The elevated blood pressure produced in pulmonary artery, pulmonary veins, pulmonary capillaries and lung vasculature is collectively known as pulmonary hypertension. The prevalence of pulmonary hypertension has been gradually increasing in industrialized nations. Pulmonary hypertension is a rare lung disorder and it is associated with various stern symptoms such as shortness of breath, dizziness, fatigue, non-productive cough, lethargy, chest pain, angina pectoris, fainting and peripheral edema. No specific medications are available to treat pulmonary hypertension, however, pulmonary hypertension could be treated depending upon the origin and magnitude of hypertension using group of medications including endothelin receptor antagonists, long acting prostacyclin and its analogue, phosphodiesterase 5 inhibitor, calcium channel blockers, anticoagulants, diuretics etc. The ongoing research works revealed numerous potential pharmacological target sites to treat pulmonary hypertension efficiently. In this review, we discussed the molecular mechanisms involved in the pathogenesis of pulmonary hypertension and detailed account of current status of medications employed in the treatment of pulmonary hypertension including their therapeutic outcomes. Moreover, the newly identified potential target sites for managing pulmonary hypertension have been discussed.