Chlorhexidine gluconate

Description

Paroex® 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 of deionized water, propylene glycol, glycerin, polyoxyl 40 hydrogenated castor oil, mint flavor, potassium acesulfame, FD&C Red #40, and D&C Red #33. Paroex® is characterized as a near-neutral solution, with a pH range of 5 to 7. Chlorhexidine gluconate serves as a salt of chlorhexidine and gluconic acid.

Uses and Indications

Paroex (Chlorhexidine Gluconate Oral Rinse USP, 0.12%) 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

Paroex (Chlorhexidine Gluconate Oral Rinse USP, 0.12%) therapy should be initiated immediately following dental prophylaxis. The recommended dosing regimen is twice daily, with oral rinsing for 30 seconds in the morning and evening, after tooth brushing. The usual dosage is 15 mL (½ FL OZ) of undiluted Paroex.

Patients must be instructed to avoid rinsing with water or other mouthwashes, brushing their teeth, or eating immediately after using Paroex. It is important to note that Paroex is not intended for ingestion; patients should expectorate the rinse after use.

Contraindications

Paroex® 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 severe allergic reactions.

Warnings and Precautions

The effect of Paroex® 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 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. Additionally, there have been reports of anaphylaxis and serious allergic reactions associated with the use of dental products containing chlorhexidine.

For patients with concurrent gingivitis and periodontitis, the presence or absence of gingival inflammation following treatment with Paroex® 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 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 likely to occur in patients with substantial plaque accumulation. Importantly, staining does not adversely affect the health of the gingiva or other oral tissues and can typically be removed through standard professional prophylactic techniques, although additional time may be required. Caution is advised when prescribing 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 Paroex® treatment if they find permanent discoloration unacceptable. In rare cases, staining in these areas may be difficult to eliminate and could necessitate the replacement of restorations.

Patients may also experience alterations in taste perception while using Paroex®. There have been rare reports of permanent taste alterations following the use of chlorhexidine gluconate oral rinse, as noted in post-marketing surveillance.

No specific laboratory tests are recommended for monitoring during the use of Paroex®.

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. Notably, clinical data indicate that 56% of users exhibited a measurable increase in facial anterior stain, with 15% developing what was considered heavy staining. Additionally, some patients may experience alterations in taste perception, with rare instances of permanent taste alteration reported.

Oral mucosal side effects have been observed during placebo-controlled adult clinical trials, with a frequency of less than 1.0%. These include aphthous ulcers, grossly obvious gingivitis, trauma, ulceration, erythema, desquamation, coated tongue, keratinization, geographic tongue, mucocele, and short frenum.

Postmarketing experiences have revealed further oral mucosal adverse reactions, including 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).

Serious adverse reactions, such as anaphylaxis and other serious allergic reactions, have been reported during postmarketing use of dental products containing chlorhexidine. These reactions necessitate careful monitoring and consideration in patients using these products.

Drug Interactions

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

No specific drug or laboratory test interactions have been identified in the available data. Therefore, routine monitoring for interactions with other medications or laboratory tests is not indicated at this time.

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 Paroex® have not been established in pediatric patients under the age of 18. Therefore, caution is advised when considering the use of this medication in this population.

Geriatric Use

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

Healthcare providers should continue to monitor geriatric patients as they would with any other demographic, considering individual patient factors and clinical judgment when prescribing Paroex.

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, 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 chlorhexidine gluconate in pregnant patients.

Lactation

It is not known whether Paroex® oral rinse is excreted in human milk. Due to the potential for many drugs to be excreted in breast milk, caution should be exercised when administering this product 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 doses) of chlorhexidine gluconate 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 Paroex® (Chlorhexidine Gluconate Oral Rinse USP, 0.12%) can lead to 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.

In cases where a small child ingests more than 4 ounces of Paroex®, it is imperative to seek medical attention promptly. Healthcare professionals should be prepared to assess the child for potential symptoms and provide appropriate management based on the severity of the situation. Monitoring and supportive care may be necessary to address any complications arising from the overdosage.

