Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Sintetica Limited, 30<sup>th</sup> Floor, 40 Bank Street, Canary Wharf, London, E14 5NR, United Kingdom
Pharmacotherapeutic group: anaesthetics, local; esters of aminobenzoic acid
ATC code: N01BA04
Chloroprocaine, is an ester-type local anaesthetic. Chloroprocaine, blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential.
The onset of action for perineural administration is very rapid (6 to 12 min) and the duration of anaesthesia may be up to 100 minutes.
Patients with a successful block without any supplementation in the first 45 minutes after readiness for surgery are 90.8% with Chloroprocaine HCl.
The European Medicines Agency has deferred the obligation to submit the results of studies with Ampres in all subsets of the paediatric population in perineural anaesthesia (peripheral nerve block) (see section 4.2 for information on paediatric use).
The plasma concentration should be negligible for perineural use.
Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase. This process could be decelerated in case of pseudocholinesterase deficiency.
The hydrolysis of chloroprocaine results in the production of ß-diethylaminoethanol and 2-chloro-4-aminobenzoic acid.
The in vitro plasma half-life of chloroprocaine in adults is 21 ± 2 seconds for males and 25 ± 1 seconds for females. The in vitro plasma half-life in neonates is 43 ± 2 seconds. In women, plasma half-lives in vivo of 3.1 ± 1.6 minutes was measured.
The metabolites, ß-diethylaminoethanol and 2-chloro-4-aminobenzoic acid, are excreted by the kidney into the urine.
Concerning acute toxicity of 2-chloroprocaine following intravenous application see section 4.9.
Preclinical studies have been conducted in the case of spinal administration. Adverse effects in non-clinical studies, were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
No studies in animals to evaluate carcinogenic potential and reproductive and developmental toxicity have been conducted with chloroprocaine.
In vitro genotoxicity studies didn’t provide evidence for 2-chloroprocaine and 4-amino-2-chlorobenzoic acid (main metabolite) to have a relevant mutagenic or clastogenic potential.
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