Composition
Contents of 1 ml of the product
Active ingredient: brinzolamide 10.0 mg
Excipients: benzalkonium chloride solution, equivalent to benzalkonium chloride 0.1 mg; disodium edetate 0.1 mg; sodium chloride 2.5 mg; tiloxapol 0.25 mg; mannitol 33.0 mg; carbomer (974P) 4.0 mg; sodium hydroxide and/or hydrochloric acid concentrated to adjust pH; purified water to 1.0 ml.
Pharmacotherapeutic group
anticoglaucoma agent - carboangidrase inhibitor
Indications
Reduction of increased intraocular pressure in:
- open-angle glaucoma;
- ocular hypertension.
Contraindications
-Hypersensitivity to the drug components or sulfonamides;
-Serious renal failure;
-Hyperchloremic acidosis.
Caution
Hypersensitivity reactions, characteristic of all sulphonamide derivatives, may occur when using Azopt® due to systemic absorption. In case of serious adverse reactions or hypersensitivity reactions the drug administration should be discontinued.
The drug use has not been studied in patients with closed-angle glaucoma, therefore its use is not recommended for this group of patients.
The development of acid-base balance disorders during the use of oral forms of carboenhydrase inhibitors has been described. The drug should be used with caution in patients at risk of renal tubular damage due to the possible risk of metabolic acidosis.
The effect of brinzolamide on corneal endothelial function in patients with corneal disorders (especially in patients with low endothelial cell number) has not been studied. Therefore, close monitoring of such patients is recommended when using brinzolamide, such patients with diabetes mellitus or corneal dystrophy.
The use of the drug has not been studied in patients with severe liver disease, therefore, the drug should be administered with caution in such patients.
Administration during pregnancy and lactation
Fertility
No clinical studies have been performed to evaluate the effect of brinzolamide in topical application in the form of eye drops on fertility of men or women. No effect on fertility was observed in experimental studies in rats after oral administration of brinzolamide.
Pregnancy
There are no or insufficient data on the use of ophthalmic agents with brinzolamide in pregnant women. Animal studies have demonstrated toxic effects on reproductive function when the drug is used systemically. It is not recommended to use Azopt® during pregnancy.
Breast-feeding
There are currently no data on whether brinzolamide or its metabolites penetrate into the female breast milk when the drug is applied topically as eye drops; however, the risk to the infant cannot be ruled out. In preclinical studies, brinzolamide was detected in minimal concentrations in the breast milk of animals after oral administration of the drug.
The decision to discontinue breastfeeding or to continue/terminate treatment with Azopt® is taken after the ratio of the benefit of breastfeeding for the child to the benefit of using the drug for the woman has been assessed.
Pediatric use
It is not recommended to use Azopt® in patients younger than 18 years of age because currently the safety and efficacy of the drug administration in patients in this age group has not been established.
Directions for use and dosages
Topically. Shake the bottle before use.
Drip 1 drop into conjunctival sac twice a day.
If a dose is missed, treatment should be continued with the next scheduled dose. The dose should not exceed the allowable amount.
The tip of the dropper bottle should not be touched on the eyelids or any surface in order to avoid contamination of the dropper bottle and its contents.
The bottle must be closed after each use.
After removing the cap, if the snap-on tamper-evident rim does not adhere to the neck, it must be removed before using the product.
Adverse effects
The following adverse reactions have been reported in clinical studies of Azopt® and have been classified according to the following criteria:
very common (≥1/10), common (≥1/100 to <1/10), infrequent (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000). In each frequency group, adverse reactions are presented in descending order of severity.
Mental disorders
Infrequent: depression.
Rare: insomnia.
Nervous system disorders
Infrequent: dizziness, paresthesia and headache.
Rare: memory disorder, somnolence.
Visual disorders
Often: blurred vision, irritation in eyes, pain in eyes, feeling of discomfort in eyes, eye hyperemia.
Infrequent: corneal erosion, pitting keratitis, keratitis, conjunctivitis, allergic conjunctivitis, blepharitis, photophobia, dry eye syndrome, asthenopia, itching in the eye, increased lacrimation, eye discharge, crust formation on the edge of the eyelid.
Rarely: corneal edema, diplopia, decreased visual acuity, photopsia, eye hypoesthesia, periorbital edema.
Hearing and labyrinth disorders
Rare: tinnitus.
Cardiac disorders
Rare: angina pectoris, disorders of heart rhythm.
Respiratory system disorders, thoracic and mediastinal organs
Infrequent: shortness of breath, nasal bleeding, rhinorrhea, oropharyngeal pain, upper respiratory tract cough syndrome, throat irritation.
Rarely: bronchial hyperresponsiveness, upper airway congestion, perinasal mucosal edema, nasal congestion, cough, dry nose.
Gastrointestinal tract disorders
Often: dysgeusia.
Infrequent: nausea, diarrhea, dyspepsia, abdominal discomfort, dry mouth.
Skin and subcutaneous tissue disorders
Infrequent: rash.
Rare: urticaria, alopecia, generalized itching.
General disorders and disorders at the injection site
Infrequent: increased fatigue.
Rare: chest pain, anxiety, asthenia, irritability.
Postmarketing observation data
The incidence of adverse reactions cannot be determined on the basis of the data obtained.
Metabolic and nutritional disorders: decreased appetite.
Nervous system disorders: hypoesthesia.
Vascular disorders: arterial hypotension.
Musculoskeletal and connective tissue disorders: arthralgia.
Azopt® is a sulfonamide. Since systemic adsorption of the drug occurs when it is used topically, adverse reactions typical of sulfonamides may occur. Rare, but fatal, severe reactions to sulfonamides may occur, including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatonecrosis, agranulocytosis, aplastic anemia, and other hematopoietic disorders.
Overdose
There is no information about the symptoms of overdose when administered topically.
When administered orally the drug may cause electrolyte imbalance, acidosis and nervous system disorders. Electrolyte levels (especially potassium) and blood pH should be controlled.
Drug interaction
Brinzolamide is a carboanhydrase inhibitor, which may be adsorbed systemically when applied topically. There are data about disorders of acid-base equilibrium as a result of using oral carboanhydrase inhibitors. The possibility of such disorders should be considered in patients taking Azopt® as well. Concomitant use with oral carboenhydrase inhibitors is not recommended because of the possibility of increased systemic adverse reactions. Salicylates in high doses increase the risk of systemic side effects.
If necessary, it can be used in combination with other topical ophthalmic drugs. In this case, the interval between their application should be at least 10 minutes. Eye ointments should be used last.
Special Directions
Shake the bottle before use.
Nasolacrimal occlusion or careful eye closure is recommended after use. This may reduce the systemic absorption of the drug when administered topically, thus reducing the likelihood of systemic adverse reactions.
Benzalkonium chloride contained in the drug may irritate the eyes and stain soft contact lenses. Avoid contact of the drug with soft contact lenses. Lenses shall be taken off and put back on not earlier than 15-20 minutes after instillation of the drug.
Influence on the ability to drive motor transport and operate machinery
Azopt® has little effect on the ability to drive and operate machinery.
If after using the drug the patient's vision is temporarily reduced or other visual impairment occurs, it is not recommended to drive vehicles and other mechanisms as well as to engage in activities requiring high attention and reaction rate until its recovery.
In addition, nervous system disorders that may affect the ability to drive or operate machinery have been described when using the drug.
Storage temperature
4℃ to 30℃
Special storage conditions
Use within 4 weeks after opening the vial.