Myocardial ischemia is caused by serious atherosclerotic narrowing of the coronary arteries; this will be presented as angina pectoris (AP) in most patients. The major risk factors that we need to be aware of are diet, exercise, hypertension, smoking, diabetes and blood lipid levels. This comprehensive review was done by using the PUBMED databases and will provide the summary of mechanism of action and clinical efficacy of traditional and emerging agents for AP. Anti-anginal treatment includes traditional drugs, 2nd generation drugs and other novel agents. The traditional therapy includes nitrates, calcium channel blockers and beta-blockers. 2nd generation includes ranolazine, nicorandil, ivabradine, trimetazidine, L-arginine and perhexiline. Some of the novel drugs include Rho kinase inhibitors, xanthine oxidase inhibitors, metabolic modulators, bosentan, capsaicin, molsidomine, omapatrilat and Omecamtiv mecarbil. Other drugs which are used include statins, ACEIs, ARBs, antiplatelet drugs, amiloride, phosphodiesterase inhibitors and thiazolidinedione. In addition to these agents if the patient continues to have persistent refractory AP then coronary revascularization or other unconventional methods could be used for relief, these include enhanced external counterpulsation, gene therapy, herbal medications and spinal cord stimulation. The most effective strategy includes multiple approaches and a multi-drug regimen with drugs which complement each other will result in a more impressive outcome. Further studies and trials are essential to prove the safety and efficacy of the novel drugs used to treat angina.