Azopt

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ANNEX I 

 

SUMMARY OF PRODUCT CHARACTERISTICS 



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1. NAME OF THE MEDICINAL PRODUCT 

 

AZOPT 10 mg/ml eye drops, suspension 

 

 

2. QUALITATIVE AND QUANTITATIVE COMPOSITION 

 

Each ml of suspension contains 10 mg brinzolamide. 

 

Excipient with known effect: 

 

Each ml of suspension contains 0.1 mg benzalkonium chloride. 

 

For a full list of excipients, see section 6.1. 

 

 

3. PHARMACEUTICAL FORM 

 

Eye drops, suspension. 

 

White to off-white suspension. 

 

 

4. CLINICAL PARTICULARS 

 

4.1 Therapeutic indications 

 

AZOPT is indicated to decrease elevated intraocular pressure in: 

• ocular hypertension 

• open-angle glaucoma 

as monotherapy in adult patients unresponsive to beta-blockers or in adult patients in whom beta-

blockers are contraindicated, or as adjunctive therapy to beta-blockers or prostaglandin analogues (see 

also section 5.1). 

 

4.2 Posology and method of administration 

 

Posology 

 

When used as monotherapy or adjunctive therapy, the dose is one drop of AZOPT in the conjunctival 

sac of the affected eye(s) twice daily. Some patients may have a better response with one drop 

three times a day. 

 

Special populations 

Elderly population 

No dose adjustment in elderly patients is necessary. 

 

Hepatic and renal impairment 

AZOPT has not been studied in patients with hepatic impairment and is therefore not recommended in 

such patients. 

 

AZOPT has not been studied in patients with severe renal impairment (creatinine clearance 

< 30 ml/min) or in patients with hyperchloraemic acidosis. Since brinzolamide and its main metabolite 

are excreted predominantly by the kidney, AZOPT is therefore contra-indicated in such patients (see 

also section 4.3). 

 



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Paediatric population 

The safety and efficacy of AZOPT in infants, children and adolescents aged 0 to 17 years have not 

been established. Currently available data are described in sections 4.8 and 5.1. AZOPT is not 

recommended for use in infants, children and adolescents. 

 

Method of administration 

 

For ocular use. 

 

Nasolacrimal occlusion or gently closing the eyelid after instillation is recommended. This may reduce 

the systemic absorption of medicinal products administered via the ocular route and result in a 

decrease in systemic side effects. 

 

Instruct the patient to shake the bottle well before use. After the cap is removed, if tamper evident snap 

collar is loose, remove before using the product. 

 

To prevent contamination of the dropper tip and suspension, care must be taken not to touch the 

eyelids, surrounding areas or other surfaces with the dropper tip of the bottle. Instruct patients to keep 

the bottle tightly closed when not in use. 

 

When substituting another ophthalmic antiglaucoma agent with AZOPT, discontinue the other agent 

and start the following day with AZOPT. 

 

If more than one topical ophthalmic medicinal product is being used, the medicines must be 

administered at least 5 minutes apart. Eye ointments should be administered last. 

 

If a dose is missed, treatment should be continued with the next dose as planned. The dose should not 

exceed one drop in the affected eye(s) three times daily. 

 

4.3 Contraindications 

 

 Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 

 Known hypersensitivity to sulphonamides (see also section 4.4). 

 Severe renal impairment. 

 Hyperchloraemic acidosis. 
 

4.4 Special warnings and precautions for use 

 

Systemic effects 

 

AZOPT is a sulphonamide inhibitor of carbonic anhydrase and, although administered topically, is 

absorbed systemically. The same types of adverse reactions that are attributable to sulphonamides may 

occur with topical administration. If signs of serious reactions or hypersensitivity occur, discontinue 

the use of this preparation. 

 

Acid-base disturbances have been reported with oral carbonic anhydrase inhibitors. Use with caution 

in patients with risk of renal impairment because the possible risk of metabolic acidosis (see 

section 4.2). 

 

Brinzolamide has not been studied in pre-term infants (less than 36 weeks gestational age) or those 

less than 1 week of age. Patients with significant renal tubular immaturity or abnormalities should only 

receive brinzolamide after careful consideration of the risk benefit balance because of the possible risk 

of metabolic acidosis. 

 

Oral carbonic anhydrase inhibitors may impair the ability to perform tasks requiring mental alertness 

and/or physical coordination. AZOPT is absorbed systemically and therefore this may occur with 

topical administration. 



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Concomitant therapy 

 

There is a potential for an additive effect on the known systemic effects of carbonic anhydrase 

inhibition in patients receiving an oral carbonic anhydrase inhibitor and AZOPT. The concomitant 

administration of AZOPT and oral carbonic anhydrase inhibitors has not been studied and is not 

recommended (see also section 4.5). 

 

AZOPT was primarily evaluated in concomitant administration with timolol during adjunctive 

glaucoma therapy. Additionally the IOP-reducing effect of AZOPT as adjunctive therapy to the 

prostaglandin analogue travoprost has been studied. No long term data are available on the use of 

AZOPT as adjunctive therapy to travoprost(see also section 5.1). 

 

There is limited experience with AZOPT in the treatment of patients with pseudoexfoliative glaucoma 

or pigmentary glaucoma. Caution should be used in treating these patients and close monitoring of 

intraocular pressure (IOP) is recommended. AZOPT has not been studied in patients with narrow-

angle glaucoma and its use is not recommended in these patients. 

