Benzocaine

(BAN, rINN)
Benzocaine Chemical formula
Synonyms: Anaesthesinum; Anestezin; Anesthamine; Bensokain; Bentsokaiini; Benzocaína; Benzocaïne; Benzocainum; Benzokain; Benzokaina; Benzokainas; Ethoform; Éthoforme; Ethyl Aminobenzoate; Ethylis Aminobenzoas. Ethyl 4-aminobenzoate.
Cyrillic synonym: Бензокаин.

💊 Chemical information

Chemical formula: C9H11NO2 = 165.2.
CAS — 94-09-7.
ATC — C05AD03; D04AB04; N01BA05; R02AD01.
ATC Vet — QC05AD03; QD04AB04; QN01AX92; QN01BA05; QR02AD01.

Pharmacopoeias.

In Chin., Eur., Int., Jpn, and US.

Ph. Eur. 6.2

(Benzocaine). Colourless crystals or a white or almost white, crystalline powder. M.p. 89° to 92°. Very slightly soluble in water; freely soluble in alcohol. Protect from light.

USP 31

(Benzocaine). Small, white crystals or a white odourless crystalline powder. M.p. 88° to 92°. Soluble 1 in 2500 of water, 1 in 5 of alcohol, 1 in 2 of chloroform, 1 in 4 of ether, and 1 in 30 to 50 of almond oil or olive oil; dissolves in dilute acids.

💊 Adverse Effects and Treatment

Abuse.

Benzocaine has been used as an adulterant or ‘cutting’ agent in the preparation of cocaine for illicit use and adverse effects such as methaemoglobinaemia have been seen after cocaine overdosage as a result of the benzocaine content.1
1. McKinney CD, et al. Benzocaine-adultered street cocaine in association with methemoglobinemia. Clin Chem 1992; 38: 596–7.

Hypersensitivity.

The incidence of positive reactions in patients patch tested with benzocaine has ranged from 3.3 to 5.9%.1,2 Patch testing with benzocaine has been recommended by The International Contact Dermatitis Research Group as an indicator of contact hypersensitivity to local anaesthetics. However, it was found that of 40 patients who had had positive reactions to benzocaine with tetracaine and cinchocaine, 21 were not allergic to benzocaine alone.3
1. Rudzki E, Kleniewska D. The epidemiology of contact dermatitis in Poland. Br J Dermatol 1970; 83: 543–5
2. Bandmann H-J, et al. Dermatitis from applied medicaments. Arch Dermatol 1972; 106: 335–7
3. Beck MH, Holden A. Benzocaine—an unsatisfactory indicator of topical local anaesthetic sensitization for the UK. Br J Dermatol 1988; 118: 91–4.

💊 Interactions

For interactions associated with local anaesthetics.

💊 Pharmacokinetics

See under Local Anaesthetics.

💊 Uses and Administration

Benzocaine, a para-aminobenzoic acid ester, is a local anaesthetic used for surface anaesthesia; it has low potency and low systemic toxicity. It is used, often with other drugs such as analgesics, antiseptics, antibacterials, antifungals, and antipruritics, for the temporary local relief of pain associated with dental conditions, oropharyngeal disorders, haemorrhoids, anal pruritus, and ear pain. Lozenges containing benzocaine in usual doses of up to 10 mg are used for the relief of sore throat. Gels, pastes, solutions, and sprays containing benzocaine in concentrations of up to 20% have been used for surface anaesthesia of the mouth and throat. Benzocaine is used in ear drops, creams, ointments, lotions, solutions, sprays, gels, and suppositories in concentrations up to 20% for topical analgesia and anaesthesia. Benzocaine has also been used as the hydrochloride.

Obesity.

It has been reported1 that despite the inclusion of benzocaine in some over-the-counter appetite suppressants there is no good evidence of its value in obesity.
1. Anonymous. A nasal decongestant and a local anesthetic for weight control? Med Lett Drugs Ther 1979; 21: 65–6.

