carbenoxolone, combinations with psycholeptics

A02BX71

Forms & Strengths

Fixed-dose combination tablets containing carbenoxolone sodium and psycholeptic agents (e.g., diazepam, chlordiazepoxide)
Oral gel or paste combinations for mucosal application (varying by regional availability)

Adult Dosing

Peptic ulcer disease / Inflammatory gastrointestinal conditions: 1 to 2 tablets (typically containing 20-50 mg carbenoxolone and low-dose psycholeptic) 3 times daily after meals, short-term course of 4 to 6 weeks
Maximal carbenoxolone dose generally not to exceed 300 mg daily to prevent mineralocorticoid toxicity

Pediatric Dosing

Safety and efficacy in pediatric patients not established; use is generally contraindicated or not recommended in children

Indications

Short-term adjunctive treatment of gastric and duodenal ulcers associated with significant anxiety or emotional distress
Symptomatic management of hyperacidity and inflammatory gastrointestinal disorders refractory to conventional antacids where sedation is concurrently indicated

Mechanism of Action

Carbenoxolone: Inhibits 11-beta-hydroxysteroid dehydrogenase, increasing local cortisol concentrations in the gastric mucosa, which enhances mucus production, mucosal blood flow, and cytoprotection while promoting ulcer healing
Psycholeptic component (e.g., benzodiazepine): Acts on central nervous system GABAA receptors to provide anxiolytic, sedative, and tranquilizing effects

Contraindications

Hypersensitivity to carbenoxolone, licorice derivatives, or any psycholeptic component
Severe cardiovascular disease (hypertension, congestive heart failure, severe edema)
Hypokalemia or conditions predisposing to electrolyte imbalance
Severe hepatic impairment or renal failure
Pregnancy and lactation
Concomitant use with other CNS depressants or acute narrow-angle glaucoma (due to psycholeptic component)

Adverse Reactions

Fluid retention and edema
Systemic hypertension
Hypokalemia leading to muscle weakness and cardiac arrhythmias
CNS depression, drowsiness, dizziness, and fatigue (from psycholeptic component)
Dependence, tolerance, and withdrawal symptoms with prolonged psycholeptic use
Headache and gastrointestinal upset

Drug Interactions

Cardiac glycosides (digoxin): Hypokalemia induced by carbenoxolone increases the risk of digitalis toxicity and fatal arrhythmias
Diuretics (thiazides and loop diuretics): Concomitant use exacerbates potassium depletion
Antihypertensive agents: Carbenoxolone antagonizes blood pressure-lowering effects due to sodium and water retention
CNS depressants (alcohol, opioids, anesthetics): Potentiates central nervous system depression from the psycholeptic agent
Corticosteroids: Increased risk of severe hypokalemia and enhanced mineralocorticoid side effects

Curated Content: Needs Vetting Before Put to Clinical Use