Brinzolamide/brimonidine

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]

Brinzolamide/brimonidine
Combination of
BrinzolamideCarbonic anhydrase inhibitor
BrimonidineAlpha-adrenergic agonist
Clinical data
Trade namesSimbrinza
AHFS/Drugs.comProfessional 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
FormulaC23H31BrN8O5S3
Molar mass675.64 g·mol−1
3D model (JSmol)
SMILES
  • 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
  • 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

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]

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. "Simbrinza- brinzolamide/brimonidine tartrate suspension/ drops". DailyMed. 9 September 2019. Retrieved 11 June 2020.
  4. "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. "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


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