Chlorhexidine gluconate

Description

0.12% chlorhexidine gluconate (CHG) is an oral rinse formulated with 1,1'-hexamethylene bis 5-(p-chlorophenyl) biguanide di-D-gluconate. The product is presented in a base that includes water, 11.6% alcohol, glycerin, PEG-40 sorbitan diisostearate, flavor, sodium saccharin, and FD&C Blue No.1. This formulation results in a near neutral solution with a pH range of 5 to 7. Chlorhexidine gluconate is characterized as a salt derived 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. This condition is characterized by redness and swelling of the gingivae, including gingival bleeding upon probing.

Chlorhexidine gluconate oral rinse has not been tested in patients with acute necrotizing ulcerative gingivitis (ANUG). For patients presenting with coexisting gingivitis and periodontitis, healthcare professionals are advised to refer to the relevant precautions.

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 of undiluted chlorhexidine gluconate oral rinse, which is to be administered twice daily. Patients should perform oral rinsing for 30 seconds in the morning and evening, ideally 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; therefore, patients must 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.

Additionally, the use of this oral rinse is not recommended for patients who find permanent discoloration of anterior facial restorations with rough surfaces or margins unacceptable, as this may occur with treatment.

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 impact of chlorhexidine gluconate oral rinse 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 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 gluconate oral rinse 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 stain, 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 through conventional professional prophylactic techniques. 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 by dental prophylaxis, patients may need to be excluded from treatment if permanent discoloration is deemed unacceptable.

Some patients may experience alterations in taste perception during treatment with chlorhexidine gluconate oral rinse. Rare cases 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 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, 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, while some patients may experience an alteration in taste perception during treatment, rare instances of permanent taste alteration have also been reported through post-marketing product surveillance.

Drug Interactions

Chlorhexidine gluconate oral rinse is associated with several interactions and effects that warrant consideration during its use.

Oral Surface Staining and Discoloration Chlorhexidine gluconate oral rinse has been observed to cause staining of oral surfaces, including tooth surfaces, restorations, and the dorsum of the tongue. Users may also experience an increase in supragingival calculus compared to control groups. Additionally, there is a potential for permanent discoloration of certain front-tooth fillings.

Alteration in Taste Perception Patients using chlorhexidine gluconate oral rinse may experience alterations in taste perception. While most changes are temporary, rare cases of permanent taste alteration have been reported through post-marketing surveillance.

Caution in Nursing Women Caution is advised when administering chlorhexidine gluconate oral rinse to nursing women, as the excretion of this drug in human milk has not been established. Monitoring for any adverse effects in both the mother and infant is recommended during treatment.

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 until further data are available to support its efficacy and safety profile in children and adolescents.

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, which underscores the need for caution in geriatric populations.

When prescribing chlorhexidine gluconate oral rinse to elderly patients, particularly those with anterior facial restorations that have rough surfaces or margins, discretion is advised. There is a potential for increased staining of teeth and other oral surfaces, especially in patients with heavier accumulations of unremoved plaque. Therefore, monitoring for oral hygiene and plaque control is recommended.

Elderly patients may also experience alterations in taste perception during treatment. While most changes are temporary, rare instances of permanent taste alteration have been reported through post-marketing surveillance. Additionally, oral irritation and local allergy-type symptoms have been spontaneously reported as side effects associated with the use of this rinse.

Healthcare providers should remain vigilant for signs of anaphylaxis and serious allergic reactions, which have been documented during postmarketing use of dental products containing chlorhexidine. Given these considerations, careful monitoring and appropriate dose modifications may be necessary to ensure the safety and efficacy of chlorhexidine gluconate oral rinse in geriatric 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 responses, 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 (2 capfuls) of the oral rinse per day.

Renal Impairment

There is no specific information 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 in small children can lead to significant adverse effects. 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’s condition and provide appropriate management based on the severity of 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 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 informed that chlorhexidine gluconate oral rinse has been prescribed by their dentist to treat gingivitis, aiming to reduce gum redness and swelling while helping to control gum bleeding. It is essential for patients to use the oral rinse regularly, as directed by their dentist, and to continue their daily brushing routine.

Patients must be advised to spit out the rinse after use, as chlorhexidine gluconate oral rinse should not be swallowed. They should be made aware of the potential for allergic reactions, which may include symptoms such as skin rash, itching, generalized swelling, breathing difficulties, lightheadedness, rapid heart rate, upset stomach, or diarrhea. In such cases, patients should seek medical attention immediately.

It is important to inform patients that chlorhexidine gluconate oral rinse is contraindicated for individuals with a known sensitivity to it or its components. Patients should also be made aware that the rinse may cause tooth discoloration or an increase in tartar (calculus) formation, particularly in areas where staining and tartar typically occur. Regular dental visits for the removal of any stain or tartar are recommended at least every six months, or more frequently if advised by their dentist.

Patients should be cautioned that chlorhexidine gluconate oral rinse may lead to 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.

Additionally, patients may experience a bitter taste from the rinse, which can affect the taste of food and beverages. This taste interference is likely to diminish with continued use. To mitigate this effect, patients should be advised to rinse with chlorhexidine gluconate oral rinse after meals and to avoid rinsing with water or other mouthwashes immediately afterward.

For any questions or concerns regarding chlorhexidine gluconate oral rinse, patients should be encouraged to contact their dentist, pharmacist, or Xttrium Laboratories, Inc. at 1-800-587-3721. Patients should also be instructed to call their healthcare provider for medical advice regarding side effects and to report any adverse 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 upon request. 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 and 30°C (59°F to 86°F) in accordance with USP controlled room temperature guidelines. Proper container requirements must be adhered to, and special handling needs should be observed to maintain product integrity.

Additional Clinical Information

Patients using chlorhexidine gluconate oral rinse are advised to perform a twice daily oral rinse for 30 seconds, both in the morning and evening, after brushing their teeth. It is crucial that patients do not rinse with water, other mouthwashes, brush their teeth, or eat immediately after using the rinse.

Clinicians should counsel patients to seek immediate medical attention if they experience allergic symptoms such as skin rash, itching, swelling, breathing difficulties, lightheadedness, rapid heart rate, upset stomach, or diarrhea. Patients may experience tooth discoloration and increased tartar formation, particularly in areas prone to staining. Regular dental visits for stain and tartar removal are recommended, and patients should maintain good oral hygiene practices to minimize discoloration. Additionally, chlorhexidine gluconate may impart a bitter taste and affect the taste of food and beverages, though this typically diminishes with continued use. Postmarketing reports have indicated rare occurrences of serious allergic reactions, permanent taste alteration, and various oral mucosal symptoms, including stomatitis and gingivitis, as well as parotid gland swelling and sialadenitis.

FDA Insert (PDF)

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

View full prescribing information (PDF)