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 详细处方信息以本药内容附件PDF文件（201111123060516.pdf）的“原文Priscribing Information”为准
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部分中文利多卡因处方资料（仅供参考）

Endo公司的Lidoderm将继续增长
    Endo公司的利多卡因贴片（Lidoderm）已上市5年之久，仍保持强劲增长，在2004年及2005年的增长率分别为73%和36%。此外，据受访医生们预计该产品不管是用于获准的适应症还是非核准适应症，其应用都将继续增多，因此预计该产品在2007年的销售额将增长到6.44亿美元，超过了华尔街所预测的5.66亿美元。Lidoderm是Endo最畅销的产品，是唯一一种FDA批准的局部用利多卡因贴剂，用于疱疹后神经痛(PHN)所引起的疼痛。该产品还用于多种非核准适应症，如：下背痛、骨关节炎、糖尿病性神经痛。实际上，据Datamonitor公司调查的医生们估计，Lidoderm的全部处方中只有27%用于PHN，其余的全部用于非核准适应症。

    Lidoderm逐年强劲增长的原因在于该产品的良好安全性及有效性，而且与2004年相比较2005年的销售代表增加了近两倍，使销售力量大大增长，还有就是该产品用于非核准适应症临床试验数据取得了满意了结果。

    据处方量较高的疼痛门诊医生称，他们所给予Lidoderm处方的PHN患者人数将保持平稳，将近全部PHN患者的60%，这就意味着处方量的增长要依赖于待处理病例的增多。而且，他们将继续给予非核准适应症患者Lidoderm处方，使其用药比例增高。

    来自四个Lidoderm高处方量的科室（疼痛门诊、神经科、风湿科、普通科）受访医生们均表示在未来两年里，他们将继续增多Lidoderm的应用。

    Lidoderm在非疼痛处理科室的应用也将日益增多，但在PHN及下背痛治疗中的市场渗透率仍低于疼痛处理科室。这表明Lidoderm仍然有很大的持续的增长潜力。

    在医生好评及明显的增长潜力的支持先，Lidoderm 2006年的销售额将较2005年增长33%达5.58亿美元，2007年的销售额将增长到6.44亿美元，分别高于华尔街5.22亿及5.66亿美元的预期。另外，受访医生中绝大多数并不认为辉瑞公司的Lyrica（一种口服药，于2005年9月在各大市场上市）将会影响到Lidoderm的应用，很大的可能是两种产品联合使用。

利多卡因贴片对骨关节炎痛同COX-2抑制剂相当
    2005年04月06日 研究人员在美国疼痛学会的波士顿会议上报告，使用利多卡因贴片（Lidoderm，Endo制药公司）来治疗膝部的骨关节炎在减轻疼痛上似乎同COX-2抑制剂塞来考昔（西乐葆）一样有效。

    美国宾州奥尔托纳关节炎和骨质疏松中心的基维兹（AlanJ.Kivitz）和同事随机指定143名病人或用Lidoderm，或用塞来考昔200mg/天。一或两个膝部每天用一次贴片，一片完整帖片用于关节前面，另一片1/3的贴片贴在关节后面。

    12周后，Lidoderm组71%、塞来考昔组72%在每天的平均疼痛强度上改善30%或以上。“这些结果令人激动，并说明应当进行Lidoderm治疗膝骨关节炎的进一步试验”，作者说，“这就是说病人有了其它选择。这样如果病人对一种药效果不够或不能耐受，就能试用另一种了，因为每位病人的反应不同。个体化治疗的关键是找到特定病人的最佳干预治疗，因此选择越多越好”。

    基维兹说，他正为某些病人开予Lidoderm，“但一般而言，保险机构不会纳入这种标签外使用的药物（目前ＦＤＡ批准Lidoderm用于治疗疱疹后神经痛），因此获得其它证明其安全有效性的研究非常重要”。这些试验，以及评估Lidoderm治疗后背痛的安全有效性，现已在进行之中。

