Drug information of Cyclosporine
Cyclosporine lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader. Cyclosporine is used to prevent organ rejection after a kidney, heart, or liver transplant. Cyclosporine is also used to treat severe psoriasis or severe rheumatoid arthritis
Mechanism of effect
Cyclosporine binds to cyclophilin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release
Used in immunosuppression for prophylactic treatment of organ transplants, cyclosporine exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle
The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. The steady state volume of distribution during intravenous dosing has been reported as 3 to 5 L/kg in solid organ transplant recipients. Cyclosporine is excreted in human milk. In the plasma, approximately 90% is bound to proteins, primarily lipoproteins. Metabolism: Hepatic, extensively metabolized by the cytochrome P450 3A enzyme system in the liver. Elimination is primarily biliary with only 6% of the dose (parent drug and metabolites) excreted in the urine. Half life: Biphasic and variable, approximately 7 hours (range 7 to 19 hours) in children and approximately 19 hours (range 10 to 27 hours) in adults.
Drug indicationspsoriasis treatment , Rheumatoid arthritis , ulcerative colitis , rejection Renal, Cardiac, and Hepatic Transplant
Usual Adult Dose for Organ Transplant - Rejection Prophylaxis IV: 2 to 4 mg/kg/day IV infusion once a day over 4 to 6 hours or 1 to 2 mg/kg IV infusion twice a day over 4 to 6 hours or 2 to 4 mg/kg/day as a continuous IV infusion over 24 hours. Capsules: 8 to 12 mg/kg/day orally in 2 divided doses. Solution: 8 to 12 mg/kg orally once a day. Doses are usually titrated downward with time to maintenance doses as low as 3 to 5 mg/kg/day. All doses should be adjusted to achieve the desired therapeutic concentration.
Drug contraindicationsRenal dysfunction , hypersensitivity to drug or its components. , Uncontrolled hypertension , malignancies
Side effectsMigraine , Headache , Hepatic dysfunction , Hypertension , Hypomagnesemia , Infections , Tremor , Kidney function abnormal , hirsutism , gum hyperplasia
InteractionsAmikacin , Ergotamine-C , Spironolactone , Everolimus , Imatinib , Betamethasone , Bortezomib , Bosentan , Pneumovax , Pimozide , Trazodone , Trastuzumab , Triamterene-H , Triamcinolone , Thymoglubin , Tinidazole , Daunorubicin , Drospirenone , Ceftriaxone , Allopurinol , Amphotericin B , Amiodarone , Erythromycin , Ezetimibe , Acetazolamide , Ethinyl Estradiol , Carvedilol , Ketoconazole , Clarithromycin , Chloroquine phosphate , Colchicine , Quinidine , Mefenamic acid , Melphalan , Nifedipine , Hydroxychloroquine , orlistat , Voriconazole , Fluoxetine , Fluconazole , Phenobarbital , Phenytoin , Griseofulvin , Lovastatin , Diltiazem , Diclofenac , Repaglinide , Sibutramine , Ciprofloxacin , Simvastatin , Propafenone , Piroxicam , Tamsulosin , Tacrolimus , Topotecan , Tolterodine , Octreotide acetate , Ibuprofen , Itraconazole , Imipenem , Indomethacin , Bupropion , Fenofibrate , Glibenclamide , Mycophenolate mofetil , Medroxyprogesterone , Meloxicam , Mitoxantrone , Naproxen , Nalidixic acid , Nervoxin , Somatropin-Human Growth hormone , Verapamil , Carbamazepine , Contraceptive DE , Cotrimoxazole , Enzalutamide , Diltigel , Sitagliptin , Rivaroxaban , Disulfiram , Bisoprolol , Rosuvastatin , fentanyl , Rifabutin , Ranolazine , Darunavir , Caspofungin , Amiloride , Fluoxymesterone , Pitavastatin , pravastatin , fluvastatin , methylene blue , Mipomersen , Axitinib , Meglumine Compound , Zileuton , Lindane , Mifepristone , Afatinib , Eluxadoline , Indinavir , Sarilumab , Etoposide , Golimumab , novafen , Hib vaccine , Butalbital and Acetaminophen , Idelalisib , brigatinib , fenoprofen , Felodipine , Diflunisal , Parecoxib , Canagliflozin , Aceclofenac , Acemetacin , Simeprevir , lumacaftor and Ivacaftor , Halofantrine , cobicistat , Delavirdine , Canakinumab , Basiliximab , Alefacept , Letermovir , Diatrizoate (Amidotrizoic acid) , Aliskiren , Butabarbital , Betrixaban , Dexlansoprazole , Secobarbital , Plazomicin , Foscarnet , elagolix , Flibanserin , Edoxaban , Entrectinib , Muromonab-CD3 , Ioxaglate , Rilonacept , Hepatitis B Vaccine , Cordyceps , Temsirolimus , ELBASVIR/GRAZOPREVIR , Lorlatinib , Troleandomycin , Iothalamate Meglumine , Glycerol Phenylbutyrate , Roxithromycin , riociguat , Sulfamethoxazole , oleandomycin , Pasireotide , Gefitinib , Remdesivir , Cannabidiol , talazoparib , ambrisentan , Typhoid vaccine (live), oral , Meningococcal conjugate vaccine , Rabies Vaccine , sitaxentan , Venetoclax , Avapritinib , Fidaxomicin , sirukumab , secukinumab , Florbetapir F18 , bacillus coagulans and inulin
1-Cyclosporine , a systemic immunosuppressant, may increase the susceptibility to infection and the development of neoplasia. 2-Cyclosporine, can cause nephrotoxicity and hepatotoxicity. Cyclosporine therapy can be associated with the occurrence of structural kidney damage and persistent renal dysfunction. 3-As in patients receiving other immunosuppressants, those patients receiving Cyclosporine are at increased risk for development of lymphomas and other malignancies
Points of recommendation
1-Adjunct therapy with adrenal corticosteroids is recommended initially for organ rejection prophylaxis 2-In general, steady state trough concentrations are measured every day for the first 2 weeks after transplantation or until the patient is stable. Thereafter, concentrations are measured once a week for the first month and then monthly for the first 12 months after transplantation. 3-A supplemental dose is not necessary with hemodialysis or peritoneal dialysis. Cyclosporine is not removed by hemodialysis