Trusopt - instructions for use, doses, side effects, contraindications

Excipients: mannitol 23.00 mg, giettella 4.75 mg, sodium citrate 2.94 mg, benzalkonium chloride 0.075 mg, sodium hydroxide for pH correction 5.5-5.8, water for injection up to 1 ml.

Description:Transparent, colorless or almost colorless, slightly viscous solution.

Pharmacotherapeutic group:Pharmacotherapeutic group antiglaucoma means - carbonic anhydrase inhibitor

ATX: & nbsp

S.01.E.C.03 Dorzolamide

Pharmacodynamics:

The composition Trusopt ® includes an inhibitor of carbonic anhydrase II - dorzolamide hydrochloride. Inhibition of carbonic anhydrase (CA) in the ciliary body of the eyeball reduces the production of intraocular fluid, presumably due to a slowing down of the synthesis of bicarbonate ions with their subsequent reduction to sodium and elimination of the liquid. As a result, the intraocular pressure (IOP) decreases.

Pharmacokinetics:

With prolonged use dorzolamide selectively accumulates in erythrocytes as a result of selective binding to carbonic anhydrase II (KA-II), while the concentration of free dorzolamide in plasma remains extremely low. Dorzolamide forms a single metabolite - N-residyl-dorzolamide, suppressing to a lesser degree than dorzolamide, the enzyme KA-II, as well as the enzyme KA-I. Metabolite accumulates in erythrocytes, communicating mainly with KA-I. Dorzolamide to a moderate extent binds to plasma proteins (about 33%). Dorzolamide and its metabolite are excreted mainly unchanged through the kidneys. After the end of treatment dorzolamide it is washed out from erythrocytes unevenly, i.e. very intensively at the beginning, which leads to a rapid and significant decrease in concentration, followed by a phase of slow elution with a half-life of about 4 months.

Indications:

Trusopt® is administered to adult patients with:

- ophthalmohypertension;

- primary open-angle glaucoma;

- pseudoexfoliation glaucoma;

- secondary glaucoma (without the angle block of the anterior chamber of the eye).

Trusopt® is administered to children:

- for the treatment of glaucoma in children from 1 week in monotherapy or as a supplement to the treatment with beta-blockers.

Contraindications:

- Age is less than 1 week;

- hypersensitivity to the components of the drug;

- chronic renal failure;

- pregnancy;

- the period of lactation.

Carefully:

Trusopt® has not been studied in patients with severe hepatic impairment and should therefore be used with caution in this patient category.

Dosing and Administration:

When using Trusopt®, the usual dosage is 1 drop to the affected eye (or both eyes) in the morning, afternoon and evening.

When replacing any antiglaucoma drug with Trusopt®, treatment with Trusopt® should be started the day after the previous drug was discontinued.

When using Trusopt® with other eye drops at the same time, they should be instilled with an interval of at least 10 minutes.

Side effects:

In Trusopt® clinical trials, 1108 patients were prescribed as monotherapy or adjunctive therapy for beta-blocker therapy.Approximately 3% of patients had the drug canceled due to local side reactions from the side of the eye, the most frequent of them were conjunctivitis and reactions from the eyelids.

The side effects recorded during the research and during the post-registration period are classified by frequency (very frequent (≥1 / 10), frequent (≥1 / 100, <1/10), infrequent (≥1 / 1000, <1/100 ), rare (≥1 / 10000, <1/1000).

From the nervous system

Often: headache.

Rarely: dizziness, paresthesia.

From the side of the organ of vision

Very often: burning and pain.

Often: superficial punctate keratitis, lacrimation, conjunctivitis, inflammation of the eyelids, itching, eyelid irritation, blurred vision.

Infrequently: iridocyclitis.

Rarely: redness of the eyes, pain, hyperkeratosis of the eyelids, transient myopia (disappearing after withdrawal of the drug), corneal edema, decreased intraocular pressure, detachment of the choroid of the eye after surgical interventions to restore the outflow of intraocular fluid.

On the part of the respiratory, thoracic and mediastinal organs

Rarely: nosebleeds.

From the gastrointestinal tract

Often: nausea, bitter taste in the mouth.

Rarely: pharyngitis, dry mouth.

From the skin and mucous membranes

Rarely: contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis.

From the side of the urinary tract

Rarely: urolithiasis.

General disorders and disorders at the site of administration

Often: asthenia, fatigue.

Rarely: allergic reactions - signs and symptoms of local reactions (eyelid) and systemic allergic reactions, including angioedema, urticaria, pruritus, rash, difficulty breathing, less often - bronchospasm.

