Olopatadin .
Olopatadine

Olopatadine selectively blocks histamine H1-receptors, inhibits
the release of inflammatory mediators from fat cells. Olopatadine is a powerful
selective antihistamine (anti-allergic) drug. Through several different mechanisms
of action develops the pharmacological effect of opopatadine.


Olopatadine is a (https://pillintrip.com/medicine/pataday)
histamine antagonist (the main mediator of allergic reactions in humans) and
prevents conjunctival liberalization of inflammatory cytokines caused by histamine
in epithelial cells. Olopatadine has a pronounced antiallergic effect. In vitro studies
it is supposed to inhibit the release of anti-inflammatory mediators by mast cells
of the conjunctiva. Olopatadine has no clinically significant effect on pupil diameter
. Olopatadine has no effect on alpha-adrenor receptors, dopamine receptors,
m1-cholinoreceptors, m2-cholinoreceptors, serotonin receptors. In patients
with passable nasolacrimal canals, local use of olopatadine in the form of burying
in the conjunctival sac reduced the severity of clinical symptoms on the nasal
side, which often accompany seasonal allergic conjunctivitis.
Olopatadine, when used topically, is subject to systemic absorption, as are other
drugs that are intended for local use. But when used topically, the systemic
absorption of olopatadine is low. The content of olopatadine in serum after
local use in ophthalmology is low and ranges from less than 0.5 ng/ml to 1.3 ng/ml
. The reported serum concentrations of olopatadine are 50 to 200 times
lower than those reported for oral use of therapeutic doses of olopatadine.




The maximum serum concentration of olopatadine is achieved within two hours
after topical use. According to the results of studies on pharmacokinetics of oral
doses of olopatadine, the half-life period is from 8 to 12 hours, the withdrawal
of the drug is carried out mainly by kidneys. 60-70% of the introduced dose of
olopatadine is excreted in the urine in unchanged form, in addition, low
concentrations of two metabolites - n-oxide and mono-desmetil are determined
in the urine. Since olopatadine is mainly excreted by kidneys in unchanged form,
the disturbance of the functional state of the kidneys leads to changes in
pharmacokinetic parameters of olopatadine, which leads to a significant (2.3 times)
increase in serum concentration of olopatadine in patients with severe renal
insufficiency (at creatinine clearance 13 ml/min). The concentration of olopatadine
in serum after its local use in the form of installations is 50 - 200 times less than
in oral use of therapeutic doses, therefore, changes in the mode of dosing of
olopatadine in the form of eye drops in patients with renal impairment are not
required. As the hepatic pathway of olopatadine removal is not the main one,
there is no need to correct the dose of olopatadine when it is used in patients
with liver functional disorders. In oral administration of 10 mg of olopatadine
in patients with hemodialysis, the serum level of olopatadine was significantly
lower on the day of hemodialysis as compared to the days when hemodialysis
was not performed. This indicates that olopatadine can be excreted by
hemodialysis. According to the results of comparative studies of pharmacokinetics
of the medicinal form of olopatadine for administration in the concentration of
10 mg in elderly (average age 74 years) and young (average age 21 years)
patients there were no significant differences in serum concentration of olopatadine,
binding to plasma proteins and parameters of drug excretion in unchanged form
and as metabolites. How to use opopatadine and dosage Olopatadine is used locally. Olopatadine is buried in a conjunctival bag one drop
each in the affected eye (eyes) 1 - 2 times a day (at intervals of 8 hours).
If necessary, the course of treatment may last up to four months. In elderly
patients, there is no need to change the dosing regime of olopatadine.
les, 2012
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