System-Organ Classes Metabolism and nutrition disorders, Vascular disorders, Cardiac disorders, Musculoskeletal and connective tissue disorders.

Clinically Significant and Serious Reactions

Serious adverse events are predominantly linked to severe disturbances in electrolytes:

  • Severe Hypokalaemia: Low potassium levels can become severe, potentially leading to dangerous changes in heart rhythm (cardiac arrhythmias) or muscle paralysis.
  • Congestive Cardiac Failure: Risk is heightened, particularly in susceptible individuals, due to the significant fluid and sodium retention caused by the medicine.

Safety Restrictions and Monitoring

Official regulatory documents place strict restrictions on Carbenoxolone use and require specific monitoring measures:

  • Contraindications: The medicine must not be used in patients with pre-existing conditions such as cardiac failure, severe hypertension, or hypokalaemia.
  • High-Risk Groups: Specific warnings are noted for elderly patients, who are considered particularly susceptible to electrolyte imbalances, and the medicine is generally contraindicated in children under 3 years old.
  • Monitoring: Regular monitoring of serum potassium levels and blood pressure is a required component of treatment to manage the major documented risks.

Overdose and Emergency Response

Overdose: When to Seek Help

Official regulatory documents indicate that the primary risks associated with Carbenoxolone over-exposure are directly linked to an exaggeration of its known systemic side effects. The most critical manifestation involves severe electrolyte disturbance.

Documented Overdose Manifestations

Physiological Systems Affected Primary Manifestation
Electrolyte Balance Sodium retention and Hypokalaemia (low potassium levels).
Population-Specific Risk Manifestations are more frequent and pronounced particularly in the elderly.

Emergency Actions and Regulatory Stance

No specific data detailing acute symptoms or dedicated treatment protocols for Carbenoxolone overdosage is available in the official prescribing information for certain formulations (e.g., topical preparations). Treatment, when data is available, is generally supportive and focuses on addressing the profound electrolyte disturbances.

The official documentation highlights that the clinical effects linked to over-exposure—specifically severe hypokalaemia—are serious health risks, which implicitly require prompt medical evaluation. The presence of any signs related to severe electrolyte imbalance following excessive use indicates the need for immediate professional medical attention. Consult a poison control center or seek emergency medical care immediately upon suspicion of overdosage.

Therapeutic Uses of Carbenoxolone

What Carbenoxolone Treats: Main Uses and Benefits


Carbenoxolone is an agent primarily used in situations involving certain distressing symptoms associated with gastrointestinal and oral lesions, notably digestive tract ulcers, especially in the stomach. It is applied across domains where additional symptomatic support is needed, helping to address groups of symptoms that may appear suddenly or intensify over time, such as pain and localized inflammation. The therapeutic domains often involve managing symptoms associated with peptic (gastric and duodenal) ulcers, esophageal ulcers, and mouth ulceration.

This medication is applicable in conditions characterized by periods of heightened symptoms, particularly those involving recurrent or episodic ulcerations. It is relevant when supportive symptom management is appropriate, as it is used to help with managing symptoms that interfere with daily comfort. As a result, it helps patients cope more steadily with difficult episodes.

“It is often used when symptoms intensify and short-term symptomatic assistance is needed for managing symptoms that are linked to organ-specific functional stress.”

Key Focus: Symptomatic support for inflammation and pain linked to ulcers.

Regulatory References

  1. National Institutes of Health MeSH database

Eligibility and Restrictions for Use

Carbenoxolone's official eligibility profile is strictly defined by regulatory documents that impose absolute prohibitions on its use in specific populations. The medicine is contra-indicated in patients with severe, pre-existing organ dysfunction, including severe cardiac impairment, severe renal impairment, or severe hepatic impairment. Use is also officially forbidden for patients with existing hypertension (high blood pressure).

Age-related restrictions designate children under 3 years and elderly patients as contra-indicated populations. Additional prohibitions apply to individuals with certain clinical statuses: the drug is contra-indicated in patients with low serum albumin and those concurrently taking cardiac glycosides. Furthermore, official labeling states that Carbenoxolone is contra-indicated for use during pregnancy and lactation. Only adults and children over 3 years who are free of these specific high-risk conditions are defined as the eligible population.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documentation details the specific interactions that arise from Carbenoxolone's mineralocorticoid-like activity, primarily impacting electrolyte balance and pharmacodynamic response.

Formally Documented Contraindications and Restrictions

Interacting Substance Official Restriction
Cardiac Glycosides (e.g., Digoxin) Formally contraindicated if the patient has pre-existing hypokalaemia or cardiac failure.

