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SUMMARY

Marketed and sold under diverse brand names such as Nucynta and among others, Tapentadol 100mg is an opioid analgesic. This benzenoid medicine shows dual mechanism of action to offer relief from moderate to severe pain. It is a fast-acting analgesic whose effectiveness is quite similar to Tramadol— an opioid pain reliever— and morphine which is a narcotic pain reliever drug.

Its analgesic effect is similar to that of oxycodone; however, buy Tapentadol  online has low potential to develop side effects. It is generally considered as a moderately strong opioid and used extensively for efficient pain management. The USFDA approved the usage of Tapentadol in November 2008.

HISTORY

Led by Helmut Buschmann,Grünenthal, the German pharmaceutical company that invented Tramadol 100mg in 1962, gave birth to its modified version -Tapentadol 100mg. It was invented in the late 1980s while the team was analyzing activity and chemistry of Tramadol. The team took Tramadol as a starting point and Tapentadol invented which showed strong agonist activity at the μ-opioid receptor, strong inhibition to norepinephrine reuptake, and reduced serotonin activity.

Tapentadol 100mg received FDA approval in 2008. It is reported that for over 25 years, Tapentadol was treated as the first new molecular entity of oral centrally acting analgesics class in the USA. Tapentadol extended release was introduced in the United States under the trade name Nucynta ER in the year 2011.

Chemical Profile and Pharmacokinetic Data

Chemical name: Tapentadol Hydrochloride
IUPAC Name: 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
Trade Names: Nucynta, Palexia, Yantil, Tapenta, Tapal, Aspadol etc.
Molecular Formula: C 14 H 23 NO
Molecular Weight: 257.80
Routes of Administration: Oral
Elimination half-life: Approximately 4 to 6 hours
Excretion: Urine and faeces
Chemical and Physical Properties
Color: White is to off-white color to yellow
State: Crystalline powder
Solubility: Easily dissolves in water, in molten in methyl alcohol, very slightly
soluble in ethanol, almost insoluble in acetone.

Tapentadol – Medical Uses

Nucynta (Tapentadol 100mg ) is useful in the treatment of moderate to severe pain in patients 18 years of age and older. It is quite useful to reduce acute pain followed by surgery or injury and for chronic musculoskeletal pain. People also buy Tapentadol online (Aspadol 100mg) for around-the-clock pain management for pain caused by diabetic neuropathy.

Tapentadol Mechanism of action

The exact action of mechanism is not fully known yet. However, studies and researches have estimated that Tapentadol shows dual mechanism of action by being an agonist* of μ-opioid receptor and actively prevents re-uptake of norepinephrine. This analgesic acts on the central nervous system majorly on increasing concentration of extracellular norepinephrine in the brain.

Agonist – An agonist is a chemical substance that attaches itself to a receptor and activates it to produce a biological response.

Tapentadol Dosage

The dosing pattern is structured by your doctor as per the severity of pain, and the previous encounter with similar medicines and the patient’s medical history. Tapentadol 100 mg dosage is given every 4 to 6 hours with regards to the intensity of pain being treated. On the first day of treatment, second dosage can be administered as soon as in one hour post the first dosage, if pain relief is not achieved with the first dosage. Do not overdose on the medicine.

Side Effects

Tapentadol causes side effects in almost all users and they generally require no medical attention. These effects disappear over period of time your body gets accustom to them. In rare incidences, some consumers have reported severe side effects caused by Nucynta.

Gastrointestinal

Common: Constipation, nausea, vomiting, diarrhoea, abdominal discomfort.
Rare: Impaired gastric emptying

 

Neurological

Common: Headache, dizziness, drowsiness, poor concentration, vertigo.

Rare: Abnormal coordination, convulsion.

Psychiatric

Common: Confusion, insomnia, anxiety, depression, restlessness, hallucinations, Tapentadol withdrawal syndrome.

Rare: Drug dependency, abnormal thinking.

Drug Interactions

Tapentadol online (Nucynta) is mainly metabolized in the liver by glucuronidation*process. This medication has low potential for pharmacokinetic drug interferences. When it was given along with naproxen, paracetamol, or aspirin, no change in plasma concentration of Tapentadol was recorded. It does not interact with drugs such as metoclopramide, omeprazole and probenecid. When administered along with other opioid pain relievers, phenothiazines, general anesthetics, hypnotics, sedatives, or other CNS depressants may show adverse effects such as respiratory depression, prolonged sedation, or hypotension.

*Glucuronidation is commonly involved in metabolism of drugs, androgens, bilirubin, glucocorticoids, mineralocorticoids, estrogens, retinoids, fatty acid derivatives, and bile acids. These often involve glycosidic bonds.

Tapentadol Warnings

Impaired Pulmonary Function

Similar to medicines with μ-opioid agonist activity, Tapentadol pain drug is contraindicated in people with respiratory depression. It is also not recommended in patients with severe bronchial asthma.

Renal and Hepatic Impairment

There is no sufficient clinical data available to establish safety of Tapentadol uses in patients with renal and hepatic dysfunction thus it is not recommended. Consult with your doctor to know more.

Pregnancy and Breastfeeding

Tapentadol has not been studied extensively for usage in pregnancy and thus need to be administered only when needed and under strict medical supervision.This medicine passes into the breast milk and thus not recommended to use in breastfeeding women.

Elderly Patients

The standard dosage of 100mg is given to elderly with no renal or hepatic impairment. However, if they are dealing with kidney and/or liver disorders administrating low dosages is recommended.

Paralytic Ileus

Tapentadol is contraindicated in people who are suspected having paralytic ileus.

Driving and operating machinery

This medication may affect the mental or physical ability of a person requiredto perform tasks that demands undivided attention such as driving vehicle or operating heavy machinery.

Alcohol

Tapentadol shows addictive effects when consumed along with alcohol given its high affinity to attach to μ-opioid receptor. This further leads to the onset of severe drowsiness or dizziness and in rare cases, prolonged sedation, hypotension, coma or death may happen.

Serotonin Toxicity

Tapentadol has weak effect on the re-uptake of serotonin. Nonetheless, using Tapentadol 100mg with serotonergic medicines such as SNRIs, SSRIs, MAOIs, TCAs, triptans and St John’s wort may cause serotonin syndrome.

Withdrawal of Tapentadol

The risk of developing withdrawal symptoms increases especially when use of Tapentadol is ceased abruptly. The symptoms may include: insomnia, nausea,  pain, anxiety, upper respiratory symptom, sweating etc. In rare cases, hallucinations have been reported. The risk of the onset of online Tapentadol withdrawal symptoms can be reduced by gradually decreasing the dose before completely discontinuing it.

Tapentadol  Abuse

Tapentadol is a schedule II drug which means it has high abuse potential yet it has safe and accepted medical usages. These medicines are abused by drug abusers and people with history of addiction disorders and/or drug/alcohol addiction. Nucynta can be abused in a similar fashion as that of opioid agonists. This needs to be taken into consideration when a doctor or pharmacist is worried about higher chances of drug misuse and abuse.

These concerns should not be obstacle in managing pain. In fact, all patients receiving Tapentadol pain drug need to be monitored for signs and symptoms of abuse and addiction. Usage of μ-opioid agonists often produces high risk of addiction in spite of moderate usage under stringent medical surveillance. The pain drug can be abused by chewing, snorting or injecting. These misconducts often pose a considerable risk that could cause overdose and in rare cases, life-threatening issues.