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Dibucaine: Drug information

Dibucaine: Drug information
(For additional information see "Dibucaine: Patient drug information" and see "Dibucaine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Nupercainal (Topical) [OTC] [DSC];
  • Nupercainal [OTC]
Pharmacologic Category
  • Antihemorrhoidal Agent;
  • Local Anesthetic
Dosing: Adult
Dermal pain/itching

Dermal pain/itching: Topical: Apply to affected area up to 3 or 4 times daily. Maximum daily dose: 30 g/day.

Hemorrhoids, anorectal pain/itch

Hemorrhoids, anorectal pain/itch:

Note: Combine with dietary modifications, bowel hygiene, and warm sitz baths for best results (Ref). General dosing guidelines provided; refer to specific product labeling for dosing instructions.

Topical (external): Apply to anal area, as needed, up to 4 times daily.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Dibucaine: Pediatric drug information")

Dermal pain/itching

Dermal pain/itching: Children ≥2 years weighing ≥16 kg and Adolescents: Topical: Apply to affected area up to 3 or 4 times daily. Maximum daily dose: 7.5 g/day for children and 30 g/day for adults

Hemorrhoids/anorectal disorders; rectal pain/itching

Hemorrhoids/anorectal disorders; rectal pain/itching: Children ≥12 years and Adolescents: Topical: Apply to affected external anal area up to 3 or 4 times daily

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling.

Adverse Reactions

There are no adverse reactions listed in the manufacturer's labeling.

Postmarketing: Dermatologic: Acute generalized exanthematous pustulosis (Cubero 2010), allergic dermatitis (including contact dermatitis, maculopapular rash, and symmetrical drug-related intertriginous and flexural exanthema [SDRIFE]) (de Groot 2022)

Contraindications

OTC labeling: When used for self-medication, do not use in or near the eyes or in children <2 years or weight <16 kg.

Warnings/Precautions

Concerns related to adverse effects:

• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).

Other warnings/precautions:

• Self-medication (OTC use): For external use only. When used for self-medication, notify health care provider and discontinue use if condition worsens, does not improve within 7 days, or if redness, irritation, swelling, bleeding, or other symptoms develop or increase. Do not put this product into the rectum using fingers or any mechanical device or applicator; do not exceed recommended dose unless directed by a health care provider. Do not use in large quantities, particularly over raw surfaces or blistered areas.

• Topical application: When topical anesthetics are used prior to cosmetic or medical procedures, the lowest amount of anesthetic necessary for pain relief should be applied. High systemic levels and toxic effects (eg, methemoglobinemia, irregular heart beats, respiratory depression, seizures, death) have been reported in patients who (without supervision of a trained professional) have applied topical anesthetics in large amounts (or to large areas of the skin), left these products on for prolonged periods of time, or have used wraps/dressings to cover the skin following application.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Ointment, External:

Nupercainal: 1% (28.4 g, 60 g)

Nupercainal (Topical): 1% (56.7 g [DSC])

Generic: 1% (28 g, 28.35 g, 56 g)

Generic Equivalent Available: US

Yes

Pricing: US

Ointment (Dibucaine (Perianal) External)

1% (per gram): $0.14

Ointment (Dibucaine External)

1% (per gram): $0.21 - $0.24

Ointment (Nupercainal External)

1% (per gram): $0.18

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Topical: For external use only; do not use in or around eyes. Prior to rectal use, clean the affected area with mild soap and warm water and rinse thoroughly; gently dry by patting or blotting with toilet tissue or a soft cloth. Do not put this product into the rectum using fingers or any mechanical device or applicator.

Administration: Pediatric

For external use only.

Rectal use: Clean the affected area with mild soap and warm water and rinse thoroughly; gently dry by patting or blotting with toilet tissue or a soft cloth. Do not put this product into the rectum using fingers or any mechanical device or applicator.

Topical dermal use: Do not use in or around eyes. Do not use in large quantities, particularly over raw surfaces or blistered areas.

Use: Labeled Indications

Dermal pain/itching: Temporary relief of pain and itching caused by sunburn, minor burns, minor cuts, scrapes, insect bites or minor skin irritation.

Hemorrhoids, anorectal pain/itch: Temporary relief of pain and itching due to hemorrhoids and other anorectal disorders.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy

Mechanism of Action

Blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Within 15 minutes.

Duration: 2 to 4 hours.

Absorption: Poor through intact skin, but well absorbed through mucous membranes and excoriated skin.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (BD) Bangladesh: Nupercainal;
  • (BR) Brazil: Nupercainal;
  • (DE) Germany: Doloposterine n;
  • (EG) Egypt: Neocaine;
  • (GB) United Kingdom: Nupercainal;
  • (GR) Greece: Nupercainal;
  • (KR) Korea, Republic of: Hemorrhoidal and topical analgesic ointment dibucaine;
  • (LT) Lithuania: Cinchocain;
  • (LV) Latvia: Cinchocain;
  • (PK) Pakistan: Cinchocaine;
  • (PR) Puerto Rico: Dibucaine | Nupercainal hc;
  • (PT) Portugal: Nupercainal;
  • (SE) Sweden: Cincain;
  • (TR) Turkey: Nupercainal;
  • (TW) Taiwan: Anesin | Dibuton | Jojo | Nupercainal;
  • (ZA) South Africa: Nupercainal
  1. Brown S, Girling C, Thapa Magar H, et al. Guidelines, guidelines and more guidelines for haemorrhoid treatment: a review to sort the wheat from the chaff. Colorectal Dis. 2022;24(6):764-772. doi:10.1111/codi.16078 [PubMed 35119707]
  2. Cubero JL, Garcés MM, Segura N, et al. Topical drug-induced acute generalized exanthematous pustulosis misdiagnosed as an oral drug-related eruption. J Investig Allergol Clin Immunol. 2010;20(7):620-621. [PubMed 21314006]
  3. Davis BR, Lee-Kong SA, Migaly J, Feingold DL, Steele SR. The American Society of Colon and Rectal Surgeons clinical practice guidelines for the management of hemorrhoids. Dis Colon Rectum. 2018;61(3):284-292. doi:10.1097/DCR.0000000000001030 [PubMed 29420423]
  4. de Groot AC. Systemic allergic dermatitis (systemic contact dermatitis) from pharmaceutical drugs: a review. Contact Dermatitis. 2022;86(3):145-164. doi:10.1111/cod.14016 [PubMed 34837391]
  5. Dibucaine ointment [prescribing information]. Allegan, MI: Perrigo; July 2014.
  6. Dibucaine ointment [prescribing information]. Melville, NY: Fougera; December 2011.
  7. Nupercainal ointment (dibucaine) [prescribing information]. Princeton, NJ: Dr. Reddy's Laboratories, Inc; received 2016.
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