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Lidocaine (INN, BAN) /ˈlaɪdɵkeɪn/, xylocaine, or lignocaine (AAN, former BAN) /ˈlɪɡnɵkeɪn/ is a common local anesthetic and class-1b antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning, and pain from skin inflammations, injected as a dental anesthetic, or used as a local anesthetic for minor surgery.

It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic healthcare system.^[1]

1 Medical uses
- 1.1 Insensitivity
2 Contraindications
3 Adverse effects
4 Overdosage
5 Interactions
6 Dosage forms
- 6.1 Adulterant in cocaine
7 Preparation
8 Pharmacokinetics
9 Pharmacodynamics
- 9.1 Anaesthesia
- 9.2 Antiarrhythmic
10 History
11 Recreational use
12 Compendial status
13 See also
14 References
15 External links

Medical uses

The efficacy profile of lidocaine as a local anesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. Therefore, lidocaine is suitable for infiltration, block, and surface anesthesia. Longer-acting substances such as bupivacaine are sometimes given preference for subdural and epidural anesthesias; lidocaine, though, has the advantage of a rapid onset of action. Epinephrine (adrenaline) vasoconstricts arteries, reducing bleeding and also delays the resorption of lidocaine, almost doubling the duration of anaesthesia. For surface anesthesia, several available formulations can be used for endoscopies, before intubations, etc. Buffering the pH of lidocaine makes local freezing less painful.^[2] Lidocaine drops can be used on the eyes for short ophthalmic procedures.

Topical lidocaine has been shown in some patients to relieve the pain of postherpetic neuralgia (a complication of shingles), though not enough study evidence exists to recommend it as a first-line treatment.^[3] Intravenous lidocaine also has uses as a temporary fix for tinnitus. Although not completely curing the disorder, it has been shown to reduce the effects by around two-thirds.^[4]^[5]

Lidocaine is also the most important class-1b antiarrhythmic drug; it is used intravenously for the treatment of ventricular arrhythmias (for acute myocardial infarction, digoxin poisoning, cardioversion, or cardiac catheterization) if amiodarone is not available or contraindicated. Lidocaine should be given for this indication after defibrillation, CPR, and vasopressors have been initiated. A routine prophylactic administration is no longer recommended for acute cardiac infarction; the overall benefit of this measure is not convincing.

Inhaled lidocaine can be used as an antitussive (cough suppressor) acting peripherally to reduce the cough reflex. This application can be implemented as a safety and comfort measure for patients who have to be intubated, as it reduces the incidence of coughing and any tracheal damage it might cause when emerging from anesthesia.^[6]^[7]^[8]

Lidocaine, along with ethanol, ammonia, and acetic acid, has also been proven to be effective in treating jellyfish stings, both numbing the affected area and preventing further nematocyst discharge.^[9]^[10]

Insensitivity

Relative insensitivity to lidocaine is genetic. In hypokalemic sensory overstimulation, relative insensitivity to lidocaine has been described in people who also have attention deficit hyperactivity disorder.^[11] In dental anesthesia, a relative insensitivity to lidocaine can occur for anatomical reasons due to unexpected positions of nerves. Some people with Ehlers-Danlos syndrome are insensitive to lidocaine.^[12]

Contraindications

Absolute contraindications for the use of lidocaine include:

Heart block, second or third degree (without pacemaker)
Severe sinoatrial block (without pacemaker)
Serious adverse drug reaction to lidocaine or amide local anesthetics
Hypersensitivity to corn and corn-related products (corn-derived dextrose is used in the mixed injections)
Concurrent treatment with quinidine, flecainide, disopyramide, procainamide (class I antiarrhythmic agents)
Prior use of amiodarone hydrochloride
Adams-Stokes syndrome^[13]
Wolff-Parkinson-White syndrome^[13]
Lidocaine viscous is not recommended by the FDA to treat tooth pain in children and infants.^[14]

Exercise caution in patients with any of these:

Hypotension not due to arrhythmia
Bradycardia
Accelerated idioventricular rhythm
Elderly patients
Pseudocholinesterase deficiency
Intra-articular infusion (this is not an approved indication and can cause chondrolysis)
Porphyria, especially acute intermittent porphyria; lidocaine has been classified as porphyrogenic because of the hepatic enzymes it induces,^[15] although clinical evidence suggests it is not.^[16] Bupivacaine is a safe alternative in this case.
Impaired liver function - people with lowered hepatic function may have an adverse reaction with repeated administration of lidocaine because the drug is metabolized by the liver. Adverse reactions may include neurological symptoms (e.g. dizziness, nausea, muscle twitches, vomiting, or seizures).^[17]

Adverse effects

Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, and allergic reactions only rarely occur.^[18] Systemic exposure to excessive quantities of lidocaine mainly result in central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. ADRs by system are:

