Produid First-Pass Effect

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Prodrugs can be exploited for improving stability of a particular drug candidate, most frequently to avoid first-pass effect. In first-pass effect (also known as presystemic metabolism) a significant portion of the drug is metabolized in the liver whereupon a small fraction of the drug reaches the systemic circulation to elicit the desired effect. The bioavailability of orally administered propanolol, an antihypertensive drug is much lower than the intravenous injection due to extensive presystemic metabolism. Cytochrome P450 isozymes are involved in its metabolism and the major metabolites are 4-hydroxypropanolol, N-desisopropylpropranolol, and propranolol O-glucuronide. Improved stability was achieved by esterification to hemisuccinate propanolol

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