Tramadol revisited

Budd, Keith; Langford, R

doi:10.1093/bja/82.4.493

Cited by 101 publications

(72 citation statements)

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“…It also inhibits reuptake of norepinephrine and serotonin in synaptic junctions (18,19). Tramadol is rapidly and extensively metabolized by hepatic O-and Ndesmethylation pathways catalyzed by cytochrome P-450 isoenzymes of 2D6, 2B6 and 3A4, orderly (20). O-desmethyl tramadol (M1) and N-desmethyl tramadol (M2) are considered as main metabolites of the drug in humans.…”

Section: Introductionmentioning

confidence: 99%

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

et al. 2012

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-Purpose. Tramadol Hydrochloride is a widely-used centrally acting analgesic drug, which has some features of being a P-gp substrate. The present study evaluates the functional involvement of Pgp in CNS distribution of tramadol. Methods. The possibe involvement of P-glycoprotein in brain distribution of tramadol was evaluated using a pharmacokinetic approach in two groups of Pgp-inhibited and control rats. Six male Sprague-Dawley rats were used in each group to collect plasma and brain at 1, 5, 10, and 30 min following two tramadol doses of 1 and 10 mg/kg. Results. The brain uptake clearances of tramadol in Pgp-inhibited and control rats were 2.47±0.56 and 2.34±0.56 ml min , respectively, for 10 mg/kg dose. The brain-to-plasma concentration ratio (Kp,app) of more than 1 in all the time points following both the high and low dose cases (sometimes more than 3) indicated the brain accumulation of the drug. Linear correlation was found between tramadol dose and both corresponding plasma and brain concentrations, but the presence of a dose-dependency was not confirmed by the data obtained for brain-to-plasma concentration ratio. Conclusion. Considering the results of the previous studies and the present research, it seems that the brain accumulation of tramadol is not affected by P-gp inhibition which implies that there may be some other transport mechanisms involved in BBB transport of tramadol.

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Section: Introductionmentioning

confidence: 99%

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

et al. 2012

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“…Tramadol is a centrally acting analgesic that has a multimodal mechanism of action [1] . It is a partial -opioid receptor agonist, blocks the reuptake of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline and enhances the release of 5-HT at spinal antinociceptive pathways [2,3] .…”

Section: Introductionmentioning

confidence: 99%

Co-Administration of Ondansetron Decreases the Analgesic Efficacy of Tramadol in Humans

Vale¹,

Oliveira²,

Assunção³

et al. 2011

Pharmacology

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Tramadol, a central analgesic acting on serotonin neurotransmission, is often co-used with ondansetron, a 5-HT₃ antagonist, for the management of postoperative pain to decrease nausea and vomiting. The aim of the study is to test the hypothesis that this drug combination raises tramadol requirement by patient-controlled analgesia (PCA). Forty patients undergoing hernioplasty or thyroidectomy were enrolled in a randomized, controlled study and allocated to receive ondansetron 4 mg i.v. (n = 20) or saline (n = 20). At 0, 1, 2, 4 and 24 h of PCA, tramadol consumption was evaluated. Tramadol consumption (mg × kg^–1 × h^–1) was higher in the ondansetron group at the 2-hour time point compared to the control group (0.24 ± 0.1 vs. 0.17 ± 0.16; p = 0.01). Our study suggests that ondansetron acutely reduces the analgesic efficacy of tramadol.

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“…Significant reduction in VAS scores were also observed by Swathi 11 Nausea and vomiting was observed in none of the patients in Group B and 4 patients in group T which is statistically significant. Tramadol is known to cause higher incidence of nausea and vomiting 17 . So drugs to control nausea and vomiting should be given when tramadol is used.…”

Section: Discussionmentioning

confidence: 99%

Epidural butorphanol for post operative analgesia in lower limb surgeries: A comparative study with epidural tramadol

Deo

Shrestha

2017

J Chitwan Med Coll

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To compare the efficacy of epidural butorphanol and tramadol for post operative analgesia in lower limb surgeries. Randomized, controlled, double blind, prospective study conducted at Department of Anaesthesia and Critical Care, Chitwan Medical College from September 1st 2015 to August 31st 2016. 60 patients of ASA Grade I and II of either sex, aged between 18-65 years willing for epidural analgesia for post operative analgesia were included in the study. They were divided into two groups: Group B- Butorphanol group and Group T- Tramadol group. Subjects of Group B received 2mg of Butorphanol and 0.25% Bupivacaine making a total volume of 10 ml and that of Group T received 100mg of Tramadol and 0.25% Bupivacaine also making a total volume of 10 ml. Analgesic efficacy was assessed by Visual Analogue Scale (VAS). The onset and duration of analgesia along with side effects were also assessed. The quality of analgesia was studied using time to independent mobilization and overall patient satisfaction. Total number of patients was 60, of ASA Grade I and II, aged between 18-65 years. The mean age of patients in Group B was 42.6±11.7 years and 46.1±11.2 years in Group T. Time of onset of analgesia after epidural injection was 7.4±0.9 minutes in Group B and 12.7±1.5 minutes in Group T and the difference was found to be statistically significant. Duration of analgesia was 317.1±99.1 minutes and 438.8±136.6 minutes in Butorphanol and Tramadol groups respectively which was also statistically significant. Sedation was significantly higher in butorphanol group whereas nausea and vomiting was higher in tramadol group. Quality of analgesia in terms of patient satisfaction was better with epidural butorphanol. Both epidural tramadol and butorphanol were effective in relieving post operative pain however butorphanol had lesser side effects and greater patient satisfaction compared to tramadol but the duration of action was relatively short.

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Tramadol revisited

Cited by 101 publications

References 0 publications

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

Co-Administration of Ondansetron Decreases the Analgesic Efficacy of Tramadol in Humans

Epidural butorphanol for post operative analgesia in lower limb surgeries: A comparative study with epidural tramadol

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