Peripheral Opioid Receptor Antagonists

Peripheral Opioid Receptor Antagonists
Accession Number

Opioid receptor antagonists which act primarily on peripheral receptors due to limited ability to cross the blood brain barrier. Typically used to treat opioid-induced constipation.

ATC Classification
DrugDrug Description
AlvimopanAn opioid antagonist used to reduce healing time of the upper and lower gastrointestinal tract following surgical procedures that involve bowel resection with primary anastomosis.
MethylnaltrexoneA μ-opioid antagonist used for the treatment of opioid-induced constipation in palliative patients that are inadequately responding to laxative therapy.
NaloxegolA peripherally-selective opioid antagonist used to treat opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.
NaloxoneAn opioid receptor antagonist used to rapidly reverse an opioid overdose. Also included in some drug formulations as an abuse deterrent to prevent injection.
NaldemedineAn opioid antagonist used to to treat opioid-induced constipation.
Drugs & Drug Targets
AlvimopanMu-type opioid receptortarget
AlvimopanKappa-type opioid receptortarget
AlvimopanDelta-type opioid receptortarget
MethylnaltrexoneMu-type opioid receptortarget
MethylnaltrexoneKappa-type opioid receptortarget
NaloxegolCytochrome P450 3A4enzyme
NaloxegolCytochrome P450 2D6enzyme
NaloxegolCytochrome P450 2C19enzyme
NaloxegolMu-type opioid receptortarget
NaloxoneMu-type opioid receptortarget
NaloxoneEstrogen receptor alphatarget
NaloxoneCyclic AMP-responsive element-binding protein 1target
NaloxoneDelta-type opioid receptortarget
NaloxoneSolute carrier organic anion transporter family member 1A2transporter
NaloxoneP-glycoprotein 1transporter
NaloxoneKappa-type opioid receptortarget
NaloxoneCytochrome P450 3A4enzyme
NaloxoneSerum albumincarrier
NaloxoneToll-like receptor 4target
NaloxoneLiver carboxylesterase 1target
NaloxoneUDP-glucuronosyltransferase 1-1enzyme
NaloxoneCytochrome P450 2C18enzyme
NaloxoneCytochrome P450 2C19enzyme
NaldemedineCytochrome P450 3A Subfamilyenzyme
NaldemedineUDP-glucuronosyltransferase 1-3enzyme
NaldemedineMu-type opioid receptortarget
NaldemedineDelta-type opioid receptortarget
NaldemedineKappa-type opioid receptortarget
NaldemedineATP-binding cassette sub-family B member 5transporter