Oftan gel eye drops. Timolol is an effective drug for the treatment of glaucoma. Rules for using the drug depending on the forms presented

After the discovery of the use of the drug propranolol in the treatment of infantile hemangiomas in 2008, it was logical to expect research on the use of this group of drugs in other pharmacological forms, such as drops and gels. The possibility of using local beta-blocker therapy, so-called topical therapy, for the treatment of infantile hemangiomas first became known in 2010.

Results available to the general public using timolol were published on a Scandinavian parenting forum. Parents of a child with segmental infantile hemangioma of the face spoke about their use of Timolol gel in the treatment of their child. Due to the progressive hemangioma, it was planned to use propranolol for the child, but identified cardiac problems did not allow this to be done. Doctors decided to use local therapy. The photographs presented showed that there was an effect and the child began to recover. At the same time, during the examination, no changes were noted in the child’s heart function, which could have been the case with the standard prescription of propranolol in the form of tablets (powders).

In the same year, the first scientific research works in this area were published. Conclusion of these works: timolol helps with this disease and promotes the recovery of children with infantile hemangiomas. But this experience was based on a small group of patients and was more of a pilot study than recommendations for doctors.

In 2012, at an international conference (ISSVA 2012) in Malmo, this problem was actively discussed and reports on this topic have already been presented. According to the results of the reports, the most effective is the use of the drug in the maximum pharmacologically available concentration of 0.5%. For ease of application, it is recommended to use a gel. American and German experts report the most effective use and successful treatment of children with Propranolol gel 1% concentration. But this gel was manufactured to their order by pharmacologists; a gel of such concentration is not commercially available. During this conference, the idea arose of creating a cream (gel) for the treatment of hemangiomas, which would allow treating children with infantile hemangiomas without the use of general therapy (propranolol). The American National Institutes of Health announced in 2012 that it had begun testing such a treatment.

Testing of the use of the special “Proporanolol Gel” is completed in 2014, but this gel has not yet appeared on the pharmacological market and remains a mystery to everyone.

In 2014 in Melbourne (ISSVA 2014), specialists from all countries were expecting the presentation of a new drug. Indeed, at the conference, the company Pierre Fabre Dermatology presented a drug for the treatment of infantile hemangiomas in children, but it was “Hemangeol” - a suspension of propranolol; no other drugs were presented. Perhaps the presentation of the new “Propranolol Gel” has been postponed until 2016 at the next ISSVA conference.

Despite the absence of a “new propanolol gel,” the treatment of children with infantile hemangiomas with local (application) therapy is in full swing and Timolol-based drops and gels are successfully used for this purpose.

The mechanism of action of beta blockers has been studied and there is no doubt that this type of treatment is effective in the treatment of infantile hemangiomas. The main issues in the application of application treatment were: the permeability of this drug through the skin and side effects from such therapy.

A large research work was devoted to the issue of penetration of beta-blockers through the skin - Evaluation of Skin Permeation of beta-blockers for Topical Drug Delivery. These studies confirmed the effectiveness of local therapy in the treatment of infantile hemangiomas. The experiment tested the percutaneous penetration of drugs: propranolol, atenolol, timolol, betaxolol. The study findings confirmed that propranolol and betaxolol are the most effective for local (application) therapy, while timolol and atenolol are in second and third place, respectively, in terms of the effectiveness of percutaneous therapy.

Clinical studies have shown that Timolol successfully penetrates the skin and exerts its therapeutic effect even at low concentrations of 0.1%. But most experts are inclined to use 0.5% Timolol as a drug for the treatment of infantile hemangiomas. .

Use of timolol for the treatment of infantile hemangioma. Hemangioma in the chest area on the right in a 6-week-old girl (A) before treatment and during treatment with timolol - (B) after one month, (C) after three months and (D) after four months of timolol use. Treatment of superficial infantile hemangiomas with timolol: Evaluation of short-term efficacy and safety in infants. Yu L1, Li S, Su B, Liu Z, Fang J, Zhu L, Huang M, Shan W, Song D, Ye B, Luo C. Exp Ther Med.2013 Aug;6(2):388-390. Epub 2013 Jun 21.

