Tramadol

DESCRIPTION / DEFINITIONS: Tramadol is a type of narcotic (a synthetic opioid) that also acts as an antidepressant in that it inhibits reuptake of serotonin and norephinephrine. See more details below.

ABUSE: Tramadol is a Schedule IV drug, which means it has medical use and has a low potential for abuse. However, research indicates that the abuse potential is a more serious problem.

ADDICTION / DEPENDENCE:Although tramadol was thought to be non-addictive in the not too distant past, it is now known to be more addictive than previously thought, as with opioids. See below for more information.

SIDE EFFECTS:  Side effects can range from dizziness, diarrhea, rapid heart rate, seizures, and many more. See more below.

WITHDRAWAL SYMPTOMS: Anxiety, tremors, panic attacks, headaches, chills, fever and seizures. See a more complete list below.

TREATMENT: Going off tramadol should be done with medical supervision. A medical detoxification program can help a person get through withdrawal safely and more comfortably.

 

DESCRIPTION / DEFINITIONS

Tramadol is a synthetic opioid. It has the same effect as any other narcotic, although it is less potent. It’s addictive, and one can develop a physical dependence on it, and it is easily abused. It also inhibits the reuptake of norepinephrine and serotonin – which is the method by which certain antidepressants (such as Selective Serotonin Reuptake Inhibitors – SSRIs) work and is therefore sometimes prescribed for depression.

Known by more than a dozen names, almost all of which offer more than one formulation, government websites include at least 211 listings for tramadol in the U.S. alone. These listings comprise a number of different brand names, manufacturers, distributors and packagers offering tramadol in a variety of tablets, capsules, extended release formulations, with various coatings and sometimes combined with other drugs such as acetaminophen. Tramadol is available in the U.S. as Synapryn, Theratramadol, Tramapap, Conzip, Ultracet, Ultram, and Ryzolt, and under several other names in different countries.

Until 2014, the DEA had not added tramadol to the list of scheduled drugs because it was thought to be non-addictive and have a low potential for abuse. However, as news of its higher-than-suspected addiction and abuse potential spread, and when it started being prescribed more often, due to the known highly addictive and dangerous nature of other opiate painkillers like OxyContin, the DEA added it to the list of Schedule IV drugs.

Many websites, and even some doctors, are not yet aware of this change in Schedule or have not updated their information. In fact, some doctors do not even know tramadol is a synthetic opioid.

Schedule IV drugs are those that have a medical use and have a low potential for abuse.

However, research has shown that the potential for abuse is more common than previously thought.

ABUSE

Tramadol is abused by taking too much of it, and by crushing the tablets and snorting them. Signs and symptoms of abuse include:

  • nausea and vomiting
  • constipation
  • fever
  • dizziness
  • appetite loss
  • trouble concentrating
  • muscle aches
  • depression
  • sweating

Severe symptoms can also include seizures and central nervous system (CNS) depression. CNS depression is specifically the result of inhibited brain activity and can result in decreased rate of breathing, decreased heart rate, and loss of consciousness possibly leading to coma or death.

ADDICTION / DEPENDENCE

Tramadol is related to opioids like codeine and morphine and can lead to psychological and physical dependence, as well as drug-seeking behavior. Drug seeking behavior can include aggressively complaining about a need for a drug and being more concerned about the drug than about the condition they’re using it for, frequent or unscheduled visits to a doctor for early refills, going to multiple doctors for prescriptions, not doing as well at work, reduction of social activities, and even obtaining drugs from family members without permission.

 

HALF LIFE AND METABOLISM

The biological half-life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.

The half life of tramadol is between 6.3 and 7.4 hours.

Tramadol is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites. The major metabolic pathways appear to be N– and O-demethylation and glucuronidation or sulfation in the liver.

The CYP enzymes are the major enzymes involved in drug metabolism, and since many drugs may increase or decrease the activity of various CYP isozymes, this is a major source of adverse drug interactions, since changes in CYP enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels, possibly causing an overdose.

