Get 10% Discount Apply Coupon Code "USA10" An opioid analgesic with central action, tapentadol is used to treat moderate to severe pain. Compared to conventional opioids, this relatively new drug may have fewer adverse effects while still providing pain relief. The central nervous system (CNS) opioid receptors are the site of tapentadol's action. It also has analgesic effects because it prevents the reuptake of the neurotransmitter norepinephrine.