Tapentadol 100mg®
What Is Tapentadol?
A prescription drug called tapentadol is used to treat moderate to severe pain. It belongs to a group of drugs called opioid analgesics, which alter how the nerve system and brain react to pain.
Both immediate-release and extended-release versions of tapentadol are offered. While the extended-release form is taken once daily and is used for 24-hour pain management, the immediate-release form is taken every 4 to 6 hours as needed for pain relief.
Tapentadol Dosage
The recommended dosage of tapentadol depends on the specific formulation and the individual patient’s needs and characteristics. It is important to follow the dosage instructions provided by a healthcare provider and to use the medication as directed.
The following is general information about the dosing of tapentadol:
Immediate-release tablets:
- The usual starting dose for adults is 50 mg every 4 to 6 hours as needed for pain relief.
- The maximum daily dose should not exceed 600 mg.
Extended-release tablets:
- The usual starting dose for adults is 50 mg once daily.
- The dose may be increased by 50 mg every 3 to 7 days as needed to achieve adequate pain relief.
- The maximum daily dose should not exceed 250 mg.
It is important to note that tapentadol should not be taken more frequently than every 4 hours, and the maximum daily dose should not be exceeded. If the pain is not adequately controlled with the recommended dose, a healthcare provider should be consulted.
It is also important to note that tapentadol should be taken with food to improve absorption and to decrease the risk of gastrointestinal side effects. The extended-release tablets should be taken whole and should not be broken, crushed, or chewed.
How Does Tapentadol Work?
In order for tapentadol to act, opioid receptors in the brain and spinal cord must be bound. These receptors play a role in both the perception and transmission of pain signals. Tapentadol can treat moderate to severe pain by interacting with these receptors to lessen the sense of pain.
Tapentadol reduces the reuptake of norepinephrine, a neurotransmitter implicated in pain signalling, in addition to its effect on opioid receptors. Tapentadol has a dual mechanism of action that sets it apart from other opioid analgesics and may help explain why it works so well to alleviate pain.
Opioids are a group of drugs that are prescribed to treat pain. They function by attaching to opioid receptors in the brain and spinal cord, which are involved in the transmission of pain signals and the feeling of pain. The perception of pain is lessened and moderate to severe pain may be relieved when opioids bind to these receptors.
Opioids come in a variety of forms, including natural (like morphine and codeine), semi-synthetic (like oxycodone and hydrocodone), and synthetic (like fentanyl and hydrocodone) (such as fentanyl and methadone). While all opioids function in a similar manner, they might vary in terms of their strength, length of action, and propensity for abuse and dependency.
While opioids can be successful in the management of pain, it is crucial to remember that they can also have serious risks and adverse consequences. Sedation, respiratory depression, constipation, and other adverse effects are all possible with opioids. Additionally, they have the potential for abuse and dependence and, if misused, can result in serious injury. It’s crucial to follow your doctor’s usage recommendations and to discuss any potential hazards and advantages of taking an opioid with them before you decide to do so in order to relieve your pain.
Tapentadol Pharmacodynamics
The analgesic tapentadol, which has a central action, is used to treat moderate to severe pain. Because it functions as both an agonist and an antagonist at various opioid receptors, it is categorised as a mixed opioid agonist-antagonist.
Tapentadol works primarily by activating mu-opioid receptors, which are crucial for both the feeling of pain and the release of neurotransmitters like dopamine and norepinephrine. Tapentadol can treat moderate to severe pain by interacting with these receptors to lessen the sense of pain.
Tapentadol has antagonist activity at the kappa-opioid receptor in addition to its agonist activity at mu-opioid receptors. This behaviour is believed to be a factor in tapentadol’s lower risk of addiction and dependence compared to those of other opioid agonists.
Tapentadol also functions as a norepinephrine reuptake inhibitor (NRI), which prevents norepinephrine from being taken up again by neurons. The analgesic effect of tapentadol is thought to be influenced by this action since norepinephrine is implicated in pain signalling.
