Peringatan Keamanan

The oral LD50 in rats is 1480 mg/kg and the TDLO in humans is 12 mg/kg.L11085

Overdose information

In cases of overdose with oral cyclosporine, forced emesis and gastric lavage are recommended 2 hours after ingestion. There are little data available in the literature regarding overdoses with cyclosporine, but hepatotoxicity and nephrotoxicity may occur.L3734 One case report of an cyclosporine overdose due to medical error was made involving a 26 year old female and noted the occurrence of nausea, flushing, tremor, vertigo and vomiting, which resolved within about 1 day. Anorexia and a feeling of increased body girth were also experienced by this patient and resolved within about 2 weeks.A189453 When overdose with cyclosporine is observed, it is important to consider that dialysis and charcoal, hemoperfusion are not effective techniques to remove cyclosporine from the body.L3734

Cyclosporine

DB00091

small molecule approved investigational vet_approved

Deskripsi

Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions. It is isolated from the fungus Beauveria nivea.A174049 Initially manufactured by Sandoz and approved for use by the FDA in 1983, cyclosporine is now available in various products by Novartis (previously known as Sandoz).L11097,L3734,L11118

Struktur Molekul 2D

Berat 1202.635
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of cyclosporine is biphasic and very variable on different conditions but it is reported in general to last 19 hours.[A174088] Prescribing information also states a terminal half-life of approximately 19 hours, but with a range between 10 to 27 hours.[L3002]
Volume Distribusi The distribution of cyclosporine in the blood consists of 33%-47% in plasma, 4%-9% in the lymphocytes, 5%-12% in the granulocytes, and 41%-58% in the erythrocytes.[L3002] The reported volume of distribution of cyclosporine ranges from 4-8 L/kg. It concentrates mainly in leucocyte-rich tissues as well as tissues that contain high amounts of fat because it is highly lipophilic.[A189402] Cyclosporine, in the eye drop formulation, crosses the blood-retinal barrier.[A174088,A189450]
Klirens (Clearance) Cyclosporin shows a linear clearance profile that ranges from 0.38 to 3 Lxh/kg[A174088], however, there is substantial inter- patient variability.[A189402] A 250 mg dose of cyclosporine in the oral soft gelatin capsule of a lipid micro-emulsion formulation shows an approximate clearance of 22.5 L/h.[A189453]

Absorpsi

The absorption of cyclosporine occurs mainly in the intestine.A174049,A189405 Absorption of cyclosporine is highly variable with a peak bioavailability of 30% sometimes occurring 1-8 hours after administration with a second peak observed in certain patients.A174088,L11097 The absorption of cyclosporine from the GI tract has been found to be incomplete, likely due to first pass effects.A189402 Cmax in both the blood and plasma occurs at approximately 3.5 hours post-dose.L3002 The Cmax of a 0.1% cyclosporine ophthalmic emulsion is 0.67 ng/mL after instilling one drop four times daily.L34694 A note on erratic absorption During chronic administration, the absorption of Sandimmune Soft Gelatin Capsules and Oral Solution have been observed to be erratic, according to Novartis prescribing information. Those being administered the soft gelatin capsules or oral solution over the long term should be regularly monitored by testing cyclosporine blood concentrations and adjusting the dose accordingly.L3002 When compared with the other oral forms of Sandimmune, Neoral capsules and solution have a higher rate of absorption that results in a higher Tmax and a 59% higher Cmax with a 29 % higher bioavailability.L3002

Metabolisme

Cyclosporine is metabolized in the intestine and the liver by CYP450 enzymes, predominantly CYP3A4 with contributions from CYP3A5.A174049,A189402 The involvement of CYP3A7 is not clearly established.A189402 Cyclosporine undergoes several metabolic pathways and about 25 different metabolites have been identified. One of its main active metabolites, AM1, demonstrates only 10-20% activity when compared to the parent drug, according to some studies.A174088,A189402 The 3 primary metabolites are M1, M9, and M4N, which are produced from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.A189402

Rute Eliminasi

After sulfate conjugation, cyclosporine remains in the bile where it is broken down to the original compound and then re-absorbed into the circulation. Cyclosporine excretion is primarily biliary with only 3-6%A189402,L3002 of the dose (including the parent drug and metabolites) excreted in the urine while 90% of the administered dose is eliminated in the bile. From the excreted proportion, under 1% of the dose is excreted as unchanged cyclosporine.A174088,L3002

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products.
  • 2. Avoid potassium-containing products. Taking products that increase serum potassium may increase the risk of hyperkalemia.
  • 3. Avoid St. John's Wort.
  • 4. Take at the same time every day. Take consistently with regard to food.

