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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]
Medical use
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]
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Tapentadol is an opioid pain medication used to treat moderate to moderately severe pain, both acute and chronic.
Product Details:
Product Name: Tapentadol Powder
CAS: 175591-09-0
MF: C14H23NO
Purity: >99.5%
Appearance: Powder
Packing: Aluminum Foil Bag or Plastic Bag
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Tapentadol hydrochloride is an opioid analgesic for treatment of moderate to severe pain. Analgesia occurs within 32 minutes of oral administration,
and lasts for 4–6 hours.
Quick Details
Product Name: Tapentadol
Synonyms: Tapentadol hydrochloride
CAS No.: 175591-23-8
Molecular Formula: C14H23NO
IUPAC: 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
Molecular weight: 221.34 g/mol
Purity: 99.6%
Appearance: White crystalline powder / off-white powder
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What should I discuss with my healthcare provider before taking tapentadol?
You should not use this medication if you are allergic to tapentadol, or if you have:
severe asthma or breathing problems; or
a blockage in your digestive tract (stomach or intestines).
Do not use tapentadol if you have taken an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include
isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, and tranylcypromine.
Tell your doctor if you have ever had:
breathing problems, sleep apnea;
a head injury, brain tumor, or seizures;
drug or alcohol addiction, or mental illness;
urination problems;
liver or kidney disease; or
problems with your gallbladder, pancreas, or thyroid
Tapentadol Hydrochloride (CAS NO : 175591-09-0)
Documents
3-[(1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol monohydrochloride, (Tapentadol HCl) is the hydrochloride salt of Tapentadol, a centrally acting synthetic analgesic. Tapentadol Hydrochloride combines μ-opioid receptor agonist activity with norepinephrine reuptake inhibition, providing effective management of moderate to severe acute and chronic pain. The compound Tapentadol Hydrochloride is preferred and supplied as a white to off-white crystalline powder, offering good solubility in water and common pharmaceutical solvents. I dual mechanism of action makes it a unique option in pain therapy, with reduced gastrointestinal side effects compared to traditional opioids. It is a CNS agent (therapeutic class) as Phenolic compound (chemical structure).
Active Ingredient
-
Tapentadol Hydrochloride 100 mg per tablet
Indications (Medical Use)
Tapentadol is a centrally acting analgesic (pain reliever) used for:
-
Moderate to severe acute pain
-
Chronic pain management (including neuropathic pain)
Mechanism of Action
-
Dual action:
-
μ-opioid receptor agonist (like opioids → reduces pain perception)
-
Norepinephrine reuptake inhibitor (NRI) (enhances pain suppression in spinal pathways)
-
Dosage (General Information)
(Exact dosage must be prescribed by a doctor)
-
Typical starting dose: 50–100 mg every 4–6 hours as needed
-
Max daily dose: Usually not exceeding 600 mg/day for acute pain
Side Effects
Common:
-
Nausea, vomiting
-
Dizziness, drowsiness
-
Constipation
-
Headache
Serious:
-
Respiratory depression (slowed breathing)
-
Risk of dependence or misuse (opioid-like properties)
-
Seizures (rare)
Precautions & Warnings
-
Controlled Substance: Potential for addiction, misuse, and dependence
-
Avoid alcohol and other CNS depressants
-
Not recommended for patients with severe respiratory depression
-
Use caution in kidney or liver impairment
-
Avoid driving or operating heavy machinery
-
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