enhance systemic absorption. Lidoca<strong>in</strong>e is <strong>in</strong>cluded <strong>in</strong>some <strong>in</strong>jections, such as depot corticosteroids, to preventpa<strong>in</strong> <strong>and</strong> itch<strong>in</strong>g caused by local irritation.Priloca<strong>in</strong>e is an amide local anesthetic with a similarpotency to lidoca<strong>in</strong>e. However, it has a slower onset ofaction, less vasodilator activity, <strong>and</strong> a slightly longerduration of action; it is also less toxic. Priloca<strong>in</strong>e isused for <strong>in</strong>filtration anesthesia <strong>and</strong> nerve blocks <strong>in</strong>solutions of 0.5%, 1%, <strong>and</strong> 2%. A 1% or 2% solutionis used for epidural anesthesia; for <strong>in</strong>travenous regionalanesthesia, 0.5% solutions are used. For dentalprocedures, a 3% solution with the vasoconstrictorfelypress<strong>in</strong> or a 4% solution without is used. A 4%solution with ep<strong>in</strong>ephr<strong>in</strong>e (1 <strong>in</strong> 200 000) is also usedfor dentistry <strong>in</strong> some countries. Carbonated solutionsof priloca<strong>in</strong>e have also been used for epidural <strong>and</strong> brachialplexus nerve blocks. Priloca<strong>in</strong>e is used for surfaceanesthesia <strong>in</strong> a eutectic mixture with lidoca<strong>in</strong>e EMLA.(ii) Doses, side effects, <strong>and</strong> toxicityThe dose of lidoca<strong>in</strong>e depends on the site of <strong>in</strong>jection<strong>and</strong> the procedure but <strong>in</strong> general, the maximum doseshould not exceed 3 mgÆkg )1 (maximum 200 mg)unless vasoconstrictor is also used. Lidoca<strong>in</strong>e hydrochloridesolutions conta<strong>in</strong><strong>in</strong>g ep<strong>in</strong>ephr<strong>in</strong>e (1 <strong>in</strong>200 000) for <strong>in</strong>filtration anesthesia <strong>and</strong> nerve blocksare available; higher concentrations of ep<strong>in</strong>ephr<strong>in</strong>e areseldom necessary, except <strong>in</strong> dentistry, where solutionsof lidoca<strong>in</strong>e hydrochloride with ep<strong>in</strong>ephr<strong>in</strong>e 1 <strong>in</strong>80 000 are traditionally used. The maximum dose ofep<strong>in</strong>ephr<strong>in</strong>e should be 5 microgm/kg )1 <strong>and</strong> of lidoca<strong>in</strong>e5mgÆkg )1 . Ep<strong>in</strong>ephr<strong>in</strong>e-conta<strong>in</strong><strong>in</strong>g solutions shouldnot be used near extremities such as for digital orpenile blocks. Lidoca<strong>in</strong>e may be used <strong>in</strong> a variety offormulations for surface anesthesia. Lidoca<strong>in</strong>e o<strong>in</strong>tmentis used for anesthesia of sk<strong>in</strong> <strong>and</strong> mucous membranes.Gels are used for anesthesia of the ur<strong>in</strong>arytract <strong>and</strong> for analgesia of aphthous ulcers. Topicalsolutions are used for surface anesthesia of mucousmembranes of the mouth, throat, <strong>and</strong> upper gastro<strong>in</strong>test<strong>in</strong>altract. For pa<strong>in</strong>ful conditions of the mouth <strong>and</strong>throat, a 2% solution may be used or a 10% spraycan be applied to mucous membranes. Eye drops conta<strong>in</strong><strong>in</strong>glidoca<strong>in</strong>e hydrochloride 4% with fluoresce<strong>in</strong>are used <strong>in</strong> tonometry. Other methods of dermal delivery<strong>in</strong>clude a transdermal patch of lidoca<strong>in</strong>e 5% forthe treatment of pa<strong>in</strong> associated with postherpetic neuralgia<strong>and</strong> an iontophoretic drug delivery system <strong>in</strong>corporat<strong>in</strong>glidoca<strong>in</strong>e <strong>and</strong> ep<strong>in</strong>ephr<strong>in</strong>e.Lidoca<strong>in</strong>e is bound to plasma prote<strong>in</strong>s, <strong>in</strong>clud<strong>in</strong>g a1-acid glycoprote<strong>in</strong> (AAG). The extent of b<strong>in</strong>d<strong>in</strong>g is variablebut is about 66%. Plasma prote<strong>in</strong> b<strong>in</strong>d<strong>in</strong>g oflidoca<strong>in</strong>e depends <strong>in</strong> part on the concentrations ofboth lidoca<strong>in</strong>e <strong>and</strong> AAG. Any alteration <strong>in</strong> the concentrationof AAG can greatly affect plasma concentrationsof lidoca<strong>in</strong>e. Plasma concentrations decl<strong>in</strong>erapidly after an <strong>in</strong>travenous dose with an <strong>in</strong>itial halflifeof