CNS excitation: nervousness, agitation, anxiety, apprehension, tingling around the mouth (circumoral paraesthesia), headache, hyperesthesia, tremor, dizziness, pupillary changes, psychosis, euphoria, hallucinations, and seizures
CNS depression with increasingly heavier exposure: drowsiness, lethargy, slurred speech, hypoesthesia, confusion, disorientation, loss of consciousness, respiratory depression and apnoea.
Cardiovascular: hypotension, bradycardia, arrhythmias, flushing, venous insufficiency, increased defibrillator threshold, edema, and/or cardiac arrest – some of which may be due to hypoxemia secondary to respiratory depression.^[19]
Respiratory: Bronchospasm, dyspnea, respiratory depression or arrest
Gastrointestinal: metallic taste, nausea, vomiting
Ears: tinnitus
Eyes: local burning, Conjunctival hyperemia, corneal epithelial changes/ulceration, diplopia, visual changes (opacification)
Skin: itching, depigmentation, rash, urticaria, edema, angioedema, bruising, inflammation of the vein at the injection site, irritation of the skin when applied topically
Blood: methemoglobinemia
Allergy

ADRs associated with the use of intravenous lidocaine are similar to toxic effects from systemic exposure above. These are dose-related and more frequent at high infusion rates (≥3 mg/min). Common ADRs include: headache, dizziness, drowsiness, confusion, visual disturbances, tinnitus, tremor, and/or paraesthesia. Infrequent ADRs associated with the use of lidocaine include: hypotension, bradycardia, arrhythmias, cardiac arrest, muscle twitching, seizures, coma, and/or respiratory depression.^[19]

It is generally safe to use lidocaine with vasoconstrictor such as epinephrine including in regions such as the nose, ears, fingers and toes.^[20] While concerns of tissue death if used in these areas have been raised evidence does not support these concerns.^[20]

Overdosage

Overdoses with lidocaine can be a result of excessive administration by topical or parenteral routes, accidental oral ingestion of topical preparations by children who are more susceptible to overdose, accidental intravenous (rather than subcutaneous, intrathecal, or paracervical) injection, or prolonged use of subcutaneous infiltration anesthesia during cosmetic surgical procedures. These occurrences have often led to severe toxicity or death in both children and adults. Lidocaine and its two major metabolites may be quantified in blood, plasma, or serum to confirm the diagnosis in potential poisoning victims or to assist in the forensic investigation in a case of fatal overdose. It is important in the interpretation of analytical results to recognize that lidocaine is often routinely administered intravenously as an antiarrhythmic agent in critical cardiac-care situations.^[21] Treatment with intravenous lipid emulsions (used for parental feeding) to reverse the effects of local anaesthetic toxicity is becoming more commonplace.^[22]

Interactions

Any drugs that are also ligands of CYP3A4 and CYP1A2 can potentially increase serum levels and potential for toxicity or decrease serum levels and the efficacy, depending on whether they induce or inhibit the enzymes, respectively. Drugs that may increase the chance of methemoglobinemia should also be considered carefully. Dronedarone and liposomal morphine are both absolutely contraindicated, as they may increase the serum levels, but hundreds of other drugs require monitoring for interaction.^[23]

Dosage forms

Lidocaine hydrochloride 2% epinephrine 1:80,000 solution for injection in a cartridge

Lidocaine hydrochloride 1% solution for injection

Topical lidocaine spray

Lidocaine, usually in the form of lidocaine hydrochloride, is available in various forms including:

Injected local anesthetic (sometimes combined with epinephrine to reduce bleeding)
Dermal patch (sometimes combined with prilocaine)
Intravenous injection
Intravenous infusion
Intraosseous infusion
Nasal instillation/spray (combined with phenylephrine)
Oral gel (often referred to as "viscous lidocaine" or abbreviated "lidocaine visc" or "lidocaine HCl visc" in pharmacology; used as teething gel)
Oral liquid
Oral and topical ointments, with and without flavoring, respectively^[24]^[25]
Topical gel (as with aloe vera gels that include lidocaine)^[26]
Topical liquid
Lidocaine HCl 2% jelly, combined with hypromellose, to anesthetize and lubricate the urethra, etc., for inserting a catheter or instrument
Topical patch (lidocaine 5%), marketed since 1999 in the US by Endo Pharmaceuticals^[27] as "Lidoderm" - and since 2007 in the UK by Grünenthal as "Versatis"
Topical ointment (lidocaine 5%) as a temporary reliever of discomfort associated anorectal disorders, such as hemorrhoids, marketed as an over-the-counter product in the US as RectiCare since 2012 by Ferndale Healthcare, Inc
Topical aerosol spray
Inhaled by nebulizer
As a component of a GI cocktail used in emergency rooms
Ophthalmic solution

Adulterant in cocaine

Lidocaine is often added to cocaine as a diluent.^[28] Cocaine numbs the gums when applied, and since lidocaine causes stronger numbness,^[29] a user gets the impression of high-quality cocaine when in actuality, the user is receiving a diluted product.^[30]

Preparation

Lidocaine may be prepared in two steps by the reaction of 2,6-xylidine with chloroacetyl chloride, followed by the reaction with diethylamine:^[31]^[32]

Preparation of lidocaine

Pharmacokinetics

The onset of action of lidocaine is about 45 to 90 sec and its duration is 10 to 20 min. It is about 95% metabolized (dealkylated) in the liver mainly by CYP3A4 to the pharmacologically active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half-life than lidocaine, but also is a less potent sodium channel blocker.^[33] The volume of distribution is 1.1-2.1 l/kg, but congestive heart failure can decrease it. About 60-80% circulates bound to the protein alpha₁ acid glycoprotein. The oral bioavailability is 35% and the topical bioavailability is 3%.

