Timolol Solofarma - instructions for use, dose, side effects, contraindications

A non-selective beta-adrenergic receptor blocker without sympathomimetic activity. Has no significant internal sympathomimetic, directly oppressing myocardium and local anesthetic (membrane-stabilizing) activity.

Blockade of beta-adrenergic receptors in the bronchi and bronchioles increases the resistance of the respiratory tract, due to the absence of antagonism to parasympathomimetic activity. This effect in patients with bronchial asthma or other bronchospastic states may pose a potential hazard.

Blockade of beta-adrenoreceptors reduces cardiac output in healthy subjects and patients with heart disease. In patients with severe myocardial dysfunction, beta-adrenergic blockade can weaken the stimulatory effect of the sympathetic nervous system necessary to maintain adequate cardiac function.

With topical application in the form of eye drops reduces both normal and increased intraocular pressure by reducing the formation of intraocular fluid. Increased intraocular pressure is the main risk factor in the pathogenesis of the development of glaucoma-specific damage to the optic nerve and narrowing the boundaries of the visual fields. Does not affect the width of the pupil and accommodation.

The exact mechanism for reducing intraocular pressure due to timolol is not known. According to the data of topography and fluorometry in humans, timolol with topical application lowers the intraocular pressure by reducing the formation of watery moisture and a slight increase in its outflow. Reducing intraocular pressure, does not affect the accommodation and the size of the pupil, so there is no deterioration in visual acuity; does not reduce the quality of night vision. The effect manifests itself 20 minutes after instillation.The maximum effect is observed after 1-2 hours. Duration 24 hours.

Pharmacokinetics:

Timolol quickly penetrates the cornea into the tissues of the eye. After instillation in the moisture of the anterior chamber of the eye, the maximum concentration (Cmax) in the blood plasma is reached after 1-2 hours. It enters the systemic bloodstream in an insignificant amount by absorption through the conjunctiva, the mucous membranes of the nose and the lacrimal tract.

('sham timolol in blood plasma is about 0.824 ng / ml and remains up to the detection threshold for 12 hours. In newborns and small children, Timaxol is substantially in excess of Cmax in adult blood plasma.Timolol half-life (T1 / 2) is 4.8 h after topical administration.Timolol metabolism is carried out by the isoeformation of CYP2D6. Timolol and the resulting metabolites are mainly excreted by the kidneys.

Indications:

Increased intraocular pressure (otazmomohypertensia), open-angle glaucoma, glaucoma on the apathetic eye and other types of secondary glaucoma, congenital glaucoma (with no effectiveness of other agents), as an additional means to reduce intraocular pressure in closed-angle glaucoma (in combination with miotics).

Contraindications:

Bronchial asthma, sinus bradycardia, atrioventricular blockade of II and III degree without a pacemaker, decompensated chronic heart failure, cardiogenic shock, severe chronic obstructive pulmonary disease, sinus node weakness syndrome. hypersensitivity to the components of the drug.

Carefully:

Cerebrovascular insufficiency, arterial hypotension, diabetes mellitus, hypoglycemia, pulmonary insufficiency, thyrotoxicosis, myasthenia gravis, sinoatrial blockade, peripheral circulatory disturbance (including Pcido syndrome), pregnancy, simultaneous administration of other beta-adrenergic blockers.

Pregnancy and lactation:

When pregnancy is used with caution, only if the expected therapeutic effect for the mother exceeds the potential risk to the fetus or child.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

At the beginning of treatment, 1-2 drops in the affected eye 2 times a day.

If intraocular pressure with normal use is normalized, you should reduce the dose to 1 drop 1 time a day in the morning.Doses in excess of 1 drop of 0.5% of thioalal solution 2 times a day do not lead to an additional decrease in intraocular pressure. If thymolol is not able to achieve the required level of intraocular pressure, consideration should be given to the use of additional antihypertensive drugs. Simultaneous application of two beta-blockers for topical application is impossible. In patients with a significantly pigmented iris, a less pronounced decrease in intraocular pressure may be noted. as well as a longer period of achievement of intraocular pressure compensation. After discontinuation of treatment, the hypotensive effect of timolol may persist in

for a few days, and in the case of a long previous treatment, the residual and potentive effect may persist for 2 to 4 weeks. When carrying out therapy with thymolol, only one eye can have an antihypertensive effect and in

contralateral eye.

