Chlorhexidine

Description

Chlorhexidine Gluconate Oral Rinse, 0.12% is an oral rinse formulation that contains 0.12% chlorhexidine gluconate (1,1-hexamethylene bis 5-(p-chlorophenyl) biguanidedi-D-gluconate). The product is presented in a base comprising 11.6% alcohol, FD&C Blue No. 1, glycerin, peppermint flavor, polysorbate 80, purified water, and saccharin sodium. This oral rinse is characterized as a near-neutral solution, with a pH range of 5 to 7. Chlorhexidine gluconate is a salt derived from chlorhexidine and gluconic acid, with the chemical structure represented as 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. This condition is characterized by redness and swelling of the gingivae, including gingival bleeding upon probing.

Chlorhexidine gluconate oral rinse, 0.12%, 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 guidance.

Dosage and Administration

Chlorhexidine gluconate oral rinse, 0.12% therapy should be initiated immediately following dental prophylaxis. The recommended regimen involves oral rinsing twice daily for 30 seconds, specifically in the morning and evening after tooth brushing. The usual dosage is 15 mL of undiluted chlorhexidine gluconate oral rinse, 0.12%.

Patients must be instructed to avoid rinsing with water or other mouthwashes, brushing their teeth, or consuming food immediately after using the chlorhexidine gluconate oral rinse, 0.12%. It is important to note that this product is not intended for ingestion; patients should expectorate the rinse after use.

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 product is not recommended for patients who find permanent discoloration of anterior facial restorations unacceptable, as this may occur with treatment.

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 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 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, 0.12%, may cause staining of oral surfaces, including teeth, restorations, and the dorsum of the tongue. While not all patients will experience significant staining, clinical data show 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.

It is important to note that staining from chlorhexidine gluconate oral rinse 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. 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 during dental prophylaxis, patients may need to be excluded from treatment with chlorhexidine gluconate oral rinse if permanent discoloration is unacceptable. In rare cases, difficult-to-remove stains may necessitate the replacement of restorations.

Patients may also experience alterations in taste perception during treatment with chlorhexidine gluconate oral rinse. There have been rare reports of permanent taste alterations following its use, as noted in 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 an alteration in taste perception. The alteration in taste perception may be temporary; however, rare instances of permanent taste alteration have been reported through postmarketing surveillance.

In clinical trials, several oral mucosal side effects were reported among participants, including aphthous ulcers, grossly obvious gingivitis, trauma, ulceration, erythema, desquamation, coated tongue, keratinization, geographic tongue, mucocele, and short frenum. Each of these occurred at a frequency of less than 1%.

Postmarketing experience has revealed additional oral mucosal symptoms that are frequently reported, such as stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, paresthesia, and minor irritation and superficial desquamation of the oral mucosa. There have also been cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis).

Serious adverse reactions include anaphylaxis and other serious allergic reactions, which have been documented during postmarketing use of dental products containing chlorhexidine.

Healthcare providers should monitor patients for these adverse reactions and provide appropriate guidance regarding the use of chlorhexidine gluconate oral rinse.

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.

The effect of chlorhexidine gluconate oral rinse, 0.12%, 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 efficacy and any potential adverse effects.

Packaging & NDC

The table below lists all NDC Code configurations of Chlorhexidine (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

Clinical effectiveness and safety of chlorhexidine gluconate oral rinse, 0.12%, have not been established in children under the age of 18. While there are no specific recommendations for geriatric patients, it is important to consider that the absence of established safety and efficacy data in younger populations does not directly imply similar outcomes in elderly patients.

Healthcare providers should exercise caution when prescribing this oral rinse to geriatric patients, particularly in the context of their overall health status and potential comorbidities. Monitoring for any adverse effects or complications is advisable, as elderly patients may have different responses to treatment compared to younger populations.

Currently, there are no dosage adjustments or specific safety concerns outlined for geriatric use; however, clinical judgment should guide the use of this product in 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 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, 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 these patients to ensure safety and efficacy.

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 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 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 at chlorhexidine gluconate doses of up to 300 mg/kg/day and 40 mg/kg/day, respectively, did not reveal 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 always predict human responses, the use of this drug during pregnancy should be considered only when clearly necessary.

In terms of animal pharmacology and toxicology, a drinking water study in rats indicated that carcinogenic effects were not 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 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 observed 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. Reports of anaphylaxis and serious allergic reactions have been documented.

Among the oral mucosal symptoms frequently reported in association with chlorhexidine gluconate oral rinse are stomatitis, gingivitis, glossitis, ulceration, dry mouth, hypesthesia, glossal edema, and paresthesia. Additionally, minor irritation and superficial desquamation of the oral mucosa have been observed in some patients.

Cases of parotid gland swelling and inflammation of the salivary glands, known as sialadenitis, have also been reported in patients using chlorhexidine gluconate oral rinse. Furthermore, rare instances of permanent taste alteration following the use of this oral rinse have been noted through postmarketing product surveillance.

Patient Counseling

Patients should be informed 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. It is essential for patients to use the oral rinse regularly as directed by their dentist, in conjunction with daily brushing. Patients should be advised to spit out the rinse after use and to avoid swallowing it.

Healthcare providers should counsel 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. It is important to note 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. Regular dental visits for the removal of any stain or tartar are crucial, with a recommendation to see the dentist at least every six months, or more frequently if advised. Both stains and tartar can be effectively removed by a dentist or hygienist.

Additionally, patients should be informed 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 chlorhexidine gluconate oral rinse has a bitter taste and can alter the taste of foods and beverages. This taste interference is generally less noticeable 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 or pharmacist. In the event of side effects, patients should call their doctor for medical advice and may report side effects to Pharmaceutical Associates, Inc. at 1-800-845-8210 or to the FDA at 1-800-FDA-1088 or via www.fda.gov/medwatch.

Storage and Handling

The product is supplied in a bottle as provided or in an amber plastic bottle equipped with a child-resistant closure. 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 ensure safety.

Additional Clinical Information

Chlorhexidine gluconate oral rinse, 0.12%, is indicated for the treatment of gingivitis, aiding in the reduction of gum redness, swelling, and bleeding. The recommended administration involves initiating therapy immediately after dental prophylaxis, with a usual dosage of 15 mL of undiluted rinse, used twice daily for 30 seconds, in the morning and evening following tooth brushing. Patients should avoid rinsing with water or other mouthwashes, brushing teeth, or eating immediately after use to ensure optimal efficacy.

Clinicians should counsel patients on potential side effects, including allergic reactions such as skin rash, swelling, and breathing difficulties, which require immediate medical attention. Patients may experience tooth discoloration and increased tartar formation, particularly in areas prone to staining, which can be managed by dental professionals. Additionally, chlorhexidine may cause permanent discoloration of some front-tooth fillings and may impart a bitter taste, affecting the flavor of foods and beverages. To mitigate taste interference, it is advisable to use the rinse after meals. Postmarketing reports have indicated rare occurrences of anaphylaxis, serious allergic reactions, and permanent taste alterations, along with various oral mucosal symptoms and salivary gland issues.

FDA Insert (PDF)

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

View full prescribing information (PDF)