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 a drinking water study involving 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 with 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 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. Reports of anaphylaxis and serious allergic reactions have been documented. Additionally, oral irritation and local allergy-type symptoms have been spontaneously reported in association with chlorhexidine gluconate rinse.

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. Minor irritation and superficial desquamation of the oral mucosa have also been noted in patients using this rinse.

Furthermore, cases of parotid gland swelling and inflammation of the salivary glands (sialadenitis) have been reported. Rare instances of permanent taste alteration following the use of chlorhexidine gluconate oral rinse have been observed through post-marketing product surveillance.

Patient Counseling

Advise patients that Paroex has been prescribed by their dentist to treat gingivitis, specifically to help reduce the redness and swelling of their gums and to assist in controlling any gum bleeding. It is essential for patients to use Paroex regularly, as directed by their dentist, in conjunction with daily brushing and flossing.

Instruct patients to spit out the rinse after use, emphasizing that Paroex should not be swallowed. Patients should be made aware of the potential for allergic reactions; they must seek immediate medical attention if they experience symptoms such as skin rash, itching, generalized swelling, breathing difficulties, lightheadedness, rapid heart rate, upset stomach, or diarrhea.

Inform patients that Paroex is contraindicated for individuals with a known sensitivity to it or its components. Additionally, patients should be counseled that the use of Paroex may lead to tooth discoloration or an increase in tartar (calculus) formation, particularly in areas where stains and tartar typically accumulate. It is important for patients to see their dentist for the removal of any stain or tartar at least every six months, or more frequently if advised by their dentist, as both can be effectively removed by a dentist or hygienist.

Patients should be made aware 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.

Discuss with patients that Paroex may have a bitter taste and can alter the taste of foods and beverages, although this effect typically diminishes with continued use. To mitigate taste interference, recommend that patients rinse with Paroex after meals and avoid rinsing with water or other mouthwashes immediately afterward.

Encourage patients to reach out to their dentist, pharmacist, or Lohxa, LLC at 1-800-641-5564 or via email at info@lohxa.com if they have any questions or comments regarding Paroex. Remind patients to contact their healthcare provider for medical advice about any side effects they may experience, and inform them that side effects can also be reported to the FDA at 1-800-FDA-1088.

Storage and Handling

The product is supplied in accordance with the following specifications. 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), as defined by USP controlled room temperature guidelines.

Proper storage conditions are essential to maintain the integrity of the product. It is recommended that the product be kept in a suitable container that protects it from environmental factors. Special handling requirements should be observed to ensure the product remains within the specified temperature range throughout its storage period.

Additional Clinical Information

The recommended administration of Paroex involves oral rinsing twice daily for 30 seconds, ideally in the morning and evening after tooth brushing. Patients should be counseled to avoid rinsing with water or other mouthwashes, brushing teeth, or eating immediately after use to ensure optimal efficacy. To minimize the medicinal taste, it is advised not to rinse with water right after using Paroex.

Patients may experience tooth discoloration and increased tartar formation, particularly in areas prone to staining. Regular dental visits for stain and tartar removal are essential, ideally every six months or as advised by a dentist. Additionally, chlorhexidine gluconate oral rinse may cause permanent discoloration of some front-tooth fillings. Patients should maintain good oral hygiene practices, including daily brushing and flossing, to mitigate discoloration. Some individuals may find the taste of Paroex bitter, which may affect the taste of foods and beverages, although this typically diminishes with continued use.

Postmarketing surveillance has reported serious allergic reactions, including anaphylaxis, and rare cases of permanent taste alteration. Common oral mucosal symptoms associated with chlorhexidine gluconate include stomatitis, gingivitis, glossitis, ulcers, dry mouth, hypesthesia, glossal edema, and paresthesia. Instances of parotid gland swelling and sialadenitis have also been documented in patients using this oral rinse.

FDA Insert (PDF)

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

View full prescribing information (PDF)