Pharmacological properties Pataday Eye Drops:
Pataday Eye Drops -selective potent antiallergic / antihistaminic, has multiple mechanisms of action. Counteracts the release of histamine (the main mediator of allergic reactions in humans) and prevents histamine-induced release of cytokines by epithelial cells of human conjunctiva. These in vitro studies indicate that Pataday Eye Drops acts on human conjunctival mast cells, inhibiting the release of inflammatory mediators. Noted that the local ophthalmic use of the drug in patients with free nasolacrimal canals reduces manifestations of signs and symptoms, often accompanied by seasonal allergic conjunctivitis. The drug has no clinically significant changes in pupil diameter.
Preclinical data obtained during standard studies on safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and studies of toxic effects on reproductive function have not revealed any danger to humans.
Pataday Eye Drops is absorbed systemically, as well as other medicines for local use. However, systemic absorption Pataday Eye Drops for topical use is low in plasma concentrations within the range of values below the limit of quantification (<0.5 ng / ml) to 1.3 ng / ml. This concentration of 50-200 times lower than with oral medication in doses that are well tolerated. Studies on the pharmacokinetics of the oral application showed that the half-life Pataday Eye Drops is about 8-12 hours, the drug is excreted mainly by the kidneys. Approximately 60-70% of the dose found in urine in the form of the active substance. Two metabolites – Desmet and mono-N-oxide were found in urine in low concentrations.
Since Pataday Eye Drops is excreted in urine mainly as unchanged active substance, its pharmacokinetics varies with impaired renal function. The maximum plasma concentration in patients with severe renal insufficiency (mean creatinine clearance – 13 ml / min) 2-3 times higher than in healthy adult volunteers. When hemodialysis patients after the drug orally at a dose of 10 mg concentration Pataday Eye Drops in blood plasma was significantly lower on the day of dialysis than in the day when he had not done that shows that Pataday Eye Drops undergoes dialysis.
In comparative studies on pharmacokinetics in the application of the drug orally at a dose of 10 mg in patients younger (average age – 21 years) and elderly (average age – 74 years) revealed no significant differences in plasma concentrations, protein binding, urinary excretion unchanged drug and metabolites.
Investigations Pataday Eye Drops for oral administration in patients with severe renal insufficiency. The results indicate that this category of patients when using Pataday Eye Drops may increase the plasma concentrations. Since the concentration in plasma after topical ophthalmic application Pataday Eye Drops in 50-200 times lower than with oral medication in doses that are well tolerated, there is no need to correct dose in the elderly and patients with impaired renal function. Metabolism in the liver is not primarily through the elimination of the drug. There is therefore no need for dosage adjustment in patients with impaired liver function.
INDICATIONS Pataday Eye Drops:
seasonal allergic conjunctivitis.
APPLICATION Pataday Eye Drops:
in the conjunctival sac of affected eye (eye) instill 1 drop Pataday Eye Drops 2 times a day (every 8 h). If necessary, treatment can last up to four months.
No need for dose adjustment for elderly patients, as well as abnormal liver function or renal function.
Can be used in pediatrics (children aged 3 years) in the same dose as adults.
CONTRAINDICATIONS Pataday Eye Drops:
Hypersensitivity to Pataday Eye Drops or other ingredients.
SIDE EFFECTS Pataday Eye Drops:
clinical trials involving about 950 patients Opatanol used for 4 months as monotherapy (4 times per day in both eyes) or adjunctive therapy to loratadine 10 mg.
5% of patients noted side effects, but only 1.4% were associated with Pataday Eye Drops. During clinical trials there were no reports of serious ocular or systemic side effects associated with the use of the drug. The most frequently – the feeling of discomfort in the eyes (0,9%). In clinical studies reported the occurrence of such side effects, which were assessed as no doubt, probably or possibly related to the application Pataday Eye Drops. The emergence of side effects was isolated (0,1-1%).
