Chlorhexidine

1950 - Synthesized in the UK.

1954 - The first commercial product appeared on the market: an external antiseptic based on chlorhexidine.

1970 - Numerous clinical studies have shown the high antibacterial activity of chlorhexidine, the treatment of hands with a skin antiseptic containing chlorhexidine was most effective.

1976 - The ability of chlorhexidine to inhibit the development of caries is shown.

1981 - Chlorhexidine was first used as an antibacterial component in lubricants used in urological practice.

1988 - The first alcohol-containing skin antiseptics appeared on the market based on a 2% chlorhexidine solution.

1992 - A central catheter impregnated with chlorhexidine was first introduced to the US market.

1993 - Chlorhexidine-soaked wipes and sponges designed for both domestic and professional use appeared on sale.

2005 - Chlorhexidine-soaked patient clothing received FDA approval.

2010-2012 - A number of medical devices have received FDA approval: catheters and implants soaked in chlorhexidine.

It is worth noting that for all the time of commercial use and scientific research of chlorhexidine, none of them could convincingly prove the possibility of the formation of chlorhexidine-resistant microorganisms . However, according to recent studies, the use of chlorhexidine can cause antibiotic resistance in bacteria (in particular, the resistance of Klebsiella pneumoniae to Colistin ) ^[2] .

Chemically, it is a dichloro-containing derivative of biguanide . The structure is very close to bigumal . The mechanism of action of chlorhexidine is to interact with phosphate groups on the surface of the cell, resulting in a shift in osmotic equilibrium, a violation of the integrity of the cell and its death.

Chlorhexidine is an antiseptic drug, active against gram-positive and gram-negative aerobic and anaerobic bacteria ( Treponema pallidum , Chlamydia spp., Ureaplasma spp., Neisseria gonorrhoeae , Gardnerella vaginalis , Bacteroides fragilis , except mycobacterium tuberculosis; protozoa ( Trichomonas vaginalis ). Also active against infections of viral etiology: HIV, herpes, hepatitis viruses, rotavirus gastroenteritis, enterovirus infections ^[3] . The drug is stable and after processing the skin (hands, surgical field, etc.) it remains on it in a certain amount, which continues to give a bactericidal effect.

The drug remains active in the presence of blood , pus , although somewhat reduced. Some strains of Pseudomonas spp., Proteus spp. Are weakly sensitive to chlorhexidine, acid-resistant forms of bacteria are resistant. Chlorhexidine acts on bacterial spores only at elevated temperatures.

They are used to treat the surgical field and hands of the surgeon, disinfect surgical instruments, as well as for purulent-septic processes (washing surgical wounds, bladder, etc.) and for the prevention of sexually transmitted diseases ( syphilis , gonorrhea , trichomoniasis ). The substance of chlorhexidine bigluconate is available as a 20% aqueous solution. The ready-to-use drug is a less concentrated aqueous or hydroalcoholic solution. So, for processing the surgical field, a 20% solution is diluted with 70% ethyl alcohol in a ratio of 1:40. The resulting 0.5% aqueous-alcoholic solution of chlorhexidine bigluconate is treated with the surgical field 2 times with an interval of 2 minutes. To quickly sterilize instruments, use the same solution for 5 minutes. To disinfect wounds, burns, use a 0.5% aqueous solution; for hand disinfection - 0.5% alcohol solution or 1% aqueous solution. When using the drug to treat the surgeon's hands, it is possible that the skin becomes dry and itchy, dermatitis; stickiness of the skin of the hands is also possible within 3-5 minutes.

Vaginal Suppositories

• one suppository contains 0.016 g of chlorhexidine bigluconate

Vaginal suppositories (infant form)

• one suppository contains 0.008 g of chlorhexidine bigluconate.
• Gel for local and external use of 0.5% (100 g of gel contains 0.5 g of chlorhexidine bigluconate).
• A solution for external use of 0.05% (100 ml of purified water contains a solution of chlorhexidine bigluconate 20% - 0.25 ml).

Solutions for rinsing the oral cavity:

• 0.2% aqueous solution;
• 0.1% solution of chlorhexidine bigluconate in ethanol (Eludryl).

