EN AR FR ES DE
► Azarga (brinzolamide + timolol) - Practical Medicine

Azarga (brinzolamide + timolol) - eye drops, suspension

The name of the preparation Character; dose; package Manufacturer Price 100% Price after refund In which pharmacy?
AZARGA eye drops, suspension; 1 ml contains: 10 mg brinzolamide, 5 mg timolol (as timolol maleate); 5 ml Novartis Europharm 79.99

Note: reimbursed drug prices are in line with the regulations in force from July 1, 2018.

The preparation contains the substance:brinzolamide + timolol

The drug is available on prescription

What is Azarga?

A topical application to the eye (in the conjunctival sac) containing a beta-blocker (timolol) and a carbonic anhydrase inhibitor (brinzolamide). Both active substances reduce intraocular pressure due to different mechanisms of action. The effect of the preparation is stronger than when each component is used as monotherapy.

What does Azarga contain and how does it work?

It is a combined preparation containing 2 active substances: timolol and brinzolamide. Timolol belongs to a group of medicines called beta-blockers (another name is beta-blockers). These drugs work by blocking certain types of receptors, called beta adrenergic receptors. These are receptors stimulated in physiological conditions by adrenaline or noradrenaline released after the activation of the sympathetic nervous system. Pharmacological blocking of receptors prevents them from being stimulated, thereby reducing the effects of adrenaline or noradrenaline on target tissues with beta receptors. Preparations from this group are mainly used as antihypertensive drugs and in the course of cardiovascular diseases. In the form of eye drops, timolol is applied topically to the conjunctival sac, where it lowers intraocular pressure by reducing the production of aqueous humor. It does not affect the width of the pupil or the eye's accommodation. From the conjunctival sac, timolol penetrates well into the eye's structures and is largely absorbed into the blood and can cause systemic side effects. The other active ingredient in the preparation, brinzolamide, is a sulphonamide used topically in ophthalmology to lower intraocular pressure. It inhibits the activity of the enzyme dehydratase (anhydrase) carbonate. Carbonate dehydratase is an enzyme found in many tissues of the body, including the eye. Inhibition of this enzyme in the processes of the ciliary body of the eye leads to a decrease in the production of aqueous humor and, consequently, to lower intraocular pressure. After administration to the conjunctival sac, brinzolamide exerts a local action, it is also absorbed into the general circulation. Brinzolamide and its metabolites are mainly excreted by the kidneys.

When to use Azarga?

It is indicated for the reduction of intraocular pressure in adults with open-angle glaucoma or ocular hypertension who have not sufficiently reduced intra-ocular pressure using monotherapy.

When not to use this preparation?

Unfortunately, even if there are indications to use the preparation, it can not always be used. You can not use the product if you are allergic (you are hypersensitive) to any of the ingredients or other medicines from the group of sulfonamides or beta-blockers.
You can not use the preparation if you are present:
· Bronchial asthma (also in the past)
· Severe obstructive pulmonary disease
· Sinus bradycardia
· 2nd or 3rd degree atrioventricular block
· Cardiogenic shock
· Symptomatic heart failure
· Severe allergic rhinitis or hyperresponsiveness of the bronchi
· Hyperchloraemic acidosis
· Severe renal dysfunction (creatinine clearance less than 30 ml / min).
Do not use the preparation in pregnant women, unless the doctor considers it absolutely necessary.

Take special care with Azarga?