 

The possible role of brinzolamide on corneal endothelial function has not been investigated in patients 

with compromised corneas (particularly in patients with low endothelial cell count). Specifically, 

patients wearing contact lenses have not been studied and careful monitoring of these patients when 

using brinzolamide is recommended, since carbonic anhydrase inhibitors may affect corneal hydration 

and wearing contact lenses might increase the risk for the cornea. Careful monitoring of patients with 

compromised corneas such as patients with diabetes mellitus or corneal dystrophies is recommended. 

 

Benzalkonium chloride, which is commonly used as a preservative in ophthalmic products, has been 

reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. Since AZOPT contains 

benzalkonium chloride, close monitoring is required with frequent or prolonged use in dry eye 

patients, or in conditions where the cornea is compromised. 

 

AZOPT has not been studied in patients wearing contact lenses. AZOPT contains benzalkonium 

chloride which may cause eye irritation and is known to discolour soft contact lenses. Contact with 

soft contact lenses is to be avoided. Patients must be instructed to remove contact lenses prior to the 

application of AZOPT and wait at least 15 minutes after instillation of the dose before reinsertion. 

 

Potential rebound effects following cessation of treatment with AZOPT have not been studied; the 

IOP-lowering effect is expected to last for 5-7 days. 

 

Paediatric population 

 

The safety and efficacy of AZOPT in infants, children and adolescents aged 0 to 17 years have not 

been established and its use is not recommended in infants, children or adolescents 

 

4.5 Interaction with other medicinal products and other forms of interaction 

 

Specific interaction studies with other medicinal products have not been performed with AZOPT. 

 

In clinical studies, AZOPT was used concomitantly with prostaglandin analogues and timolol 

ophthalmic preparations without evidence of adverse interactions. Association between AZOPT and 

miotics or adrenergic agonists has not been evaluated during adjunctive glaucoma therapy. 

 

AZOPT is a carbonic anhydrase inhibitor and, although administered topically, is absorbed 

systemically. Acid-base disturbances have been reported with oral carbonic anhydrase inhibitors. The 

potential for interactions must be considered in patients receiving AZOPT. 

 



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The cytochrome P-450 isozymes responsible for metabolism of brinzolamide include CYP3A4 (main), 

CYP2A6, CYP2C8 and CYP2C9. It is expected that inhibitors of CYP3A4 such as ketoconazole, 

itraconazole, clotrimazole, ritonavir and troleandomycin will inhibit the metabolism of brinzolamide 

by CYP3A4. Caution is advised if CYP3A4 inhibitors are given concomitantly. However, 

accumulation of brinzolamide is unlikely as renal elimination is the major route. Brinzolamide is not 

an inhibitor of cytochrome P-450 isozymes. 

 

4.6 Fertility, pregnancy and lactation 

 

Pregnancy 

 

There are no or limited amount of data from the use of ophthalmic brinzolamide in pregnant women. 

Studies in animals have shown reproductive toxicity following systemic administration (see also 

section 5.3). 

 

AZOPT is not recommended during pregnancy and in women of childbearing potential not using 

contraception. 

 

Breast-feeding 

 

It is unknown whether brinzolamide/metabolites are excreted in human milk following topical ocular 

administration. Animal studies have shown the excretion of minimal levels of brinzolamide in breast 

milk following oral administration. 

 

A risk to the newborns/infants cannot be excluded. A decision must be made whether to discontinue 

breast-feeding or to discontinue/abstain from AZOPT therapy taking in to account the benefit of 

breast-feeding for the child and the benefit of therapy for the woman. 

 

Fertility 

 

Animal studies with brinzolamide demonstrated no effect on fertility. Studies have not been performed 

to evaluate the effect of topical ocular administration of brinzolamide on human fertility. 

 

4.7 Effects on ability to drive and use machines 

 

AZOPT has a minor influence on the ability to drive and use machines. 

 

Temporary blurred vision or other visual disturbances may affect the ability to drive or use machines 

(see also section 4.8). If blurred vision occurs at instillation, the patient must wait until the vision 

clears before driving or using machines. 

 

Oral carbonic anhydrase inhibitors may impair the ability to perform tasks requiring mental alertness 

and/or physical coordination (see also section 4.4 and section 4.8). 

 

4.8 Undesirable effects 

 

Summary of the safety profile 

 

In clinical studies involving 2732 patients treated with AZOPT as monotherapy or adjunctive therapy 

to timolol maleate 5 mg/ml, the most frequently reported treatment-related adverse reactions were: 

dysgeusia (6.0%) (bitter or unusual taste, see description below) and temporary blurred vision (5.4%) 

upon instillation, lasting from a few seconds to a few minutes (see also section 4.7). 

 



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Tabulated summary of adverse reactions 

 

The following adverse reactions have been reported with brinzolamide 10mg/ml eye drops, suspension 

and are classified according to the following convention: very common (≥1/10), common (≥1/100 to 

<1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (<1/10,000), or not 

known (cannot be estimated from the available data). Within each frequency grouping, adverse 

reactions are presented in order of decreasing seriousness. The adverse reactions were obtained from 

clinical trials and post-marketing spontaneous reports. 

