1994 Local Anaesthetics
Anusol; Aveeno Anti-Itcht; Bacitraycin Plus; Bite & Itch alone, or 300 mg if used with felypressin. Doses should be Lotion; Calaclear; Caladryl Clear; Caladryl; Calagesic; Callergy reduced in elderly or debilitated patients. The dose for Pharmacokinetics Clear; Cortamoxt; Cortane-B; Cortic ND; Cyotic; EndaRoid; children over 6 months of age is up to 5 mg/kg. For dental Prilocaine is reported to be 55% bound to plasma proteins. It Enzone; Epifoam; Gold Bond Intensive Healing; HC Pram; HC infiltration or dental nerve blocks, the usual adult dose of is rapidly metabolised mainly in the liver and also in the Pramoxine; Hemorid For Women; Mediotic-HC; Neosporin + prilocaine hydrochloride without felypressin is 40 to 80 rng kidneys and is excreted in the urine mainly as metabolites. Pain Relief; Neosporin + Pain Relief; Novacort; Oticin HC; Oti (1 to 2mL) as a 4% solution; children under 10 years One of the principal metabolites excreted in the urine is a cin; Oto-End; Otomar-HC; Phicon-F; Phicon; Pram-HCA; Pram generally require about 40 rng (I mL). Similar doses of the toluidine, which is believed to cause the methaemoglobin Cart; PrameGel; Pramosone; PramOtic; Preparation H; ProCort; 4% solution with adrenaline ( 1:200 000) may be used for aemia seen after large doses. Prilocaine crosses the placenta Proctofoam-HC; SarnaUltrat; Summer's Eve Anti-Itch; Tri-Bio and during prolonged epidural anaesthesia may produce zene; Tronolane; Tucks; Zinotict; Zone-A; Zoto-HC; ZyPram. most routine dental procedures. The usual adult dose of prilocaine hydrochloride with felypressin 0.03 international methaemoglobinaemia in the fetus. It is distributed into PharmacopoeialPreparo6ons units/mL is 30 to 150mg (I to 5 mL) as a 3% solution; breast milk. USP 36: Neomycin and Polymyxin B Sulfates and Pramoxine children under 10 years generally require 30 to 60mg (I to See also under Local Anaesthetics, p. 1979.3. Hydrochloride Cream; Pramoxine Hydrochloride Cream; Pram 2mL). exine Hydrochloride Jelly. A eutectic mixture of prilocaine base 2.5% and lidocaine Absorption. Peak serum concentrations of prilocaine base 2.5% (see Surface Anaesthesia, under Lidocaine, hydrochloride attained after the use of 8.5 mL of a I% p. 1989.3) is applied as a cream under an occlusive dressing solution for retrobulbar and facial nerve block were well to produce surfa ce anaesthesia of the skin before procedures below the concentration of 20 micrograrns/mL associated requiring needle puncture, surgical treatment of localised with CNS toxicity due to prilocaine.1 lesions, and split skin grafting; it has been used similarly, but 1. Goggin M, et al. Serum concentrations of prilocaine following without an occlusive dressing, before removal of genital retrobulbar block. Br J Anaesth 1990; 64: 107-9. warts. It is also used as a eutectic gel for anaesthesia of the periodontal pockets during dental scaling and/or root planing. P. rations Typically. 1.7 g of get or less, will be sufficient for one r.�P.?. quadrant of dentition; the maximum recommended ProprielaryPreparo6ons (details are given in Volume B) quantity per treatment session is 8.5 g. Single-ingredient Preparations. Austral.: Citanest; Belg.: Citan est; Braz.: Citanest com Octapressin; Citocaina; Canad.: Citan Pharmacopoeias. In Bur. (see p. vii) and US. Action. For a comparison of the vasoactivity of prilocaine est; Denm.: Citanest Octapressin; Fin.: Citanest Octapressin; Ger.: Takipril; Xylonest; Hong Kong: Citanest Octapressint; Ph. Eur. 8: and some other local anaesthetics. see p. 1976.2. (Prilocaine). A white or almost white, crystalline Mex. : Pristesin F; Neth.: Citanest Octapressine; Citanest; Nonv.: powder. M.p. 36 degrees to 39 degrees. Slightly soluble in Citanest Octapressin; NZ: Citanest; Singapore: Citanest Octa Administration in children. The BNFC recommends that water; very soluble in alcohol and in acetone. pressin; Swed. : Citanest Octapressin; Citanest; Switz.: Xylonest; the dose of prilocaine in children should be adjusted USP 36: (Prilocaine). A wbite or almost white powder or Turk.: Citanest Octapressint; Citanest; UK: Citanest with Octa according to physical status and the nature of the proce crystal aggregates. M.p. 36 degrees to 39 degrees. Slightly pressin; Citanest; Prilotekal; USA: Citanest. dure. soluble in water; very soluble in alcohol and in acetone. For uses and dosage of prilocaine hydrochloride in Arg.• Emla; Austral.• Emla; Aus Store at a temperature below 25 degrees. Mul6·ingredient Prepara6ons. children, see above. tria: Emla; Oraqix; Belg.: Emla; Braz.: Emla; Medicaina; Canad.