SUXAMETHONIUM AND SERUM CHOLINESTERASE Comparative Studies in vitro and in vivo on the Catabolism of Suxamethonium

Abstract

From in-vitro and in-vivo studies and from earlier publications the following conclusions may be drawn concerning the pharmacology of suxamethonium. The serum cholinesterase plays a decisive role in the splitting of suxamethonium. With a purified concentrated enzyme preparation (3000 Au) cleavage was proved in vitro. In the case of genetic enzyme variants hydrolysis is diminished. Cbolinesterase-free serum is unable to split suxamethonium. Spontaneous hydrolysis may be neglected; it may play some role in the rare case of anenzymia. In vivo the serum cholinesterase is most inhibited in the third minute after the administration of suxamethonium. Spontaneous respiration recurs as soon as the activity of the serum cholinesterase has returned to its initial value. In the case of extremely low cholinesterase activity the hydrolysis of suxamethonium after a single dose of 50-70 mg is prolonged by a few minutes. A. DOENICKE; ST. SCHMIDINGER; I. KRUMEY (with the support of the Deutsche Forschungsgemeinschaft; dedicated to Professor Dr. Eugen Werle on his 65th birthday): from the Department of Anaesthesia,

Whole blood transfusion in the treatment of an acute organophosphorus poisoning – a case report

“…Doenicke et al discussed the possibility of plasma use after suxamethonium application [10] in patients with prolonged muscular block caused by BChE congenital insufficiency, and suggested full blood transfusion as a possible alternative for exogenous enzymes substitution. Another possible benefit of whole blood transfusion could be delivering a certain amount of erythrocyte cholinesterase – a potential target substrate for OP.…”

Serumcholinesterase als Modell eines Glykoproteins

“…Ihr Gehalt im Humanserum beträgt knapp 10 mg/1. Von klinischer Bedeutung ist der genetisch bedingte Pölymorphismus der Serumcholinesterase irn Zusammenhang mit ihrer Fähigkeit, das in der Anästhesie verwendete Muskelrelaxäns Succinylbischoluichlorid (Siixamethoniurnchlorid) abzubauen (4,5,6 3. Beide Rezeptoren konnten gaschromatographisch identifiziert werden, da sie als alkali-labile Kohlenhydratketten vorkommen.…”

In Vitro Interaction of Propanidid and Suxamethonium With Pooled Human Plasma Cholinesterase

“…There is evidence (Doenicke et al, 1968;Ellis, 1968;Kraunak, Pleuvry and Rees, 1977) which points to the involvement of a cholinesterase enzyme in the metabolism of the short-acting anaesthetic agent propanidid (propyl-4-NN-diethylcarbamoyknethoxy-3-methoxyphenylacetate). In human plasma the enzyme most likely to be involved in the hydrolysis of both propanidid and suxamethonium is pseudocholinesterase (E.C.…”

“…In human plasma the enzyme most likely to be involved in the hydrolysis of both propanidid and suxamethonium is pseudocholinesterase (E.C. 3.1.1.8) (Doenicke, Schmidinger and Krumey, 1968).…”