利多卡因Lidocaine 
中文别名：利多卡因、赛罗卡因、昔罗卡因、盐酸利多卡因
英文别名：Lidocainum、Lighocaine、Lignocaine
药品类别：局部麻醉药
化学名称：Acetamide, 2-diethylamino-N-(2,6-dimethylphenyl)-
  
药理药动
药效学
本品属ⅠB 类抗心律失常药。具有局麻作用。可抑制心肌细胞舒张期除极，减低心室肌及心肌传导纤维的自律性及兴奋性，但对心房及窦房结作用很轻。相对地延长有效不应期，降低心室肌兴奋性，提高室颤阈值。治疗剂量不减慢正常心肌的房室传导速度，也不减低心肌收缩力及血压，甚至加快心肌传导纤维的传导速度，减轻单向阻滞，从而消除折返性室性心律失常。
药动学
口服生物利用度低，经肝脏首次通过效应即锐减。肌注后吸收完全。吸收后迅速分布入心、脑、肾及其他血运丰富的组织，然后分布至脂肪及肌肉组织。表观分布容积约1L/kg,心力衰竭时分布容积减低。蛋白结合率约51％。吸烟者结合率可比不吸烟者高些。肌注后5～15分钟起效,一次肌注200mg后15～20分钟达治疗浓度,持续60～90分钟;静注后立即起效(约45～90秒),持续10～20分钟。治疗血药浓度为1.5～5μg/ml, 中毒血药浓度为5μg/ml以上。持续静滴3-4小时达稳态血药浓度，急性心肌梗塞者需8-10小时。90%经肝脏代谢，代谢物单乙基甘氨酰二甲苯胺(MEGX)及甘氨酰二甲苯胺(GX)具有药理活性, 持续静滴24小时以上者, 代谢产物可产生治疗及中毒作用。静注后半衰期α约10分钟,β约1～2小时。GX半衰期较长约10小时,MEGX半衰期近似原药。心衰、肝病患者、老年人及持续静滴24～36小时以上, 本品的清除减慢。由肾脏排泄，10％为原药,58％为代谢物(GX)，不能被血液透析清除。
利多卡因的局麻效能与持续时间均较普鲁卡因强，但毒性也较大。在肝内代谢的去乙基代谢产物(单乙基甘氨酰胺二甲苯)，仍具有局麻性能，毒性加大，再经酰胺酶进一步降解随尿排出，用量的 10％则以原形排出。

适应症
静注适用于因急性心肌梗塞、外科手术、洋地黄中毒及心脏导管等所致急性室性心律失常，包括室性早搏、室性心动过速及室颤。其次也用于癫痫持续状态用其他抗惊厥药无效者及局部或椎管内麻醉。