 

System Organ Classification MedDRA Preferred Term (v.15.1) 

Infections and infestations Uncommon: nasopharyngitis, pharyngitis, sinusitis 

Not Known: rhinitis 

Blood and lymphatic system 

disorders 

Uncommon: red blood cell count decreased, blood chloride 

increased 

Immune system disorders Not Known: hypersensitivity 

Metabolism and nutrition disorders Not known: decreased appetite 

Psychiatric disorders Uncommon: apathy, depression, depressed mood, libido 

decreased, nightmare, nervousness 

Rare: insomnia 

Nervous system disorders Uncommon: motor dysfunction, amnesia, dizziness, 

paraesthesia, headache 

Rare: memory impairment, somnolence 

Not Known: tremor, hypoaesthesia, ageusia 

Eye disorders Common: blurred vision, eye irritation, eye pain, foreign body 

sensation in eyes, ocular hyperaemia 

Uncommon: corneal erosion, keratitis, punctate keratitis, 

keratopathy, deposit eye, corneal staining, corneal epithelium 

defect, corneal epithelium disorder, blepharitis, eye pruritus, 

conjunctivitis, eye swelling, meibomianitis, glare, 

photophobiadry eye, allergic conjunctivitis, pterygium, scleral 

pigmentation, asthenopia, ocular discomfort, abnormal 

sensation in eye, keratoconjunctivitis sicca, subconjunctival 

cyst, conjunctival hyperaemia, eyelids pruritus, eye discharge, 

eyelid margin crusting, lacrimation increased 

Rare: corneal oedema, diplopia, visual acuity reduced, 

photopsia, hypoaesthesia eye, periorbital oedema, intraocular 

pressure increased, optic nerve cup/disc ratio increased 

Not Known: corneal disorder, visual disturbance, eye allergy, 

madarosis, eyelid disorder, erythema of eyelid 

Ear and labyrinth disorders Rare: tinnitus 

Not Known: vertigo 

Cardiac disorders Uncommon: cardio-respiratory distress, bradycardia, 

palpitations 

Rare: angina pectoris, heart rate irregular 

Not Known: arrhythmia, tachycardia, hypertension, blood 

pressure increased, blood pressure decreased, heart rate 

increased 

Respiratory, thoracic and mediastinal 

disorders 

Uncommon: dyspnoea, epistaxis, oropharyngeal pain, 

pharyngolaryngeal pain, throat irritation, upper airway cough 

syndrome, rhinorrhoea, sneezing 

Rare: bronchial hyperreactivity, upper respiratory tract 

congestion, sinus congestion, nasal congestion, cough, nasal 

dryness 

Not Known: asthma 



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Gastrointestinal disorders Common: dysgeusia 

Uncommon: oesophagitis, diarrhoea, nausea, vomiting, 

dyspepsia, upper abdominal pain, abdominal discomfort, 

stomach discomfort, flatulence, frequent bowel movements, 

gastrointestinal disorder, hypoaesthesia oral, paraesthesia oral, 

dry mouth 

Hepato-biliary disorders Not Known: liver function test abnormal 

Skin and subcutaneous tissue 

disorders 

Uncommon: rash, rash maculo-papular, skin tightness 

Rare: urticaria, alopecia, pruritus generalised 

Not Known: dermatitis, erythema 

Musculoskeletal and connective 

tissue disorders 

Uncommon: back pain, muscle spasms, myalgia 

Not Known: arthralgia, pain in extremity 

Renal and urinary disorders Uncommon: renal pain 

Not Known: pollakiuria 

Reproductive system and breast 

disorders 

Uncommon: erectile dysfunction 

General disorders and administration 

site conditions 

Uncommon: pain, chest discomfort, fatigue, feeling abnormal 

Rare: chest pain, feeling jittery, asthenia, irritability 

Not Known: peripheral oedema, malaise 

Injury, poisoning and procedural 

complications 

Uncommon: foreign body in eye 

 

Description of selected adverse events 

 

Dysgeusia (bitter or unusual taste in the mouth following instillation) was the most frequently reported 

systemic adverse reaction associated with the use of AZOPT during clinical studies. It is likely caused 

by passage of the eye drops in the nasopharynx via the nasolacrimal canal. Nasolacrimal occlusion or 

gently closing the eyelid after instillation may help reduce the incidence of this effect (see also 

section 4.2). 

 

AZOPT is a sulphonamide inhibitor of carbonic anhydrase with systemic absorption. Gastrointestinal, 

nervous system, haematological, renal and metabolic effects are generally associated with systemic 

carbonic anhydrase inhibitors. The same type of adverse reactions that are attributable to oral carbonic 

anhydrase inhibitors may occur with topical administration. 

 

No unexpected adverse reactions have been observed with AZOPT when used as adjunctive therapy to 

travoprost. The adverse reactions seen with the adjunctive therapy have been observed with each 

active substance alone. 

 

Paediatric population 

 

In small short-term clinical trials, approximately 12.5% of paediatric patients were observed to 

experience adverse reactions, the majority of which were local, non-serious ocular reactions such as 

conjunctival hyperaemia, eye irritation, eye discharge, and lacrimation increased (see also section 5.1). 

 

Reporting of suspected adverse reactions 

 

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It 

allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare 

professionals are asked to report any suspected adverse reactions via the national reporting system 

listed in Appendix V. 

 

http://www.ema.europa.eu/docs/en_GB/document_library/Template_or_form/2013/03/WC500139752.doc


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4.9 Overdose 

 

No case of overdose has been reported. 

 

Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic 

state, and possible nervous system effects may occur. Serum electrolyte levels (particularly potassium) 

and blood pH levels must be monitored. 

 

 

5. PHARMACOLOGICAL PROPERTIES 

 

5.1 Pharmacodynamic properties 

 

Pharmacotherapeutic group: Antiglaucoma preparations and miotics, carbonic anhydrase inhibitors, 

ATC code: S01EC04 

 

Mechanism of action 

 

Carbonic anhydrase (CA) is an enzyme found in many tissues of the body, including the eye. Carbonic 

anhydrase catalyses the reversible reaction involving the hydration of carbon dioxide and the 

dehydration of carbonic acid. 