The elimination half-life of lidocaine is biphasic and around 90–120 min in most patients. This may be prolonged in patients with hepatic impairment (average 343 min) or congestive heart failure (average 136 min).^[34] Lidocaine is excreted in the urine (90% as metabolites and 10% as unchanged drug).^[35]

Pharmacodynamics

Anaesthesia

Lidocaine alters signal conduction in neurons by blocking the fast voltage-gated Na⁺ channels in the neuronal cell membrane responsible for signal propagation.^[36] With sufficient blockage, the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anaesthetic effect by not merely preventing pain signals from propagating to the brain, but by stopping them before they begin. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations also affect other modalities of neuron signaling.

Antiarrhythmic

The same principle applies for this drug's actions in the heart. Blocking sodium channels in the conduction system, as well as the muscle cells of the heart, raises the depolarization threshold, making the heart less likely to initiate or conduct early action potentials that may cause an arrhythmia.^[37]

History

Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name 'xylocaine' by Swedish chemist Nils Löfgren in 1943.^[38]^[39]^[40] His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.^[38] It was first marketed in 1949.

Recreational use

Lidocaine is not currently listed by the World Anti-Doping Agency as an illegal substance.^[41] It is used as an adjuvant, adulterant, and diluent to street drugs such as cocaine and heroin.^[42]

Compendial status

Japanese Pharmacopoeia 15
United States Pharmacopeia 31^[43]

