Pharmacologic treatment of diseases of the urinary tract of horses is limited to administration of antibiotics for treatment of urinary tract infections (UTIs), administration of drugs that alter urine pH, administration of drugs that alter bladder smooth muscle function or urethral sphincter tone, and treatment of acute renal failure. The indications, mechanisms of action, pharmacokinetic characteristics, and adverse effects of these agents in each of these groups are discussed in this article. The use of the agents is discussed within the context of the pathophysiology of the disease being treated.