Simbrinza Novartis eye drops supports internal pressure reduction (5ml)

Dosage form Box x 5ml
Specifications Brimonidin Tartrat, Brinzolamide

Ingredient

Composition information	Content
Brimonidin tartrat	10mg
Brinzolamide	50mg

Uses

Indications

Simbrinza eye -sidewalks are indicated for treatment in the following cases:

Reducing intraocular pressure (IOP) in adult patients with an open angle or glaucoma without adequate control of monomer.

Pharmacological

Pharmacological group: Eye -medication. Anti -glaucoma drugs and pupils.

ATC: S01EC54

Mechanism of action

Simbrinza contains two active ingredients: Brinzolamid and Brimonidin Tartrat. These two components lower the glaucoma (IOP) in patients with open angle and glaucoma (OHT) by inhibiting the formation of the fluid from the process of forming the epidemic in the eyelid form in the eye. Although both brinzolamid and brimonidin lower the glaucoma by inhibiting the formation of the fluid, their mechanism of action is different.

Brinzolamid inhibits the anhydrase carbonic enzyme (CA-II) in the eyelid epithelium that reduces the formation of bicarbonate ions with the reduction of sodium and shipping fluid through the eyelid epithelium, leading to a reduction in epidemic formation. Brimonidin, Alpha-2 adrenergic agent, Adenylyl Cyclase enzyme inhibitors and inhibit the formation of the Camp. Moreover, using brimonidine can lead to increased flow of flow through the meter.

Pharmacokinetics

absorption

Brinzolamid is absorbed through the cornea after eye drops. This active ingredient is also absorbed in the general circulation and then the drug is strongly linked to the carbon dioxide of red blood cells. The drug concentration in plasma is very low. Sales time in the blood (> 100 days) in humans due to drugs associated with erythrocyte carbon dioxide.

Brimonidin is quickly absorbed into the eyes after use.

On rabbits, the maximum concentration in the eye reaches less than 1 hour in most cases. Peak concentration in human plasma is

In a clinical study using eye small lines, comparing the systemic pharmacokinetics in the stable state of simbrinza used 2 or 3 times/day with Brinzolamid and Brimonidin used alone with the same dose level, the blood of the blood of Brinzolamid and N-Desethylbrinzolamid in the drug combined similar to being single. Similarly, pharmacokinetics in plasma in a stable state of brimonidin form combined similar to the results recorded when using Brimonidin alone except in the Simbrinza group twice a day, in this group AUC-12 hours is about 25% lower than when using Brimonidin 2 times/day.

Distribution

Rabbit studies show that the peak concentration of Brinzolamid in the eyes after use in the spot in the previous tissues such as cornea, conjunctiva, aquatic fluid, eyelashes - iris. The drug is kept in the eye tissue due to the binding with the carbon dioxide. Brinzolamid is moderate (about 60%) with plasma proteins.

Brimonidin shows affinity for the special eye tissue in the Mi - iris due to the known characteristic of Melanin. However, clinical and non -clinical safety data shows that the drug is well tolerated and safe for long -term use.

Biological Change

Brinzolamid is metabolized by iszyme cytochrom P450 in the liver, especially CYP3A4, CYP2A6, CYP2B6, CYP2C8 and CYP2C9. The main metabolite is N-Desethylbrinzolamid, then n-Desmethoxypropyl and O-Desmethyl metabolites as well as N-Propionic acid derivatives formed by N-Propyl branch oxidation of O-Desmethyl Brinzolamid.

Brinzolamid and N-Desethylbrinzolamid do not inhibit iszyme Cytochrome P450 at at least 100 times higher concentration during the circulation.

Brimonidine is strongly metabolized by the liver aldehyde, with the formation of 2-obobonidin, 3-oxobrimonidine and 2.3-dioxobobonidine are the main metabolites. Oxidation of imidazolin separation into 5-bromo-6-guanidinoquinoxalin has also been recorded.

Elimination

Brinzolamid is excreted mainly in urine in non -change form. On humans, Brinzolamid and N-Desethylbrinzolamid in the urine account for about 60% and 6% of the dose. Data on mice shows that the drug is partially excreted (about 30%), mainly in the form of metabolites.

Brimonidin tartrat is excreted mainly in urine in the form of metabolites. On the mouse and when, the metabolites in the urine account for about 60% to 70% of oral or intravenous doses.

Before taking Simbrinza Novartis eye drops supports internal pressure reduction (5ml)

How to use

Simbrinza is only used for eye drops.

Patients should be instructed to shake the vial before use.

press the nasal tube and close your eyes for 02 minutes to help reduce the absorption of the whole body. This movement can help reduce unwanted effects and increase the effect on the spot.

