Disease relevance of Tramadol

• Impact of fibromyalgia pain on health-related quality of life before and after treatment with tramadol/acetaminophen [1].
• The most frequently occurring adverse events with tramadol were nausea, constipation, headache, and somnolence [2].
• OBJECTIVE: The objective of this study was to evaluate the efficacy and safety of tramadol in treating the pain of diabetic neuropathy [2].
• The effect of tramadol in painful polyneuropathy in relation to serum drug and metabolite levels [3].
• While it is not recommended as a supplement to general anaesthesia because of its insufficient sedative activity, tramadol has been successful in the treatment of postoperative pain [4].

Psychiatry related information on Tramadol

• Tramadol dependence with no history of substance abuse [5].
• Treatment of anorexia nervosa with tramadol [6].
• Treatment of restless legs syndrome with tramadol: an open study [7].
• Electrical pain thresholds increased and pain during suprathreshold stimulation decreased markedly on the stump and, to a lesser extent, on the contralateral limb after 1 month of treatment with amitriptyline or tramadol [8].
• CONCLUSIONS: In treatment-naive patients, both amitriptyline and tramadol provided excellent and stable phantom limb and stump pain control with no major adverse events [8].

High impact information on Tramadol

• These results suggest that activation of opioid mu-receptors by tramadol can increase the utilization of glucose and/or decrease hepatic gluconeogenesis to lower plasma glucose in diabetic rats lacking insulin [9].
• The stimulatory effects of tramadol on glycogen synthesis were also seen in hepatocytes isolated from STZ-induced diabetic rats [9].
• Moreover, similar repeated treatments with tramadol reversed the elevated mRNA and protein levels of phosphoenolpyruvate carboxykinase in the liver of STZ-induced diabetic rats [9].
• Indexes of physical functioning, role-physical, body pain, health transition, and physical component summary all improved significantly in the tramadol/acetaminophen-treated subjects [10].
• Pharmacokinetics, efficacy, and safety of analgesia with a focus on tramadol HCl [11].

Chemical compound and disease context of Tramadol

• In several comparative, well designed studies, oral and parenteral tramadol effectively relieved moderate to severe postoperative pain associated with surgery [12].
• However, in the Tramadol-Lidocaine Group, the speed of onset of sensory block was faster than in the Lidocaine Group. In the Tramadol and the Tramadol-Lidocaine Groups, the incidence of skin rash and painful or burning sensation at the injection site was increased [13].
• BACKGROUND: This study was designed to evaluate the analgesic efficacy of three doses of tramadol, administered caudally with bupivacaine, in providing postoperative pain relief in children [14].
• Effects of tramadol and O-demethyl-tramadol on human 5-HT reuptake carriers and human 5-HT3A receptors: a possible mechanism for tramadol-induced early emesis [15].
• Pain thresholds at or distant from the incision increased significantly after surgery only with tramadol plus diclofenac [16].

Biological context of Tramadol

• Modern narcotic analgesic drugs, such as tramadol, pentazocine, and buprenorphine share similarities of molecular structure with morphine which is widely believed to cause spasm of the bile duct sphincter and so impede bile flow [17].
• CONCLUSION: Fifty milligrams of tramadol is an alternative CYP2D6 phenotype probe by use of the 8-hour urinary ratio of (-)-M1/(+)-M1 [18].
• Tramadol SR capsules had identical bioavailability to tramadol immediate-release (IR) capsules with lower peak concentrations and less fluctuation in plasma concentrations [19].
• CONCLUSION: Tramadol and APAP/C had no effect on gastric emptying or small bowel transit [20].
• This study investigates whether the PM genotype has an impact on the response to tramadol analgesia in postoperative patients [21].

Anatomical context of Tramadol

• Effect of modern analgesic drugs (tramadol, pentazocine, and buprenorphine) on the bile duct sphincter in man [17].
• The biliary pressure in the control studies was similar to that following administration of all analgesics in the animals with gallbladder and following instillation of tramadol, metamizol, and acetylsalicylic acid in animals with no gallbladder [22].
• In extensive metabolizers, tramadol increased pressure pain detection (p = 0.03) and tolerance (p = 0.06) thresholds, as well as thresholds for eliciting nociceptive reflexes, after single (p = 0.0002) and repeated (p = 0.06) stimulation of the sural nerve [23].
• A total of 456 patients with moderate-to-severe pain within 5 h after extraction of two or more third molars were randomized to receive two identical encapsulated tablets containing tramadol/APAP 37.5 mg/325 mg, tramadol 50 mg, or placebo [24].
• We investigated the effects of acute and chronic tramadol treatment on T lymphocyte function and natural killer (NK) cell activity in rats receiving chronic constriction injury (CCI) of the sciatic nerve [25].

Associations of Tramadol with other chemical compounds

• The analgesic effect of 2 mg/kg tramadol was evaluated in 15 extensive and 12 poor metabolizers of sparteine in two parallel, randomized, double-blind, placebo-controlled crossover studies that used experimental pain models [23].
• METHODS: With and without paroxetine pretreatment (20 mg daily for 3 consecutive days), the formation of M1 and the analgesic effect of 150 mg of tramadol were studied in 16 healthy extensive metabolizers of sparteine in a randomized, double-blind, placebo-controlled, 4-way crossover study by use of experimental pain models [26].
• Simultaneous determination of ethamsylate, tramadol and lidocaine in human urine by capillary electrophoresis with electrochemiluminescence detection [27].
• Four chiral basic analytes, namely methadone, fluoxetine, venlafaxine, and tramadol, were selected as model compounds for investigating their stereoselective separation with highly sulfated gamma-cyclodextrin (HS gamma-CD) by capillary electrophoresis (CE)-UV and CE-mass spectrometry (MS) [28].
• In vivo effect of tramadol on locus coeruleus neurons is mediated by alpha2-adrenoceptors and modulated by serotonin [29].

Gene context of Tramadol

• Impact of CYP2D6 genotype on postoperative tramadol analgesia [21].
• METHODS: We compared a cyclooxygenase-2 inhibitor (etodolac) with two traditional drugs: a nonselective cyclooxygenase inhibitor (diclofenac) and a weak opioid (tramadol) on postoperative pain and renal function in patients undergoing coronary artery bypass operations [30].
• In studies with characterized human liver microsomal preparations, good correlations were observed between tramadol metabolism to M1 and M2 and enzymatic markers of CYP2D6 and CYP2B6, respectively [31].
• Tramadol was metabolized to M1 by cDNA-expressed CYP2D6 and to M2 by CYP2B6 and CYP3A4 [31].
• Isobolographic analysis of interaction between cyclooxygenase inhibitors and tramadol in acetic acid-induced writhing in mice [32].

Analytical, diagnostic and therapeutic context of Tramadol

• However, in most animal tests and human clinical trials, the analgesic effect of tramadol is only partially blocked by the opioid antagonist naloxone, suggesting an important nonopioid mechanism [33].
• These data indicated that the effects of such drugs on bile duct sphincter function can be safely assessed by ERCP manometry and that pentazocine adversely affects the bile duct sphincter, whilst tramadol and buprenorphine do not [17].
• Patient-controlled analgesia with tramadol has been frequently employed and was well accepted by the patients [4].
• New pharmacokinetic data show that steady-state plasma tramadol concentrations reached after oral administration of 50 mg doses every 6 hours are similar to those obtained after administration of a 100 mg single oral dose (250 micrograms/L) [34].
• Use of cyclodextrins in capillary electrophoresis: resolution of tramadol enantiomers [35].

References