Objective: Hyperprolactinemia is a clinical condition characterized by consistent elevation of plasmatic prolactin levels above 25ng/mL. The aim of this analysis was to estimate the cost-effectiveness ratios of cabergoline, bromocriptine and the sequential therapy (defined as the treatment initiated with bromocriptine followed by cabergoline) in patients with hyperprolactinemia caused by hypophyseal microadenoma within the Social Security Institute for State Workers (ISSSTE). Methods: A cost-effectiveness analysis was developed using a Bayesian decision-tree model from the Mexican payer's perspective. The model simulates costs and effectiveness in a 31-months period. Effectiveness measure was the number of months with prolactin levels controlled. Efficacy data and model transition probabilities were obtained from international literature. The comparators were cabergoline (0.5mg twice a week), bromocriptine (5mg/day) and sequential therapy. Resource use data and cost were obtained from hospital records of patients being treated at a third-level hospital from ISSSTE in Mexico City (n=43). Costs and health outcomes were discounted using a 3% annual rate. One-way and probabilistic sensitivity analyses were performed using the Monte Carlo Simulation first-order approach. Results: Cabergoline, yielded 27.9 months of patients with prolactin levels controlled followed by the sequential therapy with 20.3 months and bromocriptine (17.7 months). The mean treatment costs were US$5046±504 for cabergoline; US$4341±789 for the sequential therapy and US$3937±785 for treatment with bromocriptine. ICERs estimated using bromocriptine as the baseline treatment were US$103±89 and US$151±32 for cabergoline and sequential therapy, respectively. Based on the one-way sensitivity analysis, cabergoline strategy could be a cost-saving therapy with a reduction of 27% in its price. Probabilistic sensitivity analyses showed that carbergoline was the treatment more cost-effective (p<0.05). Conclusion: In Mexico, cabergoline treatment was the most cost-effective alternative because of its higher number of months with prolactin levels controlled and surgeries avoided. These results should be taken into account by Mexican health professionals in the management of hyperprolactinemia.