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Adverse Effects and Precautions Interactions Pharmacokinetics Profile Profile Everolimus/lnolimomab 1959 2. Curran MP. Everolimus: in patients with subependymal giant cell was deemed to be clinically relevant and they advised tor; Votubia; Ukr. : Afinitor (A<jJHHHTOp); Certican (CepTHKaH); Paediatr Drugs astrocytoma associated with tuberous sclerosis complex. against use of these 2 drugs together. Sertikan (CeprmalH)t; USA: Afinitor; Zortress; Venez. : Certican. 2012; 14: 51-60. 3. Franz DN, et al. Efficacy and safety of everolimus for subependymal giant 1. Kovarik JM, et al. Blood concentrations of everolimus are markedly cell astrocytomas associated with tuberous sclerosis complex (EXIST- I): increased by ketoconazole. J Clin Pharmacol 2005; 45: 514-18. a multicentre, randomised, placebo-controlled phase 3 trial. Lancet2013 ; Gusperimus Hydrochloride (riNNMJ 381: 125-32. Rifampicin. In a pharmacokinetic study, 1 rifampicin 4. Bissler JJ, et al. Everolimus for angiomyoliporna associated with tuberous sclerosis complex or sporadic lymphangioleiomyomatosis increased the clearance of everolimus, decreasing exposure (EXIST-2): a multicentre, randomised. double-blind. placebo-controlled to everolimus by about 63%. trial. Lancet 2013; 381: 817-24. 1. Kovarik JM, et al. Effect of rifampin on apparent clearance of everolimus. Ann Pharmacother 2002; 36: 981-5. Adverse Effects and Precautions Veropomil. Verapamil increased the bioavailability of As for Sirolimus, see p. 1967.2. everolimus; the half-life of everolimus was essentially Other adverse effects that have been reported with unchanged. The dose of everolimus should be reduced everolimus include dehydration, fatigue, diabetes mellitus, when these two drugs are given together, but the amount chest pain, heart failure, dysgeusia, insomnia, conjunctiv­ should be determined by blood concentrations and clinical itis, nail disorders, haemoptysis, dyspnoea, and skin monitoring. Verapamil concentrations may also be affected disorders such as pruritus, palmar-plantar erythrodysesthe­ by everolimus, but the mechanism is unclear; any dose sia syndrome, and ameform dermatitis. adjustment of verapamil should be guided by blood pres­ Renal function, fasting glucose concentrations, and full sure monitoring.1 blood count should be measured at baseline and periodically I. Kovarik JM, et al. Pharmacokinetic interaction between verapantil and during treatment. everolimus in healthy subjects. Br J Clin Pharmaco/ 2005; 60: 434-7. Profile Effects on the lungs. Pulmonary toxicity is a well-known adverse effect in patients given sirolimus (p. 1967.3) and Pharmacokinetics Gusperimus is a guanidine derivative that irthibits both cell­ similar toxicity has occurred1·4 in patients given everoli­ Peak plasma concentrations of everolimus occur about I to mediated and antibody-mediated immunity. It is used in the mus. 2 hours after an oral dose. Plasma protein binding is about treatment of renal graft rejection, and has been investigated l. ExpOsito V, et a/. Everolimus-related pulmonary toxicity in heart 74%. Everolimus is metabolised in the liver and to some in the management of graft-versus-host disease and transplant recipients. J Heart Lung Transplant 2008; 27: 797-800. extent in the gastrointestinal wall, and is a substrate of P­ Wegener's granulomatosis. For mention of its role in 2. Otton J, et al. Everolimus-associated pneumonitis in 3 heart transplant reversing acute graft rejection in kidney transplantation, see J Heart Lung Transplant 28: glycoprotein and the cytochrome P450 isoenzyme CYP3A4. recipients. 2009; 104-6. p. 1935.2. 3. Vandewiele B, eta!. Diffuse alveolar hemorrhage induced by everolimus. Most metabolites are excreted in the faeces with small Chest 2010; 137: 456-9. amounts found in urine. The mean elimination half-life of Gusperimus is used as the hydrochloride. A dose of 3 to 4. Depuydt P, et al. Fatal acute pulmonary injury associated with everolimus is about 30 hours. 5 mg/kg of gusperimus hydrochloride given daily for 7 days, everolimus. Ann Pharmacother 2012; 46: e7. by intravenous infusion over 3 hours, has been suggested in References. the treatment of acute renal graft rejection. Treatment may Porphyrio. The Drug Database for Acute Porphyria, com­ I. Kovarik JM, et al. Clinical development of an everolimus pediatric formulation: relative bioavailability, food effect, and steady�state be continued for a further 3 days if requlred. piled by the Norwegian Porphyria Centre (NAPOS) and pharmacokinetics. J Clin Pharmaco/ 2003; 43: 141-7. Adverse effects reported with gusperimus include bone­ the Porphyria Centre Sweden, classifies everolimus as pos­ 2. Kirchner GL et al. Clinical pharmacokinetics of everolimus. Clin marrow depression, numbness of face and extremities, Pharmacokinet 2004; 43: 83-95. sibly porphyrinogenic; it should be used only when no headache, gastrointestinal disturbances, alterations in liver safer alternative is available and precautions should be 3. Moes DJAR, et al. Population pharmacokinetics and pharmacogenetics of everolimus in renal transplant patients. Clin Pharmacokinet 2012; 51: enzyme values, and facial flushing. Rapid injection should considered in vulnerable patients.' 