Trusopt^® (Drops) Instructions for Use

Marketing Authorization Holder

Santen, Oy (Finland)

Manufactured By

Santen Pharmaceutical Co. Ltd., Noto Plant (Japan)

Contact Information

SANTEN LLC (Russia)

ATC Code

S01EC03 (Dorzolamide)

Active Substance

Dorzolamide (Rec.INN registered by WHO)

Dosage Form

Trusopt®

Eye drops 20 mg/1 ml: 5 ml bottle 1 pc. or 10 ml bottle 1 pc.

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless or almost colorless, slightly viscous solution.

Excipients : mannitol – 23 mg, hydroxyethyl cellulose – 4.75 mg, sodium citrate – 2.94 mg, benzalkonium chloride – 0.075 mg, sodium hydroxide – to adjust pH to 5.5-5.8, purified water – up to 1 ml.

5 ml – plastic bottles of the “Ocudrop Plus” type (1) – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – topical carbonic anhydrase inhibitor

Pharmacotherapeutic Group

Drugs used in ophthalmology; antiglaucoma drugs and miotic agents; carbonic anhydrase inhibitors

Pharmacological Action

The drug Trusopt^® contains the carbonic anhydrase II inhibitor – dorzolamide hydrochloride. Inhibition of carbonic anhydrase in the ciliary body of the eye reduces the production of intraocular fluid, presumably by slowing the synthesis of bicarbonate ions with their subsequent reduction to sodium and fluid removal. As a result, intraocular pressure (IOP) decreases.

Pharmacokinetics

Distribution

With prolonged use, Dorzolamide selectively accumulates in erythrocytes as a result of selective binding to carbonic anhydrase II, while the concentration of free dorzolamide in plasma remains extremely low. Dorzolamide is moderately bound to plasma proteins (about 33%).

Metabolism

Dorzolamide forms a single metabolite – N-desethyl-Dorzolamide, which inhibits carbonic anhydrase II to a lesser extent than Dorzolamide, and also inhibits carbonic anhydrase I. The metabolite accumulates in erythrocytes, binding mainly to carbonic anhydrase I.

Elimination

Dorzolamide and its metabolite are excreted mainly unchanged by the kidneys. After the end of treatment, Dorzolamide is washed out of erythrocytes unevenly, i.e., very intensively at the beginning, leading to a rapid and significant decrease in concentration, followed by a phase of slow washout with a T_1/2 of about 4 months.

Indications

Adults

• Ocular hypertension;
• Primary open-angle glaucoma;
• Pseudoexfoliative glaucoma;
• Secondary glaucoma (without angle closure).

Children

• For the treatment of glaucoma in children older than 1 week as monotherapy or as an addition to treatment with beta-blockers.

ICD codes

Dosage Regimen

The usual dose when using Trusopt^® is 1 drop into the affected eye (or both eyes) in the morning, afternoon, and evening.

When replacing any other antiglaucoma drug with Trusopt^®, treatment with Trusopt^® should be started on the day following the discontinuation of the previous drug.

When using Trusopt^® simultaneously with other eye drops, they should be instilled at least 10 minutes apart.

Instructions for use

1. Before first use, ensure that the protective strip on the outside of the bottle is intact. Unopened bottles may have a gap between the bottle and the cap.
2. Remove the protective strip to open the cap.
3. To open the bottle, unscrew the cap by turning it in the direction of the arrows on the top surface of the cap. Do not pull the cap upwards away from the bottle.
4. Tilt your head back and gently pull down the lower eyelid to create a space between the eyelid and the eye.
5. Turn the bottle over and press lightly with your thumb or index finger at the spot specially marked on the bottle so that one drop falls into the eye. Do not touch the surface of the eye or eyelid with the tip of the bottle.

If used incorrectly, ophthalmic preparations can become contaminated with common bacteria that cause eye infections. Serious damage to the eye and subsequent loss of vision can result from using contaminated ophthalmic preparations. If you suspect the product may be contaminated or if an eye infection develops, contact your doctor immediately regarding further use of the bottle.

1. If drop delivery is difficult after first opening the bottle, place the cap back on the bottle and screw the cap on (not too tightly), then unscrew the cap by turning it in the direction of the arrows on the top surface of the cap.
2. Repeat steps 4 and 5 for the other eye if the drug is to be instilled in both eyes.
3. Close the bottle with the cap by screwing it until it fits snugly against the bottle. For proper closure, the arrow on the bottle cap should align with the arrow on the bottle label. Do not screw the cap too tightly, as this may damage the bottle or cap.
4. Do not enlarge the opening of the specially designed dropper tip.