Certain diseases and other circumstances may constitute a contraindication to use or indication to change the dosage of the preparation. In some situations it may be necessary to carry out specific check-ups.
The preparation is intended only for external application, locally to the conjunctival sac.
Beta-blockers, including timolol, topically applied (to the conjunctival sac) can be absorbed and cause systemic side effects that are characteristic of this class of drugs.
In patients with heart failure, it is necessary to stabilize it before starting treatment. Patients with severe heart disease should remain under careful medical supervision in the past. It is recommended to observe whether there are signs of heart failure and control of heart rate.
The use of timolol may lead to worsening of heart failure, occasionally leading to death.
Administration of a beta-blocker (also in the form of eye drops) may occasionally result in an asthma attack or respiratory distress in patients with an increased risk of bronchospasm. Bronchospasm in patients with asthma can be life-threatening.
Patients with diabetes and those at risk of hypoglycaemia (low blood glucose) should take special care because beta-blockers may mask the symptoms of hypoglycaemia, such as palpitations, increased heart rate (tachycardia) or sweating. You should monitor your blood glucose.
The preparation may also mask the symptoms of hyperthyroidism, worsen the course of Prinzmetal vasospastic angina, severe peripheral and central circulatory disorders and hypotension.
Brynzolamide is a sulfonamide and, despite local application, it is absorbed into the systemic circulation. Therefore, adverse reactions characteristic of sulfonamides commonly used (e.g., orally), including severe hypersensitivity reactions, such as Stevens and Johnson syndrome, toxic epidermal necrolysis, or severe hematological disorders, may occur. If you suspect any hypersensitivity symptoms, please consult your doctor immediately (before re-applying the preparation). The doctor may recommend discontinuation of the preparation (in severe cases, immediate treatment may be necessary).
Oral use of carbonic anhydrase inhibitors may be associated with urolithiasis due to disturbances of the acid-base balance. The possibility of such disorders should be considered when using the preparation, because brinzolamide is absorbed into the systemic circulation.
Co-administration with other carbonic anhydrase inhibitors is not recommended orally (systemically acting) due to the risk of increased activity and side effects.
Beta-blockers may increase sensitivity to allergens and increase hypersensitivity reactions (including anaphylactic reactions including anaphylactic shock). It is possible to reduce the effectiveness of adrenaline used then. Special care should be taken when using the preparation in patients with atopic dermatitis and in people prone to allergic reactions.
Caution should be used if the product is used in parallel with other beta-blockers taken by mouth (systemically acting), due to the risk of mutual potentiation and side effects, both local and systemic.
Parallel administration of 2. topical beta-blockers or 2. topically administered carbonic anhydrase inhibitors is not recommended.
There are insufficient data on the efficacy and safety of the preparation in patients with glaucoma in the course of exfoliative pseudoexfoliation syndrome and pigment glaucoma. The use of the preparation in these groups of patients requires careful attention and close monitoring of intraocular pressure.There are no data on the use of the preparation in patients with obstructed angulation glaucoma and the use of the preparation in this group of patients is not recommended.
Brinzolamide is absorbed into the systemic circulation and, in the elderly, may, like oral medications in this group, impair the ability to perform tasks requiring increased concentration and / or motor coordination.
There are no data on the effect of the preparation on corneal endothelial function in patients with corneal damage, especially in patients with low corneal endothelial cells. During the period of application, persons using contact lenses should remain under careful medical supervision. The preparation may affect the degree of corneal hydration which may increase the corneal risk associated with the use of contact lenses. Staying under careful medical observation is also recommended in other cases of corneal damage, such as, for example, in patients with diabetes or corneal dystrophy.
The preservative of benzalkonium chloride contained in the preparation may cause point or toxic ulcerative keratopathy. If the preparation is used in patients with dry eye or corneal lesions, careful medical supervision and observation of the patient is required.
Additional information about the other ingredients of the preparation:
the preparation contains benzalkonium chloride as a preservative, which can accumulate in contact lenses and destroy them (cause discoloration); people who use contact lenses should remove them before instillation and wait at least 15 minutes before re-inserting.

Does this preparation affect the ability to drive vehicles?
Caution should be exercised because, when administered to the eye, transient visual disturbances may occur which may impair the ability to drive vehicles and operate machinery / equipment. If visual disturbances occur, do not drive or operate mechanical devices until the disorder is resolved and acute vision returns.
Brinzolamide is absorbed into the systemic circulation and, in the elderly, may, like oral medications in this group, impair the ability to perform tasks requiring increased concentration and / or motor coordination.