Interaksi Obat

2359 Data
Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cyclosporine.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Cyclosporine.
Sipuleucel-T The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Cyclosporine.
Acetazolamide The serum concentration of Cyclosporine can be increased when it is combined with Acetazolamide.
Adalimumab The serum concentration of Cyclosporine can be decreased when it is combined with Adalimumab.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Cyclosporine.
Aliskiren The serum concentration of Aliskiren can be increased when it is combined with Cyclosporine.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Cyclosporine.
Amiodarone The serum concentration of Cyclosporine can be increased when it is combined with Amiodarone.
Amphotericin B Amphotericin B may increase the nephrotoxic activities of Cyclosporine.
Ketoconazole Ketoconazole may increase the nephrotoxic activities of Cyclosporine.
Atorvastatin The excretion of Atorvastatin can be decreased when combined with Cyclosporine.
Boceprevir The serum concentration of Cyclosporine can be increased when it is combined with Boceprevir.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Cyclosporine.
Bromocriptine The serum concentration of Cyclosporine can be increased when it is combined with Bromocriptine.
Carbamazepine The serum concentration of Cyclosporine can be decreased when it is combined with Carbamazepine.
Carvedilol The serum concentration of Cyclosporine can be increased when it is combined with Carvedilol.
Caspofungin The risk or severity of adverse effects can be increased when Cyclosporine is combined with Caspofungin.
Chloramphenicol The serum concentration of Cyclosporine can be increased when it is combined with Chloramphenicol.
Glycochenodeoxycholic Acid Cyclosporine may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Prasterone sulfate Cyclosporine may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Glimepiride Cyclosporine may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Atropine Cyclosporine may decrease the excretion rate of Atropine which could result in a higher serum level.
Fluorescein Cyclosporine may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin Cyclosporine may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Cefaclor Cyclosporine may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Indocyanine green acid form Cyclosporine may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone Cyclosporine may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide Cyclosporine may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Glycyrrhizic acid Cyclosporine may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Glipizide Cyclosporine may decrease the excretion rate of Glipizide which could result in a higher serum level.
Rosiglitazone Cyclosporine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Tinidazole Cyclosporine may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Cholic Acid Cyclosporine may decrease the excretion rate of Cholic Acid which could result in a higher serum level.
Taurocholic acid Cyclosporine may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Loratadine Cyclosporine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Dipyridamole Cyclosporine may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Belantamab mafodotin Cyclosporine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Cyclosporine.
Colesevelam The serum concentration of Cyclosporine can be decreased when it is combined with Colesevelam.
Crizotinib The serum concentration of Cyclosporine can be increased when it is combined with Crizotinib.
Cyclophosphamide The serum concentration of Cyclosporine can be decreased when it is combined with Cyclophosphamide.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Cyclosporine.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Cyclosporine.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Cyclosporine.
Dronedarone The serum concentration of Dronedarone can be increased when it is combined with Cyclosporine.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Cyclosporine.
Efavirenz The serum concentration of Cyclosporine can be decreased when it is combined with Efavirenz.
Enzalutamide The serum concentration of Cyclosporine can be decreased when it is combined with Enzalutamide.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Cyclosporine.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Cyclosporine.
Ezetimibe The serum concentration of Cyclosporine can be increased when it is combined with Ezetimibe.
Fluconazole The serum concentration of Cyclosporine can be increased when it is combined with Fluconazole.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Cyclosporine.
Foscarnet Foscarnet may increase the nephrotoxic activities of Cyclosporine.
Phenytoin The serum concentration of Cyclosporine can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Cyclosporine can be decreased when it is combined with Fosphenytoin.
Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Cyclosporine.
Griseofulvin The serum concentration of Cyclosporine can be decreased when it is combined with Griseofulvin.
Imatinib The serum concentration of Cyclosporine can be increased when it is combined with Imatinib.
Imipenem Cyclosporine may increase the neurotoxic activities of Imipenem.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Cyclosporine.
Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Cyclosporine.
Melphalan Melphalan may increase the nephrotoxic activities of Cyclosporine.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Cyclosporine.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Cyclosporine.
Metoclopramide Metoclopramide can cause an increase in the absorption of Cyclosporine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Mifepristone The serum concentration of Cyclosporine can be increased when it is combined with Mifepristone.
Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Cyclosporine.
Armodafinil The serum concentration of Cyclosporine can be decreased when it is combined with Armodafinil.
Modafinil The serum concentration of Cyclosporine can be decreased when it is combined with Modafinil.
Nafcillin The metabolism of Cyclosporine can be increased when combined with Nafcillin.
Norfloxacin The metabolism of Cyclosporine can be decreased when combined with Norfloxacin.
Omeprazole The serum concentration of Cyclosporine can be increased when it is combined with Omeprazole.
Esomeprazole The serum concentration of Cyclosporine can be increased when it is combined with Esomeprazole.
Orlistat Orlistat can cause a decrease in the absorption of Cyclosporine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Cyclosporine.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Cyclosporine.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Cyclosporine.
Pyrazinamide The serum concentration of Cyclosporine can be decreased when it is combined with Pyrazinamide.
Quinupristin The serum concentration of Cyclosporine can be increased when it is combined with Quinupristin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Cyclosporine.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Cyclosporine.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Cyclosporine.
Ritonavir The serum concentration of Cyclosporine can be increased when it is combined with Ritonavir.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Cyclosporine.
Sevelamer The serum concentration of Cyclosporine can be decreased when it is combined with Sevelamer.
Silodosin The excretion of Silodosin can be decreased when combined with Cyclosporine.
Simeprevir The serum concentration of Cyclosporine can be increased when it is combined with Simeprevir.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Cyclosporine.
Sitaxentan The risk or severity of adverse effects can be increased when Cyclosporine is combined with Sitaxentan.
Sulfinpyrazone The serum concentration of Cyclosporine can be decreased when it is combined with Sulfinpyrazone.
Telaprevir The serum concentration of Cyclosporine can be increased when it is combined with Telaprevir.
Ticagrelor The serum concentration of Ticagrelor can be increased when it is combined with Cyclosporine.
Vitamin E The serum concentration of Cyclosporine can be decreased when it is combined with Vitamin E.
Remikiren Cyclosporine may decrease the antihypertensive activities of Remikiren.
Guanadrel Cyclosporine may decrease the antihypertensive activities of Guanadrel.
Candoxatril Cyclosporine may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Cyclosporine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Cyclosporine may decrease the antihypertensive activities of Metyrosine.

