Tramadol

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It may be sold in combination with paracetamol (acetaminophen) or as longer-acting formulations. Common side effects include constipation, itchiness, and nausea. Serious side effects may include seizures, increased risk of serotonin syndrome, decreased alertness, and drug addiction. A change in dosage may be recommended in those with kidney or liver problems. It is not recommended in those who are at risk of suicide or in those who are pregnant. While not recommended in women who are breastfeeding, those who take a single dose should not generally stop breastfeeding. Tramadol acts by binding to μ-opioid receptors on neurons. It is also a serotonin–norepinephrine reuptake inhibitor (SNRI). It is converted in the liver to O-desmethyltramadol, an opioid with stronger binding to the μ-opioid receptor. Tramadol was patented in 1963 and launched under the name 'Tramal' in 1977 by the West German pharmaceutical company Grünenthal GmbH. In the mid-1990s, it was approved in the United Kingdom and the United States. It is available as a generic medication and marketed under many brand names worldwide. In the United States, the wholesale cost is less than US$0.05 per dose as of 2018. In 2016, it was the 39th most prescribed medication in the United States, with more than 19 million prescriptions. Tramadol is used primarily to treat mild to severe pain, both acute and chronic. Its analgesic effects take about one hour to come into effect and 2 to 4 h to peak after oral administration with an immediate-release formulation. On a dose-by-dose basis, tramadol has about one-tenth the potency of morphine and is practically equally potent when compared with pethidine and codeine. For pain moderate in severity, its effectiveness is equivalent to that of morphine; for severe pain it is less effective than morphine. These painkilling effects last about 6 h. Available dosage forms include liquids, syrups, drops, elixirs, effervescent tablets and powders for mixing with water, capsules, tablets including extended-release formulations, suppositories, compounding powder, and injections.