Drugs List

Therapeutic Indications

Uses

Adjunctive therapy (to beta blockers or prostaglandin analogues), or monotherapy (if beta-blockers contraindicated or ineffective) to reduce elevated intraocular pressure in ocular hypertension or open angle glaucoma.

Administration

For ocular administration.

Contraindications

Renal impairment - creatinine clearance less than 30ml/minute

Hyperchloraemic acidosis

Precautions and Warnings

Children under 18 years (see Dosage - Children )

Hepatic impairment (see Dosage - Hepatic impairment )

Pregnancy (see Pregnancy )

Lactation (see Lactation )

Brinzolamide is absorbed systemically. Discontinue use if signs of serious reactions or hypersensitivity occur.

Use with caution in patients with significant renal tubular immaturity or abnormalities due to the risk of metabolic acidosis.

There is limited experience in patients with pseudoexfoliative glaucoma or pigmentary glaucoma.

There is no experience in patients with angle-closure glaucoma.

Use with caution in patients with compromised corneas (especially those with low endothelial cell count) e.g. diabetes mellitus or patients who wear contact lenses (due to effects on corneal hydration).

Contains benzalkonium chloride that may discolour soft contact lenses. Soft contact lenses should be removed before instillation of the eye drops and may be reinserted after 15 minutes.

Brinzolamide eye drops may impair the ability to perform tasks requiring mental alertness or physical co-ordination in elderly patients.

Application may cause transient blurring of vision, patients should avoid driving or operating machinery until vision is clear.

Pregnancy and Lactation

Pregnancy

At the time of writing there are no adequate data on the use of brinzolamide in pregnant women. Animal studies (at many times the human ophthalmic dose) have shown reproductive toxicity, but the potential risk for humans is unknown. Schaefer notes that brinzolamide and other carbonic anhydrase inhibitors have not been systematically studied, but eye drops may generally be used during pregnancy, particularly for compelling indications such as severe glaucoma, providing the dose is kept as low as therapeutically possible.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password at ( https://www.toxbase.org/ ) or if this is unavailable at the backup site ( https://www.TOXBASEbackup.org/ ).

Animal data - Reproductive toxicity in rats and rabbits.

Crosses placenta? - Unknown

Other information - Eye drops may generally be used during pregnancy for appropriate indications, but consider quantitative absorption via the conjunctiva and dosage and duration should be kept as low as possible.

Lactation

It is not known whether brinzolamide is excreted in human milk, but it is excreted in rat milk. The manufacturer strongly recommends avoiding brinzolamide when breastfeeding. Schaefer concludes that the use of carbonic anhydrase inhibitors such as brinzolamide are acceptable, but there are limited data available.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Drug excreted in breast milk? - Unknown in humans, but excreted in rat milk.

Considered suitable or recommended by manufacturer? - No.

UK Drugs in Lactation Advisory Service Classification - Not listed.

Drug substance licensed in infants? - No.

Side Effects

Dysgeusia
Blurred vision (transient)
Cardio-respiratory depression
Angina pectoris
Bradycardia
Arrhythmias
Decreased erythrocyte count
Headache
Somnolence
Motor disturbances
Amnesia
Dizziness
Paraesthesia
Ocular irritation
Ocular pain
Dry eyes
Ocular discharge
Ocular pruritus
Ocular hyperaemia
Keratopathy
Increased intra-ocular pressure
Conjunctivitis
Photophobia
Photopsia
Visual disturbances
Allergic conjunctivitis
Scleral disorders
Asthenopia
Abnormal sensation in eye
Keratoconjunctivitis
Conjunctival hyperaemia
Eyelid reaction
Increased lacrimation
Tinnitus
Dyspnoea
Cough
Epistaxis
Pharyngolaryngeal pain
Throat irritation
Upper respiratory tract congestion
Postnasal drip
Sneezing
Nasal dryness
Dry mouth
Oesophagitis
Diarrhoea
Nausea
Dyspepsia
Upper abdominal pain
Abdominal discomfort
Gastro-intestinal disturbances
Renal pain
Urticaria
Rash
Pruritus
Alopecia
Skin tightness
Back pain
Muscle spasm
Myalgia
Nasopharyngitis
Pharyngitis
Sinusitis
Chest pain
Asthenia
Fatigue
Malaise
Irritability
Erectile dysfunction
Apathy
Depression
Reduced libido
Nightmares
Insomnia
Nervousness
Hyperchloraemia
Optic nerve damage
Tachycardia
Hypertension
Tremor
Hypoaesthesia
Vomiting
Vertigo
Pollakiuria
Dermatitis
Arthralgia
Peripheral oedema
Abnormal liver function tests
Taste disturbances
Bronchitis
Subconjunctival cyst
Ageusia
Impaired memory
Sensation of foreign body in eye
Corneal disorders

Presentation

Ophthalmic suspension containing 10mg brinzolamide per ml.

Drugs List

Therapeutic Indications

Uses

Adjunctive therapy (to beta blockers or prostaglandin analogues), or monotherapy (if beta-blockers contraindicated or ineffective) to reduce elevated intraocular pressure in ocular hypertension or open angle glaucoma.

Dosage

Adults

Children

Patients with Renal Impairment

Patients with Hepatic Impairment

Administration

For ocular administration.

Contraindications

Renal impairment - creatinine clearance less than 30ml/minute

Hyperchloraemic acidosis

Precautions and Warnings

Children under 18 years (see Dosage - Children )

Hepatic impairment (see Dosage - Hepatic impairment )

Pregnancy (see Pregnancy )

Lactation (see Lactation )

Brinzolamide is absorbed systemically. Discontinue use if signs of serious reactions or hypersensitivity occur.

