Despite the major new insights into our knowledge of the mechanisms underlying initiation and perpetuation of atrial fibrillation (AF) gained in the last decade, the treatment of this common arrhythmia remains unsatisfactory in many patients. Although several new treatment modalities (e.g., internal cardioversion, pulmonary vein ablation, preventive pacing) have been developed, pharmacologic therapy remains the first-line therapy in most patients with AF. As illustrated by recent trials comparing rhythm control and rate control, current antifibrillatory drugs are hampered by a relatively low success rate in maintaining long-term sinus rhythm and the occurrence of proarrhythmic and other adverse events. This article discusses currently available antiarrhythmic drugs for rhythm and rate control, with special emphasis on more recently developed drugs and drugs still under development. Selective blockers of atrial ion channels (IKur and IK.ACh), multi-ion channel blockers, and selective A1-adenosine receptor antagonists are examples of the newer antiarrhythmic drugs that are expected to be more effective and safer than those currently available.