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Kaletra and Tacrolimus Intravenous

Determining the interaction of Kaletra and Tacrolimus Intravenous and the possibility of their joint administration.

Check result:
Kaletra <> Tacrolimus Intravenous
Relevance: 06.08.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Consumer information for this interaction is not currently available.MONITOR CLOSELY: Coadministration with protease inhibitors (PIs) may significantly increase the blood concentrations of tacrolimus. The proposed mechanism is PI inhibition of intestinal and hepatic CYP450 3A4, the isoenzyme responsible for the metabolic clearance of tacrolimus. Enhanced tacrolimus oral bioavailability due to inhibition of intestinal P-glycoprotein (P-gp) efflux transporter may also contribute. There have been numerous reports of tacrolimus interaction with various PI-containing regimens in the medical literature, which necessitated substantial (> 10-fold) reductions or interruptions in tacrolimus dosing. MANAGEMENT: Caution is advised when tacrolimus is used with protease inhibitors (PIs). Dosage reduction and/or prolongation of the dosing interval for tacrolimus will likely be required. Tacrolimus blood levels and renal function should be checked frequently and the dosage adjusted accordingly, particularly following initiation or discontinuation of PI therapy. Patients should be closely monitored for development of serious adverse effects such as nephrotoxicity, lymphoma and other malignancies, infections, diabetes, neurotoxicity (tremor, paraesthesia, encephalopathy, delirium, coma), hyperkalemia, QT prolongation, myocardial hypertrophy, and hypertension. Patients should be advised to seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitation, irregular heart rhythm, shortness of breath, or syncope. References Cakaloglu Y, Tredger JM, Devlin J, Williams R "Importance of cytochrome p-450IIIA activity in determining dosage and blood levels of FK 506 and cyclosporine in liver transplant recipients." Hepatology 20 (1994): 309-16 Teicher E, Vincent I, Bonhomme-Faivre L, et al. "Effect of Highly Active Antiretroviral Therapy on Tacrolimus Pharmacokinetics in Hepatitis C Virus and HIV Co-Infected Liver Transplant Recipients in the ANRS HC-08 Study." Clin Pharmacokinet 46 (2007): 941-52 Jain AK, Venkataramanan R, Shapiro R, et al. "Interaction between tacrolimus and antiretroviral agents in human immunodeficiency virus-positive liver and kidney transplantation patients." Transplant Proc 34 (2002): 1540-1 Barau C, Blouin P, Creput C, Taburet AM, Durrbach A, Furlan V "Effect of coadministered HIV-protease inhibitors on tacrolimus and sirolimus blood concentrations in a kidney transplant recipient." Fundam Clin Pharmacol 23 (2009): 423-5 "Product Information. Fortovase (saquinavir)" Roche Laboratories, Nutley, NJ. "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb, Princeton, NJ. "Product Information. Lexiva (fosamprenavir)." GlaxoSmithKline, Research Triangle Park, NC. Pea F, Tavio M, Pavan F, et al. "Drop in trough blood concentrations of tacrolimus after switching from nelfinavir to fosamprenavir in four HIV-infected liver transplant patients." Antivir Ther 13 (2008): 739-42 Jain AK, Venkataramanan R, Shapiro R, et al. "The interaction between antiretroviral agents and tacrolimus in liver and kidney transplant patients." Liver Transpl 8 (2002): 841-5 Tsapepas DS, Webber AB, Aull MJ, Figueiro JM, Saal SD "Managing the atazanavir-tacrolimus drug interaction in a renal transplant recipient." Am J Health Syst Pharm 68 (2011): 138-42 "Product Information. Prezista (darunavir)." Ortho Biotech Inc, Bridgewater, NJ. "Product Information. Agenerase (amprenavir)." Glaxo Wellcome, Research Triangle Pk, NC. "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA. "Product Information. Prograf (tacrolimus)." Fujisawa, Deerfield, IL. "Product Information. Crixivan (indinavir)." Merck & Co, Inc, West Point, PA. Mertz D, Battegay M, Marzolini C, Mayr M "Drug-Drug Interaction in a Kidney Transplant Recipient Receiving HIV Salvage Therapy and Tacrolimus." Am J Kidney Dis (2009): "Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL. Jain AB, Venkataramanan R, Eghtesad B, et al. "Effect of coadministered lopinavir and ritonavir (Kaletra) on tacrolimus blood concentration in liver transplantation patients." Liver Transpl 9 (2003): 954-60 Schonder KS, Shullo MA, Okusanya O "Tacrolimus and lopinavir/ritonavir interaction in liver transplantation." Ann Pharmacother 37 (2003): 1793-6 View all 19 references

Professional:

MONITOR CLOSELY: Coadministration with protease inhibitors (PIs) may significantly increase the blood concentrations of tacrolimus. The proposed mechanism is PI inhibition of intestinal and hepatic CYP450 3A4, the isoenzyme responsible for the metabolic clearance of tacrolimus. Enhanced tacrolimus oral bioavailability due to inhibition of intestinal P-glycoprotein (P-gp) efflux transporter may also contribute. There have been numerous reports of tacrolimus interaction with various PI-containing regimens in the medical literature, which necessitated substantial (> 10-fold) reductions or interruptions in tacrolimus dosing.

