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Tapentadol is used to treat moderate to severe acute pain in people who are at least 18 years old. Tapentadol is the first painkiller that the FDA approved that works on the brain (in November 2008). It works as both an NRI and a MOR agonist. Its "opioid sparing" effect comes from the fact that it works in two ways. This helps reduce some of the usual side effects of opioids and may lead to better compliance.


  • As with many centrally-acting painkillers, the dosing plan should be based on the severity of the pain being treated, the patient's history with similar drugs, and the ability to keep an eye on them.
  • Depending on how bad the pain is, you take 50 mg, 75 mg, or 100 mg every 4 to 6 hours.
  • If the first dose doesn't give enough pain relief on the first day, the second dose can be given as soon as an hour after the first dose. The next dose is 50 mg, 75 mg, or 100 mg every 4 to 6 hours. The dose should be changed to keep the pain under control while being well tolerated.
  • Daily doses of more than 700 mg on the first day of treatment and 600 mg on the following days have not been studied and are not recommended.
  • Tapentadol can be taken with or without food.
  • Renal Impairment
  • Patients with mild or moderate kidney damage don't need to change their dose.
  • Tapentadol  has n't been looked at in people with severe kidney damage. It is not recommended for this group of people.
  • Problems with the liver
  • Patients with mild liver damage don't need to change their dose.
  • Patients with moderate liver damage should be careful when taking tapentadol.
  • The first dose for these patients should be 50 mg, and they shouldn't have to wait less than 8 hours between doses (maximum of three doses in 24 hours). The next treatment should keep the pain under control while being well tolerated. This can be done by either shortening or lengthening the time between doses.
  • Tapentadol hasn't been studied in people with severe liver damage, so it's not a good idea to use it in this group.
  •  Patients Who Are Old

In general, the doses that are recommended for older patients with normal kidney and liver function are the same as those for younger adults with normal kidney and liver function. Because older Reference ID: 2858116 3 patients are more likely to have less kidney and liver function, it might be best to start them on the lower end of the recommended dose range.


Tapentadol tablets are round, biconvex, and film-coated. They come in 50 mg of tapentadol (yellow with "O-M" on one side and "50" on the other side), 75 mg of tapentadol (yellow-orange with "O-M" on one side and "75" on the other side), and 100 mg of tapentadol (orange with "O-M" on one side and "


  1. Pulmonary Function Not Working Well

Tapentadol, like other mu-opioid agonists, shouldn't be given to people who have trouble breathing and aren't being watched or don't have access to resuscitation equipment. TAPENTADOL® shouldn't be given to people with severe or acute bronchial asthma, hypercapnia, or a lack of resuscitation equipment.

  1.  Paralytic Ileus

Tapentadol  is n't good for people who have or might have paralytic ileus, just like drugs that act as mu-opioid agonists.

  1. Monoamine Oxidase Inhibitors

Tapentadol shouldn't be given to people who are taking monoamine oxidase (MAO) inhibitors or who have taken them in the last 14 days. This is because tapentadol could make the effects of MAO inhibitors on norepinephrine levels worse, which could cause heart problems.


  1.  Depression of Breathing
  2. The main risk of mu-opioid agonists is that they slow down breathing. Respiratory depression is more common in older or sicker patients, as well as those with low oxygen levels, high carbon dioxide levels, or blocked upper airways. Even low therapeutic doses can have a big effect on pulmonary ventilation in these patients.
  3. Tapentadol should be given with care to people who have conditions like asthma, chronic obstructive pulmonary disease (cor pulmonale), severe obesity, sleep apnea syndrome, myxedema, kyphoscoliosis, depression of the central nervous system (CNS), or coma that cause hypoxia, hypercapnia, or decreased respiratory reserve.
  4. Even normal therapeutic doses of tapentadol may cause apnea in these patients by making it harder for air to get through the airways and making it harder to breathe. Alternative painkillers that don't contain mu-opioid agonists should be looked into, and TAPENTADOL® should only be used under close medical supervision and at the lowest effective dose
  5.  Depression CNS

Patients who take tapentadol along with other mu-opioid agonist analgesics, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, or CNS depressants (like alcohol) may experience more CNS depression. If these drugs are taken with TAPENTADOL®, they may have interactions that cause breathing problems, low blood pressure, deep sedation, coma, or even death. When this kind of combined therapy is being thought about, the dose of one or both of the drugs should be lowered.

