Acute liver injury with jaundice associated with everolimus therapy has not been described, and the serum enzyme elevations associated with its use are usually mild and transient, resolving spontaneously or with dose modification. Because everolimus can lead to reactivation of chronic hepatitis B, routine screening of patients for HBsAg before starting therapy is advisable, particularly those undergoing organ transplantation. Patients who develop reactivation should be treated with an oral nucleoside analogue with potent activity against hepatitis B (entecavir or tenofovir). Everolimus is a macrolide similar in structure and function to sirolimus and temsirolimus, but these agents do not always exhibit cross sensitivity to adverse effects.
Agents used specifically for the prophylaxis against allograft rejection include cyclosporine, everolimus, mycophenolate mofetil, sirolimus and tacrolimus, as well as azathioprine and corticosteroids.
References regarding the safety and potential hepatotoxicity of the cyclosporine, everolimus, mycophenolate mofetil, sirolimus and tacrolimus are provided together at the end of the Overview section on drugs used to prevent transplant rejection.
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GnRH agonists are synthetically modeled after the natural GnRH decapeptide with specific modifications, typically in position 6 (amino acid substitution), 9 (alkylation) and 10 (deletion). These substitutions inhibit rapid degradation. Agonists with two substitutions include: leuprolide (Lupron, Eligard), buserelin (Suprefact, Suprecor), histrelin (Supprelin LA, Vantas), goserelin (Zoladex), and deslorelin (Suprelorin, Ovuplant). The agents nafarelin (Synarel) and triptorelin are agonists with single substitutions at position 6.