Dorzolamide

Dorzolamide, sold under the brand name Trusopt among others, is medications used to treat high pressure inside the eye including glaucoma.[1] It is used as an eye drop.[1] Effects begin within three hours and lasts for at least eight hours.[1] It is also available as the combination dorzolamide/timolol.[1]

Dorzolamide
Clinical data
Trade namesTrusopt, others
AHFS/Drugs.comMonograph
MedlinePlusa602022
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration
    Topical (eye drops)
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Protein binding~33%
    Elimination half-life4 months
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC10H16N2O4S3
    Molar mass324.443 g/mol g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    Common side effects include eye discomfort, eye redness, taste changes, and blurry vision.[1] Serious side effects include Steven Johnson syndrome.[1] Those allergic to sulfonamides may be allergic to dorzolamide.[1][2] Use is not recommended in pregnancy or breastfeeding.[2] It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humour.[1]

    Dorzolamide was approved for medical use in the United States in 1994.[1] It is available as a generic medication.[2] A 5 milliliter bottle in the United Kingdom costs the NHS less than 2 £ as of 2019.[2] In the United States the wholesale cost of this amount is about US$7.10.[3] In 2016 it was the 271st most prescribed medication in the United States with more than a million prescriptions.[4]

    Medical uses

    Dorzolamide hydrochloride is used to lower excessive intraocular pressure in open-angle glaucoma and ocular hypertension.

    Side effects

    Ocular stinging, burning, itching and bitter taste.[5] It causes shallowing of the anterior chamber and leads to transient myopia.

    Pharmacodynamics

    It lowers IOP by about 20%.[5]

    History

    This drug, developed by Merck, was the first drug 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.[5]

    References

    1. "Dorzolamide Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 26 March 2019.
    2. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1148. ISBN 9780857113382.
    3. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
    4. "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
    5. KD Tripari MD. Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.

    Further reading

    • 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". Vet Ophthalmol. 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.
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