• Emla; Chi/eo Eutecaina; China• Emla (,�jJIJ); Cz. • Emla; Eutecticmixture. Prilocaine forms a mixture with lidocaine Denm.: Fin.: Fr.: Infiltration anaesthesia.Addition of felypressin at a con Emla; Oraqix; Tapin; Emla; Oraqix; Tapin; that has a melting-point lower than that of either ingredi· Anesderm; Emla; Emlapatch; Oraqix; Ger.: Anesderm; Emla; centration of 0.03 international units/mL to prilocaine 3% ent. This eutectic mixture is used in the preparation of Oraqix; Gr.: Emla; Funis; Opralix; Prinex; Xylocream; Hong injection did not reduce plasma concentrations of prilo topical dosage forms. Kong: Emla; Lidiprine; India: Asthesia; Emlap; Indon.: Dolones; caine after infiltration of a 60-rng dose into the upper pre· Emla; Estesia; Topsy; Irl. : Emla; Oraqix; Israel: Duo-Caine; Prilocaine Hydrochloride (BANM, USAN, r!NNM) molar region.1 Emla; Ital. : Emla; Oraqix; Jp n: EMLA; Malaysia: Emla; Lipro; l. Cannell H, Whelpton R. Systemic uptake ofprilocaine after injection of Mex.: Emla; Neth.: Emla; Oraqix; Norw.: Emla; Oraqix; Tapin; · �,57;•·.··prlfoca;na various formulations of the drug. Br Dent J 1986; 160: 47-9. ,l>;st i� j.?;• �f!itlrdf:lorur() .··�··•.'!Jrnocalna;, . •. NZ: Emla; Oraqix; Philipp. : Emla; Emlocaine; Pol.: Emla; Port. : h!d\oj:h� .Jruf'd.de; P!tto<:iiine, · · d�; P;rikxair�hydr�J· Emla; Oraqix; Rus.: Emla (3MJia); S.Afr. • Emla; Topla; Singa · (h!arhydrat� . Pril()l
Uses and Administration EHectson the CNS. For reference to the prilocaine serum concentrations associated with CNS toxicity, see Absorp Prilocaine is a local anaesthetic of the amide type with Pharmacopoeias. In Chin Bur. (see p. vii), Int., Jpn, US, and tion under Pharmacokinetics, below. .• actions and uses similar to those described on p. 1976.1. It Viet. has a similar anaesthetic potency to lidocaine. However, it Ph. Eur. 8: (Procaine Hydrochloride). A white or almost has a slower onset of action, less vasodilator activity, and a Porphyria. The Drug Database for Acute Porphyria, corn white crystalline powder or colourless crystals. Very soluble slightly longer duration of action; it is also less toxic. piled by the Norwegian Porphyria Centre (NAPOS) and in water; soluble in alcohol. A 2% solution in water has a pH Prilocaine hydrochloride is used for infiltration anaesthesia the Porphyria Centre Sweden, classifies prilocaine as not of 5.0 to 6.5. Protect from light. and nerve blocks in solutions of 0.5%, 1%, and 2%. A 1% porphyrinogenic; it may be used as a drug of first choice solution is also used for epidural analgesia and a 2% and no precautions are needed. 1 USP 36: (Procaine Hydrochloride). Odourless, small, whlte solution is used for epidural anaesthesia; for intravenous 1. The Drug Database for Acute Porphyria. Available at: http://www. crystals or white, crystalline powder. Soluble 1 in 1 of water regional anaesthesia 0.5% solutions are used. A 3% drugs-porphyria.org (accessed 05/l0/11) and 1 in 15 of alcohol; slightly soluble in chloroform; solution with the vasoconstrictor felypressin (p. 2502.3) or a practically insoluble in ether. 4% solution without are used for dental procedures. A 4% Interactions solution with adrenaline 1 in 200 000 is also used for Incompatibility. Procaine hydrochloride bas been reported dentistry in some countries. Carbonated solutions of For interactions associated with local anaesthetics, see to be incompatible with aminophylline, barbiturates, prilocaine have also been tried in some countries in epidural p. 1979.3. magnesium sulfate, phenytoin sodium, sodium bicarb and brachial plexus nerve blocks (see under Administration, Methaemoglobinaemia may occur at lower doses of onate, and amphotericin B. p. 1976.2). Prilocaine is used for surface anaesthesia in a prilocaine in patients receiving therapy with other drugs eutectic mixture with lidocaine. (Local anaesthetic known to cause such conditions (e.g. sulfonamides such as Stabilityof solutions. Degradation of procaine in a cardio techniques are discussed on p. 1977.2.) sulfamethoxazole in co-trimoxazole). plegic solution containing magnesium, sodium, potassium, The dosage used in various local anaesthetic and calcium salts was found to be temperature depen procedures varies with the site of injection and the Neuromuscular blockers. For a possible interaction dent.1 At a storage temperature of 6 degrees the shelf-life procedure used. The recommended maximum single between mivacurium and prilocaine, see under Atracurium, of the solution was 5 weeks and this was increased to 9 dose in adults for prilocaine hydrochloride is 400 rng if used p. 2033.1. 1 weeks when the storage temperature was -10 degrees.