467-80. be avoided as an acute increase in plasma concentration I. The Drug Database for Acute Porphyria. Available at: http://www. may produce respiratory depression. drugs-porphyria.org (accessed 05/10/11) Theropeutic drug monitoring. Licensed product informa­ References. lion recommends routine monitoring of whole blood ever­ I. Ramos EL, et al. Deoxyspergualin: mechanism of action and Interactions olimus concentrations when used as an immunosuppres­ pharmacokinetics. Transplant Proc 1996; 28: 873-5. et al. sant for transplantation, or for giant-cell astrocytoma. 2. Tanabe K, Effect of deoxyspergualin on the long-term outcome of Everolimus is a substrate of cytocluome P450 isoenzyme renal transplantation. Transplant Proc 2000; 12: 1745-6. CYP3A4 and a substrate and moderate inhibitor of P­ In heart, kidney, and liver transplantation patients 3. Amada N, et al. Prophylactic use of deoxyspergualin improves long-term glycoprotein. Plasma concentrations of everolimus may be with everolimus trough levels of 3 nanograms/mL or greater graft survival in living related renal transplant recipients transfused with TransplantProc affected by inducers or competitive inhibitors of CYP3A4 or have been found to have a lower incidence of acute donor-specific blood. 2001; 33: 2256-7. et al. rejection; an upper limit of 8nanograms/mL is recom­ 4. Birck: R, 15-Deoxyspergualin in patients with refractory ANCA­ P-glycoprotein. Exposure to everolimus is increased when associated systemic vasculitis: a six�month open-label trial to evaluate given with the CYP3A4/P-glycoprotein inhibitors ciclospor­ mended. Monitoring is considered especially important in safety and efficacy. JAm Soc Nephrol 2003; 14: 440-7. in, ketoconazole, erythromycin, and verapamil. Licensed those with hepatic impairment (see under Uses and 5. Schmitt WH, et al. Prolonged treatment of refractory Wegener's product information advises avoiding the use of everolimus Administration, p. 1958. 1) and if ciclosporin formulation or granulomatosis with 15-deoxyspergualin: an open study in seven Nephrol Dial Transplant 20: dosage is changed (see Administration with Everolimus, , patients. 2005; 1083-92. with CYP3A4 or P-glycoprotein irthibitors; dosage reduc­ 6. Amada N, et al. Deoxyspergualin prophylaxis with tacrolimus further tions have been suggested if use with a moderate CYP3A4 under Ciclosporin, p. 1946.3). improves long-term graft survival in living-related renal-transplant inhibitor is necessary. Substances that are potent inducers of In giant-cell astrocytoma doses should be adjusted to recipients transfused with donor-specific blood. TransplantProc 2005; 37: CYP3A4 or P-glycoprotein may decrease exposure to attain everolimus trough concentrations of 5 to 15 nano­ 927-9. et al. grams/mL (see under Uses and Administration, p. 1958.1). 7. Nojima M, Combined therapy of deoxyspergualin and everolimus; dosage increases have been suggested if use plasmapheresis: a useful treatment for antibody-mediated acute together cannot be avoided. For dose adjustments, see Uses Use of everolimus with some other drugs may affect rejection after kidney transplantation. Transplant Proc 2005; 37: 930-3. and Administration, p. 1958.1. trough concentrations, see Administration with Other 8. Kawagishi N, et al. Usage of deoxyspergualin on steroid-resistant acute Tohoku J Exp Med In vitro results suggest that systemic concentrations of Drugs, p. 1958.2. rejection in living donor liver transplantation. 2006; 208: 225-33. everolimus after usual oral doses are unlikely to irthibitP­ Further references. 9. Flossmann 0, et a!. Deoxyspergualin in relapsing and refractory glycoprotein, CYP3A4, or CYP2D6, but theoretically, l. Kovarik JM, et a[. Exposure-response relationships for everolimus in de Wegener's granulomatosis. Ann Rheum Dis 2009; 68: 1125-30. novo kidney transplantation: defining a therapeutic range. Transplanta� everolimus may affect the bioavailability of CYP3A4 or P­ 10. Flossmann 0, Jayne DRW. Long-term treatment of relapsing Wegener's tion 2002; 73: 920-5. Rheumatology (Oxford) glycoprotein substrates when given together. granulomatosis with 15-deoxyspergualin. 2010; 2. Kovarik JM, et al. Everolimus therapeutic concentration range defined 49: 556-62. Use with live vaccines should be avoided. from a prospective trial with reduced-exposure cyclosporine in-de novo References. kidney transplantation. TherDrug Monit 2004;
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