To avoid the infection into the small tip of the drug and the solution, be careful not to let the small head of the vial touch the eyelids, the surrounding area or other surfaces. Patients should be instructed to close the jar when not in use.

Can be used simultaneously simbrinza with eye drops elsewhere to reduce intraocular pressure. If using more than an eye drops, these drugs must be used at least 05 minutes apart.

If you miss a dose, continue to use the next dose as planned.

Do not put more than 1 drop into the eyes 2 times/day.

Dosage

used for adults (including the elderly): The recommended dose is a drop of Simbrinza eye drops into the eyes 2 times/day.

liver failure and/or kidney failure:

Simbrinza has not been studied in patients with hepatic impairment, thus being cautious when taking the drug for this patient.

Simbrinza has not been studied in patients with severe renal impairment (CrCl Children:

Safe safety and effectiveness of Simbrinza in children and minors from 02 to 17 years old has not been established. There are currently no data.

There is no recommendation to use simbrinza for children or adolescents.

Do not use simbrinza for babies and children under 02 years of age due to safety concern.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose?

Patient's airway should be maintained.

Due to the Brinzolamid component of simbrinza, electrolyte disorders, acidosis and the effects on the nervous system may occur. Need to monitor the concentration of electrolytes in serum
(special potassium) and pH.

Information about the event when swallowing the brimonidine ingredient in Simbrinza eye drops in
adults is very limited. The only adverse reaction that has been recorded until now is pressure hemorrhage. There has been a report after hypotension is hypertension in the opposite.

The oral overdose of Alpha-2 Translation Drugs has been reported to cause symptoms such as
Hypotension, weakness, vomiting, drowsiness, drowsiness, slow heart rate, arrhythmia, pupils, suspension
breathing, reducing tone, lower body heat, respiratory failure and convulsions.

Children

The serious adverse reactions below after the patient inadvertently swallow the brimonidine ingredient in Simbrinza has been reported. Symptoms include central neurological inhibition, temporary coma or reducing consciousness, coma, drowsiness, reducing tone, slow heart rate, lowering heat, pale, respiratory failure and apnea, needing to be hospitalized for special care and intubation if indicated. The reported patients have completely recovered, usually within 6 - 24 hours.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

In simbrinza -related clinical studies at a dose 2 times/day, the most common adverse reactions are eye congestion and eye allergic reactions occur in about 6-7% of patients, and taste disorders (bitter taste or abnormal taste in the mouth after small drugs) occurs in about 3% of patients. Data on the safety of simbrinza is similar to that of each ingredient of the drug (Brinzolamid 10 mg/mLL and Brimonidin 2 mg/ml).

The following adverse reactions are recorded from clinical trials with simbrinza at a dose of 2 times/day and in clinical studies and after -sales monitoring with Brinzolamid and Brimonidine menu. The adverse reactions are arranged in accordance with the following conventions: Popular (≥ 1/10), common (≥ 1/100 to Infections and parasites:

Uncommon: Nasomitis 2, Sore throat 2, sinusitis 2.

Unknown: Rhinitis 2.

Uncommon: reduced red blood cells 2, chlorine increased 2.

immune system disorders:

Uncommon: Hypersensitivity 3.

Mental disorders:

Less: Near 2, depression2,3 depressed mood2, insomnia 1, reduced libido 2, nightmares 2, stress 2.

Nervous system disorders:

Common: Sleep 1, Dizziness 1, Disorders 1.

Common: Eye allergies 1, Metal inflammation 1, eye pain 1, discomfort in the eye 1, blurred vision 1, abnormal vision 3, eye congestion 1, pale conjunctiva 3.

Uncommon: corneal wear, 1 corneal edema, mi1 edema, corneal sediment (cornea settling substances) 1, conjunctiva disorders (papillae) 1, fear of light 1, dizziness 1, swelling of the eye 2, eyelid edema 1, conjunctival edema 1, dry eye 1, eye rust 1, reduction of vision 1, increased eye water Double 2, dazzling 2, reducing sensation in the eye 2, pigments and Mac2, corneal cyst 2, abnormal sensation in the eye 1, eye strain 1.

Less: dizziness 1, tinnitus 2.

Heart disorders:

Uncommon: Respiratory failure2, angina 2, arrhythmia3, broken chest drum2,3, abnormal heart rate 2, slow heart rate 2, 3, tachycardia.

Uncommon: Low blood pressure 1.

Very rare: Hypertension 3.

Uncommon: shortness of breath 2, bronchial hypersensitivity 2, sore throat 2, dry throat 2, hormone, Cam 2 bleeding, obstruction of the upper respiratory tract 2, runny nose 2, throat irritation 2, dry nose 1, nose fluid after 1, sneezing 2. Management2.

Gastrointestinal disorders:

Common: dry mouth 1.

Unknown: Unusual liver function test 2.

