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Revision as of 11:17, 7 April 2014

Template:Tramadol Tramadol (marketed as the hydrochloride salt by Janssen Pharmaceutica as Ultram in the United States, Ralivia by Biovail in Canada and many other companies throughout the world) is a centrally acting opioid analgesic used to treat moderate to moderately severe pain. It was launched and marketed as Tramal by the German pharmaceutical company Grünenthal GmbH in 1977 in West Germany, even though it would take another 20 years for it to be launched in English-speaking countries such as the UK, US and Australia.[1]

Tramadol is marketed as a racemic mixture of both R and S stereoisomers. This is because the two isomers compliment each other's analgesic activity. It is often combined with paracetamol as this is known to improve the efficacy of tramadol in relieving pain. Tramadol is a reuptake inhibitor of norepinephrine and serotonin and a weak μ-opioid receptor agonist.[2][3] Tramadol is metabolised to O-desmethyltramadol, a significantly more potent opioid.

Despite the original belief that tramadol was a purely synthetic opioid it has been recently found in a South African tree.[4]

Chemistry

Pharmacology

Tramadol acts as a μ-opioid receptor agonist,[5][6] serotonin releasing agent,[7][8][9][10] norepinephrine reuptake inhibitor,[11] NMDA receptor antagonist,[12] 5-HT2C receptor antagonist,[13] (α7)5 nicotinic acetylcholine receptor antagonist,[14] TRPV1 receptor agonist,[15] and M1 and M3 muscarinic acetylcholine receptor antagonist.[16][17]

Subjective effects

The subjective effects of opioids are extremely similar across individual substances with very little variation. These usually only differ in terms of their potency, intensity and duration. In comparison to other opioids, this particular substance can be considered as less intense in its physical and cognitive euhoria when compared with that of morphine or diacetylmorphine (heroin). It also presents greater amounts of itchiness due to higher amounts of histamine release and is considerably more stimulating than that of Codiene and Diacetylmorphine due to its effects as a serotonin reuptake inhibitor.

Toxicity and harm potential

Tramadol has not been shown to be toxic and is physically benign at reasonable dosages. As with all opiates, longer-term effects can vary but can include diminished libido, apathy and memory loss.

Tolerance and addiction potential

Tolerance to many of the effects of tramdol develops with prolonged use, including therapeutic effects. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance.

As with other opiate-based pain killers, chronic use of tramadol can be considered as highly addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.

Interactions

Its serotonergic effects enable it to interact, potentially fatally, with other serotonergics such as antidepressants (such as monoamine oxidase inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, noradrenergic and specific serotonergic antidepressants, serotonin antagonist and reuptake inhibitors, etc.), certain analgesics (such as pethidine (meperidine), tapentadol, oxycodone, dextromethorphan and fentanyl), certain anxiolytics (such as the SSRIs and buspirone), certain antibiotics (namely, linezolid and isoniazid), certain herbs (e.g. St. John's wort, syrian rue, passiflora, etc.), certain recreational drugs (e.g. MDMA), phentermine, lithium, methylene blue and numerous other therapeutic agents.[18][19] As it is a substrate of CYP3A4 and CYP2D6, hence any agents with the ability to inhibit or induce these enzymes will likely interact with tramadol.[20][21]

Legal issues

  • USA: In November 2013, the United States Drug Enforcement Administration initiated classification of Tramadol as a schedule IV controlled substance, pending a review process. Several states, including Arkansas, Kentucky, Illinois, Mississippi, New York, North Dakota, Oklahoma, Tennessee, West Virginia, Wyoming and the U.S. military have classified Tramadol as a schedule IV controlled substance under state law.[22]
  • Sweden: as of May 2008, has chosen to classify tramadol as a controlled substance in the same way as codeine and dextropropoxyphene. This means that the substance is a scheduled drug. But unlike codeine and dextropropoxyphene, a normal prescription can be used at this time.[23]

