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Sex should be considered during the selection of cardiovascular medications and dosages of cardiovascular medications. There is mounting evidence that clinically important differences between the sexes exist in the pharmacokinetic processes that determine drug concentrations and in the pharmacodynamic processes that determine physiologic responses to pharmacologic agents. Although aging also affects these processes, aging does not eliminate the sex-related differences. The major pharmacokinetic differences between the sexes, on average, are lower weight and distribution volumes in women compared with men and lower renal drug clearance in women compared with men. Sex-related differences in hepatic drug clearance are less predictable. Pharmacodynamic responses that differ between the sexes include increased adverse cardiovascular drug effects in women compared with men (torsade de pointes arrhythmias, increased risk of hemorrhagic consequences of anticoagulation or thrombolytic therapy, electrolyte abnormalities with diuretics, myopathy with HMG Co-A reductase inhibitors, cough with ACE inhibitors, and increased incidence of thrombosis). Recommendations for optimizing cardiovascular drug therapy for the older women include individualization of drug selection to minimize the number of medications and side effects; dosage adjustment based on age, size, and sex; close monitoring for side effects; and consideration of cost and access to medications. Optimal care for the older woman with cardiovascular disease will also require investigation of cardiovascular medications in older women and of therapies for cardiovascular diseases that are more common in women than men.