Tramadol is the generic name of an opiate medication that is sold under several trade names, including ConZip, Rybix, Ultram, and Ultracet (acetaminophen and tramadol). It was developed in Germany in the early 1960s and available for use in Europe in the late 1970s. The drug became available in the United States in 1995.
How Tramadol Works
Tramadol has a mechanism of action that is similar to the mechanism of action that occurs with most opiate drugs. It has an affinity for neurons in the brain that serve as receptors for endorphins and enkephalins, naturally derived neurotransmitters that decrease the subjective experience of pain and stress. In addition, other neurotransmitters are also affected by the use of opiate drugs like tramadol, such as dopamine, serotonin, and norepinephrine.
Tramadol also has some specific qualities not available in the many prescription opioid medications. It is a synthetic drug, whereas the majority of opiate drugs are substances that are derived from opium and naturally occurring to some extent. Tramadol has pain-suppressing qualities like all opiate drugs, but it also has specific actions on norepinephrine and serotonin that are not noticeable with other opiate drugs. Thus, it may have the potential to increase concentration, bring mood-enhancing effects, and facilitate sleep in some individuals.
Tramadol was originally marketed in the United States as a safer opiate drug for the control of mild to moderate pain compared to other drugs in its class, such as Vicodin (hydrocodone and acetaminophen) and OxyContin (oxycodone). Hydrocodone and oxycodone are classified as Schedule II controlled substances by the Drug Enforcement Administration (DEA) whereas tramadol is classified as a Schedule IV controlled substance. This indicates that the DEA considers tramadol to have less potential for abuse and the development of physical dependence than these other narcotic drugs.
Even so, substances containing tramadol can only be legally purchased with a prescription from a physician. Tramadol has become widely prescribed for the control of mild to moderate pain associated with surgery or other conditions.
Individuals who use tramadol for medicinal reasons typically take it in pill form. Like other opiate drugs, it readily crosses the blood-brain barrier and attaches to its targeted neuroreceptor sites in the brain, resulting in effects. It may also block the reuptake of the neurotransmitters norepinephrine and serotonin once these neurotransmitters are released into the synaptic cleft (the space between neurons). The general effect of tramadol is to increase the availability of these neurotransmitters.
The maximum medicinal dose for tramadol is considered to be 400 mg a day, and many individuals are instructed to take significantly less than that depending on their level of pain. The immediate effects of medicinal doses of tramadol include a significant reduction in a person’s perception of pain. This occurs as a result of the drug’s ability to attach to the brain and block messages regarding pain sensations. Mild euphoria that is very similar to the type of euphoria that other opiate drugs produce is
also common. This includes feelings of sedation, relaxation, lightheadedness, giddiness, and a mild loss of inhibitions.
Some individuals may also experience side effects that can include some of the following:
- Gastrointestinal issues, such as stomachache, bloating, mild nausea, vomiting, and/or constipation
- Drowsiness, dry mouth, and/or headache.
- Heartburn, muscle aches, and/or rash
These side effects often disappear with repeated use.
Some individuals may experience rarer side effects that can include more severe manifestations of the above as well as:
- Extreme feelings of sedation or lethargy
- Fever, chills, and/or significant perspiration
- Shallow breathing, visual disturbances, irregular heartbeat, and/or issues with blood pressure
- Chest pain or pain occurring in the legs, arms, calves, or lower back when active
- Cardiovascular issues, such as increased blood pressure or irregular heartbeat
- Tingling or weakness in the face or extremities (particularly the toes or fingers)
- Becoming sensitive to being touched
- Dark urine, finding blood in the urine, or issues with urinating, such as being unable to urinate or frequent urination
- Confusion, irritability, restlessness, anxiety, or depressive symptoms
- In very rare cases, hallucinations or seizures
Individuals who experience some of the rarer side effects should immediately contact their physician if they are using the drug medicinally. Individuals who are using the drug without a prescription should immediately stop using it if they experience any of these rare side effects. In fact, anyone who is not using opiate drugs like tramadol under the supervision of a physician is urged to contact a physician and attempt to stop taking the drug under their care.
