Dorzolan extra eye drops 20mg/ml+5mg/ml, 5ml

Composition

>1 ml contains: Active ingredients:  dorzolamide hydrochloride 22.26 mg, which corresponds to the content of dorzolamide 20 mg; timolol maleate 6.83 mg, which corresponds to the content of timolol 5 mg. Auxiliary substances: sodium citrate dihydrate-2.94 mg, sodium hyaluronate-1.8 mg, mannitol-16 mg, sodium hydroxide solution of 1 M-up to pH 5.6, d/i water – up to 1 ml

Pharmacological action

Combined anti-glaucoma agent.

Dorzolamide is a selective type II carbonic anhydrase inhibitor. Inhibition of ciliary body carbonic anhydrase leads to a decrease in the secretion of intraocular fluid, presumably due to a decrease in the formation of bicarbonate ions, which in turn leads to a slowdown in the transport of sodium and intraocular fluid.

Timolol is a non-selective beta-blocker. Although the exact mechanism of action of timolol in reducing intraocular pressure has not yet been established, a number of studies have shown a predominant decrease in the formation of intraocular fluid, as well as a slight increase in its outflow.

The combined action of these substances in the composition of the combined drug leads to a more pronounced decrease in intraocular pressure.

A decrease in intraocular pressure occurs 20 minutes after instillation, reaches a maximum in 2 hours and lasts for at least 24 hours.

Indications

Increased intraocular pressure in open-angle glaucoma and pseudoexfoliative glaucoma with insufficient effectiveness of monotherapy.

Contraindications

Hyperreactivity of the respiratory tract; bronchial asthma (including in the anamnesis); severe COPD; sinus bradycardia; SSS; sinoatrial block; AV block II-III degree; severe heart failure; cardiogenic shock; severe renal failure (creatinine clearance less than 30 ml/min); hyperchloremic acidosis; corneal dystrophic processes; pregnancy; lactation (breastfeeding); children and adolescents up to 18 years old; hypersensitivity to the components of the drug.

With caution

A history of cardiovascular diseases, including heart failure, grade I AV block; mild to moderate COPD; severe peripheral circulatory disorders (severe forms of Raynaud’s disease or Raynaud’s syndrome); liver failure; diabetes mellitus; urolithiasis (including in the anamnesis); hyperthyroidism; corneal disorders; elderly patients.

Side effects

The following possible adverse reactions of the active components of the combination are known. Dorzolamide from the nervous system:  headache, dizziness, asthenia/fatigue, paresthesia. From the side of the visual organ:  inflammation of the eyelid, lacrimation, irritation and peeling of the eyelid, iridocyclitis, pinpoint keratitis, transient myopia (passing after discontinuation of the drug). Allergic reactions:  angioedema, bronchospasm, urticaria, pruritus, rash. Respiratory system disorders:  a nosebleed. Timolol (topical application)Mental disorders:  depression. From the immune system:  anaphylaxis, angioedema, urticaria, local or generalized rash. Nervous system disorders:  tinnitus, paresthesia, headache, asthenia, fatigue, dizziness, insomnia, nightmares, memory loss, increased symptoms of myasthenia gravis. Respiratory system disorders:  bronchospasm (mainly in patients with previous bronchial obstructive pathology), cough, chest pain. From the side of the visual organ:  conjunctivitis, blepharitis, keratitis, decreased corneal sensitivity, dry eye syndrome; visual disorders that include changes in the refractive power of the eye (in some cases due to the withdrawal of myotics), diplopia, ptosis. From the cardiovascular system:  arrhythmia, cardiac arrest, decreased blood pressure, syncope, Raynaud’s syndrome, decreased temperature of the hands and feet. From the digestive system:  diarrhea, dyspepsia, dry mouth, pharyngeal irritation, abdominal pain. Skin and subcutaneous tissue disorders:  alopecia, a psoriasis-like rash, or an exacerbation of psoriasis. Musculoskeletal and connective tissue disorders:  lameness, systemic lupus erythematosus. From the side of the reproductive system:  decreased libido, Peyronie’s disease.

General disorders and disorders at the injection site:  edema.

In the post-marketing period, the following adverse reactions were observed when using the dorzolamide+timolol combination: shortness of breath, respiratory failure, bradycardia, AV block, choroidal detachment, nausea, contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. Cases of edema and irreversible corneal destruction have been reported in patients with chronic corneal defects and / or who have undergone intraocular surgery.

Interaction

There is a possibility of increasing the hypotensive effect and/or developing severe bradycardia with the combined use of timolol ophthalmic solution and slow calcium channel blockers, sympatholytics, beta-blockers, antiarrhythmic agents (including amiodarone), cardiac glycosides, parasympathomimetics, opioid analgesics and MAO inhibitors.