References

^ "WHO Model List of Essential Medicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ Cepeda MS, Tzortzopoulou A, Thackrey M, Hudcova J, Arora Gandhi P, Schumann R (2010). "Adjusting the pH of lidocaine for reducing pain on injection". Cochrane Database Syst Rev (12): CD006581. doi:10.1002/14651858.CD006581.pub2. PMID 21154371.
^ Khaliq W, Alam S, Puri N (2007). "Topical lidocaine for the treatment of postherpetic neuralgia". Cochrane Database Syst Rev (2): CD004846. doi:10.1002/14651858.CD004846.pub2. PMID 17443559.
^ "New hope for tinnitus sufferers". BBC News. 9 January 2008.
^ Kalcioglu MT, Bayindir T, Erdem T, Ozturan O. (2005). "Objective evaluation of the effects of intravenous lidocaine on tinnitus.". Hearing Research 199 (1-2): 81–8. doi:10.1016/j.heares.2004.08.004. PMID 15574302.
^ Adcock JJ, Douglas GJ, Garabette M, Gascoigne M, Beatch G, Walker M, Page CP (February 2003). "RSD931, a novel anti-tussive agent acting on airway sensory nerves". Br. J. Pharmacol. 138 (3): 407–16. doi:10.1038/sj.bjp.0705056. PMC 1573683. PMID 12569065.
^ Biller JA (2007). "Airway obstruction, bronchospasm, and cough". In Berger AM, Shuster JL, Von Roenn JH. Principles and practice of palliative care and supportive oncology. Hagerstwon, MD: Lippincott Williams & Wilkins. pp. 297–307. ISBN 978-0-7817-9595-1. Inhaled lidocaine is used to suppress cough during bronchoscopy. Animal studies and a few human studies suggest that lidocaine has an antitussive effect…
^ Minogue SC, Ralph J, Lampa MJ (Oct 2004). "Laryngotracheal topicalization with lidocaine before intubation decreases the incidence of coughing on emergence from general anesthesia.". Anesthesia and Analgesia 99 (4): 1253–7, table of contents. doi:10.1213/01.ANE.0000132779.27085.52. PMID 15385385.
^ Birsa LM, Verity PG, Lee RF (May 2010). "Evaluation of the effects of various chemicals on discharge of and pain caused by jellyfish nematocysts". Comp. Biochem. Physiol. C Toxicol. Pharmacol. 151 (4): 426–30. doi:10.1016/j.cbpc.2010.01.007. PMID 20116454.
^ Morabito R, Marino A, Dossena S, La Spada G (Jun 2014). "Nematocyst discharge in Pelagia noctiluca (Cnidaria, Scyphozoa) oral arms can be affected by lidocaine, ethanol, ammonia and acetic acid.". Toxicon : official journal of the International Society on Toxinology 83: 52–8. doi:10.1016/j.toxicon.2014.03.002. PMID 24637105.
^ Segal MM, Rogers GF, Needleman HL, Chapman CA (Dec 2007). "Hypokalemic sensory overstimulation.". Journal of child neurology 22 (12): 1408–10. doi:10.1177/0883073807307095. PMID 18174562.
^ Hakim AJ, Grahame R, Norris P, Hopper C (February 2005). "Local anaesthetic failure in joint hypermobility syndrome". J R Soc Med 98 (2): 84–5. doi:10.1258/jrsm.98.2.84. PMC 1079398. PMID 15684369.
^ ^a ^b "Lidocaine Hydrochloride and 5% Dextrose Injection". Safety Labeling Changes. FDA Center for Drug Evaluation and Research (CDER). January 2014.
^ "Lidocaine Viscous: Drug Safety Communication - Boxed Warning Required - Should Not Be Used to Treat Teething Pain". FDA Center for Drug Evaluation and Research (CDER). June 2014.
^ "Table 96–4. Drugs and Porphyria". Merck Manual. Merck & Company, Inc. 2011.
^ "Lidocaine - N01BB02". Drug porphyrinogenicity monograph. The Norwegian Porphyria Centre and the Swedish Porphyria Centre. strong clinical evidence points to lidocaine as probably not porphyrinogenic
^ Khan, M. Gabriel (2007). Cardiac Drug Therapy (7th ed. ed.). Totowa, NJ: Humana Press. ISBN 9781597452380.
^ Jackson D, Chen AH, Bennett CR (October 1994). "Identifying true lidocaine allergy". J Am Dent Assoc 125 (10): 1362–6. PMID 7844301.
^ ^a ^b Australian Medicines Handbook. Adelaide, S. Aust: Australian Medicines Handbook Pty Ltd. 2006. ISBN 0-9757919-2-3. ^{[page needed]}
^ ^a ^b Nielsen, LJ; Lumholt, P; Hölmich, LR (27 October 2014). "[Local anaesthesia with vasoconstrictor is safe to use in areas with end-arteries in fingers, toes, noses and ears.]". Ugeskrift for laeger 176 (44). PMID 25354008.
^ Baselt R (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 840–4. ISBN 0-9626523-7-7.
^ Picard J, Ward SC, Zumpe R, Meek T, Barlow J, Harrop-Griffiths W (February 2009). "Guidelines and the adoption of 'lipid rescue' therapy for local anaesthetic toxicity". Anaesthesia 64 (2): 122–5. doi:10.1111/j.1365-2044.2008.05816.x. PMID 19143686.
^ https://online.epocrates.com/u/104316/lidocaine/Drug+Interactions. Retrieved April 2014. Missing or empty |title= (help)
^ "Product information for lidocaine ointment, USP 5%, spearmint flavored". Product Insert. Taro Pharmaceutical Industries Ltd. Retrieved July 27, 2009.
^ "Lidocaine Ointment Prescribing Information". Drugs.com. Retrieved January 22, 2012.
^ "Solarcaine". Schering-Plough Healthcare Products, Inc. Retrieved July 27, 2009.
^ "Lidoderm (Lidocaine Patch 5%)". Our Products. Endo Pharmaceuticals. Retrieved 18 October 2012.
^ Bernardo NP, Siqueira MEPB, De Paiva MJN, Maia PP (2003). "Caffeine and other adulterants in seizures of street cocaine in Brazil". International Journal of Drug Policy 14 (4): 331–4. doi:10.1016/S0955-3959(03)00083-5.
^ Kimberly H (1997-12-15). "Take a big-picture approach when dealing with corneal sensation". Retrieved 2009-04-23. Lidocaine is more potent, with rapid diffusion and penetration.
^ "UNITED STATES of America, Plaintiff-Appellee, v. Luis A. CUELLO, Alvaro Bastides-Benitez, John Doe, a/k/a Hugo Hurtado, and Alvaro Carvajal, Defendants-Appellants". Docket No. 78-5314. United States Court of Appeals, Fifth Circuit. 1979-07-25.
^ Reilly TJ (1999). "The Preparation of Lidocaine". Journal of Chemical Education 76 (11): 1557. doi:10.1021/ed076p1557.
^ US patent 2441498, Bengt JL, Niels, ML, "Alkyl glycinanilides", issued 1948-05-11, assigned to Astra Apotekarnes Kem FAB
^ Lewin NA, Nelson LH (2006). "Chapter 61: Antidysrhythmics". In Flomenbaum N, Goldfrank LR, Hoffman RL, Howland MD, Lewin NA, Nelson LH. Goldfrank's Toxicologic Emergencies (8th ed.). New York: McGraw-Hill. pp. 963–4. ISBN 0-07-143763-0.
^ Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M (April 1973). "Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans". Ann. Intern. Med. 78 (4): 499–508. doi:10.7326/0003-4819-78-4-499. PMID 4694036.
^ Collinsworth KA, Kalman SM, Harrison DC (1974). "The clinical pharmacology of lidocaine as an antiarrhythymic drug". Circulation 50 (6): 1217–30. doi:10.1161/01.CIR.50.6.1217. PMID 4609637.
^ Carterall, William A. (2001). "Sodium Channels and Neuronal Hyperexcitability". Novartis Foundation Symposia 241. p. 206. doi:10.1002/0470846682.ch14. ISBN 9780470846681. |chapter= ignored (help)
^ Sheu SS, Lederer WJ (Oct 1985). "Lidocaine's negative inotropic and antiarrhythmic actions. Dependence on shortening of action potential duration and reduction of intracellular sodium activity.". Circulation research 57 (4): 578–90. doi:10.1161/01.res.57.4.578. PMID 2412723.
^ ^a ^b Löfgren N (1948). Studies on local anesthetics: Xylocaine: a new synthetic drug (Inaugural dissertation). Stockholm, Sweden: Ivar Heggstroms. OCLC 646046738. ^{[page needed]}
^ Löfgren N, Lundqvist B (1946). "Studies on local anaesthetics II". Svensk Kemisk Tidskrift 58: 206–17.
^ Wildsmith JAW (2011). "Lidocaine: A more complex story than 'simple' chemistry suggests". The Proceedings of the History of Anaesthesia Society 43: 9–16.
^ "The 2010 Prohibited List International Standard". The World Anti-Doping Code. World Anti-Doping Agency (WADA). 19 September 2009.
^ "New York Drug Threat Assessment". National Drug Intelligence Center. November 2002.
^ "Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test". The United States Pharmacopeial Convention. November 30, 2007.