MANAGEMENT: Caution is advised when tacrolimus is used with protease inhibitors (PIs). Dosage reduction and/or prolongation of the dosing interval for tacrolimus will likely be required. Tacrolimus blood levels and renal function should be checked frequently and the dosage adjusted accordingly, particularly following initiation or discontinuation of PI therapy. Patients should be closely monitored for development of serious adverse effects such as nephrotoxicity, lymphoma and other malignancies, infections, diabetes, neurotoxicity (tremor, paraesthesia, encephalopathy, delirium, coma), hyperkalemia, QT prolongation, myocardial hypertrophy, and hypertension. Patients should be advised to seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitation, irregular heart rhythm, shortness of breath, or syncope.

References
  • Cakaloglu Y, Tredger JM, Devlin J, Williams R "Importance of cytochrome p-450IIIA activity in determining dosage and blood levels of FK 506 and cyclosporine in liver transplant recipients." Hepatology 20 (1994): 309-16
  • Teicher E, Vincent I, Bonhomme-Faivre L, et al. "Effect of Highly Active Antiretroviral Therapy on Tacrolimus Pharmacokinetics in Hepatitis C Virus and HIV Co-Infected Liver Transplant Recipients in the ANRS HC-08 Study." Clin Pharmacokinet 46 (2007): 941-52
  • Jain AK, Venkataramanan R, Shapiro R, et al. "Interaction between tacrolimus and antiretroviral agents in human immunodeficiency virus-positive liver and kidney transplantation patients." Transplant Proc 34 (2002): 1540-1
  • Barau C, Blouin P, Creput C, Taburet AM, Durrbach A, Furlan V "Effect of coadministered HIV-protease inhibitors on tacrolimus and sirolimus blood concentrations in a kidney transplant recipient." Fundam Clin Pharmacol 23 (2009): 423-5
  • "Product Information. Fortovase (saquinavir)" Roche Laboratories, Nutley, NJ.
  • "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb, Princeton, NJ.
  • "Product Information. Lexiva (fosamprenavir)." GlaxoSmithKline, Research Triangle Park, NC.
  • Pea F, Tavio M, Pavan F, et al. "Drop in trough blood concentrations of tacrolimus after switching from nelfinavir to fosamprenavir in four HIV-infected liver transplant patients." Antivir Ther 13 (2008): 739-42
  • Jain AK, Venkataramanan R, Shapiro R, et al. "The interaction between antiretroviral agents and tacrolimus in liver and kidney transplant patients." Liver Transpl 8 (2002): 841-5
  • Tsapepas DS, Webber AB, Aull MJ, Figueiro JM, Saal SD "Managing the atazanavir-tacrolimus drug interaction in a renal transplant recipient." Am J Health Syst Pharm 68 (2011): 138-42
  • "Product Information. Prezista (darunavir)." Ortho Biotech Inc, Bridgewater, NJ.
  • "Product Information. Agenerase (amprenavir)." Glaxo Wellcome, Research Triangle Pk, NC.
  • "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA.
  • "Product Information. Prograf (tacrolimus)." Fujisawa, Deerfield, IL.
  • "Product Information. Crixivan (indinavir)." Merck & Co, Inc, West Point, PA.
  • Mertz D, Battegay M, Marzolini C, Mayr M "Drug-Drug Interaction in a Kidney Transplant Recipient Receiving HIV Salvage Therapy and Tacrolimus." Am J Kidney Dis (2009):
  • "Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL.
  • Jain AB, Venkataramanan R, Eghtesad B, et al. "Effect of coadministered lopinavir and ritonavir (Kaletra) on tacrolimus blood concentration in liver transplantation patients." Liver Transpl 9 (2003): 954-60
  • Schonder KS, Shullo MA, Okusanya O "Tacrolimus and lopinavir/ritonavir interaction in liver transplantation." Ann Pharmacother 37 (2003): 1793-6
Kaletra

Generic Name: lopinavir / ritonavir

Brand name: Kaletra

Synonyms: n.a.

Tacrolimus Intravenous

Generic Name: tacrolimus

Brand name: Astagraf XL, Envarsus XR, Prograf, Hecoria

Synonyms: Tacrolimus (oral and injection), Tacrolimus (Systemic)

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

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