How to use Captopril. Take this medication by mouth on an empty stomach (at least 1 hour before meals) as directed by your doctor, usually two to three times a day. Because of the potential for serious adverse reactions in nursing infants from captopril, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of CAPOTEN to the mother. Captopril is used alone or in combination with other medications to treat high blood pressure and heart failure. It is also used to improve survival and reduce the risk of heart failure after a heart attack in patients a heart condition called left ventricular hypertrophy (enlargement of the walls of the left side of the heart). Captopril helps control high blood pressure, but it won't cure the condition. Continue to take the drug even if you feel well. Don't stop taking captopril without first talking to your doctor. Captopril is an oral drug and a member of a class of drugs called angiotensin converting enzyme (ACE) inhibitors. ACE inhibitors are used for treating high blood pressure, heart failure, and for preventing kidney failure due to high blood pressure and diabetes. The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including captopril, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. Captopril was developed in 1975 by three researchers at the U.S. drug company Squibb (now Bristol-Myers Squibb): Miguel Ondetti, Bernard Rubin, and David Cushman. Squibb filed for U.S. patent protection on the drug in February 1976 and U.S. Patent 4,046,889 was granted in September 1977. Captopril is an ACE inhibitor. ACE stands for angiotensin converting enzyme. Captopril is used to treat high blood pressure (hypertension), congestive heart failure, kidney problems caused by diabetes, and to improve survival after a heart attack. Captopril prescription and dosage sizes information for physicians and healthcare professionals. Pharmacology, adverse reactions, warnings and side effects. Capoten (captopril) is an ACE inhibitor. ACE stands for angiotensin converting enzyme. Capoten is used to treat high blood pressure (hypertension), congestive heart failure, kidney problems caused by diabetes, and to improve survival after a heart attack.