Treatment Methylfentanyls

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Methylfentanyls

Found in:  

Fentanyl

Type/Reason added:  

Fentanyl Analog

Relative Potency:  

α-methylfentanyl:
similar to fentanyl, but more toxic (11)

(+)-cis-3-methylfentanyl: 20 times stronger than fentanyl
(-)-cis-3-methylfentanyl: about 20% of fentanyl (11)

(±)-trans-3-methylfentanyl:
similar to fentanyl (11)

Overview

The Effects

Treatment Options

Supportive Care:

Airway management and assisted ventilation, supplemental oxygen to correct hypoxia, cardiac monitoring and IV fluid administration to stabilize blood pressure and heart rate.

Antidote:

Naloxone, an opioid antagonist. Given their potency and long duration of action, multiple doses or a continuous naloxone infusion may be necessary.

Pharmacokinetics and Dynamics

Metabolism:

Mainly metabolized in the liver by CYP3A4. Some will undergo metabolism via CYP 3A5, CYP 2D6, CYP 2C19. Phase II glucuronic acid conjugates are also detected for hydroxylated metabolites.

Drug-Drug Interactions:

Methylfentanyls interact dangerously with other central nervous system depressants such as alcohol, benzodiazepines, and other opioids. These combinations drastically increase the risk of respiratory depression, coma, and death.