Home Drug Guide Cyclosporine

Drug Guide

Generic Name

Cyclosporine

Brand Names Restasis, Sandimmune, Neoral, Restasis Multidose, Gengraf, Cequa, Verkazia, Vevye

Classification

Therapeutic: Immunosuppressant

Pharmacological: Calcineurin inhibitor

FDA Approved Indications

Prevention of organ rejection in transplant patients
Treatment of chronic dry eye disease (e.g., Restasis, Cequa)
Vekazia for vernal keratoconjunctivitis

Mechanism of Action

Cyclosporine inhibits calcineurin, leading to suppression of T-lymphocyte activation and cytokine production, thereby reducing immune response and inflammation.

Dosage and Administration

Adult: Varies by formulation and condition; e.g., for dry eye, 1 drop in affected eye twice daily.

Pediatric: Use depending on condition; consult specific product guidelines.

Geriatric: No specific dose adjustment required, but caution in renal or hepatic impairment.

Renal Impairment: Use with caution; dose adjustments may be necessary based on severity.

Hepatic Impairment: Use with caution; monitor liver function.

Pharmacokinetics

Absorption: Variable; influenced by formulation and site of administration.

Distribution: Widely distributed in body fluids and tissues.

Metabolism: Metabolized primarily in the liver by CYP3A4 enzymes.

Excretion: Excreted mainly via biliary (feces) with minimal renal excretion.

Half Life: Approx. 8–27 hours, depending on formulation and patient factors.

Contraindications

Hypersensitivity to cyclosporine or any component.
Active infections.

Precautions

Monitor for infections, renal and hepatic function; potential drug interactions; malignancy risk, especially lymphomas and skin cancers; pregnancy category C; caution in lactation.

Adverse Reactions - Common

Left upper quadrant pain (Less common)
Hypertension (Common)
Headache (Common)
Gingival hyperplasia (Common)

Adverse Reactions - Serious

Nephrotoxicity (Serious)
Hypertensive crisis (Serious)
Hyperkalemia (Serious)
Malignancies (lymphoma, skin cancers) (Serious)

Drug-Drug Interactions

Potent CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) increase cyclosporine levels.
CYP3A4 inducers (e.g., rifampin) decrease levels.

Drug-Food Interactions

Grapefruit juice increases levels.

Drug-Herb Interactions

St. John’s Wort decreases cyclosporine levels.

Nursing Implications

Assessment: Monitor renal function, liver function, blood pressure, and serum drug levels.

Diagnoses:

Risk of infection
Risk for renal impairment
Risk for hypertension

Implementation: Administer as prescribed, monitor labs, assess for signs of toxicity or infection.

Evaluation: Adjust dose based on serum levels and clinical response.

Patient/Family Teaching

Take medication exactly as prescribed.
Report signs of infection, changes in vision, or symptoms of renal or hepatic dysfunction.
Avoid grapefruit juice and St. John’s Wort.
Attend regular blood tests for drug levels and organ function.

Special Considerations

Black Box Warnings:

Increased risk of lymphoma and other malignancies, especially of skin.
Potential for renal impairment.

Genetic Factors: CYP3A4 genetic polymorphisms may influence metabolism.

Lab Test Interference: May interfere with certain lab tests of renal function.

Overdose Management

Signs/Symptoms: Nausea, vomiting, tremor, kidney dysfunction, hypertension.

Treatment: Supportive care; hemodialysis generally not effective for removing cyclosporine.

Storage and Handling

Storage: Store at room temperature away from moisture and light.

Stability: Stable for specified shelf life; refer to packaging for exact stability info.