External links

U.S. National Library of Medicine: Drug Information Portal - Lidocaine
Endo Pharmaceuticals' Lidoderm website

UpToDate Contents

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1. I群抗不整脈薬の主な副作用 major side effects of class i antiarrhythmic drugs
2. 局所麻酔剤の浸潤 infiltration of local anesthetics
3. 小児における局所麻酔剤 topical anesthetics in children
4. 小児に対する手術室外での鎮静処置に使用する薬剤 pharmacologic agents for pediatric procedural sedation outside of the operating room
5. 小児に対する手術室外での鎮静処置に使用する薬剤の選択 selection of medications for pediatric procedural sedation outside of the operating room

English Journal

Working memory deficits and related disinhibition of the cAMP/PKA/CREB are alleviated by prefrontal α4β2*-nAChRs stimulation in aged mice.

Vandesquille M, Baudonnat M, Decorte L, Louis C, Lestage P, Béracochéa D.SourceCNRS, Univ. Bordeaux, INCIA UMR 5287, Bordeaux, France; Institut de Recherches SERVIER (IDRS), Croissy-sur-Seine, France.
Neurobiology of aging.Neurobiol Aging.2013 Jun;34(6):1599-609. doi: 10.1016/j.neurobiolaging.2012.10.006. Epub 2013 Jan 23.
The present study investigates in aged mice the working memory (WM) enhancing potential of the selective α4β2* nicotinic receptor agonist S 38232 as compared with the cholinesterase inhibitor donepezil, and their effect on cAMP response element binding protein (CREB) phosphorylation (pCREB) as a m
PMID 23352115

Characteristics of amorphous complex formed between indomethacin and lidocaine hydrochloride.

Shimada Y, Goto S, Uchiro H, Hirota K, Terada H.SourceFaculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Colloids and surfaces. B, Biointerfaces.Colloids Surf B Biointerfaces.2013 May 1;105:98-105. doi: 10.1016/j.colsurfb.2012.12.026. Epub 2012 Dec 31.
Indomethacin (IM) easily forms an amorphous complex with lidocaine (LC) by heat treatment. To know the mechanism involved in the formation of this complex, we studied temperature-dependent phase changes in mixtures of IM and lidocaine hydrochloride (LH), in which the cationic form of LC forms a salt
PMID 23352941

Japanese Journal

眼窩軟部組織内異物に対し侵入路を染色しこれを追跡して摘出する方法

宮地有理,ニアズアヒメテ・ジャン,渡辺克益
東京醫科大學雜誌 71(1), 51-56, 2013-01-30
NAID 10031161683

主任教授推薦論文眼窩軟部組織内異物に対し侵人路を染色しこれを追跡して摘出する方法

宮地有理,ニアズアヒメテ・ジャン,渡辺克益,Miyachi.Yuri,Nias Ahimet,Watanebe Katsueki
東京医科大学雑誌 71(1), 51-56, 2013-01
NAID 120005341569

50％ブドウ糖液を使用した胸膜癒着術の有効性

藤野孝介,久保田伊知郎,本岡大和,池田公英,森毅,鈴木実
日本呼吸器外科学会雑誌 27(6), 670-674, 2013
肺切除後の気漏や手術を避けたい気胸患者に対して50%ブドウ糖液を使用した胸膜癒着術を施行し良好な成績を得ているので報告する．方法は，50%ブドウ糖液200 mlと1%キシロカイン10 mlを胸腔内に注入する．2012年4月から7月までに11例に施行し9例で成功し，2例は不成功でありOK-432による胸膜癒着術に変更し気漏の消失に至った．この2例は高度の肺気腫を伴い気漏の量が多い症例であった．本法は …
NAID 130004495360

