Tapentadol IR (Immediate Release); A Novel Analgesic for Acute Pain

Sanjeev Kumar,Seema Rani, Ram Ch,er Siwach, Prem Verma

Journal of Pharmaceutical Research(2013)

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摘要
Acute pain is often undertreated and inadequate management may lead to poor patient outcome and potentially life - threatening complications. Opioids and nonopioid analgesics i.e. non- steroidal anti-inflammatory drugs are the groups of analgesics used to treat acute pain; unfortunately both are associated with potentially serious side effects. Opioids provide relief of moderate to severe acute pain however associated with particularly gastrointestinal side effects. Tapentadol is a FDA approved centrally acting novel analgesic for the treatment of moderate to severe acute pain with a dual mode of action as μ-opioid receptor agonist and as a nor- epinephrine reuptake inhibitor. The drug follows linear pharmacokinetics, absorbed quickly and is excreted primarily by the renal system. The analgesic effects of tapentadol are independent of metabolic activation and tapentadol has no active metabolites so theoretically tapentadol may be associated with a low potential for interindividual variations and drug–drug interactions. In various phase III trials in patients with various types of moderate to severe acute pain have shown that tapentadol immediate release IR 50 to 100 mg every 4 to 6 hours shows analgesic effect comparable to that of oxycodone IR 10 or 15 mg every 4 to 6 hours with a lower incidence of nausea, vomiting, and constipation. So, tapentadol is an important addition to the armamentarium for the management of moderate- to-severe pain.
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