Description
Pharmacological action
Combined anti-glaucoma.
Dorzolamide is a selective type II carbonic anhydrase inhibitor. Inhibition of the carbonic anhydrase of the ciliary body 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 combination drug leads to a more pronounced decrease in intraocular pressure.
A decrease in intraocular pressure occurs 20 minutes after instillation, reaches a maximum after 2 hours and lasts at least 24 hours
Indications
Increased intraocular pressure in open-angle glaucoma and pseudoexfoliation glaucoma with insufficient effectiveness of monotherapy.
Contraindications
Hyperresponsiveness of the respiratory tract bronchial asthma (including history of severe COPD sinus bradycardia SSSU sinoatrial blockade AV block II-III degree severe heart failure cardiogenic shock severe renal failure (CC less than 30 ml / min) hyperchloremic acidosis dystrophic processes in the cornea pregnancy lactation (breastfeeding and adolescence) up to 18 years of hypersensitivity to the components of the drug.
With caution
History of cardiovascular disease, including heart failure, AV blockade of degree I COPD, mild to moderate severe circulatory disorders (severe forms of Raynaud’s disease or Raynaud’s syndrome) liver failure diabetes mellitus urolithiasis (including history) corneal hyperthyroidism elderly patients.
Special instructions
Components of the combination drug may enter the systemic circulation. Since timolol is a beta-blocker, adverse reactions that develop with the systemic use of beta-blockers can be observed with topical use of this combination.
Before starting use, it is necessary to ensure adequate monitoring of the state of the cardiovascular system.
Patients with a history of cardiovascular disease, including heart failure, should be closely monitored for signs of worsening of these diseases (heart rate and blood pressure control).
Reports of fatal heart failure have been reported with 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 grade I heart block should be given beta-blockers with caution because of their ability to slow down the pulse.
Reported cases of fatal bronchospasm in patients with bronchial asthma with timolol in the form of eye drops.
In patients with mild to moderate COPD, use with caution and only if the intended benefits of the treatment outweigh the potential risk.
The drug should be used with caution in patients with severe peripheral circulatory disorders (severe forms of the disease or Raynaud’s syndrome).
Use with caution in patients with spontaneous hypoglycemia or in patients with diabetes mellitus (especially labile) with 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. Avoid abrupt withdrawal of beta-blockers due to the risk of thyrotoxic crisis.
Dorzolamide is a sulfonamide. Adverse reactions identified with the systemic use of sulfonamides can be observed 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 treating patients with atopy or severe anaphylactic reactions to various allergens with beta-adrenergic blocking agents, an increase in the response is possible upon repeated contact with these allergens. In this group of patients, the use of epinephrine in a standard therapeutic dose for the relief of allergic reactions may be ineffective.
When used in patients taking systemic beta-blockers, it is necessary to take into account the possible mutual enhancement of the pharmacological action of the drugs both in relation to the known systemic effects of beta-blockers and in relation to the reduction of intraocular pressure. Joint use with other beta-blockers is not recommended.
If it is necessary to cancel the topical use of timolol, as in the case of cancellation of systemic beta-blockers, discontinuation of therapy in patients with ischemic heart disease should be carried out gradually.
Beta-blockers used in ophthalmology can cause dry eyes. In patients with disorders of the cornea, the drug should be used with caution. Patients with low endothelial cells have an increased risk of corneal edema.
The use of systemic carbonic anhydrase inhibitors can lead to an imbalance in acid-base balance and may be accompanied by urolithiasis, especially in patients with a history of urolithiasis.
Influence on the ability to drive vehicles and mechanisms
During the period of use, it is necessary to refrain from driving vehicles and mechanisms and engage in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Composition
1 ml contains:
Active substances:
dorzolamide hydrochloride 22.26 mg, which corresponds to a dorzolamide content of 20 mg
timolol maleate 6.83 mg, which corresponds to a content of timolol 5 mg.
Excipients:
sodium citrate dihydrate – 2. 94 mg,
sodium hyaluronate – 1.8 mg,
mannitol – 16 mg,
sodium hydroxide solution 1M – up to pH 5.6,
water d / i – up to 1 ml.
Dosage and administration
For topical use. Instill 1 drop in the conjunctival sac of the eye (or both eyes) 2 times / day.
If Dorzopt Plus is prescribed as a replacement for another ophthalmic drug for the treatment of glaucoma, the latter must be canceled 1 day before the start of therapy with Dorzopt Plus.
In case of joint use with other local ophthalmic preparations, the administration of Dorzopt Plus should be carried out with an interval of 10 minutes.
With nasolacrimal occlusion (closing of the eyelids) for 2 min 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 clinical condition of the patient.
Side effects
The following possible adverse reactions to the active ingredients of the combination are known.
Dorzolamide
From the nervous system: headache, dizziness, asthenia / fatigue, paresthesia.
From the side of the organ of vision: inflammation of the eyelid, lacrimation, irritation and peeling of the eyelid, iridocyclitis, point keratitis, transient myopia (which occurs after drug withdrawal).
Allergic reactions: angioedema, bronchospasm, urticaria, pruritus, rash.
From the respiratory system: epistaxis.
Timolol (topical application)
Mental disorders: depression.
On the part of the immune system: anaphylaxis, angioedema, urticaria, local or generalized rash.
On the part of the nervous system: tinnitus, paresthesia, headache, asthenia, fatigue, dizziness, insomnia, nightmares, memory loss, increased symptoms of myasthenia gravis.
From the respiratory system: bronchospasm (mainly in patients with previous bronchial obstruction), cough, chest pain.
From the side of the organ of vision: conjunctivitis, blepharitis, keratitis, decreased sensitivity of the cornea, dry eye syndrome, visual disturbances, including changes in the refractive power of the eye (in some cases due to the abolition of myotics), diplopia, ptosis.
From the cardiovascular system: arrhythmia, cardiac arrest, decreased blood pressure, fainting, Raynaud’s syndrome, lowering the temperature of the arms and legs.
From the digestive system: diarrhea, dyspepsia, dry mouth, throat irritation, abdominal pain.
From the skin and subcutaneous tissues: alopecia, psoriasis-like rash or exacerbation of psoriasis.
From the side of the musculoskeletal system and connective tissue: lameness, systemic lupus erythematosus.
From the reproductive system: decreased libido, Peyronie’s disease.
General disorders and disorders at the injection site: edema.
In the post-registration period, the following adverse reactions were observed with the combination of dorzolamide + timolol: shortness of breath, respiratory failure, bradycardia, AV block, detachment of the choroid membrane of the eye, nausea, contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. Cases of edema and irreversible destruction of the cornea have been reported in patients with chronic corneal defects and / or undergoing intraocular surgery.
Terms of delivery from
pharmacies Prescription
Dosage form
drops eye