 

Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humour 

secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in 

sodium and fluid transport. The result is a reduction in intraocular pressure (IOP) which is a major risk 

factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide, an 

inhibitor of carbonic anhydrase II (CA-II), the predominant iso-enzyme in the eye, with an in vitro 

IC50 of 3.2 nM and a Ki of 0.13 nM against CA-II. 

 

Clinical efficacy and safety 

 

The IOP-reducing effect of AZOPT as adjunctive therapy to the prostaglandin analogue travoprost 

was studied. Following a 4 week run-in with travoprost, patients with an IOP ≥19 mmHg were 

randomized to receive added treatment with brinzolamide or timolol. An additional decrease in mean 

diurnal IOP of 3.2 to 3.4 mmHg for the brinzolamide group and 3.2 to 4.2 mmHg for the timolol group 

were observed. There was an overall higher incidence of non-serious ocular adverse reactions, mainly 

related to signs of local irritation, in the brinzolamide/travoprost groups. The events were mild and did 

not affect the overall discontinuation rates in the studies (see also section 4.8). 

 

A clinical trial was conducted with AZOPT in 32 paediatric patients less than 6 years of age, 

diagnosed with glaucoma or ocular hypertension. Some patients were naive to IOP therapy whilst 

others were on other IOP-lowering medicinal product(s). Those who had been on previous IOP 

medicinal product(s) were not required to discontinue their IOP medicinal product(s) until initiation of 

monotherapy with AZOPT. 

 

Among patients who were naive to IOP therapy (10 patients), the efficacy of AZOPT was similar to 

that seen previously in adults, with mean IOP reductions from baseline ranging up to 5 mmHg. Among 

patients who were on topical IOP-lowering medicinal product(s) (22 patients), mean IOP increased 

slightly from baseline in the AZOPT group. 

 



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5.2 Pharmacokinetic properties 

 

Following topical ocular administration, brinzolamide is absorbed into the systemic circulation. Due to 

its high affinity for CA-II, brinzolamide distributes extensively into the red blood cells (RBCs) and 

exhibits a long half-life in whole blood (mean of approximately 24 weeks). In humans, the metabolite 

N-desethylbrinzolamide is formed, which also binds to CA and accumulates in RBCs. This metabolite 

binds mainly to CA-I in the presence of brinzolamide. In plasma, both brinzolamide and N-

desethylbrinzolamide concentrations are low and generally below assay quantitation limits 

(<7.5 ng/ml). 

 

Binding to plasma proteins is not extensive (about 60%). Brinzolamide is eliminated primarily by 

renal excretion (approximately 60%). About 20% of the dose has been accounted for in urine as 

metabolite. Brinzolamide and N-desethylbrinzolamide are the predominant components in the urine 

along with trace levels (<1%) of the N-desmethoxypropyl and O-desmethyl metabolites. 

 

In an oral pharmacokinetic study, healthy volunteers received 1 mg capsules of brinzolamide twice 

daily for up to 32 weeks and RBC CA activity was measured to assess the degree of systemic CA 

inhibition. 

 

Brinzolamide saturation of RBC CA-II was achieved within 4 weeks (RBC concentrations of 

approximately 20 µM). N-Desethylbrinzolamide accumulated in RBCs to steady state within 20-

28 weeks reaching concentrations ranging from 6-30 µM. The inhibition of total RBC CA activity at 

steady state was approximately 70-75%. 

 

Subjects with moderate renal impairment (creatinine clearance of 30-60 ml/minute) were administered 

1 mg of brinzolamide twice daily orally for up to 54 weeks. Brinzolamide RBC concentration ranged 

from about 20 to 40 µM by week 4 of treatment. At steady-state, brinzolamide and its metabolite RBC 

concentrations ranged from 22.0 to 46.1 and 17.1 to 88.6 µM, respectively. 

 

N-desethylbrinzolamide RBC concentrations increased and total RBC CA activity decreased with 

decreasing creatinine clearance but brinzolamide RBC concentrations and CA-II activity remained 

unchanged. In subjects with the highest degree of renal impairment inhibition of total CA activity was 

greater although it was inferior to 90% at steady-state. 

 

In a topical ocular study, at steady-state, brinzolamide RBC concentrations were similar to those found 

in the oral study, but levels of N-desethylbrinzolamide were lower. Carbonic anhydrase activity was 

approximately 40-70% of predose levels. 

 

5.3 Preclinical safety data 

 

Non-clinical data reveal no special hazard for humans based on conventional studies of safety 

pharmacology, repeated dose toxicity, genotoxicity, and carcinogenic potential. 

 

Developmental toxicity studies in rabbits with oral doses of brinzolamide of up to 6 mg/kg/day 

(125 times the recommended human ophthalmic dose) revealed no effect on foetal development 

despite significant maternal toxicity. Similar studies in rats resulted in slightly reduced ossification of 

skull and sternebrae of foetuses of dams receiving brinzolamide at doses of 18 mg/kg/day (375 times 

the recommended human ophthalmic dose), but not 6 mg/kg/day. These findings occurred at doses that 

caused metabolic acidosis with decreased body weight gain in dams and decreased foetal weights. 

Dose-related decreases in foetal weights were observed in pups of dams receiving brinzolamide orally 

ranging from a slight decrease (about 5-6%) at 2 mg/kg/day to nearly 14% at 18 mg/kg/day. During 

lactation, the no adverse effect level in the offspring was 5 mg/kg/day. 

