Calcineurin inhibitor immunosuppressant

Cyclosporine: What to Know Before You Take It

Also sold as Neoral, Sandimmune, Gengraf

What Cyclosporine Is Used For

1 INDICATIONS AND USAGE VEVYE indicated for the treatment of the signs and symptoms of dry eye disease. VEVYE (cyclosporine ophthalmic solution) 0.1% is a calcineurin inhibitor immunosuppressant indicated for the treatment of the signs and symptoms of dry eye disease. ( 1 )

Warnings

5 WARNINGS AND PRECAUTIONS Care should be taken to not touch the eye or other surfaces with the bottle tip to avoid potential for eye injury and/or contamination. ( 5.1 ) 5.1 Potential for Eye Injury and Contamination To avoid the potential for eye injury and/or contamination, patients should not touch the bottle tip to the eye or other surfaces. 5.2 Use with Contact Lenses VEVYE should not be administered while wearing contact lenses. If contact lenses are worn, they should be removed prior to administration of the solution. Lenses may be reinserted 15 minutes following administration of VEVYE ophthalmic solution.

Contraindications

4 CONTRAINDICATIONS None. None. ( 4 )

Cyclosporine Drug Interactions (36)

Cyclosporine + Simvastatin

Concomitant use of cyclosporine, danazol or gemfibrozil [see DRUG INTERACTIONS ( 7.1 )].

Contraindicated interaction

Cyclosporine + Atorvastatin

Concomitant use of cyclosporine, gemfibrozil, tipranavir plus ritonavir, or glecaprevir plus pibrentasvir with atorvastatin is not recommended.

Major interaction

Cyclosporine + Clarithromycin

Gastroprokinetic Agents: Cisapride Contraindicated Cisapride: [See Contraindications ( 4.2 )] Lipid-lowering agents: Lomitapide Lovastatin Simvastatin Contraindicated Lomitapide, Lovastatin, Simvastatin: Clarithromycin may increase the exposure of these drugs by inhibition of CYP3A metabolism, thereby increasing the risk of toxicities from these drugs [see Contraindications ( 4.5 ) and Warnings and Precautions ( 5.4 )] Atorvastatin, Pravastatin, Fluvastatin: [See Warnings and Precautions ( 5.…

Major interaction

Cyclosporine + Lovastatin

Cyclosporine: The use of lovastatin with cyclosporine should be avoided.

Major interaction

Cyclosporine + Rosuvastatin

Steps to Prevent or Reduce the Risk of Myopathy and Rhabdomyolysis The concomitant use of rosuvastatin with cyclosporine or gemfibrozil is not recommended.

Major interaction

Cyclosporine + Adalimumab

Upon initiation or discontinuation of IDACIO in patients being treated with CYP450 substrates with a narrow therapeutic index, monitoring of the effect (e.g., warfarin) or drug concentration (e.g., cyclosporine or theophylline) is recommended and the individual dose of the drug product may be adjusted as needed.

Moderate interaction

Cyclosporine + Allopurinol

Cyclosporine Clinical Impact Concomitant use of allopurinol increases cyclosporine concentrations, which may increase the risk of adverse reactions.

Moderate interaction

Cyclosporine + Amlodipine

Immunosuppressants Amlodipine may increase the systemic exposure of cyclosporine or tacrolimus when co-administered.

Moderate interaction

Cyclosporine + Carbamazepine

In addition, carbamazepine causes, or would be expected to cause, decreased levels of the following drugs, for which monitoring of concentrations or dosage adjustment may be necessary: acetaminophen, albendazole, alprazolam, aprepitant, buprenorphone, bupropion, citalopram, clonazepam, clozapine, corticosteroids (e.g., prednisolone, dexamethasone), cyclosporine, dicumarol, dihydropyridine calcium channel blockers (e.g., felodipine), doxycycline, ethosuximide, everolimus, haloperidol, imatinib…

Moderate interaction

Cyclosporine + Carvedilol

( 7.4 ) Cyclosporine or digoxin levels may increase.

Moderate interaction

Cyclosporine + Celecoxib

Cyclosporine Clinical Impact: Concomitant use of celecoxib and cyclosporine may increase cyclosporine’s nephrotoxicity.

Moderate interaction

Cyclosporine + Colchicine

Concomitant use of atorvastatin, simvastatin, pravastatin, fluvastatin, lovastatin, gemfibrozil, fenofibrate, fenofibric acid or benzafibrate (themselves associated with myotoxicity) or cyclosporine with colchicine tablets may potentiate the development of myopathy [see Error!

Moderate interaction

Cyclosporine + Fluconazole

(See PRECAUTIONS .) Cyclosporine: Cyclosporine AUC and C max were determined before and after the administration of fluconazole 200 mg daily for 14 days in eight renal transplant patients who had been on cyclosporine therapy for at least 6 months and on a stable cyclosporine dose for at least 6 weeks.

