Home›Rapamycin

Rapamycin

mTOR Inhibitor ImmunosuppressantKinase InhibitormTOR Inhibitors

Route: Oral

58 interactions on record⛔ Black Box Warning

Rapamycin has 58 known drug interactions based on U.S. FDA drug labeling data. Of these, 16 are contraindicated combinations that should be avoided entirely. 5 are classified as major interactions requiring close medical supervision. Notable interactions include combinations with Boceprevir, Clarithromycin, Erythromycin. Patients taking Rapamycin should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 58
Contraindicated: 16
Major: 5
Moderate: 31

Contraindicated (16)

Rapamycin + Boceprevir— Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.
Rapamycin + Clarithromycin— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…
Rapamycin + Erythromycin— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…
Rapamycin + Grapefruit Juice— Grapefruit juice inhibits CYP3A4-mediated metabolism of sirolimus and must not be taken with or used for dilution of sir…
Rapamycin + Indinavir— Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.
Rapamycin + Itraconazole— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…
Rapamycin + Ketoconazole— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…
Rapamycin + Mifepristone— Mifepristone increases sirolimus exposure; concomitant use is contraindicated due to narrow therapeutic range.
Rapamycin + Posaconazole— Posaconazole increases sirolimus blood concentrations approximately 9-fold, resulting in sirolimus toxicity.
Rapamycin + Posaconazole Delayed-Release— Posaconazole increases sirolimus blood concentrations approximately 9-fold, resulting in sirolimus toxicity. Contraindic…
Rapamycin + Rifabutin— Strong CYP3A4/P-gp inducer that decreases sirolimus concentrations. Avoid concomitant use; consider alternative agents.
Rapamycin + Rifampin— Strong CYP3A4/P-gp inducer that decreases sirolimus concentrations. Avoid concomitant use; consider alternative agents.
Rapamycin + Ritonavir— Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.
Rapamycin + Telaprevir— Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.
Rapamycin + Telithromycin— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…
Rapamycin + Voriconazole— Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents…

Major (5)

Rapamycin + Benazepril Hydrochloride And Hydrochlorothiazide— mTOR inhibitor coadministration with ACE inhibitor may increase risk for angioedema.
Rapamycin + Cannabidiol— May increase sirolimus blood levels. Therapeutic drug monitoring and sirolimus dose reduction should be considered.
Rapamycin + Cyclosporine— Cyclosporine increases sirolimus concentrations. Sirolimus should be taken 4 hours after cyclosporine administration. Do…
Rapamycin + Grapefruit Products— Grapefruit is a CYP3A4 inhibitor that may increase sirolimus concentrations, increasing the risk of adverse reactions. C…
Rapamycin + Ranolazine— CYP3A substrate with narrow therapeutic range. Dose adjustment may be required as ranolazine increases plasma concentrat…

Moderate (31)

Rapamycin + Benazepril Hydrochloride— 7.5 Mammalian Target of Rapamycin (mTOR) Inhibitors Patients receiving coadministration of ACE inhibitor and mTOR inhibi…
Rapamycin + Bromocriptine— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Carbamazepine— Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Cimetidine— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Cisapride— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Cotrimoxazole— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Danazol— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Deferasirox— Deferasirox may induce CYP3A4 resulting in decreased sirolimus concentration. Monitor for reduced effectiveness.
Rapamycin + Diltiazem— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Dronedarone— Monitor and adjust dosage as needed. Dronedarone is a CYP3A and P-gp inhibitor that increases exposure of narrow therape…
Rapamycin + Enalapril Maleate— mTOR (Mammalian Target of Rapamycin) Inhibitors Patients receiving coadministration of ACE inhibitor and mTOR inhibitor …
Rapamycin + Enalapril Maleate And Hydrochlorothiazide— mTOR (mammalian target of rapamycin) inhibitors: Patients receiving coadministration of ACE inhibitor and mTOR inhibitor…
Rapamycin + Fluconazole— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Isavuconazonium Sulfate— Increase in sirolimus exposure. Monitor drug concentrations and adjust dose as needed.
Rapamycin + Letermovir— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Lisinopril And Hydrochlorothiazide Tablets— mTOR (mammalian target of rapamycin) inhibitors: Patients receiving coadministration of ACE inhibitor and mTOR inhibitor…
Rapamycin + Methenamine, Sodium Phosphate, Monobasic, Monohydrate, Phenyl Salicylate, Methylene Blue, And Hyoscyamine Sulfate— Methylene blue inhibits CYP3A4/5 metabolism. Sirolimus has narrow therapeutic index; clinical relevance unknown but conc…
Rapamycin + Metoclopramide— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Micafungin— Micafungin increases sirolimus AUC by 21%. Monitor for sirolimus toxicity and reduce dosage if necessary.
Rapamycin + Micafungin Sodium— Micafungin increases sirolimus AUC by 21%. Monitor for toxicity and reduce sirolimus dosage if necessary.
Rapamycin + Nicardipine— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Palbociclib— Sensitive CYP3A substrate with narrow therapeutic index. Dose may need reduction when coadministered with palbociclib.
Rapamycin + Perindopril Erbumine— 7.9 mTOR Inhibitors Patients taking concomitant mTOR (mammalian target of rapamycin) inhibitor therapy may be at increas…
Rapamycin + Phenobarbital— Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Phenytoin— Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Rifapentine— Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + St. John'S Wort— Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Trandolapril— Mammalian Target of Rapamycin (mTOR) Inhibitors Patients taking concomitant mTOR inhibitor (e.g., temsirolimus, sirolimu…
Rapamycin + Trandolapril And Verapamil Hydrochloride— Mammalian Target of Rapamycin (mTOR) Inhibitors Patients taking concomitant mTOR inhibitor (e.g., temsirolimus, sirolimu…
Rapamycin + Troleandomycin— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.
Rapamycin + Verapamil— Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations; verapamil concentrations may also increa…

