Brinzolamide
K.O.Romparm Company S.R.L.
679 Items
2019-09-19
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Clinical Pharmacology
Antiglaucoma drug - a local carbonic anhydrase inhibitor. Carboanhydrase is an enzyme present in many tissues of the body, including eye tissue. Catalyzes reversible reactions in which carbon dioxide hydration and hydrolysis of carbonic acid occurs. In humans, carbonic anhydrase is present in the form of a number of isoenzymes, the most active of which is carbonic anhydrase II (CA-II), which is found primarily in erythrocytes and in other tissues. Inhibition of carbonic anhydrase II in the ciliary body of the eye reduces the production of intraocular fluid due to the slowing down of the formation of bicarbonate ions, followed by a decrease in sodium and fluid transport. The result is a reduction in intraocular pressure.
Indications
Reducing elevated intraocular pressure with:
- Open-angle glaucoma,
- Eye hypertension.
Composition
Excipients: mannitol, carbomer 974P, tyloxapol, disodium edetate, sodium chloride, hydrochloric acid and / or sodium hydroxide solution (to maintain pH), purified water, benzalkonium chloride 0.01% (as a preservative).
- Brand name: Azopt
- Active ingredient: Brinzolamide
- Dosage form: Azopt eye drops. Eye drops.
- Manufacturer: Alcon
- Country of Origin: USA
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Dosage and Administration
The drug is instilled in 1 drop in the conjunctival sac of the affected eye (or eyes) 2 times / day.
Before use, shake the vial.
Adverse reactions
On the part of the organ of vision: 5-10% - blurred vision; 1-5% - blepharitis, keratitis, dry eyes, redness, foreign body sensation in the eye, discharge from the eyes, discomfort, pain, itchy eyes;
On the part of the digestive system: 5-10% - bitter, sour or unusual taste in the mouth;
On the part of the respiratory system: 1-5% - rhinitis;
Since the cardiovascular system:
From the urinary system:
Allergic reactions:
Other: 1-5% - headache, dermatitis;
Contraindications
Hypersensitivity to the drug.
Drug interactions
With simultaneous use of Azopt and carbonic anhydrase inhibitors for systemic use, it is possible to enhance systemic reactions associated with inhibition of the enzyme. Therefore, it is not recommended to prescribe such a combination.
High dose salicylates
With the simultaneous use of Azopt and salicylates in high doses, acid-base and electrolyte balance may be disturbed.
Pregnancy and Lactation
Adequate and strictly controlled clinical studies of the safety of Azopt in pregnant women have not been conducted. Therefore, the use of the drug Azopt during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus.
It is not known whether brinzolamide is excreted in breast milk. Therefore, if necessary, the appointment of Azopt during lactation should decide on the termination of breastfeeding.
Special instructions
With caution should appoint Azopt with severe violations of the liver.
Since Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe impaired renal function (CC
Keep in mind that brinzolamid is a sulfonamide. Since it is systemically absorbed when applied topically, side reactions may develop, incl. severe allergic reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatonecrosis, agranulocytosis, aplastic anemia). Sensitization of the body with sulfonamides may develop if the drug is administered repeatedly with violations of instructions for its use. With the development of severe adverse reactions, the use of the drug should be discontinued.
It should be borne in mind that the chloride contained in the Azopt benzalkonium preparation may accumulate in contact lenses, so the lenses should be removed before instillation and installed back no earlier than 15 minutes after the drug is applied.
When using multiple drugs, the interval between instillation should be at least 15 minutes.
Do not touch the eye with the dropper tip.
Use in Pediatrics
The efficacy and safety of the use of the drug Azopt in children has not been established.
Influence on ability to drive motor transport and control mechanisms
Immediately after applying Azopt, blurred vision may temporarily occur. Therefore, the patient should be careful when driving vehicles and working with equipment.
In case of impaired renal function
Since Azopt and its metabolites are excreted in the urine, the drug is not recommended for patients with severe impaired renal function (CC
With abnormal liver function
With caution should appoint Azopt with severe violations of the liver.
Use in childhood
The efficacy and safety of the use of the drug Azopt in children has not been established.
Overdosage
There is no data on overdose at local use of Azopt.
Symptoms: in case of overdose caused by accidental ingestion of the drug, there may be: electrolyte imbalance, acidosis, disorders of the nervous system.
Treatment: if necessary, conduct symptomatic therapy.It is also necessary to control blood pH, electrolyte level (especially potassium).
- ChemInform Abstract: Enantioselective Synthesis of Brinzolamide (AL-4862), a New Topical Carbonic Anhydrase Inhibitor. The “DCAT Route” to Thiophenesulfonamides.
- Timolol versus brinzolamide added to travoprost in glaucoma or ocular hypertension
- Corneal Edema in Glaucoma Patients After the Addition of Brinzolamide 1% Ophthalmic Suspension
- Switching from Dorzolamide to Brinzolamide: Effect on Intraocular Pressure and Patient Comfort
- Effects of topical administration of 1% brinzolamide on normal cat eyes
- Short-term ocular tolerability of dorzolamide 2% and brinzolamide 1% vs placebo in primary open-angle glaucoma and ocular hypertension subjects
- Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification
- Effects of topical administration of 1% brinzolamide on intraocular pressure in clinically normal horses
- A randomized, investigator-masked, 4-week study comparing timolol maleate 0.5%, brinzolamide 1%, and brimonidine tartrate 0.2% as adjunctive therapies to travoprost 0.004% in adults with primary open-angle glaucoma or ocular hypertension
- Efficacy of brinzolamide and levobetaxolol in pediatric glaucomas: A randomized clinical trial
- Effect of topical brinzolamide 1% and brimonidine 0.2% on intraocular pressure after phacoemulsification
- Brinzolamide 1% versus apraclonidine 0.5% to prevent intraocular pressure elevation after neodymium:YAG laser posterior capsulotomy
- Comparison of the Ocular Hypotensive Efficacy of Adjunctive Brimonidine 0.15% or Brinzolamide 1% in Combination with Travoprost 0.004%
- Intraocular Pressure-Lowering Efficacy of Brinzolamide 1%/Timolol 0.5% Fixed Combination Compared with Brinzolamide 1% and Timolol 0.5%
- Comparing Diurnal and Nocturnal Effects of Brinzolamide and Timolol on Intraocular Pressure in Patients Receiving Latanoprost Monotherapy
- Brimonidine Tartrate 0.15%, Dorzolamide Hydrochloride 2%, and Brinzolamide 1% Compared as Adjunctive Therapy to Prostaglandin Analogs
- Contrast Sensitivity and Optical Quality of the Eye after Instillation of Timolol Maleate Gel-Forming Solution and Brinzolamide Ophthalmic Suspension
- Comparison of topical brinzolamide 1% and dorzolamide 2% eye drops given twice daily in addition to timolol 0.5% in patients with primary open-angle glaucoma or ocular hypertension
- Clinical efficacy and safety of brinzolamide (Azopt™), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension
- Effect of brinzolamide and dorzolamide on aqueous humor flow in human eyes
- The long-term safety and efficacy of brinzolamide 1.0% (Azopt) in patients with primary open-angle glaucoma or ocular hypertension
- Adjunctive Therapy With Brinzolamide 1% Ophthalmic Suspension (Azopt®) in Patients With Open-Angle Glaucoma or Ocular Hypertension Maintained on Timolol Therapy
- The Efficacy and Safety of Brinzolamide 1% Ophthalmic Suspension (Azopt®) as a Primary Therapy in Patients With Open-Angle Glaucoma or Ocular Hypertension
- Preclinical Overview of Brinzolamide
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