A 13-week-old girl with an infantile hemangioma in the right maxillofacial region (A) before treatment and after timolol (B) after one month, (C) after three months, and (D) after four months of timolol. Treatment of superficial infantile hemangiomas with timolol: Evaluation of short-term efficacy and safety in infants. Yu L1, Li S, Su B, Liu Z, Fang J, Zhu L, Huang M, Shan W, Song D, Ye B, Luo C. Exp Ther Med.2013 Aug;6(2):388-390. Epub 2013 Jun 21.

Application of propranolol-based gel.

The next serious issue was the study of the development of possible side effects from the use of this therapy, but as studies have shown, Timolol gel at a concentration of 0.5% does not have a systemic effect on the body (effect on the heart, pancreas, bronchi), its concentration in plasma is lower permissible limit (QL = 0.8 ng/ml). However, according to doctors, contraindications and side effects of systemic beta blockers should be taken into account.

In conclusion, I would like to summarize the information on this topic: the use of 0.5% Timolol is an effective, fairly safe method of treating small superficial infantile hemangiomas during the period of their active growth in children under 6 months/

Despite the availability of this drug in the pharmacy chain, any prescription of treatment should be carried out by a doctor, taking into account the clinical situation and general health of the patient.

P.S. In our clinic we have extensive experience in using local therapy, but we will talk about this in the next publication.

Bibliography:

1. Topical treatment for capillary hemangioma of the eyelid using beta-blocker solution. Guo S, Ni N. Arch Ophthalmol. 2010 Feb;128(2):255-6. doi: 10.1001/archophthalmol.2009.370.
2. Topical timolol gel for infantile hemangiomas: a study pilot. Pope E, Chakkittakandiyil A. Arch Dermatol. 2010 May;146(5):564-5. doi: 10.1001/archdermatol.2010.67.
3. Topical Propranolol Therapy for Infantile Hemangiomas. Karin Kunzi-Rapp, M.D., Department of Dermatology and Allergic Diseases, Ulm, Institute for Laser Technologies in Medicine and Metrology, University of Ulm, Ulm, Germany
4. https://clinicaltrials.gov/ct2/show/NCT01512173?intr=propranolol&lead=Pierre+Fabre&rank=2
5. Evaluation of skin permeation of β-blockers for topical drug delivery. Chantasart D1, Hao J, Li SK. Pharm Res.2013 Mar;30(3):866-77. doi:10.1007/s11095-012-0928-9. Epub 2012 Dec 4.
6. Topical timolol maleate for treatment of infantile haemangiomas: preliminary results of a prospective study. Semkova K1, Kazandjieva J. Clin Exp Dermatol.2013 Mar;38(2):143-6. doi: 10.1111/j.1365-2230.2012.04425.x. Epub 2012 Jun 25.
7. Treatment of superficial infantile hemangiomas with timolol: Evaluation of short-term efficacy and safety in infants. Yu L1, Li S, Su B, Liu Z, Fang J, Zhu L, Huang M, Shan W, Song D, Ye B, Luo C. Exp Ther Med.2013 Aug;6(2):388-390. Epub 2013 Jun 21.
8. Topical timolol 0.5% gel-forming solution for small deep facial infantile hemangiomas. Sorrell J1, Chamlin SL. Pediatr Dermatol.2013 Sep-Oct;30(5):592-4. doi: 10.1111/pde.12209. Epub 2013 Jul 26.
9. Management of superficial infantile capillary hemangiomas with topical timolol maleate solution. Rizvi SA1, Yusuf F, Sharma R, Rizvi SW. Semin Ophthalmol.2015 Jan;30(1):62-4. doi: 10.3109/08820538.2013.821505. Epub 2013 Sep
10. Infantile Hemangioma of the Eyelid Treated with Timolol Gel. Fernandez-Ballesteros MD, et al. Hemangioma infantil palpebral tratado con timolol gel. Actas Dermosifiliogr.2012;103:444-6.

The effectiveness of using this remedy in the fight against hemangioma is due to the ability of the active substance called timolol, which easily penetrates through the pores of the epidermis to the source of the problem, while providing a therapeutic effect.

It is worth highlighting a number of important characteristics:

Despite the advantages and prospects for treating hemangioma, the drug has certain limitations in use. Therefore, it is prohibited for use in patients with:

• hypersensitivity to the components of the drug;
• chronic bronchitis of non-allergic type;
• heart failure (acute, chronic form);
• chest problems;
• lesions of the respiratory tract of a diffuse nature;
• problems with the nasopharynx in terms of the presence of vascular tone;
• last degree of left ventricular failure;
• lesions of the autonomic nervous system.

