Buy Tapentadol (Nucynta) Cas 175591-23-8

Tapentadol, sold under the brand names Nucynta and Palexia among others, is a synthetic opioid analgesic with a dual mode of action as a highly selective full agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI).^[6] Tapentadol is used medically for the treatment of moderate to severe pain.^[2] It is highly addictive and is a commonly abused drug.^{[2][8][9][10]}

Frequently reported adverse effects include euphoria, constipation, nausea, vomiting, headaches, loss of appetite, drowsiness, dizziness, itching, dry mouth, and sweating.^[11] More severe adverse reactions can occur, including addiction and dependence, substance abuse, respiratory depression, and an elevated risk of serotonin syndrome.^[12][13] Concurrent use of tapentadol with serotonergic drugs or central nervous system depressants – including alcohol, cannabis, benzodiazepines, and other opioids – can heighten the risks of excessive serotonin accumulation, profound sedation, dangerously slowed breathing and death.^[9][14]

Analgesia occurs within 32 minutes of oral administration, and lasts for 4–6 hours.^[15] Tapentadol is taken by mouth, and is available in immediate-release and controlled-release formulations.^[16] Tapentadol’s combined mechanism of action is often compared to that of tramadol.^[15] Unlike tramadol, tapentadol is not metabolised by cytochrome P450 enzymes, but rather through glucuronidation.^[17] Due to this, tapentadol has fewer interactions with other medications and fewer side effects when compared with tramadol.^[17]

Like tramadol, tapentadol affects both the opioid system and the norepinephrine system to relieve pain.^[18] Unlike tramadol, it has only weak effects on the reuptake of serotonin and is a significantly more potent opioid with no known active metabolites.^[15][19] The potency of tapentadol is somewhere between that of tramadol and morphine,^[20] with an analgesic efficacy comparable to that of oxycodone despite a lower incidence of side effects.^[6] The CDC Opioid Guidelines Calculator estimates a conversation rate of 50mg of tapentadol equaling 10 mg of oral oxycodone in terms of opioid receptor activation.^[21]

In the late 1980s, Grünenthal developed tapentadol to improve on tramadol,^[22] which they had created in 1962.^[23] Their goal was to design a molecule that minimized serotonin activity, strongly activated the μ-opioid receptor, inhibited norepinephrine reuptake, and worked without metabolic activation.^[22] The result was tapentadol. Due to the high risk of addiction, substance misuse, and dependence,^[24][10][14] tapentadol is a Schedule II controlled substance in the United States,^[25] a Schedule 8 controlled drug in Australia,^[26] and a Class A controlled substance in the United Kingdom.^[27]

Tapentadol is used for the treatment of moderate to severe pain for both acute (following e.g. injury or surgery) and chronic musculoskeletal pain.^[28] It is also specifically indicated for controlling the pain of diabetic neuropathy when around-the-clock opioid medication is required.

Extended-release formulations of tapentadol are not indicated for use in the management of acute pain and are instead indicated only for the relief of severe, disabling pain, that is long-term in nature and cannot be controlled by any other pharmacological means.^[6][29][30]

Tapentadol is pregnancy category C. There are no adequate and well-controlled studies of tapentadol in pregnant women, and tapentadol is not recommended for use in women during and immediately prior to labor and delivery.^[30]

There are no adequate and well-controlled studies of tapentadol in children.^[30]