List of Opioid Tolerant Pain Medications

Opioid medication is prescribed regularly throughout the world for short-term and chronic pain conditions. Opioids bind to receptors in the central nervous system to decrease the pain signals. A similar but separate product is an opiate, which is a natural byproduct of opium products, whereas an opioid is a synthetic chemical.

Causes of Tolerance

• Tolerance is commonly attributed to two separate categories: inherited factors (factors present in the patient prior to the use of opioids) and compensatory changes (resulting from use).

  Inherited factors in tolerance result from genetic issues within the body’s makeup, such as differences in the brain cell opioid receptors or a genetic predisposition to tolerance based on prior use by the mother of the patient.

  Compensatory changes in tolerance result from the use of opioids to reduce pain. Over time, opioid use results in a rise of cholecystokinin (CCK) levels in the gastrointestinal tract, an area that also attaches opioid receptors. The rise in CCK levels leads to the tolerance and an increase in anti-opioid activity in the brain.
  One way to decrease tolerance is to lower the amount of pain medication being administered. The largest complaint about this method is that it does not help the pain, only increases it due to less pain medication being received. Because of this, the most common way to deal with opioid tolerance is to switch to an alternate medicine.

Tramadol

• Tramadol is a non-narcotic pain reliever that has opioid-receptor properties. It is used for moderate to moderately severe pain and has off-label uses for opioid withdrawal/anti-depressant withdrawal.

Progulmide

• Progulmide is a CCK antagonist originally intended for stomach ulcer use that has a side effect of preventing and reversing tolerance of opioid tolerance. When administered alongside narcotics, it can enhance the analgesic pain-relieving effects of the medication.

Ketamine

• The use of ketamine administered along with opioids in extremely low doses has been found to lower the likelihood of opioid tolerance. Ketamine is a drug used primarily in anesthesia, but it also has sedative and analgesic properties.