Chlorhexidine gluconate

Description

Chlorhexidine gluconate oral rinse USP, 0.12% is an oral rinse that contains 0.12% chlorhexidine gluconate (1,1’-hexamethylene bis 5-(p-chlorophenyl) biguanidedi-D-gluconate) in a base comprising 11.6% alcohol, FD&C Blue No. 1, glycerin, peppermint flavor, polysorbate 80, purified water, and saccharin sodium. The solution is near-neutral, with a pH range of 5-7. Chlorhexidine gluconate is a salt formed from chlorhexidine and gluconic acid, with the chemical formula C22H30Cl2N10•2C6H12O7 and a molecular weight of 897.72.

Uses and Indications

Chlorhexidine gluconate oral rinse, 0.12% is indicated for use between dental visits as part of a professional program for the treatment of gingivitis, characterized by redness and swelling of the gingivae, including gingival bleeding upon probing.

This formulation has not been tested in patients with acute necrotizing ulcerative gingivitis (ANUG). For patients presenting with coexisting gingivitis and periodontitis, healthcare professionals should refer to the precautions section for further guidance.

No teratogenic or nonteratogenic effects have been reported.

Dosage and Administration

Chlorhexidine gluconate oral rinse, 0.12% therapy should be initiated immediately following dental prophylaxis. The recommended dosage for adults and children over the age of 12 is 15 mL of undiluted solution, administered as an oral rinse twice daily. Patients should perform the rinsing for a duration of 30 seconds, ideally in the morning and evening after tooth brushing.

It is essential that patients are instructed to avoid rinsing with water or other mouthwashes, brushing their teeth, or consuming food immediately after using the rinse. Chlorhexidine gluconate oral rinse, 0.12% is not intended for ingestion; therefore, it should be expectorated after use.

Patients utilizing this oral rinse should be reevaluated and provided with a thorough dental prophylaxis at intervals not exceeding six months to ensure continued oral health and efficacy of the treatment.

Contraindications

Chlorhexidine gluconate oral rinse, 0.12% is contraindicated in individuals with a known hypersensitivity to chlorhexidine gluconate or any other ingredients in the formulation.

Additionally, the use of this oral rinse is not recommended for patients who have anterior facial restorations with rough surfaces or margins, as permanent discoloration may occur, which could be unacceptable for these individuals.

Warnings and Precautions

The effect of chlorhexidine gluconate oral rinse, 0.12%, on periodontitis has not been established. Clinical studies have indicated an increase in supragingival calculus among users of chlorhexidine gluconate oral rinse compared to control groups. The potential for chlorhexidine gluconate to increase subgingival calculus remains undetermined. It is recommended that calculus deposits be removed through dental prophylaxis at intervals not exceeding six months.

Anaphylaxis and serious allergic reactions have been reported in postmarketing experiences with dental products containing chlorhexidine. Healthcare professionals should remain vigilant for these adverse reactions.

For patients with coexisting gingivitis and periodontitis, the presence or absence of gingival inflammation following treatment with chlorhexidine gluconate oral rinse should not be relied upon as a primary indicator of underlying periodontitis. Chlorhexidine gluconate oral rinse may cause staining of oral surfaces, including teeth, restorations, and the dorsum of the tongue. While not all patients will experience significant staining, clinical testing revealed that 56% of chlorhexidine users exhibited a measurable increase in facial anterior stain after six months, compared to 35% of control users. Furthermore, 15% of chlorhexidine users developed what was classified as heavy staining, in contrast to 1% of control users.

It is important to note that staining resulting from chlorhexidine gluconate oral rinse does not adversely affect the health of the gingivae or other oral tissues. Most stains can be removed from tooth surfaces using conventional professional prophylactic techniques, although additional time may be necessary to complete the procedure. Caution should be exercised when prescribing this rinse to patients with anterior facial restorations that have rough surfaces or margins. If natural stains cannot be removed from these surfaces through dental prophylaxis, patients may need to be excluded from treatment with chlorhexidine gluconate oral rinse if permanent discoloration is deemed unacceptable. In some cases, stains in these areas may be difficult to remove and could necessitate the replacement of restorations.

Patients may also experience alterations in taste perception during treatment with chlorhexidine gluconate oral rinse. Rare instances of permanent taste alteration have been reported through postmarketing surveillance. Healthcare professionals should monitor patients for these potential side effects and provide appropriate guidance.

Side Effects

Patients using chlorhexidine gluconate oral rinse may experience a range of adverse reactions. Common side effects include an increase in staining of teeth and other oral surfaces, an increase in calculus formation, and alterations in taste perception.

In clinical trials, oral mucosal side effects were reported in less than 1% of participants and included aphthous ulcers, grossly obvious gingivitis, trauma, ulceration, erythema, desquamation, coated tongue, keratinization, geographic tongue, mucocele, and short frenum.