For the treatment of hemangioma, it is advisable to use this drug, manufactured in the form of a gel.

Rules for using the drug depending on the forms presented

As mentioned earlier, the drug is available in the form of a gel or drops. Treatment in this regard has some features:

• The product is in the form of a gel. This form is most effective if we are talking about curing a benign neoplasm in the form of a hemangioma. The procedure involves applying the product at least 2 times a day to the formation itself. The first results will be noticeable in 5-6 days. If used regularly for a month, the neoplasm loses its bright color, then this process stops, but it is practically invisible on the skin. The full therapeutic effect is achieved after a few months.
• Timolol drip version. This form is also actively used for treatment. The product is applied in its pure form in an amount of about 3 drops to the place where the formation is located. The procedure must be repeated about 4 times a day. It is recommended to make compresses-bandages on which the product is applied. Place sterile gauze on top or secure the compress with a special plaster. The frequency of this procedure can also reach up to 3 times a day.

From the point of view of compatibility with other drugs and medications, the question is ambiguous, since the manifestations can be different - from lowering blood pressure to heart problems. Therefore, the prescription of Timolol should be preceded by a doctor studying all the patient’s concomitant diseases.

There are eye diseases that cause increased intraocular pressure. This leads to optic nerve atrophy and the development of visual field defects. When the pathological process begins to progress, complete loss of vision is possible. All these phenomena are assessed by ophthalmologists as signs of glaucoma. In such cases, they recommend using Timolol in the form of eye drops.

The main direction of action of the product is to prevent the formation of aqueous humor, which affects intraocular pressure. Timolol promotes the outflow of intraocular fluid; it is characterized by good tolerability and a minimum of side effects.

Timolol release form

In the pharmacy chain, the drug Timolol is presented in the form:

1. Eye drops from different manufacturers (Timolol, Oftan Timolol, Timolol-Akos, Timolol-Pos, Timolol-Mez, etc.). Each brand is distinguished by the presence of individual substances that are part of the product - all of them are recorded in the instructions for Timolol;
2. Tablets for oral use;
3. Timolol gel for hemangioma and other benign formations on the skin;
4. Oftan Timogel eye gel;
5. Let's take a closer look at the drug Timolol in the form of eye drops.

Composition of the ophthalmic drug Timolol

The main active substance included in the product is timolol. In addition to it, the drug includes a number of auxiliary components:

• Sterile water, which is a universal solvent.

Eye drops are a clear, odorless liquid. Available in plastic bottles with a volume of 5 ml and a substance concentration of 0.25% or 0.5%.

Indications for use

Timolol can be used by people over 18 years of age. It is used to treat:

1. Angle-closure type (in parallel with the use of miotics);
2. Secondary glaucoma (afactual, uveal, post-traumatic);
3. Used for increased intraocular pressure after various inflammatory processes.

How does Timolol work?

The drug belongs to the category of non-selective beta-adrenergic receptor blockers. When Timolol is applied topically, the level of aqueous humor decreases, which significantly reduces intraocular pressure. At the same time, the drug does not have a negative effect on accommodation, vision does not decrease, and pupil sizes do not change.

The drops begin to act 25 minutes after application. The antiglaucoma effect lasts for 24 hours. The pharmaceutical drug is excreted through the kidneys.

Directions for use and doses

When opening the bottle, turn the cap, separating it from the protective ring. A spike located inside the cap punches a hole. Before use, the bottle should be held in your hand so that the contents warm up to body temperature.

Thanks to the special configuration of the bottle, the solution is released in doses. With one press on the bottom of the bottle you can squeeze out only one drop. This eliminates the possibility of a jet of solution escaping, which is a common cause of overdose of eye drops.

The product is instilled into the conjunctival sac of the diseased eye. After this, close the eyes and gently press the inner corner of the eye with a finger for one to two minutes so that the solution does not get into the tear ducts. This will help avoid side effects.

In the first days, drop one drop of a 0.25 percent solution, morning and evening. When intraocular pressure stabilizes, once a day is sufficient. If the treatment does not give the desired result, the doctor may prescribe a 0.5 percent solution. The doctor determines the duration of the course of therapy individually.

