Captopril's main uses are based on its vasodilation and inhibition of some renal function activities.  These benefits are most clearly seen in:
* Hypertension
* Cardiac conditions such as congestive heart failure and after myocardial infarction
* Preservation of kidney function in diabetic nephropathy.
Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although one study has been negative. Formal clinical trials in depressed patients have not been reported.
It has also been investigated for use in the treatment of cancer. Captopril stereoisomers were also reported to inhibit some metallo-β-lactamases.