How does methadone work?
Like other opioids, methadone acts by binding to opioid receptors. Specifically, it binds to mu-type opioid receptors located on nerve cells. This binding inhibits the nerve cells’ excitability and the transmission of pain signals to the brain, resulting in less pain.
Methadone in clinical trials
A randomized, placebo-controlled clinical trial (NCT00761085) assessed the effect of methadone in children and adults with sickle cell disease and other types of sickle cell disease who experience a vaso-occlusive crisis (VOC). Participants were assigned to receive either a single dose of methadone injected into the bloodstream in addition to standard pain therapy (morphine or hydromorphone) or standard pain therapy alone. In the morning following a VOC, participants received a single dose of 0.1 mg per kilogram of body weight of methadone. The dose was escalated up to 0.125 mg/kg if the patient’s pain wasn’t entirely under control and had no respiratory depression up to eight hours after the first methadone administration.
A total of 12 children and 11 adults were treated with methadone in addition to standard pain therapy, and 12 children and 12 adults were treated with standard pain therapy alone. The pain was assessed on a scale of 1 (no pain) to 5 (highest pain).
Results of the study, published in the journal Pediatric Blood & Cancer, showed that in children, pain relief was significantly higher at 12, 24 and 48 hours after receiving methadone than in the control group. Adults in the methadone group experienced no difference in pain relief compared with the control group.
Methadone should not be used longer than necessary, as prolonged use can result in dependency.
Methadone use may cause severe breathing problems. Breathing should be carefully monitored while taking the medication, especially during the first 24 to 72 hours of treatment and after a dose increase.
Common side effects of methadone include weight gain, stomach pain, headache, mood changes, and vision problems. Additional side effects include seizures, extreme drowsiness, and swelling of the eyes, throat, face, mouth or tongue. These side effects can be severe and might require immediate medical attention.
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