Tramadol drug is used for pain relief
Tramadol (generic for Ultram) is a prescription medication used for the management of moderate to moderately severe pain. Tramadol® has been prescribed to more than 55 million patients worldwide; Ultram® has been prescribed to more than 21 million patients in the U.S.

Effects of tramadol on nerve action potentials in rat: comparisons with benzocaine and lidocaine.

Guven M, Mert T, Gunay I.

Cukurova University Medical School, Department of Biophysics, Adana, Turkey. guvenm@cu.edu.tr

The effects of tramadol on repetitively elicited action potentials were studied in rat sciatic nerve, using the sucrose gap method. Tramadol's local anesthetic-like effects were compared with lidocaine and benzocaine at single or 10, 40, and 100 Hz stimulations. Tramadol and lidocaine both produced approximately the same level of conduction block. The depolarization time of the compound action potentials (CAP) measured from the beginning to the peak of the CAPs, was extended by lidocaine and tramadol, but benzocaine had no effect in this respect. Tramadol extended half width of CAP more than lidocaine. Lidocaine and tramadol produced similar conduction-block patterns, which were different from benzocaine. The results suggested that tramadol enhanced the nerve conduction like lidocaine. However, their frequency-dependent block patterns were similar. It was concluded that tramadol may block the Na+ channels following the hydrophilic pathway like lidocaine and block K+ channels more than lidocaine. These may accounted for the local anesthetic-like effects of tramadol.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15804720&query_hl=2

[Effect of tramadol on regeneration after experimental sciatic nerve injury.]

[Article in Turkish]

Gunes Y, Mert T, Daglioglu YK, Ozbek H, Gunay I, Ozcengiz D, Isik G.

Cukurova University Faculty of Medicine, Department of Anesthesiology, Adana, Turkey. ygunes@cu.edu.tr.

Abnormal impulses in peripheral nerves play a critical role in neuropathic pain syndromes. The voltage-gated Na+ channels that underlie the action potential are main targets for clinically useful drugs in the pain therapy. Systemic tramadol has been shown to have clinical efficacy against some forms of neuropathic pain. Therefore, we investigated the mechanisms of action of tramadol by an in vitro model by sucrose-gap technique. Tramadol produced concentration-dependent and frequency-dependent decrements in CAP amplitude. Also, injured nerves were more sensitive to tramadol. Tramadol decreased the amplitude of the delayed depolarization and the hyperpolarizing afterpotentials. In conclusion, blocking potencies of small concentration tramadol on the delayed depolarization and hyperpolarizing afterpotential in regeneration period may be contributed for understanding of the action mechanisms of tramadol on neuropathic pain therapy.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15791498&query_hl=2

Role of 5-HT1A and 5-HT1B receptors in the antinociceptive effect of tramadol.

Rojas-Corrales MO, Berrocoso E, Mico JA.

Pharmacology and Neuroscience Research Group (CTS-510), Department of Neuroscience, Faculty of Medicine, University of Cadiz, Plaza Fragela 9, 11003-Cadiz, Spain.

Tramadol, (1RS,2RS)-2-[(dimethylamine)-methyl]-1-(3-methoxyphenyl)-cyclohexanol hydrochloride, is an atypical centrally acting analgesic agent with relatively weak opioid receptor affinity and which, like some antidepressants, is able to inhibit the reuptake of serotonin (5-hydroxytryptamine, 5-HT) in the raphe nucleus. We have previously demonstrated that pindolol, a beta-adrenoceptor blocker/5-hydroxytryptamine(1A/1B) receptor antagonist, enhanced tramadol antinociception and that the selective 5-HT1A agonist 8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) reduced it. These effects were related to the negative feedback control that regulates raphe region neurones. The current study examines the ability of the selective antagonist at somatodendritic 5-HT1A receptors, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl) cyclohexane carboxamide (WAY100635, 0.8 mg/kg), the selective antagonist at terminal 5-HT1B receptors, N-[3-(2-dimethylamino) ethoxy-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-(1,1'-biphenyl)-4-carboxamide (SB216641, 0.1-0.8 mg/kg) and the selective agonist at 5-HT1B receptors, 1,4-tDihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo[3,2-b] pyridin-5-one (CP93129, 0.2-0.4 mg/kg), to modify the antinociceptive effect of 4-64 mg/kg of tramadol in the hot plate test in mice. The results show that 0.8 mg/kg of WAY100635 enhanced antinociceptive effect of tramadol while neither agonism nor antagonism at the 5-HT1B receptor modifies it significantly at the doses tested. These results account for involvement of the somatodendritic 5-HT1A receptors in the analgesic effect of tramadol and support the supraspinal interaction of serotonin and the opioid system in the regulation of pain.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15777775&query_hl=2

Intravenous Ketoprofen in Postoperative Pain Treatment after Major Abdominal Surgery.

Oberhofer D, Skok J, Nesek-Adam V.

Department of Anaesthesiology and Intensive Care, Sveti Duh General Hospital, Sveti Duh 64, 10000, Zagreb, Croatia, dagmar.oberhofer@zg.htnet.hr.

In recent years considerable attention has been paid to the treatment of postoperative pain, with regard to the favorable effect of adequate analgesia on patient outcome. Multimodal analgesia (e.g., opioids and nonsteroidal anti-inflammatory drugs [NSAIDs] or local anesthetics) is recommended for effective postoperative pain relief. There are few data on the use of NSAIDs in postoperative pain treatment after abdominal surgery. We conducted a randomized, double-blind, placebo-controlled study to assess the analgesic efficacy and safety of ketoprofen after major abdominal surgery. One and nine hours postoperatively patients received 100 mg of ketoprofen i.v. (n = 21) or placebo (n = 22) in addition to a pain-treatment protocol consisting of continuous infusion of tramadol 200 mg and metamizol 5 g over 24 hours with additional 25 mg i.v. tramadol in case of inadequate analgesia. Pain was assessed by numeric rating scale at rest and at deep breath 3, 6, 12, and 24 hours postoperatively and the total dose of tramadol used in the first 24 hours was recorded. Patients in the ketoprofen group had significantly lower pain scores both at rest and at deep breath, at 3 (p < 0.01), 6, and 12 hours (p < 0.05) postoperatively. The 24-hour use of tramadol was significantly lower in the ketoprofen group (p < 0.01), with less nausea and vomiting. There were no bleeding complications or other adverse events related to ketoprofen therapy. The study showed the value of short-term use of ketoprofen to improve the quality of analgesia after major abdominal surgery without significant adverse effects.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15776297&query_hl=2

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