Drug information of Cyclosporine

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

Pharmacodynamic

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

Pharmacokinetics

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 indications

psoriasis treatment , Rheumatoid arthritis , ulcerative colitis , rejection Renal, Cardiac, and Hepatic Transplant

Dosage

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 contraindications

Renal dysfunction , hypersensitivity to drug or its components. , Uncontrolled hypertension , malignancies

Side effects

Migraine , Headache , Hepatic dysfunction , Hypertension , Hypomagnesemia , Infections , Tremor , Kidney function abnormal , hirsutism , gum hyperplasia

Interactions

Atorvastatin , Amikacin , Ergotamine-C , Spironolactone , Everolimus , Imatinib , Betamethasone , Bortezomib , Bosentan , Pneumovax , Pimozide , Trazodone , Trastuzumab , Triamterene-H , Triamcinolone , Thymoglubin , Tinidazole , Daunorubicin , Drospirenone , Royal jelly , Allopurinol , Amphotericin B , Amiodarone , Erythromycin , Ezetimibe , Acetazolamide , Clarithromycin , Chloroquine phosphate , Colchicine , Quinidine , Ethinyl Estradiol , Nifedipine , Hydroxychloroquine , orlistat , Voriconazole , Carvedilol , Ketoconazole , Phenobarbital , Phenytoin , Griseofulvin , Lovastatin , Mefenamic acid , Melphalan , Repaglinide , Sibutramine , Ciprofloxacin , Simvastatin , Fluoxetine , Fluconazole , Tamsulosin , Tacrolimus , Topotecan , Tolterodine , Diltiazem , Diclofenac , Octreotide acetate , Ibuprofen , Itraconazole , Imipenem , Propafenone , Piroxicam , Fenofibrate , Glibenclamide , Mycophenolate mofetil , Medroxyprogesterone , Meloxicam , Mitoxantrone , Nalidixic acid , Nervoxin , Somatropin-Human Growth hormone , Verapamil , Vitamin E , 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 , 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 , 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 , Cannabidiol , talazoparib , ambrisentan , Typhoid vaccine (live), oral , Meningococcal conjugate vaccine , Rabies Vaccine , bempedoic acid , sitaxentan , Venetoclax , Avapritinib , Fidaxomicin , sirukumab , secukinumab , Florbetapir F18 , bacillus coagulans and inulin , Anidulafungin , Glucobay (Acarbose) , Avelumab , Efalizumab , Halcinonide

Alerts

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

Pregnancy level

C

Related drugs

Tacrolimus