Rapamycin + Boceprevir⛔Contraindicated

Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.

Rapamycin + Clarithromycin⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Erythromycin⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Grapefruit Juice⛔Contraindicated

Grapefruit juice inhibits CYP3A4-mediated metabolism of sirolimus and must not be taken with or used for dilution of sirolimus.

Rapamycin + Indinavir⛔Contraindicated

Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.

Rapamycin + Itraconazole⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Ketoconazole⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Mifepristone⛔Contraindicated

Mifepristone increases sirolimus exposure; concomitant use is contraindicated due to narrow therapeutic range.

Rapamycin + Posaconazole⛔Contraindicated

Posaconazole increases sirolimus blood concentrations approximately 9-fold, resulting in sirolimus toxicity.

Rapamycin + Posaconazole Delayed-Release⛔Contraindicated

Posaconazole increases sirolimus blood concentrations approximately 9-fold, resulting in sirolimus toxicity. Contraindicated.

Rapamycin + Rifabutin⛔Contraindicated

Strong CYP3A4/P-gp inducer that decreases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Rifampin⛔Contraindicated

Strong CYP3A4/P-gp inducer that decreases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Ritonavir⛔Contraindicated

Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.

Rapamycin + Telaprevir⛔Contraindicated

Protease inhibitor and strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use.

Rapamycin + Telithromycin⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Voriconazole⛔Contraindicated

Strong CYP3A4/P-gp inhibitor that increases sirolimus concentrations. Avoid concomitant use; consider alternative agents.

Rapamycin + Benazepril Hydrochloride And Hydrochlorothiazide⚠️Major

mTOR inhibitor coadministration with ACE inhibitor may increase risk for angioedema.

Rapamycin + Cannabidiol⚠️Major

May increase sirolimus blood levels. Therapeutic drug monitoring and sirolimus dose reduction should be considered.

Rapamycin + Cyclosporine⚠️Major

Cyclosporine increases sirolimus concentrations. Sirolimus should be taken 4 hours after cyclosporine administration. Dose adjustment may be needed if cyclosporine is withdrawn.

Rapamycin + Grapefruit Products⚠️Major

Grapefruit is a CYP3A4 inhibitor that may increase sirolimus concentrations, increasing the risk of adverse reactions. Concomitant use should be avoided.

Rapamycin + Ranolazine⚠️Major

CYP3A substrate with narrow therapeutic range. Dose adjustment may be required as ranolazine increases plasma concentrations.

Rapamycin + Benazepril Hydrochloride🟡Moderate

7.5 Mammalian Target of Rapamycin (mTOR) Inhibitors Patients receiving coadministration of ACE inhibitor and mTOR inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy may be at increased risk for angioedema.

Rapamycin + Bromocriptine🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Carbamazepine🟡Moderate

Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Cimetidine🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Cisapride🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Cotrimoxazole🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Danazol🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Deferasirox🟡Moderate

Deferasirox may induce CYP3A4 resulting in decreased sirolimus concentration. Monitor for reduced effectiveness.

Rapamycin + Diltiazem🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Dronedarone🟡Moderate

Monitor and adjust dosage as needed. Dronedarone is a CYP3A and P-gp inhibitor that increases exposure of narrow therapeutic index substrates.

