利多卡因
Lidocaine
Lidocaine hydrochloride
別名: Xylocaine MPF · EMLA · Intubeaze · Lignadrin · Lignol · Locovetic · Lidoderm · lidocaini hydrochloridum · lignocaine hydrochloride · Lidocainum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
經審核的 v13 劑量證據
結構化劑量計算證據Regional anesthesia (extra-label) — CRI via peritoneal wound catheter
須由已驗證獸醫確認
NA
必須一併考量的臨床脈絡 (5)
- 1. Lidocaine formulation concentration, administration volume, site of administration, administration technique (eg, aspiration prior to injection), and underlying patient condition(s) are important interrelated factors that determine lidocaine’s safe and effective use.
- 2. All dosages below use 2% lidocaine (20 mg/mL) unless otherwise specified.
- Infiltration: dilute to 0.5% concentration (for each 1 mL of lidocaine 2% solution, dilute with 3 mL sterile water)
- Regional anesthesia (extra-label):
- Lidocaine should be stored at room temperature, at 15°C to 30°C (59°F-86°F).
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
利多卡因 (Lidocaine) 是一種多功能的醯胺類 (amide) 局部麻醉劑與 IB 類抗心律不整藥物。在獸醫學中，它不僅廣泛用於局部或區域麻醉，還常以全身性給藥的方式來控制心室心律不整、神經性疼痛以及胃腸道運動障礙。
主要臨床應用包括：
- 抗心律不整治療： 治療犬隻急性、危及生命的心室性心搏過速 (VT) 和心室性早搏 (VPCs) 的首選藥物。
- 全身性鎮痛： 常以恆速輸注 (CRI) 方式給藥，並經常與鴉片類藥物及氯胺酮 (Ketamine) 併用（例如 MLK CRI），以提供深度的輔助鎮痛、降低吸入性麻醉劑的最低肺泡濃度 (MAC)，並減輕神經性疼痛或痛覺過敏。
- 促腸胃蠕動與抗發炎作用： 在馬匹中，全身性利多卡因常被用於治療或預防術後腸阻塞 (ileus)，並能清除活性氧物質 (ROS)，從而減少再灌注損傷。
臨床要點： 貓對利多卡因的心臟抑制和中樞神經系統 (CNS) 毒性反應明顯更為敏感。其在貓科動物的全身性使用仍具爭議，必須極度謹慎並精確控制劑量。
作用機轉
Lidocaine exerts its effects through multiple mechanisms depending on the target tissue:
- Antiarrhythmic Action (Class IB): Lidocaine binds to and blocks fast voltage-gated sodium channels (Nav1.5) in the myocardium. It exhibits use-dependent and state-dependent blockade, meaning it preferentially binds to sodium channels in their inactive state (which occurs during depolarization). This action → attenuates phase 4 diastolic depolarization → decreases automaticity → suppresses ectopic ventricular pacemakers without significantly affecting the SA or AV nodes at therapeutic levels.
- Local Anesthetic/Analgesic Action: Blocks neuronal voltage-gated sodium channels, preventing the influx of sodium required for the initiation and conduction of action potentials in peripheral nerves. Systemically, it reduces ectopic firing from damaged afferent neurons, providing relief from neuropathic pain.
- Prokinetic & Cytoprotective Action: The exact mechanism for enhancing intestinal motility (especially in equine ileus) is multifactorial, likely involving suppression of sympathetic inhibitory reflexes, direct anti-inflammatory effects, and acting as a scavenger of reactive oxygen species (ROS) to prevent lipid peroxidation and reperfusion injury.
安全性與警告
禁忌症
- Known hypersensitivity to amide-class local anesthetics
- Severe SA, AV, or intraventricular heart block (unless artificially paced)
- Adams-Stokes syndrome
- Intravenous use of lidocaine products containing epinephrine
- Continuous rate infusion (CRI) in cats during the perioperative period (due to negative haemodynamic effects)
- Intravenous administration of lidocaine solutions containing adrenaline
- Use of adrenaline-containing solutions for complete ring block of an extremity (danger of ischaemic necrosis)
不良反應
- CNS toxicity (dose-related): drowsiness, depression, ataxia, nystagmus, muscle tremors, seizures
- Gastrointestinal: nausea and vomiting (usually transient)
- Cardiovascular: hypotension (especially with rapid IV bolus), bradycardia, PR and QRS interval prolongation, circulatory collapse at toxic doses
- Cats: heightened risk of severe cardiodepression and CNS signs
- Muscle fasciculations
- Laryngeal oedema (in cats, associated with CFC propellants in unlicensed aerosols)
注意事項
Use with extreme caution in cats due to heightened sensitivity to CNS and cardiodepressant effects. Use cautiously in patients with liver disease, congestive heart failure, shock, hypovolemia, severe respiratory depression, or marked hypoxia. Patients susceptible to malignant hyperthermia require intensified monitoring. NEVER administer lidocaine containing epinephrine intravenously.
