A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).

Medicinal name:
  • Cyclobenzaprine hydrochloride 5 MG Oral Tablet
  • Cyclobenzaprine hydrochloride 10 MG Oral Tablet
  • Pack [Cyclessa 28 Day]
  • Cyproheptadine hydrochloride 4 MG Oral Tablet
  • Duloxetine 30 MG Delayed Release Oral Capsule [Cymbalta]
  • Cyclobenzaprine hydrochloride 7.5 MG Oral Tablet
  • Cyclophosphamide 25 MG Oral Tablet
  • Bromocriptine 0.8 MG Oral Tablet [Cycloset]
  • Cyclosporine 25 MG Oral Capsule
  • Pack [Cyclafem 1/35 28 Day]
  • Pack [Cyclafem 7/7/7 28 Day]
  • Cyclosporine, modified 100 MG Oral Capsule
  • Duloxetine 20 MG Delayed Release Oral Capsule [Cymbalta]
  • Cyclophosphamide 50 MG Oral Tablet
  • Misoprostol 0.1 MG Oral Tablet [Cytotec]
  • Cyclophosphamide 50 MG Oral Capsule
  • Liothyronine sodium 0.005 MG Oral Tablet [Cytomel]
  • Duloxetine 60 MG Delayed Release Oral Capsule [Cymbalta]
  • Misoprostol 0.2 MG Oral Tablet [Cytotec]
  • Liothyronine sodium 0.05 MG Oral Tablet [Cytomel]
  • Cycloserine 250 MG Oral Capsule
  • Cyclosporine, modified 25 MG Oral Capsule
  • Cysteamine 50 MG Oral Capsule [Cystagon]
  • Cyclosporine 100 MG Oral Capsule
  • Cyclophosphamide 25 MG Oral Capsule
  • Liothyronine sodium 0.025 MG Oral Tablet [Cytomel]
  • Cysteamine 150 MG Oral Capsule [Cystagon]
  • Cyclosporine, modified 50 MG Oral Capsule
  • Methenamine 162 MG / Sodium Salicylate 162.5 MG Oral Tablet [Cystex]
  • Cyclizine Hydrochloride 25 MG Oral Tablet [Cyclivert]

CY - Pharmacology:

CY binds to cyclophillin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. CY also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. CY emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca.

CY for patients

The emulsion from one individual single-use vial is to be used immediately after opening for administration to one or both eyes, and the remaining contents should be discarded immediately after administration.

Do not allow the tip of the vial to touch the eye or any surface, as this may contaminate the emulsion.

RESTASIS™ should not be administered while wearing contact lenses. Patients with decreased tear production typically should not wear contact lenses. If contact lenses are worn, they should be removed prior to the administration of the emulsion. Lenses may be reinserted 15 minutes following administration of RESTASIS™ ophthalmic emulsion.

CY Interactions

All of the individual drugs cited below are well substantiated to interact with cyclosporine. In addition, concomitant non-steroidal anti-inflammatory drugs, particularly in the setting of dehydration, may potentiate renal dysfunction.

Drugs That May Potentiate Renal Dysfunction

Antibiotics Antineoplastics Anti-inflammatory Drugs Gastrointestinal Agents
ciprofloxacin gentamicin tobramycin vancomycin trimethoprim with sulfamethoxazole           melphalan azapropazon colchicine diclofenac naproxen sulindac             cimetidine ranitidine
amphotericin B ketoconazole             Immunosuppressives
Other Drugs
fibric acid derivatives (e.g. bezafibrate, fenofibrate)

Drugs That Alter CY Concentrations:

Compounds that decrease cyclosporine absorption such as orlistat should be avoided. CY is extensively metabolized by cytochrome P-450 3A. 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 SandimmuneÃ? (cyclosporine) dosage adjustment are essential when these drugs are used concomitantly.