用法用量
成人常用量：①肌内注射，一次按体重 4.3mg/kg，60—90分钟后可重复一次；②静脉注射，按体重 1mg/kg(一般用 50—100mg)作为首次负荷量静注 2—3分钟，必要时每 5分钟后再重复注射 1—2次，一小时内最大量不超过 300mg；③静脉滴注，用负荷量后可继续以每分钟 1—4mg速度静滴维持；或以每分钟按体重 0.015—0.03mg/kg速度静脉滴注。老年人、心力衰竭、心源性休克、肝血流量减少、肝或肾功能障碍时应减少用量，以每分钟0.5—1mg静滴。
极量：肌内或静脉注射 1小时内最大负荷量按体重 4.5mg/kg(或 300mg)。最大维持量为每分钟 4mg。
[制剂与规格]盐酸利多卡因注射液(1)5ml：100mg(2)20ml：400mg。
1．成人常用量①骶管阻滞用于分娩镇痛，用量以 200mg(1.0％)为限；用于外科止痛可酌增至 200—250mg(1.0—1.5％)。②硬脊膜外阻滞，胸腰段，250—300mg(1.5—2.0％)。③浸润局麻或静注区域阻滞，50～200mg(0.25—0.5％)。④外周神经阻滞，臂丛(单侧)250—300mg(1.5％)；牙科，20—100mg(2.0％)；肋间神经(每支)，30mg(1.0％)；宫颈旁浸润，左右侧各 100mg(0.5—1.0％)；椎旁脊神经阻滞(每支)，20—50mg(1.0％)；阴部神经，左右侧各 100mg(0.5—1.0％)。⑤交感神经节阻滞，颈星状神经 50mg(1.0％)，腰 50—100mg(1.0％)。⑥一次限量，一般不要超过 200mg(4.0mg/kg)，药液中加用肾上腺素用量可增至 200—250mg(6.0mg/kg)。静注区域阻滞，极量 4mg/kg。治疗用药静注，第一次初量 1mg/kg，极量 4mg/kg，成人静滴每分钟以 1mg为限。反复多次给药，相距间隔时间不得短于 60分钟。
2．小儿常用量随个体而异，一次给药最高总量不得超过 4.0—4.5mg/kg，常用 0.25—0.5％溶液，特殊情况才用 1.0％溶液。
[附]外用给药的剂型及用法与用量：
1．软膏剂5％，牙科可涂于口腔内吹干的粘膜表面；2.5％的软膏供皮肤外用，治疗瘙痒。
2。冻胶剂2％，成人常用采涂抹于食管、咽喉、气管或尿道等导管的外壁；妇女作阴道检查时可用棉花签沾 5～7ml涂于局部；尿道扩张术或膀胱镜检查时用量可达 400mg。24小时处方以 600mg为限。
3，漱口液 2％，用于口腔病，成人每次用 15ml，漱后吐出，每 3小时一次；用于咽痛，需要时可吞咽，处方 24小时以 8次的用量为限，即 2.4g，小儿酌减。
4。外用液4％，一般在作胃镜前直接涂抹或喷雾于咽喉或口腔粘膜表面，偶作鼻腔填塞，每次 24小时处方不得超过 3.0mg/kg，小儿慎用。
5。气雾剂或喷雾剂2—4％，可供作内窥镜用，每次 10—30ml，处方限量 3.0mg/kg。
阻滞麻醉,1-2%溶液,一次不超过0.4g;表面麻醉,1-2%溶液,喷雾或蘸药贴敷,一次不超过0.25g; 浸润麻醉,1-2%溶液,每小时不超过0.4g;治心律失常,一次静注1-3mg/kg,如无效,10-15分钟后同量再注一次.同时取100mg加于5-10%葡萄糖液100-200ml内作静滴,一次治疗总量4-6mg/kg.

不良反应
总的发生率约为 6.3％，多数不良反应与剂量有关。
(1)神经：头昏、眩晕、恶心、呕吐、倦怠、说话不清、感觉异常及肌肉颤抖、惊厥、神智不清及呼吸抑制，需减药或停药。惊厥时可静注地西泮、短效巴比妥制剂或短效肌肉松弛剂。
(2)心血管：①大剂量可产生严重窦性心动过缓、心脏停博、严重房室传导阻滞及心肌收缩力减低，需及时停药，必要时用阿托品、异丙肾上腺素或起博器治疗；血压下降时给予吸氧、纠正酸中毒及升压药；保持气道通畅等及其他复苏措施；②心房扑动患者用时可能使心室率增快。
(3)过敏反应：有皮疹及水肿等表现应停药，严重者可致呼吸停止，皮肤试验对预测过敏反应价值有限。
头晕,眼发黑,静注后可能出现心动过缓,房室传导阻滞,室颤,剂量过大有惊厥,心脏停博,过敏性休克,思睡,昏迷,抽搐. 个别病例可有视神经炎,出现暂时的失明。
脊髓注射或外用利多卡因均可能导致致命的支气管痉挛。成人可能出现呼吸窘迫综合征，但较罕见。
随着血药浓度的增加可能产生轻度头痛和耳鸣，视觉障碍，肌肉颤搐，惊厥，神志丧失最后至昏迷。在极高血药浓度下可引起心血管抑制和呼吸停止。这些不良反应的产生与误入血管内有完全关系。
据报道，利多卡因在体外能抑制人白细胞的随机运动性和吞噬能力。
有报告发生心动过缓、室上性心动过速、扭转性心律失常或低血压者。
利多卡因中毒的中枢神经系统表现为思睡、昏迷、抽搐或呼吸受抑制，最常见于快速静脉注入，特别是充血性心衰或肝病患者。

