Aphthous Stomatitis Medication

Updated: May 14, 2018
  • Author: Ginat W Mirowski, MD, DMD; Chief Editor: William D James, MD  more...
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Medication

Medication Summary

Therapy for this condition is aimed at palliating symptoms, shortening healing time, and reducing the number of episodes (prophylaxis)

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Corticosteroids

Class Summary

Topical steroids are the first-line therapy. They are used to suppress immunologic- and inflammatory-mediated attacks resulting in ulceration. They are used to treat idiopathic and acquired autoimmune disorders.

Prednisone (Deltasone)

Prednisone is a systemic corticosteroid for cases of severe aphthae; it is inactive and must be metabolized to the active metabolite prednisolone. Close follow-up care and monitoring are required to monitor for candidiasis and other secondary infections and adverse reactions. Prednisone is available in a 5 mg/5 mL solution.

Dexamethasone (Decadron, Dexasone)

Dexamethasone is the drug of choice for recurrent aphthous ulcers and various inflammatory diseases. It decreases inflammation by suppressing the migration of polymorphonuclear leukocytes and reducing capillary permeability. An elixir of 0.5 mg/5 mL (high potency, substituted, fluorinated) may be used.

Triamcinolone topical (Aristocort)

Topical triamcinolone is for inflammatory dermatoses responsive to steroids; it decreases inflammation by suppressing the migration of polymorphonuclear leukocytes and reversing capillary permeability. It is advisable when local disease is accessible to the patient. Use 0.1% gel.

Fluocinonide (Fluonex, Lidex)

Fluocinonide is a high-potency topical corticosteroid that inhibits cell proliferation; it is immunosuppressive and anti-inflammatory. It is advisable when local disease is accessible to the patient. Use 0.05% gel.

Clobetasol propionate (Temovate)

Clobetasol propionate is a class I superpotent topical steroid that suppresses mitosis and increases the synthesis of proteins that decrease inflammation and cause vasoconstriction. Use 0.05% gel.

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Anesthetics

Class Summary

These agents locally relieve pain of recurrent aphthous ulcers.

Lidocaine anesthetic (Xylocaine)

Lidocaine anesthetic is an amide-type local anesthetic. It decreases permeability to sodium ions in neuronal membranes and inhibits depolarization, blocking the transmission of nerve impulses. Use 2% viscous solution.

Benzocaine (Americaine, Anbesol)

Benzocaine is a para-aminobenzoic acid (PABA) derivative, ester-type local anesthetic that is minimally absorbed. It inhibits neuronal membrane depolarization, blocking nerve impulses.

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Coating agents

Class Summary

These agents protect and bolster natural mucosal barrier.

Sucralfate (Carafate)

Sucralfate is a sulfate-aluminum complex, which coats ulcer surfaces, forming a physical barrier. In this way, it protects the ulcer surface from irritation. Some studies have reported improvement in symptomology and duration of ulcers, while other studies have found that sucralfate is not effective in the treatment of recurrent aphthous ulcers.

Bismuth subsalicylate (Kaopectate, Kaopectate Extra Strength, Maalox Total Relief)

Bismuth subsalicylate has been used to reduce pain from oral ulcers by protecting raw mucosa. It may also accelerate reepithelialization, although its mechanism of action is largely unknown. Some clinicians advise patients to include bismuth subsalicylate in mouthwash recipes along with other ingredients, such as liquid diphenhydramine.

Bioadherent oral (Gelclair)

This oral bioadherent adheres to the mucosal surface of mouth and forms a protective coating that shields exposed and overstimulated nerve endings. Ingredients include water, maltodextrin, propylene glycol, polyvinylpyrrolidone (PVP), sodium hyaluronate, potassium sorbate, sodium benzoate, hydroxy ethylcellulose, polyethylene glycol (PEG)–40, hydrogenated castor oil, disodium edetate, benzalkonium chloride, flavoring, saccharin sodium, and glycyrrhetinic acid.

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Topical occlusives

Class Summary

These agents are indicated for topical application to hold closed easily approximated skin edges of wounds. They may be helpful in aphthous ulcers.

2-Octyl cyanoacrylate

Over-the-counter formulations of cyanoacrylate (essentially Super Glue) form a waterproof occlusive barrier over ulcers.

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Immunosuppressants

Class Summary

These agents blunt immunologically mediated destruction leading to mucosal ulceration. Systemic immunosuppressants are indicated for severe and recalcitrant cases of aphthous stomatitis.

Colchicine (Colcrys, Mitigare)

Colchicine is an anti-inflammatory agent that inhibits microtubule polymerization.  Studies have shown that colchicine is effective in reducing pain from aphthous ulcers, as well as decreasing the frequency of ulcer formation. Adverse effects include gastrointestinal upset, such as diarrhea, and neutropenia. Use 0.6 mg thrice daily.

Montelukast (Singulair)

Montelukast sodium is an immunosuppressive agent that acts via leukotriene receptor antagonism. It blocks leukotrienes, downstream metabolic products of arachidonic acid, from binding to receptors located on neutrophils and macrophages and thereby blocks their activation, chemotaxis, and degranulation. It is reported to have equal efficacy as prednisone in the treatment of recurrent aphthous stomatitis, with fewer adverse effects.

