Chlorhexidine gluconate

Description

This product is an oral rinse formulated with 0.12% chlorhexidine gluconate (1,1'-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 oil, saccharin sodium, and FD&C Blue #1. The pH of the solution is maintained within a near-neutral range of 5 to 7, with adjustments possible using hydrochloric acid or sodium hydroxide. Chlorhexidine gluconate, a salt of chlorhexidine and gluconic acid, has a molecular formula of C22H30Cl2N10•2C6H12O7 and a molecular weight of 897.77. The structural formula is provided as part of the product specifications.

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 of undiluted chlorhexidine gluconate oral rinse, which should be administered twice daily. Patients are advised to perform oral rinsing for 30 seconds in the morning and evening, following their toothbrushing routine.

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. Additionally, chlorhexidine gluconate oral rinse is not intended for ingestion; patients should expectorate the solution after rinsing.

Contraindications

This product is contraindicated in individuals with a known hypersensitivity to chlorhexidine gluconate or any other ingredients in the formulation.

Additionally, the use of chlorhexidine gluconate is not recommended for patients for whom permanent discoloration of anterior facial restorations is unacceptable.

Warnings and Precautions

The effect of chlorhexidine gluconate on periodontitis remains undetermined. Clinical studies have indicated an increase in supragingival calculus among users of chlorhexidine gluconate oral rinse compared to control groups. However, it is not established whether chlorhexidine gluconate contributes to an increase in subgingival calculus. 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 potential adverse reactions.

For patients presenting with coexisting gingivitis and periodontitis, the presence or absence of gingival inflammation following treatment with chlorhexidine gluconate should not be relied upon as a primary indicator of underlying periodontitis.

Chlorhexidine gluconate oral rinse may lead to 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 chlorhexidine gluconate users exhibited a measurable increase in facial anterior stain after six months, compared to 35% of control users. Furthermore, 15% of chlorhexidine gluconate users developed what was classified as heavy staining, in contrast to only 1% of control users. Staining is more pronounced in individuals with higher plaque accumulation.

It is important to note that staining resulting from chlorhexidine gluconate use 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 thorough cleaning.

Caution is advised when prescribing chlorhexidine gluconate to patients with anterior facial restorations that have rough surfaces or margins. If natural stains cannot be effectively removed from these surfaces during dental prophylaxis, patients may need to be excluded from treatment with chlorhexidine gluconate if they find permanent discoloration unacceptable. Stains in these areas may be challenging to remove and, in rare cases, could necessitate the replacement of restorations.

Some patients may experience alterations in taste perception while using chlorhexidine gluconate oral rinse. There have been rare reports of permanent taste alterations following treatment, as noted in postmarketing surveillance.

No specific laboratory tests are recommended for monitoring the use of chlorhexidine gluconate oral rinse. Healthcare professionals should exercise clinical judgment and discretion when considering treatment options for their patients.

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 alterations in taste perception.

In clinical trials, oral mucosal side effects were reported in less than 1.0% 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 alterations in taste perception during treatment, rare instances of permanent taste alteration following use have also been documented.

Drug Interactions

Anaphylaxis and serious allergic reactions 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 on periodontitis remains undetermined. Clinicians are advised to consider this uncertainty when interpreting laboratory test results related to periodontal health and to monitor patients accordingly.

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 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 have not been established in children under the age of 18. While there are no specific geriatric use recommendations or dosage adjustments provided, it is important to note that no safety concerns or special precautions for elderly patients are explicitly stated in the prescribing information.

Healthcare providers should continue to monitor geriatric patients as they would with any other population, ensuring that treatment is appropriate based on individual patient needs and responses.

Pregnancy

Pregnancy category B. 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. Due to the limitations of animal reproduction studies in predicting human response, this drug 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 medication in pregnant patients.

Lactation

It is not known whether this drug 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 to lactating mothers.

In 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 chlorhexidine gluconate oral rinse per day.

Renal Impairment

Patients with renal impairment may not have specific information regarding dosage adjustments, special monitoring, or safety considerations outlined in the prescribing information. Therefore, healthcare professionals should exercise caution and consider individual patient factors when prescribing to patients with reduced kidney function. Regular monitoring of renal function is advisable to ensure safe and effective use of the medication in this population.

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 considered as part of standard clinical practice.

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 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, 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 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 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 and an increase in tartar (calculus) formation, particularly in areas where stains and tartar typically accumulate. Regular dental visits for the removal of stains and tartar are recommended at least every six months, or more frequently if advised by their dentist. 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 maintain a daily brushing and flossing routine, paying special attention to areas that begin to show discoloration. It is also important to inform patients that the rinse may have a bitter taste and can alter the taste of foods and beverages, although this effect typically diminishes with continued use. To reduce taste interference, patients should be advised to use the rinse after meals and to refrain from rinsing with water or other mouthwashes immediately afterward.

Patients should feel free to reach out to their dentist or pharmacist with any questions or comments regarding Chlorhexidine Gluconate Oral Rinse. They should also be instructed to contact their healthcare provider for medical advice concerning any side effects experienced. Side effects can be reported to the FDA at 1-800-FDA-1088. Lastly, it is crucial to remind patients to keep this and all medications out of the reach of children.

Storage and Handling

The product is supplied in its original container or in amber glass bottles. It should be stored at a temperature range of 20°-25°C (68°-77°F), with permissible excursions between 15°-30°C (59°-86°F) as defined by USP Controlled Room Temperature guidelines. Proper adherence to these storage conditions is essential to maintain the integrity and efficacy of the product.

Additional Clinical Information

Patients using chlorhexidine gluconate oral rinse are advised to perform a twice daily oral rinse for 30 seconds, using 15 mL of the undiluted solution, ideally after tooth brushing in the morning and evening. It is crucial that patients do not rinse with water, use other mouthwashes, brush their teeth, or eat immediately after using the rinse.

Clinicians should counsel patients on potential allergic reactions, including symptoms such as skin rash, difficulty breathing, and rapid heart rate, which require immediate medical attention. Patients may experience tooth discoloration and increased tartar formation, necessitating dental visits for removal at least every six months. To minimize discoloration, daily brushing and flossing are recommended, particularly in areas prone to staining. Additionally, the rinse may impart a bitter taste that can affect the flavor of foods and beverages, though this typically diminishes with continued use. Reports from postmarketing experience indicate that serious allergic reactions, including anaphylaxis, as well as oral mucosal symptoms like stomatitis and dry mouth, have occurred. Cases of parotid gland swelling and sialadenitis have also been documented.

FDA Insert (PDF)

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

View full prescribing information (PDF)