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The pharmacology of tramadol.
Drugs. 1994; 47 Suppl 1:3-7.D

Abstract

(+/-)-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 monaminergic pathways. Indeed, after a single oral dose, the role of the mu-receptor agonist component of the antinociceptive effect of tramadol appears to be minor, with most of the analgesic effect being attributable to nonopioid properties of the parent compound. Approximately 2-fold accumulation of the parent compound and the M1 metabolite may be expected during multiple dose treatment. The duration of analgesic effect after a single oral dose of tramadol 100 mg is about 6 hours. Clinical experience has confirmed that tramadol is an effective and relatively safe analgesic that may be of value in several pain conditions not requiring treatment with strong opioids.

Authors+Show Affiliations

Division of Clinical Pharmacology and Pain Clinic, University Hospital, Geneva, Switzerland.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

7517823

Citation

Dayer, P, et al. "The Pharmacology of Tramadol." Drugs, vol. 47 Suppl 1, 1994, pp. 3-7.
Dayer P, Collart L, Desmeules J. The pharmacology of tramadol. Drugs. 1994;47 Suppl 1:3-7.
Dayer, P., Collart, L., & Desmeules, J. (1994). The pharmacology of tramadol. Drugs, 47 Suppl 1, 3-7.
Dayer P, Collart L, Desmeules J. The Pharmacology of Tramadol. Drugs. 1994;47 Suppl 1:3-7. PubMed PMID: 7517823.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The pharmacology of tramadol. AU - Dayer,P, AU - Collart,L, AU - Desmeules,J, PY - 1994/1/1/pubmed PY - 1994/1/1/medline PY - 1994/1/1/entrez SP - 3 EP - 7 JF - Drugs JO - Drugs VL - 47 Suppl 1 N2 - (+/-)-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 monaminergic pathways. Indeed, after a single oral dose, the role of the mu-receptor agonist component of the antinociceptive effect of tramadol appears to be minor, with most of the analgesic effect being attributable to nonopioid properties of the parent compound. Approximately 2-fold accumulation of the parent compound and the M1 metabolite may be expected during multiple dose treatment. The duration of analgesic effect after a single oral dose of tramadol 100 mg is about 6 hours. Clinical experience has confirmed that tramadol is an effective and relatively safe analgesic that may be of value in several pain conditions not requiring treatment with strong opioids. SN - 0012-6667 UR - https://www.unboundmedicine.com/medline/citation/7517823/The_pharmacology_of_tramadol_ L2 - https://dx.doi.org/10.2165/00003495-199400471-00003 DB - PRIME DP - Unbound Medicine ER -