All cross-references refer to entries in Volume A 1995
Using carbon dioxide instead of nitrogen in the head space 80% of the para-aminobenzoic acid is excreted unchanged anaesthesia and nerve block in dental procedures. did not affect stability of procaine. or conjugated in the urine. About 30% of the Propoxycaine has a more rapid onset and a longer duration I. Synave R, et a!. Stability of procaine hydrochloride in a cardioplegic diethylaminoethanol is excreted in the urine, the remainder of action than that of procaine. solution containing bicarbonate. J Clin Hosp Phann 1985; 10: 385-8. being metabolised in the liver. See also under Local Anaesthetics, p. 1979.3. Preparations Uses and Administration ...... PharmacopoeialPreparations Procaine hydrochloride, a para -aminobenzoic acid ester, is a USP 36: Propoxycaine and Procaine Hydrochlorides and local anaesthetic with actions and uses similar to those ProprietaryPreparations (details are given in Volume B) Levonordefrin Injection; Propoxycaine and Procaine Hydro described on p. 1976.1. Because of its poor penetration of Single-ingredient Preparations.Arg. : Endocaina; Fadacaina; Pro chlorides and Norepinephrine Bitartrate Injection. intact mucous membranes, procaine is ineffective for canest; Austda: Geroaslan H3t; Gerovital H3t; Novanaest; surface application and has been chiefly used by injection, Canad.: Novocaint; Ger.: Hewedolor Procain; Lophakomp-Pro although in general it has been replaced by lidocaine and cain; Pasconeural-Injektopas; Hong Kong: Gerovital H3t; Ital.: Proxymetacaine Hydrochloride other local anaesthetics. It has a slow onset of action and a Lenident; Singapore: Procanol; USA: Novocaint; Venez.: Artro (BANM, r/NNM) short duration of action. It has vasodilator activity and cel; Bioquel; Genaplex. therefore a vasoconstrictor may be added to delay Arg. : 6-Copin; Dastonil; Gingeron; absorption and increase the duration of action. Procaine Multi-ingredient Preparations. KH3t; Levantol Procaina; Longevital; Otalex G; Otonorthia; has mainly been used for infiltration anaesthesia, peripheral Austral.: Cardioplegia Concentrate; Austria: KH3; Braz.: nerve blocks, and spinal block. (Local anaesthetic Aftine; Bismu-Jet; Claudemor; Colutoide; Dentisant; Fonergin; techniques are discussed on p. 1977.2.) It has also been Otoloide; Oturga; Chile: Biocord-E; Biocord; Diltotal; Infor; used in cardioplegic solutions to protect the myocardium Pantibant; China: Compound Anisodine (J!::ilt\"i'iPW/l); Jinquan during cardiac surgery. (�;R);Cz. : Solutio Thomas cum Procaino; Denm.: Kardioplext; Procaine hydrochloride is given in concentrations of 0.5 Fr.: Otylol; Ger.: Gero H3 Aslant; Hewedolor plus Coffeint; to 2%. The dosage depends on the site of injection and the Otalgan; Gr.: Cardioplegia; KH3; Hong Kong: Cardioplegia; procedure used, as well as the status of the patient. KH3; Hung.: Hemorid; Hemorid; India: Cardiplegin; Florodd; Procaine hydrochloride has been used with propox KP-Plegia; Indon.: Cardioplegia; Irl.: Cardioplegia; Ital.: Dento ycaine in dentistry. sedina; Ginvapast; Neo-Ustiol; Otalgan; Otomidone; Otopax; Procaine forms poorly soluble salts or conjugates with Ustiosan; Malaysia: Cardioplegia; NZ: KH3; Rus.: Menovasin (Meuoml3lrn); OrrocnaBHH ; some drugs, for example penicillin, and is used to prolong Ottoslavin ( ) Solutan (CoJIYfaH)t; S. A r. : Universal Earache Dropst; Singapore: Cardioplegia; their action after injection. It may also reduce the pain of f Spain: Anestesia Local Braun S/A; Co Bucal; Coliriocilina NOTE. PROX is a code approved by the BP 2014 for use on injection. Adren