Oxymorphone or 14-hydroxydihydromorphinone is a semi-synthetic opioid analgesic that is derived from thebaine and is approximately six to eight times more potent than morphine. It is a powerful opioid agonist that specifically binds to mu-opioid receptor, is marketed in oral form (Opana, Opana ER) in 5, 10, 20, and 40 mg tablets, as a suppository (Numorphan) in
5 mg, and as an injectable hydrochloride salt in 1 mg doses. Until its removal from the US market in the early 1970s, oxymorphone (popularly known as "blues") was one of the most sought-after opioids by the intravenous drug using population. Containing very few insoluble binders which made them easy to inject, the extended release blue-colored tablets were profoundly potent when used intravenously. These tablets were known to be extremely euphoric which is comparable to or better than heroin. As with other opioids, oxymorphone can cause physical dependency and has the potential for abuse. Being especially potent, oxymorphone can be used to alleviate dyspnea in patients with left ventricular failure.
Having been shown by placebo-controlled trials to be effective in alleviating moderate to severe pain associated with osteoarthritis (Matsumoto et al. 2005, Mcllwain and Ahdieh 2005), cancer (Sloan et al. 2005), orthopedic surgery (Ahdieh et al. 2004), and chronic low back pain (Hale et al. 2005, Gammaitoni et al. 2007), oxymorphone may be a new treatment option for use in the illicit or licit substance-abusing patient and for use during opioid rotation. For patients with addictive disorder, it is an option for the relief of moderate to severe pain, as a preoperative medication to alleviate apprehension, maintain anesthesia, and as an obstetric analgesic. At least in chronic low back pain patients, oxymorphone is found equally effective in both opioid-naive and opioid-experienced patients. It may be given in 0.5 mg increments up to a total of 2 mg especially in patients who have required at least 4 mg of hydromorphone. The extended release formulation is designed to continuously release drug during the 12-h period and its pharmacokinetic properties are consistent with its use for around the clock therapy. A steady state is usually achieved within 3 days with a relatively stable plasma concentration (Adams and Ahdieh 2004). Having both the extended- and immediate-release formulations provide flexibility in dosing that is useful when converting patients from different opioids (Adams and Ahdieh 2004, Adams and Ahdieh 2005).
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