Dorzolamide
 | |
 | |
| Clinical data | |
|---|---|
| Trade names | Trusopt, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a602022 |
| Routes of administration | eye drops |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Protein binding | ~33% |
| Elimination half-life | 4 months |
| Identifiers | |
| |
| CAS Number |
|
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII |
|
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.229.271 |
| Chemical and physical data | |
| Formula | C10H16N2O4S3 |
| Molar mass | 324.43 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?) (verify) | |
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.[3] It is used as an eye drop.[3] Effects begin within three hours and last for at least eight hours.[3] It is also available as the combination dorzolamide/timolol.[3][4]
Common side effects include eye discomfort, eye redness, taste changes, and blurry vision.[3] Serious side effects include Steven Johnson syndrome.[3] Those allergic to sulfonamides may be allergic to dorzolamide.[3][5] Use is not recommended in pregnancy or breastfeeding.[5] It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humor.[3]
Dorzolamide was approved for medical use in the United States in 1994.[3] It is available as a generic medication.[5] In 2022, it was the 201st most commonly prescribed medication in the United States, with more than 2 million prescriptions.[6][7]
Medical uses
[edit]Dorzolamide is used to lower excessive intraocular pressure in open-angle glaucoma and ocular hypertension.[3] This drug is able to cross the cornea, reach the ciliary body of the eye, and produce systemic effects on the carbonic anhydrase enzyme within the eye.
Side effects
[edit]Ocular stinging, burning, itching and bitter taste.[8] It causes shallowing of the anterior chamber and leads to transient myopia. As a second generation carbonic anhydrase inhibitor, dorzolamide avoids systemic effects associated with first generation carbonic anhydrase inhibitors such as acetazolamide, methazolamide, and dichlorphenamide.
Pharmacodynamics
[edit]![[icon]](/https/en.wikipedia.org/wiki/File:Wiki_letter_w_cropped.svg){kind=small} | This section needs expansion. You can help by adding to it. (January 2019) |
Dorzolamide lowers intraocular pressure by about 20%.[8] Normally, carbonic anhydrase converts carbonic acid (H2CO3) into bicarbonate (HCO3), releasing a proton (H+) into solution. The H+ is then exchanged for sodium (Na+) ions, which facilitates the production of aqueous humor [citation needed]. By blocking the function of carbonic anhydrase, the Na+/H+ exchange is unable to occur, which leads to a decrease in Na+ in the cell and prevents aqueous humor production [citation needed].
History
[edit]Dorzolamide, developed by Merck, was the first medication in human therapy (market introduction 1995) that resulted from structure-based drug design. It was developed to circumvent the systemic side effects of acetazolamide which has to be taken orally.[8]
References
[edit]- ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
- ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
- ^ a b c d e f g h i j "Dorzolamide Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 26 March 2019.
- ^ "Dorzolamide (Ophthalmic Route) Description and Brand Names". Mayo Clinic. Retrieved 3 November 2023.
- ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1148. ISBN 9780857113382.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Dorzolamide Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
- ^ a b c KD Tripari MD (2004). Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.
Further reading
[edit]- Kubinyi H (1999). "Chance favors the prepared mind--from serendipity to rational drug design". J Recept Signal Transduct Res. 19 (1–4): 15–39. doi:10.3109/10799899909036635. PMID 10071748.
- Plummer C, MacKay E, Gelatt K (2006). "Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs". Veterinary Ophthalmology. 9 (4): 245–9. doi:10.1111/j.1463-5224.2006.00469.x. PMID 16771760.
- Grover S, Apushkin M, Fishman G (2006). "Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa". Am J Ophthalmol. 141 (5): 850–8. doi:10.1016/j.ajo.2005.12.030. PMID 16546110.
- Almeida G, Faria e Souza S (2006). "Effect of topical dorzolamide on rabbit central corneal thickness". Braz J Med Biol Res. 39 (2): 277–81. doi:10.1590/S0100-879X2006000200015. PMID 16470316. S2CID 31212591.