Products
Oxymorphone is commercially available in the United States as tablets and sustained-release tablets and has also been administered parenterally and rectally. It is not registered in many countries. Oxymorphone has been approved in the U.S. since 1959 (brand names: Numorphan, Opana, Opana ER, generics). It is a narcotic drug. Due to the potential for abuse, the Food and Drug Administration (FDA) asked Endo Pharmaceuticals in 2017 to withdraw Opana ER from the market. The company complied with that directive that same year.
Structure and properties
Oxymorphone (C17H19NO4, Mr = 301.3 g/mol) is usually present in drugs in the form of the salt oxymorphone hydrochloride, a white, odorless powder that is highly soluble in water. It is a semisynthetic opioid that can be derived from thebaine or morphine and is closely related to hydromorphone.
Effects
Oxymorphone has analgesic, depressant, antianxiety, cough-irritant, and psychotropic properties. The effects are due to selective agonism at μ-opioid receptors. Oxymorphone is about ten times more potent than morphine and crosses the blood–brain barrier well due to its lipophilicity. The half-life is in the range of about 8 hours.
Indications
For the treatment of moderate to severe pain.
Dosage
According to the professional information. Dose is adjusted on an individual basis. Discontinuation should be gradual. Oxymorphone may be administered perorally, rectally, or parenterally, among other routes.
Abuse
Like other opioids, oxymorphone can be abused as a depressant and psychotropic intoxicant. Because of the health risks and high potential for dependence, this is strongly discouraged.
Contraindications
- Hypersensitivity
- Respiratory depression
- Bronchial asthma
- Paralytic intestinal obstruction
- Liver dysfunction
Full precautions can be found in the drug label.
Interactions
Metabolism occurs mainly via glucuronidation, and an active metabolite is also formed. According to the literature, unlike other opioids, oxymorphone is not a CYP450 substrate. Drug-drug interactions have been described with central depressant drugs, alcohol, other opioids, opioid antagonists, cimetidine, anticholinergics, and MAO inhibitors, among others.
Adverse effects
The most common possible adverse effects include nausea, fever, drowsiness, vomiting, pruritus, headache, dizziness, constipation, and confusion. An overdose is life-threatening.