Priloca<strong>in</strong>e has relatively low toxicity compared withmost amide-type local anesthetics. It is 55% bound toplasma prote<strong>in</strong>s <strong>and</strong> is rapidly metabolized ma<strong>in</strong>ly <strong>in</strong>the liver <strong>and</strong> kidneys <strong>and</strong> is excreted <strong>in</strong> the ur<strong>in</strong>e. Oneof the pr<strong>in</strong>cipal metabolites is o-toluid<strong>in</strong>e, which isbelieved to cause the methemoglob<strong>in</strong>emia observedafter large doses. It crosses the placenta <strong>and</strong> dur<strong>in</strong>gprolonged epidural anesthesia may producemethemoglob<strong>in</strong>emia <strong>in</strong> the fetus. It is distributed <strong>in</strong>tobreast milk. The peak serum concentration of priloca<strong>in</strong>eassociated with CNS toxicity is 20 mgÆml )1 .Symptoms usually occur when doses of priloca<strong>in</strong>ehydrochloride exceed about 8 mgÆkg )1 but the veryyoung may be more susceptible. Methemoglob<strong>in</strong>emiahas been observed <strong>in</strong> neonates whose mothers receivedpriloca<strong>in</strong>e shortly before delivery <strong>and</strong> it has also beenreported after prolonged topical application of a priloca<strong>in</strong>e/lidoca<strong>in</strong>eeutectic mixture <strong>in</strong> children. Methemoglob<strong>in</strong>emiamay be treated by giv<strong>in</strong>g oxygen followed,if necessary, by IV methylthion<strong>in</strong>ium chloride.Priloca<strong>in</strong>e should be used with caution <strong>in</strong> patientswith anemia, congenital or acquired methemoglob<strong>in</strong>emia,cardiac or ventilatory failure, or hypoxia. Priloca<strong>in</strong>ehas been associated with acute attacks ofporphyria <strong>and</strong> is considered unsafe <strong>in</strong> porphyricpatients. Methemoglob<strong>in</strong>emia may occur at lowerdoses of priloca<strong>in</strong>e <strong>in</strong> patients receiv<strong>in</strong>g therapy withother drugs known to cause such conditions (e.g., sulfonamidessuch as sulfamethoxazole <strong>in</strong> co-trimoxazole).(iii) EMLALidoca<strong>in</strong>e forms a mixture with priloca<strong>in</strong>e that has amelt<strong>in</strong>g po<strong>in</strong>t lower than that of either <strong>in</strong>gredient. Thiseutectic mixture conta<strong>in</strong><strong>in</strong>g lidoca<strong>in</strong>e 2.5% <strong>and</strong> priloca<strong>in</strong>e2.5% can produce local anesthesia when appliedto <strong>in</strong>tact sk<strong>in</strong> as a cream. It is used extensively for proceduralpa<strong>in</strong> <strong>in</strong>clud<strong>in</strong>g venepuncture, <strong>in</strong>travenous orarterial cannulation, lumbar puncture, m<strong>in</strong>or dermatologicalprocedures, <strong>and</strong> others (see section 4.0). Theeutectic cream is usually applied to sk<strong>in</strong> under anocclusive dress<strong>in</strong>g for at least 60 m<strong>in</strong> <strong>and</strong> a maximumof 5 h. Transient paleness, redness, <strong>and</strong> edema of thesk<strong>in</strong> may occur follow<strong>in</strong>g application.Eutectic mixtures of lidoca<strong>in</strong>e <strong>and</strong> priloca<strong>in</strong>e areused <strong>in</strong> neonates <strong>and</strong> are safe <strong>in</strong> s<strong>in</strong>gle doses. Therehas been concern that excessive absorption (particularlyof priloca<strong>in</strong>e) might lead to methemoglob<strong>in</strong>emiaparticularly after multiple applications. For this reason,the maximum number of doses per day should belimited <strong>in</strong> the neonate. In some countries, EMLA hasbeen licensed for use <strong>in</strong> neonates provided that theirgestational age is at least 37 weeks, <strong>and</strong> that methemoglob<strong>in</strong>values are monitored <strong>in</strong> those aged 3 months orless. In fact, systemic absorption of both drugs fromthe eutectic cream appears to be m<strong>in</strong>imal