CyclosporineA Non Modified

Brand Name

Company

Class

Mechanism of Action

Indications

Contraindication

Warnings

Special Precautions

Adverse Reactions

Drug Interactions

Sandimmune®

Cyclosporine

Novartis1

Apotex2

Immunosuppressant produced as a metabolite by the fungus species Beauvaria nivea Gams1 Tolypocladium inflatum Gams2

Preferential inhibition of T lymphocytes

Suppresses activation of T lymphocytes by inhibiting production and release of lymphokines, specifically interleukin-2

Prophylaxis of graft rejection in kidney, liver, and heart allogeneic transplantation

Treatment of chronic rejection previously treated with other immunosuppressants

Hypersensitivity to cyclosporine or polyoxyethylated castor oil

Nephrotoxicity Hepatotoxicity

Increased susceptibility to infection and lymphoma Erratic absorption of soft gelatin capsules and oral solution necessitates repeated monitoring of cyclosporine blood levels Anaphylactic reactions with IV formulation

Hypertension may occur and require therapy with antihypertensives (potassium-sparing diuretics should not be used) Repeated laboratory monitoring is required Pregnancy Category C

Renal dysfunction Tremor Hirsutism Hypertension Gum hyperplasia

(25% - renal, 38% - cardiac, (21% - renal, 31% - cardiac, (21% - renal, 28% - cardiac, (13% - renal, 53% - cardiac, ( 9% - renal, 5% - cardiac,

37% - hepatic) 55% - hepatic) 45% - hepatic) 27% - hepatic) 16% - hepatic)

Drugs with Synergistic Nephrotoxicity

• Ketoconazole • Vancomycin

• Azapropazon • Diclofenac

Drugs that Increase Cyclosporine Levels

• Diltiazem • Ketoconazole

• Erythromycin • Verapamil

• Methylprednisolone • Metoclopramide

• Drugs which inhibit cytochrome P450 3A4 Drugs that Decrease Cyclosporine Levels

• Rifampin • Phenobarbitol

• Carbamazepine • Phenytoin

• Drugs which induce cytochrome P450 3A4 Reduced Clearance with Cyclosporine

• Prednisone

• Lovastatin

Tobramycin Melphalan Ranitidine Naproxen

Nicardipine Itraconazole Fluconazole

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