Muscle relaxants

Dr Sonaike

Introduction

These are drugs that interrupt transmission of neural impulses

at the Neuro-Muscular Junction {NMJ} skeletal muscle. Also
referred to as NMB.
Classification: Depolarizing {suxamethonium, decamethonium}
and non depolarizing {pancuronium, atracurium, dtubocurare, gallamine etc}.
Based on duration of action; ultra-short {suxamethonium}, short
{mivacurium}, intermediate {atracurium, vecuronium,
rocuronium}, long acting {pancuronium, pipecuronium,
doxacurium, gallamine}.
Based on chemical structure; benzyl- isoquinolium {atracurium,
mivacurium}, aminosteroids {pancuronium, vecuronium,
rocuronium}.

Suxamethonium

A depolarizing muscle relaxant, also known as succinylcholine.

Presented as suxamethonium chloride, clear solutions of
50mg/ml in 2/10ml glass bottle. It is water soluble.
Dose is 1-1.5mg/kg for tracheal intubation.
Onset of action is 60 90 secs
Duration is 3 mins, total recovery time is 12-15 mins.
Mechanism of action- initial depolarization and muscle
contraction {fasciculation} then flaccid {relaxation}.
Repolarization does not occur.
Reversal of NMB is by plasma cholinesterase enzyme formerly
called pseudo cholinesterase. Neostigmine is contra-indicated.

Suxamethonium contd.

Uses:
Rapid sequence induction in cases of full-stomachemergency/likely unfasted, obstetrics, intraabdominal masses, diabetic neuropathy.
Anticipated difficult intubation- obese,
mandibular/facial injuries, retropharyngeal abscess.
Side-effects; muscle pains {prevented by precurarisation}, increased IOP, increased intra-gastric
pressure {avoid in cases of hiatus hernia},
hyperkalaemia, sinus bradycardia, anaphylactic
reactions {rare though}.

Pancuronium

A non-depolarizing muscle relaxant, presented as pancuronium

bromide as 2mg/ml.
Dose 0.1mg/kg
Onset of action 3 4 mins
Duration of action, long up to 1 hour. Potentiated by potent inhalational
agents, renal dysfunction. Produces metabolites that are active hence
best avoided in patients with liver disease.
A benzyl- isoquinolium, thought to be competitive with Ach at nicotinic
ends of the NMJ. Panc does not stimulate histamine release {safe in
asthmatics}. It has direct sympathomimetic and vagolytic effects thus
will cause tachycardia and hypertension.
It inhibits plasma cholinesterase hence will prolong effect of drugs that
needs this enzyme for metabolism.

Atracurium

Introduced into clinical practice in 1982.

A non depolarizing muscle relaxant, presented as
atracurium besylate. Dose is 0.5mg/kg
Onset of action- 2-2.5mins
Duration of action- 20-25min, brisk recovery.
Causes release of histamine, but does not have direct
cardiovascular effect.
Undergoes Hofmann degradation to produce
laudanosine{a metabolite that has epileptogenic
properties}

Anticholinesterase

Agents used in clinical practice to inhibit the action of

acetylcholinesterase at the NMJ thus prolong the
action of Ach thus reverses the residual effects of nondepolarizing NMB.
Most commonly used are- neostigmine, but
edrophonium and pyridostigmine are available.
Neostigmine, combines reversibly with
acetylcholinesterase with effects lasting about 30 mins.
Dose 0.04-0.06mg/kg and used in combination with
anticholinergics {bradycardia, salivation, sweating,
bronchospasm, increased intestinal motility and blurred
vision}

Neuromuscular monitoring

No clinical tool is available but crude estimate of muscle

contraction is used, using current up to 50mA for a fraction of
ms. Readily accessible nerves such as ulnar, facial, lateral
popliteal nerve. The muscular contraction is assessed by
visual or tactile means- mechanomyography,
electromyography.
Modes of stimulation- twitch, ToF, TS, PTF,DBS.
Indications; prolonged anaesthesia, when infusions of NMB has
been used ,renal/hepatic dysfunction, previous history of
prolonged effects, neuromuscular disorders, unexpected poor
recovery.