Part of a growing problem
Traditionally, the narcotic (opioid) painkillers have been the mainstay of pain medicine. Most of these drugs are Schedule II (oxycodone, morphine, etc.) or Schedule III (e.g., hydrocodone). There have been new innovations such as the sustained release brand of oxycodone with the trade name OxyContin®. All of these narcotic medications are very familiar to the addiction clinician, as prescription pain killer abuse and addiction is becoming one of the most rapidly growing addiction problems.

Ultram® (tramadol) manufactured by Ortho-McNeil Pharmaceutical came onto the American pharmaceutical landscape in 1995 as a non-scheduled painkiller. Today it remains a non-controlled (not scheduled under the Controlled Substances Act) drug, although some states have looked at the abuse and dependency potential of the drug and regulated it in a similar fashion to hydrocodone.

Tramadol can be easily obtained over the Internet through a large number of pharmaceutical resources. The medication can be obtained by simply ordering the drug with a credit card. With many of these sites, there is no requirement for a medical history to be given or for any type of physician approval. As more and more cases of abuse and addiction are documented, there will be pressure on regulatory bodies to schedule and regulate this drug. This pressure will have to overcome the vast amount of marketing dollars spent by the pharmaceutical industry that would like to see the drug remain non-controlled and easily available.

The skinny on tramadol
Tramadol is an effective pain reliever (analgesic). It is used in the management of moderate to moderately severe pain. Its mode of action resembles that of the narcotics, but the pharmaceutical research states that the drug has significantly less potential for abuse and addiction than the narcotics. Tramadol is as effective as narcotics in relieving pain, but does not depress respiration, a side effect of most narcotics. Tramadol is not a nonsteroidal anti-inflammatory drug (NSAID), and does not have the increased risk of stomach ulceration and internal bleeding that can occur with the use of NSAIDs.

Tramadol helps the body’s system relieve pain in two ways. Laboratory studies suggest that first, tramadol acts directly on parts of the brain and spinal cord to reduce the amount of pain. Second, it reduces the size of the pain signal passed from one nerve to another. While the mode of action of tramadol is not completely understood, there appears to be at least two complementary mechanisms in action: tramadol and its M1 metabolite bind to opioid receptors, and secondly the drug is a weak inhibiter of the re-uptake of norepinephrine and serotonin. Serotonin and norepinephrine are neurotransmitters involved in the pain pathways.

Negative effects
Tramadol can impair thinking and the physical abilities required for driving or operating machinery. Tramadol should be avoided in patients intoxicated with alcohol, hypnotics, and narcotics. Large doses of tramadol administered with alcohol or anesthetic agents can impair breathing. Tramadol should be avoided in patients with a history of opiate addiction or hypersensitivity to opiate medications. Cases of abuse and dependence on tramadol have been reported, although initially addiction to the drug was felt to be nonexistent or at least very rare. Reports from the field, however, are telling a different story. It should not be used in opioid-dependent patients. Since tramadol can reinitiate physical dependence, it should not be used for patients with a tendency toward drug abuse, or a history of drug dependence.

Tramadol is generally well-tolerated and side effects are usually short-lasting. The most commonly reported side effects include nausea, constipation, dizziness, headache, drowsiness, and vomiting. Less commonly reported ones include itching, sweating, dry mouth, diarrhea, rash, visual disturbances, and vertigo. Cases of tramadol overdose, including fatalities associated with both intentional and unintentional overdose, have been reported. Manifestations of overdose are similar to those of other opiate agonists, with the most serious potential consequences being respiratory depression, lethargy, coma, seizure, cardiac arrest, and death.

When treating tramadol overdose, attention should be given to maintaining an adequate airway along with general supportive treatment. Although an opiate antagonist (e.g., naloxone) will reverse some, but not all, manifestations of tramadol overdose, the risk of seizures also is increased with administration of naloxone. Seizures following the administration of toxic doses of tramadol can be suppressed with barbiturates or benzodiazepines.

The drug in context
In the early 1970s, the pharmaceutical company that put the early benzodiazepines
— Valium® and Librium® — on the market stated that there was no known reported cases of addiction to these drugs. Over time, both of these medications became known as drugs of addiction and it was understood that abrupt withdrawal could create a life-threatening event. Often it takes time to fully appreciate the addiction potential of newly marketed pharmacological agents. Tramadol is turning out to be another such agent.

Amid glowing reports of pain treatment effectiveness and little or no addiction potential, tramadol sounded too good to be true. As time passes, the addiction field is hearing more and more reports of addiction and desperation, especially from those with addiction histories who are given this medication and told not to worry. Remember, it is said that in 1898 Bayer Pharmaceutical Company manufactured a drug to be used in the treatment of cocaine addiction. The drug was named after a female hero and called heroin.

Cardwell C. Nuckols, PhD, is President of Cardwell C. Nuckols & Assoc., LLC a national and international training and consulting organization. He can be reached at This e-mail address is being protected from spam bots, you need JavaScript enabled to view it

References
DEA Intelligence Brief. (2003). http://www.usdoj.gov/dea/pubs/intel/02052/02052.html
DEA Notice of Intent to Schedule Alpha-methyltryptamine and 5methoxy-Ndiisopropyltryptamine. (2003). http://www.cognitiveliberty.org/dll/amt_5meo-dipt_Dea_notice.htm.
Drug Testing Basics. (2003). From Erowid. http://www.erowid.org/psychoactives/testing/testing_info1.shtml.
Me-O-DIPT User’s Guide. (2003). From Erowid. http://www.erowid.org/chemicals/5meo_dipt/5meo_diptguide.shtml.
Shulgin, A. & Shulgin, A. (2003). From Erowid online text Tihkal. http://www.erowid.org/library/books_online/tihkal/tihkal37.shtml.

This article is published in Counselor,The Magazine for Addiction Professionals, October 2003, v.4, n.5, pp. 28-29.

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