Target Protein

Guided entry of tail-anchored proteins factor CAMLG CAMLG
Protein phosphatase 3 catalytic subunit alpha PPP3CA
Calcineurin subunit B type 2 PPP3R2
Peptidyl-prolyl cis-trans isomerase A PPIA
Peptidyl-prolyl cis-trans isomerase F, mitochondrial PPIF

Referensi & Sumber

Synthesis reference: Hans Dietl, "Pharmaceutical preparation containing cyclosporine(s) for intravenous administration and a process for its production." U.S. Patent US5527537, issued October, 1990.
Artikel (PubMed)
  • PMID: 8196726
    Lichtiger S, Present DH, Kornbluth A, Gelernt I, Bauer J, Galler G, Michelassi F, Hanauer S: Cyclosporine in severe ulcerative colitis refractory to steroid therapy. N Engl J Med. 1994 Jun 30;330(26):1841-5.
  • PMID: 24682697
    Forsythe P, Paterson S: Ciclosporin 10 years on: indications and efficacy. Vet Rec. 2014 Mar;174 Suppl 2:13-21. doi: 10.1136/vr.102484.
  • PMID: 7545467
    Cockerill GW, Bert AG, Ryan GR, Gamble JR, Vadas MA, Cockerill PN: Regulation of granulocyte-macrophage colony-stimulating factor and E-selectin expression in endothelial cells by cyclosporin A and the T-cell transcription factor NFAT. Blood. 1995 Oct 1;86(7):2689-98.
  • PMID: 28315447
    Lallemand F, Schmitt M, Bourges JL, Gurny R, Benita S, Garrigue JS: Cyclosporine A delivery to the eye: A comprehensive review of academic and industrial efforts. Eur J Pharm Biopharm. 2017 Aug;117:14-28. doi: 10.1016/j.ejpb.2017.03.006. Epub 2017 Mar 14.
  • PMID: 7691501
    Faulds D, Goa KL, Benfield P: Cyclosporin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in immunoregulatory disorders. Drugs. 1993 Jun;45(6):953-1040. doi: 10.2165/00003495-199345060-00007.
  • PMID: 11472356
    Kappers-Klunne MC, van't Veer MB: Cyclosporin A for the treatment of patients with chronic idiopathic thrombocytopenic purpura refractory to corticosteroids or splenectomy. Br J Haematol. 2001 Jul;114(1):121-5. doi: 10.1046/j.1365-2141.2001.02893.x.
  • PMID: 22323881
    Lee SH, Chung H, Yu HG: Clinical outcomes of cyclosporine treatment for noninfectious uveitis. Korean J Ophthalmol. 2012 Feb;26(1):21-5. doi: 10.3341/kjo.2012.26.1.21. Epub 2012 Jan 14.
  • PMID: 29319493
    Yang TH, Wu TH, Chang YL, Liao HT, Hsu CC, Tsai CY, Chou YC: Cyclosporine for the treatment of lupus nephritis in patients with systemic lupus erythematosus. Clin Nephrol. 2018 Apr;89(4):277-285. doi: 10.5414/CN109325.
Menampilkan 8 dari 19 artikel.

Contoh Produk & Brand

Produk: 114 • International brands: 2
Produk
  • Apo-cyclosporine Oral Solution
    Solution • 100 mg / mL • Oral • Canada • Generic • Approved
  • Aqua-stasis
    Liquid • 0.0005 g/100mL • Ophthalmic • US
  • Cequa
    Solution / drops • 0.0009 g/1mL • Ophthalmic; Topical • US • Approved
  • Cequa
    Solution / drops • 0.0009 mg/1mL • Ophthalmic; Topical • US • Approved
  • Cequa
    Solution • 0.09 % w/v • Ophthalmic • Canada • Approved
  • Cyclo-derm
    Liquid • 0.25 g/100mL • Topical • US
  • Cyclosporine
    Capsule, liquid filled • 100 mg/1 • Oral • US • Generic • Approved
  • Cyclosporine
    Capsule, liquid filled • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 114 produk.
International Brands
  • Sangcya — Sangstat Medical Corp.
  • Verkazia — Santen Inc.

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