Moderate interaction

Cyclosporine + Furosemide

Concomitant use of cyclosporine and furosemide is associated with increased risk of gouty arthritis secondary to furosemide-induced hyperurecemia and cyclosporine impairment of renal urate excretion.

Moderate interaction

Cyclosporine + Indomethacin

Cyclosporine Clinical Impact: Concomitant use of indomethacin capsules and cyclosporine may increase cyclosporine’s nephrotoxicity.

Moderate interaction

Cyclosporine + Itraconazole

Budesonide (inhalation) a Budesonide (non-inhalation) Ciclesonide (inhalation) Cyclosporine (IV) a Cyclosporine (non-IV) Dexamethasone a Fluticasone (inhalation) a Fluticasone (nasal)Methylprednisolone a Tacrolimus (IV) a Tacrolimus (oral) Monitor for adverse reactions.

Moderate interaction

Cyclosporine + Meloxicam

Cyclosporine Clinical Impact: Concomitant use of meloxicam and cyclosporine may increase cyclosporine's nephrotoxicity.

Moderate interaction

Cyclosporine + Naproxen

Cyclosporine Clinical Impact: Concomitant use of naproxen tablets or naproxen sodium tablets and cyclosporine may increase cyclosporine’s nephrotoxicity.

Moderate interaction

Cyclosporine + Phenytoin

Phenytoin when given with the combination of fosamprenavir and ritonavir may increase the concentration of amprenavir Calcium channel blockers Nifedipine, nimodipine, nisoldipine, verapamil Other Albendazole (decreases active metabolite), chlorpropamide, clozapine, cyclosporine, digoxin, disopyramide, folic acid, methadone, mexiletine, praziquantel, quetiapine a The effect of phenytoin on phenobarbital, valproic acid and sodium valproate serum levels is unpredictable 7.3 Drug/Laboratory Test …

Moderate interaction

Cyclosporine + Pravastatin

7 DRUG INTERACTIONS For the concurrent therapy of either cyclosporine, fibrates, niacin (nicotinic acid), or erythromycin, the risk of myopathy increases [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.3) ].

Moderate interaction

Cyclosporine + Rifampin

Glipizide Decrease exposure Immunosuppressive Agents Cyclosporine Decrease exposure Tacrolimus Prevention or Management: Monitoring of whole blood concentrations and appropriate dosage adjustments of tacrolimus are recommended when rifampin and tacrolimus are used concomitantly.

Moderate interaction

Cyclosporine + Verapamil

Cyclosporine: Verapamil therapy may increase serum levels of cyclosporine.

Moderate interaction

Cyclosporine + Amiodarone

Cyclosporine Increased plasma levels of cyclosporine have been reported resulting in elevated creatinine, despite reduction of cyclosporine dose.

Minor interaction

Cyclosporine + Ciprofloxacin

However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, enhance the effects of the oral anticoagulant, warfarin, and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving cyclosporine concomitantly.

Minor interaction

Cyclosporine + Dexamethasone

Cyclosporine: Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently.

Minor interaction

Cyclosporine + Digoxin

Conivaptan 33% 43% Diltiazem 20% NA Indomethacin 40% NA Mirabegron 29% 27% Nefazodone 27% 15% Nifedipine 45% NA Propantheline 24% 24% Quinine NA 33% Rabeprazole 29% 19% Saquinavir 27% 49% Spironolactone 25% NA Telmisartan 20 to 49% NA Tricagrelor 31% 28% Tolvaptan 30% 20% Trimethoprim 22 to 28% NA Digoxin concentrations increased, but magnitude is unclear Alprazolam, azithromycin, cyclosporine, diclofenac, diphenoxylate, epoprostenol, esomeprazole, ibuprofen, ketoconazole, lansoprazole, metfo…

Minor interaction

Cyclosporine + Diltiazem

Cyclosporine : A pharmacokinetic interaction between diltiazem and cyclosporine has been observed during studies involving renal and cardiac transplant patients.

Minor interaction

Cyclosporine + Ezetimibe

Table 3: Clinically Important Drug Interactions with Ezetimibe Cyclosporine Clinical Impact: Concomitant use of ezetimibe and cyclosporine increases ezetimibe and cyclosporine concentrations.

Minor interaction

Cyclosporine + Fenofibrate

7.2 Immunosuppressants Immunosuppressants such as cyclosporine and tacrolimus can produce nephrotoxicity with decreases in creatinine clearance and rises in serum creatinine, and because renal excretion is the primary elimination route of fibrate drugs including fenofibrate, there is a risk that an interaction will lead to deterioration of renal function.

Minor interaction

Cyclosporine + Hydroxychloroquine

7.6 Cyclosporine An increased plasma cyclosporine level was reported when cyclosporine and hydroxychloroquine sulfate tablets were co-administered.