禁忌症
(1)交叉过敏反应，对其他胺类局麻药过敏者可能对本品也过敏，但利多卡因与普鲁卡因胺、奎尼丁间尚无交叉过敏反应的报道。
(2)已有报道分娩前静注本品，数分钟胎儿血药浓度可达母亲血药浓度的 55—100％。也有报道母亲用药后导致胎儿心动过缓或过速，甚至引起新生儿高铁血红蛋白血症，孕妇用药须权衡利弊。新生儿用药可引起中毒，早产儿的 T1／2为 3.16小时，较正常婴儿长(1.8小时)。
(3)老年人用药应根据需要及耐受程度调整剂量，一般高龄患者(＞70岁)剂量应减半。
(4)下列情况应禁用；①阿斯综合征；②严重心脏阻滞，包括 Ⅱ或 Ⅲ度房室传导阻滞、双束支阻滞；③严重窦房结功能障碍。
(5)下列情况应慎用；①充血性心力衰竭，严重心肌受损；②肝功能障碍；③老年人；④低血容量及休克；⑤不完全性房室传导阻滞或室内传导阻滞；⑥肝血流量减低；⑦肾功能障碍；⑧严重塞性心动过缓；⑨预激综合征(可能加重)。
对患心脏和肝脏疾病的病人，应减少利多卡因的剂量，在肝病患者中此药的半衰期较长。由于它能迅速通过胎盘和在新生儿体内的半衰期延长，所以有可能引起新生儿抑制。观察到通常只有在原有心率缓慢的胎儿才会出现致死的心动过缓。
严重房室传导阻滞禁用。

药物相互作用
(1)β受体阻滞药可以减少肝血流量，故合用时可能减低肝脏对本品的清除，不良反应增多加剧。
(2)神经肌肉阻滞药合用较大剂量利多卡因(按体重 5mg/kg以上)，可使这类药的阻滞作用增强。
(3)与抗惊厥药合用，可增加心肌抑制作用，产生心脏停搏。此外二者合用，中枢神经系统不良反应也增加。苯妥英钠及苯巴比妥也可以增快本品的肝脏代谢，从而降低静注后的血药浓度。曾有报道用本品静注再加以戊巴比妥静注时，可产生窒息致死。
(4)与普鲁卡因胺合用，可产生一过性谵妄及幻觉，但不影响本品的血药浓度。
(5)异丙肾上腺素，试验证明因增加肝血流量，故本品的总清除率随之增高。
(6)去甲肾上腺素，试验证明因减低肝血流量，故本品的总清除率下降。
(7)西咪替丁可减少本品的清除。
有报告普萘洛尔使利多卡因清除减少，而增大不良反应的发生率。利多卡因与β受体拮抗剂合用有良好的相互作用。

Lidoderm
Generic Name: lidocaine topical (LYE doe kane TOP i kal)
Brand Names: AneCream, AneCream with Tegaderm, Anestacon, Bactine, LidaMantle, Lidocream, Lidoderm, Lidosense5, LMX 4, LMX 4 with Tegaderm, LMX 5, Medi-Quik Spray, Senatec, Xylocaine Jelly, Xylocaine Topical, Zilactin-L

What is Lidoderm?
Lidoderm is a local anesthetic (numbing medication). It works by blocking nerve signals in your body.