Although tramadol is considered to be relatively mild compared to other opiate drugs, individuals can overdose on it. The symptoms of a tramadol overdose include:
- Pinpoint or narrowed pupils
- Respiratory suppression or a total cessation of breathing
- A significantly slowed heart rate
- Substantial muscle weakness, unconsciousness, or a comatose state
- Cold, clammy, skin and bluish lips or fingernails
In rare cases, serotonin syndrome may occur. This is a potentially life-threatening condition where the neurons in the brain that release the neurotransmitter serotonin become overactive and release massive amounts of serotonin into the system.
The development of seizures as a result of an allergic reaction or an overdose of tramadol represents a severe and potentially fatal occurrence. Seizures result from the unrestrained firing of neurons in a particular area of the brain that spreads to surrounding systems. The severity of the seizure depends on how far this unrestricted and uncoordinated rate of neuron firing spreads. When only a small portion of the brain is affected, only certain functions may be affected, such as speech, uncontrolled movements in one arm, or difficulty concentrating. When larger areas are involved, the effects can be more generalized and potentially dangerous due to individuals harming themselves as a result of convulsing, breathing cessation, or significant damage to the brain due to unrestricted neuronal activity.
Research studies have indicated that any seizure risk associated with products that contain tramadol is most often due to people combining tramadol with other drugs, such as alcohol or other opiate drugs. However, some research has also suggested that certain types of antidepressants may increase seizure risk if used with tramadol. The risk to develop seizures as a result of tramadol abuse also increases with the dosage an individual uses. The potential risk factors that are often listed as increasing the probability that one will develop seizures as a result of using tramadol include:
- A history of a seizure disorder (e.g., epilepsy)
- A history of head trauma or head injury
- A central nervous system infection of some type
- Going through the withdrawal syndrome from other types of drugs, such as benzodiazepines or alcohol
- Combining tramadol with other drugs like alcohol
- Using extremely high doses of tramadol
The seizure risk associated with tramadol use is extremely small (near zero) when tramadol is used according to its prescribed instructions and under the supervision of a physician. Seizures associated with tramadol use are almost always associated with individuals who abuse the drug.
The Abuse of Tramadol
According to the latest data provided by the Substance Abuse and Mental Health Services Administration (SAMHSA), tramadol products are among the most prescribed opiate substances in the country. In 2015, approximately 18.5 million individuals reported using tramadol. Of these individuals, approximately 1.8 million reported misusing the drug at some time.
Misuse does not necessarily imply drug abuse or the development of a substance use disorder; however, all individuals who develop substance use disorders begin by misusing the drug in some manner. Misuse of a drug simply means using it under circumstances or for reasons that are not consistent with its prescribed purposes. Many individuals who only misuse a drug occasionally do not go on to develop problems, but a significant proportion of individuals who misuse drugs may wind up abusing them.
It was originally believed by many that tramadol was a drug that had a low potential for abuse and physical dependence, but based on data provided by organizations like SAMHSA, this view has become substantially altered. At high doses, such as those taken by individuals who habitually misuse or abuse the drug, it acts in a very similar manner to other opiate drugs that are considered to be significantly more dangerous. In addition, individuals do develop physical dependence to tramadol. Individuals who use the drug according to its prescribed purposes and under the supervision of a physician are far less likely to have issues with physical dependence and would not be considered to be abusing the drug.