On the part of the vision: discomfort, itching, redness, discharge, keratitis, dry eyes, swelling of eyelids, foreign body sensation, photophobia.
Common side effects: asthenia.
The nervous system: dizziness, headache.
With the respiratory system: dry nose.
On the other side-effects detected in post-marketing period of the drug Pataday Eye Drops, reported very rarely (<0.01%). They usually were associated with allergy / antihistamine: blurred vision, dry mouth, rhinitis, erythema.
SPECIAL INSTRUCTIONS Pataday Eye Drops:
Opatanol an antiallergic / antihistamine, which is applied topically, but is absorbed systemically. In case of serious reactions or hypersensitivity should stop using the product.
Cases were reported of a point keratopathy and / or toxic ulcerative keratopathy, which involve the use of benzalkonium chloride in ophthalmic drugs as a preservative. Since Pataday Eye Drops contains benzalkonium chloride, should closely monitor patients with the syndrome of dry eyes or corneal damage that often or for a long time to use the drug.
To prevent contamination of the tip of the dropper and a p-pa, you must follow careful not to touch the eyelids, surrounding areas or other surfaces of the tip of the dropper bottle.
Contact lenses. Patients should be informed that should not be used Opatanol while wearing contact lenses, you should wait 10-15 minutes after instillation of the medication before inserting contact lenses.
During pregnancy and lactation. Need to take a precautionary assignment of the drug to pregnant due to the lack of clinical data regarding use of the drug during pregnancy. Experimental studies revealed no direct or indirect negative impact of the application during pregnancy on the development of the embryo / fetus, childbirth and the newborn. Pataday Eye Drops is not recommended during lactation. In experimental studies Pataday Eye Drops turned out in the milk of rats after oral administration, caused a slowdown of female babies, which were injected with doses of systemic Pataday Eye Drops, significantly exceeding the maximum recommended dose in the application subkonyunktivalno in humans. It is not known whether topical administration to be the cause of systemic absorption, sufficient for the appearance of a certain amount of drug in breast milk.
Effects on ability to drive vehicles or work with dangerous machinery. As in the case of other eye drops, temporary blurred vision or other visual disturbances may affect these abilities. If blurred vision occurs during the instillation, the patient must wait until until the vision becomes clearer, before proceeding to the above studies.
INTERACTION Pataday Eye Drops:
studies on the interaction Pataday Eye Drops with other drugs was not performed.
In vitro studies have shown that Pataday Eye Drops does not inhibit metabolic reactions isoenzymes 1A2, 2S8, 2S9, 2S19, 2D6, 2E1 and cytochrome P450 3A4. These results suggest that Pataday Eye Drops does not lead to the metabolic interaction with other active substances during their concomitant use.
In the case of other ophthalmic resources necessary to withstand the interval 5-10 minutes between their application.
OVERDOSE Pataday Eye Drops:
no data on overdose accidental or intentional swallowing. In experimental studies Pataday Eye Drops showed low acute toxicity. Accidental ingestion of the contents of the vial Opatanola lead to the maximum systemic effects of 5 mg Pataday Eye Drops. This action may occur when using doses of 0.5 mg / ml in a child weighing 10 kg in the case of 100% absorption.
Increase in Q-T interval in dogs noted only when using the drug in doses that far exceed the maximum dose for humans, indicating a low probability of increasing the Q-T interval for clinical use. In a study involving 102 healthy volunteers, young men and women, elderly people who have used 5 mg 2 times a day orally for 2.5 days, noted a slight increase in Q-T interval compared to placebo. In this study, established levels of peak concentrations Pataday Eye Drops in blood plasma (35-127 ng / ml) for at least 70 times higher than those in the local application Pataday Eye Drops on the influence on cardiac repolarization.
In case of overdose should conduct an appropriate examination and treatment of the patient.
STORAGE:
not apply more than 4 weeks after first opening the vial. After each use to tightly close the bottle-dropper.