Postmarketing experience has revealed additional oral mucosal symptoms that are frequently reported, such as stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, and paresthesia. Other side effects noted include oral irritation, local allergy-type symptoms, minor irritation and superficial desquamation of the oral mucosa, parotid gland swelling, and inflammation of the salivary glands (sialadenitis).

It is important to note that anaphylaxis and serious allergic reactions have been reported during postmarketing use of dental products containing chlorhexidine. Furthermore, some patients may experience alterations in taste perception during treatment, with rare instances of permanent taste alteration documented through postmarketing product surveillance.

Drug Interactions

There are currently no documented drug interactions associated with this medication. Additionally, there are no known interactions with laboratory tests. As such, no specific recommendations for dosage adjustments or monitoring are warranted at this time.

Packaging & NDC

The table below lists all NDC Code configurations of Chlorhexidine Gluconate, the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.

Pediatric Use

Clinical effectiveness and safety of chlorhexidine gluconate oral rinse, 0.12%, have not been established in pediatric patients under the age of 18. Therefore, caution is advised when considering its use in this population.

Geriatric Use

Elderly patients may require special consideration when using chlorhexidine gluconate oral rinse, 0.12%. The clinical effectiveness and safety of this product have not been established in individuals under the age of 18, indicating that its use in geriatric patients should be approached with caution, particularly in those with specific dental conditions.

Caution is advised when administering chlorhexidine gluconate oral rinse to nursing women, as the effects on lactation have not been fully evaluated. Additionally, an increase in supragingival calculus has been observed in users of chlorhexidine gluconate oral rinse compared to control groups, which may be a relevant consideration for elderly patients who may already be at risk for dental complications.

While staining resulting from the use of chlorhexidine gluconate oral rinse does not adversely affect the health of the gingivae or other oral tissues, discretion should be exercised when prescribing this rinse to patients with anterior facial restorations that have rough surfaces or margins, as staining may be more pronounced in these cases.

Elderly patients may also experience alterations in taste perception during treatment. It is important to note that rare instances of permanent taste alteration have been reported through postmarketing surveillance, which may impact the quality of life for some geriatric patients. Therefore, healthcare providers should monitor for these potential side effects and consider them when determining the appropriateness of chlorhexidine gluconate oral rinse for elderly patients.

Pregnancy

Reproduction studies conducted in rats and rabbits at chlorhexidine gluconate doses up to 300 mg/kg/day and 40 mg/kg/day, respectively, have not demonstrated evidence of harm to the fetus. However, there is a lack of adequate and well-controlled studies in pregnant women. Due to the limitations of animal reproduction studies in predicting human response, chlorhexidine gluconate should be used during pregnancy only if clearly needed. Healthcare professionals are advised to weigh the potential benefits against any possible risks when considering the use of this drug in pregnant patients.

Lactation

It is not known whether chlorhexidine gluconate is excreted in human milk. Due to the potential for many drugs to be excreted in breast milk, caution should be exercised when administering chlorhexidine gluconate oral rinse to lactating mothers.

In animal studies involving parturition and lactation with rats, no evidence of impaired parturition or toxic effects on suckling pups was observed when chlorhexidine gluconate was administered to dams at doses exceeding 100 times the amount that would result from a human ingesting 30 mL of chlorhexidine gluconate oral rinse, 0.12% per day.

Renal Impairment

There is no specific information available regarding dosage adjustments, special monitoring, or safety considerations for patients with renal impairment. Healthcare professionals should exercise caution when prescribing to patients with reduced kidney function, as the absence of detailed guidance necessitates careful clinical judgment. Regular monitoring of renal function may be advisable in this patient population.

Hepatic Impairment

Patients with hepatic impairment have not been specifically studied in relation to the use of this medication. Consequently, there are no established dosage adjustments, special monitoring requirements, or precautions outlined for individuals with compromised liver function. It is recommended that healthcare providers exercise caution when prescribing this medication to patients with hepatic impairment, given the lack of data on its safety and efficacy in this population. Regular monitoring of liver function may be prudent in these cases, although specific parameters are not defined in the available information.

Overdosage

Ingestion of chlorhexidine gluconate oral rinse, 0.12%, can lead to significant adverse effects, particularly in small children. Specifically, the ingestion of 1 or 2 ounces by a child weighing approximately 10 kg may result in gastric distress, which can manifest as nausea. Additionally, there may be signs indicative of alcohol intoxication due to the formulation of the rinse.

In cases where a small child ingests more than 4 ounces of chlorhexidine gluconate oral rinse, or if any signs of alcohol intoxication are observed, it is imperative that medical attention is sought immediately. Prompt evaluation and management by healthcare professionals are essential to address potential complications associated with overdosage.