Some potential signs that an individual is abusing tramadol include:
- Use by a person who does not have a prescription for it
- Attempts to get numerous prescriptions for the drug from different doctors (a practice often termed “doctor shopping”)
- Other drug-seeking behavior, such as stealing the drug, asking to borrow it from a friend who has a prescription for it, or trying to buy it illicitly
- Regularly using more of the drug than prescribed, using it more often than prescribed, or using it in conjunction with other drugs, such as alcohol or other painkillers that are not prescribed
- Financial issues, problems at work, issues in personal relationships, or legal problems as a result of use of tramadol
- Continually using tramadol in situations where it is dangerous to do so, such as prior to operating machinery or driving
- Giving up important activities in favor of using tramadol
- Failing to fulfill major role obligations as a result of tramadol use
- Often appearing mildly or moderately intoxicated despite not drinking alcohol
- The development of tolerance to tramadol in an individual who does not have a prescription for the drug
- The development of withdrawal symptoms from tramadol in an individual who does not use the drug for medicinal purposes
Individuals who abuse tramadol on a consistent basis for more than a few weeks are likely to develop some level of tolerance to the drug. Over time, they are also likely to develop a withdrawal syndrome associated with discontinuing the drug. Various symptoms are associated with withdrawal from tramadol.
- Within 24 hours of discontinuing the drug, flulike symptoms may develop. These include nausea, fever, chills, vomiting, headache, irritability, restlessness, and similar symptoms, which can become quite intense.
- Psychological symptoms may occur, such as issues with mood (depression and/or anxiety), irritability, insomnia, and significant restlessness.
- Other physical symptoms can include alterations in blood pressure and heart rate, loss of appetite, and cognitive issues, such as suspiciousness, confusion, anxiety (even panic attacks), and issues with depression.
- Significant cravings to find and use tramadol are common.
- The symptoms of withdrawal from tramadol will most often peak within 3-5 days after the person has stopped using the drug and last 7-10 days.
The formal symptoms associated with withdrawal from tramadol are not considered to be potentially serious in the same way as the withdrawal syndrome that occurs with alcohol can produce life-threatening seizures; however, other associated complications, such as dehydration from vomiting and not eating or issues with judgment, may place an individual at significant risk for harm. Some individuals may have extreme emotional reactions that include thoughts of self-harm or that border on psychosis, and these individuals are at serious risk for self-harm.
Individuals who develop an opiate use disorder as a result of abusing tramadol will benefit from a formal treatment plan.
- Initial enrollment in a physician-assisted withdrawal management program, often referred to as medical detox, is recommended. Depending on the severity of the abuse, the individual may be administered an opioid replacement medication, such as Suboxone (buprenorphine and naloxone), on a tapering schedule, or in some cases, they may be placed on a tapering schedule of tramadol.
A tapering schedule consists of a physician beginning with a dose of the medication that results in the individual not experiencing any withdrawal symptoms and, then, slowly weaning the individual off the drug by decreasing the dosage at significant intervals. Each dosage decrease allows the individual to slowly adjust to declining levels of the drug in the system without experiencing any withdrawal symptoms. Other medications may also be used. Depending on the severity of the individual’s substance use disorder, this program may be performed in an inpatient unit or as an outpatient. There are advantages to both, depending on the needs of the individual.
- Substance use disorder therapy is the cornerstone of treatment for any substance use disorder, and it is essential that the person becomes involved in it. Therapy can be delivered in individual sessions, group sessions, or both. Substance use disorder therapy is typically of a cognitive-behavioral nature and helps the individual to understand the reasons for their substance abuse, address them, develop coping skills, create a relapse prevention plan for the future, and address any other issues.
- Significant social support from family, friends, or social support groups, such as 12-Step groups (e.g., Narcotics Anonymous), is important. Social support, like substance use disorder therapy, is a key factor that contributes to a successful recovery.
- Other interventions, medical or behavioral, that are needed for the specific case may be used. Individuals with substance use disorders are not all the same, and adjustments to the formal treatment protocol for substance use disorders must be made in order for the specific program to be successful. Interventions for co-occurring disorders, vocational training, family therapy, adjunctive therapy like music or art therapy, etc., can all be used, depending on the needs of the individual.
The key component to recovery from any substance use disorder is to remain in treatment for a sufficient length of time. This means staying in treatment for years following abstinence in most cases. Most often, substance use disorder therapy is time-limited, and individuals will transition from formal therapy once they have developed the sufficient skills to move on and continue in other interventions, such as participation in 12-Step groups, community support groups, etc.