across <strong>in</strong>tactsk<strong>in</strong> even after prolonged or extensive use. However,EMLA should not be used <strong>in</strong> <strong>in</strong>fants under 1 yearwho are receiv<strong>in</strong>g methemoglob<strong>in</strong>-<strong>in</strong>duc<strong>in</strong>g drugs; itshould not be used on wounds or mucous membranesor for atopic dermatitis. EMLA should not be appliedto or near the eyes because it causes corneal irritation,<strong>and</strong> it should not be <strong>in</strong>stilled <strong>in</strong>to the middle ear. Itshould be used with caution <strong>in</strong> patients with anemia orcongenital or acquired methemoglob<strong>in</strong>emia.6.2.3 Tetraca<strong>in</strong>e (amethoca<strong>in</strong>e)(i) PreparationsTetraca<strong>in</strong>e is a potent, para-am<strong>in</strong>obenzoic acid esterlocal anesthetic used for surface anesthesia <strong>and</strong> sp<strong>in</strong>alblock. It is highly lipophilic <strong>and</strong> can penetrate <strong>in</strong>tactsk<strong>in</strong>. Its use <strong>in</strong> other local anesthetic techniques isrestricted by its systemic toxicity.For anesthesia of the eye, solutions conta<strong>in</strong><strong>in</strong>g 0.5–1% tetraca<strong>in</strong>e hydrochloride <strong>and</strong> o<strong>in</strong>tments conta<strong>in</strong><strong>in</strong>g0.5% tetraca<strong>in</strong>e have been used. Instillation of a 0.5%solution produces anesthesia with<strong>in</strong> 25 s that lasts for15 m<strong>in</strong> or longer <strong>and</strong> is suitable for use before m<strong>in</strong>orsurgical procedures.A 4% gel (Ametop) is used as a percutaneous localanesthetic. This formulation of 4% tetraca<strong>in</strong>e producesmore rapid <strong>and</strong> prolonged surface anesthesia thanEMLA <strong>and</strong> is significantly better <strong>in</strong> reduc<strong>in</strong>g pa<strong>in</strong>caused by laser treatment of port w<strong>in</strong>e sta<strong>in</strong>s <strong>and</strong> forvenous cannulation. A transdermal patch is effective,<strong>and</strong> patches conta<strong>in</strong><strong>in</strong>g a mixture of lidoca<strong>in</strong>e <strong>and</strong> tetraca<strong>in</strong>ehave also been tried. Tetraca<strong>in</strong>e has been<strong>in</strong>corporated <strong>in</strong>to a mucosa-adhesive polymer film torelieve the pa<strong>in</strong> of oral lesions result<strong>in</strong>g from radiation<strong>and</strong> ant<strong>in</strong>eoplastic therapy. Liposome-encapsulated tetraca<strong>in</strong>ecan provide adequate surface anesthesia.LAT (LET) 4% lidoca<strong>in</strong>e, 0.1% ep<strong>in</strong>ephr<strong>in</strong>e, <strong>and</strong>0.5% tetraca<strong>in</strong>e have been comb<strong>in</strong>ed <strong>in</strong> a gel <strong>and</strong>applied as a surface anesthetic to lacerations of thesk<strong>in</strong> especially the face <strong>and</strong> scalp. It is less a pa<strong>in</strong>fulalternative to LA <strong>in</strong>filtration prior to suture of lacerations.(ii) Dosage side effects <strong>and</strong> toxicityTetraca<strong>in</strong>e: A st<strong>in</strong>g<strong>in</strong>g sensation may occur when tetraca<strong>in</strong>eis used <strong>in</strong> the eye. Absorption of tetraca<strong>in</strong>e frommucous membranes is rapid, <strong>and</strong> adverse reactions canª 2012 Blackwell Publish<strong>in</strong>g Ltd, Pediatric Anesthesia, 22 (Suppl. 1), 1–79 69
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doi: 10.1111/j.1460-9592.2012.3838.
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1.6 Contact informationCorresponden
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RecommendationsChildren’s self-re
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Topical anesthetic preparations, fo
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2.7.6 Laparoscopic surgeryGood prac
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In order to assess pain, effective
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Postoperative painl NCCPC-PV (Non-C
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68 Broome ME, Richtsmeier A, Maikle
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