Nonclinical Toxicology

Reproduction studies conducted in rats and rabbits with chlorhexidine gluconate at doses of up to 300 mg/kg/day and 40 mg/kg/day, respectively, did not demonstrate any evidence of teratogenic effects on the fetus. However, it is important to note that adequate and well-controlled studies in pregnant women have not been performed. Given that animal reproduction studies may not reliably predict human outcomes, the use of this drug during pregnancy should be considered only when clearly necessary.

In terms of carcinogenicity, a drinking water study in rats revealed no carcinogenic effects at doses up to 38 mg/kg/day. Additionally, mutagenic effects were not observed in two mammalian in vivo mutagenesis studies involving chlorhexidine gluconate. The highest doses administered in a mouse dominant-lethal assay and a hamster cytogenetics test were 1000 mg/kg/day and 250 mg/kg/day, respectively. Furthermore, no evidence of impaired fertility was noted in rats at doses up to 100 mg/kg/day.

Postmarketing Experience

Postmarketing experience has identified several adverse events associated with the use of dental products containing chlorhexidine. Anaphylaxis and serious allergic reactions have been reported. Among the oral mucosal symptoms frequently noted are stomatitis, gingivitis, glossitis, ulcer, dry mouth, hypesthesia, glossal edema, and paresthesia. Additionally, minor irritation and superficial desquamation of the oral mucosa have been observed in patients using chlorhexidine gluconate oral rinse.

Reports have also included cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis) in patients utilizing chlorhexidine gluconate oral rinse. Furthermore, rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse have been documented through postmarketing product surveillance.

Patient Counseling

Advise patients that chlorhexidine gluconate oral rinse, 0.12%, has been prescribed by their dentist to treat gingivitis, aiming to reduce gum redness and swelling while helping to control gum bleeding. Patients should be instructed to use the oral rinse regularly as directed by their dentist, in conjunction with daily brushing. It is important for patients to spit out the rinse after use and to avoid swallowing it.

Inform patients to seek immediate medical attention if they experience any allergic symptoms, which may include skin rash, itching, generalized swelling, breathing difficulties, lightheadedness, rapid heart rate, upset stomach, or diarrhea. Emphasize that chlorhexidine gluconate oral rinse should not be used by individuals who have a known sensitivity to it or its components.

Patients should be made aware that the use of chlorhexidine gluconate oral rinse may lead to tooth discoloration or an increase in tartar (calculus) formation, particularly in areas where staining and tartar typically occur. It is essential for patients to visit their dentist for the removal of any stain or tartar at least every six months, or more frequently if advised by their dentist. Both stain and tartar can be effectively removed by a dentist or hygienist.

Additionally, inform patients that chlorhexidine gluconate oral rinse may cause permanent discoloration of some front-tooth fillings. To minimize the risk of discoloration, patients should be encouraged to brush and floss daily, paying special attention to areas that begin to show discoloration.

Patients may find that the rinse has a bitter taste and that it can alter the taste of foods and beverages. This taste interference is generally less noticeable with continued use. To mitigate this effect, advise patients to use the rinse after meals and to refrain from rinsing with water or other mouthwashes immediately after using chlorhexidine gluconate oral rinse.

Encourage patients to reach out to their dentist or pharmacist if they have any questions or comments regarding the oral rinse. Instruct them to contact their doctor for medical advice about any side effects they may experience. Patients can report side effects to Pharmaceutical Associates, Inc. at 1-800-845-8210 or to the FDA at 1-800-FDA-1088 or via the website www.fda.gov/medwatch.

Storage and Handling

The product is supplied in a bottle equipped with a child-resistant closure to ensure safety. It is essential to store the product at a temperature range of 20° to 25°C (68° to 77°F), in accordance with USP Controlled Room Temperature guidelines. Additionally, it is crucial to keep the product out of reach of children to prevent accidental ingestion.

Additional Clinical Information

Patients using chlorhexidine gluconate oral rinse, 0.12%, may experience staining of the teeth; however, this staining does not adversely affect the health of the gingivae or other oral tissues. Most stains can be removed through conventional professional prophylactic techniques, although additional time may be required. Clinicians should exercise discretion when prescribing this rinse to patients with anterior facial restorations that have rough surfaces or margins, as natural stains may be difficult to remove and could lead to permanent discoloration, necessitating restoration replacement in rare cases.

Additionally, some patients may notice an alteration in taste perception during treatment. Postmarketing surveillance has reported rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse.

FDA Insert (PDF)

This document is the official FDA-approved prescribing information for Chlorhexidine Gluconate as submitted by PAI Holdings, LLC dba PAI Pharma. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)