Chlorhexidine as a prophylactic and therapeutic agent is used topically and topically. 0.05%, 0.2% and 0.5% aqueous solutions are used in the form of irrigation, rinsing and application - 5-10 ml of the solution is applied to the affected surface of the skin or mucous membranes with an exposure of 1-3 minutes 2-3 times a day (on a swab or by irrigation). Processing of medical instruments and work surfaces is carried out with a clean sponge moistened with an antiseptic solution, or by soaking. For the prevention of sexually transmitted diseases, the drug is effective if it is used no later than 2 hours after sexual intercourse. Using the nozzle, insert the contents of the vial into the urethra for men (2-3 ml), women (1-2 ml) and in the vagina (5-10 ml) for 2-3 minutes. To process the skin of the inner surfaces of the thighs, pubis, genitals. After the procedure, do not urinate for 2 hours. Complex treatment of urethritis and urethroprostatitis is carried out by injecting 2-3 ml of a 0.05% solution of chlorhexidine bigluconate 1-2 times a day into the urethra, the course is 10 days, the procedures are prescribed every other day. Intravaginally, 1 suppository 3-4 times a day for 7-20 days, depending on the nature of the disease. A rinse and gel for topical administration are usually prescribed 2-3 times a day. Patch: remove the protective film from the patch surface without touching the bandage with your fingers, and apply it to the damaged area of ​​the skin. Press the edges of the patch with your fingers so that the sticky part of the patch fixes the bandage.

In 2013, WHO included a 7% solution of chlorhexidine bigluconate in the list of essential medicines ^[4] . In accordance with the recommendations of the WHO, the umbilical cord (umbilical wound) is treated with a 7% solution, which reduces the likelihood of infection in newborns.

Vaginal Suppositories

• treatment of vaginal infections ( bacterial vaginosis , trichomoniasis , non-specific, mixed infections)
• emergency individual prevention of sexually transmitted infections ( syphilis , gonorrhea , trichomoniasis , chlamydia , ureaplasmosis )
• rehabilitation of the birth canal to prepare for delivery and management of the postpartum period in women at risk for infectious and inflammatory complications

Vaginal suppositories can be used in all trimesters of pregnancy and during lactation. Vaginal suppositories gently affect the mucous membrane, while maintaining normal vaginal microflora.

Vaginal suppositories (infant form)

• local treatment

Gel for local and external use 0.5%

• treatment of wounds, abrasions, scratches, burns, scratches
• treatment and prevention of infections of the skin and mucous membranes
• use in dentistry ( gingivitis , stomatitis and periodontitis )
• acne treatment (as part of complex therapy)
• skin care after cosmetic procedures (piercing, tattooing, depilation)
• protection against microbes in public places, in nature

0.5% alcohol solution of chlorhexidine

• hand treatment of medical personnel, surgeons, skin treatment of the operating and injection fields
• treatment of surgical wounds with an exposure of 1-2 minutes
• disinfection of medical devices, dental instruments, surfaces of devices

0.05% aqueous solution of chlorhexidine bigluconate

• washing of wounds, abrasions, scratches, burns, scratching, insect bites
• use in dentistry (gingivitis, stomatitis, alveolitis, periodontitis)
• treatment of ENT diseases ( pharyngitis , laryngitis , tonsillitis , otitis media )
• protection against microbes in public places, in nature
• prevention of sexually transmitted infections

0.2% aqueous solution of chlorhexidine bigluconate

• treatment and rehabilitation of the genital tract in gynecology, urology during medical diagnostic procedures
• disinfection of removable dentures

0.5% aqueous solution of chlorhexidine bigluconate

• treatment of wounds and burns, treatment of infected scuffs and cracks of the skin, open mucous membranes
• sterilization of a medical instrument at a temperature of 70 ° C

1% aqueous solution of chlorhexidine bigluconate

• for general disinfection of rooms, sanitary equipment, etc.
• treatment of the surgical field and hands of the surgeon before surgery, skin disinfection, treatment of postoperative and burn wounds

Hypersensitivity to the drug, dermatitis , allergic reactions. The simultaneous use of iodine preparations is undesirable in order to avoid the development of dermatitis. Chlorhexidine solutions should not be used to treat the conjunctiva and to rinse the cavities.

Caution

Use with caution in childhood.

Chlorhexidine is used to prevent STDs only as an emergency measure (condom rupture, accidental sexual contact). Regular and repeated instillations of chlorhexidine in the urethra can cause chemical burns (especially with individual hypersensitivity to the drug), which can ultimately lead to such a serious complication as urethral stricture .

Vaginal suppositories . Allergic reactions, itching, occurring after drug withdrawal are possible. Bleeding of various intensities is possible.