Cantrol effectiveness of the drug is recommended to be performed approximately 3-4 weeks after the start of therapy (not earlier than in 1-2 weeks).With prolonged use of thymol thyme, weakening of the effect is possible.

Transition from another antihypertensive therapy:

When switching from therapy with one beta-adrenergic blocker to therapy with another drug from the group of beta-blockers it is recommended to complete a full day of therapy with a previously used hypotensive agent, and the next day to begin instillation of timolol 0.25% in each affected eye 1 drop 2 times a day .

In the absence of an adequate response to therapy, the dose may be increased to one drop of 0.5% timolol solution in each affected eye twice a day.

When switching to therapy with an antihypertensive drug from another group, except for beta-blockers. continue instillations of the previously prescribed drug with the addition of instillation of one drop of 0.25% solution of timolol into each affected eye twice a day. The next day, the earlier treatment is canceled and timolol therapy is provided.

Use in the pediatric population

According to limited data, timolol can be recommended to reduce intraocular pressure in infantile and juvenile congenital glaucoma in the preoperative period or in the case of ineffective surgical treatment.Before using the drug, you should carefully evaluate the risks and benefits of using timolol in the pediatric population by carefully collecting anamnesis regarding systemic disorders.

In case the benefit outweighs the risk, it is recommended to use timolol in the lowest possible concentration available, 1 drop every 1 day. If there is insufficient control of intraocular pressure, it is necessary to switch to application 2 times a day for

1 drop with an interval between instillations of 12 hours. It is necessary to control eye and systemic side effects within 1-2 hours after the first instillation, especially in newborns and children under 3 years, due to the possibility of developing apnea and respiration according to the Chain-Stokes type. It is necessary to warn parents of the child receiving treatment with timolol that the drug should be canceled in case the child develops side effects and the respiratory system, in particular coughing and sneezing.

Treatment with Timolol is carried out, as a rule, for a long time. A break in treatment or a change in the dosage of the drug is carried out only on the instructions of the attending physician.

Side effects:

Undesirable reactions that occurred after ingestion of timolol and other beta-blockers may be regarded as potential side effects, and for eye care thymolol in the drug form, eye drops.

Undesirable reactions, which were obtained during clinical trials and during post-marketing surveillance of thymol-lal drugs in the drug form, eye drops

The incidence of side effects, both in the course of the studies and in iostmarket monitoring, was assessed as follows: very often (> 1/10); often (> 1/100 to <1/10); sometimes (> 1/1000 to <1/100); rarely (> 1/10000 to <1/1000); very rarely (<1/10000), the frequency is unknown (the available data can not be estimated).

General reactions

With an unknown frequency: headache, asthenia / fatigue, chest pain.

From the side of the organ of vision

Common: blurred vision, eye pain, burning and itching in the eyes, discomfort in the eye, conjunctival injection.

Infrequent: blepharitis, spot keratitis, keratitis, conjunctivitis, iritis, diplopia, erosion of the cornea, corneal ulcer, lacrimation or a decrease in tearing, photophobia, sensation of "sand" in the eyes, edema of the eyelids, edema of the conjunctiva, ptosis.

Rarely: uveitis, double vision, pigmentation of the cornea, erythema eyelids.

Very rarely: the development of calcification of the cornea with significant damage due to the presence of phosphates in the composition of drops.

With an unknown frequency: a decrease in the sensitivity of the cornea, a detachment of vascular gauzes in the postoperative period of antiglaucomatous surgery.

From the side of the cardiovascular system Infrequent: bradycardia, hypotension.

Rarely: myocardial infarction, a decrease or increase in blood pressure, intermittent claudication.

With unknown frequency: cardiac arrest, atrioventricular block, arrhythmia, heart palpitations, congestive heart failure, Raynaud phenomenon.

From the side of the digestive system infrequently: dysgeusia.

Rarely: dyspepsia, dryness of the oral mucosa, abdominal pain.

With an unknown frequency: nausea, vomiting, diarrhea.

