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Providing straightforward information pertaining to drugs, drug use & drug policy. The Grey Pages promotes drug-related literacy and advocates a system of viable and tolerant drug policies. This is my personal collection of commentaries, essays, tid-bits, and other such writings on everything ranging from drug use, drug policy and drug-myths, to drug-science, addiction, human behavior, and the workings of the human brain. I started this blog with a particular focus on opioids, and over the past year have found my interest gravitate toward the intriguing, ever-changing world of designer intoxicants (i.e. "research chemicals" or "designer drugs").

Friday, December 10, 2010

First New Analgesic Compound In 25 Years - Nucynta (Tapentadol)




Tapentadol: This is the first centrally acting analgesic (pain reliever) of its type to be released to the market in over 25 years. Chemically, tapentadol is closely related to the weaker drug, tramadol. It was in fact synthesized to emulate the properties of tramadol's highly active metabolite known as M1, or O-Desmethyltramadol - the main metabolite of tramadol, having roughly 200x stronger binding affinity for the mu opioid receptor.

Tapentadol works through two mechanisms; acting as a norepinephrine reuptake inhibitor (or NRI) and as a mu opioid receptor agonist. Drugs of the norepinephrine reuptake inhibitor class are commonly used as secondary analgesics to supplement opioids, and additionally for treating depressive and anxiety spectrum disorders. A norepinephrine reuptake inhibitor can be expected to have stimulating 'upper'-like qualities; drugs of the amphetamine class act on norepinephrine.

Together, the combination of NRI as well as opioid activity can be expected to provide better pain relief than either of the two alone. Tapentadol provides a dual mode of action in a single compound.

The potency of this drug falls into the mid-range of narcotics, similar to oxycodone and hydrocodone. Milligram for milligram, tapentadol is less potent than these drugs, therefore the drug is manufactured in strengths of 50mg, 75mg, and 100mg tablets. Opiate users and addicts report desired pleasant effects and euphoria to become apparent in the higher dose range of 200mg to 300mg however this will vary based on individual tolerance to opioids.

Some have reported the overall effects to be similar to those of oxycodone. Relief of pain, euphoria, chattiness and sociability, empathy, increased energy, miosis, constipation and possible respiratory depression in high doses are all likely effects a lesser degree of sedation relative to other narcotics and likely stimulant effects are to be expected.

Nucynta is available in the three dosages pictured below: 50mg, 75mg, and 100mg.





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