 

 



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6. PHARMACEUTICAL PARTICULARS 

 

6.1 List of excipients 

 

Benzalkonium chloride 

Mannitol (E421) 

Carbomer 974P 

Tyloxapol 

Edetate disodium 

Sodium chloride 

Hydrochloric acid/sodium hydroxide (to adjust pH) 

Purified water 

 

6.2 Incompatibilities 

 

Not applicable. 

 

6.3 Shelf-life 

 

2 years. 

 

4 weeks after first opening. 

 

6.4 Special precautions for storage 

 

This medicinal product does not require any special storage conditions. 

 

6.5 Nature and contents of container 

 

5 and 10 ml opaque low density polyethylene bottles with polypropylene screw caps (droptainer). 

 

The following pack sizes are available: outer cartons containing 1 x 5 ml, 3 x 5 ml and 1 x 10 ml 

bottles. Not all pack sizes may be marketed. 

 

6.6 Special precautions for disposal 

 

No special requirements. 

 

 

7. MARKETING AUTHORISATION HOLDER 

 

Novartis Europharm Limited 

Vista Building 

Elm Park, Merrion Road 

Dublin 4 

Ireland 

 

 

8. MARKETING AUTHORISATION NUMBERS 

 

EU/1/00/129/001-3 

 

 

9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 

 

Date of first authorisation: 9 March 2000 

Date of latest renewal: 29 January 2010 



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10. DATE OF REVISION OF THE TEXT 
 

 

Detailed information on this medicinal product is available on the website of the European Medicines 

Agency http://www.ema.europa.eu 

http://www.ema.europa.eu/


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ANNEX II 

 

A MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE 
 

B CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND 

USE 

 

C OTHER CONDITIONS AND REQUIREMENTS OF THE 

MARKETING AUTHORISATION 

 

D CONDITIONS OR RESTRICTIONS WITH REGARD TO THE 

SAFE AND EFFECTIVE USE OF THE MEDICINAL PRODUCT 



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A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE 

 

Name and address of the manufacturer responsible for batch release 

 

S.A. Alcon-Couvreur N.V., 

Rijksweg 14, 

B-2870 Puurs, 

Belgium. 

 

or 

 

Alcon Cusí, S.A., 

Camil Fabra 58, 

08320 El Masnou, 

Barcelona, 

Spain. 

 

The printed package leaflet of the medicinal product must state the name and address of the 

manufacturer responsible for the release of the concerned batch. 

 

 

B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE 

 

Medicinal product subject to medical prescription 

 

 

C. OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING 

AUTHORISATION 

 

 Periodic Safety Update Reports 
 

The requirements for submission of periodic safety update reports for this medicinal product are set 

out in the list of Union reference dates (EURD list) provided for under Article 107c(7) of Directive 

2001/83/EC and any subsequent updates published on the European medicines web-portal. 

 

 

D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND 

EFFECTIVE USE OF THE MEDICINAL PRODUCT 

 

 Risk Management Plan (RMP) 
 

The MAH shall perform the required pharmacovigilance activities and interventions detailed in the 

agreed RMP presented in Module 1.8.2 of the Marketing Authorisation and any agreed subsequent 

updates of the RMP. 

 

An updated RMP should be submitted: 

 At the request of the European Medicines Agency; 

 Whenever the risk management system is modified, especially as the result of new information 
being received that may lead to a significant change to the benefit/risk profile or as the result of 

an important (pharmacovigilance or risk minimisation) milestone being reached. 



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ANNEX III 

 

LABELLING AND PACKAGE LEAFLET 



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A. LABELLING 



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PARTICULARS TO APPEAR ON THE OUTER PACKAGING 

 

CARTON FOR SINGLE BOTTLE, 5 ml, 10 ml + CARTON FOR 3 x 5 ml BOTTLES 

 

 

1. NAME OF THE MEDICINAL PRODUCT 

 

AZOPT 10 mg/ml eye drops, suspension 

brinzolamide 

 

 

2. STATEMENT OF ACTIVE SUBSTANCE 

 

Each ml of suspension contains 10 mg of brinzolamide. 

 

 

3. LIST OF EXCIPIENTS 

 

Contains benzalkonium chloride, mannitol (E421), carbomer 974P, tyloxapol, edetate disodium, 

sodium chloride, hydrochloric acid/sodium hydroxide (to adjust pH) and purified water. See the 

package leaflet for further information. 

 

 

4. PHARMACEUTICAL FORM AND CONTENTS 

 

Eye drops, suspension 

 

5 ml 

10 ml 

3 x 5ml 

 

 

5. METHOD AND ROUTE OF ADMINISTRATION 

 

Read the package leaflet before use. 

Shake well before use. 

Ocular use 

 

 

6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 

OF THE SIGHT AND REACH OF CHILDREN 

 

Keep out of the sight and reach of children. 

 

 

7. OTHER SPECIAL WARNING(S), IF NECESSARY 

 

 



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8. EXPIRY DATE 

 

EXP 

Discard four weeks after first opening. 

Opened: 

Opened (1): 

Opened (2): 

Opened (3): 

 

 

9. SPECIAL STORAGE CONDITIONS 

 

 

10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 

OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 

APPROPRIATE 

 

 

11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 

 

Novartis Europharm Limited 

Vista Building 

Elm Park, Merrion Road 

Dublin 4 

Ireland 

 

 

12. MARKETING AUTHORISATION NUMBERS 

 

EU/1/00/129/001 1 x 5 ml 

EU/1/00/129/002 1 x 10 ml 

EU/1/00/129/003 3 x 5 ml 

 

 

13. BATCH NUMBER 

 

Lot 

 

 

14. GENERAL CLASSIFICATION FOR SUPPLY 

 

Medicinal product subject to medical prescription. 

