What is tramadol?

History of Use

Tramadol was first synthesized in 1962 by the German pharmaceutical company Grünenthal. Tramadol has been in clinical use in Germany since 1977. Originally marketed as a safe painkiller with a low risk of abuse, tramadol became the most prescribed opioid on the European market. It was introduced to the prescription drug market in the United States in 1995 as Ultram, a nontraditional, centrally acting analgesic. Tramadol has a nonscheduled status, meaning it has a low potential for abuse.

Tramadol produces pleasurable sensations and relaxation without increased drowsiness, enabling people to remain productive while managing pain. It is an easily available opiate and can be habit forming because of its morphine-like properties. Because of reports of increased tramadol misuse, it has been labeled a drug of concern by the US Food and Drug Administration and thus requires additional label warnings. Some US states have classified tramadol as a controlled substance.

Effects and Potential Risks

Tramadol is a nontraditional, centrally acting opioid analgesic with morphine-like pain-relieving activity. It has a dual mechanism of pain relief because it includes a mixture of enantiomers.

Studies suggest that tramadol activity is mediated through both opioid and non-opioid or monoaminergic mechanisms. It exhibits opioid activity by binding to specific opioid receptors in the brain that decrease pain perception. Monoaminergic activity is displayed by inhibiting the reuptake of norepinephrine and serotonin, neurotransmitters responsible for altering pain response in the brain.

The short-term effects of tramadol include feelings of euphoria, mood elevation, and relaxation. Tramadol is usually well tolerated but can be associated with negative short-term effects, including nausea, vomiting, constipation, drowsiness, dizziness, vertigo, weakness, and headache.

Long-term use of tramadol can be associated with drug dependence and possible addiction. Abruptly stopping tramadol may generate opiate-like withdrawal symptoms such as anxiety, agitation, sweating, abdominal upset, and hallucinations.

Bibliography

Grond, Stefan, and Armin Sablotzki. “Clinical Pharmacology of Tramadol.” Clinical Pharmacokinetics 43.13 (2004): 879–923. Print.

Raffa, Robert B. “Basic Pharmacology Relevant to Drug Abuse Assessment: Tramadol as Example.” Journal of Clinical Pharmacy and Therapeutics 33.2 (2008): 101–8. Print.

Senay, Edward C., et al. “Physical Dependence on Ultram (Tramadol Hydrochloride): Both Opioid-Like and Atypical Withdrawal Symptoms Occur.” Drug and Alcohol Dependence 69.3 (2003): 233–41. Print.