Instructions for use OPATANOL

Pharmacodynamics and pharmacokinetics

The drug is a selective histamine H1 receptor inhibitor that also inhibits the release of inflammatory mediators from mast cells . It has pronounced antiallergic properties.

When applied topically, systemic absorption of the drug is quite low. The maximum concentration of the active substance in plasma is observed after 2 hours. The half-life in plasma is 3 hours. Mainly, the medicine is excreted through the kidneys. About 65% is excreted unchanged.

Instructions for use OPATANOL

Suction

Olopatadine, like other topical drugs, undergoes systemic absorption. However, systemic absorption of topically administered olopatadine is negligible, and plasma concentrations can vary from the lowest quantifiable value (<0.5 ng/mL) to 1.3 ng/mL. These concentrations are 50-200 times lower than the concentrations after the administration of well-tolerated doses of the drug orally.

Metabolism and excretion

When studying pharmacokinetic parameters when prescribing the drug orally, it was revealed that T1/2 of olopatadine in plasma ranges from 8 to 12 hours, and excretion is carried out mainly by the kidneys. Approximately 60-70% of the dose received is found in the urine as the active substance. Two metabolites were also found in urine in low concentrations: monodesmethyl and N-oxide.

Pharmacokinetics in special clinical situations

In pharmacokinetic studies following oral administration of 10 mg olopatadine in young (mean age 21 years) and elderly (mean age 74 years) patients, there were no significant differences between plasma concentrations (AUC), protein binding, and urinary excretion of the parent drug unchanged. and not found in the form of metabolites.

Since olopatadine is excreted by the kidneys mainly in the form of unchanged active substance, impaired renal function causes changes in the pharmacokinetic parameters of olopatadine - in patients with severely impaired renal function (average CC value - 13.0 ml/min), its Cmax in plasma is 2.3 times higher than in healthy people adults. Following oral administration of 10 mg in hemodialysis patients (without urinary excretion), olopatadine plasma concentrations were significantly lower on the day of the procedure than on other days, suggesting that hemodialysis may promote the elimination of olopatadine.

A study was conducted in patients with severe renal impairment in which olopatadine was administered orally. The results obtained indicate a higher plasma concentration of olopatadine in this group of patients. Since plasma concentrations of olopatadine after instillation of the drug Opatanol into the eyes are 50-100 times lower than after oral administration in well-tolerated doses, dose adjustment is not required when prescribed to elderly patients or patients with impaired renal function.

Hepatic metabolism is a less significant route of drug elimination. No dose adjustment is required for liver dysfunction.

Side effects

When using the drug, the following local reactions are possible: lacrimation , conjunctival hyperemia , burning and pain, as well as an unpleasant sensation of a foreign body in the eyes, iritis , keratitis , blurred vision, swelling of the eyelids.

In addition, systemic manifestations such as dizziness , weakness, pharyngitis , sinusitis , headache , nausea, rhinitis , and changes in taste are likely.

Types of eye allergies

There are a wide variety of forms of eye allergies, the most common of which are allergic dermatitis and conjunctivitis. But it should be noted that an allergic reaction can affect all structures of the eye and cause damage to them, for example, keratitis (inflammation of the cornea), papilledema, uveitis, etc. An allergic process in the eyes or eyelids can be either an independent disease (a reaction to the ingestion of cosmetics, medications, or be a manifestation of a systemic disease (hay fever, etc.).[1]

Fig. 1 Manifestation of allergies in the eyes: conjunctivitis, blepharitis and their combination (blepharoconjunctivitis)

Analogues of Opatanol

Level 4 ATX code matches: Polinadim
Vizin Alergy

Zaditen

Cromohexal

Lecrolin

Ketotifen

Analogs of Opatanol eye drops that have the same level 4 ATC code:

• Ifiral;
• Allergodil;
• Alergokrom;
• Ketotifen;
• Lastakaft;
• Cromo Sandoz;
• Lecrolin;
• Kromofarm.

All Opatanol analogues have their own application characteristics, so it is not recommended to use them without consulting a specialist.

List of eye drops for allergies

Material prepared by: Sagonenko Dmitry Alekseevich

Ophthalmologist, site consultant

Opatanol price, where to buy

In most cases, the price of Opatanol eye drops is considered very high. However, if the product helps, patients believe that such a cost is justified. The price of Opatanol is on average 360 ​​rubles.