  1.  Head injury and higher pressure inside the head
  2. Because opioid painkillers slow breathing and keep carbon dioxide in the body, they can raise the pressure of the cerebrospinal fluid. So, tapentadol shouldn't be given to people who might be affected by high cerebrospinal fluid pressure, like those who have signs of a head injury and high intracranial pressure. Due to their effects on pupillary response and consciousness, opioid painkillers can make it hard to tell how a patient with a head injury is doing.
  3. Tapentadol  should be used with care in people who have had a head injury, have lesions inside the brain, or have other causes of high intracranial pressure.
  4.  Misuse and Abuse

Tapentadol is a Schedule II drug because it is a mu-opioid agonist. Drug addicts and people who abuse drugs look for these kinds of drugs. Changing the use of Schedule II drugs is a crime that can lead to jail time.

Tapentadol can be abused in the same way that legal or illegal opioid agonists can. This should be taken into account when a doctor or pharmacist prescribes or gives out TAPENTADOL® when they are worried about an increased risk of misuse and abuse. The right way to treat pain shouldn't be stopped by worries about abuse and addiction. But all patients who are given mu-opioid agonists need to be carefully watched for signs of abuse and addiction. This is because even when mu-opioid agonist analgesics are used as prescribed. Tapentadol  could be abused by breaking it up, chewing it, snorting it, or injecting it. The person who does these things is at a high risk of overdosing and dying.

  1.  How to Drive and Run Machines

Patients should know that tapentadol may make it hard for them to think or move well enough to do things that could be dangerous, like driving a car or running machinery. This is normal, especially at the start of treatment, when the dose changes, or when the drug is taken with alcohol or sleep aids.

  1.  How Alcohol and Drugs of Abuse Work Together

Because it acts as a mu-opioid agonist, tapentadol may make the effects of alcohol, opioids, or illegal drugs that affect the central nervous system (CNS) worse when taken together.

  1. Seizures

Tapentadol hasn't been tested in a systematic way on people who have a seizure disorder, and these people were left out of clinical studies. Tapentadol shouldn't be given to people who have had seizures in the past or who have any condition that makes them more likely to have seizures.

  1.  Serotonin Syndrome Risk

With the use of Serotonin and Norepinephrine Reuptake Inhibitor (SNRI) products like tapentadol, a potentially life-threatening serotonin syndrome can happen. This is especially true when serotonergic drugs like SSRIs, SNRIs, tricyclic antidepressants (TCAs), MAOIs, and triptans are taken at the same time, as well as when serotonin metabolism is slowed down by (including MAOIs). This could happen if you take the recommended dose. Serotonin syndrome can cause changes in mental state (like agitation, hallucinations, or coma), autonomic instability (like tachycardia, fluctuating blood pressure, or high body temperature), neuromuscular abnormalities (like hyperreflexia or lack of coordination), and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).

  1. Withdrawal

If tapentadol is stopped suddenly, it could cause withdrawal symptoms. Some of these symptoms are anxiety, sweating, insomnia, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection, and rarely, hallucinations. Tapentadol can be taken less often to lessen withdrawal symptoms [see Drug Abuse and Dependence (9.3)].

  1.  Problems with the liver

In a study of tapentadol, people whose livers didn't work well had higher serum concentrations than people whose livers worked normally. Patients with moderate liver damage should be careful when taking tapentadol. Tapentadol has not been studied in people with severe liver damage, so it is not recommended for use in this group.

  1.  Use in Diseases of the Pancreas or Biliary Tract

Tapentadol, like other mu-opioid agonists, may cause spasm of the sphincter of Oddi. Patients with biliary tract disease, such as acute pancreatitis, should be careful when taking this drug.


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