💊 Preparations

USP 31: Antipyrine and Benzocaine Otic Solution; Antipyrine, Benzocaine, and Phenylephrine Hydrochloride Otic Solution; Benzocaine and Menthol Topical Aerosol; Benzocaine Cream; Benzocaine Gel; Benzocaine Lozenges; Benzocaine Ointment; Benzocaine Otic Solution; Benzocaine Topical Aerosol; Benzocaine Topical Solution; Benzocaine, Butamben, and Tetracaine Hydrochloride Gel; Benzocaine, Butamben, and Tetracaine Hydrochloride Ointment; Benzocaine, Butamben, and Tetracaine Hydrochloride Topical Aerosol; Benzocaine, Butamben, and Tetracaine Hydrochloride Topical Solution.

Proprietary Preparations

Arg.: Cerax; Lanacaina†; Lodoc; Austral.: Applicaine; Austria: Anaestherit; Braz.: Solarcaine; Canad.: Anbesol; Anbesol Baby; Anbesol Extra Strength; Baby Orajel; Detane†; Maintain; ManDelay; Orajel; Outgro; Zilactin Baby; Zilactin Tooth & Gum Pain Reliever; Zilactin Toothache Swab; Zilactin-B; Chile: Anbesol; Baby Orajel†; BBdent Gel Topico; Dentispray; Foille; Kalmafta; Orajel†; Cz.: Babydent; Ger.: Anaesthesin; Anaesthesin N; Flavamed Halstabletten†; Kontakto Derm†; Labocane; Subcutin N; Zahnerol N†; Hung.: Babydent; Israel: Anadent; Baby Gel; Lanacane; Maintain; Mex.: Auralyt; Gomas Garde B; Graneodin B; NZ: Solarcaine; Pol.: Baby Orajel; Orajel; Port.: Dentispray; Topigel; Rus.: Relief Advance (Релиф Адванс); S.Afr.: Kiddigum; Spain: Dentispray; Gartricin†; Hurricaine; Lanacane; Nani Pre Dental; UK: AAA; Burneze; Lanacane; Orajel; Ultra Chloraseptic; Ultracare; USA: Americaine Anesthetic†; Americaine Otic†; Americaine†; Baby Anbesol; Baby Orajel; Benz-O-Sthetic; Benzodent; Chigger-Tox; Dent’s Extra Strength Toothache Gum; Dent’s Maximum Strength Toothache Drops; Dent-O-Kain; Dermoplast; Detane; Hurricaine; Lanacane; Medicone; Mycinettes; Numzident†; Orabase Baby; Orabase Gel; Orabase-B; Orajel; OraMagic Plus; Otocain; SensoGARD; Trocaine; Zilactin-B Medicated. Multi-ingredient: Arg.: Adermicina; Adermicina A; Algiodent; Anginotrat; Apracur Bucofaringeo†; Arnecrem†; Aseptobron Caramelos; Aseptobron N; Bagociletas; Balsamina; Bucoangin N; Bucotricin; Caext; Callicida; Caramelos Antibioticos; Caramelos Antibioticos Lefmar; Caramelos Oriental; Carnot Colutorio; Cartiflex; Collubiazol; Coltix†; Cristalomicina; Dermo Vagisil Crema; Dermosan; Detebencil; Dotrin; Esculeol P; Esmedent con Fluor; Fanaletas; Filotricin A; Flebotropin†; Fonergine; Gargaletas; Graneodin; Graneodin N; Hexa-Defital; Iodotiazol†; Leroid†; Lyndan; Muco-Anestyl†; Mucobase; Muelita; Nene Dent; Neo Coltirot; No-Tos Pocket; Oralsone C; Otocalmia; Otoseptil; Parencias†; Pastillas Lorbi; Pastillas Medex; Pruripelen†; Pulmosan