Use with caution in patients with significant renal tubular immaturity or abnormalities due to the risk of metabolic acidosis.

There is limited experience in patients with pseudoexfoliative glaucoma or pigmentary glaucoma.

There is no experience in patients with angle-closure glaucoma.

Use with caution in patients with compromised corneas (especially those with low endothelial cell count) e.g. diabetes mellitus or patients who wear contact lenses (due to effects on corneal hydration).

Contains benzalkonium chloride that may discolour soft contact lenses. Soft contact lenses should be removed before instillation of the eye drops and may be reinserted after 15 minutes.

Brinzolamide eye drops may impair the ability to perform tasks requiring mental alertness or physical co-ordination in elderly patients.

Application may cause transient blurring of vision, patients should avoid driving or operating machinery until vision is clear.

Pregnancy and Lactation

Pregnancy

At the time of writing there are no adequate data on the use of brinzolamide in pregnant women. Animal studies (at many times the human ophthalmic dose) have shown reproductive toxicity, but the potential risk for humans is unknown. Schaefer notes that brinzolamide and other carbonic anhydrase inhibitors have not been systematically studied, but eye drops may generally be used during pregnancy, particularly for compelling indications such as severe glaucoma, providing the dose is kept as low as therapeutically possible.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password at ( https://www.toxbase.org/ ) or if this is unavailable at the backup site ( https://www.TOXBASEbackup.org/ ).

Animal data - Reproductive toxicity in rats and rabbits.

Crosses placenta? - Unknown

Other information - Eye drops may generally be used during pregnancy for appropriate indications, but consider quantitative absorption via the conjunctiva and dosage and duration should be kept as low as possible.

Lactation

It is not known whether brinzolamide is excreted in human milk, but it is excreted in rat milk. The manufacturer strongly recommends avoiding brinzolamide when breastfeeding. Schaefer concludes that the use of carbonic anhydrase inhibitors such as brinzolamide are acceptable, but there are limited data available.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Drug excreted in breast milk? - Unknown in humans, but excreted in rat milk.

Considered suitable or recommended by manufacturer? - No.

UK Drugs in Lactation Advisory Service Classification - Not listed.

Drug substance licensed in infants? - No.

Effects on Ability to Drive and Operate Machinery

Instillation of eye drops may cause transient blurring of vision. Avoid driving or operating machinery until vision is clear.

Brinzolamide eye drops may impair the ability to perform tasks requiring mental alertness or physical co-ordination in elderly patients.

Counselling

Advise patient that the product is a suspension and that they should shake the bottle well before use.

Advise patient to wash their hands prior to use.

Advise patient to avoid contact of the dropper with the eye or other surfaces as contamination leading to ophthalmic infection may occur.

Advise patients to leave an interval of at least 5 minutes before instilling another ophthalmic medication.

Advise patient to compress the lacrimal sac during administration and for one minute afterwards, to reduce systemic absorption.

Advise patients that instillation of eye drops may cause transient blurring of vision and to avoid driving or operating machinery until vision is clear. In addition, brinzolamide eye drops may impair the ability to perform tasks requiring mental alertness or physical co-ordination in elderly patients.

Advise patient to remove soft contact lenses before instillation of the eye drops and re-insert them after 15 minutes.

Advise patient to discard eye drops 4 weeks after first opening.

Side Effects

Dysgeusia
Blurred vision (transient)
Cardio-respiratory depression
Angina pectoris
Bradycardia
Arrhythmias
Decreased erythrocyte count
Headache
Somnolence
Motor disturbances
Amnesia
Dizziness
Paraesthesia
Ocular irritation
Ocular pain
Dry eyes
Ocular discharge
Ocular pruritus
Ocular hyperaemia
Keratopathy
Increased intra-ocular pressure
Conjunctivitis
Photophobia
Photopsia
Visual disturbances
Allergic conjunctivitis
Scleral disorders
Asthenopia
Abnormal sensation in eye
Keratoconjunctivitis
Conjunctival hyperaemia
Eyelid reaction
Increased lacrimation
Tinnitus
Dyspnoea
Cough
Epistaxis
Pharyngolaryngeal pain
Throat irritation
Upper respiratory tract congestion
Postnasal drip
Sneezing
Nasal dryness
Dry mouth
Oesophagitis
Diarrhoea
Nausea
Dyspepsia
Upper abdominal pain
Abdominal discomfort
Gastro-intestinal disturbances
Renal pain
Urticaria
Rash
Pruritus
Alopecia
Skin tightness
Back pain
Muscle spasm
Myalgia
Nasopharyngitis
Pharyngitis
Sinusitis
Chest pain
Asthenia
Fatigue
Malaise
Irritability
Erectile dysfunction
Apathy
Depression
Reduced libido
Nightmares
Insomnia
Nervousness
Hyperchloraemia
Optic nerve damage
Tachycardia
Hypertension
Tremor
Hypoaesthesia
Vomiting
Vertigo
Pollakiuria
Dermatitis
Arthralgia
Peripheral oedema
Abnormal liver function tests
Taste disturbances
Bronchitis
Subconjunctival cyst
Ageusia
Impaired memory
Sensation of foreign body in eye
Corneal disorders

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( https://www.toxbase.org/ ) or if this is unavailable at the backup site ( https://www.TOXBASEbackup.org/ ).

Shelf Life and Storage

No special requirements.

Discard any unused contents 4 weeks after opening.

Further Information

Last Full Review Date: November 2011

Reference Sources

Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

Summary of Product Characteristics: Azopt eye drops, suspension. Novartis Europharm Limited. Revised May 2017.

NICE Evidence Services Available at: www.nice.org.uk Last accessed:23 August 2017