Clinically Significant Pharmacodynamic Interactions

Co-administration with several classes of medicine is documented to reinforce or antagonize Carbenoxolone's effects. The combination with Diuretics (thiazide and loop types) and Adrenal Corticosteroids is noted to exacerbate the risk of hypokalaemia and related mineralocorticoid-like effects. Conversely, the use of Spironolactone or Amiloride is associated with a formal antagonism of therapeutic efficacy.

Pharmacokinetic and Population-Specific Notes

Interaction notes include the potential for Chlorpropamide to cause delayed absorption. Regulatory information also specifies that the severity of interaction effects, particularly those related to electrolyte imbalance, is formally heightened in elderly patients and considered more clinically significant in those with severe renal or hepatic impairment.

Mechanism of Action

Carbenoxolone functions as a non-selective inhibitor of 11beta-hydroxysteroid dehydrogenase (11beta-HSD) enzymes, primarily targeting the Type 1 isozyme (11beta-HSD1) and, to a lesser extent, the Type 2 isozyme (11beta-HSD2). In tissues expressing 11beta-HSD2, such as the renal collecting duct and gastrointestinal tract, its inhibitory action blocks the enzyme's conversion of active cortisol to inactive cortisone. This antagonism of 11beta-HSD2 increases the local bioavailability of cortisol, leading to the activation of mineralocorticoid receptors (MR), which have a high affinity for glucocorticoids when 11beta-HSD2 is inhibited. The subsequent MR signaling cascade includes upregulation of the epithelial sodium channel (ENaC) and the Na^+/ K^+-ATPase pump in renal tubules. This downstream effect promotes sodium reabsorption and potassium excretion in the kidney. Carbenoxolone also acts as a non-specific blocker of gap junctions, which are intercellular channels formed by connexin proteins. This interaction modifies direct cell-to-cell communication and electric coupling across multiple tissues.

Dosage and Administration Information

How to Use Carbenoxolone: Administration Guidelines

Carbenoxolone is administered via distinct routes depending on the target site, based on standard clinical parameters that define the dosage, frequency, and duration of use.


Administration Routes and Dosing Patterns

The medication is available for oral use in the form of tablets or capsules, and for topical use as a 2% gel or cream. This dual availability dictates two separate administration protocols. For gastrointestinal applications, the oral route is used with a common adult dosing regimen starting at 100 mg three times daily. For localized oral lesions, a 2% topical formulation is applied directly.


Frequency, Timing, and Duration

Oral use requires divided daily dosing, typically administered two to four times per day, and is prescribed for a defined treatment course, generally spanning four to six weeks. This period reflects the intended duration for the resolution of acute conditions. For the topical gel, application is prescribed four times daily. Instructions for the topical route emphasize that the gel must be applied after meals and at bedtime. This specific timing aims to maximize the duration of contact between the drug and the mucosal lesion, thereby ensuring optimal use of the localized preparation. Topical use is constrained to a shorter duration; if symptoms persist beyond two weeks, the patient should seek reassessment.


Special Administration Constraints

The topical formulation is restricted to oromucosal and cutaneous application only and must not be ingested for a systemic effect. Furthermore, the 2% topical gel is generally limited to use in adults and children over 3 years of age, establishing a clear age-specific constraint on administration. Lower dosages are advised for oral formulations in older adults where appropriate, reflecting population-specific use considerations.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Carbenoxolone


Evidence for Use in Benign Gastric Ulceration

Carbenoxolone was studied for its use in benign gastric ulceration, which relates to ulcers located in the stomach lining. Studies that explored this application include short-term Randomized Controlled Trials (RCTs) and double-blind trials, as well as comparative clinical trials. Research examined measurements of ulcer healing rates, assessed using endoscopy, and monitored patient-reported outcomes describing perceived discomfort and symptoms related to physical discomfort. These studies primarily applied to adult outpatients who had endoscopically confirmed ulcers.

Studies focusing on episodes where symptoms become more noticeable reported findings that included measurements of ulcer healing, with patterns observed in the studied groups. The findings help contextualize how patients reported their experience when the compound was studied for conditions characterized by fluctuating manifestations. Comparative evidence is lacking against some contemporary anti-ulcer treatments.

Evidence for Use in Other Peptic Ulcers and Oral Lesions

Carbenoxolone was also evaluated in studies exploring its application in other areas of the digestive tract and mouth. Research examined outcomes related to physical discomfort, such as the time required for the lesion or ulcer to heal, and the reduction in reported localized pain. Findings were observed in some studies for duodenal ulcers, but the volume of evidence for this indication is less extensive than research for gastric ulcers.