Drugs That Increase CY Concentrations

Calcium Channel Blockers Antifungals Antibiotics Glucocorticoids Other Drugs
diltiazem nicardipine verapamil           fluconazole itraconazole ketoconazole           azithromycin clarithromycin erythromycin quinupristin/ dalfopristin         methylprednisolone               allopurinol amiodarone bromocriptine colchicine danazol imatinib metoclopramide oral contraceptives  

The HIV protease inhibitors (e.g., indinavir, nelfinavir, ritonavir, and saquinavir) are known to inhibit cytochrome P-450 3A 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 CY Concentrations

Antibiotics Anticonvulsants Other Drugs/Dietary Supplements
nafcillin rifampin     carbamazepine phenobarbital phenytoin     octreotide orlistat sulfinpyrazone terbinafine ticlopidine St. Johns Wort        

There have been reports of a serious drug interaction between cyclosporine and the herbal dietary supplement, St. Johns Wort. This interaction has been reported to produce a marked reduction in the blood concentrations of cyclosporine, resulting in subtherapeutic levels, rejection of transplanted organs, and graft loss.

Rifabutin is known to increase the metabolism of other drugs metabolized by the cytochrome P-450 system. The interaction between rifabutin and cyclosporine has not been studied. Care should be exercised when these two drugs are administered concomitantly.

Nonsteroidal Anti-inflammatory Drug (NSAID) Interactions: Clinical status and serum creatinine should be closely monitored when cyclosporine is used with nonsteroidal antiinflammatory agents in rheumatoid arthritis patients.

Pharmacodynamic interactions have been reported to occur between cyclosporine and both naproxen and sulindac, in that concomitant use is associated with additive decreases in renal function, as determined by 99mTc-diethylenetriaminepentaacetic acid (DTPA) and (p-aminohippuric acid) PAH clearances. Although concomitant administration of diclofenac does not affect blood levels of cyclosporine, it has been associated with approximate doubling of diclofenac blood levels and occasional reports of reversible decreases in renal function. Consequently, the dose of diclofenac should be in the lower end of the therapeutic range.

Methotrexate Interaction: Preliminary data indicate that when methotrexate and cyclosporine were co-administered to rheumatoid arthritis patients (N=20), methotrexate concentrations (AUCs) were increased approximately 30% and the concentrations (AUCs) of its metabolite, 7-hydroxy methotrexate, were decreased by approximately 80%. The clinical significance of this interaction is not known. CY concentrations do not appear to have been altered (N=6).

Other Drug Interactions: CY may reduce the clearance of digoxin, colchicine, prednisolone and HMG-CoA reductase inhibitors (statins). Severe digitalis toxicity has been seen within days of starting cyclosporine in several patients taking digoxin. There are also reports on the potential of cyclosporine to enhance the toxic effects of colchicine such as myopathy and neuropathy, especially in patients with renal dysfunction. If digoxin or colchicine are used concurrently with cyclosporine, close clinical observation is required in order to enable early detection of toxic manifestations of digoxin or colchicine, followed by reduction of dosage and its withdrawal.

Literature and postmarketing cases of myotoxicity, including muscle pain and weakness, myositis, and rhabdomyolysis, have been reported with concomitant administration of cyclosporine with lovastatin, simvastatin, atorvastatin, pravastatin, and rarely, fluvastatin. When concurrently administered with cyclosporine, the dosage of these statins should be reduced according to label recommendations. Statin therapy needs to be temporarily withheld or discontinued in patients with signs and symptoms of myopathy or those with risk factors predisposing to severe renal injury, including renal failure, secondary to rhabdomyolysis. CY should not be used with potassium-sparing diuretics because hyperkalemia can occur. Caution is also required when cyclosporine is co-administered with potassium sparing drugs (e.g. angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists), potassium containing drugs as well as in patients on a potassium rich diet. Control of potassium levels in these situations is advisable.

Elevations in serum creatinine were observed in studies using sirolimus in combination with full-dose cyclosporine. This effect is often reversible with cyclosporine dose reduction. Simultaneous co-administration of cyclosporine significantly increases blood levels of sirolimus. To minimize increases in sirolimus blood concentrations, it is recommended that sirolimus be given 4 hours after cyclosporine administration.

During treatment with cyclosporine, vaccination may be less effective. The use of live vaccines should be avoided. Frequent gingival hyperplasia with nifedipine, and convulsions with high dose methylprednisolone have been reported.

