Azopt Eye Drops – antiglaucoma drug, an inhibitor of carbonic anhydrase II. Lowers intraocular pressure by decreasing production of intraocular fluid. It is used for elevated intraocular pressure in open angle glaucoma.
Structure and Composition Azopt Eye Drops:
Azopt Ophthalmic Suspension 1% in vials of 5 ml with dropper Drop container.
Azopt 1 ml suspension contains: brinzolamid 10 mg, and excipients.
Active-active substance Azopt Eye Drops:
Brinzolamide.
Properties / Action Azopt Eye Drops:
Azopt – antiglaucoma drug, an inhibitor of carbonic anhydrase II.
Azopt lowers intraocular pressure by decreasing production of intraocular fluid. Inhibition of carbonic anhydrase II in the ciliary body of the eye reduces the production of aqueous humor (eye fluid), due to slowing of bicarbonate ion formation with subsequent reduction in sodium and fluid transport.
Pharmacokinetics Azopt Eye Drops:
When applied topically Azopt brinzolamid penetrates into the systemic circulation. With prolonged use brinzolamid accumulates in red blood cells due to the coupling with the carbonic anhydrase II. Metabolite N-dizetil also accumulates in red blood cells, but due to connection with the carbonic anhydrase I. Communication brinzolamida to plasma proteins – about 60%. Brinzolamida concentration in plasma at a constant taking Azopt – below 10 ng / ml. Metabolized to form N-dizetil brinzolamida, N-dezmetoksipropila, O-Desmet. The half-life (T1 / 2) – about 110 days. Excreted in the urine, mainly unchanged.
Indications Azopt Eye Drops:
• ocular hypertension (elevated intraocular pressure) with open-angle glaucoma.
Dosage and administration Azopt Eye Drops:
Azopt instill 1 drop into conjunctival sac of the affected eye (or eyes), 2 times per day. Before using Azopt vial should be shaken. Do not touch the tip of the eye dropper bottle.
The simultaneous use of other local ophthalmic means the interval between instillation must be at least 10-15 minutes.
Overdose Azopt Eye Drops:
Data on overdose Azopt local application no. When you receive inside Azopt may experience the following symptoms: disturbance of electrolyte balance, acidosis, disorders of the nervous system.
Treatment: If necessary, symptomatic treatment. Requires monitoring of blood pH, electrolyte levels, especially potassium.
Contraindications Azopt Eye Drops:
• Individual intolerance (including history of hypersensitivity) components Azopt.
Azopt is used with caution:
• pregnancy and lactation;
• Children’s age (safety and efficacy in children have not been established).
Application of pregnancy and breastfeeding:
Adequate and well controlled clinical studies on the safety of Azopt in pregnant women was conducted. The use of Azopt in pregnancy is possible only if the expected effect of therapy outweighs the potential risk to the fetus.
It is not known whether it falls brinzolamid in breast milk of nursing women. If necessary, use Azopt during lactation should decide the issue of termination of breastfeeding.
Side effects Azopt Eye Drops:
Azopt well tolerated. The most frequently reported blurred vision, bitter, sour or unusual taste in the mouth.
On the part of the vision: blurred vision (10.5%), blepharitis, keratitis, dermatitis, dry eye, redness, foreign body sensation in the eye, eye discharge, discomfort, pain, itching eyes (1.5%), conjunctivitis, keratoconjunctivitis, keratopathy, initial symptoms of blepharitis (adhesion of the eyelids or crust on the edges of the eyelids), tearing, diplopia, asthenopia (less than 1%).
From the digestive system (GI): bitter, sour taste in the mouth (5-10%), dry mouth, indigestion, nausea, diarrhea (1%); gepatonekroz (rare).
With the respiratory system: rhinitis (1.5%) dyspnea, pharyngitis (1%).
Cardio-vascular system: chest pain, hypertension (less than 1%).
With the urinary system: a pain in the kidneys (less than 1%).
From the hemopoietic system: agranulocytosis, aplastic anemia (rare).
Allergic reactions: urticaria (less than 1%), Stevens-Johnson syndrome, toxic epidermal necrolysis (rare).
Other: headache (1.5%), alopecia, dizziness (1%).
Special warnings and precautions Azopt Eye Drops:
Azopt contains brinzolamid, which is a sulfonamide and, although applied topically exposed to systemic absorption. In this regard, the application of Azopt may have adverse reactions specific to sulphonamides (co-trimoxazole, Sulfadimidine, sulfadimetoksin, silver sulfadiazine, etc.), including severe reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant gepatonekroz, agranulocytosis, aplastic anemia and other blood disorders. Allergy to sulfonamides may occur with repeated use, regardless of route of administration. When a serious adverse hypersensitivity reactions should discontinue use of Azopt.
Precautions should be appointed Azopt with severe hepatic dysfunction (adequate clinical studies are not conducted).
The use of Azopt in patients with acute attack of angle-closure glaucoma has not been studied. In patients with acute angle-closure glaucoma in addition to agents used in oftalmogipertenzii, additional therapeutic measures.
Since Azopt and its metabolites are excreted in the urine, it is not recommended for patients with severely impaired renal function (creatinine clearance less than 30 ml per minute).
Keep in mind that part of the Azopt benzalkonium chloride can accumulate in contact lenses. Before using Azopt should remove contact lenses and wear them no earlier than 15 minutes after application of drops.
Efficacy and safety of Azopt in children has not been established.
Effects on ability to drive vehicles and management mechanisms:
Immediately after applying Azopt may temporarily cause blurred vision. The patient should be cautious when driving vehicles and working with technology.
Drug Interactions Azopt Eye Drops
With simultaneous application of inhibitors of carbonic anhydrase and Azopt (diakarb, trusopt, etc.) for regular use may increase systemic reactions associated with the inhibition of carbonic anhydrase. Not recommended for simultaneous use of Azopt and oral carbonic anhydrase inhibitors.
While the application Azopt and large doses of salicylates (aspirin, etc.) may be in breach of acid-base and electrolyte balance. When Azoptom therapy should take into account the possibility of such drug interactions in patients.
Storage Conditions Azopt Eye Drops:
Keep out of reach of children, at temperatures from 4 to 30 ° C.
Shelf life: 2 years. After opening the vial must be used within 4 weeks.
Conditions of supply of pharmacies: prescription.