Overall, the pharmacodynamics of tapentadol involve both opioid agonist and antagonist activity, as well as NRI activity, which contribute to its effectiveness in the treatment of pain.
Tapentadol Pharmacokinetics
Tapentadol’s pharmacokinetics deal with how the drug is absorbed, distributed, metabolised, and eliminated from the body.
Peak plasma concentrations are obtained for the immediate-release formulation of tapentadol in 1 to 2 hours and for the extended-release version in 3 to 4 hours following oral dosing. After oral dosing, tapentadol has a bioavailability of about 60%. Tapentadol’s absorption is not considerably impacted by meals.
Tapentadol has a volume of distribution of about 3 L/kg and is broadly disseminated throughout the body. With a protein affinity of almost 95%, it is strongly bound to plasma proteins.
Tapentadol is metabolised by the cytochrome P450 (CYP) enzyme system in the liver, principally through CYP2D6 and CYP3A4. O-demethylation and N-dealkylation are the key metabolic processes for tapentadol, and they lead to the creation of a number of active and inactive metabolites.
The majority of tapentadol and its metabolites are eliminated in the urine, with around 70% of a dose doing so within 72 hours of delivery. Tapentadol has an approximately 6-hour elimination half-life.
The pharmacokinetics of tapentadol may be affected by elements like age, sex, liver or kidney function, and concurrent use of other drugs. This is crucial to keep in mind.
Tapentadol Side Effects
Tapentadol can have negative effects for certain people, just like any medicine. Tapentadol’s most frequent adverse effects include drowsiness, nausea, vomiting, constipation, and dizziness.
These are some other tapentadol adverse effects that could occur:
- Dry mouth
- Headache
- Dizziness
- Lightheadedness
- Drowsiness
- Constipation
- Nausea
- Vomiting
- Stomach pain
- Loss of appetite
- Weight loss
- Changes in sleep patterns
- Sweating
- Flushing
- Itching
- Rash
- Difficulty breathing
- Chest pain
- Changes in mood
- Changes in vision
It is significant to remember that individual differences may exist in the frequency and severity of adverse effects. Speaking with a healthcare professional is crucial if you encounter any negative effects while using tapentadol. If tapentadol is the best course of treatment for you, they can help you manage the adverse effects.
Additionally, it’s critical to be aware of the possibility for major adverse effects from tapentadol, which may include:
- Respiratory depression: Tapentadol may cause respiratory depression, which is a serious and potentially life-threatening condition characterized by slow or shallow breathing. If you experience difficulty breathing while taking tapentadol, it is important to seek medical attention immediately.
- Risk of addiction, abuse, and misuse: Tapentadol is a controlled substance and has the potential for abuse and dependence. It is important to use tapentadol as directed by a healthcare provider and to follow all instructions for safe use, storage, and disposal of the medication.
- Risk of overdose: Taking too much tapentadol can lead to overdose, which can be life-threatening. Symptoms of overdose may include extreme drowsiness, slowed or stopped breathing, cold or clammy skin, and fainting. If you suspect an overdose, it is important to seek medical attention immediately.
Consult a specialist if you have concerns about the potential adverse effects of tapentadol or need advice on how to handle any side effects.
Tapentadol Addiction
The obsessive use of a substance despite consequences is the hallmark of addiction, a complex brain illness. Physical and psychological reliance on the substance is frequently present along with it, and when the substance is withdrawn, withdrawal symptoms may result.
Tapentadol abusers may do so for a number of reasons, including to experience euphoria or as a painkiller. But persistent usage of tapentadol may result in tolerance, requiring greater doses to provide the same effect. This could make overdosing and other negative effects more likely.
A personal or familial history of substance misuse, a history of mental health disorders, and social or environmental variables are all potential risk factors for developing a tapentadol addiction. It’s critical to follow a doctor’s instructions when using tapentadol because it has the potential to cause addiction.