Adverse Reactions

In clinical trials, Trusopt^® was administered to 1108 patients as monotherapy or as adjunctive therapy to beta-blockers. Approximately 3% of patients discontinued the drug due to local ocular adverse reactions, the most common of which were conjunctivitis and eyelid reactions.

Adverse effects recorded during studies and during the post-marketing period are classified by frequency: very common (>1/10), common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10,000, <1/1000).

Nervous system disorders: common – headache; rare – dizziness, paresthesia.

Eye disorders: very common – burning and stinging; common – superficial punctate keratitis, lacrimation, conjunctivitis, blepharitis, itching, eyelid irritation, blurred vision; uncommon – iridocyclitis; rare – eye redness, pain, eyelid hyperkeratosis, transient myopia (resolving after drug discontinuation), corneal edema, decreased intraocular pressure, choroidal detachment after filtration surgery.

Respiratory system disorders: rare – epistaxis, pharyngitis.

Gastrointestinal disorders: common – nausea, bitter taste; rare – dry mouth.

Skin and subcutaneous tissue disorders: rare – contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis.

Renal and urinary disorders: rare – urolithiasis.

Allergic reactions: rare – signs and symptoms of local reactions (eyelid) and systemic allergic reactions including angioedema, urticaria, pruritus, rash, difficulty breathing, less commonly – bronchospasm.

General disorders and administration site conditions: common – asthenia, fatigue.

Children

In a 3-month double-blind, multicenter, active-controlled study involving 184 children under 6 years of age, the adverse reaction profile of Trusopt^® was comparable to that in adult patients. The most frequent adverse reactions associated with the use of Trusopt^® in children under 2 years of age were conjunctival hyperemia (5.4%) and eye discharge (3.6%). In children from 2 to 6 years old, the most frequent adverse reactions were eye burning sensation (12.1%), conjunctival hyperemia (7.6%), eye pain (3%), blepharitis (3%).

Contraindications

• Chronic renal failure;
• Pregnancy;
• Lactation (breastfeeding);
• Age under 1 week;
• Hypersensitivity to the drug components.

With caution

The use of Trusopt^® has not been studied in patients with severe hepatic impairment, and therefore the drug should be used with caution in this category of patients.

Use in Pregnancy and Lactation

Trusopt^® is contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

In patients with severe hepatic impairment, the drug should be used with caution.

Use in Renal Impairment

Contraindicated in chronic renal failure.

Pediatric Use

The drug is used in children older than 1 week.

Special Precautions

Patients who wear contact lenses should consult their doctor before using Trusopt^®, as the preservative in the drug may cause eye irritation. Trusopt^® contains benzalkonium chloride as a preservative, which can be adsorbed by contact lenses. Lenses should be removed before using the drug; lenses should not be reinserted earlier than 15 minutes after instillation of the drug. Benzalkonium chloride may discolor soft contact lenses.

Effect on ability to drive vehicles and operate machinery

During treatment with Trusopt^®, it is necessary to refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms Electrolyte imbalance, development of metabolic acidosis, and occurrence of drowsiness, nausea, dizziness, headache, weakness, unusual dreams, dysphagia are possible.

Treatment Plasma electrolyte concentrations (especially potassium) and blood pH should be monitored. In case of overdose, symptomatic therapy aimed at maintaining vital body functions is carried out.

Drug Interactions

No specific studies on the interaction of Trusopt^® with other drugs have been conducted.

In clinical trials, Trusopt^® was prescribed in combination with other drugs without negative manifestations of drug interaction, including with timolol and betaxolol eye drops, as well as systemic drugs: ACE inhibitors, calcium channel blockers, diuretics, NSAIDs (including acetylsalicylic acid), hormones (estrogen, insulin, thyroxine).

The possibility of mutual enhancement of systemic effects of oral carbonic anhydrase inhibitors and Trusopt^® when used simultaneously cannot be excluded. Combination therapy with systemic drugs and topical carbonic anhydrase inhibitors (Trusopt^®) has not been studied in clinical trials.

Trusopt^® is a carbonic anhydrase inhibitor, and although applied topically, it is partially absorbed and may have systemic effects. In clinical trials, the use of Trusopt^® was not accompanied by acid-base balance disorders. However, such phenomena have been observed with the use of carbonic anhydrase inhibitors, including as a result of drug interactions with other drugs (as a manifestation of toxicity against the background of high-dose salicylates). Thus, when prescribing Trusopt^®, the possibility of such drug interactions should be kept in mind.

The patient should inform the doctor about all medications they are taking or plan to take, including over-the-counter drugs.

Particular attention should be paid to the intake of high doses of acetylsalicylic acid.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 30°C (86°F).

Shelf Life

Shelf life – 2 years.

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

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.