Tapentadol is rapidly absorbed; oral bioavailability after single dose administration is 32% thanks to extensive first pass metabolism. Plasma steady-state concentration is achieved in 25-30 h when the drug is run orally every 6 h.
Tapentadol is cosmopolitan throughout the body. Following intravenous (IV) administration, the quantity of distribution is 540±98 L. Only 20% of the drug is sure to plasma proteins.
Metabolism and elimination
Tapentadol follows first-order elimination kinetics. Half life is 4 h. the entire clearance is 1530±177 ml/min.
Dosage and formulation
Tapentadol is out there as 50, 75, and 100 mg oral tablets. Maximum dosage is 600-700 mg in divided doses every 4-6 h. In India, it’s marketed under the trade names Vorth TP (Glenmark Pharmaceuticals), Tydol (Ranbaxy Laboratories Ltd.), and Dolproxyvon (Wockhardt Ltd.). It are often administered with or without food. Tapentadol is out there as immediate-release (IR) and extended-release (ER) formulations. A study has been published regarding the conversion of buy tapentadol online IR to ER, which suggests that an immediate milligram to milligram conversion on a complete daily dose basis is acceptable . The IV formulation is presently under clinical trials and its use isn’t yet approved
The efficacy of Tapentadol for relief of moderate to severe acute pain has been evaluated in three randomized, test , phase three studies.In one among the postoperative pain study, patients received Tapentadol 50 or 75 mg, oxycodone 10 mg, or placebo every 4-6 h for 72 h following bunionectomy; within the other postoperative pain study, patients received Tapentadol 50, 75. In both studies, improvements in pain intensity were observed with Tapentadol that were almost like those observed with oxycodone supported pain intensity measurements on the numerical rating scale (NRS).The results of the study showed that single doses of Tapentadol 75 mg or higher effectively reduced pain during a dose-related fashion and were well-tolerated relative to morphine.
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Efficacy for short-term use in chronic inflammatory pain was examined in patients with the end-stage degenerative joint disease over a period of 10 days while awaiting knee or hip replacement surgery during a double-blind placebo-controlled trial; Tapentadol 50 mg and 75 mg and oxycodone 10 mg produced significant reductions in pain intensity as compared with placebo and Tapentadol wasn’t inferior to oxycodone. during a recent analysis of pooled data from three-phase, three studies in patients with chronic osteoarthritis knee or low back pain evaluating the efficacy and tolerability of Tapentadol as compared with placebo and oxycodone showed that Tapentadol (100-250 mg, twice daily) provided efficacy that was almost like that by oxycodone (20-50 mg, twice daily) with a superior gastrointestinal tolerability profile and fewer treatment discontinuations. A phase three trial in patients with painful diabetic peripheral neuropathy showed the efficacy of Tapentadol in neuropathic pain.NRI action of Tapentadol makes it especially useful in neuropathic pain.
Comparison with Tramadol
Tramadol is that the other analgesic with dual mechanism of action. Hence, it might be pertinent to match both the drugs. Tapentadol has several advantages as compared with Tramadol. The comparison of both the drugs is summarised in
Limitations of Tapentadol as compared to Tramadol
At present IV/IM formulation of Tapentadol isn’t approved to be used , hence in situations where the patient is fasting Tapentadol can’t be used. overnight tramadol are often administered through various routes like oral IV, IM, suppository, and epidural, whereas Tapentadol can only be administered oral. Tapentadol is costlier in comparison to tramadol or other opioids.
Safety and Tolerability
Opioids are commonly related to side effects like nausea, vomiting, constipation, dizziness, headache, somnolence, and pruritis. These adverse effects could also be dose limiting and are often severe enough for patients to discontinue therapy. The tolerability of Tapentadol has been evaluated in trials during which patients with acute pain received multiple oral doses. the foremost common adverse effects noted with Tapentadol were nausea, vomiting, constipation, dizziness, somnolence, headache, and pruritis; these effects are typical of a MOR agonist. The incidence of those adverse effects has been reported to be lesser with Tapentadol as compared thereto by opioids like morphine and oxycodone; this will possibly flow from to lower affinity of Tapentadol for MOR as compared to other opioids.
Tapentadol doesn’t cause significant respiratory depression. Studies have shown that abrupt discontinuation of the drug after long-term therapy doesn’t cause opioid-like withdrawal symptoms and, albeit they are doing occur, these symptoms are mild. Long-term therapy wasn’t related to clinically significant changes in laboratory values (including hepatic and renal parameters), vital signs, or Electrocardiography findings.