Tapentadol 100mg: a new analgesic among opioids

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Tapentadol is a brand-new, centrally acting analgesic with a dual mode of action that combines noradrenaline reuptake inhibition and mu-opioid receptor agonism in a single molecule. It has a lower side effect profile when compared to opioids and nonsteroidal anti-inflammatory drugs. Tapentadol 100mg is a good analgesic for treating acute, chronic, and neuropathic pain because of its dual mechanism of action.

Tapentadol anlgesic

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Tapentadol online is a non-racemic chemical that is 3-((1R,2R)-3-(dimethylamino)-1-ethyl-2-methyl propyl) phenol hydrochloride. Tapentadol’s chemical structure is C14H23NO.HCl. It was initially created in the USA and sold under the trade name Nucynta by Ortho-McNeil-Janssen Pharmaceuticals.

The two mechanisms of action of tapentadol—MOR agonism and noradrenaline reuptake inhibition—allow it to reduce pain (NRI). When compared to delta- and kappa-opioid receptors, it has a more than or equal to the ten-fold affinity for MOR. Compared to morphine, tapentadol has a 44-fold reduced affinity for MOR. NRI raises noradrenaline (NA) levels, which activates inhibitory alpha-2 receptors to provide analgesia. Its opioid-sparing actions are a result of this dual mode of action. Although tapentadol has a negligible effect on serotonin reuptake, it does have an analgesic effect. Despite having a lesser affinity for binding to MOR than morphine, tapentadol still has an analgesic effect that is only 2-3 times as strong. This is because the drug still has a noradrenergic mechanism of action.

opioid addiction

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Absorption

Tapentadol has a quick half-life and a 32 percent oral bioavailability after a single dose due to substantial first-pass metabolism. When the medication is taken orally every 6 hours, plasma steady-state concentration is reached in 25–30 hours.

Distribution

The body has a large distribution of tapentadol. After intravenous (IV) dosing, the distribution’s volume is 54098 L. Plasma proteins are only able to bind 20% of the medication.

Metabolic process and eviction

A significant amount of tapentadol’s metabolites are inactive (97 percent of the administered dose). Tapentadol-O-glucuronide is the main metabolite, and the main pathway of metabolism is conjugation with glucuronic acid to form glucuronides. Additionally, CYP2C9, CYP2C19, and CYP2D6 metabolize it into N-desmethyl tapentadol and hydroxyl tapentadol, which are then further metabolized by conjugation. The metabolism does not rely heavily on CYP enzymes. The analgesic effect is unrelated to any of the metabolites. None of the CYP isoforms’ activities are either inhibited or stimulated by tapentadol.

First-order elimination kinetics apply to tapentadol. Nearly all (99%) of the time, tapentadol and its metabolites are eliminated by the kidneys. The half-life is 4 hours. 1530177 ml/min is the overall clearance.

metabolic process

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Medication and preparation

There are oral pills of tapentadol in strengths of 50, 75, and 100 mg. The maximum dose is divided into doses of 600–700 mg every 4–6 hours.  It is sold in India under the brand names Vorth TP, Tydol, and Dolproxyvon, all of which are manufactured by Glenmark Pharmaceuticals. Whether taken with or without the meal is up to you. Both immediate-release (IR) and extended-release (ER) versions of tapentadol are offered. A study on the conversion of tapentadol IR to ER was published, and the results imply that a direct milligram-to-milligram conversion based on the total daily dose is appropriate. Clinical trials are currently being conducted on the IV formulation, and its use is not yet authorized.

Unique Group

Tapentadol’s safety in young patients under the age of 18 as well as in expectant and nursing mothers has not yet been determined. Patients with severe renal impairment are not advised to use it. In patients with moderate hepatic impairment, tapentadol should be taken with caution and at a lower dosage; it is not suggested for use in people with severe hepatic impairment. In senior people, it is best to start with lower suggested doses.

Drug interactions

Tapentadol drug interactions Because of its limited protein binding and low likelihood of displacement responses. There is little chance of pharmacokinetic medication interactions with tapentadol. When tapentadol was taken alongside paracetamol, naproxen, or aspirin, no appreciable change in tapentadol’s plasma levels was seen. Both Tapentadol and metoclopramide, as well as omeprazole and probenecid, do not interact with one another. Tapentadol may cause further CNS depression in patients who are already taking other opioids, general anesthetics, phenothiazines, sedative-hypnotics, or other CNS depressants like alcohol. This additional CNS depression may show up as respiratory depression, hypotension, or deep sleepiness.

Contraindications

Patients with pulmonary impairment (acute bronchial asthma, severe respiratory depression) in unmonitored environments or without resuscitation tools

Ileus paralytics

Use of MAOIs currently or recently (within 14 days) due to a probable rise in NA levels that could result in adverse cardiovascular events.

Indications

  • Acute discomfort ranging from mild to severe
  • Enduring pain
  • The ache that is neurotic

Conclusion

The other analgesic with a dual mode of action is tramadol. It is also considered one of the most effective analgesics among other opioid medications.