Tapentadol

Tapentadol

Tapentadol is an opioid analgesic belonging to the benzenoid class of medications. It is a less well-known opioid medication; however, it is a highly effective painkiller with a dual mechanism of action which targets the central nervous system. It is a licenced medication which has been developed for therapeutic purposes and it is available with a prescription in the UK. This medication is sold under several brand names with Palexia and Nucynta being the most popular. If you are unable to get a prescription from your GP, you can buy Tapentadol online from our pharmacy based here in the UK without the need for a prescription!

Note: image for illustrative purposes only - FDA & EMA approved medication sold here.
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Pack of 30 x 50 mg tablets £34.99
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Pack of 180 x 50 mg tablets £172.99

Tapentadol Treatment for Pain

As we briefly mentioned earlier, Tapentadol is an opioid analgesic used for the treatment of moderate to severe, acute and chronic pain. It is also used for pain relief when it is a primary symptom of certain conditions. Acute pain is defined as suddenly occurring short-term pain caused by a specific illness or injury. Examples of this include illnesses such as appendicitis, injuries such a broken bone, or pain after surgery. Acute pain can be useful as it informs your body that something is wrong, for example, if you acquire an illness that needs immediate treatment, you will need a sign strong enough to urge you to seek help. When you are aware of this however, you no longer have a need for this information and pain relief becomes essential. It would be unbearable to experience a broken leg without pain relief after the initial biological mechanisms wear off. Chronic pain is essentially long-lasting pain which is severe enough to warrant therapeutic intervention. Examples of chronic conditions include the following:

  • Diabetic neuropathy - Hyperglycaemia (high blood glucose levels) caused by both type 1 and type 2 diabetes damages nerve cells over time. This damage can affect nerves in different parts of the body, such as nerves which detect the sensation of touch and pain, those which control movement, and nerves which control automatic functions. This results in nerve pain which is similar to that of peripheral neuropathy and fibromyalgia, which are also examples of conditions which can be managed with painkillers.
  • Arthritis - Different types of arthritis exist with the most common being osteoarthritis and rheumatoid arthritis. The former causes the bones around the joints to become brittle and wear away while the latter is an autoimmune disease and causes inflammation. Both types are progressive diseases meaning that it gets worse as time goes on, so pain management will be necessary on a long-term basis.
  • Cancer related pain - This can be either acute or chronic and has a number of factors. Some short-term pain can be due to treatment such as chemotherapy whereas long-term pain can be due to tumours putting pressure on bones or nerves. Cancer is a complex and serious disease, and the management of pain is essential to relieve one aspect, which can also help with the emotional difficulty of dealing with this devastating disease. If or when cancer goes into remission or is cured, the associated pain usually goes away, and medication can be stopped.

Chronic pain isn't limited to physical discomfort, but it can have psychological effects and lead to mental ill health, so managing symptoms is very important.

How Does Tapentadol Work?

The Tapentadol mechanism of action is similar to other opioid based medications targeting opioid receptors in the central nervous system. The central nervous system comprises the brain and spinal cord, and the neurons (nerve cells) connect to the peripheral nervous system throughout the rest of the body. These neurons transmit information from the central nervous system to the peripheral nervous system using electrical signals and this controls all of our functions and perceptions, including the perception of touch and pain. In between each neuron is a tiny gap called a synapse, and this is where the majority of receptors are located. Chemicals called neurotransmitters regulate the electrical activity within the central and peripheral nervous system and medication can cause the production of either stimulatory or inhibitory neurotransmitters. Unlike most other opioids it has a dual mechanism of action, so as well as being an opioid agonist it is also inhibits the reuptake of noradrenaline, making it a potent painkiller. Both mechanisms ensure that there are higher levels of these neurotransmitters in the brain by stimulating the production of opioids and preventing naturally produced noradrenaline from being reabsorbed back into the neuron via the synapse. Opioids reduce the sensation of pain by lowering the transmission of nociceptive (pain) signals thereby increasing your pain threshold. The exact mechanism of action of noradrenaline is unclear, however there have been a significant number of clinical trials which show that it reduces the perception of pain effectively.

How Quickly Does Tapentadol Work?

Tapentadol is rapidly absorbed and has a quick onset of action of just half an hour on average after ingestion, which is useful if your symptoms come on suddenly. It reaches peak plasma concentration after an hour and 15 minutes so this is when it will be most effective. The rate of absorption is slower if the medication is taken with food, however the difference is not significant, and the level of absorption is not affected. Tapentadol bioavailability is surprisingly low at just 32%, which means that 68% is lost in the process of first pass metabolism which occurs as the active ingredient of the medication travels from the gastrointestinal (GI) tract to the neuronal receptors in the brain where it exerts its effects. Despite its low bioavailability, it is a potent medication, and this is partly because it doesn't have to metabolise into morphine within the body to achieve its therapeutic benefits, but rather targets opioid receptors directly. The Tapentadol half-life is 4 hours, and it has a duration of action of 4 to 6 hours. This means that you will feel the effects of the medication for this long before needing to take your next dose, which we will explain in more detail shortly. We sometimes get asked 'does Tapentadol show up on a drug test?' and the short answer to this is yes. As it is an opioid based medication, this is detectable. The elimination half-life is the time it takes for half of the medication to be metabolised and excreted from the body. This means that the medication will be in your body and detectable for at least twice as long as this amount of time.