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★リンクテーブル★

リンク元	「リドカイン」
関連記事	「Xylocaine」

「リドカイン」

Lidocaine
Systematic (IUPAC) name
	2-(diethylamino)-; N-(2,6-dimethylphenyl)acetamide
Clinical data
Trade names	Xylocaine
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	AU: A; US: B;
Legal status	AU: Prescription Only (S4); US: ℞-only (OTC for ≤1%);
Routes of; administration	intravenous, subcutaneous, topical, oral
Pharmacokinetic data
Bioavailability	35% (oral); 3% (topical)
Metabolism	Hepatic, 90% CYP1A2-mediated
Half-life	1.5–2 hours
Excretion	renal
Identifiers
CAS Registry Number	137-58-6 ; 73-78-9 (hydrochloride)
ATC code	C01BB01 C05AD01 D04AB01 N01BB02 R02AD02 S01HA07 S02DA01
PubChem	CID 367
IUPHAR ligand	2623
DrugBank	DB00281
ChemSpider	3548
UNII	98PI200987
KEGG	D00358
ChEBI	CHEBI:6456
ChEMBL	CHEMBL79
Synonyms	N-(2,6-dimethylphenyl)-N2,N2-diethylglycinamide
Chemical data
Formula	C14H22N2O
Molecular mass	234.34 g/mol
	SMILES O=C(Nc1c(cccc1C)C)CN(CC)CC;
	InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) ; Key:NNJVILVZKWQKPM-UHFFFAOYSA-N ;
Physical data
Melting point	68 °C (154 °F)
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　　[★]

英: lidocaine
化: 塩酸リドカイン lidocaine hydrochloride
商: キシロカイン xylocaine Xylocain、リグノカイン lignocaine Lignocain; ＴＤゼット、アネトカイン、アネトカインビスカス、エムラ、オーラ、オリベス、キシレステシン、キシレステシンA、キシロカイン、セフメタゾン、チエナム、デンタカイン、ネイサート、ネリコルト、ネリザ、ネリダロン、ネリプロクト、パートラン、パートランビスカス、パートランポンプ、フリードカイン、ヘモリサット、ヘルミチン、ヘルミチンS、ペンマリン、ペンレス、ボラザ、ボラザG、メドカイン、ユーパッチ、ラセナゾリン、歯科用キシロカインカートリッジ; (ジフルコルトロン、リドカイン)ネイサート、ネリコルト、ネリザ、ネリダロン、ネリプロクト
関: 抗不整脈薬、プロカイン

アニリド系
局所麻酔薬 (SPC.172)
抗不整脈薬

クラスIb

Naチャネルブロック

APD短縮

作用機序

Naチャネル遮断

薬理作用

活動電位の最大分極速度を抑制

結合解離速度は早く、正常心拍の伝導を阻害しない。

APDの短縮はリドカインのNaチャネルに対する結合解離が早いため？？ (→Sicillian Gambitの分類)

動態

適応

心室性不整脈
心肺蘇生　アミオダロンの方がよく使われる
無効：心房細動、心房頻拍

注意

禁忌

副作用

「Xylocaine」

　　[★]

キシロカイン

関: lidocaine、lidocaine hydrochloride、lignocaine

lidocaine

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[pmid21154371-2] Cepeda MS, Tzortzopoulou A, Thackrey M, Hudcova J, Arora Gandhi P, Schumann R (2010). "Adjusting the pH of lidocaine for reducing pain on injection". Cochrane Database Syst Rev (12): CD006581. doi:10.1002/14651858.CD006581.pub2. PMID 21154371.

[pmid17443559-3] Khaliq W, Alam S, Puri N (2007). "Topical lidocaine for the treatment of postherpetic neuralgia". Cochrane Database Syst Rev (2): CD004846. doi:10.1002/14651858.CD004846.pub2. PMID 17443559.

[4] "New hope for tinnitus sufferers". BBC News. 9 January 2008.

[5] Kalcioglu MT, Bayindir T, Erdem T, Ozturan O. (2005). "Objective evaluation of the effects of intravenous lidocaine on tinnitus.". Hearing Research 199 (1-2): 81–8. doi:10.1016/j.heares.2004.08.004. PMID 15574302.

[pmid12569065-6] Adcock JJ, Douglas GJ, Garabette M, Gascoigne M, Beatch G, Walker M, Page CP (February 2003). "RSD931, a novel anti-tussive agent acting on airway sensory nerves". Br. J. Pharmacol. 138 (3): 407–16. doi:10.1038/sj.bjp.0705056. PMC 1573683. PMID 12569065.

[isbn0-7817-9595-8-7] Biller JA (2007). "Airway obstruction, bronchospasm, and cough". In Berger AM, Shuster JL, Von Roenn JH. Principles and practice of palliative care and supportive oncology. Hagerstwon, MD: Lippincott Williams & Wilkins. pp. 297–307. ISBN 978-0-7817-9595-1. Inhaled lidocaine is used to suppress cough during bronchoscopy. Animal studies and a few human studies suggest that lidocaine has an antitussive effect…

[8] Minogue SC, Ralph J, Lampa MJ (Oct 2004). "Laryngotracheal topicalization with lidocaine before intubation decreases the incidence of coughing on emergence from general anesthesia.". Anesthesia and Analgesia 99 (4): 1253–7, table of contents. doi:10.1213/01.ANE.0000132779.27085.52. PMID 15385385.

