Patients with chronic kidney disease (CKD) constitute a population at high risk for adverse drug reactions and/or drug-drug interactions. Renal dysfunction-induced pathophysiological changes may alter both medication pharmacodynamics and handling. Most pharmacokinetic parameters are adversely affected by impaired kidney function, among which reduced glomerular filtration and altered tubular secretion and reabsorption lead to the most specific alterations. Dosages of drugs cleared by the kidney should usually be adjusted according to creatinine clearance. Recommended methods for maintenance dosing adjustments are dose reductions, lengthening the dosing interval, or both. Appropriate drug selection and dosing in patients with CKD is imperative to avoid drug adverse events and to ensure optimal patient outcomes.