Drugs to facilitate recovery of neuromuscular blockade and muscle strength

Saitoh, Yuhji

doi:10.1007/s00540-005-0336-y

Cited by 5 publications

(7 citation statements)

References 42 publications

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“…Nicorandil enhances membrane K+ conductance in skeletal muscle and increases contraction of the skeletal muscle and quickens recovery from neuromuscular blockade. [3]…”

Section: Discussionmentioning

confidence: 99%

“…[8] in their study found that infusion of amino acids @ 100ml/ hour speeds the recovery from vecuronium induced neuromuscular blockade in anaesthetized patients. This could be probably explained by the fact that amino-acid–enriched solutions supply energy to the skeletal muscles, causing an increase in muscle strength and hastening recovery from neuromuscular blockade by generating heat in the skeletal muscles and thus improving the hypothermia during general anaesthesia,[3]…”

Section: Discussionmentioning

confidence: 99%

“…[1] Our case report suggests that that the infusion of amino acid solution hastened the recovery from residual neuromuscular blockade. [23] Previous studies have reported that intravenous amino acid infusions exert enhanced thermogenic effects during general anaesthesia. [2]…”

Section: Introductionmentioning

confidence: 99%

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Role of amino acid infusion in delayed recovery from neuromuscular blockers

Kalra¹,

Wadhwa²

2010

Indian J Anaesth

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This case report highlights the anaesthetic management of a patient who had residual muscle paralysis following neuromuscular blockade, which was attributed to hypothermia and corrected by administration of amino acid solution. The various causes of residual neuromuscular blockade should be considered when treating such a patient. Amino acid infusion has been found to hasten the recovery from neuromuscular block due to vecuronium bromide aggravated by hypothermia.

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“…Nicorandil enhances membrane K+ conductance in skeletal muscle and increases contraction of the skeletal muscle and quickens recovery from neuromuscular blockade. [3]…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Role of amino acid infusion in delayed recovery from neuromuscular blockers

Kalra¹,

Wadhwa²

2010

Indian J Anaesth

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“…Modulators of the K ATP channels are promising in those conditions associated with impaired skeletal muscle functionality. Openers restore muscle contraction in humans affected by periodic paralysis, myotonia, and in neuromuscular disorders associated with impaired fiber excitability and contraction; deficiency of skeletal muscle K ATP channels is associated with reduced muscle contractility in the rat (Saitoh, 2005;Cifelli et al, 2007). Blockers targeting the Kir6.2 subunit may be effective in the insulin-resistant state and diabetes type II with neuromuscular symptoms associated with abnormal openings of the skeletal muscle, neuronal, and pancreatic K ATP channels (Koster et al, 2005;Flechtner et al, 2006).…”

Section: Potassium Channel Modulators and Skeletal Muscle 57mentioning

confidence: 99%

“…contractility function in humans after neuromuscular blocker-induced paralysis (Saitoh, 2005). Pinacidil is capable of reducing the severity and frequency of paralysis in patients affected by hypokalemic periodic paralyses (hypoPP); however, the patients suffer severe hypotension, which limits its use in this muscle disorder (Links et al, 1992).…”

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confidence: 99%

Molecular Determinants for the Activating/Blocking Actions of the 2H-1,4-Benzoxazine Derivatives, a Class of Potassium Channel Modulators Targeting the Skeletal Muscle K_ATP Channels

