"Neuromuscular blocking agents for fast-tracking anaesthesia"

Hermann Mellinghoff, MD

Department of Anaesthesiology, University Hospital, D-50924 KOELN, Germany

 

The choice of anaesthetics with a rapid and predictable recovery is essential for a rapid turnover of patients in the operating theatre. "Fast-tracking“ after surgery is an attempt to decrease the time from the end of surgery to the extubation of the trachea. A muscle relaxant well suited for "fast-tracking" should produce a rapid onset and a short duration of action and its offset period should allow equally rapid recovery from neuromuscular block.

The onset of action of neuromuscular block

Decreased neuromuscular blocking potency as well as a rapid clearance seem to be responsi­ble for a more rapid onset of action of muscle relaxants. Onset after the injection of muscle relaxants decreases with increasing molar potency. Consistent with these findings, rapacu­ro­nium (ED95 of 1.0 mg/kg active moiety) has a more rapid onset of action than any of the other nondepolarizing muscle relaxants and, when injected in doses of 1.5-2.5mg/kg, ap­pears to have an onset of action compatible with that of succinylcholine. Muscle relaxants are injected during induction of anaesthesia to facilitate tracheal intubation. A rapid onset of ac­tion has become expected at least in part due to the rapid onset of neuromuscular block of succinylcholine. However, is well accepted, that the time from injection of a muscle relaxant to its maximum effect is in the order of less than one minute (succinylcholine) to up to three minutes (cisatracurium). This implies that, even when the choice of the muscle relaxant for "fast-tracking" is based on a rapid onset of action, the time saved is minimal. Furthermore, it was shown, that onset of neuromuscular block produced by muscle relaxants is faster at the laryngeal muscles than at the adductor pollicis muscles, and that therefore the clinician is not forced to wait for complete abolition of the peripheral twitch response.

The duration of action of muscle relaxants

With muscle relaxants of ultra-short (succinylcholine), short (mivacurium), intermediate (atracurium, vecuronium, cisatracurium and rocuronium) and long duration of action (pan­curonium) the anaesthesiologist has a wide array of drugs at his disposal. It is obvious, that the choice of a muscle relaxant depends on the estimated duration of the surgical procedure. Preference should be given to muscle relaxants with a short or intermediate duration of action because they can easily be adapted to a varying duration of surgery.

The recovery from neuromuscular block

Recovery from neuromuscular block is assumed to be complete when any effect of a muscle relaxant has disappeared. As more than 70% of the acetylcholine re­ceptors may be occupied by muscle relaxants before any reduction of the twitch response to nerve stimulation is detectable, these drugs may not have disappeared from the organism even when no effect of the twitch response to nerve stimulation can be measured. For a long time, a train-of-four (TOF) fade ratio of >0.70 following nerve stimulation has been regarded as a reliable indicator of acceptable clinical recovery. Once that ratio was greater than 0.70, muscle strength was assumed to have returned to a near-normal state, as indicated by sensitive clinical tests, such as head-lift. In 1997, Kopman presented re­sults that indicated that a TOF-ratio of 0.70 can no longer be regarded as an indicator for adequate neuromuscular function. He reports, that even at TOF-ratios of 0.90 after mivacurium, visual disturbances were present in all subjects. Diplopia and inability to follow moving ob­jects even persisted when the TOF-ratio had fully recovered. Also, when the TOF-ratio was <0.75, "all subjects were uncomfortable".

 

Reversal of neuromuscular block

The use of long-acting muscle relaxants like pancuronium has been shown to be associated with a prolonged postoperative recovery. Even after the administration of mivacurium, a high incidence of residual block was demonstrated in one study when the neuromuscular block had not been antagonized at the end of surgery. Consequently, even after short-acting muscle relaxants spontaneous recovery can be slow enough to make residual block visible in the recovery room. Accordingly, pharmacologic reversal of neuromuscular block should be based on the findings of neuromuscular monitoring and considered whenever necessary, possibly even after the use of a short-acting relaxant. On the other hand the choice of a short- or intermediate-acting muscle relaxant for fast-tracking anaesthesia concepts is underlined by those findings.

Suitable non-depolarizing muscle relaxants

In the context of fast-tracking anaesthesia, the administration of long-acting muscle relaxants is not appropriate. Therefore, only intermediate and short-acting muscle relaxants will be presented. These drugs can be classified into two chemical groups: aminosteroidal muscle relaxants (rocuronium, rapacuronium) and those of the benzylisoquinolinium type (mivacurium, cisatracurium). Rocuronium (ED95 0.30 mg/kg) has a time course of action similar to that of vecuronium, with the exception that its onset of action is faster. After 1.5mg/kg rapacuronium, the onset of action is almost as rapid as that of succinylcholine, although with a greater variation. The duration of action of 1.5mg/kg rapacuronium has been reported to be 14 min. In another study, spontaneous recovery after repeat doses of rapacuro­nium was 70 minutes. Its 3-desacetyl metabolite (Org9488) has neuromuscular blocking activity and a clearance lower than the parent compound and thus gradually prolongs the recovery from neuromuscular block after increasing doses of rapacuronium. Mivacurium is a  short-acting non-depolarizing muscle relaxant (ED95 0.08 mg/kg). The rapid hydrolysis by plasma cholinesterase is responsible for its short duration of action. A study on the time course characteristics of neuromuscular block of up to 10 consecutive repeat doses of mivacurium confirmed the recovery after mivacurium to be rapid and predictable. Cisatracurium (ED95 0.05 mg/kg) is the cis-cis isomer of atracurium. Following intubation doses, onset of action is attained at ca 3 min. The recovery profile of cisatracurium is independent of the administered dose or organ dysfunction. Cisatracurium does not induce dose-dependent histamine release and even after 8*ED95 displays a haemodynamically stable profile.

CONCLUSION

The different pharmacology of the two groups of muscle relaxants is reflected in different pharmacodynamic profiles: the aminosteroidal muscle relaxants rocuronium and rapacuronium have a low potency providing a fast onset of action. The benzylisoquinolinium muscle relaxants mivacurium and cisatracurium are rapidly metabolized into inactive compounds providing reliable and fast recovery characteristics, even after repeated bolus dose administration or continuous infusion.

Recent studies suggest the importance of an almost complete recovery of neuromuscular transmission to achieve full neuromuscular function after the administration of muscle relaxants. This is particularly important when muscle relaxants are used in the context of new fast-tracking anaesthesia concepts. Discharge of patients from the recovery area is only possible when no effect of a muscle relaxants impairs any muscle function of the patient. These rules almost exclude the use of a long-acting muscle relaxant for fast-tracking anaesthesia, and even influences the choice among the intermediate- and short-acting muscle relaxants. In general, the anaesthesiologist should know in detail the pharmacologic properties of a chosen muscle relaxant, and restrict this choice to the muscle relaxant with a sufficiently short duration of action and a rapid and predictable recovery profile for fast-tracking anaesthesia.