Background. The author reviewed the history of, federal regulations regarding, risks of and adverse drug reactions of five compound topical anesthetics: tetracaine, adrenaline/epinephrine and cocaine (TAC); lidocaine, adrenaline/epinephrine and tetracaine (LET); lidocaine, tetracaine and phenylephrine (TAC 20 percent Alternate); lidocaine, prilocaine and tetracaine (Profound); and lidocaine, prilocaine, tetracaine and phenylephrine with thickeners (Profound PET).

Types of Studies Reviewed. The author reviewed clinical trials, case reports, descriptive articles, and U.S. Food and Drug Administration (FDA) regulations and recent public advisory warnings regarding the federal approval of and risks associated with the use of compound topical anesthetics.

Results. Compound topical anesthetics are neither FDA-regulated nor -unregulated. Some compounding pharmacies bypass the new FDA drug approval process, which is based on reliable scientific data and ensures that a marketed drug is safe, effective, properly manufactured and accurately labeled. Two deaths have been attributed to the lay use of compound topical anesthetics. In response, the FDA has announced the strengthening of its efforts against unapproved drug products.

Clinical Implications. Compound topical anesthetics may be an effective alternative to local infiltration for some minimally invasive dental procedures; however, legitimate concerns exist in regard to their safety. Until they become federally regulated, compound topical anesthetics remain unapproved drug products whose benefits may not outweigh their risks for dental patients.

Key Words: Topical anesthetics; U.S. Food and Drug Administration; compounding

Abbreviations: CPG: Compliance Policy Guide • FDA: U.S. Food and Drug Administration • FDAMA: Food and Drug Administration Modernization Act • LET: Lidocaine, adrenaline/epinephrine and tetracaine • PABA: Para-aminobenzoic acid • TAC: Tetracaine, adrenaline/epinephrine and cocaine • TADs: Temporary anchorage devices