Dosage Information for Tapentadol

Your Tapentadol dosage routine will depend on the severity of your pain, whether it is acute or chronic, and certain factors such as your sensitivity to medication. Tapentadol 50 mg tablets are often prescribed as a starting dose and the strength can be increased as necessary. For acute intermittent pain you can take your recommended dose when you feel your symptoms are not adequately managed by over-the-counter painkillers. You can take more throughout the day as long as you leave a gap of 4 hours in between each dose. Tapentadol immediate release tablets are the most appropriate form for the treatment of severe acute pain, such as after surgery or a serious accident. This will more than likely need to be taken throughout the day to maintain a consistent level in your system. Tapentadol 100 mg is commonly used to treat moderate to severe chronic pain. Again, the doses need to be spaced evenly throughout the day to ensure that the medication doesn't build up in your system. Snorting Tapentadol or crushing it in any way should never be tried as this will cause the medication to be absorbed far too quickly, potentially resulting in an overdose. A Tapentadol overdose is very dangerous so you should take extra care while you are using this medication.

Does Tapentadol Cause Side Effects?

Before you buy Tapentadol it's a good idea to be aware of the risks as well as the benefits. Side effects are uncommon, but they do occur in some people. Luckily, they are usually mild for those that experience them and resolve on their own after a short period of time. Some of the more common Tapentadol side effects include the following:

  • Drowsiness
  • Dry mouth
  • Nausea
  • Headache
  • Itchiness

You do not need to stop taking the medication if you experience any of the above unless you find them too much and would prefer to. Some people experience more serious side effects, however this is rare. You should discontinue your treatment and seek medical assistance if you experience any of the following:

  • Difficulty breathing
  • Hallucinations or delusions
  • Seizures
  • Anaphylaxis

Should I Take Tapentadol or Tramadol?

The two medications are structurally very similar, however there are some key differences between them. Of the two, Tramadol is a more potent serotonin reuptake inhibitor, which means higher levels of the neurotransmitter serotonin will remain in your system for longer, which helps with pain relief. Tapentadol is a much more potent opioid and does not rely on the need to metabolise into morphine in order to exert its effects. The potency of Tramadol on the other hand relies on genetic disposition as it is metabolised by cytochrome P450 enzymes into its stronger metabolites. The efficacy of these enzymes vary from person to person depending on the individuals genetic coding. If you were to lack the genes that code for the enzymes completely, you would have very little benefit from the medication but still experience the side effects. Tapentadol compared to oxycodone are similar in terms of strength, but the former has fewer side effects which makes it a superior medication. So, even though it less well-known Tapentadol is considered a better medication within the scientific community due to it high efficacy and safety profile and less side effects than other strong opioids.

Who Shouldn't Take Tapentadol?

Although safe for most people over the age of 18, there are some Tapentadol warnings which apply to certain people who should avoid it. You should consult with your GP before taking it if any of the following apply to you:

  • You are allergic to any of the Tapentadol ingredients
  • You have breathing problems
  • You have been treated for addiction
  • You are pregnant or breastfeeding

There are also some Tapentadol drug interactions to be aware of. You should not take the following at the same time:

  • Benzodiazepines
  • Other opioid analgesics
  • Central nervous system depressants

Before You Buy Tapentadol

People are starting to use Tapentadol in the UK more and more because it is so effective. But before you buy Tapentadol or any other opioid based medication, it is important to consider whether this is the best option for you. As it has the potential for physical dependence it should ideally be used as a short-term treatment option. This isn't always possible when it comes to treating chronic conditions and, in these cases, a consistent dosage routine should be maintained. If you have been taking it long-term and need to stop taking it then you should gradually taper off the medication as stopping it abruptly can cause unpleasant withdrawals. Tapentadol withdrawal symptoms include nausea, vomiting, fever, muscular aches and pains, and insomnia.

Where to Buy Tapentadol?

You can get a prescription from your GP, or you can buy Tapentadol online if that is proving difficult. We understand that it is not always possible to get an appointment and that some doctors can be reluctant to prescribe pain medication for longer than 2 or 3 weeks. We believe that you should be able to buy the painkillers you know work for you without the hassle of trying to convince your GP. You can buy Tapentadol and other pain medications at affordable prices, with quick delivery from our online, UK based pharmacy. Visit www.sleepingtabletsdirect.com for our full product range.

Important Information

While this medication may be consumed with or without food, it is not recommended that patients consume it on a completely empty stomach. Likewise, the effects of this medication will be dulled, or seem weaker, if taken on a full stomach, or after eating a heavy meal.

This Medication Should:

  • be consumed in accordance with the patient information leaflet.
  • be swallowed whole; do not crush, chew or suck these tablets / capsules.
  • be stored in a cool dry place / at room temperature (20°C - 25°C).
  • be kept out of the reach of children at all times (minors under the age of 18).

This Medication Should Not

  • be mixed with alcohol - even one drink can be dangerous.
  • be used if pregnant, breastfeeding (or planning to become pregnant).
  • be shared - even with friends or family experiencing symptoms similar to yours.
  • be taken when planning to drive or operate dangerous machinery.

NOTE: If you, or anyone you know, have taken too much of this medication, or if you are experiencing any unwanted side-effects such as a rash, difficulty breathing or swelling of any kind, you should contact a doctor immediately.

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