A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Restasis Pharmacology, Pharmacokinetics, Studies, Metabolism - Cyclosporine
Restasis Pharmacology, Pharmacokinetics, Studies, Metabolism - Cyclosporine
CLINICAL PHARMACOLOGY
Mechanism of action:
Cyclosporine is an immunosuppressive agent when administered
systemically.
In patients whose tear production is presumed to be suppressed
due to ocular inflammation associated with keratoconjunctivitis sicca, cyclosporine
emulsion is thought to act as a partial immunomodulator. The exact mechanism
of action is not known.
Pharmacokinetics:
Blood cyclosporin A concentrations were measured using a specific
high pressure liquid chromatography-mass spectrometry assay. Blood concentrations
of cyclosporine, in all the samples collected, after topical administration
of RESTASIS™ 0.05%, BID, in humans for up to 12 months, were below the
quantitation limit of 0.1 ng/mL. There was no detectable drug accumulation in
blood during 12 months of treatment with RESTASIS™ ophthalmic emulsion.
Clinical Evaluations:
Four multicenter, randomized, adequate and well-controlled
clinical studies were performed in approximately 1200 patients with moderate
to severe keratoconjunctivitis sicca. RESTASIS™ demonstrated statistically
significant increases in Schirmer wetting of 10 mm versus vehicle at six months
in patients whose tear production was presumed to be suppressed due to ocular
inflammation. This effect was seen in approximately 15% of RESTASIS™ ophthalmic
emulsion treated patients versus approximately 5% of vehicle treated patients.
Increased tear production was not seen in patients currentlytaking topical anti-inflammatory
drugs or using punctal plugs.
No increase in bacterial or fungal ocular infections was reported
following administration of RESTASIS™.
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