Lidoderm is used to relieve post-shingles pain. Apply Lidoderm only to intact skin with no blisters.

Lidocaine topical in other formulations is used to reduce pain or discomfort caused by skin irritations such as sunburn, insect bites, poison ivy, poison oak, poison sumac, and minor cuts, scratches, hemorrhoids, and burns. Lidocaine topical can also be used to treat sores inside the mouth, during dental procedures to numb the gums, and to numb the skin for a medical procedure (such as getting stiches).

Important information about Lidoderm
An overdose of Lidoderm can cause fatal side effects if too much lidocaine is absorbed through your skin and into your blood. This is more likely to occur when using a numbing medicine without the advice of a medical doctor (such as during a cosmetic procedure like laser hair removal). Overdose symptoms may include uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops). Your body may absorb more lidocaine if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of Lidoderm needed to numb the skin or relieve pain. Do not use large amounts of Lidoderm, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.

Before using Lidoderm
An overdose of numbing medications can cause fatal side effects if too much of the medicine is absorbed through your skin and into your blood.

Overdose is more likely to occur when using a numbing medicine without the advice of a medical doctor (such as during a cosmetic procedure like laser hair removal). Symptoms may include uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops).

Do not use Lidoderm if you are allergic to any other type of numbing medicine.

Before using Lidoderm, tell your doctor if you are allergic to any drugs, or if you have liver disease, or broken, swollen, or damaged skin. You may not be able to use Lidoderm, or you may need dosage adjustments or special tests during treatment.

FDA pregnancy category B. Lidoderm is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Lidocaine can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use Lidoderm?
Use Lidoderm exactly as directed on the label, or as it has been prescribed by your doctor. Do not use the medication in larger amounts, or use it for longer than recommended.

Your body may absorb more lidocaine if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of this medication needed to numb the skin or relieve pain. Do not use large amounts of Lidoderm, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.

Do not apply Lidoderm to swollen skin areas or deep puncture wounds. Avoid using the medicine on skin that is raw or blistered, such as a severe burn or abrasion.

Lidoderm may be applied with your finger tips or a cotton swab. Follow your doctor's instructions.

Store Lidoderm at room temperature away from moisture and heat.

What happens if I miss a dose?
Since Lidoderm is used as needed, you may not be on a dosing schedule. If you are using the medication regularly, use the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and use the medicine at your next regularly scheduled time. Do not use extra medicine to make up the missed dose.

What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine. Lidoderm applied to the skin is not likely to cause an overdose unless you apply more than the recommended dose. Overdose may also occur if you apply heat, bandages, or plastic wrap to treated skin areas.

Improper use of Lidoderm may result in death.

Overdose symptoms may include drowsiness, confusion, nervousness, ringing in your ears, blurred vision, feeling hot or cold, numbness, muscle twitches, uneven heartbeats, seizure (convulsions), slowed breathing, or respiratory failure (breathing stops).

What should I avoid while using Lidoderm?
Do not allow Lidoderm to come into contact with your eyes. If it does, rinse with water.

Avoid using other topical medications on the affected area unless your doctor has told you to.

Lidoderm side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Lidoderm: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using Lidoderm and call your doctor at once if you have any of these serious side effects:
uneven heartbeats;
drowsiness, confusion;
tremors, seizure (convulsions); or
blurred vision.

Less serious Lidoderm side effects include:
mild irritation, redness, or swelling where the medication is applied;
numbness in places where the medicine is accidentally applied.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Lidoderm?
Before using Lidoderm, tell your doctor if you are taking medication to treat a heart rhythm disorder, such as:
quinidine (Quinidex, Quinaglute);
disopyramide (Norpace);
flecainide (Tambocor);
mexiletine (Mexitil);
procainamide (Procan, Pronestyl);
tocainide (Tonocard); or
propafenone (Rythmol).

This list is not complete and there may be other drugs that can interact with Lidoderm. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?
Your pharmacist has information about Lidoderm.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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