Skin and subcutaneous tissue disorders:

Uncommon: contact dermatitis 1, urticaria 2, erythema 2, rash with small acne in DA2, body itching 2, hair loss 2, stretch DA2.

Less: back pain2, muscle spasm 2, muscle pain 2.

Less: Kidney pain 2.

Uncommon: erectile dysfunction 2.

Less: pain 2, chest abnormal 2, abnormal feeling 2, restless sensation 2, irritation 2, drug saving 1.

2: Additional adverse reactions are recorded when using Brinzolamid components.

3: Additional adverse reactions are recorded when using Brimonidine components.

Describe the selective adverse adverse reactions

The taste disorder is the most common adverse adverse reaction related to the use of simbrinza (3.4%). This reaction occurs due to the drug passing through the nose and throat line and mainly due to the Brinzolamid composition of Simbrinza.

Click on the nasal tube or close the eyes after the drug can reduce this adverse effect (see the dosage and usage).

Simbrinza contains brinzolamid is a sulphonamid conductor that inhibits the carbon dioxide anhydrase. Effects on gastrointestinal, nervous system, hematology, kidneys and metabolism are mainly related to the bodydrase inhibitors. Unwanted effects of the same type are thought to be caused by the carbon dioxide inhibitors that can appear when treated on the spot.

Common adverse reactions related to the Brimonidine component of Simbrinza include eye allergies, fatigue and/or drowsiness and dry mouth. Using brimonidine mitigates blood pressure. Some patients when using simbrinza have similar blood pressure loss when using single brimonidine.

Notify the doctor with unwanted effects when using the drug.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Simbrinza eye is contraindicated in the following cases:

Hypersensitivity to the active ingredient or any excipient ingredient in the ingredient section or with sulphonamids. severe renal failure.

Be cautious when used

This drug is not used by injection. Patients should be instructed not to swallow Simbrinza.

Effects on the eyes

Simbrinza has not been studied in patients with narrow -angle glaucoma and does not recommend the use of drugs for these patients.

The possible role of Brinzolamid on the corneal endothelium has not been studied in patients with damaged cornea (especially in patients with low number of endothelial cells). In particular, patients wearing contact lenses have not been researched, recommended carefully monitoring these patients when using brinzolamid because the Anhydrase carbon inhibitor may affect corneal hydration and contact lenses that can increase the risk of corneal disease. Carefully monitor the patient with damaged cornea such as diabetes patients or corneal dysplasia. Simbrinza can be used while wearing contact lenses with careful supervision (see below "Benzalkonium chloride").

Brimonidin tartrat can cause eye allergies. If allergic reactions appear, treatment should be stopped.

Slow hypersensitivity reaction in the eye has been recorded to Brimonidin Tartrat with a number of reports related to internal pressure increased.

Potential effects after stopping treatment with unchanged simbrinza. While the time to reduce the internal pressure of Simbrinza has not been studied, the effect of reducing the internal pressure of Brinzolamid is expected to last 5-7 days. The effect of reducing the intraocular pressure of Brimonidin may be longer.

Systemic effect

Simbrinza contains brinzolamid, a sulphonamid inhibitor of anhydrase carbon dioxide and although used on the spot, the drug is absorbed in the body. Similar adverse reactions related to sulphonamid may occur with local use.

If signs of serious or hypersensitivity reactions appear, this drug should be stopped.

Heart disorders

After using simbrinza, mild blood pressure decrease is observed in some patients. Should be cautious when using simbrinza simultaneously with other drugs such as antihypertensive drugs and/or cardiac glycosides or on patients with severe or unstable cardiovascular disorders and uncontrolled. Be cautious when using simbrinza for patients with depression, cerebral anemia or coronary artery, raynaud syndrome, hypotension or vascular inflammation.

Acid-base balance disorders

Acid-base balance disorders have been recorded with oral carbon dioxide inhibitors. Simbrinza contains brinzolamid, an Anhydrase carbonic inhibitor, although used on the spot but is absorbed the whole body. The adverse reactions of oral carbon inhibitors (such as acid-base balance disorders) may appear when used on the spot.

Use carefully for patients with the risk of renal impairment due to the risk of metabolic acidosis may occur. Contraindicated use of simbrinza for patients with severe renal impairment (see the control item).

Hepatic failure

Simbrinza has not been studied in patients with hepatic failure; Should be cautious when treating these patients.

alertness

Oral carbonic inhibitors can affect the ability to perform jobs that require alertness or the coordination between parts of the body in elderly patients. Simbrinza eye drops are absorbed throughout the body and therefore this effect can appear when used on the spot.

benzalkonium chloride

Simbrinza contains benzalkonium chloride that can cause eye irritation and have been known to change soft contact lenses. Avoid exposed to soft contact lenses. Patients should be instructed to remove contact lenses before using simbrinza and wait at least 15 minutes before wearing again.

benzalkonium chloride has been recorded to cause keratitis and/or corneal ulcer. Need to monitor tightly when using the drug regularly or prolonged.