藥物交互作用
Lidocaine infusions reduce MAC requirements. Additive cardiodepression may occur, especially in cats.
May cause additive or antagonistic cardiac effects; enhanced risk of toxicity.
May decrease lidocaine clearance, increasing lidocaine levels and effects.
Diuretic-induced hypokalemia may reduce the antiarrhythmic efficacy of lidocaine.
May induce hepatic enzymes, increasing lidocaine metabolism and decreasing its serum levels.
May decrease hepatic blood flow and lidocaine clearance, increasing lidocaine levels.
Large doses of lidocaine may prolong succinylcholine-induced apnea.
May cause increased myocardial depression
監測
- Continuous ECG monitoring (especially during IV bolus or CRI)
- Signs of CNS toxicity (ataxia, tremors, seizures)
- Blood pressure (monitor for hypotension)
- Serum lidocaine levels if available (Therapeutic range: 1-6 micrograms/mL)
- ECG (especially during IV therapy for arrhythmias)
- Heart rate
- CNS signs (monitor for fasciculations or seizures)
藥物動力學
半衰期
吸收
High first-pass effect makes it ineffective orally. Following a therapeutic IV bolus, onset of action is generally within 2 minutes with a duration of 10-20 minutes.
分佈
Rapidly redistributed from plasma into highly perfused organs (kidney, liver, lungs, heart), then widely throughout body tissues. High affinity for fat and adipose tissue. Bound to plasma proteins (primarily alpha1-acid glycoprotein). Vd is approximately 4.5 L/kg in dogs.
代謝
Rapidly metabolized in the liver to active metabolites (MEGX and GX).
排除
Less than 10% of a parenteral dose is excreted unchanged in the urine.
過量
In dogs, toxicity may result if serum levels exceed 8 micrograms/mL.
- Clinical Signs: Ataxia, nystagmus, depression, seizures, bradycardia, hypotension, and at very high levels, circulatory collapse.
- Management: Because lidocaine is rapidly metabolized, simply stopping the infusion or reducing the rate (with close monitoring) is often sufficient for minor signs.
- Seizure Control: Treat seizures or excitement with diazepam or a short/ultrashort-acting barbiturate. > Warning: Longer-acting barbiturates (e.g., pentobarbital) should be avoided.
- Cardiovascular Support: Treat circulatory depression with IV fluids, pressor agents, and initiate CPR if necessary.
可用產品
劑型
- Injection: 0.5%, 1%, 1.5%, 2%, 4% solutions
- Premixed IV infusion solutions (with D5W)
- Topical: patches, ointments, creams, lotions, gels, sprays, and jellies
- Injectable: 1% solution
- Injectable: 2% solution (some contain adrenaline)
- Topical: 2% solution
- Topical: 4% solution
- Topical: 2.5% cream (with prilocaine)
- Transdermal: 5% patches
獸醫用
- Lidocaine HCl for Injection: 2% (20 mg/mL) in 100 mL & 250 mL multi-use vials
- Intubeaze 2% topical solution
- Lignadrin injectable
- Lignol injectable
- Locaine injectable
- Locovetic injectable
人用標示
- Lidocaine Hydrochloride Injection: 0.5%, 1%, 1.5%, 2% & 4% in various vials, ampules, and syringes
- Lidocaine Hydrochloride with Dextrose Injection: 1.5% or 5% with 7.5% dextrose
- Premixed IV infusions in D5W (2 mg/mL, 4 mg/mL, 5 mg/mL)
- Topical liquids, patches, ointments, creams, lotions, gels, sprays, and jellies
- EMLA 2.5% cream (with prilocaine)
- Xylocaine 4% topical solution
- Lidoderm 5% transdermal patch
各地核准狀態
POM-V classification
POM-V classification
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at temperatures less than 40°C, preferably between 15-30°C. Avoid freezing.
飼主須知
利多卡因是一種強效藥物，通常僅在獸醫院內由專業的獸醫人員使用。
- 用途： 主要用於矯正危及生命的心律不整，或在重大手術及創傷後提供持續的疼痛控制（通常與其他止痛藥物混合使用）。
- 監測： 由於此藥物是直接透過靜脈注射進入血液，您的寵物將會接受密切的監測（通常包括心電圖和血壓測量），以確保劑量安全且有效。
- 副作用： 如果出現副作用，通常較為輕微，且在調整藥物輸注速率後會迅速消退。如果您的寵物處於清醒狀態，請留意是否有嗜睡、肌肉顫抖或噁心等跡象。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。