VA Class:DE700
ATC Class:C05AD04
Dibucaine is a local anesthetic with a long duration of action.
Dibucaine is used topically for the temporary relief of pain and itching associated with minor burns, sunburn, minor cuts or scrapes, insect bites, or minor skin irritations. Dibucaine ointment is also used topically for the temporary relief of pain, itching, and burning caused by hemorrhoids.
Dibucaine is applied topically in the form of a cream or ointment. Dibucaine ointment may also be administered rectally using a rectal applicator.
For the temporary relief of pain and itching associated with various skin conditions, dibucaine 1% ointment is applied to affected areas gently and if necessary, covered with a light dressing. No more than 30 or 7.5 g of the ointment should be used by adults or children, respectively, in any 24-hour period. When dibucaine 0.5% cream is used for the temporary relief of pain and itching associated with various skin conditions, the cream is applied liberally to affected areas and rubbed in gently.
For the temporary relief of pain, itching, and burning caused by hemorrhoids, dibucaine 1% ointment may be instilled into the rectum using a rectal applicator. The ointment may be administered each morning and evening and after each bowel movement. Additional ointment may be applied topically to anal tissues. No more than 30 g of the ointment should be used by adults in any 24-hour period.
Some commercially available rectal and topical formulations of dibucaine contain acetone sodium bisulfite, a sulfite that may cause allergic-type reactions, including anaphylaxis and life-threatening or less severe asthmatic episodes, in certain susceptible individuals. The overall prevalence of sulfite sensitivity in the general population is unknown but probably low; such sensitivity appears to occur more frequently in asthmatic than in nonasthmatic individuals.
Topical dibucaine preparations should not be used in or near the eyes. The preparations should not be used in large quantities, especially over denuded surfaces or blistered areas. Topical dibucaine preparations are not intended for prolonged or extensive use. If dibucaine preparations are used for self-medication and the condition worsens or symptoms persist for more than 7 days or clear and occur again within a few days, the drug should be discontinued and a physician consulted. If rectal bleeding occurs during use of dibucaine ointment for pain, itching, and burning of hemorrhoids or if rash, irritation, swelling, pain, bleeding, or other symptoms develop or increase during use of dibucaine preparations, the drug should be discontinued and a physician consulted. Dibucaine should not be used in individuals with known hypersensitivity to the drug or other amide-type local anesthetics.
Serious adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) have been reported following topical application of local anesthetics to the skin; these events have occurred following application of extemporaneously prepared topical preparations containing high concentrations of anesthetics for cosmetic procedures and following use for indications approved by the US Food and Drug Administration (FDA).
Life-threatening adverse effects (e.g., irregular heart beat, seizures, breathing difficulties, coma, death) may occur when topical anesthetics are applied to a large area of skin, when the area of application is covered with an occlusive dressing, if a large amount of topical anesthetic is applied, if the anesthetic is applied to irritated or broken skin, or if the skin temperature increases (from exercise or use of a heating pad).101, 102 When applied in such a manner, the amount of anesthetic that is absorbed systemically is unpredictable and the plasma concentrations achieved may be high enough to cause life-threatening adverse effects.101, 102 Use of lidocaine gel has been investigated to reduce discomfort during mammography.101, 103 During the study, the topical anesthetic was spread over a wide area of the chest and covered with an occlusive dressing.101, 103 Whether such use could result in serious reactions has not been determined.101, 103 Patients should speak with their clinician if they are considering using a topical anesthetic before obtaining a mammogram.101
When a topical anesthetic is needed for a procedure, use of an FDA-approved preparation has been recommended. A preparation containing the lowest concentration of anesthetic likely to be effective should be used; a small amount of topical anesthetic should be applied to the affected area for the shortest period necessary for the desired effect. When the topical anesthetic will be applied by the patient, the patient should apply the topical preparation as directed by a clinician, and should not apply the topical preparation to broken or irritated skin.101
Dibucaine is a local anesthetic of the amide type with a long duration of action. Dibucaine occurs as a white to off-white powder and has a slight, characteristic odor. The drug is slightly soluble in water.
Dibucaine darkens on exposure to light. Dibucaine cream and ointment should be stored in collapsible tubes or tight, light-resistant containers at a temperature less than 40°C, preferably between 15-30°C.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Rectal or Topical | Ointment | 1%* | Dibucaine Rectal or Topical Ointment | |
Nupercainal® Hemorrhoidal and Anesthetic Ointment | Novartis | |||
Topical | Cream | 0.5% | Nupercainal® Pain-Relief Cream | Novartis |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions September 1, 2009. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
101. Food and Drug Administration. FDA Public Health Advisory: Potential hazards of skin products containing numbing ingredients for relieving pain from mammography and other medical tests and conditions. 2009 Jan 16. From FDA website. [Web]
102. Food and Drug Administration. Topical Anesthetics. MedWatch alert. Rockville, MD; 2009 Jan 16. From FDA website. [Web]
103. Lambertz CK, Johnson CJ, Montgomery PG et al. Premedication to reduce discomfort during screening mammography. Radiology . 2008; 248:765-72. [PubMed 18647845]