Chlorhexidine gluconate

Description

Chlorhexidine Gluconate 0.12% Oral Rinse, USP is an oral rinse formulation that contains 0.12% chlorhexidine gluconate, which is chemically defined as 1, 11-hexamethylene bis 5-(p-chlorophenyl) biguanide di-D-gluconate. The formulation includes a base composed of water, 11.6% alcohol, glycerin, PEG-40 sorbitan diisostearate, peppermint flavor, sodium saccharin, and FD&C Blue No. 1. Chlorhexidine gluconate is a salt derived from chlorhexidine and gluconic acid, presenting a near-neutral pH range of 5-7. The molecular formula of chlorhexidine gluconate is C22H30Cl2N10·2C6H12O7, with a molecular weight of 897. The chemical structure is represented as follows:

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, 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 therapy should be initiated immediately following dental prophylaxis. The recommended dosage is 15 mL (1 tablespoon) of undiluted chlorhexidine gluconate oral rinse, to be used twice daily. Patients should perform oral rinsing for 30 seconds in the morning and evening, after brushing their teeth.

It is essential to instruct patients not to rinse with water or other mouthwashes, brush their teeth, or consume food immediately after using the oral rinse. Chlorhexidine gluconate oral rinse is not intended for ingestion; patients should expectorate the solution after rinsing.

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 due to the potential for allergic responses.

Warnings and Precautions

The effect of chlorhexidine gluconate oral rinse on periodontitis has not been established. Healthcare professionals should be aware that clinical testing has indicated an increase in supragingival calculus among users of chlorhexidine gluconate oral rinse compared to control users. However, it remains unclear whether the use of this oral rinse contributes to an increase in subgingival calculus.

To mitigate the potential accumulation of calculus, it is recommended that calculus deposits be removed through dental prophylaxis at intervals not exceeding six months.

Additionally, healthcare providers should exercise caution, as anaphylaxis and serious allergic reactions have been reported in postmarketing experiences with dental products containing chlorhexidine. Monitoring for signs of hypersensitivity is advised, and appropriate measures should be taken should such reactions occur.

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 an alteration 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, paresthesia, minor irritation, superficial desquamation of the oral mucosa, parotid gland swelling, and inflammation of the salivary glands (sialadenitis).

Warnings associated with the use of chlorhexidine gluconate oral rinse include the potential for anaphylaxis and serious allergic reactions, which have been documented during postmarketing use of dental products containing chlorhexidine.

Precautions should be taken as some patients may experience alterations in taste perception during treatment. Rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse have also been reported through post-marketing product surveillance.

Drug Interactions

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

Currently, there are no specific drug or laboratory test interactions identified in the available data. Therefore, routine monitoring for drug interactions or laboratory test interference is not indicated at this time.

Packaging & NDC

The table below lists all NDC Code configurations of Chlorhexidine Gluconate 0.12% Oral Rinse, 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. Caution is advised when administering this product to children, as ingestion of 1 or 2 ounces by a small child (approximately 10 kg body weight) may lead to gastric distress, including nausea, or signs of alcohol intoxication. If a small child ingests more than 4 ounces of chlorhexidine gluconate oral rinse or exhibits signs of alcohol intoxication, medical attention should be sought immediately.

Geriatric Use

Elderly patients may experience specific considerations 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, which underscores the need for caution in geriatric populations.

When administering chlorhexidine gluconate oral rinse to elderly patients, healthcare providers should be vigilant regarding potential side effects. Common adverse reactions include an increase in staining of teeth and other oral surfaces, heightened calculus formation, and alterations in taste perception. Notably, some patients may experience a temporary alteration in taste perception, while rare instances of permanent taste alteration have been reported through post-marketing surveillance.

Additionally, elderly patients may report oral irritation and local allergy-type symptoms, which have been spontaneously documented. Minor irritation and superficial desquamation of the oral mucosa are also noted side effects associated with the use of this rinse. Furthermore, there have been cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis) linked to chlorhexidine gluconate oral rinse use.

Given these considerations, healthcare providers should exercise caution and monitor elderly patients closely for any adverse effects during treatment with chlorhexidine gluconate oral rinse. Adjustments to the treatment regimen may be necessary based on individual patient responses and tolerability.

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, adequate and well-controlled studies in pregnant women have not been performed. 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 human 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 (2 tablespoons) of the oral rinse per day.

Renal Impairment

Patients with renal impairment have not been specifically addressed in the available prescribing information. There are no dosage adjustments, special monitoring requirements, or safety considerations outlined for individuals with reduced kidney function. Healthcare professionals should exercise caution and consider the lack of data when prescribing to 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 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

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 reveal 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. Due to the limitations of animal reproduction studies in predicting human responses, the use of this drug during pregnancy should be considered only when clearly necessary.

In studies assessing 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 tablespoons) of the oral rinse daily.

Carcinogenicity was evaluated in a drinking water study in rats, where no carcinogenic effects were observed at doses up to 38 mg/kg/day. Additionally, mutagenicity was assessed in two mammalian in vivo mutagenesis studies, with no mutagenic effects detected. 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 oral mucosal symptoms frequently noted are stomatitis, gingivitis, glossitis, ulcers, 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 post-marketing product surveillance.

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.

Healthcare providers should advise patients that chlorhexidine gluconate oral rinse therapy should be initiated directly following a dental prophylaxis. Patients using this oral rinse should be reevaluated and provided with a thorough prophylaxis at intervals no longer than six months. The recommended usage is twice daily oral rinsing for 30 seconds, both in the morning and evening after tooth brushing, with a usual dosage of 15 ml (1 tablespoon) of undiluted chlorhexidine gluconate oral rinse.

Patients should be made aware 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 not all patients will experience a visually significant increase in tooth staining, and such staining does not adversely affect the health of the gingivae or other oral tissues. Stains resulting from the use of chlorhexidine gluconate oral rinse can typically be removed from most tooth surfaces through conventional professional prophylactic techniques.

Healthcare providers should exercise discretion 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 by dental prophylaxis, patients should be excluded from treatment with chlorhexidine gluconate oral rinse if permanent discoloration is unacceptable.

Additionally, some patients may experience an alteration in taste perception while undergoing treatment with chlorhexidine gluconate oral rinse. Rare instances of permanent taste alteration following the use of this rinse have been reported through post-marketing product surveillance. Caution should be exercised when administering chlorhexidine gluconate oral rinse to nursing women.

Storage and Handling

The product is supplied in original containers or amber glass bottles. It should be stored at a temperature range of 20°C to 25°C (68°F to 77°F), with permissible excursions between 15°C to 30°C (59°F to 86°F). It is essential to keep the product out of reach of children to ensure safety.

Additional Clinical Information

Chlorhexidine gluconate oral rinse therapy should be initiated immediately following dental prophylaxis, with a recommended administration of 15 ml (1 tablespoon) of undiluted rinse twice daily for 30 seconds, ideally 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.

Clinicians should inform patients that chlorhexidine gluconate oral rinse may cause staining of oral surfaces, including teeth, restorations, and the dorsum of the tongue. Some patients may also experience alterations in taste perception during treatment. Caution is advised when administering this rinse to nursing women. Postmarketing reports have indicated serious allergic reactions, including anaphylaxis, and rare cases of permanent taste alteration. Common oral mucosal symptoms reported include stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, and paresthesia.

FDA Insert (PDF)

This document is the official FDA-approved prescribing information for Chlorhexidine Gluconate 0.12% Oral Rinse as submitted by Chartwell RX, LLC. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)