Lhdj. Booij, NEUROMUSCULAR-TRANSMISSION AND ITS PHARMACOLOGICAL BLOCKADE .2. PHARMACOLOGY OF NEUROMUSCULAR BLOCKING-AGENTS, Pharmacy world & science, 19(1), 1997, pp. 13-34
Clinically, neuromuscular blockade is induced with either depolarizing
or non-depolarizing relaxants. Suxamethonium is the only depolarizing
relaxant still in use. It is hydrolysed in Is the plasma by pseudo-ch
olinesterase (plasma cholinesterase). In some patients and in particul
ar diseases the plasma cholinesterase activity is low and hence the ef
fect of suxamethonium prolonged. Suxamethonium is characterized by sid
e-effects such as myalgia, fasciculations and in intraocular, intracra
nial and intragastric pressure; More serious adverse reactions are mas
seter muscle spasm and potassium release, in patients with some neurom
uscular diseases and increase in extrajunctional acetylcholine recepto
rs. As non-depolarizing muscle relaxants benzylisoquinolines and stero
idal compounds are mainly used. Each relaxant has its own pharmacologi
cal characteristics. The effect of most relaxants depends on liver and
renal function because the pharmacokinetic behaviour is strongly depe
ndent on these organs. Also, acid-base balance disturbances, change in
temperature, and neurological diseases have an effect on the profile
of the relaxants. A number of drugs (anaesthetics, antibiotics, antiep
ileptics, etc.) have an effect on neuromuscular transmission, and thus
interact with the relaxants. Some non-depolarizing relaxants cause hi
stamine release and cardiovascular effects.