Module 2: Basic Pharmacology of Controlled Drugs and Substances

Lesson 3

Other agents – Tramadol

Tramadol is an opioid analgesic, meaning it shares similar pharmacological properties to those of pure opiates and the semi-synthetic opiates that are controlled under the CDSA. Its primary indication is for mild-to-moderate pain when other non-opioid agents have been ineffective. Tramadol’s primary mechanisms of action include acting as an opioid on μ-opioid receptors to exert analgesic effect and augmenting the action of serotonin and norepinephrine to provide pain relief, as well as some antidepressant effects (Young & Juurlink, 2013). It also exerts agonist and antagonist effects on other receptors, including nicotinic acetylcholine, muscarinic acetylcholine, and NMDA receptors. Because it is metabolized by CYP2D6 (an isoenzyme of cytochrome P450), the pharmacodynamics and pharmacokinetics related to poor-metabolizers and rapid-metabolizers must be kept in mind when prescribing, adjusting doses, and monitoring effects. Caution should be taken for use in patients with a history of seizure disorders, patients under 18 years of age, or individuals with a history of suicide or addiction.  Tramadol is also available in a combination form, known as Tramacet, which contains acetaminophen to enhance the analgesic properties.


  • Young, J. S. W., & Juurlink, D. N. (2013). Tramadol. CMAJ, 185 (8), E352. doi:10.1503/cmaj.121592