Astrt; Eupnol; Kanafosal Prednit; Kanafosalt; Neoco single unit doses of eye drops containing proxymetacaine Procaine-N-glucoside hydrochloride has been included lant; Nulacin Fermentost; Oftalmol Ocular; Otosedolt; Switz. : hydrochloride where the individual container may be too in a preparation for gastrointestinal disorders, and procaine Anaestalgint; Ginvapast; Otalgan; Otosan; Thai.: Cardioplegia; small to bear all the appropriate labelling information. ascorbate has been included in a multivitamin preparation. KH3t; Ukr.: Menovasan (MeuoBa3aH). PROXFLN is a similar code approved for eye drops containing proxymetacaine hydrochloride and fluorescein Arg. : Betametasona B 12; Braz.: Dexaco Action. For a comparison of the vasoactivity of procaine Used asan adjunct in:. sodium. and some other local anaesthetics, see p. 1976.2. bal; Dexador; Dexagil; Dexaneurin; Ger.: Eukalisan Nt. Pharmacopoeias. In Br. and US. Homoeopathic Preparations. Ger.: NeyChon Nr 68; NeyGero Nr Dementia. Procaine hydrochloride has been used for 64; NeyGeront Vitalkapsein A. BP 2014: (Proxymetacaine Hydrochloride). A white or many years for its anti-ageing effects including the pre almost white, odourless or almost odourless, crystalline vention of dementia (p. 388.1) and cognitive impairment Pharmacopoeial Preparations powder. Soluble in water and in chloroform; very soluble in USP 36: Procaine and Tetracaine Hydrochlorides and Levonor but its value is not established. A systematic review1 found dehydrated alcohol; practically insoluble in ether. A 1% defrin Injection; Procaine Hydrochloride and Epinephrine no evidence of its benefit; some serious adverse effects solution in water has a pH of 5.7 to 6.4. Protect from light. Injection; Procaine Hydrochloride Injection; Propoxycaine and were associated with long-term use. Procaine Hydrochlorides and Levonordefrin Injection; Propox USP 36: (Proparacaine Hydrochloride). A white to off 1. Szatmilri S, Bereczki D. Procaine treatments for cognition and dementia. ycaine and Procaine Hydrochlorides and Norepinephrine white, or faintly buff-coloured, odourless, crystalline Available in The Cochrane Database of Systematic Reviews; Issue 4. Bitartrate Injection. powder. Soluble in water, in warm alcohol, and in methyl Chichester: John Wiley; 2008 (accessed 231l2/09). alcohol; insoluble in ether and in benzene. Adverse Effects, Treatment, and Precautions ...... Propanocaine Hydrochloride (riNNMJ Uses and Administration As for Local Anaesthetics in general, p. 1978.1, p. 1979.1, 467Ch; ·•. c�e···· ·p�qparrocarra; •.• f'ropapP<"afna, and p. 1979.1, respectively. .!-lidroclorut9 . · Proxymetacaine hydrochloride, a meta �aminobenzoic acid hldr<;�cloruro .de; Propanocafne, gntor!Jydrat� .derf't(,lpano-· ester, is a local anaesthetic with actions and uses similar to H�ctro<;MIOtid m; · those described on p. 1976.1. It is used for surface Effects an the cardiovascular system. Severe hypotension Cilirtl V flPQf!afloKa��.f!�tl:ti:ro>benzoic acid ester, is a local 10 minutes for up to 3 applications, or 1 or 2 drops are of procaine hydrochloride, 4.8% gave a positive reaction. I anaesthetic (p. 1976.1) that has been used topically for instilled 2 to 3 minutes before the procedure. For deeper l For reports of hypersensitivity including anaphylactic surface anaesthesia. anaesthesia such as needed for cataract extraction drop is reactions associated with procaine and other local anaes instilled every 5 to 10 minutes to a total of 5 to 7 thetics, see under Adverse Effects of Local Anaesthetics, applications. p. 1978.2. (details are given in Volume