Ophthalmology is the branch of medicine devoted to the study, diagnosis, and treatment of disorders affecting the eye and visual system, as glaucoma is. It is a leading cause of irreversible blindness worldwide and is commonly diagnosed solely in advanced stages of the disease when important and irreversible losses of visual field have already occurred. One of the major therapeutic options for its management is based on the inhibition of the metalloenzyme Carbonic Anhydrases. Indeed, CA inhibitors (CAIs) diminish ocular hypertension in glaucomatous patients by mainly reducing the rate of bicarbonate formation and thus, the secretion of the aqueous humor. This chapter presents an overview of the current CAIs used for treating glaucoma and introduces the latest pharmaceutical advancements in this field.