Gel . Allergic reactions, dry skin, itching, discoloration of the skin, dermatitis, stickiness of the skin of the hands (3–7 min) when using the gel, photosensitivity (the phenomenon of increasing the sensitivity of the body (most often the skin and mucous membranes) to ultraviolet radiation). In the treatment of gingivitis - staining of tooth enamel, tartar deposition, taste disturbance. Enamel staining and calculus deposition occurs in case of prolonged use of the drug.

Solution . Very rarely causes allergic reactions, itching, passing after the drug is discontinued.

In case of accidental ingestion of the drug, it is practically not absorbed; gastric lavage is indicated using milk, mild soap, gelatin or a raw egg.

There is no specific antidote, therefore, in case of side effects, symptomatic therapy is carried out.

• Concomitant use with iodine is not recommended.
• Chlorhexidine is incompatible with detergents containing an anionic group ( saponins , sodium lauryl sulfate, sulfonic acid , sodium carboxymethyl cellulose) and soaps. The presence of soap can inactivate chlorhexidine, so the soap residues must be thoroughly washed off before using the drug.
• It forms a toxic compound when mixed with sodium hypochlorite (NaOCl) - para-chloraniline ( p- NH ₂ C ₆ H ₄ Cl). There is evidence that parachloraniline is toxic ^[5] (Burkhardt-Holm et al., 1999) ^{[ incomplete references ]} and may cause the formation of methemoglobin ^[5] .
• Ethanol enhances the effectiveness of chlorhexidine.

Vaginal suppositories. External genitalia does not affect the effectiveness and tolerance of vaginal suppositories, since the drug is used intravaginally.

Solution and gel. Avoid getting the drug into the wounds of patients with open craniocerebral trauma, spinal cord injuries, perforation of the tympanic membrane. If the solution enters the mucous membranes of the eye, they should be washed quickly and thoroughly with water. Safety Data Sheets ( MSDS ) for chlorhexidine bigluconate.

The ingress of hypochlorite whitening substances onto tissues that were previously in contact with chlorhexidine-containing preparations may contribute to the appearance of brown spots on them. The bactericidal effect increases with increasing temperature of the solution. At temperatures above 100 ° C, the drug partially decomposes.

Aqueous solutions of chlorhexidine salts can decompose (especially when heated and alkaline pH ) with the formation of trace amounts of 4-chloroaniline, which has carcinogenic properties.

Case described ^{[ where? ]} development of methemoglobinemia and cyanosis in premature babies in the incubator due to 4-chloroaniline poisoning . The incubator was equipped with a humidifier with a solution of chlorhexidine, which, when heated, can decompose to 4-chloroaniline.

• The drug Disteril, produced abroad, contains 1.5% chlorhexidine bigluconate and 15% benzalkonium (a surface-active antiseptic), as well as a dye. The addition of benzalkonium enhances the disinfecting effect, and the dye allows you to accurately determine the area of ​​the treated skin. It is used for processing the surgical field, disinfection of medical equipment.
• Sibicort (Sibicort). Ointment containing chlorhexidine bigluconate (1%) and hydrocortisone (1%). It has antibacterial and anti-inflammatory properties. Used for acute and chronic eczema , dermatitis with concomitant bacterial infections. The ointment is applied to the affected area of ​​the skin with a thin layer 1-3 times a day for several days. Long-term use is not recommended. Contraindications: viral skin diseases, allergy to chlorhexidine. Release form: in tubes of 20, 50 and 100 g
• Included in some toothpastes and mouthwashes .
• As a 4% solution, it is part of many veterinary preparations, shampoos for pets.
• In the form of a 7-15% solution, it is used to treat a cow's udder.
• Included in the composition of the Anti-Angin Formula - a local anesthetic, antifungal and antibacterial agent.
• Desiskrab - alcohol 0.5% solution, used as a skin antiseptic, active against bacteria, fungi, viruses, mycobacteria .
• Dezin - an aqueous 20% solution, concentrate, is used to prepare ready-to-use aqueous and alcohol solutions of the desired concentration.
• Sebidin (lozenges) - Pharmacological action - chlorhexidine: antibacterial, bactericidal, antiseptic.

Destroys the cell membranes of bacteria.

• Miramistin

• Chlorhexidine (neopr.) . State Register of Medicines (May 26, 2016). Date of treatment May 26, 2016.
• 4-chloroaniline: Concise International Chemical Assessment Document 48.— Geneva: World Health Organization, 2003.— 62 p.