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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.
An equianalgesic chart is a conversion chart that lists equivalent doses of analgesics (drugs used to relieve pain). Equianalgesic charts are used for calculation of an equivalent dose (a dose which would offer an equal amount of analgesia) between different analgesics. [1]
Duration of effect is dose-related; at recommended doses, antihypertensive and haemodynamic effects have been shown to be maintained for at least 24 hours. [21] [22] Enalapril has a slower onset of action than Captopril but a greater duration of action. However, unlike Captopril, Enalapril does not have a thiol moiety.
Enalapril is actually a prodrug; the active metabolite is enalaprilat. [27] The di-acid metabolite of enalapril, enalaprilat, and its lysine analogue lisinopril are potent inhibitors of angiotensin-converting enzyme (ACE); they do not contain sulphydryl groups. Both drugs can be assayed by high-pressure liquid chromatography and by ...
Its main focus is on drugs with a narrow therapeutic range, i.e. drugs that can easily be under- or overdosed. [1] TDM aimed at improving patient care by individually adjusting the dose of drugs for which clinical experience or clinical trials have shown it improved outcome in the general or special populations.
Therefore, the dose required to give a certain plasma concentration can be determined if the V D for that drug is known. The V D is not a physiological value; it is more a reflection of how a drug will distribute throughout the body depending on several physicochemical properties, e.g. solubility, charge, size, etc.
where De is the effective dose, B bioavailability and Da the administered dose. Therefore, if a drug has a bioavailability of 0.8 (or 80%) and it is administered in a dose of 100 mg, the equation will demonstrate the following: De = 0.8 × 100 mg = 80 mg
To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value of the deviation range is employed to represent real bioavailability and to calculate the drug dose needed for the drug taker to achieve systemic concentrations similar to the intravenous formulation. [4]