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The combination of naltrexone and guanfacine is a pharmaceutical therapy being investigated by the Baylor College of Medicine for the treatment of heroin dependence and the prevention of relapse in detoxified individuals. Naltrexone is a small molecule mu-opioid receptor antagonist that blocks the euphoric effects of opioids and reduces cravings. Guanfacine is an alpha-2A adrenergic receptor agonist, traditionally used as an antihypertensive, which is hypothesized to manage noradrenergic-mediated withdrawal symptoms and reduce stress-induced relapse. This specific combination was evaluated in a Phase 2 randomized, double-blind, placebo-controlled factorial study (NCT00218400) led by Dr. Thomas R. Kosten in St. Petersburg, Russian Federation.
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