Dosage of Azarga

The preparation is in the form of eye drops. Use the product as directed by your doctor. Do not exceed the recommended doses because it will not increase the effectiveness of the drug and may harm your health and life. If you have any doubts regarding the use of the preparation, consult a physician.
Adults:
Usually 1 drop 2 times a day, into the conjunctival sac.
To minimize the systemic absorption of the product, it is recommended to close the eyelid or to gently compress the nasolabial canal after instillation.
If other medicines were used before in the treatment of glaucoma, the physician will determine an individual scheme for changing the method of treatment.
If other preparations administered to the eyes are used in parallel, wait at least 5 minutes between administrations of the next drugs.
Shake the bottle thoroughly before using the product. Keep the bottle tightly closed.
Wash your hands before using the product. Do not touch the surface of the eye or the eyelid or any other surface with the dropper tip, as this may contaminate the product and lead to eye infection. The infection can cause serious eye damage or blindness.
Contraindication is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 ml / min) or with hyperchloraemic acidosis.
Children:
The safety and efficacy of the preparation in children and adolescents up to 18 years has not been established and its use is not recommended in this age group.

Can Azarga be used during pregnancy and breastfeeding?

During pregnancy, do not use any medicine without consulting your doctor!
It is very important that before using any medicine during pregnancy or breastfeeding, consult a physician and explain beyond any doubt the potential risks and benefits associated with the use of the drug. If you are pregnant or plan to become pregnant, please inform the doctor prescribing the prescription for this medicine.
Do not use the preparation during pregnancy unless the doctor deems it necessary.
Before using the preparation during breastfeeding, consult a doctor.

Can I use other preparations in parallel?

Tell your doctor about all medicines you have recently taken, including those that are over the counter.
No specific interaction studies have been performed with other drugs.
The brinzolamide contained in the preparation is a carbonic anhydrase inhibitor. If the preparation is used in parallel with other carbonic anhydrase inhibitors when taken orally (acting systemically), there is a risk of increased activity and side effects, such as acid-base imbalance. Combination therapy is not recommended.
Caution should be exercised if drugs inhibiting the activity of cytochrome P450 3A4 is co-administered, such as, for example, ketoconazole, itraconazole, clotrimazole, ritonavir, troleandomycin; these drugs may inhibit brinzolamide metabolism, but should not cause accumulation.
The preparation contains timolol, a drug from the beta-blocker group. Caution should be exercised if the preparation is used in parallel with the following drugs (generally administered), due to the risk of increased action leading to a reduction in heart rate (bradycardia) and marked hypotension:
· Beta-blockers (another name: beta-blockers)
· Calcium channel antagonists (eg verapamil, diltiazem, nifedipine)
· Anti-arrhythmic drugs
· Digitalis glycosides
· parasympathomimetics
Antihypertensives, such as, for example, reserpine, clonidine, methyldopa, guanethidine, guanfacine.
During the period of application, the use of antihypertensives, such as clonidine, should not be discontinued suddenly due to the risk of a sudden increase in blood pressure.
Quinidine and other drugs that inhibit the activity of the cytochrome P450 2D6 isoenzyme can inhibit the metabolism of thymolol and potentiate its action, which can lead to lower blood pressure and lower heart rate (bradycardia).
Special care should be taken if the product is used in parallel with insulin or oral antidiabetic agents; beta-blockers may mask the symptoms of hypoglycaemia; you should monitor your blood glucose, especially at the beginning of treatment. It may be necessary to adjust the dosage of antidiabetic medicines by your doctor.
The use of two locally active beta-blockers or second locally active carbonic anhydrase inhibitors is not recommended.
In the case of topical use of other ophthalmic preparations, a minimum of 5 minutes should be allowed between each administration of the medicines.

What side effects can occur?

