Lidoxan lozenzges menthol 5 mg/1 mg. №24

Description

Lidoxan menthol Storage
active substances: chlorhexidine dihydrochloride, lidocaine hydrochloride;

1 lollipop contains chlorhexidine dihydrochloride 5 mg and lidocaine hydrochloride 1 mg;

Excipients: menthol (levomenthol), citric acid anhydrous, magnesium stearate, sorbitol (E 420).

Lidoxan menthol Dosage form
Lollipops.

Main physical and chemical properties: round tablets of white or almost white color with small specks of mint taste and smell.

Lidoxan menthol Pharmacotherapeutic group
Drugs used in diseases of the throat. ATX code R02A.

Pharmacological properties
Pharmacodynamics. Lidocaine hydrochloride is a peripheral local amide-type anesthetic. It exhibits a superficial analgesic effect without delaying the conduction of nerve impulses at the injection site.

As a local anesthetic, lidocaine has the same mechanism of action as other drugs in this group: it blocks the generation and conduction of nerve impulses in sensitive, motor and autonomic nerve fibers. It directly affects cell membranes, inhibiting the entry of sodium ions into nerve fibers through membranes. Due to the progressive spread of the anesthetic effect, the threshold of electrical excitation in the peripheral nerves increases, the conduction of the nerve impulse slows down, and the reproduction of the action potential weakens, which ultimately leads to complete blocking of the nerve impulse. In general, local anesthetics block autonomic nerves, small nonmyelinated (pain sensations) and small myelinated nerves (pain sensations, temperature) rather than large myelinated fibers (sensation of touch, pressure).

At the molecular level, lidocaine specifically blocks sodium ion channels in the inactive state, which prevents the generation of action potentials, preventing the conduction of nerve impulses when topically applied lidocaine near the nerve.

Effects on peripheral nerves are important when lidocaine is used as a local anesthetic. The relationship between efficacy and toxicity is favorable. Allergic reactions to lidocaine are very rare.

Chlorhexidine is a cationic antiseptic that has antibacterial effects on both gram-positive and gram-negative microorganisms (eg, Micrococcus sp., Staphylococcus sp., Streptococcus sp., Bacillus sp., Clostridium sp., Corynebacterium sp.). It also has an antifungal effect on dermatophytes and fungi. The drug acts as a bacteriostatic in low concentrations, and in high concentrations has a bactericidal effect.

Chlorhexidine carries a powerful positive charge – thus, it is adsorbed on negatively charged areas of the bacterial cell wall and on extracellular structures. Absorption is specific and localized in the relevant areas of the bacterial cell wall containing phosphates.

Chlorhexidine binds to the bacterial cytoplasmic membrane. It is adsorbed on the negatively charged surface of the teeth, on the plates located in the mouth or the membrane of the oral cavity. Small amounts of active substances enter the gastrointestinal tract with saliva. Chlorhexidine is not absorbable. Lidocaine can be absorbed through the mucous membranes of the mouth and pharynx. However, most of it is destroyed without reaching the systemic blood flow.

Pharmacokinetics.

Chlorhexidine

Absorption

Chlorhexidine is poorly absorbed after topical or oral administration. After topical application to the affected area of ​​skin, chlorhexidine is absorbed by the outer layer of the skin, which causes a prolonged bactericidal effect on the skin. Pharmacokinetic studies have shown that approximately 30% of chlorhexidine remains in the mouth after lavage and is then gradually released into saliva. Patients swallow about 4% chlorhexidine.

Distribution

Following oral administration, plasma protein binding of chlorhexidine is insufficient.

Metabolism and excretion

Chlorhexidine does not accumulate. Only a small part is metabolized. 10% of the absorbed active substance is excreted in the urine, and 90% – in the feces.

Lidocaine

Absorption

The degree of systemic absorption of lidocaine depends on the site and route of administration. It is rapidly absorbed from the digestive tract, mucous membranes and through damaged skin, but most of it decomposes before entering the systemic circulation. Absorption from mucous membranes after topical application depends on perfusion and total dose. 30 minutes after administration, less than 17% of the dose may be excreted unchanged from the gastrointestinal tract and less than 1.5% from other tissues.

The anesthetic effect of lidocaine after topical application is manifested in two to five minutes and lasts from 30 to 45 minutes. Anesthesia is superficial and does not extend to submucosal structures.

Distribution

Lidocaine is well distributed in tissues (kidneys, lungs, liver, heart, adipose tissue). Lidocaine crosses the blood-brain barrier and the placenta and is excreted in human breast milk.