Brinzolamide/brimonidine

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Brinzolamide/brimonidine
Combination of
Brinzolamide Carbonic anhydrase inhibitor
Brimonidine Alpha-adrenergic agonist
Clinical data
Trade names Simbrinza
AHFS/Drugs.com Professional Drug Facts
License data
Pregnancy
category
Routes of
administration
Eye drop
ATC code
Legal status
Legal status
  • UK: POM (Prescription only) [2]
  • US: ℞-only [3]
  • EU:Rx-only [4]
  • In general: ℞ (Prescription only)
Identifiers
PubChem CID
KEGG
Chemical and physical data
Formula C23H31BrN8O5S3
Molar mass 675.64 g·mol−1
3D model (JSmol)
  • CCNC1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC.C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br
  • InChI=1S/C12H21N3O5S3.C11H10BrN5/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17;12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17);1-4H,5-6H2,(H2,15,16,17)/t10-;/m0./s1
  • Key:KAKYNGJFPXFCDD-PPHPATTJSA-N

Brinzolamide/brimonidine, sold under the brand name Simbrinza, is a fixed-dose combination medication used to reduce intra-ocular pressure (pressure inside the eye) in adults with ocular hypertension (high intra-ocular pressure) or in those with an eye condition known as open-angle glaucoma. [4] [3] It contains brinzolamide and brimonidine tartrate. [4] [3] It is used as an eye drop. [4] [3]

Contents

The most common side effects include ocular hyperaemia (red eye), allergic reactions in the eye, and dysgeusia (taste disturbances). [4] [3]

Open-angle glaucoma (a condition where the aqueous humour, the watery fluid inside the eyeball, cannot drain away properly) and other causes of high pressure in the eye increase the risk of damage to the retina and the optic nerve (the nerve that sends signals from the eye to the brain). [4] This can result in serious vision loss and even blindness. [4]

The active substances, brinzolamide and brimonidine tartrate, help to reduce intra-ocular pressure by reducing the production of aqueous humour. [4] Brinzolamide works by blocking an enzyme called carbonic anhydrase, which produces bicarbonate needed for the production of the aqueous humour, while brimonidine tartrate blocks another enzyme known as adenylate cyclase, which is also involved in the production of the aqueous humour. [4] Brimonidine also increases the drainage of aqueous humour from the front of the eye. [4]

Brinzolamide/brimonidine was approved for medical use in the United States in April 2013, and in the European Union in July 2014. [5] [4]

Medical uses

Brinzolamide/brimonidine is indicated to decrease of elevated intraocular pressure (IOP) in adults with open-angle glaucoma or ocular hypertension for whom monotherapy provides insufficient IOP reduction. [4] [3]

History

Brinzolamide/brimonidine was approved for medical use in the United States in April 2013, and in the European Union in July 2014. [5] [4]

Related Research Articles

<span class="mw-page-title-main">Glaucoma</span> Group of eye diseases

Glaucoma is a group of eye diseases that lead to damage of the optic nerve, which transmits visual information from the eye to the brain. Glaucoma may cause vision loss if left untreated. It has been called the "silent thief of sight" because the loss of vision usually occurs slowly over a long period of time. A major risk factor for glaucoma is increased pressure within the eye, known as intraocular pressure (IOP). It is associated with old age, a family history of glaucoma, and certain medical conditions or medications. The word glaucoma comes from the Ancient Greek word γλαυκóς, meaning 'gleaming, blue-green, gray'.

<span class="mw-page-title-main">Pilocarpine</span> Medication used to treat glaucoma and dry mouth

Pilocarpine is a medication used to reduce pressure inside the eye and treat dry mouth. As an eye drop it is used to manage angle closure glaucoma until surgery can be performed, ocular hypertension, primary open angle glaucoma, and to constrict the pupil after dilation. However, due to its side effects it is no longer typically used for long-term management. Onset of effects with the drops is typically within an hour and lasts for up to a day. By mouth it is used for dry mouth as a result of Sjögren syndrome or radiation therapy.

<span class="mw-page-title-main">Intraocular pressure</span> Fluid pressure inside the eye

Intraocular pressure (IOP) is the fluid pressure inside the eye. Tonometry is the method eye care professionals use to determine this. IOP is an important aspect in the evaluation of patients at risk of glaucoma. Most tonometers are calibrated to measure pressure in millimeters of mercury (mmHg).

<span class="mw-page-title-main">Betaxolol</span> Chemical compound

Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and angina. It is also a adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm as timolol may. Betaxolol also shows greater affinity for beta1 receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye. This effect is thought to be caused by reducing the production of the liquid within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.

<span class="mw-page-title-main">Latanoprost</span> Chemical compound

Latanoprost, sold under the brand name Xalatan among others, is a medication used to treat increased pressure inside the eye. This includes ocular hypertension and open-angle glaucoma. Latanaprost is applied as eye drops to the eyes. Onset of effects is usually within four hours, and they last for up to a day.