 

 

15. INSTRUCTIONS ON USE 

 

 

16 INFORMATION IN BRAILLE 

 

azopt 

 

 



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17. UNIQUE IDENTIFIER – 2D BARCODE 

 

2D barcode carrying the unique identifier included. 

 

 

18. UNIQUE IDENTIFIER - HUMAN READABLE DATA 

 

PC: 

SN: 

NN: 



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MINIMUM PARTICULARS TO APPEAR ON SMALL IMMEDIATE PACKAGING UNITS 

 

BOTTLE LABEL, 5 ml & 10 ml 

 

 

1. NAME OF THE MEDICINAL PRODUCT AND ROUTE OF ADMINISTRATION 

 

AZOPT 10 mg/ml eye drops, suspension 

brinzolamide 

Ocular use 

 

 

2. METHOD OF ADMINISTRATION 

 

Read the package leaflet before use. 

Discard 4 weeks after first opening. 

Opened: 

 

 

3. EXPIRY DATE 

 

EXP 

 

 

4. BATCH NUMBER 

 

Lot 

 

 

5. CONTENTS BY WEIGHT, BY VOLUME OR BY UNIT 

 

5 ml 

10 ml 

 

 

6 OTHER 



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B. PACKAGE LEAFLET 



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Package leaflet: Information for the user 
 

AZOPT 10 mg/ml eye drops, suspension 

brinzolamide 

 

Read all of this leaflet carefully before you start using this medicine because it contains 

important information for you. 

- Keep this leaflet. You may need to read it again. 
- If you have any further questions, ask your doctor or your pharmacist. 
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, 

even if their signs of illness are the same as yours. 

- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side 
effects not listed in this leaflet. See section 4. 

 

What is in this leaflet 

 

1. What AZOPT is and what it is used for 

2. What you need to know before you use AZOPT 

3. How to use AZOPT 

4. Possible side effects 

5. How to store AZOPT 

6. Contents of the pack and other information 

 

 

1. What AZOPT is and what it is used for 

 

AZOPT contains brinzolamide which belongs to a group of medicines called carbonic anhydrase 

inhibitors. It reduces pressure within the eye. 

 

AZOPT eye drops are used to treat high pressure in the eye. This pressure can lead to an illness called 

glaucoma. 

 

If the pressure in the eye is too high, it can damage your sight. 

 

 

2. What you need to know before you use AZOPT 

 

Do not use AZOPT 

- if you have severe kidney problems. 

- if you are allergic to brinzolamide or any of the other ingredients of this medicine (listed in 

section 6). 

- if you are allergic to medicines called sulphonamides. Examples include medicines used to treat 

diabetes and infections and also diuretics (water tablets). AZOPT may cause the same allergy. 

- if you have too much acidity in your blood (a condition called hyperchloraemic acidosis). 

 

If you have further questions, ask your doctor for advice. 

 

Warnings and precautions 

Talk to your doctor or pharmacist before using AZOPT: 

- if you have kidney or liver problems. 

- if you have dry eyes or cornea problems. 

- if you are taking other sulphonamide medicines 

- if you have a specific form of glaucoma in which the pressure inside the eye rises due to 

deposits that block fluid draining out (pseudoexfoliative glaucoma or pigmentary glaucoma) or 

a specific form of glaucoma in which the pressure inside the eye (sometimes rapidly) rises 

because the eye bulges forward and blocks fluid draining out (narrow-angle glaucoma) 

 



22 

Children and adolescents 

AZOPT is not to be used by infants, children or adolescents under 18 years of age unless advised by 

your doctor. 

 

Other medicines and AZOPT 

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other 

medicines, including medicines obtained without a prescription. 

 

If you are taking another carbonic anhydrase inhibitor (acetazolamide or dorzolamide, see 

section 1 What AZOPT is and what it is used for), talk to your doctor. 

 

Pregnancy and breast-feeding 

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask 

your doctor or pharmacist for advice before using this medicine. 

 

Women who may become pregnant are advised to use effective contraception during AZOPT 

treatment. The use of AZOPT is not recommended during pregnancy or breast-feeding. Do not use 

AZOPT unless clearly indicated by your doctor. 

 

Ask your doctor or pharmacist for advice before taking any medicine. 

 

Driving and using machines 

Do not drive or use machines until your vision is clear. You may find that your vision is blurred for a 

time just after using AZOPT. 

 

AZOPT may impair the ability to perform tasks requiring mental alertness and/or physical 

coordination. If affected, take care when driving or using machines. 

 

AZOPT contains benzalkonium chloride 

 

This medicine contains 3.35 µg benzalkonium chloride per drop (= 1 dose) which is equivalent to 

0.01% or 0.1 mg/ml. 

 

AZOPT contains a preservative (benzalkonium chloride) which may be absorbed by soft contact 

lenses and may change the colour of the contact lenses. You should remove contact lenses before 

using this medicine and put them back 15 minutes afterwards. Benzalkonium chloride may also cause 

eye irritation, especially if you have dry eyes or disorders of the cornea (the clear layer at the front of 

the eye). If you feel abnormal eye sensation, stinging or pain in the eye after using this medicine, talk 

to your doctor. 

