The options to help patients with oral and perioral pain problems such as neuropathies, burning mouth syndrome, neuromas and neuralgias. Vehicle-carrier agents and bases have been developed that can penetrate the mucosa and cutaneous tissues and transport the active medication to the treatment site. Dentists have been using topical agents with increasing frequency as part of the therapeutic protocol for orofacial painful neuropathy.

Several topical intraoral medications are used in the treatment of oral ulcerations and infections, including antifungals; nonsteroidal anti-inflammatory drugs (NSAIDs); and corticosteroids. Because of their rapid onset and low side-effect profile, topical medications offer a distinct advantage over systemic administration for orofacial disorders. Medicated lollipops, lozenges, and adhering powders are ideal for keeping an antibiotic or antifungal in contact with an infected area in the mouth.

Topical Anesthetic Combinations

Topically applied anesthetics provide a degree of anesthesia to non-keratinized tissue (e.g., oral mucous membrane) to a depth of 2 to 3 mms. This permits the initial penetration of mucous membrane to be accomplished painlessly. Topical anesthetics are used in concentrations that are higher than those used when the drug is injected. For example, lidocaine injection is a 2% solution, but when used topically as a gel or ointment it is commonly 5%. Benzocaine, the most commonly used topical anesthetic, is commonly used in a 10 to 20% concentration in a gel, ointment or spray. Flavored topical anesthetics containing prilocaine, lidocaine and tetracaine, with or without phenylephrine, can be prepared by our compounding pharmacists.

Topical Anesthetics -Combinations of your Choice for Specific Needs

Methemoglobinemia (MHb) is a potentially serious blood condition and an uncommon adverse reaction known to be associated with benzocaine. This condition reduces the ability of red blood cells to deliver oxygen throughout the body, which can lead to bluish discoloration of the skin, nausea and fatigue. It can progress to stupor, coma and death. Almost all reported cases of benzocaine-induced MHb were associated with high-concentration preparations (14 percent to 20 percent benzocaine). Compounding pharmacies can formulate low concentration or benzocaine-free topical anesthetics, including combinations of other topical anesthetics such as lidocaine and tetracaine or prilocaine.

Treatment for Recurrent Aphthous Stomatitis

In a clinical randomized crossover trial, minocycline 0.2% and tetracycline 0.25% aqueous oral rinses were assessed in patients with frequent episodes of RAS. Minocycline mouthwashes as compared to topical tetracycline rinses resulted in significantly improved pain control, by reducing the severity and duration of pain. Topical minocycline rinse may be a potential treatment for other non-infectious inflammatory ulcerative oral mucosal diseases.

Topical Sucralfate for Pain after Oral CO2 Laser Surgery

A prospective trial assessed the effect of topical sucralfate on postoperative pain scores and other secondary outcomes including the frequency and duration of analgesic use and postoperative bleeding episodes after CO2 laser treatment of oral leukoplakia.

After surgery, the patient was instructed to rinse his or her mouth with 10 mL of a sucralfate mouthrinse (sucralfate group, n=40), or 10 mL of water without sucralfate (control group, n=40) for 2 minutes and then swallow it, 4 times a day for a period of 7 days. Scores were compared between the 2 groups from the operative day to postoperative day 6. Patients in the sucralfate group experienced significantly less postoperative pain on postoperative days 1 and 2. Although there was no significant difference in frequency and duration of analgesic use between the 2 groups, a trend toward lower frequency and fewer days of analgesic use in the sucralfate group was observed.

Topical sucralfate can be considered a feasible adjuvant medication for the control of pain after CO2 laser treatment of oral leukoplakia.

Dyclonine Topical Anesthetic Solution

Dyclonine HCl 0.5% and 1.0% Topical Solutions are listed in the “Discontinued Drug Product List” section of the Orange Book as Dyclone™ products were NOT withdrawn from commercial manufacture for reasons of safety or effectiveness.Unlike the original product which had an unpleasant taste, compounded dyclonine topical anesthetic solution can be formulated in mint and several other pleasing flavors.

