Class: Anti-infectives, Miscellaneous
Chemical Name: N,N″-Bis(4-chlorophenyl)-3,12-diimino- 2,4,11,13-tetraazatetradecanediimidamide di-d-gluconate
Molecular Formula: C22H30Cl2N10•2C6H12O7
CAS Number: 18472-51-0
Brands: Paroex, Peridex, PerioChip, PerioGard
Medically reviewed on April 16, 2018
Uses for Chlorhexidine Gluconate
Used subgingivally (extended-release insert) for treatment of adult periodontitis as an adjunct to scaling and root planing to reduce periodontal pocket depth;3 used as part of a periodontal maintenance program that includes good oral hygiene.3
Prevention of Dental Caries
Has been used as a topical oral solution for prevention of dental plaque and dental caries† when conventional oral hygiene measures are difficult or impossible, such as in patients with fractured jaws, periodontal surgery, or orthodontic treatments and in patients with seizure disorders, rheumatoid arthritis, mental retardation, and cerebral palsy.8 33 34 44
Mucositis and Other Oral Complications in Individuals with Altered Immunocompetence
Has been used as a topical oral solution to decrease incidence and severity of mucositis† and other oral complications† in patients with altered immunocompetence, including those undergoing bone marrow transplantation,10 11 14 20 21 radiation therapy,15 21 38 or chemotherapy.12 13 15 19 20 21 38
Has been used as a topical oral solution as adjunct to surgical debridement, plaque removal, and systemic anti-infectives in treatment of linear gingival erythema†, necrotizing ulcerative gingivitis†, and necrotizing ulcerative periodontitis† in immunocompromised individuals, including patients with HIV infection.88 89
Such use has been beneficial for prevention or treatment of oral complications in some immunocompromised individuals,10 12 13 14 15 20 21 62 but inconsistent results reported in some studies.11 19 20 21
Oropharyngeal Decontamination in Critically Ill Patients
Has been used as a topical oral solution for oral hygiene and oropharyngeal decontamination in an attempt to decrease the incidence of nosocomial respiratory tract infections in critically ill patients†, including immunocompromised patients and those undergoing mechanical ventilation or heart surgery.19 21 39 85 86
Chlorhexidine Gluconate Dosage and Administration
Oral, Topical Use Only
Immediately prior to initiation of treatment, provide professional dental prophylaxis.1 2 90 91 Reevaluate patient with thorough dental prophylaxis throughout treatment at intervals not exceeding 6 months.1 2 90 91
Instruct patients to brush their teeth immediately prior to each use of the topical oral solution.1 2 90 91 Then, place appropriate volume of the oral solution into the mouth, swish for 30 seconds, and expectorate the solution.1 2 90 91
Administered subgingivally as extended-release inserts into periodontal pockets by a dental health-care provider.3
Place a single insert containing 2.5 mg of chlorhexidine gluconate into each periodontal pocket that has a probing depth ≥5 mm.3
Isolate periodontal pocket and dry surrounding area prior to insertion.3 Grasp flat end of insert with forceps and place (curved end first) into periodontal pocket to its maximum depth.3 If necessary, further maneuver insert into position using tips of forceps or a flat instrument.3
Advise patients to avoid dental floss at insertion sites for 10 days after placement.3
If insert dislodges ≤48 hours after placement, place a new insert.3 If insert dislodges >48 hours but <7 days after placement, do not replace insert; reevaluate at 3 months and place new insert if pocket depth has not been reduced to <5 mm.3 If insert dislodges ≥7 days after placement, no action required since this is considered a full course of treatment.3
Inserts will biodegrade within periodontal pockets and do not need to be manually removed.3
Consult manufacturer’s literature for additional information on subgingival administration of chlorhexidine inserts.3
Oral, Topical Use Only
Dosage varies depending on size, shape, and number of periodontal pockets treated.3
Place new insert every 3 months into pockets that continue to have a probing depth of ≥5 mm.3
Consider other treatment options (e.g., combination therapy, surgical intervention) if periodontal pockets with a probing depth of ≥5 mm do not respond within 9–12 months.79
Maximum of 8 inserts during a single visit.3
Cautions for Chlorhexidine Gluconate
Serious allergic reactions, including fatal anaphylaxis, reported rarely with topical chlorhexidine preparations used on the skin (e.g., solutions, washes, sponges, swabs), including OTC topical preparations.4 45 48 63 64 66 92
Hypersensitivity reactions can occur within minutes following topical exposure.92 Symptoms may include wheezing or difficulty breathing, facial swelling, urticaria that can quickly progress to more serious symptoms, severe rash, or life-threatening shock.92
Prior to prescribing or recommending any preparation that contains chlorhexidine, ask patients whether they have ever had an allergic reaction to antiseptics or any preparation containing chlorhexidine.92
If allergic reaction occurs or is suspected, discontinue the drug and carefully monitor the reaction and provide immediate respiratory and/or cardiovascular support as needed.92
Precautions Related to Topical Oral Solution
Possible staining of teeth and other oral surfaces, such as tooth surfaces, restorations, and dorsum of the tongue.1 2 4 5 8 10 18 90 91 Stains usually can be removed by conventional professional prophylactic techniques, although additional time may be required to complete the prophylaxis.1 2 90 91
