Tramadol: A Synthetic Opioid Analysis

Tramadol is a synthetic opioid analgesic used to relief pain. It is an odorless powder, which is white, bitter, and crystalline in shape and it is readily soluble in water and ethanol. The molecular formula of tramadol is C16 H25 NO2 . HCl and figure 1 shows the chemical structure of tramadol. In the 1960s, Grünenthal GmbH developed tramadol. It has an analgesic potency that is about one tenth of that of morphine. In addition to its pain relieving properties, it has anti-depressive and anxiolytic properties (Kusari ,S., etall,2015). Tramadol 's metabolism occurs in the liver by demethylation, which is mediated by CYP3A4 and CYP2B6, glucuronidation, and sulfation. Metabolism of tramadol via CYP2D6 result in the generation of an active metabolite

The label use of tramadol is for the management of moderate to severe pain. For example, it is used for the treatment of dental pain after an oral surgery, such as extraction of impacted molars. In addition, tramadol is used for chronic conditions, such as cancer related pain, low-back pain and bone pain. The extended release formulations of tramadol, such as Ultram ER, are indicated for the treatment of moderate to severe persistent pain. They are used in adults that have the need of around-the clock treatment of pain for prolonged period of time. The reason for the use of once-daily tramadol ER is that it results in less frequent fluctuations in plasma concentrations than the equivalent daily doses of short-acting tramadol. Moreover, tramadol is used in the management of postoperative pain. The off-label indications of tramadol include its use as an adjuvant in the treatment of arthralgia associated with osteoarthritis and treatment of postherpetic neuralgia (Clinical Pharmacology,

There is an extended release formulation of tramadol used to treat persistent severe pain. In addition, it is hepatically metabolized and is converted to an active metabolite. Tramadol has a weak opioid property at μ-opioid receptors and monoaminergic activity. Moreover, tramadol is generally well endured, however, it has side effects such as insomnia, drowsiness, dizziness, headache, central nervous system stimulation. To add, Tramadol can stop or slow breathing when starting using this drug or changing its dose. Dependence can occur even within the normal doses of tramadol. There are numerous drug interactions with tramadol, for example, CNS depressant effect of alcohol are enhanced when used with tramadol. Furthermore, serotonin syndrome can result from the use of monoamine oxidase inhibitors with tramadol as they increase the serotonergic effect of tramadol. Moreover, it is contraindicated in people who have experienced hypersensitivity to tramadol, or opioid analgesics and during monoamine oxidase inhibitor