See also

References

  1. ↑ Tramadol as an analgesic for mild to moderate cancer pain | http://www.if-pan.krakow.pl/pjp/pdf/2009/6_978.pdf
  2. ↑ Induction of 5-hydroxytryptamine release by tramadol, fenfluramine and reserpine | http://www.sciencedirect.com/science/article/pii/S0014299998001952
  3. ↑ p-Methylthioamphetamine and 1-(m-chlorophenyl)piperazine, two non-neurotoxic 5-HT releasers in vivo, differ from neurotoxic amphetamine derivatives in their mode of action at 5-HT nerve endings in vitro | http://onlinelibrary.wiley.com/doi/10.1046/j.1471-4159.2002.01073.x/abstract
  4. ↑ Occurrence of the Synthetic Analgesic Tramadol in an African Medicinal Plant | http://onlinelibrary.wiley.com/doi/10.1002/anie.201305697/abstract
  5. ↑ Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids | http://www.ncbi.nlm.nih.gov/pubmed/2849950
  6. ↑ Influence of tramadol on neurotransmitter systems of the rat brain | http://www.ncbi.nlm.nih.gov/pubmed/8955860
  7. ↑ Induction of 5-hydroxytryptamine release by tramadol, fenfluramine and reserpine | http://www.ncbi.nlm.nih.gov/pubmed/8955860
  8. ↑ p-Methylthioamphetamine and 1-(m-chlorophenyl)piperazine, two non-neurotoxic 5-HT releasers in vivo, differ from neurotoxic amphetamine derivatives in their mode of action at 5-HT nerve endings in vitro | http://onlinelibrary.wiley.com/doi/10.1046/j.1471-4159.2002.01073.x/abstract
  9. ↑ Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1908625/
  10. ↑ Actions of tramadol, its enantiomers and principal metabolite, O-desmethyltramadol, on serotonin (5-HT) efflux and uptake in the rat dorsal raphe nucleus | http://bja.oxfordjournals.org/content/79/3/352
  11. ↑ Influence of tramadol on neurotransmitter systems of the rat brain | http://www.ncbi.nlm.nih.gov/pubmed/8955860
  12. ↑ The Effects of Tramadol and Its Metabolite on Glycine, γ-Aminobutyric AcidA, and N-Methyl-d-Aspartate Receptors Expressed in Xenopus Oocytes | http://journals.lww.com/anesthesia-analgesia/pages/articleviewer.aspx?year=2005&issue=05000&article=00037&type=abstract
  13. ↑ The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes | http://journals.lww.com/anesthesia-analgesia/pages/articleviewer.aspx?year=2004&issue=05000&article=00038&type=abstract
  14. ↑ The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes | http://journals.lww.com/anesthesia-analgesia/pages/articleviewer.aspx?year=2004&issue=05000&article=00038&type=abstract
  15. ↑ The analgesic drug, tramadol, acts as an agonist of the transient receptor potential vanilloid-1 | http://www.ncbi.nlm.nih.gov/pubmed/18499628
  16. ↑ Inhibition by tramadol of muscarinic receptor-induced responses in cultured adrenal medullary cells and in Xenopus laevis oocytes expressing cloned M1 receptors | http://www.ncbi.nlm.nih.gov/pubmed/11561087
  17. ↑ The Inhibitory Effects of Tramadol on Muscarinic Receptor-Induced Responses in Xenopus Oocytes Expressing Cloned M3 Receptors | http://journals.lww.com/anesthesia-analgesia/pages/articleviewer.aspx?year=2002&issue=11000&article=00031&type=abstract
  18. ↑ https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2010-PI-03844-3
  19. ↑ Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3
  20. ↑ Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3
  21. ↑ Tramadol sustained release capsules | http://link.springer.com/article/10.2165%2F00003495-200666020-00006
  22. ↑ http://www.nabp.net/news/tennessee-news-tramadol-and-carisoprodol-now-classified-schedule-iv
  23. ↑ http://www.lakemedelsverket.se/Alla-nyheter/NYHETER-2008/Substansen-tramadol-nu-narkotikaklassad-pa-samma-satt-som-kodein-och-dextropropoxifen/
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