Tricarico

Mele²,

Camerino³

et al. 2008

Mol Pharmacol

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The 2H-1,4-benzoxazine derivatives are modulators of the skeletal muscle ATP-sensitive-K ϩ channels (K ATP ), activating it in the presence of ATP but inhibiting it in the absence of nucleotide. To investigate the molecular determinants for the activating/blocking actions of these compounds, novel molecules with different alkyl or aryl-alkyl substitutes at position 2 of the 1,4-benzoxazine ring were prepared. The effects of the lengthening of the alkyl chain and of branched substitutes, as well as of the introduction of aliphatic/aromatic rings on the activity of the molecules, were investigated on the skeletal muscle K ATP channels of the rat, in excised-patch experiments, in the presence or absence of internal ATP (10 Ϫ4 M). In the presence of ATP, the 2-n-hexyl analog was the most potent activator (DE 50 ϭ 1.08 ϫ 10 Ϫ10 M), whereas the 2-phenylethyl was not effective. The rank order of efficacy of the openers was 2-n-hexyl Ն2-cyclohexylmethyl Ͼ2-isopropyl ϭ 2-n-butyl Ն 2-phenyl Ն 2-benzyl ϭ 2-isobutyl analogs. In the absence of ATP, the 2-phenyl analog was the most potent inhibitor (IC 50 ϭ 2.5 ϫ 10 Ϫ11 M); the rank order of efficacy of the blockers was 2-phenyl Ն 2-n-hexyl Ͼ 2-n-butyl Ͼ 2-cyclohexylmethyl, whereas the 2-phenylethyl, 2-benzyl, and 2-isobutyl 1,4-benzoxazine analogs were not effective; the 2-isopropyl analog activated the K ATP channel even in the absence of nucleotide. Therefore, distinct molecular determinants for the activating or blocking actions for these compounds can be found. For example, the replacement of the linear with the branched alkyl substitutes at the position 2 of the 1,4-benzoxazine nucleus determines the molecular switch from blockers to openers. These compounds were 100-fold more potent and effective as openers than other KCO against the muscle K ATP channels.Potassium channel openers (KCO) are chemically diverse compounds that belong to a number of structural classes, including benzopyrans (cromakalim, bimakalim), benzothiadiazines (diazoxide), cyanoguanidines (pinacidil), cyclobutenediones (WAY-151616), nicotinamides (nicorandil), pyrimidines (minoxidil), tertiary carbinoles (ZD-6169), thioformamides (aprikalim), and dihydropyridine-like structures (ZM-244085) (Mannhold, 2004;Jahangir and Terzic, 2005). Several derivatives of these compounds have been synthesized and tested against the ATP sensitive K ϩ -channel (K ATP ) subunits expressed in cell lines, which is the primary target for KCO action.These compounds show a broad spectrum of therapeutic applications, including asthma, urinary incontinence, hypertension, angina, hypoglycemia, neuromuscular disorders, and some forms of epilepsy (Andersson, 1992;Longman and Hamilton, 1992). KCO drugs exert their effects on pancreatic ␤ cells, neurons, and vascular/nonvascular smooth muscle and cardiac muscle by opening K ATP channels, thus shifting the membrane potential toward the reversal potential for potassium and reducing cellular electrical activity. In skeletal muscle, nicorandil is effective in restoring the depr...

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Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

Kim

Sung

Yang

2017

Korean J Anesthesiol

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Neuromuscular blockade plays an important role in the safe management of patient airways, surgical field improvement, and respiratory care. Rapid-sequence induction of anesthesia is indispensable to emergency surgery and obstetric anesthesia, and its purpose is to obtain a stable airway, adequate depth of anesthesia, and appropriate respiration within a short period of time without causing irritation or damage to the patient. There has been a continued search for new neuromuscular blocking drugs (NMBDs) with a rapid onset of action. Factors that affect the onset time include the potency of the NMBDs, the rate of NMBDs reaching the effect site, the onset time by dose control, metabolism and elimination of NMBDs, buffered diffusion to the effect site, nicotinic acetylcholine receptor subunit affinity, drugs that affect acetylcholine (ACh) production and release at the neuromuscular junction, drugs that inhibit plasma cholinesterase, presynaptic receptors responsible for ACh release at the neuromuscular junction, anesthetics or drugs that affect muscle contractility, site and methods for monitoring neuromuscular function, individual variability, and coexisting disease. NMBDs with rapid onset without major adverse events are expected in the next few years, and the development of lower potency NMBDs will continue. Anesthesiologists should be aware of the use of NMBDs in the management of anesthesia. The choice of NMBD and determination of the appropriate dosage to modulate neuromuscular blockade characteristics such as onset time and duration of neuromuscular blockade should be considered along with factors that affect the effects of the NMBDs. In this review, we discuss the factors that affect the onset time of NMBDs.

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Drugs to facilitate recovery of neuromuscular blockade and muscle strength

Cited by 5 publications

References 42 publications

Role of amino acid infusion in delayed recovery from neuromuscular blockers

Role of amino acid infusion in delayed recovery from neuromuscular blockers

Molecular Determinants for the Activating/Blocking Actions of the 2H-1,4-Benzoxazine Derivatives, a Class of Potassium Channel Modulators Targeting the Skeletal Muscle K_ATP Channels

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

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Drugs to facilitate recovery of neuromuscular blockade and muscle strength

Cited by 5 publications

References 42 publications

Role of amino acid infusion in delayed recovery from neuromuscular blockers

Role of amino acid infusion in delayed recovery from neuromuscular blockers

Molecular Determinants for the Activating/Blocking Actions of the 2H-1,4-Benzoxazine Derivatives, a Class of Potassium Channel Modulators Targeting the Skeletal Muscle KATP Channels

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

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Molecular Determinants for the Activating/Blocking Actions of the 2H-1,4-Benzoxazine Derivatives, a Class of Potassium Channel Modulators Targeting the Skeletal Muscle K_ATP Channels