Chlorhexidine gluconate

Description

Chlorhexidine gluconate oral rinse USP, 0.12% is an oral rinse formulation that contains 0.12% chlorhexidine gluconate, which is chemically defined as 1,1’-hexamethylene bis 5-(p-chlorophenyl) biguanide di-D-gluconate. The product is presented as a near neutral solution with a pH range of 5-7. The inactive ingredients include water, propylene glycol, glycerin, sorbitol, polyoxyl 40 hydrogenated castor oil, flavor, cetylpyridinium chloride, and FD&C blue no. 1. Chlorhexidine gluconate is a salt derived from chlorhexidine and gluconic acid.

Uses and Indications

Chlorhexidine gluconate oral rinse USP, 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 USP, 0.12% therapy should be initiated immediately following dental prophylaxis. The recommended regimen involves oral rinsing twice daily, specifically in the morning and evening, for a duration of 30 seconds after tooth brushing.

The usual dosage is 1/2 fluid ounce (15 mL), which corresponds to one unit-dose cup of undiluted chlorhexidine gluconate oral rinse USP, 0.12%. It is imperative that patients are instructed not to rinse with water or other mouthwashes, brush their teeth, or consume food immediately after using the rinse. Additionally, chlorhexidine gluconate oral rinse USP, 0.12% is not intended for ingestion and should be expectorated following the rinsing process.

Contraindications

Chlorhexidine gluconate oral rinse USP, 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 for whom permanent discoloration of the teeth or oral mucosa is unacceptable, as this may occur with treatment.

Warnings and Precautions

The effect of chlorhexidine gluconate oral rinse USP, 0.12% on periodontitis has not been established. Clinical studies have indicated an increase in supragingival calculus among users of this oral rinse compared to control groups. The potential impact of chlorhexidine gluconate on 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 presenting with both gingivitis and periodontitis, the presence or absence of gingival inflammation following treatment with chlorhexidine gluconate oral rinse USP, 0.12% should not be interpreted as a definitive indicator of underlying periodontitis.

Chlorhexidine gluconate oral rinse USP, 0.12% may cause staining of oral surfaces, including teeth, restorations, and the dorsum of the tongue. Not all patients will experience significant staining; however, clinical testing revealed that 56% of 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. Staining is more pronounced in individuals with higher plaque accumulation, although it 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 necessary.

Caution is advised when prescribing chlorhexidine gluconate oral rinse USP, 0.12% to patients with anterior facial restorations that have rough surfaces or margins. If natural stains cannot be removed from these surfaces during dental prophylaxis, patients may need to be excluded from treatment if permanent discoloration is 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 USP, 0.12%. Rare instances of permanent taste alteration have been reported through postmarketing surveillance.

Side Effects

Patients using chlorhexidine gluconate oral rinse may experience a range of adverse reactions, which can be categorized by frequency and seriousness.

Common side effects include an increase in staining of teeth and other oral surfaces, an increase in calculus formation, and alterations in taste perception. Notably, some patients may experience a permanent alteration in taste perception, as rare instances have been reported through postmarketing surveillance.

Oral irritation and local allergy-type symptoms have been spontaneously reported in association with the use of chlorhexidine gluconate rinse. Additionally, during placebo-controlled adult clinical trials, various oral mucosal side effects were observed, albeit with a frequency of less than 1.0%. These include aphthous ulcers, grossly obvious gingivitis, trauma, ulceration, erythema, desquamation, coated tongue, keratinization, geographic tongue, mucocele, and short frenum.

Postmarketing reports have identified the most frequently reported oral mucosal symptoms as stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, and paresthesia. Minor irritation and superficial desquamation of the oral mucosa have also been noted in patients using the rinse.

Serious adverse reactions include anaphylaxis and other serious allergic reactions, which have been reported during postmarketing use of dental products containing chlorhexidine. Furthermore, cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis) have been documented in patients using chlorhexidine gluconate oral rinse.

Healthcare professionals should monitor patients for these adverse reactions and provide appropriate guidance and management as necessary.

Drug Interactions

Anaphylaxis and serious allergic reactions have been reported in postmarketing use with dental products containing chlorhexidine. Healthcare professionals should be vigilant for signs of hypersensitivity in patients using these products.

No specific drug or laboratory test interactions have been identified in the available data. Therefore, routine monitoring for interactions with other medications or laboratory tests is not indicated 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 USP, 0.12%, have not been established in pediatric patients under the age of 18. Therefore, its use in this population is not recommended until further data are available to support its safety and efficacy.

Geriatric Use

Clinical effectiveness and safety of chlorhexidine gluconate oral rinse USP, 0.12% have not been established in children under the age of 18. However, there are no specific recommendations, dosage adjustments, or safety concerns noted for elderly patients.

Healthcare providers should exercise caution when prescribing this product to geriatric patients, as individual responses may vary. Monitoring for any adverse effects or complications is advisable, given the lack of established data in this population.

