The Pharmacology of Tramadol

  title={The Pharmacology of Tramadol},
  author={Pierre Dayer and L Collart and Jules A. Desmeules},
Summary(±)-Tramadol is a central analgesic with low affinity for opioid receptors. The rate of production of its M1 metabolite (O-demethyl tramadol) is influenced by debrisoquine-type polymorphism, and this metabolite shows a higher affinity for opioid receptors than the parent drug. Experimental and clinical data suggest that tramadol may also exert its analgesic effect through direct modulation of central monoaminergic pathways. Indeed, after a single oral dose, the role of the μ-receptor… 
ADME and toxicity considerations for tramadol: from basic research to clinical implications
This review provides a comprehensive view on the pharmacokinetic, pharmacodynamic, and toxicity of tramadol with a deep look on its side effects, biochemical and pathological changes, and possible drug interactions.
Association between opioid use disorder (tramadol) and serum level of interleukin-2
It was found that patients with opioid use disorder (tramadol) have significantly elevated serum levels of IL-2 than healthy controls, and this elevation was dose related.
Retrospective analysis reveals significant association of hypoglycemia with tramadol and methadone in contrast to other opioids
Over twelve million reports from United States Food and Drug Administration Adverse Event Reporting System were analyzed and provided evidence of increased propensity for hypoglycemia in patients taking tramadol when compared to patients taking other opioids, serotonin-norepinephrine reuptake inhibitors, and drugs affecting NMDAR activity.
of Emergency Practice and Trauma Case Report
The shoulder dislocation following tramadol-induced seizure is evaluated and its potential difference with other shoulder dislocations is evaluated.
Pharmacokinetics of tramadol and its major metabolites in alpacas following intravenous and oral administration.
Because of the poor bioavailability and adverse effects noted in this study, the oral administration of tramadol in alpacas cannot be recommended without further research.
An open label trial of the effects and safety profile of extended-release tramadol in the management of chronic pain.
Comparison the analgesic effects of single dose administration of tramadol or piroxicam on postoperative pain after cesarean delivery.
It might be concluded that injections of 20 mg piroxicam (single dose therapy) could relieve postoperative pain after cesarean section as well as tramadol and it could reduce opioid analgesic requirements with less adverse side effects during the first postoperative 24 h.
Tramadol Dependence: A Case Series from India
Seven cases, all men, who sought treatment at the centre for tramadol-dependence, with the majority using other opioids at some point in their lives, underscore the need for caution, while using tramadolia in substance-dependent patients.
Inhibition and structural changes of liver alkaline phosphatase by tramadol.
It is shown that tramadol can bind to alakaline phosphatase and inhibit the enzyme in an un-competitive manner and also conformational changes in enzyme occurred when the drug bound to enzyme-substrate complex.


Analgesic oral efficacy of tramadol hydrochloride in postoperative pain.
Tramadol hydrochloride at both dose levels is an effective analgesic agent and at 150 mg is statistically superior to the acetaminophen-propoxyphene combination.
Analgesic oral efficacy of tramadol hydrochloride in postoperative pain
Tramadol hydrochloride at both dose levels is an effective analgesic agent and at 150 mg is statistically superior to the acetaminophen‐propoxyphene combination.
Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids.
The influence of replacing the phenolic hydroxyl by the methoxy group on opioid receptor binding, analgesic and antitussive action was investigated in the corresponding couples morphine-codeine,
Central analgesic effect of acetaminophen but not of aspirin
Findings show that acetaminophen‐induced analgesia is centrally mediated, in contrast to aspirin, and the time delay between plasma concentration kinetics and acetaminphen analgesic effect is another argument in favor of its direct action on the central nervous system.
Central analgesic effects of desipramine, fluvoxamine, and moclobemide after single oral dosing: A study in healthy volunteers
The antinociceptive effect of three antidepressants with different postulated modes of action was evaluated after single oral dosing in a randomized, double‐blind, placebo‐controlled crossover study in 10 healthy volunteers.
Bioavailability of enteral tramadol formulations. 1st communication: capsules.
The absolute bioavailability of tramadol hydrochloride after the oral administration of Tramal capsules was determined in a balanced cross-over study in 10 male volunteers in what is believed to be a first for this type of study.
New Clinical Experience with Tramadol
New pharmacokinetic data show that steady-state plasma tramadol concentrations reached after oral administration of 50mg doses every 6 hours are similar to those obtained after administration of a 100mg single oral dose (250 μg/L).
Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an 'atypical' opioid analgesic.
The results suggest that tramadol-induced antinociception is mediated by opioid (mu) and nonopioid (inhibition of monoamine uptake) mechanisms, and is consistent with the clinical experience of a wide separation between analgesia and typical opioid side effects.