B) l. Rudzki E, Kleniewska D. The epidemiology of contact dermatitis in ProprietaryPreparations Trigeminal neuralgia. There have been anecdotal reports Poland. Br J Dermatol 1970; 83: 543-5. Multi-ingredient Preparations. Spain: Detrainet. that proxymetacaine eye drops relieved trigeminal neur algia (p. 11.2) refractory to carbamazepine.I.2 However, a Systemic lupus erythematosus. The limited theoretical controlled study failed to show any benefit.' risk from using procaine for local anaesthesia in patients Propoxycaine Hydrochloride (riNNMI l. Zavon MR, Fichte CM. Trigeminal neuralgia relieved by ophthalmic who have had procainamide-induced SLE was aired some anesthetic. lAMA 1991; 265: 2807. years ago.1·3 hlidrodoruro Gle•r:>ra po�icaina; . Prop<�'>icafna, hidr�forvfll!·de; 2. Zavon MR, Fichte CM. Trigeminal neuralgia relieved by optical . anesthesia. 1991; 266: 1649. l. Dubois EL Procaine anesthesia after procainamide-induced systemic Chlorhydrate. de; Propox.yc�ini Hydrochlor lAMA Propoxyca'ine; · : 3. Kondziolka D, et al. The effect of single-application topical ophthalmic erythematosus. lAMA 1977; 238: 2201. idufl1;.,.,prpp(l )l �i!liUJ'll' • f;l p()F!O,KC\o'I�(!V!H(! anesthesia in patients with trigeminal neuralgia: a randomized double 2. Alarc6n-Segovia D. Procaine anesthesia after procainamide-induced · � � · ChloriJ:!�:.• . . blind placebo-controlled trial. J Neurosurg 1994; 80: 993-7. systemic erythematosus. lAMA 1977; 238: 2201. f�PQxnopvt,q, . • • • • . . 3. Lee SL. Procaine anesthesia after procainamide-induced systemic 2-Diethy!Qminoethyl . 4:"amino-:2-propoxyt:JenzQate hydro erythematosus. lAMA 1977; 238: 2201. chloride• Adverse Effects, Treatment, and Precautions
C,oHi�N�O,,Hc;ti"330•9 \ . . ·. 86'43- 1 As for Local Anaesthetics in general, p. 1978.1, p. 1979.1, Interactions 0\,S.<--: (prdpoxycainei: and p. 1979.1, respectively. For interactions associated with local anaesthetics, see hydrochloride) . A severe immediate-type corneal reaction to proxymeta p. 1979.3. UN/1•7':'0.K49f)Q39[3 46. caine may rarely occur. Allergic contact dermatitis has also Pharmacopoeias. In us. been reported. Diuretics. Use with acetazolamide extends the plasma half USP 36: life of procaine. 1 (Propoxycaine Hydrochloride). A white odourless Effects an the skin. Exacerbation of Stevens-Johnson crystalline solid. discolours on prolonged exposure to light l. Calvo R, et al. Effects of disease and acetazolamide on procaine It syndrome has been reported1 in a woman after hydrolysis by red blood cell enzymes. Clin Pharmacol Ther 1980; 27: 179- and air. Soluble 1 in 2 of water, I in 10 of alcohol, and I in ophthalmic anaesthesia with proxymetacaine hydro 83. 80 of ether; practically insoluble in acetone and in chloride. chloroform. A 2% solution in water has a pH of about 5.4. 1. Ward B, et al. Dermatologic reaction in Stevens-Johnson syndrome after Pharmacokinetics Protect from light. ophthalmic anesthesia with proparacaine hydrochloride. Am 1 Ophthalmol 1978; 86: 133-5. Procaine is poorly absorbed from mucous membranes and is usually given parenterally. It is rapidly hydrolysed by Profile plasma cholinesterase to para -aminobenzoic acid and Propoxycaine hydrochloride, a para-aminobenzoic acid Interactions diethylaminoethanol; some may also be metabolised in ester, is a local anaesthetic (p. 1976.1 ). It has been used with For interactions associated with local anaesthetics, see the liver. Only about 6% is bound to plasma proteins. About procaine hydrochloride and a vasoconstrictor for infiltration p. 1979.3.
The symbol t denotes a preparation no longer actively marketed