Children

Simbriza's safety and effectiveness in children and minors from 2 to 17 years old have not been established. Brimonidine overdose symptoms (including consciousness, hypotension, reduced tone, slow heartbeat, hypothermia, cyanosis and shortness of breath) have been recorded in infants and young children using Brimonidine eye drops, partly in the treatment of congenital glaucoma. Therefore contraindicated use of simbrinza for children under 2 years old.

Treatment for children 2 years and older (especially between 2-7 years old and/or weight

The effect of drugs on driving and operating machinery

Simbrinza has a moderate influence on driving and operating machinery.

Simbrinza can cause dizziness, fatigue and/or drowsiness, so it can affect the ability to drive and operate machinery. Temporary blurred vision or other vision disorders may affect the ability to drive or operate machinery. If blurred vision appears after the drug, the patient needs to wait until it is clear before driving or operating machinery.

Oral carbon dioxide inhibitors can reduce the ability to perform jobs that require alertness or need to coordinate between parts of the body in the elderly.

Use drugs for women during pregnancy and lactation

Pregnant women:

No or very little data for using simbrinza for pregnant women. Brinzolamid causes pregnancy deformities on rats but does not cause rabbits after using systemic sugar. Animal studies with oral brimonidin does not show the harmful effects on reproductive toxicity. In animal studies, Brimonidin passes through the placenta and goes into the fetal circulation with limited level.

It is not recommended to use simbrinza during pregnancy and for women who are likely to not use contraception.

breastfeeding women:

It is unclear whether the locally used simbrinza will excrete in human milk. The pharmacological/toxic data in animal studies shows that after oral use, the minimum concentration of Brinzolamid has been found in breast milk. Brimonidin is used to be excreted in breast milk.

Do not use simbrinza for breastfeeding women.

reproductive ability:

It is not recommended to use simbrinza during pregnancy and for women who are likely to not use contraception.

Clinical non -clinical research data does not show any effect of Brinzolamid to fertility. There is no data assessment of the effect of simbrinza used on the spot to fertility in humans.

Interactive drug

There is no specific drug interaction research conducted with simbrinza.

Contraindicated to use simbrinza for patients who are taking monoamine inhibitors of oxidase and patients taking antidepressants that affect noradrenergic transmission (such as three -round antidepressants and mianserin). The three -round antidepressants can reduce the ophthalmic response of simbrinza.

Should be cautious due to the ability to combine or enhance the central neurological inhibition (such as alcohol, barbiturates, opium, sedative or anesthetic).

There is no data on the concentration of catecholamine during the circulation after using simbrinza. However, patients use drugs that affect the metabolism and absorption of amines during the circulation (such as chlorpromazin, methylphenidate, reserpine, recovery inhibitors of serotonin-noradrenalin) should be cautious.

The α-adrenergic agonist group (such as Brimonidin Tartrat) may reduce heart rate and blood pressure. A slight decreased blood pressure has been recorded in some patients after using simbrinza. Be cautious when using drugs such as drugs for hypertension or cardiac glycosides simultaneously with simbrinza.

Be cautious when starting (or changing dose) of the drug and has a systemic effect (regardless of the dosage form) that can interact with the α-adrenergic owner or affect the effects of these drugs such as copper or antagonism with adrenergic receptors (such as isoprenalin, prazosin).

Brinzolamid is an Anhydrase carbon diminal inhibitor, although used on the spot but is absorbed the whole body. Acid-base balance disorders have been recorded with oral carbon dioxide inhibitors. Need to consider the ability to interact in patients using simbrinza.

Has the potential to have a well -trunk effect on the known systemic effect of the Anhydrase carbon dioxide inhibitor in patients using an oral carbonic inhibitor or oral and Brinzolamide used on the spot. It is not recommended to simultaneously use simbrinza with oral carbon dioxide inhibitors.

Cytochrom P-450 iszymes involved in the metabolism of Brinzolamid including CYP3A4 (main enzyme), CYP2A6, CYP2B6, CYP2C8 and CYP2C9. It is expected that CYP3A4 inhibitors such as Ketoconazole, Itraconazole, Clotrimazol, Ritonavir and Troleandomycin will inhibit the metabolism of Brinzolamid through CYP3A4. Caution should be taken when used simultaneously with CYP3A4 inhibitors. However, there is no cumulative brinzolamid due to renal excretion is the main excretion path. Brinzolamid does not inhibit cytochrom P-450 iszyme.

Storage

Leave a cool place, avoid light, temperatures below 30⁰C.

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