Introduction
Tapentadol is an analgesic medication used to manage moderate to severe pain. Not being a pro-drug, the medication is readily absorbed without relying on metabolic enzymes. Tapentadol is a moderately strong opioid that has been FDA-approved and MHRA-approved for pain conditions. It is available in tablet and injection form in immediate-release and extended-release formulations.
Working
Tapentadol is a centrally acting analgesic with a dual mechanism of action, combining mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule.
Analgesic equivalence with Tapentadol is achieved with lower opioid receptor activity than other opioids, making it a safer and tolerable option. Noradrenaline reuptake of the drug works on the sympathetic nerves and provides intrinsic relief from pain. The noradrenergic component of Tapentadol interacts with the opioid component, and both synergistically contribute to the analgesic effect of the substance.
Strength and doses
Tapentadol is available in strengths of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, and 250 mg, of which Tapentadol 100 mg is the most commonly used dose. Tapentadol dosage varies in each patient and depends on the.
- Pain condition for which they have advised the drug
- Intensity of pain
- The treatment plan of the surgeon
- Presence of systemic conditions
- Age of the patient
For immediate release formulations of the medication, an initial dose of 50 mg to 100 mg orally is advised every four to six hours for pain with subsequent dosing of 50, 75, or 100 mg orally every 4 to 6 hours, taking care not to exceed the Tapentadol maximum dose beyond 700 mg on the first day and 600 mg on subsequent days.
For extended release formulations, an initial dose of 50 mg is advised orally twice a day and individually titrated to a dose that provides adequate analgesia and minimizes adverse reactions. Take care to stay within the dose of 50 mg twice daily every three days.
In hepatic conditions, renal conditions, and elderly patients, the dose is modulated for patient safety.
Onset
Tapentadol immediate release tablets have an onset period of 32 minutes and attain peak plasma concentrations within 1-2 hours of use. Tapentadol has a half-life of 3.93 hours and provides effective analgesic activity for 4-6 hours. The drug stays in the body for around 22 hours till the completion of its half-lives, after which it is eliminated through metabolic wastes. Factors like age, food intake, and drug interactions can affect the absorption and, subsequently, the onset and analgesic effect of the drug.
Tapentadol extended-release has a 12-hour duration of effect and is useful in patients with chronic osteoarthritis, low back pain, and pain associated with diabetic peripheral neuropathy.
How to use
To use Tapentadol correctly –
- Swallow the drug instead of breaking or powdering it.
- Start on a low dose of the medication and gradually increase the dose taking into consideration your tolerance to the medication.
- Do not exceed 700 mg dose on the first day of use and 600 mg dose on the subsequent days.
- Avoid the use of heavy meals, grape juice, caffeinated beverages, and alcoholic beverages with Tapentadol.
- Do Not overdose on the medication to make up for a missed dose.
Side effects
- Mild side effects -:Â itching, increasing sweating, nausea, indigestion, dry mouth, decreased appetite, and feeling of body temperature change.
- Moderate side effects -:Â somnolence, fatigue, muscle fatigue, feeling of weakness, rashes, sleeping problems, flushing.
- Severe side effects -:Â hallucinations, anxiety, confusion, abnormal dreams.
Usually, Tapentadol-associated side effects are of a mild to moderate nature and reverse after a while. On observing recurrent Tapentadol side effects or increased intensity of the effects, discontinue the medication and get urgent medical attention.
Drug interactions
Tapentadol with antipsychoticsÂ
Antipsychotics like duloxetine, venlafaxine, escitalopram, and desvenlafaxine, when used concomitantly with Tapentadole, can increase the risk of serotonin syndrome leading to symptoms of confusion, hallucination, seizure, extreme changes in blood pressure.
Tapentadol with anticonvulsants
Anticonvulsants like Pregabalin, when used simultaneously with Tapentadol, can lead to side effects of respiratory distress, coma, and even death of the individual.
Tapentadol with narcotic analgesics
Narcotic analgesics like Naloxone and Oxycodone can increase the plasma concentrations of the drug in the blood and lead to overdose symptoms of dizziness, confusion, and impaired motor function.
Tapentadol with anxiolytics and anti convulsants
Medications like Diazepam and Alprazolam, combined with Tapentadol, can lead to respiratory depression and result in life-threatening complications in the patient.
Precautions
- Do not drive or operate heavy machinery while using the medication.
- Don’t use it in pregnant or breastfeeding conditions.
- Use the medication cautiously if you have a history of alcohol abuse or benzo addiction.
- Don’t use it for an extended time, as the drug has addiction potential and may lead to withdrawal symptoms.
FAQs
What is Tapentadol?
Tapentadol is a potent analgesic medication used to treat moderate to severe pain. Studies have shown that 3.3 mg of oral Tapentandol is equivalent to 1 mg of oral morphine equivalence in both opioid naive and tolerant patients, with a safer user profile because of its unique opioid-binding properties. Additionally, the dual mechanism of action of the medication makes it a suitable option for a wide range of analgesic functions, including chronic pain, nociceptive pain, and intrinsic pain conditions.
Where to buy Tapentadol in the UK?
Tapentadol is available under the brand name Palexia in the UK and is a prescription-only medication. You need a prescription confirming your pain diagnosis and advising your use of the medication to obtain the drug from pharmacies dealing with Tapentadol and its derivatives. You can even order the medication and its refills from selected physician’s clinics licensed to dispense Tapentadol outside pharmacies.
Can you order Tapentadol online?
You can order Tapentadol online in the UK from online portals licensed to dispense you the generic versions of the medication. Online ordering enables you to obtain the drug quickly and easily with added discounts from the websites. Before ordering, ensure it is a genuine portal that will help you obtain authentic versions of the drug. Confirm your allergy status regarding the drug and ensure the medication is well within its expiry period.
Does Tapentadol cause weight gain?
Studies have shown that the use of Tapentadol, especially in those above 60 years of age who have been using the medication for over six months, has resulted in weight gain over a particular time. Males have been observed to be more prone to increased weight than females to the use of Tapentadol.
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