Rapamycin + Enalapril Maleate🟡Moderate

mTOR (Mammalian Target of Rapamycin) Inhibitors Patients receiving coadministration of ACE inhibitor and mTOR inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy may be at increased risk for angioedema (see WARNINGS, Head and Neck Angioedema ).

Rapamycin + Enalapril Maleate And Hydrochlorothiazide🟡Moderate

mTOR (mammalian target of rapamycin) inhibitors: Patients receiving coadministration of ACE inhibitor and mTOR inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy may be at increased risk for angioedema (see WARNINGS ).

Rapamycin + Fluconazole🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Isavuconazonium Sulfate🟡Moderate

Increase in sirolimus exposure. Monitor drug concentrations and adjust dose as needed.

Rapamycin + Letermovir🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Lisinopril And Hydrochlorothiazide Tablets🟡Moderate

Rapamycin + Methenamine, Sodium Phosphate, Monobasic, Monohydrate, Phenyl Salicylate, Methylene Blue, And Hyoscyamine Sulfate🟡Moderate

Methylene blue inhibits CYP3A4/5 metabolism. Sirolimus has narrow therapeutic index; clinical relevance unknown but concurrent use requires caution.

Rapamycin + Metoclopramide🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Micafungin🟡Moderate

Micafungin increases sirolimus AUC by 21%. Monitor for sirolimus toxicity and reduce dosage if necessary.

Rapamycin + Micafungin Sodium🟡Moderate

Micafungin increases sirolimus AUC by 21%. Monitor for toxicity and reduce sirolimus dosage if necessary.

Rapamycin + Nicardipine🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Palbociclib🟡Moderate

Sensitive CYP3A substrate with narrow therapeutic index. Dose may need reduction when coadministered with palbociclib.

Rapamycin + Perindopril Erbumine🟡Moderate

7.9 mTOR Inhibitors Patients taking concomitant mTOR (mammalian target of rapamycin) inhibitor therapy may be at increased risk for angioedema [see Warnings and Precautions (5.1) ].

Rapamycin + Phenobarbital🟡Moderate

Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Phenytoin🟡Moderate

Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Rifapentine🟡Moderate

Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + St. John'S Wort🟡Moderate

Weak/moderate CYP3A4/P-gp inducer that may decrease sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Trandolapril🟡Moderate

Mammalian Target of Rapamycin (mTOR) Inhibitors Patients taking concomitant mTOR inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy may be at increased risk for angioedema (see Warnings – Head and Neck Angioedema).

Rapamycin + Trandolapril And Verapamil Hydrochloride🟡Moderate

Rapamycin + Troleandomycin🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations. Monitor and adjust dosage as needed.

Rapamycin + Verapamil🟡Moderate

Weak/moderate CYP3A4/P-gp inhibitor that may increase sirolimus concentrations; verapamil concentrations may also increase. Monitor and adjust dosage as needed.

Rapamycin + Amlodipine And Benazepril Hydrochlorideℹ️Unknown

Mammalian Target of Rapamycin (mTOR) Inhibitors: The risk of angioedema may be increased in patients receiving coadministration of ACE inhibitors and mTOR inhibitors (e.g., temsirolimus, sirolimus, everolimus).

Rapamycin + Lisinoprilℹ️Unknown

7.7 Mammalian Target of Rapamycin (mTOR) Inhibitors Patients taking concomitant mTOR inhibitor (e.g.

Rapamycin + Ritonavir 100 Mgℹ️Unknown

Immunosuppressants: cyclosporine, tacrolimus, sirolimus (rapamycin) ↑ immunosuppressants Therapeutic concentration monitoring is recommended for immunosuppressant agents when co-administered with ritonavir.

Rapamycin + Temsirolimusℹ️Unknown

7.3 Angioedema with ACE inhibitors and Calcium Channel Blockers Angioedema has been reported in patients taking mammalian target of rapamycin (mTOR) inhibitors in combination with ramipril and/or amlodipine.

Rapamycin + Temsirolimus Injectionℹ️Unknown

7.3 Angioedema with ACE inhibitors and Calcium Channel Blokers Angioedema has been reported in patients taking mammalian target of rapamycin (mTOR) inhibitors in combination with ramipril and/or amlodipine.

Rapamycin + Verapamil Hydrochlorideℹ️Unknown

Mammalian target of rapamycin (mTOR) inhibitors: In a study of 25 healthy volunteers with co-administration of verapamil with sirolimus, whole blood sirolimus C max and AUC were increased 130% and 120%, respectively.

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine. For informational purposes only. Always consult your pharmacist or physician.