Pregnancy

Reproduction studies have been conducted in rats and rabbits at chlorhexidine gluconate doses up to 300 mg/kg/day and 40 mg/kg/day, respectively, without revealing evidence of harm to the fetus. However, adequate and well-controlled studies in pregnant women have not been performed. Therefore, while the drug is classified as Pregnancy Category B, it is important to note that animal reproduction studies are not always predictive of human response. Consequently, chlorhexidine gluconate should be used during pregnancy only if clearly needed, and healthcare professionals should weigh the potential benefits against any possible risks to the fetus.

Lactation

It is not known whether chlorhexidine gluconate oral rinse USP, 0.12% is excreted in human milk. Due to the potential for many drugs to be excreted in human milk, caution should be exercised when administering this product 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 person ingesting 30 mL (2 doses) of the oral rinse per day. However, the relevance of these findings to human breastfeeding is not established.

Renal Impairment

Patients with renal impairment have not been specifically addressed in the available data regarding dosage adjustments, special monitoring, or safety considerations. Therefore, healthcare professionals should exercise caution when prescribing this medication to patients with reduced kidney function, as the lack of information necessitates careful clinical judgment and monitoring.

Hepatic Impairment

Patients with hepatic impairment have not been specifically studied in relation to the use of this medication. Consequently, there are no 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 USP, 0.12% can lead to 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.

In cases where a small child ingests more than 4 ounces of chlorhexidine gluconate oral rinse USP, 0.12%, it is imperative that medical attention is sought immediately. Healthcare professionals should be prepared to assess the child for symptoms of overdosage and provide appropriate management based on the severity of the symptoms presented.

Nonclinical Toxicology

In a drinking water study conducted in rats, no carcinogenic effects were observed at doses up to 38 mg/kg/day. Additionally, mutagenic effects were not detected in two mammalian in vivo mutagenesis studies involving chlorhexidine gluconate. The highest doses administered in these studies included 1000 mg/kg/day in a mouse dominant-lethal assay and 250 mg/kg/day in a hamster cytogenetics test. Furthermore, there was no evidence of impaired fertility 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 most frequently reported oral mucosal symptoms linked to chlorhexidine gluconate oral rinse USP, 0.12% 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 this oral rinse. Reports have also included cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis). Oral irritation and local allergy-type symptoms have been spontaneously reported as side effects associated with the use of chlorhexidine gluconate rinse. Furthermore, rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse USP, 0.12% have been documented through postmarketing product surveillance.

Patient Counseling

Advise patients that chlorhexidine gluconate oral rinse USP, 0.12% has been prescribed by their dentist to treat gingivitis, aiming to reduce gum redness and swelling, as well as to help control gum bleeding. It is essential for patients to use the rinse regularly, as directed by their dentist, in conjunction with daily brushing, and to spit out the rinse after use. Emphasize that the rinse should not be swallowed.

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. Additionally, clarify that chlorhexidine gluconate oral rinse USP, 0.12% should not be used by individuals who have a known sensitivity to it or its components.

Patients should be made aware that the rinse may lead to tooth discoloration and an increase in tartar (calculus) formation, particularly in areas where staining and tartar typically occur. It is important 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.

Caution patients that chlorhexidine gluconate oral rinse USP, 0.12% 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 can alter the taste of foods and beverages; however, this effect typically diminishes with continued use. To reduce taste interference, recommend that patients rinse with chlorhexidine gluconate oral rinse USP, 0.12% after meals and advise them not to rinse with water or other mouthwashes immediately after using the rinse.

Encourage patients to reach out to their dentist, pharmacist, or VistaPharm, Inc. at 1-888-655-1505 if they have any questions or comments regarding chlorhexidine gluconate oral rinse USP, 0.12%. Additionally, patients should be instructed to contact their healthcare provider for medical advice about any side effects and to report side effects to the FDA at 1-800-FDA-1088.

Storage and Handling

The product is supplied in various package configurations, with specific NDC numbers available for identification. It should be stored at a temperature range of 20° to 25°C (68° to 77°F). Temporary excursions are permissible between 15° to 30°C (59° to 86°F), in accordance with USP Controlled Room Temperature guidelines. Proper storage conditions are essential to maintain the integrity and efficacy of the product.

Additional Clinical Information

Chlorhexidine gluconate oral rinse USP, 0.12% should be initiated immediately following dental prophylaxis, with a recommended administration of twice daily for 30 seconds, in the morning and evening after tooth brushing. Patients are advised not to rinse with water or other mouthwashes, brush their teeth, or eat immediately after using the rinse to ensure optimal efficacy.

Clinicians should counsel patients regarding potential side effects, including tooth discoloration and increased tartar formation, particularly in areas prone to staining. Regular dental visits, at least every six months, are essential for the removal of any stain or tartar. Patients should also be informed that the rinse may cause permanent discoloration of some front tooth fillings and may have a bitter taste that can affect the flavor of foods and beverages. To mitigate taste interference, it is recommended to use the rinse after meals. Postmarketing surveillance has reported serious allergic reactions, including anaphylaxis, as well as oral mucosal symptoms such as stomatitis and dry mouth. Additionally, rare cases of permanent taste alteration and parotid gland swelling have been documented.

FDA Insert (PDF)

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

View full prescribing information (PDF)