Chemotherapy-Induced Oral Mucositis Medication

Updated: Mar 14, 2023
  • Author: Nathaniel S Treister, DMD, DMSc; Chief Editor: Jeff Burgess, DDS, MSD  more...
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Medication

Medication Summary

Oral mucositis is a self-limited condition. Currently, no approved preventive or therapeutic agent consistently prevents oral mucositis in all clinical settings.

Palifermin, or human recombinant keratinocyte growth factor (KGF), given intravenously significantly reduces the incidence, duration, and severity of oral mucositis in patients undergoing autologous hematopoietic cell transplantation (HCT) and has been approved for use in patients with hematologic malignancies undergoing high-dose chemotherapy with or without concomitant total body irradiation, with autologous or allogeneic stem cell transplantation. [6, 20, 21] Human KGF may be considered for hematologic malignancies. [22]

Medications are used for prophylaxis against viral and fungal infections, decontamination of the oral cavity, and palliation for pain. This section discusses common medications used for prophylaxis, decontamination, and topical palliation only.

Palliation

Topical palliation for pain may be as simple as frequent sodium chloride solution or salt/bicarbonate of soda rinses and ice chips. Often, 2% viscous lidocaine is used alone or is mixed in equal volumes with diphenhydramine hydrochloride and bismuth subsalicylate (Kaopectate) or even aluminum hydroxide/magnesium hydroxide (Maalox) as a soothing mouth rinse. Topically applied morphine solution has demonstrated efficacy in controlling symptoms. With increasing severity of mucositis, and especially when involving the esophagus, systemic opioids may be indicated.

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Antifungals

Class Summary

These agents are used prophylactically against candidal infections in all patients. Reevaluate the diagnosis if no clinical response is detected.

Nystatin (Nystex, Mycostatin, Nilstat)

Nystatin is a fungicidal and fungistatic antibiotic obtained from Streptomyces noursei. It is effective against various yeasts and yeastlike fungi. It changes the permeability of the fungal cell membrane after binding to cell membrane sterols, causing cellular contents to leak. Nystatin is not absorbed significantly from the GI tract.

Clotrimazole (Lotrimin, Mycelex, Femazole)

Clotrimazole is a broad-spectrum antifungal agent that inhibits yeast growth by altering cell membrane permeability, causing death of fungal cells. Reevaluate the diagnosis if no clinical improvement is seen after 4 weeks.

Fluconazole (Diflucan)

Fluconazole has fungistatic activity. It is a synthetic oral antifungal (broad-spectrum bistriazole) that selectively inhibits fungal cytochrome P-450 and sterol C-14 alpha-demethylation, which prevents the conversion of lanosterol to ergosterol, thereby disrupting cellular membranes.

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Antibacterials

Class Summary

Rinses are the basis of the oral decontamination regimen.

Chlorhexidine oral (Peridex, PerioChip, PerioGard)

Chlorhexidine oral is an effective, safe, and reliable antiseptic mouthwash. It is a polybiguanide with bactericidal activity; it is usually supplied as gluconate salt. At physiologic pH, salt dissociates to a cation that binds to bacterial cell walls. Chlorhexidine is active against gram-positive and gram-negative organisms, facultative anaerobes, aerobes, and yeast. Precede use of the solution by flossing and brushing teeth, if possible. Completely rinse toothpaste from mouth.

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Anesthetics

Class Summary

Oral rinses are used to reduce pain and discomfort.

Viscous lidocaine 2% (Xylocaine, Dilocaine, Anestacon)

Viscous lidocaine 2% decreases permeability to sodium ions in neuronal membranes. This results in inhibition of depolarization, blocking the transmission of nerve impulses.

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Antivirals

Class Summary

Nucleoside analogs are initially phosphorylated by viral thymidine kinase to eventually form a nucleoside triphosphate. Once phosphorylated, it causes DNA chain termination when acted on by DNA polymerase. These molecules inhibit herpes simplex virus (HSV) polymerase with 30-50 times the potency of human alpha-DNA polymerase.

Acyclovir (Zovirax)

Use acyclovir for patients who have been exposed to HSV or varicella-zoster virus (VZV) infection. Reactivation of such infections occurs in 70-90% of patients who have antibodies to these agents and can aggravate preexisting oral mucositis and result in systemic infection. It inhibits the activity of HSV-1 and HSV-2. Patients experience less pain and faster resolution of cutaneous lesions when used within 48 hours of rash onset. Acyclovir may prevent recurrent outbreaks. Early initiation of therapy is imperative.

Valacyclovir (Valtrex)

Valacyclovir is a prodrug and is rapidly converted to the active drug acyclovir. It is more expensive but has better bioavailability and a more convenient dosing regimen than acyclovir.

Famciclovir (Famvir)

Famciclovir is for prophylactic use to prevent recurrent HSV infections. It is a prodrug, which, when biotransformed into its active metabolite, penciclovir, may inhibit viral DNA synthesis/replication. It inhibits viral DNA polymerase.

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Oral Rinses

Class Summary

Mucoadhesive action reduces pain by adhering to the mucosal surface of the mouth.

Magic Mouthwash

Magic mouthwashes in general form a viscous adhesive substance that protects the oral lining.

Artificial saliva (Caphosol, Aquoral, Oasis)

These preparations typically contain methylcellulose, sorbitol, and salts to moisten and lubricate the mouth.

Bioadherent oral (Gelclair)

This agent adheres to the mucosal surface of the 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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Growth factors

Class Summary

Human KGF may be considered for hematologic malignancies.

Palifermin (Kepivance)

Palifermin is a human KGF that enhances epithelial cell proliferation, differentiation, and migration. The KGF receptor is not present on hematopoietic cells, but has enhanced growth of human epithelial tumor cell lines in vitro. It is indicated to decrease severe oral mucositis incidence and duration in patients with hematologic malignancies.

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