I wanted to write a little bit about tramadol, which also goes by the brand name Ultram. I use this medication fairly often, and wanted to give some insight on its use.
It’s a centrally acting analgesic which is not considered to be a true opioid. It works in two ways:
1. Binds to the mu opioid receptor
2. Inhibits the re-uptake of serotonin and norepinephrine
The medication is a racemic mixture. The positive enantiomer binds to the mu receptor and the negative enantiomer prevents the re-uptake of norepinephrine. After ingestion, the active metabolite is O-desmethyltramadol – which has a a higher affinity to the mu opioid receptor.
It is structurally similar to codeine and morphine, however, this was not considered to be a scheduled substance until very recently. Starting August 18th, 2014, the DEA has placed tramadol as a schedule IV drug.
Whether tramadol has abuse potential and/or is associated with addiction has been up for debate. They have decided to go ahead and make this a scheduled drug because it has long been considered a “loop hole drug which is addictive, abused, and diverted.”
Indications for its use are to treat moderate to severe pain. Immediate release typically takes one hour to take effect, 3 hours to reach its peak, and lasts for about 6 hours. It has about 1/10th the potency of morphine and is equal in potency to codeine.
The max daily amount is 400mg/day and doses over this can be toxic leading to seizure and CNS excitation – careful with serotonin syndrome! Also, be aware that the seizure threshold can be lowered even with the recommended doses. There is less of a risk of respiratory depression and/or constipation when compared to traditional opioids.
Usually, patients are prescribed 50mg-100mg every 6 hours as needed for pain. The extended release form is usually given round the clock for the management of chronic pain and is not usually given on an as needed basis. There also seems to be a synergistic effect when tramadol is combined with acetaminophen. Patients with a creatine clearance less than 30mL/min should be placed on twice a day dosing with a maximum dose of 200mg/day.
It is a considered to be a category C in pregnancy and should not be used first line in the management of pain. Acetaminophen is always the preferred agent to treat pain during pregnancy. Tramadol should definitely be avoided in nursing mothers as this will pass into the breast milk.
Tramadol is a good alternative to traditional opioids for the treatment of moderate to severe pain. Like with anything else, there are possible adverse reactions, especially with incorrect use. Although it has traditionally been thought of as being a safer alternative when compared to traditional opioids, there are still consequences if not taken as directed.