Chlorhexidine gluconate

Description

Chlorhexidine gluconate oral rinse is formulated to contain 0.12% chlorhexidine gluconate, which is chemically defined as 1,11-hexamethylene bis5-(p-chlorophenyl) biguanide di-D-gluconate. The product is presented in a base that includes water, 11.6% alcohol, glycerin, PEG-40 sorbitan diisostearate, flavoring agents, sodium saccharin, and FD&C Blue No.1. This oral rinse is characterized as a near neutral solution, with a pH range of 5 to 7. Chlorhexidine gluconate itself is a salt formed from chlorhexidine and gluconic acid.

Uses and Indications

Chlorhexidine gluconate oral rinse 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 drug has not been tested in patients with acute necrotizing ulcerative gingivitis (ANUG). For patients presenting with coexisting gingivitis and periodontitis, refer to the PRECAUTIONS section for additional guidance.

Dosage and Administration

Chlorhexidine gluconate oral rinse therapy should be initiated immediately following dental prophylaxis. The recommended dosage is 15 mL of undiluted chlorhexidine gluconate oral rinse, which is marked in the cap. Patients are advised to use the rinse twice daily, specifically in the morning and evening, for a duration of 30 seconds after brushing their teeth.

It is essential that patients do not rinse with water or other mouthwashes, brush their teeth, or consume food immediately after using the chlorhexidine gluconate oral rinse. Additionally, healthcare professionals should emphasize that the rinse is not intended for ingestion and must be expectorated following use.

Contraindications

Chlorhexidine gluconate oral rinse is contraindicated in individuals with a known hypersensitivity to chlorhexidine gluconate or any other ingredients in the formulation. Use in these patients may lead to adverse reactions.

Warnings and Precautions

The effect of chlorhexidine gluconate oral rinse 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 oral rinse 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 users exhibited a measurable increase in facial anterior stain after six months, compared to 35% of control users. Furthermore, 15% of chlorhexidine gluconate oral rinse users developed what was classified as heavy staining, in contrast to only 1% of control users.

Staining is more pronounced in patients with substantial plaque accumulation. 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 through conventional professional prophylactic techniques, although additional time may be required for completion.

Caution should be exercised when prescribing chlorhexidine gluconate oral rinse 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 with chlorhexidine gluconate oral rinse if they find permanent discoloration 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 post-marketing surveillance. Healthcare professionals should monitor patients for these potential side effects and provide appropriate guidance.

Side Effects

Patients may experience a range of adverse reactions associated with the use of dental products containing chlorhexidine. 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 reports have identified additional adverse reactions, such as stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, and paresthesia. Other observed effects 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 serious allergic reactions, including anaphylaxis, have been reported during postmarketing use of chlorhexidine-containing dental products.

Drug Interactions

Serious allergic reactions, including anaphylaxis, have been reported in postmarketing experiences with dental products containing chlorhexidine. Healthcare professionals should be vigilant for signs of hypersensitivity in patients using these products and take appropriate action if such reactions occur.

Additionally, the impact of chlorhexidine gluconate oral rinse on periodontitis has not been established. Therefore, clinicians should exercise caution when considering its use for this indication and may need to monitor patients closely for any changes in their periodontal condition.

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 have not been established in pediatric patients under the age of 18. Therefore, its use in this population is not recommended. Healthcare professionals should exercise caution when considering this treatment for children and adolescents, as the lack of established data may impact therapeutic decisions.

Geriatric Use

Elderly patients may require special consideration when using chlorhexidine gluconate oral rinse. The clinical effectiveness and safety of this product have not been established in individuals under the age of 18, and caution should be exercised when administering it to nursing women.

In clinical testing, an increase in supragingival calculus was observed among users of chlorhexidine gluconate oral rinse compared to control users. Additionally, there have been reports of anaphylaxis and serious allergic reactions associated with dental products containing chlorhexidine during postmarketing use.