 

 

3. How to use AZOPT 
 

Always use this medicine exactly as your doctor or pharmacist has told you. Check with your doctor 

or pharmacist if you are not sure. 

 

Only use AZOPT for your eyes. Do not swallow or inject. 

 

The recommended dose is 

1 drop in the affected eye or eyes twice a day - morning and night. 

Use this much unless your doctor told you to do something different. Only use AZOPT in both eyes if 

your doctor told you to. Take it for as long as your doctor told you to. 

 



23 

How to use 

   
 1 2 3 

 

 Get the AZOPT bottle and a mirror 

 Wash your hands 

 Shake the bottle and twist off the cap. After the cap is removed, if the tamper evident snap collar 
is loose, remove before using product. 

 Hold the bottle, pointing down, between your thumb and middle finger 

 Tilt your head back. Pull down your eyelid with a clean finger, until there is a ‘pocket’ between 
the eyelid and your eye. The drop will go in here (picture 1) 

 Bring the bottle tip close to the eye. Use the mirror if it helps 

 Do not touch your eye or eyelid, surrounding areas or other surfaces with the dropper. It could 
infect the drops 

 Gently press on the base of the bottle to release one drop of AZOPT at a time. 

 Do not squeeze the bottle: it is designed so that a gentle press on the bottom is all that it needs 
(picture 2) 

 After using AZOPT, press a finger to the corner of your eye, by the nose (picture 3) for at least 
1 minute. This helps to stop AZOPT getting into the rest of the body. 

 If you take drops in both eyes, repeat the steps for your other eye. 

 Put the bottle cap back on firmly immediately after use 

 Use up one bottle before opening the next bottle. 
 

If a drop misses your eye, try again. 

 

If you are using other eye drops, leave at least 5 minutes between putting in AZOPT and the other 

drops. Eye ointments should be administered last. 

 

If you use more AZOPT than you should 

If you get too much in your eyes, rinse it all out with warm water. Do not put in any more drops until 

it’s time for your next regular dose. 

 

If you forget to use AZOPT 
Use a single drop as soon as you remember, and then go back to your regular routine. Do not use a 

double dose to make up for a forgotten dose. 

 

If you stop using AZOPT 

If you stop using AZOPT without speaking to your doctor, the pressure in your eye will not be 

controlled which could lead to loss of sight. 

 

 

4. Possible side effects 

 

Like all medicines, this medicine can cause side effects, although not everyone gets them. 

 

The following side effects have been seen with AZOPT. 

 



24 

Common side effects 

(may affect up to 1 in 10 people) 

 

- Effects in the eye: blurred vision, eye irritation, eye pain, eye discharge, itchy eye, dry eye, 
abnormal eye sensation, redness of the eye. 

 

- General side effects: bad taste. 
 

Uncommon side effects 

(may affect up to 1 in 100 people) 

 

- Effects in the eye: sensitivity to light, inflammation or infection of the conjunctiva, eye 
swelling, eyelid itching, redness or swelling, deposits in eye, glare, burning sensation, growth 

on surface of eye, increased pigmentation of the eye, tired eyes, eyelid crusting, or increased 

tear production. 

 

- General side effects: decreased or reduced heart function, a forceful heartbeat that may be rapid 
or irregular, decreased heart rate, difficulty breathing, shortness of breath, cough, decreased red 

blood cell count in blood, increased chlorine level in blood, dizziness, difficulty with memory, 

depression, nervousness, decreased emotional interest, nightmare, generalized weakness, 

fatigue, feeling abnormal, pain, movement problems, decreased sex drive, male sexual 

difficulty, cold symptoms, chest congestion, sinus infection, throat irritation, throat pain, 

abnormal or decreased sensation in mouth, inflammation of the lining of the oesophagus, 

abdominal pain, nausea, vomiting, upset stomach, frequent bowel movements, diarrhoea, 

intestinal gas, digestive disorder, kidney pain, muscle pain, muscle spasms, back pain, nose 

bleeds, runny nose, stuffy nose, sneezing, rash, abnormal skin sensation, itching, smooth skin 

rash or redness covered by elevated bumps, skin tightness, headache, dry mouth, debris in eye. 

 

Rare side effects 
(may affect up to 1 in 1,000 people) 

 

- Effects in the eye: corneal swelling, double or reduced vision, abnormal vision, flashes of light 
in the field of vision, decreased eye sensation, swelling around the eye, increased pressure in 

eye, damage to the optic nerve. 

 

- General side effects: memory impairment, drowsiness, chest pain, upper respiratory tract 
congestion, sinus congestion, nasal congestion, dry nose, ringing in ears, hair loss, generalized 

itching, feeling jittery, irritability, irregular heart rate, body weakness, difficulty sleeping, 

wheezing, itchy skin rash. 

 

Not known (frequency cannot be estimated from the available data): 

 

- Effects in the eye: eyelid abnormality, visual disturbance, corneal disorder, eye allergy, 
decreased growth or number of eyelashes, eyelid redness. 

 

- General side effects: increased allergic symptoms, decreased sensation, tremor, loss or decrease 
in taste, decreased blood pressure, increased blood pressure, increased heart rate, joint pain, 

asthma, pain in extremity, skin redness, inflammation, or itching, abnormal liver blood tests, 

swelling of the extremities, frequent urination, decreased appetite, feeling unwell. 

 

Reporting of side effects 
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects 

not listed in this leaflet. You can also report side effects directly via the national reporting system 

listed in Appendix V. By reporting side effects you can help provide more information on the safety of 

this medicine. 

