The influence of bambuterol (carbamylated terbutaline) on the duration of action of succinylcholine-induced paralysis in humans

Abstract

Bambuterol (bis-dimethylcarbamyalated terbutaline) is being investigated as an orally administered prolonged-acting treatment for bronchospasm. Adding two carbamate groups to terbutaline results in bambuterol, an inert prodrug compound that is broken enzymatically to yield the active compound, terbutaline. Because bambuterol is slowly bioconverted, has a high affinity for lung tissue, and is bioconverted in the lung, it can be administered once daily for the treatment of asthma. However, as the carbamate groups are cleaved from bambuterol, they selectively inhibit the activity of pseudocholinesterase, the enzyme responsible for the degradation of succinylcholine. Therefore, we determined the interaction of bambuterol-induced decreases in pseudocholinesterase activity and succinylcholine-induced neuromuscular blockade.