[pmid20116454-9] Birsa LM, Verity PG, Lee RF (May 2010). "Evaluation of the effects of various chemicals on discharge of and pain caused by jellyfish nematocysts". Comp. Biochem. Physiol. C Toxicol. Pharmacol. 151 (4): 426–30. doi:10.1016/j.cbpc.2010.01.007. PMID 20116454.

[10] Morabito R, Marino A, Dossena S, La Spada G (Jun 2014). "Nematocyst discharge in Pelagia noctiluca (Cnidaria, Scyphozoa) oral arms can be affected by lidocaine, ethanol, ammonia and acetic acid.". Toxicon : official journal of the International Society on Toxinology 83: 52–8. doi:10.1016/j.toxicon.2014.03.002. PMID 24637105.

[11] Segal MM, Rogers GF, Needleman HL, Chapman CA (Dec 2007). "Hypokalemic sensory overstimulation.". Journal of child neurology 22 (12): 1408–10. doi:10.1177/0883073807307095. PMID 18174562.

[pmid15684369-12] Hakim AJ, Grahame R, Norris P, Hopper C (February 2005). "Local anaesthetic failure in joint hypermobility syndrome". J R Soc Med 98 (2): 84–5. doi:10.1258/jrsm.98.2.84. PMC 1079398. PMID 15684369.

[MedWatch_Lidocaine_HCl-13] "Lidocaine Hydrochloride and 5% Dextrose Injection". Safety Labeling Changes. FDA Center for Drug Evaluation and Research (CDER). January 2014.

[MedWatch_Lidocaine_Viscous-14] "Lidocaine Viscous: Drug Safety Communication - Boxed Warning Required - Should Not Be Used to Treat Teething Pain". FDA Center for Drug Evaluation and Research (CDER). June 2014.

[url_www.merckmanuals.com-15] "Table 96–4. Drugs and Porphyria". Merck Manual. Merck & Company, Inc. 2011.

[urlLidocaine_-_N01BB02_-_Drug_porphyrinogenicity_monograph-16] "Lidocaine - N01BB02". Drug porphyrinogenicity monograph. The Norwegian Porphyria Centre and the Swedish Porphyria Centre. strong clinical evidence points to lidocaine as probably not porphyrinogenic

[Khan-17] Khan, M. Gabriel (2007). Cardiac Drug Therapy (7th ed. ed.). Totowa, NJ: Humana Press. ISBN 9781597452380.

[pmid7844301-18] Jackson D, Chen AH, Bennett CR (October 1994). "Identifying true lidocaine allergy". J Am Dent Assoc 125 (10): 1362–6. PMID 7844301.

[rossi-19] Australian Medicines Handbook. Adelaide, S. Aust: Australian Medicines Handbook Pty Ltd. 2006. ISBN 0-9757919-2-3. ^{[page needed]}

[Nie2014-20] Nielsen, LJ; Lumholt, P; Hölmich, LR (27 October 2014). "[Local anaesthesia with vasoconstrictor is safe to use in areas with end-arteries in fingers, toes, noses and ears.]". Ugeskrift for laeger 176 (44). PMID 25354008.

[isbn0-9626523-7-7-21] Baselt R (2008). Disposition of Toxic Drugs and Chemicals in Man (8th ed.). Foster City, CA: Biomedical Publications. pp. 840–4. ISBN 0-9626523-7-7.

[pmid19143686-22] Picard J, Ward SC, Zumpe R, Meek T, Barlow J, Harrop-Griffiths W (February 2009). "Guidelines and the adoption of 'lipid rescue' therapy for local anaesthetic toxicity". Anaesthesia 64 (2): 122–5. doi:10.1111/j.1365-2044.2008.05816.x. PMID 19143686.

[epocrates-23] ttps://online.epocrates.com/u/104316/lidocaine/Drug+Interactions. Retrieved April 2014. Missing or empty |title= (help)

[url_www.taro.com-24] "Product information for lidocaine ointment, USP 5%, spearmint flavored". Product Insert. Taro Pharmaceutical Industries Ltd. Retrieved July 27, 2009.

[urlLidocaine_Ointment_Official_FDA_information.2C_side_effects_and_uses.-25] "Lidocaine Ointment Prescribing Information". Drugs.com. Retrieved January 22, 2012.

[urlwww.solarcaine.com-26] "Solarcaine". Schering-Plough Healthcare Products, Inc. Retrieved July 27, 2009.

[urlEndo_Pharmaceuticals_.7C_All_Products_of_Endo_Pharmaceuticals-27] "Lidoderm (Lidocaine Patch 5%)". Our Products. Endo Pharmaceuticals. Retrieved 18 October 2012.