Effect on periodontitis not determined.1 2 90 91 If used as a mouthwash or oral rinse in patients with coexisting gingivitis and periodontitis, presence or absence of gingival inflammation following treatment should not be used as a major indicator of underlying periodontitis.1 2 90 91
Precautions Related to Subgingival Inserts
Use in acutely abscessed periodontal pockets not studied and not recommended.3 Management of periodontal disease should include consideration of potentially contributing medical disorders, such as cancer, diabetes, and compromised immune function.3
Avoid dental floss at insertion site for 10 days after placement; flossing might dislodge insert.3
Some mild to moderate sensitivity is normal during first week after placement of a subgingival insert; however, dentist should be promptly notified if pain, swelling, or other problems occur.3
Subgingival insert: Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.3 No overall differences in safety or efficacy between geriatric and younger adults.3
Common Adverse Effects
Chlorhexidine Gluconate Pharmacokinetics
Topical oral solution: Systemic absorption does not appear to occur following use as a mouthwash or oral rinse.78
Following use of a 0.12% topical oral solution of chlorhexidine gluconate as a mouthwash or oral rinse, approximately 30% of drug is retained in oral cavity.1 2 5 8 34 90 91 The drug is bound to phosphate groups principally on coatings of mucous membrane surfaces8 and gradually released into oral fluids1 2 5 8 34 90 91 for up to 24 hours.8
Following subgingival administration of biodegradable extended-release insert containing 2.5 mg of chlorhexidine gluconate, the drug is slowly released into periodontal pocket.3 50 In vitro study indicates approximately 40% of the drug is released during first 24 hours and remainder is released in almost linear manner over 7–10 days.3
Following oral administration† of a 300-mg dose of chlorhexidine gluconate, peak plasma concentrations of 0.206 mcg/mL were attained 30 minutes after the dose; however, the drug was undetectable in plasma 12 hours after the dose.1 2 77 90
Oral, Topical Use Only
20–25° C (may be exposed to 15–30°).3
Actions and Spectrum
Cationic compound; antibacterial activity results from attraction between positively charged chlorhexidine and negatively charged bacterial cell surfaces.3 5 8 Becomes adsorbed onto cell surfaces of susceptible organisms and disrupts cell membrane integrity resulting in increased permeability.8 33 34
Topical oral solution: When used as a mouthwash or oral rinse, chlorhexidine binds to negatively charged surfaces within the oral cavity, including hydroxyapatite of tooth enamel, pellicle on tooth surface, oral mucosa, salivary glycoproteins, and bacteria and extracellular polysaccharides of bacterial origin.5 8 33 34 Can provide a persistent bacteriostatic effect at tooth surface.8 33 34 May provide antiplaque effects because of bacteriostatic or bactericidal effects on salivary bacteria and bacteria adhering to tooth surfaces.34
Subgingival insert: After placement into periodontal pockets, numbers of some organisms associated with periodontal disease, including Porphyromonas gingivalis, Prevotella intermedia, Bacteroides forsythus, and Campylobacter rectus, were reduced.3 Clinical importance unknown.3
Active against some aerobic and anaerobic gram-positive and gram-negative bacteria.8 22 33 54 55 56 57 60 Also has some activity against Chlamydia trachomatis,74 certain fungi,8 33 42 49 59 and certain viruses,33 53 but is inactive against mycobacteria.71
Advice to Patients
Topical oral solution: Advise patients to use the solution on a regular basis as directed by their dental health-care provider and to brush their teeth immediately prior to each use.1 2 90 91 Importance of expectorating the solution after 30 seconds and importance of not rinsing with water or other mouthwashes and not brushing their teeth or eating immediately after using the solution.1 2 90 91
Topical oral solution: Advise patients that the solution may cause some tooth discoloration or increase in tartar (calculus) formation.1 2 90 91 Importance of contacting dental health-care provider for removal of any stain or tartar at least every 6 months or more frequently if needed.1 2 90 91
Topical oral solution: Advise patients that the solution may taste bitter and can affect how foods and beverages taste; this usually becomes less noticeable with continued use.2 90 91 Using the solution after meals may avoid taste interference.2 90 91
Subgingival insert: Advise patients to avoid dental floss at the insertion site for 10 days following insert placement.3 Importance of notifying dental health-care professional if an insert is dislodged or if pain, swelling, or other problems occur.3
Subgingival insert: Advise patients that some mild to moderate sensitivity is normal during first week after insert placement; importance of promptly notifying dental health-care provider if pain, swelling, or other problems occur.3
Advise patients receiving topical oral solution or subgingival insert to immediately contact a clinician and stop using the product if they experience any symptoms of an allergic reaction (e.g., rash, itching, hives, generalized or facial swelling, wheezing or breathing difficulties, lightheadedness, rapid heart rate, shock, upset stomach or diarrhea).2 3 90 91 92
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Oral (Topical Use Only)
Chlorhexidine Gluconate Oral Rinse
PerioGard Alcohol Free
AHFS DI Essentials. © Copyright 2018, Selected Revisions April 16, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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