 

 

http://www.ema.europa.eu/docs/en_GB/document_library/Template_or_form/2013/03/WC500139752.doc


25 

5. How to store AZOPT 
 

Keep this medicine out of the sight and reach of children. 

 

Do not use this medicine after the expiry date which is stated on the bottle and box after “EXP”. The 

expiry date refers to the last day of the month. 

 

This medicine does not require any special storage conditions. 

 

You must throw away a bottle four weeks after you first opened it, to prevent infections. Write 

down the date you opened each bottle in the space below and in the space on the bottle label and box. 

For a pack containing a single bottle, write only one date. 

 

Opened (1): 

Opened (2): 

Opened (3): 

 

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to 

throw away medicines you no longer use. These measures will help protect the environment. 

 

 

6 Contents of the pack and other information 

 

What AZOPT contains 

 

- The active substance is brinzolamide. Each millilitre contains 10 mg of brinzolamide. 
- The other ingredients are benzalkonium chloride, carbomer 974P, edetate disodium, mannitol 

(E421), purified water, sodium chloride, tyloxapol. Tiny amounts of hydrochloric acid or 

sodium hydroxide are added to keep acidity levels (pH levels) normal. 

 

What AZOPT looks like and contents of the pack 

AZOPT is a milky liquid (a suspension) supplied in a pack containing a 5 ml or a 10 ml plastic 

(droptainer) bottle with a screw cap, or in a pack containing three 5 ml plastic (droptainer) bottles with 

screw caps. Not all pack sizes may be marketed. 

 

Marketing Authorisation Holder 
 

Novartis Europharm Limited 

Vista Building 

Elm Park, Merrion Road 

Dublin 4 

Ireland 

 

Manufacturer 
S.A. Alcon - Couvreur N.V. 

Rijksweg 14 

B-2870 Puurs 

Belgium 

 

Alcon Cusí, S.A. 

Camil Fabra 58 

08320 El Masnou 

Spain 

 

For any information about this medicine, please contact the local representative of the Marketing 

Authorisation Holder: 

 



26 

België/Belgique/Belgien 

Novartis Pharma N.V. 

Tél/Tel: +32 2 246 16 11 

 

Lietuva 
SIA „Novartis Baltics“ Lietuvos filialas 

Tel: +370 5 269 16 50 

България 

Novartis Bulgaria EOOD 

Тел.: +359 2 489 98 28 

 

Luxembourg/Luxemburg 
Novartis Pharma N.V. 

Tél/Tel: +32 2 246 16 11 

 

Česká republika 
Novartis s.r.o. 

Tel: +420 225 775 111 

Magyarország 

Novartis Hungária Kft. 

Tel.: +36 1 457 65 00 

Danmark 

Novartis Healthcare A/S 

Tlf: +45 39 16 84 00 

 

Malta 

Novartis Pharma Services Inc. 

Tel: +356 2122 2872 

Deutschland 
Novartis Pharma GmbH 

Tel: +49 911 273 0 

Nederland 
Novartis Pharma B.V. 

Tel: +31 26 37 82 111 

 

Eesti 

SIA Novartis Baltics Eesti filiaal 

Tel: +372 66 30 810 

 

Norge 

Novartis Norge AS 

Tlf: +47 23 05 20 00 

Ελλάδα 
Novartis (Hellas) A.E.B.E. 

Τηλ: +30 210 281 17 12 

 

Österreich 
Novartis Pharma GmbH 

Tel: +43 1 86 6570 

España 

Novartis Farmacéutica, S.A. 

Tel: +34 93 306 42 00 

Polska 

Novartis Poland Sp. z o.o. 

Tel.: +48 22 375 4888 

 

France 

Novartis Pharma S.A.S. 

Tél: +33 1 55 47 66 00 

Portugal 
Novartis Farma - Produtos Farmacêuticos, S.A. 

Tel: +351 21 000 8600 

 

Hrvatska 
Novartis Hrvatska d.o.o. 

Tel. +385 1 6274 220 

România 

Novartis Pharma Services Romania SRL 

Tel: +40 21 31299 01 

 

Ireland 

Novartis Ireland Limited 

Tel: +353 1 260 12 55 

Slovenija 
Novartis Pharma Services Inc. 

Tel: +386 1 300 75 50 

 

Ísland 

Vistor hf. 

Sími: +354 535 7000 

Slovenská republika 

Novartis Slovakia s.r.o. 

Tel: + 421 2 5542 5439 

 

Italia 
Novartis Farma S.p.A. 

Tel: +39 02 96 54 1 

 

Suomi/Finland 

Novartis Finland Oy 

Puh/Tel: +358 (0)10 6133 200 

Κύπρος 
Novartis Pharma Services Inc. 

Τηλ: +357 22 690 690 

 

Sverige 
Novartis Sverige AB 

Tel: +46 8 732 32 00 



27 

Latvija 

SIA “Novartis Baltics” 

Tel: +371 67 887 070 

 

United Kingdom 
Novartis Pharmaceuticals UK Ltd. 

Tel: +44 1276 698370 

 

This leaflet was last revised in 

 

Other sources of information 

Detailed information on this medicine is available on the European Medicines Agency website 

http://www.ema.europa.eu 

http://www.ema.europa.eu/

	SUMMARY OF PRODUCT CHARACTERISTICS
	A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE
	B CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE
	C. OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING AUTHORISATION
	D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND EFFECTIVE USE OF THE MEDICINAL PRODUCT
	A. LABELLING
	B. PACKAGE LEAFLET