Indications
● Prevention of graft rejection following solid organ transplantation
● Treatment of transplant cellular rejection in patients previously receiving other immunosuppressive agents
● Prevention of graft rejection following allogeneic bone marrow and stem cell transplantation
● Prevention or treatment of graft-versus-host disease
Mode of Action
Cyclosporine binds to cyclophilin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. Cyclosporine emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca.
Pharmacokinetics
Absorption: The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. The extent of absorption is dependent on the individual patient, the patient population, and the formulation.
Protein binding: In the plasma, approximately 90% is bound to proteins, primarily lipoproteins. In blood, the distribution is concentration dependent. Approximately 33% to 47% is in plasma, 4% to 9% in lymphocytes, 5% to 12% in granulocytes, and 41% to 58% in erythrocytes.
Metabolism: Hepatic, extensively metabolized by the cytochrome P450 3A enzyme system in the liver. It is also metabolized in the gastrointestinal tract and kidney to a lesser degree. The metabolites are significantly less potent than the parent compound. The major metabolites (M1, M9, and M4N) result from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.
Route of elimination: Elimination is primarily biliary with only 6% of the dose (parent drug and metabolites) excreted in the urine. Only 0.1% of the dose is excreted in the urine as unchanged drug
Side Effects
● Shaking
● Headache
● Dizziness
● Unusual growth of body hair,
● Nausea/vomiting
● Diarrhea
● Stomach upset
Contraindication
Hypersensitivity to the active substance or to any of the excipients
Disclaimer:The data uploaded is made from content already available on internet.The company holds no right of it and is not responsible for any wrong information.
