Pharmacologie du tramadol

  title={Pharmacologie du tramadol},
  author={Pierre Dayer and Jules Alexandre Desmeules and L. Collart},
RésuméLe (±)-tramadol est un analgésique central à faible affinité pour les récepteurs opiacés. Le taux de production de son métabolite M1 (O-déméthyl tramadol), de manière analogue à la codéine, est contrôlé par le polymorphisme génétique de type débrisoquine (CYP2D6) et le dérivé M1 présente, par rapport à la molécule mère, une plus forte affinité pour les récepteurs opiacés. Des données expérimentales et cliniques indiquent que le tramadol exerce aussi son effet antalgique par une action au… 
Fármacos analgésicos opioides
Los analgésicos opioides constituyen un grupo de fármacos que se caracterizan por poseer afinidad selectiva por los receptores opioides, así como otros efectos subjetivos que tienden a favorecer la instauración oficial de una conducta de autoadministración denominada farmacodependencia.
Mechanistic and functional differentiation of tapentadol and tramadol
Tapentadol, a schedule-II controlled substance, is well-suited for pain conditions requiring a strong opioid component—and it has the benefit of greater gastrointestinal tolerability compared to classical strong opioids.
Comparative pharmacology and toxicology of tramadol and tapentadol
Although more studies are needed to provide clear guidance on the opioid of choice, tapentadol shows some advantages, as it does not require CYP450 system activation and has minimal serotonergic effects, which leads to less side effects and lower abuse liability.
Discovery and development of tramadol for the treatment of pain
The combination of monoamine and opioid mechanisms opens new avenues for the design of innovative analgesic drugs to treat moderate to severe pain.
Eficacia analgésica de una combinación utilizada en perras sometidas a ovariohisterectomía
La combinacion ensayada produjo una adecuada analgesia sin causar alteraciones hemodinamicas y respiratorias re­levantes, asi asi tambien establecer la calidad y el tiempo of recuperacion.
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.
Capillary Electrophoresis Methods for the Determination of Tramadol: A Review
Tramadol is a widely used opioid analgesic frequently prescribed for treatment of moderate to severe, acute and chronic pain. It has a complex mechanism of action, acting both as a central opiate
Population pharmacokinetic analysis of tramadol and O-desmethyltramadol with genetic polymorphism of CYP2D6
The parent-metabolite model successfully characterized the PK of tramadol and its metabolite M1 in healthy Korean male subjects and could be applied to evaluate plasma tramadl concentrations after various dosing regimens.


Pharmacology and Clinical Experience with Tramadol in Osteoarthritis
Tramadol would appear to be particularly useful in the elderly population affected by osteoarthritis because, unlike nonsteroidal anti-inflammatory drugs, it does not aggravate hypertension or congestive heart failure, nor does it have the potential to cause peptic ulcer disease.
A Risk-Benefit Assessment of Tramadol in the Management of Pain
A risk-benefit assessment of tramadol in the management of acute and chronic pain syndromes is provided and it is recommended as a safe and efficient drug for step II according to the World Health Organization guidelines for cancer pain management.
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,
Characterization of the unusual antinociceptive profile of tramadol in mice
The lack of complete cross‐tolerance between tramadol and morphine supports the suggestion of a non‐opioid mechanism for this compound, whereas the complete antagonism by naloxone apparently reflects the opioid component of its mechanism in this test.
Contribution of monoaminergic modulation to the analgesic effect of tramadol.
1. In humans, the central analgesic effect of tramadol 100 mg orally is only partially reversed by the opioid antagonist naloxone (0.8 mg intravenously). As suggested by in vitro and animal data
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.
A comparison of the effects of tramadol and morphine on gastric emptying in man
It is concluded that tramadol at a dose of 1 mgkg−1 does not delay gastric emptying in humans.
A novel approach to the pharmacology of analgesics.
  • R. Raffa
  • Biology
    The American journal of medicine
  • 1996
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).