Topical Medication to Treat Orofacial Neuropathic Pain

The Department of Diagnostic Sciences, Division of Orofacial Pain, University of Medicine and Dentistry of New Jersey, Newark, conducted a study to evaluate the effect of topical medications alone or in combination with systemic medications in the treatment of orofacial neuropathic pain conditions. A retrospective chart review was performed for 39 patients who were diagnosed with a neuropathic pain condition such as deafferentation pain, traumatic neuroma, or trigeminal or glossopharyngeal neuralgia, and were treated for orofacial neuropathic pain at the Orofacial Pain Clinic.

The review concluded that topical medication as single treatment or in combination with systemic medications can reduce orofacial neuropathic pain severity.

“The topical medication can be ordered from a compounding pharmacy where it can be formulated to contain carbamazepine 4%, lidocaine 1%, ketoprofen 4%, ketamine 4%, and gabapentin 4%. Carbamazepine and gabapentin ... act by suppressing paroxysmal discharges and reducing neuronal hyperexcitability. Lidocaine, which is a local anesthetic, acts by blocking sodium channels, preventing nerve depolarization.Ketoprofen has anti-inflammatory activity.Last, ketamine blocks N-methyl-D-aspartate (NMDA) receptors, whose hyperactivity contributes to maintenance of neuropathic pain.” The topical preparation should utilize penetration enhancers such as anhydrous gel base and bio-adhesive copolymers. These are used to carry the medication transdermally and transmucosally. “

Update on Burning Mouth Syndrome

Burning mouth syndrome (BMS), also referred to as glossopyrosis or glossodynia (when the burning occurs on the tongue only) is usually described as oral burning pain, sometimes with dysesthetic qualities similar to those present in other neuropathic pain conditions. The dorsal tongue, palate, lips and gingival tissues, individually or in combination, are the most common sites involved. Bilateral or unilateral oral burning pain has been found to be associated with jaw pain or uncontrollable tightness, taste changes, subjective dry mouth, geographic and fissured tongue, painful teeth, headache, neck and shoulder pain, difficulty speaking, nausea, gagging and swallowing difficulties. BMS has been reported to follow dental treatment, antibiotic usage and a severe upper respiratory infection. The lack of pathology to account for the pain can be frustrating. Pain is constant, progressively increases over the day, and usually decreases during eating. Patients, who are frequently distressed by their unremitting symptoms, may demonstrate psychological abnormalities including anxiety and depression.

Therapy for BMS involves the use of centrally acting medications for neuropathic pain, such as tricyclic antidepressants, benzodiazepines or gabapentin. Clonazepam is a benzodiazepine used either topically or in low doses orally, which appears to have excellent efficacy in the relief of the symptoms related to BMS. Topical medications, including clonidine, may be considered for application to local sites.

A combination of oral medications for the management of BMS (clonazepam, gabapentin, baclofen, and lamotrigine) significantly decreased pain in 38 or 45 patients. The most common adverse effect reported with the medication protocol was drowsiness followed by dizziness and perceived changes in mood. These results suggest that BMS may be treated with lower doses of a combination of medications rather than higher doses of a single medication, which may help to limit adverse effects such as drowsiness or dizziness.

The formulation for a mouthrinse containing clonazepam 1 mg per 5 ml has been reported. It is hypothesised that clonazepam acts locally to disrupt the mechanism(s) underlying stomatodynia. Topical formulations of gabapentin, ketamine, clonidine, and baclofen have been used to treat chronic neuropathic pain at various bodily sites.

Triamcinolone Acetonide Oral Rinse for Treating Oral Lichen Planus

Corticosteroids are the class of drug most commonly used for the treatment of oral lichen planus. Triamcinolone acetonide paste is the most widely available commercial preparation for the treatment of oral lichen planus, but is difficult to apply to mucosa and patients have reported an unpleasant sticky sensation. Delivery of corticosteroids via an oral rinse has the advantage of providing drug contact with the distal, hard-to-reach crevices and surfaces of the oral cavity, which can prevent new eruptions.

The use of a 0.1% triamcinolone acetonide aqueous suspension as an oral rinse in the treatment of symptomatic oral lichen planus has proven to be more effective than the 0.1% dental paste. This preparation must be compounded extemporaneously and should not contain flavorings (which stimulate salivation and therefore dilute the preparation in the mouth, decreasing its effectiveness) or preservatives (which may sting or burn the mucosa). Also, researchers have formulated a triamcinolone acetonide solution for use as an oral rinse, which is more convenient to use and more palatable than the commercially available triamcinolone acetonide paste, with similar therapeutic efficacy.