Let's first understand mechanism of action of Cyclosporine.
Mechanism of Action:
Mechanism of Action:
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Cyclosporine acts by binding with cyclophilin (a type of immunophilin protein) present in T cells (T lymphocytes). Thus it prevents activation of T cells i.e. dephosphorylation of T cells and inhibits release of various cytokines like interleukins, interferon gamma which further propagate the immune mediated inflammation.
Vicious Cycle of Dry Eye
Vicious Cycle of Dry Eye
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"Cyclosporine acts by Inhibiting T cell activation and thus inhibits the release of inflammatory cytokines which lare responsible for disease progression."
It is Immunosuppressant !!!
How safe is cyclosporine???
1. Blood cyclosporin A concentrations were below quantitation limit (0.1 ng/mL) after topical application of cyclosporine 0.05% emulsion to the eye twice daily for up to 12 months. (n=128)
No detectable drug accumulation in blood during 12 months of treatment
2. In another study when cyclosporine ophthalmic emulsion given in increased concentration ie. 0.1% for 1 to 3 years, was found to be safe, well tolerated, and not associated with systemic side effects. n= 412; The only treatment related adverse events were burning (10.8%), stinging (3.9%) and conjunctival hyperemia (3.4%).
3. Plasma levels of cyclosporine were below the level of detection and no patient was discontinued due to any treatment related adverse effects when Cyclosporine 0.05% was given 3-8 times daily over a period of 1-70 months.
How safe is cyclosporine???
1. Blood cyclosporin A concentrations were below quantitation limit (0.1 ng/mL) after topical application of cyclosporine 0.05% emulsion to the eye twice daily for up to 12 months. (n=128)
No detectable drug accumulation in blood during 12 months of treatment
2. In another study when cyclosporine ophthalmic emulsion given in increased concentration ie. 0.1% for 1 to 3 years, was found to be safe, well tolerated, and not associated with systemic side effects. n= 412; The only treatment related adverse events were burning (10.8%), stinging (3.9%) and conjunctival hyperemia (3.4%).
3. Plasma levels of cyclosporine were below the level of detection and no patient was discontinued due to any treatment related adverse effects when Cyclosporine 0.05% was given 3-8 times daily over a period of 1-70 months.
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Why it takes 3-4 months to show the maximum response??
T cells live in the body for approximately 110 days, it takes 3 to 6 months to see maximal effects, although many patients begin to experience results within the first month of therapy. Activated lymphocytes must be removed from the lacrimal gland tissues for optimal response and recovery of normal function.
Cyclosporine does not turn off the function of the lymphocytes once they have already been activated. Instead, it prevents additional lymphocytes from joining the fray.
Why it takes 3-4 months to show the maximum response??
T cells live in the body for approximately 110 days, it takes 3 to 6 months to see maximal effects, although many patients begin to experience results within the first month of therapy. Activated lymphocytes must be removed from the lacrimal gland tissues for optimal response and recovery of normal function.
Cyclosporine does not turn off the function of the lymphocytes once they have already been activated. Instead, it prevents additional lymphocytes from joining the fray.