From the immune system With an unknown frequency: systemic lupus erythematosus.

Mental disorders Rarely: depression.

With an unknown frequency: insomnia, memory loss, nightmares.

From the side of the nervous system Infrequently: a headache.

Rarely: cerebral ischemia, dizziness, migraine.

With unknown frequency: cerebral circulation, fainting, paresthesia, dizziness, aggravation of myasthenia gravis flow.

From the side of the rut and subcutaneous tissues Rsko: swelling of the face, erythema.

With an unknown frequency: psoriasis or worsening of psoriasis, a localized rash, and elopecia.

From the side of connective tissue With an unknown frequency: arthropathy. muscle pain.

Allergic reactions

With unknown frequency: systemic allergic reactions, including anaphylaxis, angioedema, hives, local or generalized rash. itching.

From the respiratory system and mediastinal organs Infrequent: respiratory failure, dyspnea, bronchitis.

Rarely: bronchospasm (mainly in patients with already existing bronchospastic conditions), cough, nasal congestion, upper respiratory tract infection.

From the endocrine system

With unknown frequency: subclinical course of hypoglycemia in patients with diabetes mellitus (see section "Special instructions").

From the genitourinary system

With unknown frequency: retroperitoneal fibrosis, sexual dysfunction (including impotence), decreased libido, Peyronie's disease.

From the side of ENT organs With an unknown frequency: ringing in the ears.

Undesirable reactions that occurred after taking timolol or other beta-a) repo blockers inside

Allergic reactions: erythematous rash, fever, accompanied by oolio in the throat, laryngiasis, accompanied by a distress syndrome.

General reactions and reactions at the injection site: pain in the limbs, reduced exercise tolerance, weight loss.

From the side of the cardiovascular system: aggravation of arterial insufficiency, in dilation.

From the digestive system: gastrointestinal ool. hepatomegaly. vomiting. thrombosis of the mesenteric arteries, ischemic colitis.

On the part of the blood and lymphatic system: netrombotsitopenicheskaya purpura, thrombocytopenic purpura, agranulocytosis.

On the part of the endocrine system: hyperglycemia, hypoglycemia.

From the skin and subcutaneous tissues: itching, skin irritation, increased pigmentation, sweating.

From the musculoskeletal system: arthralgia.

On the part of the nervous system / mental disorders: vertigo, reduction in the concentration of charging, reversible suppression of mental functions, progressing to catatonia, acute reversible syndrome,characterized by a violation of orientation in time and space, emotional lability, some difficulty in perception and a reduced ability to perform neuropsychiatric tests.

On the part of the respiratory system: wheezing, bronchial obstruction.

From the genitourinary system: difficulty urinating.

Overdose:

It is possible to develop systemic effects characteristic of beta-blockers: dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea and vomiting, loss of consciousness, hypotension, dyspnea, generalized convulsions, cardiogenic shock, heart failure and cardiac arrest.

If you randomly take timolol inside, you should wash your stomach and take activated charcoal. It is shown that the drug can not be removed from the body by hemodialysis.

With the development of bradycardia and bradyarrhythmia (with atrioventricular blockade of II and III degree), intravenous atropine sulfate at a dose of 0.25 to 2 mg is recommended; and the green of partial relief of bradycardia shows the administration of isoprenaline. In cases of labored ectopic bradycardia, consideration should be given to installing a pacemaker.When hypotension is recommended reception simiatomimetikov, such as dopamine, dobutamine, neadrenaline. In the absence of effect - the introduction of glucagon.

In the development of acute heart failure, the use of digitalis and diuretics, as well as oxygen therapy, with intravenous administration of aminophylline

Interaction:

The joint use of the drug with eye drops containing adrenaline can cause a dilated pupil.

A specific action of the drug is a decrease in intraocular pressure, which can be enhanced by simultaneous use of eye drops containing epinephrine and pilocarpine.

Two different running-adrenoblocker should not be instilled in the same eye. Arterial hypotension and bradycardia can increase with simultaneous use of the drug with catheter antagonists, reserpine and systemic beta-blockers.

CYP2D6 inhibitors, such as quinidine and cimetidip may increase the concentration of timolol in the plasma.

