Hexetidine, Chlorobutanol Hemihydrate, Choline Salicylate

Pharmacological properties

the properties of the drug are due to the action of its three active ingredients - hexetidine, choline salicylate, chlorobutanol hemihydrate.

The antibacterial and antifungal effect is due to hexetidine, which exhibits antibacterial activity against gram-positive and gram-negative microorganisms (both aerobes and anaerobes). With respect to aerobic microorganisms, it has a mainly bacteriostatic effect and a weak bactericidal effect. Hexetidine has a pronounced bactericidal effect on anaerobic microorganisms. The mechanism of action of hexetidine is based on the competitive substitution of thiamine: the structure of hexetidine is similar to the structure of thiamine, which is necessary for the growth of microorganisms.

The anti-inflammatory effect is due to choline salicylate, which belongs to the group of NSAIDs and has analgesic, antipyretic and anti-inflammatory effects.

The analgesic activity is also due to the local anesthetic chlorobutanol, used in otolaryngology (nose drops, rinses) and dentistry (applications and irrigation) mainly as a painkiller.

Pharmacokinetics Active substances are fixed on the oral mucosa, from where they are then gradually released.

Indications

Local treatment of diseases and inflammatory processes of the oral cavity and pharynx in adults and children over 2.5 years of age: gingivitis, stomatitis; periodontitis; aphthae and teething pain; postoperative oral care; tonsillitis, acute and chronic tonsillitis, pharyngitis, laryngitis.

Application

R-r is used as a local means for rinsing the oral cavity.

For one rinse of the oral cavity: 2 teaspoons of the drug should be dissolved in ¼ cup of warm water. 2 to 4 rinses per day. Do not swallow.

Spray is used for irrigation of the oral cavity.

Adults: 1 spray 4-6 times a day

Children aged 2.5 to 15 years: 1 spray 2-3 times a day.

The course of treatment is no more than 5 days.

Contraindications

Do not use in children under the age of 2.5 years. do not use if allergies to the components of the drug are detected.

Side effects

Allergic reactions: irritation, skin reactions. in this case, treatment must be stopped.

special instructions

Long-term use is not recommended, as this can lead to disturbance of the microbial balance in the oral cavity and throat.

Use during pregnancy or lactation. During pregnancy and lactation, the drug is used only as prescribed by the doctor and only if the benefit of using the drug for the mother outweighs the risk to the fetus.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Does not affect.

Children. Used in children over the age of 2.5 years. The safety of the drug in children under 2.5 years of age has not been investigated.

Interactions

Do not use simultaneously with drugs containing antiseptics.

Overdose

No drug overdose has been reported.

Storage conditions

At a temperature not exceeding 25 ° C. do not freeze.

Actual information

Angilex is a drug often prescribed by otolaryngologists, dentists and general practitioners. It belongs to the group of medicines used for diseases of the throat, is dispensed from pharmacies without a doctor’s prescription.

Its composition (according to the instructions of the Ministry of Health) includes the following active substances: hexetidine, choline salicylate, chlorobutanol hemihydrate. Available in the form of a spray and oral solution.

Principles of use, mechanism of action of the drug Angilex

Angilex - a drug that has a local antiseptic, anti-inflammatory, analgesic effect. Its active substance hexetidine acts bacteriostatically on aerobic microorganisms, the bactericidal effect is weak. But anaerobes are bactericidal.The mechanism of action is a competitive interaction with thiamine: in its chemical structure, hexetidine is similar to thiamine, which is necessary for the growth of microorganisms. Anti-inflammatory and analgesic effects are realized due to blockade of the COX enzyme. Choline salicylate is responsible for the anti-inflammatory activity of the drug, also has an analgesic and antipyretic effect. The analgesic effect is provided by chlorobutanol.

Drug use Angilex it is advisable in complex therapy for inflammatory diseases of the oropharynx, for example, tonsillitis, pharyngitis. Angilex effective for periodontal diseases, stomatitis, fungal infections of the oral cavity (complex therapy). It is prescribed as part of the treatment of acute respiratory viral infections (with sore throat).

