Masui. The Japanese journal of anesthesiology
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For many years, much effort has been done to develop non-depolarizing neuromuscular blocking agents of rapid onset and short duration. It has been shown that rocuronium bromide is a nondepolarizing, steroidal muscle relaxant with fast onset and short-to-intermediate duration of action. In addition, rocuronium-induced neuromuscular blockade can be readily and consistently reversed following the administration of reversal agents. The pharmacology and pharmacodynamics of rocuronium bromide are summarized in this review.
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Review
[New ultra-short-acting beta-blockers: landiolol and esmolol--the effects on cardiovascular system].
Esmolol and landiolol are ultra-short-acting intravenous beta-blockers. Both drugs have high cardioselectivity (beta1/beta2 selectivity of esmolol : 33, landiolol: 255) and short elimination half time (esmolol : 9 min, landiolol : 4 min). Since the duration of beta-adrenergic blockade is short and cardioselectivity is high compared with traditional intravenous beta-blocker propranolol, both drugs are titrated easily. ⋯ There are not many clinical trials on landiolol. However, since landiolol has higher cardioselectivity and tends to have less cardiodepressant effect than esmolol, clinical indication of landiolol may be extended. Additional data from large studies are required to evaluate the clinical efficacy and safety of landiolol for a variety of diseases.
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Dexmedetomidine, a potent and highly selective alpha2-agonist, provides a unique "conscious sedation" (patients appear to be asleep, but are readily roused), analgesia, without respiratory depression. In order to provide a comfortable sedation to the ICU patients, careful evaluation of sedation and analgesia level, and the consistent treatment by medical teams are necessary. ⋯ The major problem with dexmedetomidine is its hemodynamic effects. Because this drug often causes hypotension, hypertension and bradycardia, it should be used under the control by skilled medical teams.
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Sugammadex, a chemically modified gamma-cyclodextrin, was synthesized as a selective reversal agent for rocuronium, a steroidal neuromuscular blocking agent. The lipophilic cavity of sugammadex molecule encapsulates the lipophilic steroid rings of rocuronium and forms 1:1 host-guest complex. Additionally, negatively charged carboxyl groups around the rim of cyclic sugammadex easily attract a positively charged quaternary nitrogen of rocuronium. ⋯ Therefore, undesired side effects attendant with anticholinesterases are not seen. No recurarization was also observed. The majority of the complexes is excreted via the kidney, but the reversal effects are complete even in patients with renal failure.
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Besides its cardioinhibitory effects, short-acting beta1-adrenergic receptor antagonists, landiolol and esmolol are reported to exert antinociceptive and anesthetic sparing effects in animal and human subjects. For example, esmolol reduces the anesthetic requirements for skin incision during propofol/N2O and morphine anesthesia in human and inhibits nociceptive responses following formalin injection in rats. It is also suggested that landiolol decreases BIS response to tracheal intubation during sevoflurane anesthesia. ⋯ The merits to use short-acting beta1-adrenergic receptor antagonists as anesthetic adjuvants could be to reduce anesthetic and opioid requirements (thus, to avoid its side effects such as nausea and vomiting), to maintain hemodynamic stability, and to achieve early recovery from anesthesia. Administration of a sufficient dose of a short-acting beta1-adrenergic receptor antagonist, for example by neuraxial route, may potentially be a new treatment strategy for the perioperative pain, although further study is necessary to establish its efficacy and toxicity. Short-acting beta1-adrenergic receptor antagonists will be used as agents for antinociception in future.