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GENGRAF ORAL SOLUTION(十六)
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Other Drugs |
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fibric acid derivatives
(e.g.,bezafibrate, fenofibrate) |
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methotrexate |
Drugs That Alter Cyclosporine Concentrations
Compounds that decrease cyclosporine absorption such as orlistat should be avoided. Cyclosporine is extensively metabolized by cytochrome P-450 III-A. Substances that inhibit this enzyme could decrease metabolism and increase cyclosporine concentrations. Substances that are inducers of cytochrome P-450 activity could increase metabolism and decrease cyclosporine concentrations. Monitoring of circulating cyclosporine concentrations and appropriate Gengraf (cyclosporine oral solution, USP [MODIFIED]) dosage adjustment are essential when these drugs are used concomitantly (see DOSAGE AND ADMINISTRATION - Blood Concentration Monitoring).
Drugs That Increase Cyclosporine Concentrations
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Calcium Channel Blockers |
Antifungals |
Antibiotics |
Glucocorticoids |
Other Drugs |
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diltiazem |
fluconazole |
azithromycin |
methylprednisolone |
allopurinol |
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nicardipine |
itraconazole |
clarithromycin |
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bromocriptine |
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verapamil |
ketoconazole |
erythromycin |
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danazol |
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voriconazole |
quinupristin/ |
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metoclopramide |
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dalfopristin |
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colchicine |
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amiodarone |
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imatinib |
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oral contraceptives |
The HIV protease inhibitors (e.g., indinavir, nelfinavir, ritonavir, and saquinavir) are known to inhibit cytochrome P-450 III-A and thus could potentially increase the concentrations of cyclosporine, however no formal studies of the interaction are available. Care should be exercised when these drugs are administered concomitantly.
Grapefruit and grapefruit juice affect metabolism, increasing blood concentrations of cyclosporine, thus should be avoided.
Drugs/Dietary Supplements That Decrease Cyclosporine Concentrations
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Antibiotics |
Anticonvulsants |
Other Drugs |
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nafcillin |
carbamazepine |
octreotide |
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rifampin |
phenobarbital |
ticlopidine |
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phenytoin |
orlistat |
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sulf |
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