What is Tramadol?
Tramadol hydrochloride (trademarked as Conzip, Ryzolt, Ultracet, Ultram in the USA, Ralivia, Zytram XL Durella{CR-100/200 mg} in Canada or Adolonta in Spain) is a centrally acting synthetic analgesic used to treat moderate to moderately severe pain. The drug has a wide range of applications, including treatment of rheumatoid arthritis, restless legs syndrome, motor neurone disease and fibromyalgia. It was launched and marketed as Tramal by the German pharmaceutical company Grünenthal GmbH in 1977.
Tramadol is a weak receptor agonist and is a reuptake inhibitor of serotonin and of norepinephrine. Tramadol is metabolized to O-desmethyltramadol, a significantly more potent opioid agonist. Tramadol and its major metabolite(s) are distinguished from other more potent opioid agonists by relative selectivity for opioid receptors.
Availability and usage
100mg tramadol injection, marketed by the original 'Contramal' trade-mark owner, Grünenthal GmbH (Hungarian release).
50 mg Tramadol HCl tablets (generic Ultram) marketed by Akyma Pharmaceuticals. Immediate release tramadol HCl is available in many generic preparations.
Bottle of 30 tablets of 200 mg extended-release tramadol HCl (generic Ultram ER) marketed by Patriot. Extended-release tramadol is commonly available in 100, 200, and 300 mg strengths to be taken once daily. It is often prescribed with tramadol-APAP (Ultracet) or regular immediate-release tramadol HCl (Ultram/Tramal/Rybix) for breakthrough pain.
Tramadol HCl for injection
Tramadol is classified as a central nervous system drug usually marketed as the hydrochloride salt (tramadol hydrochloride); the tartrate is seen on rare occasions, and rarely (in the US at least) tramadol is available for both injection (intravenous and/or intramuscular) and oral administration. The most well known dosing unit is the 50 mg generic tablet made by several manufacturers. It is also commonly available in conjunction with APAP (paracetamol, acetaminophen) as Ultracet or Tramacet, in the form of a smaller dose of 37.5 mg tramadol and 325 mg of APAP.
Tramadol is not a federally controlled drug, however the following U.S. states have elected to make tramadol a schedule IV controlled drug: Arkansas, Tennessee, Illinois, New Mexico, New York, Ohio, West Virginia, Kentucky, Wyoming, Mississippi, North Dakota, Oklahoma and the U.S. military, with other states considering similar actions.
Tramadol comes in many forms, including:
capsules (regular and extended release)
tablets (regular, extended release, chewable, low-residue and/or uncoated tablets that can be taken by the sublingual and buccal routes)
suppositories
effervescent tablets and powders
ampules of sterile solution for SC, IM, and IV injection
preservative-free solutions for injection by the various spinal routes (epidural, intrathecal, caudal, and others)
powders for compounding
liquids both with and without alcohol for oral and sub-lingual administration, available in regular phials and bottles, dropper bottles, bottles with a pump similar to those used with liquid soap and phials with droppers built into the cap
tablets and capsules containing (acetaminophen/APAP), aspirin and other agents.
Tramadol is regularly used in the form of an ingredient in multi-agent topical gels, creams, and solutions for nerve pain, rectal foam, concentrated retention enema, and a skin plaster (transdermal patch) quite similar to those used with lidocaine.
Tramadol has a characteristic and unpleasant taste which is mildly bitter but much less so than morphine and codeine. Oral and sublingual drops and liquid preparations come with and without added flavoring. This different flavouring is considered to be a standard. Its relative effectiveness via transmucosal routes (i.e. sublingual, buccal, rectal) is similar to that of codeine, and, like codeine, it is also metabolized in the liver to stronger metabolites (see below).
Patients taking SSRIs (Prozac, Zoloft, etc.), SNRIs (Effexor, etc.), TCAs, MAOIs or other strong opioids (oxycodone, methadone, fentanyl, morphine), as well as the elderly (> 75 years old), pediatric (< 18 years old), and those with severely reduced renal (kidney) or hepatic (liver) function should consult their doctor regarding adjusted dosing or whether to use tramadol at all.