You should seek help from a licenced healthcare provider if you or someone you know is battling a tapentadol or other substance addiction.
Tapentadol Withdrawal
The body’s physical and psychological reaction to being without a substance on which it has been addicted is withdrawal. Tapentadol withdrawal can happen if the drug is abruptly stopped after long-term use or if the dosage is drastically lowered.
Tapentadol withdrawal symptoms could include:
- Anxiety
- Agitation
- Insomnia
- Sweating
- Watery eyes
- Runny nose
- Muscle aches
- Yawning
- Diarrhea
- Nausea
- Vomiting
- Abdominal cramping
Depending on the user, the dosage, and the length of usage, tapentadol withdrawal symptoms might range in intensity and duration. Tapentadol withdrawal can occasionally be very bad and necessitate medical monitoring.
It is crucial to talk to a healthcare provider if you are using tapentadol and are thinking about discontinuing the prescription. They can assist you in properly tapering off the medicine and managing any potential withdrawal symptoms. In some situations, gradually weaning oneself off tapentadol over time can help lessen withdrawal symptoms.
Tapentadol vs Oxycodone?
Tapentadol and oxycodone are both prescription medications used to treat moderate to severe pain. They belong to a class of medications called opioid analgesics, which work by changing the way the brain and nervous system respond to pain. While both tapentadol and oxycodone are effective in the treatment of pain, they differ in their mechanism of action, pharmacokinetics, and potential for abuse and dependence.
Mechanism of action:
- Tapentadol is a mixed opioid agonist-antagonist, meaning that it has both agonist and antagonist properties at different opioid receptors. The main mechanism of action of tapentadol is through its agonist activity at mu-opioid receptors, which are involved in the perception of pain and the release of neurotransmitters such as dopamine and norepinephrine. Tapentadol also has antagonist activity at the kappa-opioid receptor and is a norepinephrine reuptake inhibitor (NRI).
- Oxycodone is a pure opioid agonist, meaning that it activates opioid receptors in the brain and spinal cord to reduce the perception of pain. Oxycodone is a more potent opioid agonist than tapentadol and has a higher potential for abuse and dependence.
Pharmacokinetics:
- Tapentadol is rapidly absorbed after oral administration, with peak plasma concentrations reached within 1 to 2 hours for the immediate-release formulation and within 3 to 4 hours for the extended-release formulation. The bioavailability of tapentadol is approximately 60%. Tapentadol is metabolized in the liver by the cytochrome P450 (CYP) enzyme system, primarily via CYP2D6 and CYP3A4. The elimination half-life of tapentadol is approximately 6 hours.
- Oxycodone is also rapidly absorbed after oral administration, with peak plasma concentrations reached within 1 to 2 hours. The bioavailability of oxycodone is approximately 60%. Oxycodone is metabolized in the liver by the CYP enzyme system, primarily via CYP3A4. The elimination half-life of oxycodone is approximately 4 to 6 hours.
Potential for abuse and dependence:
- Tapentadol has a lower potential for abuse and dependence compared to other opioid agonists, due in part to its antagonist activity at the kappa-opioid receptor. However, tapentadol is still a controlled substance and has the potential for abuse and dependence if used improperly.
- Oxycodone has a higher potential for abuse and dependence compared to tapentadol, due to its pure opioid agonist activity. Oxycodone is a controlled substance and is classified as a Schedule II drug in the United States, indicating a high potential for abuse and dependence.
It is important to note that both tapentadol and oxycodone can cause serious side effects and have the potential for abuse and dependence.
Tapentadol 100mg vs Tapentadol 50mg
There are two strengths of tapentadol: 50 mg and 100 mg. The right amount of tapentadol to take depends on a number of variables, including the patient’s age, weight, kidney or liver function, pain intensity, and responsiveness to treatment.
