Brinzolamide eye drops

Pharmacological action Carbonic anhydrase (CA) is present in many body tissues, including tissues. Carbonic anhydrase catalyzes the reversible reaction of carbonic anhydrase hydration to carbonic acid and carbonic acid dehydration. Inhibition of carbonic anhydrase in the ciliary body of the eye can reduce the secretion of aqueous humor. It may be through reducing the generation of carbonate ions, thereby reducing the transport of sodium and water, and ultimately reducing intraocular pressure. Intraocular pressure is an important risk factor for glaucomatous optic nerve damage and glaucomatous visual field loss. Brinzolamide mainly inhibits the dominant carbonic anhydrase type 2 isoenzyme in ocular tissues. In vitro tests have an effective inhibition concentration of 50% of 3.2nM, and the Ki value for carbonic anhydrase type 2 isoenzyme is 0.13nM. Toxicology studies have shown that 1%, 2% and 4% brinzolamide eye drops, 4 times a day, have mild, statistically significant corneal thickening in rabbit eyes after 1-6 months of use, but no similar changes have been found in other species. Chronic administration of brinzolamide to mice at 8 mg/kg body weight per day (250 times the recommended human ocular dose) resulted in changes associated with carbonic anhydrase inhibition, such as changes in urine volume and electrolyte composition, and mild changes in serum electrolytes. A significant increase in the incidence of bladder tumors was observed after 24 months of oral administration of brinzolamide to female rats at 10 mg/kg body weight per day (250 times the recommended human ocular dose). Dose-dependent bladder proliferative changes were observed at 1, 3, and 10 mg/kg per day in female rats, or 3 and 10 mg/kg per day in male rats. The statistically significant increase in the incidence of bladder tumors in rats was mainly due to an increase in the incidence of a bladder tumor that was only seen in rats. In developmental toxicity studies in rabbits, oral brinzolamide doses as high as 6 mg/kg body weight per day (125 times the recommended human ocular dose) had no effect on embryonic development despite significant maternal toxicity. In similar studies in mice, mild reductions in fetal skull and sternum calcification were observed when dams were given oral brinzolamide at doses up to 18 mg/kg body weight per day (375 times the recommended human ocular dose), but not at 6 mg/kg body weight per day. These findings occurred at doses sufficient to cause acidosis and reduced maternal weight gain and fetal weight loss, and dose-related weight loss of 5-6% and nearly 14% was observed in puppies when dams were given oral brinzolamide at doses of 2 and 18 mg/kg body weight per day, respectively.

Brinzolamide, benzalkonium chloride, mannitol, carbomer 974P, tylosin, edetate, sodium chloride, hydrochloric acid/sodium hydroxide (to adjust pH) and purified water. Chemical name: R)-()-4-ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6-hydrogensulfonyl-1,1-dioxide Molecular weight: C12H21N3O5S3

White or off-white uniform suspension.

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When used as a single or combined treatment, the dosage is 1 drop of Perimelin into the conjunctival sac of the affected eye, twice a day. Some patients have better results when applied three times a day. It is usually recommended to compress the nasolacrimal duct or gently close the eyes after applying the medicine. This can reduce the systemic absorbed dose when applied to the eye, thereby reducing systemic side effects. When using Perimelin to replace another anti-glaucoma drug, stop using the drug and start using Perimelin the next day. If more than one anti-glaucoma eye drop is used at the same time, the instillation time of each drug should be at least 5 minutes apart.

In clinical studies with more than 1,500 patients using Pailimin alone or in combination with 0.5% timolol, the most common treatment-related adverse reactions and local symptoms were: taste changes (bitter or unpleasant taste in the mouth) (5.3%), transient blurred vision after instillation, lasting from a few seconds to a few minutes (4.8%). The following are adverse reactions reported in clinical studies of Pailimin that are definite, probably or possibly treatment-related. Their incidence is common (less than 10%) or uncommon (less than 1%). Ocular effects Common: blurred vision, eye discomfort (burning or stinging when instilling the drug), foreign body sensation and eye congestion. Uncommon: dry eyes, eye pain, increased eye discharge, itching, keratitis, blepharitis, conjunctivitis, eyelid induration, sticky feeling, tearing, eye fatigue, corneal lesions, conjunctival follicles and abnormal vision. The following ocular effects are only seen when Pailimin is used in combination with timolol: Uncommon: corneal erosion. Systemic effects: Pailimin is a sulfonamide carbonic anhydrase inhibitor that can be absorbed systemically. Therefore, although no other side effects related to this type of drug have been found in clinical observations, these adverse reactions may occur. Abnormal taste (bitter mouth and peculiar taste after instillation) is the most common systemic adverse reaction reported in clinical observations related to the use of PailiminTM. This may be related to the drug reaching the nasopharynx through the nasolacrimal duct. Pressing the nasolacrimal duct and gently closing the eyes after instillation can help reduce the occurrence of this adverse reaction (see [Dosage and Administration]). Systemic overall effects are rare: chest pain, hair loss. Gastrointestinal reactions are common: taste changes (bitter mouth or peculiar taste). Rare: dry mouth, nausea and indigestion. Allergic reactions are rare: dermatitis. Nervous system effects are common: headache. Rare: paresthesia, characterized by numbness and tingling in the limbs, depression and dizziness. Respiratory system effects are rare: rhinitis, dyspnea, pharyngitis, tracheitis, epistaxis and hemorrhage. Effects on the gastrointestinal tract, nervous system, hematopoietic system, kidneys and metabolism are generally related to the systemic application of carbonic anhydrase inhibitors, but the same adverse reactions related to oral carbonic anhydrase inhibitors may occur when applied to the eyes.

1. Those who are allergic to brinzolamide or its ingredients. 2. Those who are known to be allergic to sulfonamide. 3. Those with severe renal insufficiency.

Precautions for children: There is no data on the efficacy and safety of Pilimab in children under 18 years of age. Pilimab is not recommended for these patients. Precautions for pregnancy and lactation: Pregnant women have not studied the use of Pilimab in pregnant women. Animal experiments have shown reproductive toxicity (see 5.3). The potential harm to humans is still unknown. Pregnant women should not use Pilimab unless clearly needed. It is not known whether brin-zolomide is excreted in human milk for lactating women, but it can be excreted in mouse milk. Therefore, it is strongly recommended to avoid the use of Pilimab while breastfeeding. Precautions for the elderly: There is no need to change the dosage of the drug for the elderly.

If used with other drugs, drug interactions may occur. Please consult your doctor or pharmacist for details.

seal.

5ml:50mg(1%)

24 months