II. Indications
- Solid Organ Transplant immunosuppression (maintenance prevention of rejection)
III. Preparations
- Cyclosporine (Sandimmune)
- Tacrolimus (Prograf)
- Voclosporin
IV. Adverse Effects
- Cardiovascular adverse effects
- Hypertension
- Hyperlipidemia (Cyclosporine)
- Neurologic adverse effects
- Miscellaneous adverse effects
- Nephrotoxicity
- Hyperkalemia
- Gingival Hyperplasia (Cyclosporine)
- Diabetes Mellitus (Tacrolimus)
V. Drug Interactions: Agents that increase Calcineurin Inhibitor concentrations
- See Cytochrome P-450 3A4
- Antibiotics
- Aminoglycosides
- Ofloxacin (other Fluoroquinolones such as Ciprofloxacin and Levofloxacin may be used with caution)
- Erythromycin (and Clarithromycin to a lesser extent)
- Metronidazole (Flagyl)
-
Antifungal agents
- Amphoteracin B
- Fluconazole
- Itraconazole
- Ketoconazole
- Cardiovascular agents
- Amiodarone
- Spironolactone (Hyperkalemia risk)
- Nondihydropyridine Calcium Channel Blockers (Diltiazem, Verapamil)
- Foods
- Grapefruit (and juice)
- Pineapple, papaya (affect Cyclosporine)
- Pomegantes (and juice)
- Misellaneous agents
VI. Drug Interactions: Agents that decrease Calcineurin Inhbitor concentrations
- See Cytochrome P-450 3A4
- Antibiotics
- Seizure medications
- Supplements
- Echinacea (risk of transplant rejection)
- St. John's Wort
- Gastrointestinal agents
- Miscellaneous agents
Images: Related links to external sites (from Bing)
Related Studies (from Trip Database) Open in New Window
| cyclosporine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| CYCLOSPORINE 100 MG CAPSULE | Generic | $7.68 each |
| CYCLOSPORINE 25 MG CAPSULE | Generic | $1.87 each |
| CYCLOSPORINE MODIFIED 100 MG | Generic | $2.27 each |
| CYCLOSPORINE MODIFIED 25 MG | Generic | $0.70 each |
| CYCLOSPORINE MODIFIED 50 MG | Generic | $1.18 each |
| sandimmune (on 1/4/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| SANDIMMUNE 100 MG CAPSULE | Generic | $7.68 each |
| SANDIMMUNE 25 MG CAPSULE | Generic | $1.87 each |
| tacrolimus (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| TACROLIMUS 0.03% OINTMENT | Generic | $5.70 per gram |
| TACROLIMUS 0.1% OINTMENT | Generic | $5.69 per gram |
| TACROLIMUS 0.5 MG CAPSULE | Generic | $0.27 each |
| TACROLIMUS 1 MG CAPSULE | Generic | $0.29 each |
| TACROLIMUS 5 MG CAPSULE | Generic | $2.20 each |
| prograf (on 1/4/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| PROGRAF 0.5 MG CAPSULE | Generic | $0.27 each |
| PROGRAF 1 MG CAPSULE | Generic | $0.29 each |
Ontology: Cyclosporine (C0010592)
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (CHV) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body |
| Definition (NCI) | A natural cyclic polypeptide immunosuppressant isolated from the fungus Beauveria nivea. The exact mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. (NCI04) |
| Definition (NCI_NCI-GLOSS) | A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body. It is also used in clinical trials to make cancer cells more sensitive to anticancer drugs. |
| Definition (MSH) | 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). |
| Definition (CSP) | 11-residue cyclic peptide produced by certain fungi which has antifungal and T cell specific immunosuppressive properties. |
| Definition (PDQ) | A natural cyclic polypeptide immunosuppressant isolated from the fungus Beauveria nivea. The exact mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39201&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39201&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C406" NCI Thesaurus) |
| Concepts | Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) |
| MSH | D016572 |
| SnomedCT | 387467008, 255649004, 80906007 |
| LNC | LP16098-3, MTHU005140, LA16776-9 |