• Online pharmacies in RussiaRussia

ZdravCity

• Opatanol eye drops 0.1% 5mlS.A.
  Alcon-Couvreur nv RUR 528 order

Types of eye drops for allergies

Vasoconstrictor drops

These drugs constrict blood vessels, thereby reducing redness and swelling of the mucous membrane. They only eliminate the symptoms, but do not solve the problem. Such drops can be used “once”, in case of urgent need to “look beautiful” for several hours. With long-term use, they are addictive, and their subsequent withdrawal can create a “withdrawal effect” - a rapid return of all manifestations of the disease.[2]

Fig. 2 The main vasoconstrictor drugs - “Vizin”, “Okumetil”, “Octilia”

Antihistamine eye drops

Drugs in this group prevent the accumulation of histamine, which is one of the main factors in the development of allergic reactions. These are H1 receptor blockers, they reduce the tissue response to histamine. Antihistamine eye drops are effective against symptoms such as itching and swelling. As a rule, they are prescribed as the first remedy for the treatment of allergic eye diseases.

These include “Allergodil”, “Visallergol”, “Spersallerg”, “Opatanol”.

Combined antihistamine eye drops containing an additional vasoconstrictor component (“Polynadim”) have the fastest and most pronounced effect.[3]

Fig. 3 Basic antihistamine drops for allergies

Mast cell stabilizers

Medicines in this group block the release of histamine and other substances that cause allergy symptoms from mast cells, highly specialized immune cells that play a major role in the development of an allergic reaction.

A feature of drugs belonging to this group is the accumulation effect - they do not act immediately after administration: the effect is achieved more slowly, but lasts longer. Therefore, in order to reduce symptoms, it is recommended to start taking these anti-allergy medications early, before the start of the allergy season.[4]

This group of drugs includes drops based on disodium cromoglycate “Kromhexal”, “Lecrolin”, “High-Krom”, “Kromitsin”, etc.

Fig. 4 Drops for the prevention of allergies - mast cell stabilizers

Anti-inflammatory eye drops for allergies

Anti-inflammatory drugs for instillation are divided into two groups:

Corticosteroid drugs. Eye drops containing corticosteroids are sometimes used to relieve acute allergic symptoms, but they are usually prescribed only for a short period of time due to the fact that they cause side effects with long-term use.[5] This group of medications includes Dexamethasone, Maxidex and hydrocortisone eye ointment.

Fig. 5 Glucocorticosteroids (GCS) in the form of ophthalmic agents.

Nonsteroidal anti-inflammatory drugs (NSAIDs). Eye drops containing non-steroidal anti-inflammatory drugs are prescribed to reduce inflammation, swelling and other manifestations of allergic reactions.[6] Among the drugs in this group: Indocollir, Diclofenac, Naklof, Diklo F.

Fig.6 Non-steroidal anti-inflammatory drugs (NSAIDs) in the form of drops

Tear substitutes

Tear substitutes have a moisturizing effect on the eyes, coping with allergy symptoms such as dryness, redness and irritation of the mucous membrane. To provide an additional calming (cooling) effect for allergic inflammation, it is recommended to store these eye drops in the refrigerator.

Tear substitutes are completely safe, so they can be used without restrictions as needed. Such drops significantly improve the comfort and quality of life of patients with allergies.

This group of drugs includes “Kationorm”, “Okutiarz”, “Oftagel”.

Fig. 7 Tear substitutes (moisturizing drops) used for eye allergies

“Cationorm” is a unique cationic emulsion that is suitable for people with glaucoma, blepharitis, allergic conjunctivitis and people using hormone replacement therapy (menopausal hormones, oral contraceptives). The drug restores all three layers of tears and prevents itching and redness of the eyes. Cationorm helps with severe pain and dryness in the eyes that appears in the morning, and quickly relieves discomfort. Drops can be applied directly to lenses. Drops should be used 1-2 drops into the eye sac 1-4 times a day.[7]

"Ocutiarz" - eye drops based on hyaluronic acid (a natural component of human tears) with an ultra-high molecular weight help to quickly relieve dryness and eliminate pain in the eyes that occurs occasionally after prolonged visual work (computer syndrome in office employees, motorists/motorcyclists, frequent fliers , travelers, students). In addition, the drops are suitable for people after ophthalmic surgery and people who have recently worn contact lenses. They do not contain preservatives and can be in direct contact with lenses. Directions for use: 1-4 times a day, 1 drop.[8]

“Oftagel” is an eye gel with carbomer in maximum concentration that moisturizes the ocular surface for a long time, eliminates pain and lacrimation of the eyes, and does not require frequent instillation; it can be used once a day as a means of additional eye hydration. Suitable for people who do not have the opportunity or desire to use drops during the day. Use 1 drop of the drug 1 – 4 times a day, depending on the severity of symptoms.[9]