Psoriasis patients receiving other immunosuppressive agents or radiation therapy (including PUVA and UVB) should not receive concurrent cyclosporine because of the possibility of excessive immunosuppression.

For additional information on CY Drug Interactions please contact Novartis Medical Affairs Department at 888-NOW-NOVA (888-669-6682).

CY Contraindications

RESTASIS is contraindicated in patients with active ocular infections and in patients with known or suspected hypersensitivity to any of the ingredients in the formulation.

Manufacturers name:

  • Aurobindo Pharma Limited
  • Lake Erie Medical DBA Quality Care Product LLC
  • Amneal Pharmaceuticals
  • Organon USA Inc
  • PD-Rx Pharmaceuticals, Inc
  • Bryant Ranch Prepack
  • MedVantx, Inc
  • RedPharm Drug Inc
  • Pharmaceutica North America, Inc
  • Eli Lilly and Company
  • Blenheim Pharmacal, Inc
  • Carilion Materials Management
  • Glenmark Generics Inc, USA
  • Physicians Total Care, Inc
  • Mylan Pharmaceuticals Inc
  • Roxane Laboratories, Inc
  • Santarus, Inc
  • Apotex Corp
  • Unit Dose Services
  • Liberty Pharmaceuticals, Inc
  • Watson Laboratories, Inc
  • Qualitest Pharmaceuticals
  • Northwind Pharmaceuticals, LLC
  • Lake Erie Medical DBA Quality Care Products LLC
  • Camber Pharmaceuticals
  • State of Florida DOH Central Pharmacy
  • Aphena Pharma Solutions - Tennessee, LLC
  • Cardinal Health
  • McKesson Packaging Services Business Unit of McKesson Corporation
  • American Health Packaging
  • Aidarex Pharmaceuticals LLC
  • Rebel Distributors
  • Rebel Distributors Corp
  • Pfizer Laboratories Div Pfizer Inc
  • Keltman Pharmaceuticals Inc
  • Preferred Pharmaceuticals, Inc
  • RxChange Co
  • Sandoz Inc
  • NCS HealthCare of KY, Inc dba Vangard Labs
  • IVAX Pharmaceuticals, Inc
  • Breckenridge Pharmaceutical, Inc
  • Clinical Solutions Wholesale
  • Ranbaxy Pharmaceuticals Inc
  • KVK-TECH, Inc
  • Par Pharmaceutical Inc
  • GD Searle LLC Division of Pfizer Inc
  • Legacy Pharmaceutical Packaging
  • Lake Erie Medical & Surgical Supply DBA Quality Care Products LLC
  • CorePharma, LLC
  • AvPAK
  • Proficient Rx LP
  • Purdue GMP Center LLC
  • St Marys Medical Park Pharmacy
  • HJ Harkins Company, Inc
  • Cypress Pharmaceutical, Inc
  • Rising Pharmaceuticals, Inc
  • Mylan Institutional Inc
  • Northwind Pharmaceuticals
  • McKesson Contract Packaging
  • Mutual Pharmaceutical
  • Eon Labs, Inc
  • Lake Erie Medical Surgical & Supply DBA Quality Care Products LLC
  • Dispensing Solutions, Inc
  • Boscogen, Inc
  • Apotheca, Inc
  • CO Truxton, Inc
  • Golden State Medical Supply, Inc
  • Purdue GMP Center LLC dba The Chao Center
  • ReadyMeds
  • AvKARE, Inc
  • Teva Pharmaceuticals USA Inc
  • Major Pharmaceuticals
  • McKesson Packaging Services a business unit of McKesson Corporation
  • Laboratoires Boiron
  • A-S Medication Solutions LLC
  • KLE 2, Inc
  • Pliva Inc
  • DSE Healthcare Solutions, LLC
  • SA3, LLC
  • Contract Pharmacy Services-PA
  • New Horizon Rx Group, LLC
  • Laser Pharmaceuticals, LLC

Generic name, Overdose, Half Life CY, Food Interactions, Chemical, etc..

CY see also Hibiscus flowers

Brand Names containing Cyclosporine