Caramelos; Razagleda Plus†; Salicrem; Sapucai†; Suavisan N; Suavisan†; Sulfanoral T; Tavinex; Austral.: Animine; Auralgan; Ayrton’s Chilblain; Cepacaine; Cepacol Anaesthetic; Cepacol Cough & Sore Throat; Cornkil†; Le Trim-BM†; Nyal Toothache Drops; Rectinol; Austria: Dequalinetten; Dorithricin; Herposicc; Sulgan 99; Tyrothricin comp; Tyrothricin compositum; Belg.: Transvane; Braz.: Albicon; Amidalin†; Amigdagen; Amigdamicin†; Andolba; Anginotricin; Bromil; Cepacaina; Cetildrops†; Claudemor; Dentalivio†; Dequadin; Fenotricin†; Gargotan†; Gingilone; Larintil†; Malvatricin Pastilhas; Malvona†; Mentozil†; Mirorroidin†; Neopiridin; Otovix†; Passilin†; Predmicin; Sanilin; Senol†; Silencium; Traumac; Canad.: Anbesol Maximum Strength; Antibiotic Cold Sore Ointment; Appedrine†; Auralgan; Bionet; Boil Ease†; Cepacol Extra Strength; Chloraseptic Lozenges; Dexatrim†; Endospray†; Kank-A; Lanacane Medicated Cream; Onrectal; Orajel Mouth Sore Medicine; Orajel Ultra Mouth Sore; Osmopak-Plus; Oxipor; Rectogel; Rectogel HC; Solarcaine; Sore Throat Lozenges; Tanac; Thermo-Gel; Throat Lozenges; Thunas Pile†; Vagisil; Chile: Aucusik; Cariamyl; Kank-Eze; Konirub; Lerfimin; Medikem†; Orajel Compuesto†; Otandrol; Solarcaine Spray Aerosol; Cz.: Dr Rentschler Halstabletten†; Herbadent; Hexoral; Hexoraletten N; Denm.: Dolodent; Hexokain; Fin.: Bafucin; Toncils; Fr.: Nestosyl; Sedorrhoide; Ger.: Anaesthesin-Rivanol; Combustin Heilsalbe; Dolo-Dobendan; Dorithricin Original; Eulatin NN; Frubizin Forte†; Gelum†; Hexoraletten N; Inspirol Halsschmerztabletten†; Nordapanin N†; Nordathricin N†; Salistoperm†; Stipo†; Trachiform†; Tyrosolvetten†; Gr.: Myalgesic†; Hong Kong: Borraginol-N; Pharynx; Setronges†; Tyricine; Tyrocaine; Tyrothricin Co; Hung.: Almagel A; Dorithricin; India: Chloromycetin Ear Drops; Clearwax; Healex; Nit-N-Mite†; Paraxin Ear†; Perfocyn; Proctosedyl; Scaboma; Tytin; Waxolve; Indon.: Benzomid; Borraginol-N; Borraginol-S; FG Ointment; Otolin; Irl.: Dequacaine; Merocaine; Tyrozets; Israel: Anadent†; Dentin; Gingisan; Hemo; Kalgaron; KankA; Noxacorn; Otomycin; Proctozorin-N; Pronestin; Rafathricin with Benzocaine; Rectozorin; Ital.: Antiscabbia Candioli al DDT Terapeutico; Antiscabbia CM; Boma; Dentosedina; Fialetta Odontalgica Dr Knapp; Foille Scottature; Foille Sole; Golamixin; Labocaina; Pinselina Knapp; Prepacort H; Preparazione Antiemorroidaria†; Proctidol; Proctosedyl; Proctosoll; Sedalen Cort†; Sedilene Procto†; Malaysia: Cetylpyridinium B; Horf; Pharynx; Setronges†; Mex.: Cepacaina; Cloran Otico; Graneodin D Mentol; Ofodex; Otifar; Otolone†; Soldrin; Sufrexal P; Trociletas B; NZ: Auralgan; Cepacaine; Cepacol