[28] Bernardo NP, Siqueira MEPB, De Paiva MJN, Maia PP (2003). "Caffeine and other adulterants in seizures of street cocaine in Brazil". International Journal of Drug Policy 14 (4): 331–4. doi:10.1016/S0955-3959(03)00083-5.

[29] Kimberly H (1997-12-15). "Take a big-picture approach when dealing with corneal sensation". Retrieved 2009-04-23. Lidocaine is more potent, with rapid diffusion and penetration.

[url599_F.2d_635-30] "UNITED STATES of America, Plaintiff-Appellee, v. Luis A. CUELLO, Alvaro Bastides-Benitez, John Doe, a/k/a Hugo Hurtado, and Alvaro Carvajal, Defendants-Appellants". Docket No. 78-5314. United States Court of Appeals, Fifth Circuit. 1979-07-25.

[31] Reilly TJ (1999). "The Preparation of Lidocaine". Journal of Chemical Education 76 (11): 1557. doi:10.1021/ed076p1557.

[32] US patent 2441498, Bengt JL, Niels, ML, "Alkyl glycinanilides", issued 1948-05-11, assigned to Astra Apotekarnes Kem FAB

[isbn0-07-143763-0-33] Lewin NA, Nelson LH (2006). "Chapter 61: Antidysrhythmics". In Flomenbaum N, Goldfrank LR, Hoffman RL, Howland MD, Lewin NA, Nelson LH. Goldfrank's Toxicologic Emergencies (8th ed.). New York: McGraw-Hill. pp. 963–4. ISBN 0-07-143763-0.

[pmid4694036-34] Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M (April 1973). "Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans". Ann. Intern. Med. 78 (4): 499–508. doi:10.7326/0003-4819-78-4-499. PMID 4694036.

[pmid4609637-35] Collinsworth KA, Kalman SM, Harrison DC (1974). "The clinical pharmacology of lidocaine as an antiarrhythymic drug". Circulation 50 (6): 1217–30. doi:10.1161/01.CIR.50.6.1217. PMID 4609637.

[novartis-36] Carterall, William A. (2001). "Sodium Channels and Neuronal Hyperexcitability". Novartis Foundation Symposia 241. p. 206. doi:10.1002/0470846682.ch14. ISBN 9780470846681. |chapter= ignored (help)

[37] Sheu SS, Lederer WJ (Oct 1985). "Lidocaine's negative inotropic and antiarrhythmic actions. Dependence on shortening of action potential duration and reduction of intracellular sodium activity.". Circulation research 57 (4): 578–90. doi:10.1161/01.res.57.4.578. PMID 2412723.

[lofgren_1948-38] Löfgren N (1948). Studies on local anesthetics: Xylocaine: a new synthetic drug (Inaugural dissertation). Stockholm, Sweden: Ivar Heggstroms. OCLC 646046738. ^{[page needed]}

[39] Löfgren N, Lundqvist B (1946). "Studies on local anaesthetics II". Svensk Kemisk Tidskrift 58: 206–17.

[40] Wildsmith JAW (2011). "Lidocaine: A more complex story than 'simple' chemistry suggests". The Proceedings of the History of Anaesthesia Society 43: 9–16.

[url_www.wada-ama.org-41] "The 2010 Prohibited List International Standard". The World Anti-Doping Code. World Anti-Doping Agency (WADA). 19 September 2009.

[42] "New York Drug Threat Assessment". National Drug Intelligence Center. November 2002.

[43] "Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test". The United States Pharmacopeial Convention. November 30, 2007.

Systematic (IUPAC) name


2-(diethylamino)- N-(2,6-dimethylphenyl)acetamide
Clinical data
Trade names	Xylocaine
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy category	AU: A US: B
Legal status	AU: Prescription Only (S4) US: ℞-only (OTC for ≤1%)
Routes of administration	intravenous, subcutaneous, topical, oral
Pharmacokinetic data
Bioavailability	35% (oral) 3% (topical)
Metabolism	Hepatic, 90% CYP1A2-mediated
Half-life	1.5–2 hours
Excretion	renal
Identifiers
CAS Registry Number	137-58-6^Y 73-78-9 (hydrochloride)
ATC code	C01BB01 C05AD01 D04AB01 N01BB02 R02AD02 S01HA07 S02DA01
PubChem	CID 367
IUPHAR ligand	2623
DrugBank	DB00281^Y
ChemSpider	3548^Y
UNII	98PI200987^Y
KEGG	D00358^Y
ChEBI	CHEBI:6456^Y
ChEMBL	CHEMBL79^Y
Synonyms	N-(2,6-dimethylphenyl)-N²,N²-diethylglycinamide
Chemical data
Formula	C₁₄H₂₂N₂O
Molecular mass	234.34 g/mol
SMILES O=C(Nc1c(cccc1C)C)CN(CC)CC
InChI InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) ^Y Key:NNJVILVZKWQKPM-UHFFFAOYSA-N ^Y
Physical data
Melting point	68 °C (154 °F)
Y (what is this?) (verify)

匿名

検索

案内

xylocaine