Clofazimine (Lamprene)

Clofazimine is an immunosuppressive and anti-inflammatory agent with antibacterial properties that has shown efficacy in reducing the frequency of ulcers and symptoms in patients who continue to experience ulcers. Although its precise mechanism of action is unclear, it has been shown to accumulate in phagocytes, increase lysosomal enzyme production, and inhibit neutrophil migration.

Azathioprine (Imuran)

Azathioprine is largely converted to the active metabolites 6-mercaptopurine and 6-thioinosinic acid; it antagonizes purine metabolism and inhibits the synthesis of DNA, RNA, and proteins. It may decrease the proliferation of immune cells, lowering autoimmune activity. It may decrease the proliferation of immune cells, lowering autoimmune activity.

Thalidomide (Thalomid)

Thalidomide was the first FDA-approved therapy for recurrent aphthous ulcer. It is an immunomodulatory agent that may suppress excessive production of tumor necrosis factor (TNF)‒alpha and may down-regulate selected cell-surface adhesion molecules involved in leukocyte migration. Close follow-up, including nerve conduction studies and electromyography every 6 months, is recommended in patients using thalidomide.

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Topical immunomodulators

Class Summary

These agents are inhibitors of the formation and/or release of inflammatory mediators.

Cyclosporine (Gengraf, Neoral, Sandimmune)

Cyclosporine is a potent immunosuppressant that binds cyclophilin on lymphocytes to inhibit calcineurin and thereby prevent the production of interleukin 2. In this way, it dampens the immune response and particularly the action of T cells. Cyclosporine has been tested as a systemic agent and a topical paste with mixed reports of efficacy, but it is now most often used effectively as an oral rinse.

Amlexanox (Aphthasol)

Amlexanox is an adhesive oral paste whose mechanism of action is unknown. It appears to accelerate the healing of aphthous ulcers. Amlexanox appears as a beige-colored paste. It is a potent inhibitor of the formation and release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils, and mononuclear cells in in vitro studies. Amlexanox is FDA approved for the treatment of recurrent aphthous stomatitis.

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Retinoids

Class Summary

Retinoids are a class of drugs closely related to vitamin A. They are used to regulate epithelial cell differentiation and have also been shown to have immunomodulatory and anti-inflammatory effects.

Isotretinoin (Absorica, Amnesteem, Claravis)

Researchers have found systemic isotretinoin to be an effective therapy for recurrent aphthous ulcers. Additionally, isotretinoin (0.1% gel) has been used in the treatment of oral lichen planus with reported efficacy, and it may also be useful in the treatment of recurrent aphthous ulcers.

Tretinoin topical (Atralin, Avita, Refissa)

Tretinoin in an adhesive base (0.1%) has been used in the treatment of oral lichen planus with reported efficacy, and it may also be useful in the treatment of recurrent aphthous ulcers.

Retinoic acid

Retinoic acid in an oral base (0.05%) has been used in the treatment of oral lichen planus with reported efficacy, and it may also be useful in the treatment of recurrent aphthous ulcers.

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Antibacterial agents

Class Summary

These agents treat inflammation of the oral mucosa caused by bacterial or fungal actions.

Chlorhexidine oral (Peridex, PerioChip, PerioGard)

Chlorhexidine gluconate is an adjunct treatment for gingival disease; it binds to negatively charged bacterial cell walls and extramicrobial complex, causing bacteriostatic and bactericidal effects. Chlorhexidine gluconate is an effective, safe, and reliable topical wash or oral mouthwash antiseptic.

Tetracycline

Tetracycline treats gram-positive and gram-negative organisms and mycoplasmal, chlamydial, and rickettsial infections. It inhibits bacterial protein synthesis by binding with 30S and possibly 50S ribosomal subunits. Use the oral suspension. It may have an anti-inflammatory in addition to antibacterial mechanism of action.

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Hemorheologic agents

Class Summary

Hemorheologic agents may be beneficial in patients who do not respond to other therapies; they are not first-line treatment.

Pentoxifylline (Pentoxil, Trental)

Pentoxifylline inhibits the production of TNF-alpha and reduces the migration of neutrophils. Its specific action in aphthous stomatitis is unclear, but it has been shown to reduce the severity and frequency of episodes.

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Secretagogues

Class Summary

As xerostomia may exacerbate or even contribute to the development of aphthous ulcers, treatment with agents known to increase saliva production may be of benefit to some patients.

Cevimeline (Evoxac)

Cevimeline is a parasympathomimetic agent that acts via muscarinic acetylcholine receptors to induce salivation. Use cevimeline at 30 mg  orally thrice daily.

Pilocarpine (Pilocarpine PO, Salagen)

Pilocarpine is a parasympathomimetic agent that acts via muscarinic acetylcholine receptors to induce salivation. Use 5 mg, 1-2 tablets, 3-4 times per day, not to exceed 30 g/day.

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Ear, Eye, Nose & Throat, Herbals

Class Summary

These agents may be used as adjunct topical treatments to shorten healing time and reduce pain.

Quercetin

Quercetin is a plant flavonoid that has been shown to stimulate gastric epithelial cell proliferation and may be used as an adjunct topical agent to shorten healing time and reduce pain.

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