<span class="mw-page-title-main">Timolol</span> Chemical compound

Timolol is a beta blocker medication used either by mouth or as eye drops. As eye drops it is used to treat increased pressure inside the eye such as in ocular hypertension and glaucoma. By mouth it is used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines.

Ocular hypertension is the presence of elevated fluid pressure inside the eye, usually with no optic nerve damage or visual field loss.

<span class="mw-page-title-main">Brimonidine</span> Chemical compound

Brimonidine is an α2 agonist medication used to treat open-angle glaucoma, ocular hypertension, and rosacea. In rosacea it improves the redness. It is used as eye drops or applied to the skin.

<span class="mw-page-title-main">Brinzolamide</span> Chemical compound

Brinzolamide is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

<span class="mw-page-title-main">Dorzolamide</span> Chemical compound

Dorzolamide, sold under the brand name Trusopt among others, is a medication used to treat high pressure inside the eye, including in cases of glaucoma. It is used as an eye drop. Effects begin within three hours and last for at least eight hours. It is also available as the combination dorzolamide/timolol.

<span class="mw-page-title-main">Levobunolol</span> Chemical compound

Levobunolol is a non-selective beta blocker. It is used topically in the form of eye drops to manage ocular hypertension and open-angle glaucoma.

<span class="mw-page-title-main">Bimatoprost</span> Chemical compound

Bimatoprost, sold under the brand name Lumigan among others, is a medication used to treat high pressure inside the eye including glaucoma. Specifically it is used for open angle glaucoma when other agents are not sufficient. It may also be used to increase the size of the eyelashes. It is used as an eye drop and effects generally occur within four hours.

Brimonidine/timolol, sold under the brand name Combigan among others, is a fixed-dose combination medication eye drop used for the treatment of glaucoma. It is a combination of brimonidine and timolol.

<span class="mw-page-title-main">Tafluprost</span> Chemical compound

Tafluprost is a prostaglandin analogue. It is used topically to control the progression of open-angle glaucoma and in the management of ocular hypertension, alone or in combination with other medication. It reduces intraocular pressure by increasing the outflow of aqueous fluid from the eyes.

Ripasudil, a derivative of fasudil, is a rho kinase inhibitor drug used for the treatment of glaucoma and ocular hypertension.

<span class="mw-page-title-main">Netarsudil</span> Chemical compound

Netarsudil, sold under the brand name Rhopressa among others, is a medication for the treatment of glaucoma. In the United States, in December 2017, the Food and Drug Administration (FDA) approved a 0.02% ophthalmic solution for the lowering of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension. The European Medicines Agency approved it in 2019 for the same uses under the brand name Rhokiinsa.

Bimatoprost/timolol, sold under the brand name Ganfort, is a medication for the treatment of certain conditions involving high pressure in the eyes, specifically open angle glaucoma and ocular hypertension. It is available as eye drops.

Netarsudil/latanoprost, sold under the brand name Rocklatan among others, is a fixed-dose combination medication use to treat elevated intraocular pressure (IOP) in people with open-angle glaucoma or ocular hypertension. It contains netarsudil mesylate and latanoprost. It is applied as eye drops to the eyes.

<span class="mw-page-title-main">Secondary glaucoma</span>

Secondary glaucoma is a collection of progressive optic nerve disorders associated with a rise in intraocular pressure (IOP) which results in the loss of vision. In clinical settings, it is defined as the occurrence of IOP above 21 mmHg requiring the prescription of IOP-managing drugs. It can be broadly divided into two subtypes: secondary open-angle glaucoma and secondary angle-closure glaucoma, depending on the closure of the angle between the cornea and the iris. Principal causes of secondary glaucoma include optic nerve trauma or damage, eye disease, surgery, neovascularization, tumours and use of steroid and sulfa drugs. Risk factors for secondary glaucoma include uveitis, cataract surgery and also intraocular tumours. Common treatments are designed according to the type and the underlying causative condition, in addition to the consequent rise in IOP. These include drug therapy, the use of miotics, surgery or laser therapy.

<span class="mw-page-title-main">Uveitic glaucoma</span> Glaucoma caused by uveitis or its treatments

Uveitic glaucoma is most commonly a progression stage of noninfectious anterior uveitis or iritis.

References

  1. "Brimonidine / brinzolamide ophthalmic (Simbrinza) Use During Pregnancy". Drugs.com. 5 August 2019. Retrieved 11 June 2020.
  2. "Simbrinza 10 mg/mL + 2 mg/mL eye drops, suspension - Summary of Product Characteristics (SmPC)". (emc). 17 January 2020. Retrieved 11 June 2020.
  3. 1 2 3 4 5 6 "Simbrinza- brinzolamide/brimonidine tartrate suspension/ drops". DailyMed. 9 September 2019. Retrieved 11 June 2020.
  4. 1 2 3 4 5 6 7 8 9 10 11 12 13 "Simbrinza EPAR". European Medicines Agency. Retrieved 11 June 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  5. 1 2 "Drug Approval Package: Simbrinza (brinzolamide/brimonidine tartrate) NDA #204251". U.S. Food and Drug Administration (FDA). 26 September 2013. Retrieved 11 June 2020.

Further reading