Tapentadol, with a half-life of 4 hours, stays in the system for approximately 20 to 22 hours. The half-life of a medication is the time it takes for half of the drug to be removed from the body.
On the other hand, Tapentadol Extended-Release(ER) lasts in the system for about 1.23 days. The ER formulation provides sustained drug release over an extended period, making it last longer.
The FDA approves Tapentadol, an opioid analgesic, for managing severe chronic pain. It is available under the brand names Palexia, Nucynta, and Aspadol. The use of Tapentadol for fibromyalgia, post-surgical pain, and diabetic neuropathic pain is also clinically approved.
The Drug Enforcement Administration has classified Tapentadol as a Schedule II controlled substance. It indicates that the analgesic has a high potential for abuse and dependency.
Therefore, patients taking Tapentadol or its brands might wonder how long Tapentadol stays in the system.
Understanding the duration is crucial for both patients and healthcare providers. For patients, knowing how long the medication stays active can help manage pain, avoid potential overdoses or adverse effects, and adhere to dosing schedules. This information helps healthcare providers manage dosages, effective treatment, and potential drug interactions.
Understanding Tapentadol Metabolism
After administration, tapentadol is readily absorbed in the body. It undergoes comprehensive metabolism in the liver to form metabolites or inactive compounds.
Tapentadol metabolism primarily occurs in two phases: phase I and phase II.
Phase I Metabolism
Tapentadol is metabolized by enzymes such as CYP2C9, CYP2C19, and CYP2D6. The metabolites formed in this phase are N-desmethyl tapentadol and hydroxyl tapentadol.
Phase II metabolism
Tapentadol and its phase I metabolites undergo conjugation with glucuronic acid. This process produces glucuronides, with tapentadol-O-glucuronide being the major metabolite formed. These glucuronides are inactive and are eventually excreted from the body via the kidneys.
Excretion
The metabolites of Tapentadol are primarily eliminated through the kidney, and a small portion is eliminated through feces.
It should be noted here that several factors can affect metabolism, including kidney and liver functions, genetics, concurrent medications, age, and gender.
Tapentadol Half-Life
The half-life of a medicine is the time it takes for half of the drug to be eliminated from the body. This duration provides information on how long a medication remains in the system.
The half-life of Tapentadol is approximately 3.93 hours [1].
This duration is also crucial in determining dose adjustments, the dosage gap and frequency of Tapentadol to maintain the analgesic effect.
How Long Does Tapentadol Stay In Your System?- A Theoretical Evaluation
The standard dose of Palexia, Nucynta, or Aspadol is 100 mg. So, let us consider when a 100mg dosage was initially taken as a "zero" hour. Taking the half-life of Tapentadol into consideration, here is a breakdown of how long it takes for the body to completely eliminate Tapentadol.
|
Tapentadol level Remaining |
Time |
|---|---|
|
100% |
00 hrs |
|
50% |
3.93 hrs |
|
25% |
7.86 hrs |
|
12.50% |
11.79 hrs |
|
6.25% |
15.72 hrs |
|
3.13% |
19.65 hrs |
Based on the medication's half-life and our calculation, Tapentadol stays in your body for about 20 to 22 hours. However, it may differ based on numerous health factors.
Based on the same calculation, with a half-life of 4.4 to 5.9 hours, Tapentadol ER stays in the system for 1.23 days, as shown in the table below.
|
Tapentadol ER level Remaining |
Time |
|---|---|
|
100% |
00 hrs |
|
50% |
5.90 hrs |
|
25% |
11.80 hrs |
|
12.50% |
17.70 hrs |
|
6.25% |
23.60 hrs |
|
3.13% |
1.23 days |
Factors Influencing The Elimination Time
The factors influencing the elimination of Tapentadol are listed below-
Dosage And Frequency of Use-
The intake of a higher or more frequent dose can result in drug accumulation. In such cases, it takes longer to eliminate them from the body. A higher dose of the drug can also affect the metabolic process. Hence, it slows the elimination rate and prolongs its detectability in drug screenings.
Metabolic rate-
As mentioned earlier, Tapentadol is metabolized in the liver like most medications.
People with a faster metabolic rate eliminate Tapentadol quickly, thus lowering the detectability window. People with a liver disorder or slower metabolism take longer to break down the drug, making Tapentadol stay longer in the system.
Individual Physiology-
A few biological characteristics may contribute to determining how long Tapentadol stays in the system, including organ functioning, body mass, age, and hydration level.
People with higher body mass store the drug in fat molecules that act as reservoirs. It gradually releases the drug into the bloodstream and prolongs the effect.
Liver function declines with age; a thirty percent (30%) reduction is seen in older adults. It slows metabolic activity, thus taking longer to eliminate Tapentadol.
Drug Interactions-
Tapentadol can interact with other medications to alter its efficacy and increase the risk of side effects.
Moreover, Tapentadol interaction with other drugs or substances can alter its metabolic and clearance rate. In such cases, it increases or slows down the drug elimination process.
Will Tapentadol Show Up On A Drug Test?
Based on the type of drug test and the last dose taken, its presence may be detected in the body.
Specific drug tests can detect Tapentadol through blood, hair, urine, and saliva samples.
Tapentadol Urine Drug Screen-
Tapentadol can be detected in the urine for 3 to 4 days from the last dose administered [2]. It may, however, last for a longer period in people with renal (kidney) disorders.
Elimination Timeline of Tapentadol From Hair-
Tapentadol can be detected in the hair follicle for up to 30 days.
Detection in Saliva-
The detection time of Tapentadol in the saliva is around 5 to 6 hours.
Blood Test-
Tapentadol can be detected in the blood for about 24 to 48 hours after the last dose is administered.
Tapentadol Withdrawal And Safety Considerations
Tapentadol dosage should be taken as per the prescribed instructions. Doing so will help avoid the risks of side effects and help manage pain effectively.
Long-term use of Tapentadol can increase the risks of developing tolerance, dependence, and addiction.
Tapentadol analgesics should not be discontinued abruptly. It can cause symptoms of withdrawal like anxiety, insomnia, nausea, sweating, and muscle aches. The Tapentadol withdrawal timeline can vary from person to person and can last for up to a few days. To minimise the risks, tapering off or slowly decreasing the dose is recommended.
Author Note for Readers:
All the information and facts stated are checked in the drug database and are accurate based on pharmacological properties.