Like all medicines Azarga can cause side effects, although it will not occur in all patients who use this medicine. Remember that the expected benefits of using the drug are usually greater than the damage resulting from the occurrence of side effects.
Local eye / eye reactions such as blurred vision, irritation, eye pain, feeling of a foreign body in the eye, eye dryness, eye discharge, pruritus, ocular congestion and conjunctivitis, discomfort, corneal erosions may occur. punctate keratitis, allergic conjunctivitis, corneal diseases, inflammation of the anterior chamber of the eye, abnormal sensation in the eye, allergic blepharitis, blepharitis, swelling and eyelid itching, eyelid erythema, tearing, conjunctival congestion, visual disturbances.
Systemic side effects may occur such as: headache and / or dizziness, taste disturbances (bitter or abnormal mouthfeel), insomnia, low blood pressure, sore throat and larynx, rhinorrhea, cough, chronic obstructive pulmonary disease, lichen flat.
Brynzolamide is a sulfonamide and, despite local application, it is absorbed into the systemic circulation. Therefore, adverse reactions characteristic of sulfonamides commonly used (e.g., orally), including severe hypersensitivity reactions, such as Stevens and Johnson syndrome, toxic epidermal necrolysis, or severe hematological disorders, may occur.
Timolol is a beta-blocker.Beta-blockers applied topically to the conjunctival sac can be absorbed and cause systemic side effects that are characteristic of this group of drugs.
Adverse reactions may also occur, which occurred when each of the active substances was used as monotherapy, including:
· In the case of brinzolamide, side effects related to the eye / eyes, such as blurred vision, blurred vision, eye irritation, eye pain, dry eye, discharge from the eye, pruritus and congestion of the eyeball and conjunctiva, feeling of foreign body presence in the eye, erosions cornea, keratitis, punctate keratitis, corneal injury, increased intraocular pressure, conjunctivitis, thyroiditis, photophobia, abnormal sensation in the eye, scleral and / or corneal discoloration, conjunctival bile, eyelid pruritus, eyelid inflammation, eyelid edema, tearing, loss of eyelashes; as well as systemic side effects such as: headache and dizziness, bitter or unusual taste in the mouth, memory problems, movement disorders, paresthesia, sensory disturbances, tremors, apathy, depression, nightmares, insomnia / drowsiness, nervousness, noise in ears, reduction / increase in heart rate, arrhythmias, palpitations, cardiorespiratory failure, angina pectoris, chest pain, shortness of breath, airway hyperresponsiveness, cough, asthma, pharyngitis and sinusitis, rhinitis, throat irritation, pain larynx and throat, runny nose, inflammation of the mouth, inflammation of the esophagus, diarrhea, nausea, vomiting, indigestion, abdominal pain, abnormal liver function tests, reduced number of red blood cells, increase in blood chloride, back pain, muscle cramps, muscle aches and pains joints, kidney pain, increased frequency of urination, sexual dysfunction (impot entity), malaise, weakness, fatigue, peripheral edema, hypersensitivity reactions (including urticaria, rash, pruritus, angioneurotic edema), alopecia, dermatitis, erythema;
· In the case of timolol side effects such as: irritation (burning, stinging), conjunctivitis, keratitis, dry eyes, drooping eyelids, reduced corneal sensitivity, blurred vision, double vision, retinal detachment (after filtration ); as well as systemic side effects such as: reduced heart rate (bradycardia), arrhythmias, cerebral stroke / ischemia, heart failure, cardiac arrest, decreased atrioventricular conduction velocity, hypotension, worsening of angina, worsening of disturbances peripheral circulation (severity of Raynaud's syndrome, severity of intermittent claudication, cold feet and hands), bronchospasm in patients with bronchial asthma or obstructive airways disease, shortness of breath, cough, respiratory failure, nasal congestion, weakness, fatigue, chest pain, pain in the limbs, alopecia, exacerbation of psoriasis, hypersensitivity reactions (rash, urticaria, pruritus, angioneurotic edema, anaphylactic reactions), headaches and / or dizziness, depression, sleep disorders, impaired memory, worsening of myasthenia gravis (including eyelid drooping), paresthesia , concentrate disorders nausea, vomiting, diarrhea, dry mouth, sexual dysfunction (impotence), masking of symptoms of hypoglycaemia, systemic lupus erythematosus.