OPIOID INDUCED HYPERALGESIA

There is increasing medical research showing that taking opioids like tramadol for longer than six months will create a condition called Opioid Induced Hyperalgesia. This is a condition where the opioids actually make the pain receptors more sensitive and, therefore, make the pain greater. A person with this condition is required to take more and more of the opioid to try to address the pain but finds that the pain actually increases. The increased dosages increase the likelihood of addition and overdose.

 

SIDE EFFECTS

The drug label includes some of following side effects, and says that tramadol has the same effects of other opioids. Because tramadol also inhibits the reuptake of Serotonin and Norepinephrine (which results in an excess of Serotonin and Norepinephrene), it can also have the side effects of antidepressants. Side effects include:

  • allergic reactions such as pruritus, hives, bronchospasm, angioedema (fluid swelling under the skin), toxic epidermal necrolysis and Stevens-Johnson syndrome
  • anaphylaxis –  an acute allergic reaction that prompts the immune system to respond. The symptoms can include fainting, lightheadedness, low blood pressure, dizziness, or flushing, difficulty breathing, rapid breathing, shortness of breath or wheezing, hives, swelling under the skin, blue skin from poor circulation, or rashes, nausea or vomiting, fast heart rate, feeling of impending doom, itching, tongue swelling, difficulty swallowing, facial swelling, mental confusion, nasal congestion, or impaired voice.
  • anxiety
  • central nervous system and respiratory depression when combined with alcohol, hypnotics, narcotics, centrally acting analgesics, opioids or psychotropic drugs
  • constipation
  • delusions
  • diarrhea
  • dizziness
  • drowsiness
  • fainting
  • fast heart rate
  • fever
  • hallucinations
  • headache
  • impairment of the mental or physical ability to perform potentially hazardous tasks such as driving or operating machinery
  • increased risk of central nervous system and respiratory depression
  • loss of coordination
  • nausea
  • nervousness
  • numbness
  • orthostatic hypotension – low blood pressure upon standing causing dizziness and possibly fainting
  • overactive reflexes
  • paranoia
  • pruritis – severe itching of the skin
  • seizures (convulsions), at a normal dosage and above. Seizures are even more likely when the drug is combined with other opioids or with antidepressants (SSRIs, MAO Inhibitors, or TCAs).
  • serotonin syndrome – serotonin syndrome is a group of side effects that include, agitation or restlessness, confusion, rapid heart rate and high blood pressure, dilated pupils, loss of muscle coordination or twitching muscles, muscle rigidity, heavy sweating, diarrhea, headache, shivering, goose bumps, high fever, seizures, irregular heartbeat, and unconsciousness. Serotonin syndrome symptoms usually occur within several hours of taking a new drug or increasing the dose of a drug you’re already taking. The risk of serotonin syndrome is even higher if tramadol is taken with other serotonergic medications such as antidepressants Serotonergic drugs are used to treat migraine, depression and other mood disorders. Serotonin syndrome can be fatal if not treated immediately.
  • skin rash
  • slowed breathing
  • somnolence – sleepiness
  • spinning sensation
  • suicidal thoughts or actions
  • sweating
  • upset stomach
  • vomiting

 

WITHDRAWAL SYMPTOMS

Severity of withdrawal symptoms with tramadol can vary from person to person, depending on how long they’ve been taking the drug and at what dosage, as well as how they personally respond to the drug and to withdrawal. Generally, the symptoms can include:

  • aggressiveness
  • anxiety, sometimes severe
  • chills
  • depression
  • diarrhea
  • flu-like symptoms
  • hallucinations
  • headaches
  • insomnia
  • irritability
  • mood swings
  • nausea
  • nightmares
  • pain
  • panic attacks
  • paresthesias – tingling or pricking (“pins and needles”), caused chiefly by pressure on or damage to peripheral nerves
  • piloerection – hair standing on end
  • poor appetite
  • rigors – a sudden feeling of cold with shivering accompanied by a rise in temperature, often with copious sweating, especially at the onset or height of a fever.
  • sweating
  • tremors
  • upper respiratory symptoms

TREATMENT

Tramadol should never be stopped abruptly. Doctors advise lowering the dose very slowly, under their guidance and supervision. Even so, the withdrawal symptoms can be severe. A medical-supervised drug detoxification program can help make stopping tramadol safer and more comfortable. Call us to talk to a Detox Advisor.