Cyclosporine (Oral)

Generic Details

Generic Name

Cyclosporine Oral

Other Names

  • Ciclosporin
  • Cyclosporin A

Drug Class

  • Immunosuppressant

Chemical Formula

C62H111N11O12

Molecular Weight

1202.61 g/mol

Mechanism of Action

  • Inhibits T-cell activation and proliferation by blocking interleukin-2 production

Indications

  • Prevention of organ rejection in transplant patients
  • Treatment of severe psoriasis
  • Treatment of severe atopic dermatitis

Common Dosage Forms

  • Capsules
  • Oral solution

Typical Dosage

  • 2-6 mg/kg/day in two divided doses for organ transplantation

Pediatric Dosage

  • Dosing based on body weight and medical condition

Geriatric Dosage

  • Usually lower starting doses due to decreased renal function

Side Effects

  • Hypertension
  • Nephrotoxicity
  • Tremors
  • Headache
  • Gastrointestinal issues

Contraindications

  • Hypersensitivity to cyclosporine
  • Uncontrolled hypertension
  • Severe renal impairment

Pregnancy Category

  • Category C - Animal studies have shown adverse effects on the fetus, use only if benefits outweigh risks

Lactation Safety

  • Use with caution, excretion into breast milk is unknown

Drug Interactions

  • Nephrotoxic drugs
  • Hepatotoxic drugs
  • Strong CYP3A4 inhibitors
  • Grapefruit juice

Overdose Symptoms

  • Nausea
  • Vomiting
  • Headache
  • Blurred vision

Antidote for Overdose

  • Supportive care and symptomatic treatment

Storage Conditions

  • Store at room temperature below 25°C (77°F)
  • Protect from light and moisture

Pharmacokinetics

  • Absorption: Variable and incomplete
  • Distribution: Highly bound to plasma proteins, distributes mainly in the blood and lymphatic system
  • Metabolism: Extensively metabolized in the liver by CYP3A4 enzymes
  • Excretion: Mainly via bile as metabolites

Precautions

  • Regular monitoring of blood pressure, renal function, and drug levels
  • Avoid live vaccines during treatment
  • Avoid exposure to sunlight due to increased risk of skin cancer

Warnings

  • Increased risk of infections and lymphoma
  • Nephrotoxicity can occur with high doses
  • May increase the risk of developing malignancies

Others

  • Avoid abrupt discontinuation of therapy to prevent rejection in transplant patients