Morphinan Derivatives for the Treatment of Drug Overdose

A method of treating an opioid toxicity or overdose in a subject in need thereof comprising administrating a first opioid receptor antagonist followed by a compound of Formula I:

• or a pharmaceutically acceptable salt, ester or prodrug thereof wherein;
• R1 is —(CH2)n-c-C3H5, —(CH2)n-c-C4H7, —(CH2)n-c-C5H9, —(CH2)n—CH═CH2 or —(CH2)n—CH═C(CH3)2 wherein n is independently 0, 1, 2 or 3;
• R2 is —CONH2 or —CSNH2;
• R3 and R4 are independently H, —OH or together R3 and R4 form an —O— or —S— group;
• R5 is H or C1-C8 alkyl;
• and
• R6 and R7 are independently H, —OH, OCH3 or together R6 and R7 form a ═O or ═CH2 group.