Long-Term Studies and Follow-up Duration

When Carbenoxolone was evaluated in studies for ulcer healing, the follow-up durations were limited, typically focused on a short-term period of 4 to 6 weeks. Research explores short-term symptom changes, but long-term effects are not fully established. There is limited information for long-term outcomes, such as the durability of the healing effect or the persistence of recurrence rates beyond the short observation window.

What Is Still Uncertain About Carbenoxolone Research

Data for certain groups remain insufficient; research for populations such as children or those with various comorbid conditions is limited. The sample sizes were modest in many of the studies exploring healing patterns, and the age of the key research means that the study results reflect the specific conditions under which they were conducted. Furthermore, comparative evidence is lacking against some newer therapies. Evidence highlights what is known—and what is still uncertain—meaning research provides context but not individual predictions.

Frequently Asked Questions (FAQ)

Common questions about Carbenoxolone (FAQ)


Q: Can Carbenoxolone be given to children?

Official product information contra-indicates the use of the medicine in children under 3 years old. For the topical gel formulation, official documents describe its use for adults and children over 3 years of age. Eligibility is addressed by official regulatory documents, which note specific age and condition-based restrictions.

Q: What should I do if I experience muscle weakness while taking Carbenoxolone?

Muscle weakness is a documented common side effect associated with low potassium levels (hypokalaemia) caused by the medicine. Regulatory documents mention that persistent symptoms or changes in health are typically reviewed by a healthcare professional.

Q: Does Carbenoxolone need to be taken before or after food?

The timing for using the medicine varies by the form used. For the oral tablet formulation, some product information describes use before meals. For the topical gel, official instructions require that it be applied after meals and again at bedtime.

Q: Is it true that Carbenoxolone is derived from licorice?

Carbenoxolone is a synthetic chemical derivative of glycyrrhetinic acid, which is a compound found in natural licorice root. It is described in authoritative sources as being structurally related to glycyrrhizin, the primary compound found in licorice.

Q: What is the risk of Carbenoxolone causing heart problems?

Official documentation indicates a risk of serious adverse reactions, which include congestive cardiac failure. This risk is primarily linked to the effect of sodium and water retention caused by the medicine, which increases fluid volume.

Q: Why does Carbenoxolone sometimes cause fluid retention?

Carbenoxolone’s effects include causing the kidney to reabsorb sodium. This physiological change, in turn, can cause the body to retain sodium and water, which is a commonly reported adverse reaction.

Q: Is Carbenoxolone considered a steroid?

Carbenoxolone is chemically classified as a triterpenoid derivative and an anti-ulcer agent. While official sources describe it as having a steroid-like chemical structure and exhibiting mineralocorticoid-like activity, it is not classified as a standard corticosteroid medicine.

Q: Are there different strengths or formulations of Carbenoxolone available?

Yes, Carbenoxolone has been available in various forms depending on the target site. These include forms for oral administration, such as tablets and capsules (commonly 100 mg), and specialized preparations for topical use, such as oral gels (e.g., 2% concentration) or mouthwash.

Q: Is Carbenoxolone used for acid reflux (GERD)?

Authoritative databases indicate that Carbenoxolone is used to treat conditions characterized by damage to the digestive tract lining. These indications include peptic ulcer and gastroesophageal reflux disease (GERD).

Q: What does the research say about Carbenoxolone and esophageal ulcers?

Authoritative sources and indication documentation describe Carbenoxolone as being indicated for various ulcerations and related inflammation in the upper digestive tract, which includes esophageal ulcers.

Q: What is the typical length of time a person uses Carbenoxolone?

According to official product information, the oral medication is prescribed for a defined treatment course. This duration typically spans four to six weeks and is intended for the resolution of acute conditions.

Q: Can I drive or operate machinery while taking Carbenoxolone?

Official product information for the topical gel formulation states that its use is unlikely to result in any impairment of the ability of patients to drive or operate machinery.

How should Carbenoxolone be stored and disposed of?

How to Store and Dispose of Carbenoxolone

Official regulatory documents define specific storage and disposal requirements for carbenoxolone, primarily focusing on maintaining the product's integrity and ensuring safety.


Storage Requirements

Storage Element Official Regulatory Requirement
Temperature Do not store the medicine above 25 C.
Container Seal The cap must be replaced tightly after use (e.g., for oral gel formulations).
Stability Do not use the medicine after the expiry date printed on the packaging.
Child Safety Keep this medicine out of the sight and reach of children.

️ Disposal Instructions

Expired or unused carbenoxolone must not be thrown away via wastewater or general household waste. Disposal must follow mandatory environmental guidelines. You are instructed to ask your pharmacist how to properly discard any medicines you no longer use to help protect the environment.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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