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It is a drug that activates mu-opioid receptors and modulates the uptake of norepinephrine, a neurochemical messenger pathway which plays a role in pain modulation. In addition to its potential to lower pain, the actions of Tapentadol are known to have an effect on respiration, mental state, consciousness, bowel movement, and physical dependence.

Since opioids have differential actions among people, the same medicine will have differential efficacy and side effects depending on the individual. Diagnosis, age, organ dysfunction, medication use, history of substance abuse, sleep disorders, and respiratory issues as well as previous exposure to opioids are some factors influencing prescription.

There are immediate-release and extended-release formulations of Tapentadol, each of them having different time course of delivery of active ingredients. Immediate-release formulation can be used for acute pain management while extended-release formulation may be appropriate for the treatment of selected patients with chronic pain requiring continuous treatment with opioids.

They cannot be interchanged with each other. Extended-release drugs have special handling and prescription requirements since modification of such drugs increases the likelihood of overdose and respiratory depression.

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