Children

During a 3-month, double-blind, multicentre study using an active drug as a control conducted with the participation of 184 children under the age of 6, the profile of adverse reactions of Trusopt® was comparable to the profile of adverse reactions in adult patients. The most common adverse reactions associated with the use of Trusopt®, in children under 2 years of age, were conjunctival injection (5.4%) and discharge from the eyes (3.6%). In children from 2 to 6 years, the most frequent adverse reactions were a burning sensation in the eye (12.1%), conjunctival injection (7.6%), eye pain (3%), inflammation of the eyelids (3%).

Overdose:

Possible electrolyte disorders, the development of metabolic acidosis and the emergence of drowsiness, nausea, dizziness, headache, weakness, unusual dreams, dysphagia. Plasma concentrations of electrolytes (especially potassium) and blood pH values should be monitored.

In case of an overdose, symptomatic therapy is performed, aimed at maintaining the vital functions of the body.

Interaction:

Special studies to study the interaction of the drug Trusopt ® with other drugs have not been conducted. In clinical trials, Trusopt® was administered in combination with other medications without negative effects of inter-drug interaction, including: with eye drops of timolol and betaxolol, and also with systemic drugs: ACE inhibitors, calcium channel blockers, diuretics, non-steroidal anti-inflammatory drugs (including acetylsalicylic acid), hormones (estrogen, insulin, thyroxine).

The possibility of mutual reinforcement of the systemic effects of carbonic anhydrase inhibitors for internal use and Trusopt® during their simultaneous use is not ruled out.Combined treatment with systemic drugs and local inhibitors of carbonic anhydrase (Trusopt®) has not been studied in clinical trials.

Trusopt® is an inhibitor of carbonic anhydrase and, although applied topically, is partially absorbed and can have a systemic effect.

In clinical trials, the use of Trusopt® was not accompanied by a violation of the acid-base balance. However, similar phenomena were observed with the use of inhibitors of carbonic anhydrase, including as a result of inter-drug interaction with other drugs (as a manifestation of toxicity against the background of high doses of salicylates). Thus, when prescribing Trusopt®, one should not forget about the possibility of such inter-drug interactions.

The patient should inform the doctor about all medications that he uses or plans to use, including those that are sold without a prescription.

It should pay special attention to the reception of high doses of acetylsalicylic acid.

Special instructions:

Use in patients using contact lenses:

Patients who wear contact lenses should consult a doctor before using Trusopt®, since the preservative included in the product may cause eye irritation. The drug Trusopt® contains as a preservative benzalkonium chloride, which can be adsorbed by contact lenses. Before using the drug, the lens must be removed; Do not wear the lens before 15 minutes after instillation. Benzalkonium chloride It is able to discolor soft eye lenses.

Instructions for use:

1. Before using the product for the first time, it must be ensured that the protective strip on the outside of the vial is intact. Unopened vials may have a gap between the vial and the cap (see Figure 1).

2. Remove the protective strip to open the cap (see Figure 2).

3. To open the bottle, unscrew the cap by turning it in the direction of the arrowheads on the top surface of the cap. Do not pull the cap upward from the vial (see Figure 3).

4. Tilt the head back and slightly pull the lower eyelid downward to create a space between the eyelid and the eye (cm.Fig. 4).

5. Turn the bottle upside down by holding the thumb or index finger in the finger pressure position, as shown. Lightly press the vial to drop one drop into the eye, as prescribed by the doctor. DO NOT touch the surface of the eye or the eyelid by the VACUUM of the Vial (see Figure 5).

If used improperly, ophthalmic preparations can be infected with common bacteria - pathogens of eye diseases. Severe eye damage and subsequent loss of vision may result from the use of infected ophthalmic drugs. If you suspect that the drug may be contaminated or if an eye infection develops, you should immediately contact your doctor about the further use of the vial.

6. If the application of drops is difficult after first opening the bottle, you should put the cap back on the bottle and tighten the cap (not very much), then unscrew the cap by turning it in the direction of the indicating arrows on the top surface of the cap.

7. Repeat steps 4 and 5 for the other eye, if prescribed by your doctor.

8. Close the bottle with a cap, tightening it until it comes into contact with the bottle.To close correctly, the arrow on the bottle cap must match the arrow on the vial label. Do not tighten the cap too much, otherwise the bottle or cap may be damaged.

9. Do not enlarge the opening of a specially designed dispenser tip.

Effect on the ability to drive transp. cf. and fur:

During the treatment with the drug Trusopt®, one should refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Eye drops, 20 mg / ml.

Packaging:

5 ml or 10 ml in a plastic bottle type Okumeter Plus.

One bottle of the type "Okumeter Plus" together with instructions for use in a cardboard bundle.

Storage conditions:

Store at a temperature of no higher than 30 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

2 years.

After the first opening of the bottle, Trusopt® should not be used for more than 4 weeks.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription