Dorzolamide

  • (4S, 6S )-4 -ethylamino- 6-methyl- 7,7- dioxo- 5 ,6 -dihydro -4H -thieno [5,4 -b] thiopyran -2-sulfonamide
  • (all- S)-4 -ethylamino- 6-methyl- 7,7- dioxo- 5 ,6 -dihydro -4H -thieno [5,4 -b] thiopyran -2-sulfonamide
  • C10H16N2O4S3 ( dorzolamide )
  • C10H16N2O4S3 · HCl ( dorzolamide hydrochloride · )

S01EC03

Carbonic anhydrase inhibitors

  • 324.44 g · mol -1 ( dorzolamide )
  • 360.9 g · mol -1 ( · dorzolamide hydrochloride)

264 ° C ( · dorzolamide hydrochloride)

  • > 250 mg · kg -1 ( LD50, dog, oral)
  • 1320 mg · kg -1 ( LD50, mouse, oral)
  • 1927 mg · kg -1 ( LD50, rat, oral)

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Dorzolamide is a sulfur - and nitrogen-containing, chiral heterocyclic chemical compound derived from thiophene. Because of their effectiveness as carbonic anhydrase inhibitors, the pure (4S, 6S) -isomer is used as a drug in eye drops for the lowering of intraocular pressure.

A structurally related and similar -acting drug is brinzolamide.

Properties

Dorzolamide is a white, crystalline powder which is readily soluble in water, slightly in methanol or ethanol. Instead of the base, the hydrochloride is used as a drug because of the improved handling and solubility in water.

Clinical trials

The efficacy of dorzolamide as a finished product Trusopt has been in clinical trials in patients tested with glaucoma and elevated intraocular pressure ( 23 mmHg). Here, the preparation was in a 2% dosage reduce the pressure to 13 to 22 %. These values ​​were constant over a test period of one year. In combination with the beta-blocker timolol in Germany dorzolamide as a finished product Cosopt ®. It is for the treatment of elevated intraocular pressure (IOP ) in patients with open-angle glaucoma or pseudoexfoliation when monotherapy is not sufficient with a beta blocker.

Side effects

Common side effects include: nausea, bitter taste, headache, weakness and fatigue, on the eye: burning and stinging, superficial punctate keratitis, tearing, conjunctivitis, blepharitis, Lidreizung, itching of the eyes, blurred vision.

Trade names

Trusopt (D, A, CH), Dorzo -Vision ( D)

Cosopt (D, A, CH), and generic (A)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Active ingredient
292277
de