Functional Medicine for Life, Tapentadol

• Tapentadol (Nucynta among others) is an acting opioid analgesic of the benzenoid class. It is a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor. Analgesia occurs within 32 minutes of oral administration, and lasts for 4–6 hours. It is like tramadol in its dual mechanism of action. Unlike tramadol, it has only weak effects on the reuptake of serotonin. Tapentadol is a more potent opioid with no known active metabolite. Not a pro-drug and so does not rely on metabolism to produce its therapeutic effects. This makes it a useful moderate-potency analgesic option for patients. Who do not respond to more used opioids due to genetic disposition. As well as providing a more consistent dosage-response range among the patient population. The potency of tapentadol is somewhere between that of tramadol and morphine. With an analgesic efficacy comparable to oxycodone despite lower side effects. It is generally regarded as a strong opioid. In India, Central Drug Standard Control Organisation (CDSCO) approved tapentadol immediate-release (IR). Preparations (50, 75 and 100 mg) for moderate to severe acute pain Extended-release (ER) preparations 50,100,150 and 200 mg. It is for severe acute pain in April 2011 and December 2013.

• Medical use

• Tapentadol used for the treatment of moderate to severe pain. For both acute (following injury, surgery, etc.) and chronic musculoskeletal pain. It is also indicated for controlling the pain of diabetic neuropathy. When around-the-clock opioid medication is required. Extended-release formulations of tapentadol are not indicated for management of acute pain. Tapentadol is Pregnancy Category C. There are no adequate and well-controlled studies of tapentadol in pregnant women. Tapentadol is not recommended for use in women before labour and delivery. There are no adequate and well-controlled studies of tapentadol in children.

• Adverse effects

• The most reported side effects of tapentadol therapy in clinical trials: Nausea, vomiting, dizziness, sleepiness, itchiness, dry mouth, headache, and fatigue. Although early preclinical animal trials suggested. Tapentadol has a reduced abuse liability compared to other opioid analgesics the US DEA. The same category as stronger opioids more used (morphine, oxycodone, and fentanyl) Tapentadol has been demonstrated to reduce the seizure threshold in patients. Tapentadol should be used in patients with a history of seizures. And in patients who are also taking one or more other drugs. Which have also demonstrated to reduce the seizure threshold. Patients at high risk include those using other serotonergic and adrenergic medications. As well as patients with head trauma, metabolic disorders. And those in alcohol and/or drug withdrawals. Tapentadol has been demonstrated to produce hypotension (low blood pressure). It should be used with caution in patients with low blood pressure. Patients who are taking one or more medications are also known to reduce blood pressure.

• Interactions

• Combination with SSRIs/SNRIs, SRAs, serotonin receptor agonists may lead to lethal serotonin syndrome. Combination with MAOIs may also result in an adrenergic storm. Use of tapentadol with alcohol results in increased impairment, sedation, respiratory depression, and death. Tapentadol is metabolise the hepatic enzymes (CYP2C9, CYP2C19, and CYP2D6) It has interactions with drugs. It enhances or represses the activity/expression of one or more of these enzymes. It works well with substrates of these enzymes (due to competition for the enzyme). Some enzyme mediators/substrates need dosing adjustments to one or both medications. The combination of tapentadol and alcohol may result in increased plasma tapentadol concentrations. It produces respiratory depression to a degree greater than the sum of the two drugs. When administered, patients should be cautioned against alcohol consumption. When taking tapentadol the combination may be fatal. Don’t forget to store tapentadol in a closed place in a cool temperature. Protect this medicine from direct sun exposure, and keep it out of reach of children.