This review presents the pharmacotherapeutic approaches available in the treatment of glaucomatous optic neuropathy. Although its etiology is multi-factorial, currently, the main therapy is to decrease intraocular pressure. New therapies are being developed; the current trend is a retinal ganglion cell neuroprotection. Neuroprotection is achieved by combining antihypertensive agents with drugs that directly protect the optic nerve by promoting cell survival and inhibition of neuronal signals that initiate apoptosis. The treatment should also preserve the ocular hemodynamics, ensure proper patient compliance and be free of side effects.