Interaction of Timolol with other pharmaceuticals

When Timolol interacts
With other drugs, the body’s reaction can be very different, so before using it you need to familiarize yourself with this topic.

• When using Epinephrine, Pilocarpine, muscle relaxants in combination with Timolol, the therapeutic effect of these drugs increases, which can lead to the risk of overdose.
• The use of cardiac glycosides simultaneously with drops can cause acute left ventricular failure, a sharp drop in blood pressure and impaired atrioventricular conduction.
• It is not recommended to prescribe Reserpine during treatment with Timolol, otherwise severe bradycardia and a rapid drop in blood pressure are possible.
• It is unacceptable to use local anesthetics together with eye drops - this is fraught with complications of the cardiovascular system.

During the course of treatment with Timolol, you should refrain from drinking alcohol to avoid side effects.

Contraindications

Since Timolol drops have a number of contraindications, you should consult an ophthalmologist before starting treatment.

The drug is contraindicated:

1. Patients under 18 years of age;
2. During pregnancy and lactation;
3. Hypersensitivity to the ingredients of the drops;
4. Bronchial asthma;
5. Chronic obstructive pulmonary diseases;
6. Heart failure;
7. Acute rhinitis;
8. Dystrophic diseases of the cornea;
9. Sinus bradycardia;
10. Diabetes mellitus;
11. After a myocardial infarction.

Side effects

In most cases, the drug was well tolerated, which is confirmed by positive reviews of Timolol. However, if you do not follow the instructions, as well as in the presence of individual sensitivity, side effects are possible, which are expressed in:

• Pain, burning or itching during installation;
• Photophobia;
• Dry eyes and watery eyes;
• Swelling of the eyelids;
• Double vision;
• Redness of the mucous membrane of the eye;
• Pupil dilation.

Typically, such phenomena disappear within 20 minutes after applying the drops. In rare cases, Timolol can cause headache, general weakness, dizziness, shortness of breath, cough, rapid heartbeat, and dyspepsia. In such situations, treatment with Timolol should be discontinued.

special instructions

When undergoing a course of therapy, it is important to adhere to the following recommendations.

1. Before installation, remove contact lenses from your eyes;
2. Instill another ophthalmic drug no earlier than 20 minutes after using Timolol;
3. Refrain from driving a car, as short-term double vision and blurred vision, as well as decreased concentration, are possible;
4. Regularly see your doctor to monitor the condition of the cornea, visual acuity, visual field, etc.

You will learn how to apply eye drops correctly from our video.

Timolol: analogues

Analogs of Timolol include ophthalmic drugs that have antiglaucoma effects. You can replace Timolol with Oftan Timolol, Oftimol, Okumed, Iotim, Unitimol, Kusimol, Okuril, Arutimol, Glautam, Timadren, etc.

If you need to change the drug, be sure to consult with an ophthalmologist, since each pharmaceutical product is characterized by its own characteristics and has certain contraindications.

Timolol (eye drops 0.5%, in a 5 ml dropper bottle)

Timolol is a prescription drug belonging to the group of adrenergic blockers and antiglaucoma drugs. In the form of eye drops, it is included in the list of vital medications.

pharmachologic effect

Reduces output, excitability, contractility and the need for oxygen in the middle muscular layer of the heart - the myocardium. Used orally for high blood pressure, to prevent migraine-like pain of vascular origin and to prevent heart attacks. The cardioprotective effect allows in some cases to avoid the risk of sudden death due to myocardial infarction.

In the form of eye drops, it is used for open-angle and secondary glaucoma. The action is to reduce the secretion and outflow of aqueous humor in the middle shell of the eye - the ciliary body involved in the process of accommodation, as a result of which intraocular pressure decreases. Thanks to the topical use of timolol, IOP control during sleep is possible. The effect is observed 15-30 minutes after instillation and lasts from 12 to 24 hours.

Contraindications

Prescription for internal or local administration is not allowed for the following pathologies:

• sinus bradycardia;
• history of bronchial asthma;
• disorders of atrioventricular conduction of the heart;
• heart failure;
• chronic obstructive pulmonary diseases;
• cardiogenic shock;
• corneal dystrophy;
• severe allergic processes of the nasal mucosa.