| English | Cyclosporin, Cyclosporin A, Cyclosporine, Cyclosporine A, Ciclosporin, cyclosporine, cyclosporine (medication), cyclosporin-A (medication), cyclosporin-A, Cyclosporin - chemical, CYCLOSPORINE, Cyclosporine [Chemical/Ingredient], cyclosporin a, cyclosporine a, ciclosporins, cycloSPORINE, ciclosporin, Cyclosporin - chemical (substance), Ciclosporin - chemical, CYA - Cyclosporin, Cyclosporin product, CSA - Cyclosporin A, CYA - Cyclosporin A, Cyclosporine (product), Cyclosporine (substance), cyclosporin, cyclosporin A, CYSP, Ciclosporin product, CsA, CycloSPORINE A, CycloSPORINE |
| Swedish | Ciklosporin |
| Czech | cyklosporin, Consupren, cyklosporin A |
| Finnish | Siklosporiini |
| French | Ciclosporine, Cyclosporine, Ciclosporine A, Cyclosporine A |
| Russian | TSIKLOSPORIN A, TSIKLOSPORIN, ЦИКЛОСПОРИН A, ЦИКЛОСПОРИН |
| Japanese | サイクロスポリン, シクロスポリンA, サイクロスポリンA, シクロスポリン, サンディミュン, ネオーラル, ネオメルク, アマドラ, シクポラール, パピロック |
| Croatian | CIKLOSPORIN |
| Polish | Cyklosporyna A |
| Spanish | ciclosporina - sustancia química, ciclosporina - sustancia química (sustancia), ciclosporina (producto), ciclosporina (sustancia), ciclosporina A, ciclosporina, Ciclosporina, Ciclosporina A |
| German | Cyclosporin A, Cyclosporin |
| Italian | Ciclosporina |
| Portuguese | Ciclosporina A, Ciclosporina |
Ontology: Tacrolimus (C0085149)
| Definition (NCI_NCI-GLOSS) | A drug used to help reduce the risk of rejection by the body of organ and bone marrow transplants. |
| Definition (NCI) | A macrolide isolated from Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12 protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus possesses similar immunosuppressive properties to cyclosporine, but is more potent. |
| Definition (MSH) | A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro. |
| Definition (PDQ) | A macrolide isolated from the fungus Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12 protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus possesses similar immunosuppressive properties to cyclosporine, but is more potent. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42009&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42009&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1311" NCI Thesaurus) |
| Concepts | Organic Chemical (T109) |
| MSH | D016559 |
| SnomedCT | 395305001, 109129008, 386975001 |
| LNC | LP15182-6, MTHU001849 |
| English | 15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-, monohydrate, (3S-(3R*(E(1S*,3S*,4S*)),4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*))-, Tacrolimus, Hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, Fujimycin, TACROLIMUS, 15,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-p, Tacrolimus [Chemical/Ingredient], tacrolimus, Tacrolimus [skin], Tacrolimus [skin] (product), tacrolimus (medication), immunosuppressives tacrolimus, Tacrolimus (product), Tacrolimus (substance) |
| Swedish | Takrolimus |
| Czech | takrolimus, FK-506 |
| Finnish | Takrolimuusi |
| German | Tacrolimus |
| Russian | TAKROLIMUS, FK-506, ТАКРОЛИМУС |
| Japanese | プログラフ, タリムス, タクロリムス水和物, タクロリムス, プロトピック, アドバグラフ, グラセプター |
| Spanish | tacrolimús, tacrolimus, tacrolimus (producto), tacrolimús (producto), tacrolimús (sustancia), tacrolimus (piel), tacrolimus (piel) (producto), Tacrolimús, tacrolimus (sustancia), Tacrolimus |
| French | Tacrolimus |
| Polish | Takrolimus, FK-506 |
| Portuguese | Tacrolimus, Tacrolimo |
| Italian | Tacrolimus |
Ontology: Calcineurin inhibitor (C1562036)
| Definition (MSH) | Compounds that inhibit or block the PHOSPHATASE activity of CALCINEURIN. |
| Concepts | Pharmacologic Substance (T121) |
| MSH | D065095 |
| SnomedCT | 416587008, 416798007 |
| English | Calcineurin inhibitors, Calcineurin inhibitor, Calcineurin Antagonists, Calcineurin Inhibitors, Calcineurin Blockers, Protein Phosphatase-2B Inhibitors, Protein Phosphatase 2B Inhibitors, Protein Phosphatase 3 Inhibitors, Calcineurin antagonist, Calcineurin inhibitor (product), Calcineurin inhibitor (substance) |
| Spanish | inhibidor de la calcineurina (producto), inhibidor de la calcineurina (sustancia), inhibidor de la calcineurina |
Ontology: voclosporin (C2607219)
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | C484071 |
| English | voclosporin |
