Aim of this review is to give complete information about this new drug Tapentadol. It is a centrally-acting opioid analgesic, having a potency between morphine and tramadol. Tapentadol has been approved as immediate release tablets in 50 mg, 75 mg and 100 mg formulation by the United States Food and drug administration.The U.S. Drug Enforcement Agency has placed Tapentadol (which is now being marketed as brand name NUCYNTA(TM) [New synthetic]), into Schedule II of the Controlled Substances Act.3 The chemical name for tapentadol is (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol.4It has a unique dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor1. As a mu-opioid agonist, it binds to and activates mu-opioid receptors in the central nervous system. It modifies sensory and affective aspects of pain, inhibits the transmission of pain at the spinal cord and affects activity at parts of the brain that control pain perception. After oral administration 32% of the drug is absorbed. It is widely distributed in the body. The plasma protein binding is low and amounts to approximately 20%. It can be given in the form of oral tablets dose of 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending on pain intensity. It has efficacy in a broad spectrum of acute and chronic pain models and possibly an improved tolerability profile.
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