The therapeutic effect of the active components of the drug Angilex

Hexetidine

Hexetidine is an antiseptic derivative of pyrimidine, its effectiveness and safety when applied topically have been confirmed in many studies.

The antiviral properties of hexetidine in infections of the respiratory tract and herpes virus have been studied in vitro. It was found that hexetidine is non-cytotoxic to human cells, however, it weakens the effect of highly virulent influenza viruses A / H5N1, A / H1N1pdm, MS virus and herpes simplex virus type 1 by 100 times or more. Hexetidine possesses these properties even with short-term use (within 30 s) (Deryabin P.G. et al., 2016).

In one study, the therapeutic effects of a 0.1% solution and 0.2% hexetidine aerosol for topical application were studied. Hexetidine was found to be a safe antiseptic with a wide spectrum of antibacterial activity in vitro and in vivo. It also has local anesthetizing, astringent and deodorizing effects. In addition, it prevents the formation of microbial biofilms. Pathogens have low resistance to hexetidine (Capic E. et al, 2002). The above characteristics of hexetidine explain the effectiveness of the drug Angilex and its use in the treatment of infections of the oral cavity and throat.

One study compared the effectiveness of 0.1% hexetidine and 0.1% chlorhexidine in the form of a mouthwash. These solutions were prescribed to patients with gingivitis or periodontitis. The therapeutic efficacy and side effects of both drugs have been studied. As a result of the study, the following conclusions were made: a solution of hexetidine is an alternative to a solution of chlorhexidine, since during the treatment of the above diseases it is no less effective. Side effects of both substances were similar, but hexetidine had a lesser effect on discoloration of tooth enamel (Ernst C.P. et al., 2005).

However, when prescribing drugs containing hexetidine, it should be borne in mind that there are studies that confirm a large number of side effects when using hexetidine. In them, hexetidine was compared with placebo and chlorhexidine in the treatment of gingivitis. The authors of relatively new studies focus on the fact that chlorhexidine should be used, since it is better tolerated by patients (Afennich F. et al., 2011). At the same time, in a study comparing the therapeutic efficacy of fluconazole and hexetidine as a topical treatment for oral candidiasis in patients with dentures, it was found that hexetidine is better tolerated by patients than fluconazole and causes fewer side effects. The therapy of oral candidiasis with hexetidine was effective and, given its greater safety, it was recommended to prescribe hexetidine (Koray M. at al., 2005).

In dental practice, hexetidine has been studied as a drug for the prevention of caries. It reduces plaque formation.The active substances used to prevent caries should prevent the formation of a biofilm of pathogenic bacteria without affecting the biological balance of the microflora of the oral cavity. The appointment of antimicrobial agents is primarily characteristic of secondary and tertiary prophylaxis (in order to prevent recolonization by pathogenic microorganisms) to prevent relapse of the disease. The results of these studies indicate that hexetidine is able to inhibit the development and maturation of pathogenic biofilms, and also affect the metabolism of bacteria (Baehni P.C., Takeuchi Y., 2003).

Subgingival plaque (tartar) is one of the problems in dentistry. Reducing its formation is a key point in the prevention of caries and periodontal diseases. Only mechanical plaque removal during brushing is not always effective. The properties of hexetidine to inhibit plaque formation were investigated by a group of European scientists. According to the results of studies, it was concluded that hexetidine slows down the formation of plaque, therefore it is used as a prophylaxis of the development of gingivitis, and also has an anti-inflammatory effect and, therefore, can be used in the complex therapy of this disease. Conclusions were also made about the safety of the drug for wide clinical use. Hexetidine is effective against C. albicans, often colonizing dentures. It was also found that hexetidine can be used in dental practice both in the form of a solution for rinsing the oral cavity and in the form of an oral spray. To prevent colonization of dentures by pathogenic microorganisms, it was proposed to treat them by immersing in a 0.1% solution of hexetidine overnight (8 hours) (Aoun G et al., 2005).

