羅庫溴銨
羅庫溴銨（Rocuronium bromide）是一種氨基類固醇類、競爭性、**非去極化神經肌肉阻斷劑（NMBA）**。它主要作為全身麻醉的輔助藥物，以促進快速氣管插管，並在精細的手術過程中（如眼科、神經外科或胸腔外科手術）提供深度的骨骼肌鬆弛。 主要藥理特徵包括： * **起效快速至中等**：與維庫溴銨（vecuronium）或阿曲庫銨（atracurium）相比，起效更快（比維庫溴銨快2-3倍），幾乎與琥珀膽鹼（succinylcholine）一樣快，但不良反應較少。 * **中等作用時間**：作用時間與維庫溴銨和阿曲庫銨相似。 * **心血管穩定性**：與較舊的神經肌肉阻斷劑相比，對心血管和組織胺釋放的影響極小。 > **臨床要點：** 像羅庫溴銨這類神經肌肉阻斷劑**完全沒有鎮痛、鎮靜或失憶的作用**。若給予清醒或麻醉深度不足的病患，將導致病患在完全清醒且能感受到疼痛的情況下全身癱瘓，這是一種極度恐懼的體驗。因此，它**只能**用於已深度麻醉且能立即提供機械式呼吸輔助的病患。
作用機制: Rocuronium acts by competitively antagonizing acetylcholine (ACh) at the neuromuscular junction. * **Mechanism**: It binds to **nicotinic cholinergic receptors** at the motor end plate of skeletal muscle. * **Pathway**: Rocuronium occupies the receptor site → prevents ACh from binding → inhibits depolarization of the muscle cell membrane → results in flaccid paralysis. * **Reversal**: Because the blockade is competitive, it can be antagonized by increasing the concentration of ACh in the synaptic cleft. This is achieved using **acetylcholinesterase inhibitors** (e.g., neostigmine, edrophonium). Alternatively, rocuronium can be directly encapsulated and inactivated in the plasma by the selective relaxant binding agent **sugammadex**.
各物種劑量
- As a neuromuscular blocker · 0.6 mg/kg IV · IV · Single dose · Rapid onset, short duration of action, and does not cause significant changes in heart rate.
- Neuromuscular blockade / Endotracheal intubation · 0.3-0.6 mg/kg i.v. · IV · Single dose · Approx 20 min at 0.6 mg/kg · 0.6 mg/kg has a rapid onset and short duration of action (20 min). Requires prompt successful intubation and ventilation.
- As a neuromuscular blocker · 0.6 mg/kg IV · IV · Single dose · Provided predictable blockade without hemodynamic changes, but large variation between individuals; monitoring of neuromuscular block is essential.
- As a neuromuscular blocker · 0.5 mg/kg bolus and then a CRI was started immediately at 0.2 mg/kg/hour · IV · Bolus followed by CRI · Authors concluded it was effective and easily applicable, but further work is required on infusion titration.
- Neuromuscular blockade during anaesthesia · 0.4 mg/kg i.v. followed, when required, by a maintenance dose of 0.16 mg/kg i.v. prn or continuous rate infusion of 0.2 mg/kg/h · IV · prn or CRI · As needed during surgery · Monitoring with a nerve stimulator is recommended.
- Centralize the globe for ophthalmic surgery · 0.05-0.1 mg/kg i.v. · IV · Single dose or prn · As needed · Considerably lower doses are required for this indication.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
禁忌症
- Hypersensitivity to rocuronium or other neuromuscular blocking agents
- Patients who are not adequately anesthetized or sedated
- Settings lacking immediate access to intubation, mechanical ventilation, and oxygen therapy
- Conscious or inadequately anaesthetized animals
- Lack of positive pressure ventilation facilities
不良反應
- Changes in heart rate (mild, transient tachycardia)
- Changes in blood pressure (hypotension or hypertension)
- Severe anaphylaxis (reported in humans)
- Histaminoid reactions (rare)
- Severe burning pain at the injection site (if administered before deep anesthesia is achieved)
- Increased heart rate
- Mild hypertension (at high doses)
藥物相互作用
- Other Non-depolarizing Muscle Relaxants · May have a synergistic effect if used concurrently with rocuronium.
- Succinylcholine · May speed the onset of action and enhance the neuromuscular blocking actions of rocuronium; do not give rocuronium until succinylcholine effects have subsided.
- Aminoglycosides (e.g., gentamicin, amikacin) · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Inhalant Anesthetics (halothane, isoflurane, sevoflurane) · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Clindamycin, Lincomycin · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Dantrolene · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Magnesium Salts · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Piperacillin, Mezlocillin · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Quinidine · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Tetracyclines · May enhance or prolong the neuromuscular blocking activity of rocuronium.
- Verapamil · May enhance or prolong the neuromuscular blocking activity of rocuronium.
監測
- Degree of neuromuscular blockade (using a peripheral nerve stimulator/Train-of-Four monitor)
- Heart rate and rhythm
- Blood pressure
- Oxygenation (SpO2) and ventilation (End-tidal CO2)
- Depth of anesthesia
- Neuromuscular blockade depth (using a peripheral nerve stimulator)
- Heart rate and blood pressure
- Spontaneous respiratory effort during recovery
過量
Overdosage with neuromuscular blocking agents results in **prolonged neuromuscular blockade** (extended paralysis). * **Primary Treatment**: Maintenance of a patent airway, continuous mechanical ventilation, oxygenation, and adequate sedation/anesthesia until full recovery of muscle function is assured. * **Reversal**: Only after spontaneous evidence of recovery is observed should administration of an anticholinesterase drug (e.g., neostigmine) combined with an anticholinergic agent (e.g., atropine or glycopyrrolate to prevent severe bradycardia) be considered. * **Specific Antidote**: Rocuronium's effects can be rapidly and specifically reversed by **sugammadex**, a cyclodextrin binding agent that encapsulates the drug in the plasma.
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