Excretion of Neostigmine labelled with Carbon-14 in Urine

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ALTHOUGH neostigmine (prostigmin) has been used for about thirty years for the treatment of myasthenia gravis, and later for the post-operative reversal of tubocurarine, relatively little seems to be known about the mechanisms involved in its metabolism and excretion. The inhibition of plasma cholinesterase has been used as a convenient indicator of neostigmine concentration, and it has been shown that after administration to dogs and to patients with myasthenia gravis, elimination of neostigmine depends on the dose and method of administration1. Some of these conclusions have been confirmed in more recent work where a colorimetric method was used for the measurement of neostigmine in urine2. Thus when neostigmine methylsulphate is given by intramuscular injection to patients with myasthenia gravis, about 50 per cent of the dose is excreted unchanged, whereas after oral administration little or no unchanged drug can be detected in the urine2,6.

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