Pathogenic microorganisms cause the development of inflammatory processes in the oral cavity and pharynx. In one in vitro study, the activity of 4 antiseptics (cetyltrimethylammonium naproxenate, chlorhexidine, benzidamine, hexetidine) was compared with 4 antibiotics (amoxicillin, amoxicillin and clavulanic acid, clarithromycin, cefaclor). The effect of drugs of both groups on microorganisms that colonize the oropharynx and respiratory tract, including Streptococcus pyogenes and Streptococcus pneumoniae, was studied. This study showed that the selected group of bacteria was more sensitive to the group of antiseptics than to amoxicillin and amoxicillin and clavulanic acid. As a result of the study, it was found that the antiseptics described above can be used against pathogenic microorganisms of the oral cavity and throat (Pilloni A.P. et al., 2002).

Hexetidine was also used to treat the endotracheal tube in mechanical ventilation in patients in the intensive care unit. According to the results of the study, it was concluded that the resistance of 1% hexetidine-containing PVC to microbial adhesion was higher than that of native PVC. Therefore, it is suggested that this method can reduce the incidence of ventilator-associated pneumonia (a special form of pneumonia that occurs in patients on mechanical ventilation) (Jones D.S. et al., 2002).

Choline Salicylate

Choline salicylate is an effective and well-tolerated anti-inflammatory drug that has been known since the 60s of the 20th century when it was used as an antipyretic drug (Broh-Kahn Rh., 1960). Choline salicylate is also used to treat rheumatic diseases, especially rheumatoid arthritis, as part of ear and eye drops, to treat otitis media, gingivitis and eliminate plaque (Scully F.J., 2010).

Choline salicylate has proven itself in the treatment of inflammatory gum disease (Brodniewicz Z. et al., 1986), and due to its analgesic properties, in the treatment of ulcerative lesions of the oral cavity (Daniel A. et al., 1960).

As an effective anti-inflammatory and analgesic drug, choline salicylate is recommended to be included in the complex treatment of acute catarrhal otitis media (Razvozzhaev A.A. et al., 2012).

In one study, the irritant effect of 2% choline salicylate in the form of eye drops was studied. For 5 minutes, they acted on rabbit corneal cells. Then, corneal cell viability was determined. As a result of the study, it was found that the drug has low cytotoxicity. After its use, cell viability was more than 70% (Wroblewska K. et al., 2015).

An interesting study was conducted in 1986. It was previously believed that choline salicylate can be prescribed to people with hypersensitivity to acetylsalicylic acid and other NSAIDs. But cases of the development of hypersensitivity and exacerbation of bronchial asthma after taking salicylate choline have been described. Thus, we can conclude that it is possible to develop a cross-reaction of hypersensitivity (Chudvin D.S. et al., 1986). Accordingly, prescribe the drug Angilex such patients should be used with extreme caution.

There is also information that the use of drugs containing choline salicylate in the treatment of diseases of the oral cavity can lead to the development of refractory gastric ulcers (Lim Y.C. et al., 2014). This side effect is especially true for self-medication with drugs containing this active substance. Patients should be informed about a possible ulcerative lesion of the gastrointestinal tract as a side effect of drugs containing choline salicylate, as well as the danger of their uncontrolled use.

Chlorobutanol Hemihydrate

Chlorobutanol is part of some sedatives and anesthetics. When used internally, it has a sedative effect. Locally, it is prescribed as an antiseptic, has a distracting effect, moderate anti-inflammatory properties are characteristic.

In studies of the toxicity of chlorobutanol, it was found that this active substance has low toxicity. It is part of a large number of medicines. However, it should be prescribed with extreme caution to patients with impaired liver and kidney function. Possible occurrence of impaired speech, dysarthria, drowsiness, hemodynamic impairment. The development of toxic effects is possible with prolonged uncontrolled use of drugs containing chlorobutanol hemihydrate (Nordt S.P. et al., 1996).

It must be remembered that in in vitro studies, chlorobutanol had an adverse effect on mouse embryo tissue. Studies in mice have revealed that it crosses the placenta and has a toxic effect on the tissue of a developing embryo (Smith W.S. et al., 1997).

Conclusion

Angilex is a drug whose active substances are selected in such a way that the therapeutic effect of each is complementary and mutually reinforced. However, it must be remembered that the drug has contraindications and side effects, so before using it, you need to consult a doctor, even despite the fact that it refers to over-the-counter drugs.