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Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril . The thiol functional group of captopril was replaced with a carboxylic acid group, but additional modifications were required to achieve a potency similar to captopril.
Enalaprilat was developed first, partly to overcome these limitations of captopril. The sulfhydryl moiety was replaced by a carboxylate moiety, but additional modifications were required in its structure-based design to achieve a potency similar to captopril. Enalaprilat, however, had a problem of its own in that it had poor oral availability.
Lisinopril is the lysine-analog of enalaprilat, the active metabolite of enalapril. [15] ... the elimination half-life is much longer, at around 30 hours. [18]
The other elimination pathways are less important in the elimination of drugs, except in very specific cases, such as the respiratory tract for alcohol or anaesthetic gases. The case of mother's milk is of special importance. The liver and kidneys of newly born infants are relatively undeveloped and they are highly sensitive to a drug's toxic ...
The results were 2 active inhibitors: Enalaprilat and Lisinopril. These compounds both have phenylalanine in R position which occupies the S 1 groove in the enzyme. The result was thus these two new, potent tripeptide analogues with zinc-coordinating carboxyl group: Enalaprilat and Lisinopril. [1] [9]
In pharmacology, clearance is a pharmacokinetic parameter representing the efficiency of drug elimination. This is the rate of elimination of a substance divided by its concentration. [1] The parameter also indicates the theoretical volume of plasma from which a substance would be completely removed per unit time.
Alternatively, since the radioactive decay contributes to the "physical (i.e. radioactive)" half-life, while the metabolic elimination processes determines the "biological" half-life of the radionuclide, the two act as parallel paths for elimination of the radioactivity, the effective half-life could also be represented by the formula: [1] [2]
A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. [1] [2] Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted ().