Ciclosporin

Immunosuppressant drug used in organ transplantation and autoimmune diseases

Ciclosporin
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

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

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

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

Ciclosporin is primarily used in:

• Organ transplantation: To prevent rejection of kidney, liver, heart, and other organ transplants.
• Autoimmune diseases: Such as rheumatoid arthritis, psoriasis, and Crohn's disease.
• Ophthalmology: As an eye drop formulation to treat dry eye syndrome.

Side Effects

Common side effects of ciclosporin include:

• Hypertension
• Nephrotoxicity
• Hirsutism
• Gingival hyperplasia
• Hyperlipidemia

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

Pharmacokinetics

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

Ciclosporin is available in several formulations, including:

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

Related Pages

• Immunosuppressive drug
• Organ transplantation
• Autoimmune disease