Elevated liver enzymes, especially transaminases, were noted decades ago in patients given high doses (eg, 300 mg/day) as experimental obesity treatment. They reversed when the drug was halted, as they have when occasionally observed in patients taking normal doses.166 If the enzymes are not reduced, brief hospitalization to stop Inhibitors,research,lifescience,medical excess alcohol intake or tests for such excessive drinking can be diagnostic.167,168 Patients should be evaluated for viral hepatitis, which is very common among former

IV users. Because of the possibility of hepatic effects, baseline liver function tests should be carried out. If abnormal (greater than 3 to 5 times normal), naltrexone should not be started. Monthly lab retests for the first 3 months can be a useful precaution. Although naltrexone affects a variety of endocrine functions,169-172 such effects have not been associated with particular problems. Likewise, although upregulation of opioid receptors has been reported in rodents, it was not found in a human study. Thus, the main risk of heroin Inhibitors,research,lifescience,medical overdose post naltrexone appears to be from loss of tolerance.148 Treatment of pain When patients on naltrexone need analgesia, such as after surgery or in emergency situations, nonsteroidal anti-inflammatory Inhibitors,research,lifescience,medical drugs (NSAIDs,

eg, Ketorolac) should be tried. If not adequate, the blockade can be surmounted by large doses of full agonists but this should only be done in an environment where emergency ventilation is selleck kinase inhibitor available as in a hospital or emergency room because of the danger of overdose. Duration of maintenance There are no clear guidelines on the duration of naltrexone maintenance Inhibitors,research,lifescience,medical although, in general, 6 to 12 months are probably a minimum depending on the circumstances. Careful clinical evaluation of relapse risk should be done prior to the decision to discontinue naltrexone. The 30-day depot injection may improve compliance. Because naltrexone is an antagonist, it can be stopped abruptly without

with_ drawal symptoms. Inhibitors,research,lifescience,medical The high dropout rates and patient preference for agonist treatments will probably continue to keep antagonists in a secondary role and in select populations unless agonist maintenance is not available.173,174 Conclusion Compared with other drugs of abuse, opioid dependence benefits from a wider Bumetanide range of available pharmacological tools for treatment. In spite of this, the large majority of the 1 million heroin addicts and 2 to 3 million prescription opioid abusers are not receiving treatment, and those who enter often only seek detoxification, from which early relapse is the most common outcome. The most successful treatment is long-term maintenance on agonists such as methadone and buprenorphine, but a variety of obstacles, including government regulations, cost, availability, and stigma, combine to diminish their use.