Elderly patients may also experience alterations in taste perception while undergoing treatment with chlorhexidine gluconate oral rinse. Rare instances of permanent taste alteration have been documented through post-marketing surveillance. Other side effects reported include oral irritation and local allergy-type symptoms, as well as minor irritation and superficial desquamation of the oral mucosa.

Furthermore, there have been cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis) in patients using chlorhexidine gluconate oral rinse. Given these potential adverse effects, careful monitoring and consideration of dose modifications may be warranted in geriatric patients.

Pregnancy

Reproduction studies have been conducted in rats and rabbits with chlorhexidine gluconate at doses up to 300 mg/kg/day and 40 mg/kg/day, respectively, and have not demonstrated evidence of harm to the fetus. Based on these findings, chlorhexidine gluconate is classified as Pregnancy Category B. However, it is important to note that adequate and well-controlled studies in pregnant women have not been performed.

Due to the limitations of animal reproduction studies in predicting human outcomes, 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 studies involving parturition and lactation in 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 (2 capfuls) of the oral rinse per day.

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 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 can lead to significant adverse effects, particularly in small children. Specifically, the consumption 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 to seek medical attention promptly. Healthcare professionals should be prepared to assess the child for potential complications 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, 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 most frequently reported oral mucosal symptoms linked to chlorhexidine gluconate oral rinse 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). Oral irritation and local allergy-type symptoms have been spontaneously reported as side effects associated with the use of chlorhexidine gluconate rinse.

Patient Counseling

Patients should be instructed not to rinse with water or other mouthwashes, brush their teeth, or eat immediately after using chlorhexidine gluconate oral rinse. It is important to emphasize that chlorhexidine gluconate oral rinse is not intended for ingestion and should be expectorated after rinsing.

The recommended usage involves rinsing twice daily for 30 seconds, both in the morning and evening, following tooth brushing. The usual dosage is 15 mL, as marked in the cap, of undiluted chlorhexidine gluconate oral rinse. Therapy with chlorhexidine gluconate oral rinse should be initiated directly after a dental prophylaxis.

Healthcare providers should ensure that patients using chlorhexidine gluconate oral rinse are reevaluated and receive a thorough prophylaxis at intervals no longer than six months. It is also important to inform patients that chlorhexidine gluconate oral rinse can cause staining of oral surfaces, including tooth surfaces, restorations, and the dorsum of the tongue. However, it should be noted that staining does not adversely affect the health of the gingivae or other oral tissues, and stains can typically be removed from most tooth surfaces through conventional professional prophylactic techniques.

Patients may experience an alteration in taste perception while undergoing treatment with chlorhexidine gluconate oral rinse. Healthcare providers should make patients aware that rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse have been reported through post-marketing product surveillance.

Caution should be exercised when administering chlorhexidine gluconate oral rinse to nursing women. Additionally, patients should be informed that they may be excluded from treatment with chlorhexidine gluconate oral rinse if permanent discoloration of anterior facial restorations is unacceptable.

Storage and Handling

The product is supplied as a blue liquid in 1-pint (473 mL) amber plastic bottles equipped with child-resistant closures. It should be stored at a temperature range of 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F) in accordance with USP controlled room temperature guidelines.

Additional Clinical Information

Patients using chlorhexidine gluconate oral rinse are advised to rinse twice daily for 30 seconds, both in the morning and evening, after brushing their teeth. The usual dosage is 15 mL of undiluted rinse, and patients should refrain from rinsing with water or other mouthwashes, brushing their teeth, or eating immediately after use. It is important to note that the rinse is not intended for ingestion and should be expectorated.

Clinicians should counsel patients about potential side effects, including staining of oral surfaces such as teeth and the tongue, although not all patients will experience significant staining. Stains can typically be removed through professional dental cleaning, and the staining does not negatively impact the health of the gums or other oral tissues. Some patients may notice changes in taste perception during treatment, with rare reports of permanent taste alteration. Post-marketing surveillance has identified oral mucosal symptoms such as stomatitis, gingivitis, and dry mouth, as well as cases of parotid gland swelling and sialadenitis associated with the use of the rinse.

FDA Insert (PDF)

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

View full prescribing information (PDF)