Included in the formulation
АТХ:A.02.B.X.01 Carbenoksolon
Pharmacodynamics:Carbenoksolon - a derivative of glycyrrhizic acid with a steroid structure of the molecule, identical to substances found in the licorice root. The substance interacts with endogenous corticoids, powerfully inhibiting the enzyme 11β-HSD, which has long been used in the treatment of gastrointestinal ulcers and other inflammatory reactions. Pharmacological action - mineralocorticoid, glucocorticoid, anti-inflammatory. Reduces the rate of exfoliation of mucocytes, increases the formation of mucin and bicarbonates (neutralizes H +) and increases the viscosity of mucus. Stimulates the blood supply to the gastric mucosa, inhibits the release of hydrolases.
Pharmacokinetics:Quickly and fairly fully absorbed (80%) when taken orally, the blood almost completely binds to proteins. The maximum concentration is achieved in 1-2 hours. The connection with plasma proteins is almost 100%. The volume of distribution is 0.1 l / kg. 98% is biotransformed in the liver by the formation of esters with glucuronic acid. Metabolites are excreted in urine (60%) and bile. Subjected to enterohepatic circulation. The half-life is 16 h.
Indications:Inflammation of the oral mucosa without signs of infection.
XI.K00-K14.K12 Stomatitis and related lesions
Contraindications:Hypersensitivity to the drug; infectious process in the oral cavity.
Carefully:Severe violations of kidney function, liver and cardiac function. Childhood.
Pregnancy and lactation:The FDA action category is not defined. Adequate and well-controlled studies have not been conducted. Use with caution in pregnancy! There is no data on the penetration of the drug into breast milk. Use with caution in lactation.
Dosing and Administration:The gel is applied to the affected parts of the oral cavity, after eating and before bedtime for a long time (up to 3 weeks). Application in elderly patients
In the elderly, use with caution in view of contraindications, because of the possibility of systemic side effects and the presence of concomitant pathology.
Side effects:Allergic reactions: skin rash, itching, fever. Electrolyte imbalance in long-term systemic application.
In connection with the structural generality of carbenoxolone and aldosterone, there is a delay in the body of sodium and water, an increase in the release of potassium,resulting in edema and hypokalemia, hypertension.
Interaction:If the combination is applied simultaneously atenolol + chlorthalidone with carbenoxolone, an increase in the excretion of potassium ions is possible. Spironolactone reduces the effect (competition for receptors).
Strengthens cardiotropic cardiac glycosides.
Carbenoxolone in combination with furosemide increases the risk of hypokalemia.
Hydrochlorothiazide (in combination hydrochlorothiazide + ramipril) can cause electrolyte imbalance, especially hypokalemia, with simultaneous use with carbenoxolone.
Special instructions:To avoid side effects of carbenoxolone, aldosterone antagonists should not be administered, since they inhibit the therapeutic effect of the drug. The therapeutic value of carbenoksolon in the treatment of peptic ulcer remains in question, since it is known about the high frequency of natural remission (healing) of ulcers of the duodenum. To substantiate the preventive use of the drug (for prolonging the remission of peptic ulcer) further research is needed.
Nootropic effects of carbenoxolone were studied. It all started with the observation that a prolonged exposure to glucocorticosteroids can adversely affect cognitive function. Carbenoksolon can reduce the content of active molecules of glucocorticosteroids in the brain tissue by inhibiting 11β-HSD, the enzyme, the regenerating cortisol molecule (active glucocorticosteroid) from the molecule of the inactive precursor-cortisone.
In a study on this issue, it was shown that carbenoxolone improves the fluency of pronouncing words in elderly healthy patients aged 55-75 years. In patients with type 2 diabetes at the age of 52-70 years, the drug improved memory for words. However, it was noted that carbenoxolone causes an increase in the accumulation of cortisol in the kidneys, thus provoking hypertension, so patients together with the drug received a potassium-sparing diuretic amiloride during the study.