Minor interaction

Cyclosporine + Levofloxacin

7.6 Cyclosporine No significant effect of levofloxacin on the peak plasma concentrations, AUC, and other disposition parameters for cyclosporine was detected in a clinical study involving healthy volunteers.

Minor interaction

Cyclosporine + Methotrexate

The risk of cutaneous malignancies is further increased when cyclosporine is administered to patients with psoriasis who received prior methotrexate.

Minor interaction

Cyclosporine + Metoclopramide

digoxin) by metoclopramide, whereas the rate and/or extent of absorption of drugs from the small bowel may be increased (e.g., acetaminophen, tetracycline, levodopa, ethanol, cyclosporine).

Minor interaction

Cyclosporine + Modafinil

7 DRUG INTERACTIONS Effects of Modafinil on CYP3A4/5 Substrates The clearance of drugs that are substrates for CYP3A4/5 (e.g., steroidal contraceptives, cyclosporine, midazolam, and triazolam) may be increased by modafinil via induction of metabolic enzymes, which results in lower systemic exposure.

Minor interaction

Cyclosporine + Tacrolimus

( 7.1 , 7.2 , 7.3 ) 7.1 Mycophenolic Acid When tacrolimus extended-release capsules is prescribed with a given dose of a mycophenolic acid (MPA) product, exposure to MPA is higher with tacrolimus extended-release capsules co-administration than with cyclosporine co-administration with MPA, because cyclosporine interrupts the enterohepatic recirculation of MPA while tacrolimus does not.

Minor interaction

Cyclosporine + Warfarin

Table 2: Examples of CYP450 Interactions with Warfarin Enzyme Inhibitors Inducers CYP2C9 amiodarone, capecitabine, cotrimoxazole, etravirine, fluconazole, fluvastatin, fluvoxamine, metronidazole, miconazole, oxandrolone, sulfinpyrazone, tigecycline, voriconazole, zafirlukast aprepitant, bosentan, carbamazepine, phenobarbital, rifampin CYP1A2 acyclovir, allopurinol, caffeine, cimetidine, ciprofloxacin, disulfiram, enoxacin, famotidine, fluvoxamine, methoxsalen, mexiletine, norfloxacin, oral co…

Minor interaction

Check Cyclosporine against your full medication list in our free Interaction Checker

Most-Reported Side Effects

Based on 112,236 reports in the FDA Adverse Event Reporting System (FAERS). Reports do not prove the drug caused the effect.

drug ineffective13,504eye irritation9,368off label use9,168eye pain4,411product use in unapproved indication4,267pyrexia4,111headache3,752nausea3,683diarrhoea3,634fatigue3,421pneumonia3,328condition aggravated3,237

Explore full Cyclosporine safety data in our free FDA Safety Explorer

FDA Recalls (7)

Class IIITerminatedSep 7, 2023

Subpotent: Out of Specification result observed for low assay

Recalling firm: SUN PHARMACEUTICAL INDUSTRIES INC

Class IITerminatedSep 16, 2022

CGMP deviations: Out of specification results obtained during routine stability testing for ethanol content.

Recalling firm: Novartis Pharmaceuticals Corporation

Class IIITerminatedApr 1, 2022

Subpotent Drug and Presence of Particulate Matter: low out-of-specification results obtained for assay and the presence of particulate matter.

Recalling firm: SUN PHARMACEUTICAL INDUSTRIES INC

Class IIITerminatedMay 7, 2021

Subpotent and Presence of Particulates .

Recalling firm: SUN PHARMACEUTICAL INDUSTRIES INC

Class IIITerminatedFeb 22, 2021

Subpotent

Recalling firm: SUN PHARMACEUTICAL INDUSTRIES INC

Class IITerminatedFeb 8, 2017

Failed Impurities/Degradations Specifications; out of specification results for Maximum Unknown Impurities and Total Impurities

Recalling firm: Amerisource Health Services

Class IITerminatedFeb 3, 2017

Failed Impurities/Degradations Specifications; out of specification results for Maximum Unknown Impurities and Total Impurities.

Recalling firm: Apotex Inc.

Food & Drink Interactions

Grapefruit and grapefruit juice

Avoid grapefruit and grapefruit juice with affected medications, or ask your pharmacist which specific statin/blood-pressure options are not affected. The effect can last a day or more, so separating by a few hours does not reliably avoid it.

St. John's wort (herbal supplement)

Tell your provider and pharmacist before using St. John's wort — it interacts with a wide range of prescription medicines.

This information is educational — not medical advice.

This page is provided for general educational purposes and summarizes publicly available data from sources such as the U.S. Food & Drug Administration. It is not a substitute for the judgment of a licensed clinician and should not be used to start, stop, or change any medication. It may be incomplete or out of date, and individual circumstances vary. Always talk with your prescriber or pharmacist about your specific medications and health conditions. If you think you may have a medical emergency, call 911.

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