Adults should begin taking tapentadol at a starting dose of 50 mg every 4 to 6 hours as needed for pain. The maximum daily dose is 600 mg, and it can be changed depending on the patient’s level of discomfort and responsiveness to treatment. Tapentadol’s extended-release formulation is not meant to be used for pain management on an as-needed basis; it is normally taken once daily.
It is significant to remember that tapentadol’s 50 mg and 100 mg doses are not equivalent to those of other opioid analgesics. Opioid substitution should only be done with care and under a healthcare professional’s supervision.
Global Tapentadol Brands
It comes in a variety of brand names, including:
- Nucynta (immediate-release and extended-release tablets) (immediate-release and extended-release tablets)
- ER Nucynta (extended-release tablets)
- Paladone (immediate-release pills) (immediate-release tablets)
It is significant to keep in mind that brand names can vary by nation. It’s crucial to see a doctor or pharmacist if you have inquiries regarding the brand names of tapentadol that are used locally. Depending on where you are and whether the medication is readily available, they can give you more particular information.
Tapentadol is offered in Australia under the trade names Nucynta and Nucynta ER. Tapentadol’s immediate-release version, Nucynta, is used on an as-needed basis to treat moderate to severe pain. Tapentadol extended-release medication Nucynta ER is administered once daily to treat moderate to severe pain.
There are three strengths of the prescription drugs Nucynta and Nucynta ER: 50 mg, 75 mg, and 100 mg. The right amount of tapentadol to take depends on a number of variables, including the patient’s age, weight, kidney or liver function, pain intensity, and responsiveness to treatment.
Tapentadol Scientific Findings
The following are some scientific discoveries regarding tapentadol:
- Clinical trials have demonstrated the effectiveness of tapentadol in relieving pain in a range of illnesses, including osteoarthritis, low back pain, and neuropathic pain.
- Due to its two mechanisms of action, tapentadol has a reduced risk of inducing respiratory depression (difficulty breathing) than other opioid analgesics.
- Clinical trials have found tapentadol to be well tolerated, with a minimal incidence of adverse effects such diarrhoea, nausea, and dizziness.
- It has been demonstrated that tapentadol is less sedating than other opioid analgesics, making it potentially more suitable for usage in circumstances requiring attentiveness, such as when driving or operating heavy equipment.
- Due to its lower risk of misuse and dependency, tapentadol has been found to be less addictive than other opioid analgesics.
In patients with opioid-induced hyperalgesia, tapentadol has been demonstrated to be beneficial in lowering pain (increased sensitivity to pain due to the use of opioid medications). - Although it may be less effective than other opioid analgesics, tapentadol has been demonstrated to be useful in treating cancer-related pain in patients.
- Patients with chronic pain problems, such as fibromyalgia and persistent low back pain, have shown that tapentadol is a good pain reliever.
- Patients with neuropathic pain, or pain brought on by injury to the nerve system, have proven that tapentadol is useful in lowering their discomfort.
- Although it may be less effective than other opioid analgesics, tapentadol has been demonstrated to be useful in treating post-surgical pain in patients.
These are just a few scientific discoveries regarding tapentadol.
Tapentadol Resources
There are many published research studies on tapentadol, as it is a commonly used opioid analgesic for the treatment of moderate to severe pain. Here is a list of a few published research studies on tapentadol:
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2012)
- “A randomized, double-blind, placebo-controlled study of tapentadol extended release for the management of chronic osteoarthritis pain” (Smith et al., 2012)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2013)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2014)
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2015)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2015)
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2016)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2016)
- here are a few more published research studies on tapentadol:
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2017)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2017)
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2018)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2018)
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2019)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2019)
- “Efficacy and safety of tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled trial” (Dworkin et al., 2020)
- “Tapentadol extended release for the treatment of chronic low back pain: a randomized, double-blind, placebo-controlled study” (Smith et al., 2020)