Anaesthetic; Cepacol Cough Discs; Lanacane; Solarcaine; Toothache Drops†; Philipp.: Auralgan; United Home Burn Ointment; Pol.: Dentosept A; Dermopur; Hemorol; Icy Rub; Puder Plynny; Puder Plynny z Anestezyna; Pudroderm; Pudrospan; Rectosec; Sanofil; Sapoven AT; Savarix; Septolete Plus; Variderm; Port.: Afonina; Anginova; Claudemor†; Dek; Dropcina; Halitol†; Hibitane Menta†; Hibitane†; Medifon; Mentocaina R; Otoceril; Solpic†; Tantum Verde; Rus.: Almagel A (Алмагель А); Anaesthesol (Анестезол); Heparin Ointment (Гепариновая Мазь); Nigepan (Нигепан); Septolete Plus (Септолете Плюс); S.Afr.: AAA†; Auralyt; Aurasept; Aurone Forte; Benzet†; Calasthetic; Cepacaine; Cepacol Cough Discs; Cetoxol; Covancaine; Covotop; Endcol Lozenges; Histamed; Medi-Kain†; Medi-Keel A; Orochlor; Otised; OtoPhen Forte; Oxipor VHC; Prodol; Trochain; Viodor; Singapore: Dorithricin; Pharynx; Spain: Angileptol; Antihemorroidal; Bucodrin; Bucometasana; Bucospray; Callicida Rojo; Callivoro Marthand; Callix; Caltoson Balsamico; Cicatral; Cremsol; Dentikrisos; Diformiltricina; Drill; Edifaringen; Faringenilo; Faringesic; Gargaril; Garydol; Gradin Del D Andreu†; Grietalgen; Grietalgen Hidrocort†; Hemoal; Hemodren Compuesto†; Hibitane; Mastiol; Miozets; Nasopomada; Neo Analsona; Oto Difusor†; Oto Vitna†; Otocerum; Otonina†; Otosedol Biotico; Pastillas Koki Ment Tiro; Phonal; Sedofarin; Topicaina†; Tos Mai; Vicks Formula 44†; Swed.: Bafucin; Switz.: Benzocaine PD; Neocones; Thai.: Auralgan†; Doproct; Iwazin; Sigatricin; Trocacin; Troneo†; Turk.: Emedur; Kataljin; Kortos; Ma-Ka-Ta; UK: Anthisan Plus; Dequacaine; Intralgin†; Merocaine; Rinstead; Solarcaine; Tyrozets; Wasp-Eze; USA: Aerocaine†; Allergen; Americaine First Aid†; Anbesol; Anbesol Cold Sore Therapy; Auralgan; Auroguard Otic; Auroto†; Babee; Bicozene; Boil Ease; Boyol Salve; Calamycin; Cepacol Anesthetic; Cepacol Maximum Strength Sore Throat; Cepacol Ultra Sore Throat Plus Cough; Cetacaine; Chiggerex; Chloraseptic Sore Throat; Cough-X; Cy-Gesic; Cylex; Dendracin Neurodendtraxcin; Dentapaine; Dermacoat; Dermasept Antifungal; Dermoplast Antibacterial; Double-Action Toothache Kit; Foille; Fungi-Nail; Hem-Prep; Kank-A; Legatrin Rub; Lipmagik; Maximum Strength Anbesol; Medicone Derma†; Numzit†; Orabase Lip; Orajel Mouth Aid; Orajel PM; Orasept; Orasol; Otocalm†; Pazo; Rectagene Medicated Rectal Balm; Rid-a-Pain; Solarcaine; Soothaderm; Sting-Eze; Sting-Kill; Tanac; Tanac Dual Core; Therevac Plus; Tigan†; Toothache Gel; Triban†; Tympagesic†; Unguentine Maximum Strength; Vagi-Gard Medicated Cream; Vagisil; Z-Xtra; Venez.: Claudemor†; Otan; Otofrin†.
Published October 13, 2018.