When combined with the use of timolol and inhibitors of the CYP2D6 isoenzyme (for example, quinidine or selective serotonin reuptake inhibitors), a potentiated effect of systemic beta-adrenergic blockade (for example, heart rate reduction, depression) has been reported.

Systemic beta-blockers may increase the effect of hypoglycemic drugs.

Systemic beta-blockers may increase the severity of arterial hypertension, which is the effect of clonidine withdrawal.

There are few data on the development of mydriasis with the combined use of timolol and epinephrine.

There is a possibility that the known systemic effects of carbonic anhydrase inhibition may be enhanced by the combined use of topical and systemic carbonic anhydrase inhibitors.

How to take, course of use and dosage

For topical application. Instill 1 drop into the conjunctival sac of the eye (or both eyes) 2 times a day.

If the drug Dorzopt Plus is prescribed as a substitute for another ophthalmic drug for the treatment of glaucoma, the latter should be discontinued 1 day before the start of therapy with Dorzopt Plus.

In the case of combined use with other topical ophthalmic drugs, Dorzopt Plus should be administered at intervals of 10 minutes.

With nasolacrimal occlusion (closing of the eyelids) for 2 minutes after instillation of the drug, its systemic absorption decreases, which can lead to increased local action.

The duration of treatment is determined by the doctor depending on the patient’s clinical condition.

Special instructions

The components of the combined drug can enter the systemic bloodstream. Since timolol is a beta-blocker, adverse reactions that develop with systemic use of beta-blockers may occur with topical application of this combination.

Before starting the application, it is necessary to ensure adequate monitoring of the state of the cardiovascular system.

Patients with a history of cardiovascular diseases, including heart failure, should be closely monitored for signs of worsening of these diseases (heart rate and blood pressure monitoring). There have been reports of fatal cases of heart failure with the use of timolol in the form of eye drops. When the first signs or symptoms of heart failure appear, the use of this medicine should be discontinued.

Patients with first-degree heart block should be prescribed beta-blockers with caution due to their ability to slow down pulse conduction.

There have been reports of cases of bronchospasm with a fatal outcome in patients with bronchial asthma on the background of the use of timolol in the form of eye drops.

In patients with mild to moderate COPD, T should be used with caution and only if the intended benefit of treatment outweighs the potential risk.

The drug should be used with caution in patients with severe peripheral circulatory disorders (severe forms of Raynaud’s disease or syndrome). Use with caution in patients with spontaneous hypoglycemia or in patients with diabetes mellitus (especially with a labile course) against the background of the use of insulin or oral hypoglycemic drugs, since beta-blockers can mask the symptoms of hypoglycemia.

Beta-blockers may mask some of the clinical signs of hyperthyroidism (such as tachycardia). If hyperthyroidism is suspected, patients should be closely monitored. Abrupt withdrawal of beta-blockers should be avoided due to the risk of developing a thyrotoxic crisis.

Dorzolamide is a sulfonamide. Adverse reactions detected with systemic use of sulfonamides may occur with topical application (Stevens-Johnson syndrome and toxic epidermal necrolysis). If there are signs of serious hypersensitivity reactions, the use of the drug should be discontinued.

When treated with beta-blockers in patients with atopic or severe anaphylactic reactions to various allergens in the anamnesis, it is possible to increase the response with repeated contact with these allergens.In this group of patients, the use of epinephrine in a standard therapeutic dose to stop allergic reactions may not be effective.

When used in patients taking systemic beta-blockers, it is necessary to take into account the possible mutual strengthening of the pharmacological action of drugs both in relation to the known systemic effects of beta-blockers and in relation to reducing intraocular pressure. Concomitant use with other beta-blockers is not recommended.

If it is necessary to discontinue topical use of timolol, as in the case of discontinuation of systemic beta-blockers, discontinuation of therapy in patients with CHD should be carried out gradually.

Beta-blockers used in ophthalmology can cause dryness of the eye mucosa. In patients with corneal disorders, the drug should be used with caution. Patients with low endothelial cell counts have an increased risk of developing corneal edema.

The use of systemic carbonic anhydrase inhibitors can lead to a violation of the acid-base balance and be accompanied by urolithiasis, especially in patients with a history of urolithiasis.

Influence on the ability to drive vehicles and mechanisms

During the application period, it is necessary to refrain from driving vehicles and mechanisms and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Active ingredient

Dorzolamide, Timolol

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

For adults as directed by your doctor

Indications

Glaucoma, Vascular eye diseases