Nucynta

AU:C N02AX06(WHO) AU:S8(Controlled drug)BR:Class A1(Narcotic drugs)CA:Schedule IDE:Anlage III(Special prescription form required)UK:Class A (Schedule 2 CD)US:Schedule IIUN:UnscheduledEU:Rx-only 3-[(1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl]phenol 175591-23-8YHCl:175591-09-0Y 9838022 7477 DB06204Y 8013742Y H8A007M585HCl:71204KII53Y D06007Y ChEMBL1201776Y DTXSID30170003 Interactive image Oc1cc(ccc1)[C@@H]([C@@H](C)CN(C)C)CC InChI=1S/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1YKey:KWTWDQCKEHXFFR-SMDDNHRTSA-NY Tapentadol, sold under the brand namesNucyntaandPalexiaamong others, is a syntheticopioidanalgesicwith a dual mode of action as ahighly selectivefull agonistof theμ-opioid receptorand as anorepinephrine reuptake inhibitor(NRI).Tapentadol is used medically for the treatment of moderate to severepain.It is highly addictive and is a commonlyabused drug. Frequently reported adverse effects includeeuphoria,constipation,nausea,vomiting,headaches,loss of appetite,drowsiness,dizziness,itching,dry mouth, andsweating.More severe adverse reactions can occur, includingaddictionanddependence,substance abuse,respiratory depression, and an elevated risk ofserotonin syndrome.Concurrent use of tapentadol withserotonergic drugsor central nervous systemdepressants– includingalcohol,cannabis,benzodiazepines, and other opioids – can heighten the risks of excessive serotonin accumulation, profoundsedation, dangerously slowed breathing and death. Analgesia occurs within 32 minutes of oral administration, and lasts for 4–6 hours.Tapentadol is takenby mouth, and is available inimmediate-releaseandcontrolled-releaseformulations.Tapentadol's combined mechanism of action is often compared to that oftramadol.Unlike tramadol, tapentadol is not metabolised bycytochrome P450enzymes, but rather throughglucuronidation.Due to this, tapentadol has fewer interactions with other medications and fewer side effects when compared with tramadol. Like tramadol, tapentadol affects both theopioidsystem and thenorepinephrinesystem to relieve pain.Unlike tramadol, it has only weak effects on the reuptake ofserotoninand is a significantly more potent opioid with no known active metabolites.Thepotencyof tapentadol is somewhere between that of tramadol andmorphine,with ananalgesicefficacy comparable to that ofoxycodonedespite a lower incidence of side effects.The CDC Opioid Guidelines Calculator estimates a conversation rate of 50mg of tapentadol equaling 10 mg of oraloxycodonein terms of opioid receptor activation. In the late 1980s,Grünenthaldeveloped tapentadol to improve ontramadol,which they had created in 1962.Their goal was to design a molecule that minimized serotonin activity, strongly activated theμ-opioid receptor, inhibitednorepinephrinereuptake, and worked without metabolic activation.The result was tapentadol. Due to the high risk of addiction,substance misuse, anddependence,tapentadol is aSchedule II controlled substancein the United States,aSchedule 8 controlled drugin Australia,and aClass A controlled substancein the United Kingdom.