Simultaneous use with insulin or oral antidiabetics can lead to hypoglycemia.

Timolol strengthens the action of muscle relaxants, so it is necessary to cancel the drug 48 hours before the planned surgical intervention under general anesthesia.

These data can also refer to medicines that were applied shortly before.

Special instructions:

In the postoperative period of antiglaucomatous operations and with the use of drugs that reduce the secretion of intraocular fluid, the development of a detachment of the choroid of the eye is possible.

The use of timolol by patients with atopy or severe pathological reactions to various allergens in a history can provoke more severe reactions in response to accidental, diagnostic or therapeutic management of allergens. Such patients may respond poorly to the administration of conventional doses of epinephrine to relieve anaphylactic reactions.

Beta-adrenoblockers are able to mask a number of clinical symptoms of hyperthyroidism (and particular tachycardia). Care is required when using beta-aarenoblokatorov in patients with the possibility of developing thyrotoxicosis.

In patients without a history of heart failure, prolonged myocardial depression in some cases may lead todevelopment of heart failure. When the first signs of heart failure occur timolol necessary cancel. Caution is needed when assigning timolol to patients with atrioventricular blockade of the 1st degree, Prinzmetal angina and peripheral circulatory disorders (Raynaud phenomenon).

The main pathogenetic aspect of treating closed-angle glaucoma is the need to open the anterior chamber angle, which is achieved by narrowing the pupil with miotics. In connection with the lack of the influence of timolol on the diameter of the pupil in the treatment of zluztugolnoy glaucoma, the drug can be used only in combination with miotics. Because of the possible effect of beta-adrenoreceptor blockers on blood pressure and the number of heartbeats, these agents should be used with caution in patients with cerebral circulation insufficiency. If, after the initiation of therapy with timolol, signs or symptoms of a decrease in cerebral circulation develop, the need for therapy with local beta-blockers should be reviewed.

The use of timolol may increase muscle weakness in myasthenia gravis (for example.cause increased diplopia, ptosis and general weakness). In some patients with myasthenia gravis and other myasthenic diseases, there was an increase in muscle weakness with timolol.

When used simultaneously with other drugs, the interval between instillations should be at least 15 minutes.

When used, it is necessary to monitor the function of release, the state of the cornea and assess the magnitude of the visual fields at least once every 6 months.

The drug contains a preservative benzalkonium chloride, which can cause eye irritation, can be absorbed by soft contact lenses, causing a change in their color and adversely affecting the eyes. Contact lenses should be removed prior to application of the preparation and, if necessary, dressed again no earlier than 15 minutes after instillation.

With long-term use of the drug, the toxic effect of the benzalkonium chloride preservative on the corneal epithelium (the development of point keratopathy and / or toxic ulcerative keratopathy) is possible.

Cases of development of bacterial keratitis in patients who used timolol in containers for multiple dosing of ophthalmic drugs. These containers were unintentionally contaminated with patients with concomitant diseases of the cornea.

When translating patients for treatment with timolol, correction of refractive changes caused by previously used miotics may be necessary.

The drug, like other beta-blockers, can hide the possible symptoms of hypoglycemia in the blood in patients with diabetes mellitus.

In the case of an upcoming surgical intervention under general anesthesia, it is necessary to cancel the drug 48 hours before the surgery, as it enhances the action of muscle relaxants and general anesthetics.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions in connection with the profile of side effects (in particular, from the side of the eye and nervous system).

Form release / dosage:

Eye drops 0.5%.

5 ml per bottle with a dropper of low-density polyethylene and a lid with a control of the first opening or a flask-dropper made of high-density polyethylene, complete with a cap screwed and stopper-dropper.

For 1 or 3 bottles together with instructions for use in a pack of cardboard.

Packaging:

For 1 or 3 bottles together with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

After opening the bottle - 1 month.

Do not use after the expiration date!

Terms of leave from pharmacies:On prescription

Registration number:LP-003087

Date of registration:13.07.2015

The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia

Manufacturer: & nbsp

GROTEKS, LLC Russia

Representation: & nbspGROTEKS, LLCGROTEKS, LLC

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Timolol Solofarma (Nimolol)