Ciclosporin

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(Redirected from Cyclosporine)

Immunosuppressant drug used in organ transplantation and autoimmune diseases


Ciclosporin
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Ciclosporin, also known as cyclosporine, is an immunosuppressant medication widely used in organ transplantation to prevent rejection of the transplanted organ. It is also used in the treatment of various autoimmune diseases.

History[edit | edit source]

Ciclosporin was discovered in 1971 by researchers at Sandoz (now Novartis) in Switzerland. It was isolated from the fungus Tolypocladium inflatum and was found to have potent immunosuppressive properties. The drug was first used in humans in 1978 and received approval for medical use in 1983.

Mechanism of Action[edit | edit source]

Ciclosporin works by inhibiting the activity of calcineurin, a protein phosphatase involved in activating T-cells of the immune system. By preventing the activation of T-cells, ciclosporin reduces the immune response, which is beneficial in preventing organ rejection and treating autoimmune diseases.

Medical Uses[edit | edit source]

Ciclosporin is primarily used in:

Side Effects[edit | edit source]

Common side effects of ciclosporin include:

Long-term use of ciclosporin can lead to increased risk of infections and malignancies due to its immunosuppressive effects.

Pharmacokinetics[edit | edit source]

Ciclosporin is metabolized in the liver by the cytochrome P450 enzyme system, particularly CYP3A4. It is excreted primarily in the bile and has a variable half-life depending on the individual.

Formulations[edit | edit source]

Ciclosporin is available in several formulations, including:

  • Oral capsules
  • Oral solution
  • Intravenous injection
  • Ophthalmic emulsion (eye drops)

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