2010/09/17

Azopt


Composition, structure and packing

Ophthalmic Suspension 1% 1 ml brinzolamid 10 mg.

Excipients: mannitol, Carbomer 974R, tiloksapol, disodium edetate, sodium chloride, hydrochloric acid and / or sodium hydroxide solution (to maintain the pH), purified water, benzalkonium chloride 0.01% (as preservative).

Clinico-pharmacological group: antiglaucoma drug - local carbonic anhydrase inhibitor.

Pharmacological action

Antiglaucoma medication - a local carbonic anhydrase inhibitor. Carbonic anhydrase - an enzyme that is present in many tissues, including tissues of the eye. Catalyzes the reversible reaction, which is the hydration of carbon dioxide and the hydrolysis of carbonic acid. In humans, carbonic anhydrase is present in a number of isoenzymes, the most active of them - carbonic anhydrase II (CA-II), is found primarily in red blood cells and other tissues.

Inhibition of carbonic anhydrase II in the ciliary body eye reduces intraocular fluid production due to delay formation of bicarbonate ions with subsequent reduction in transport of sodium and fluid. The result is a reduction of intraocular pressure.

Pharmacokinetics

Absorption

When applied topically brinzolamid absorbed into the systemic circulation.

Distribution

Plasma protein binding is 60%.

Metabolism

Brinzolamid absorbed in the red blood cells due to selective binding to carbonic anhydrase II. Metabolized to form N-dezetilbrinzolamida, which binds to carbonic anhydrase (mainly carbonic anhydrase-I) and also accumulates in red blood cells.

Since brinzolamid and its metabolite accumulate in red blood cells, their concentration in plasma below the limit of quantification (<10 ng / ml).

Withdrawal

T1 / 2 is 111 days. Brinzolamid excreted in the urine unchanged and as metabolites - the main (N-dezetilbrinzolamid) and small concentrations of other metabolites (N-and O-dezmetoksipropil Desmet).

Statement

To reduce elevated intraocular pressure:
open-angle glaucoma;
ocular hypertension.

Dosage regimen

The drug instilled 1 drop into the conjunctival sac of the affected eye (or eyes), 2 times / day. Before using the product vial should be shaken.

Side effect
On the part of the organ of vision: 5-10% - blurred vision; 1-5% - blepharitis, keratitis, dry eyes, hyperemia, foreign body sensation in the eye, discharge from the eyes, discomfort, pain, itching eyes, <1% - conjunctivitis, keratoconjunctivitis, keratopathy, initial symptoms of blepharitis (adhesion of the eyelids or crusts on the edges of the century), epiphora, diplopia, asthenopia.
On the part of the digestive system: 5-10% - bitter, sour or unusual taste in the mouth; <1% - dry mouth, dyspepsia, nausea, diarrhea.
On the part of the respiratory system: 1-5% - rhinitis; <1% - shortness of breath, sore throat.
Since the cardiovascular system: <1% - chest pain, hypertension.
From the urinary system: <1% - a pain in the kidneys.
Allergic reactions: <1% - urticaria.

Other: 1.5% - headache, dermatitis, <1% - alopecia, dizziness.

Contraindications
Hypersensitivity to the drug's components.

Pregnancy and lactation

There are no adequate and strictly controlled clinical trials the safety of Azopta in pregnant women was conducted. Therefore, the use of the drug during pregnancy Azopt is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. It is not known whether allocated brinzolamid with breast milk. Therefore, the need to appoint Azopta during lactation should resolve the issue of termination of breastfeeding.

Application for violations of liver function

Precautions should be prescribed for severe violations of Azopt liver function.

Application for violations of renal function

Since Azopt and its metabolites are excreted in the urine, the drug is not recommended to be considered in patients with severe impaired renal function (CC <30 ml / min).

Cautions

Precautions should be prescribed for severe violations of Azopt liver function. Since Azopt and its metabolites are excreted in the urine, the drug is not recommended to be considered in patients with severe impaired renal function (CC <30 ml / min).

Note that brinzolamid is sulfanilamides. As a local application is its systemic absorption, may develop adverse reactions, including severe allergic reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis, gepatonekroz, agranulocytosis, aplastic anemia). Sulphonamide sensitization can develop in the event that drug is given again with the instructions on its use. With the development of severe adverse reactions to use the drug should be discontinued.

Note that part of the preparation Azopt benzalkonium chloride can accumulate in contact lenses, so lenses should be removed before instillation and set back no earlier than 15 minutes after using the product. When using multiple medicines interval between instillation must be at least 15 minutes. Do not touch the tip of the eye dropper bottle.

Use in Pediatrics

Efficacy and safety of the drug Azopt children not installed. Effects on ability to drive vehicles and management mechanisms Immediately after the application Azopta may temporarily appear blurred vision. Therefore, patients should exercise caution when driving and when working with technology.

Overdose

Data on overdose at local application Azopta no.

In case of overdose caused by accidental drug intake by mouth, may experience the following symptoms: a violation of electrolyte balance, acidosis, disorders of the nervous system.

Treatment: If necessary, a symptomatic therapy, also need to monitor blood pH, electrolytes (especially potassium).

Drug Interactions

With simultaneous application of inhibitors of carbonic anhydrase Azopta for systemic use may be increased systemic reactions associated with inhibition of the enzyme. It is therefore not advisable to appoint such a combination.

With simultaneous application Azopta and salicylates in high doses may be a violation of the acid-base and electrolyte balance.

Terms and Conditions of storage

The drug should be stored at a temperature of 4 ° to 30 ° C in places inaccessible to children. Shelf life - 2 years. After opening the bottle of medication should be used within 4 weeks.