Restrictions on use are for patients with the following diseases:

• emphysema;
• Raynaud's syndrome;
• vasomotor rhinitis;
• Chronical bronchitis;
• diabetes mellitus and hypoglycemia;
• severe functional disorders of the liver and kidneys;
• hyperthyroidism;
• increased stomach acidity.

Also, women should not use the solution during pregnancy, during breastfeeding, young children, the elderly or those who are hypersensitive to the components of the drug.

Mode of application

Before instillation, the bottle should be turned over and shaken sharply once. Inject a drop into each eye 1-2 times a day. Exceeding the dosage can cause headaches, dizziness, arrhythmia, nausea, vomiting, and bronchospasm.

Precautionary measures

It is necessary to visit a doctor every 6 months to monitor tear production, visual field, intraocular pressure and corneal integrity. In addition, regular monitoring of blood pressure and pulse is important.

Use with caution for employees whose work requires increased concentration.

Study the prices for timolol in pharmacies in Chelyabinsk, they may vary. Choose the most profitable option for you in the nearest pharmacies in the city.

Benzalkonium chloride, lysine monohydrate, sodium acetate trihydrate, water, sorbitol.

Release form

Oftan Timogel is produced in the form of a gel. The gel is odorless and colorless and is capable of opalescence. In cardboard packs there are polyethylene bottles of 5 grams.

pharmachologic effect

Antiglaucoma drug .

Pharmacodynamics and pharmacokinetics

The active ingredient of the drug Oftan Timogel is non-selective beta blocker . It has the ability to reduce by reducing the intensity of aqueous humor production.

Antiglaucoma drug affects the process of fluid outflow inside the eye. The product also has a weak anesthetic effect and does not affect accommodation and the size of the pupils. Deterioration of vision or night blindness is not observed during use of the product. The mechanism of action of the active component has not yet been fully studied.

The effect of the medicine develops within several hours after instillation and lasts 24 hours.

The drug can penetrate into the systemic circulation through small vessels conjunctiva , lacrimal tract or nasal mucosa. Rarely, one and a half hours after use, the medicine can be detected in the serum. It should be noted that timolol excreted in breast milk and found in low concentrations in urine for a long period after ingestion.

Indications for use

Oftan Timogel is prescribed:

• with increased intraocular pressure ;
• for treatment open angle ;
• at uveal, post-traumatic, aphakic glaucoma .

Contraindications

The medicine is contraindicated:

• at dystrophic diseases of the cornea eyes;
• at ;
• at bradycardia ;
• people suffering;
• for chronic bronchospasm ;
• at AV block second and third degrees;
• at cardiogenic shock ;
• persons prone to the components of the product or timolol maleate .

Please be careful:

• at pulmonary insufficiency ;
• under the age of 12;
• for severe cerebrovascular insufficiency ;
• sick;
• at , hypoglycemia , ;
• combining medicine with other beta blockers ;
• for chronic heart failure .

Side effects

The most common local reactions:

• discomfort in the eyes;
• pain and burning immediately after applying the gel;
• conjunctival hyperemia .

Rarely may occur:

• problems with vision clarity (disappears after 3 minutes);
• special sensitivity to light, lacrimation;
• edema epithelial tissue on the cornea;
• eyelid hyperemia ;
• , blepharitis , ;
• the appearance of more persistent visual impairment ( refractive error , diplopia , surface point keratopathy );

The following adverse reactions may occur if the medicine enters the systemic circulation.

If acute heart failure occurs, you should use diuretics , oxygen, drugs foxgloves , aminophylline , .

Interaction

Combine medicine with caution with drugs foxgloves , verapamine , , (intramuscular) and X-ray contrast agents containing iodine .

When combining Oftan Timogel with cimetidine , content in timolol may increase significantly.

Terms of sale

In order to purchase the medicine, a prescription is required.

Storage conditions

The drug should be kept away from children. The temperature should not exceed 25 degrees; the medicine should not be frozen.
After opening the bottle, it should be stored upside down in a cardboard box.

Best before date

A year and six months.

Once opened, the medicine can be stored for a month.

special instructions

At angle-closure glaucoma it is recommended to combine the medicine with miotics .

If any dermatological reactions occur during treatment, you should stop taking the drug and consult your doctor.

In patients suffering