Conditions which Affect the Pharmacokinetic Profile of Amlodipine
Because of the unusual pharmacokinetic profile of amlodipine (slow onset and long duration of action, high bioavailability and slow rate of clearance) (Chapter 7), coupled with its vascular selectivity (Chapter 8), this particular calcium antagonist would seem to be well suited for use in the long-term management of hypertensive patients and of patients with other cardiovascular disorders. It is worth considering, therefore, whether its pharmacokinetic profile is affected by conditions which are likely to be encountered in either of these populations. For example, it is necessary to consider whether age, renal impairment, hepatic disorders, or the concomitant administration of other drugs, alters its pharmacokinetic profile and clinical usefulness. Possible use in combination with other drugs includes not only its use in combination with beta blockers or digoxin, but also as an “add-on” therapy in patients not well controlled on existing therapy, as, for example in hypertensives not adequately controlled with an ACE inhibitor such as enala-pril. In this later case, the combination of these two regimes, enalapril and amlodipine, has been found to be effective and well tolerated (Jensen et al., 1990).
KeywordsCalcium Antagonist Pharmacokinetic Profile Beta Blocker Grapefruit Juice Peak Plasma Level
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