diprenorphine

Diprenorphine is a potent, non-selective opioid receptor antagonist primarily used in veterinary medicine to reverse the effects of extremely powerful opioids such as etorphine and carfentanil, which are often administered for tranquilizing large animals like elephants and rhinos. It is considered the strongest commercially available opioid antagonist, with an antagonistic potency approximately 100 times greater than nalorphine. Diprenorphine binds with high affinity to all three major opioid receptor subtypes—mu (MOR), kappa (KOR), and delta (DOR)—and acts mainly as an antagonist but also exhibits weak partial agonist activity, particularly at the kappa-opioid receptor. Due to its pharmacological profile and risk of producing some opioid effects or hallucinations in humans, it is not approved for human use; instead, naloxone or naltrexone are preferred for reversing opioid toxicity in people. Diprenorphine is supplied alongside etorphine or carfentanil specifically for use in wildlife immobilization procedures[1][2][4][5].

Brand names

Revivon

Other names

diprenorfin