S01EC04 - Brinzolamide |
Propably not porphyrinogenic |
PNP |
Rationale
sulfonamide derivative preferentially distributed to red blood cells. Probably insignificant hepatic load. Very long final elimination time from erythrocytes.
Chemical description
(To be edited, initial data ST OCT 04) sulfonamide used in eyedrops (10 mg/mL) to reduce the intraocular pressure in glaucoma. Isopropyl ester prodrug to an active prostaglandine analogue. Conversion to the active acid form takes place through hydrolysis. Reaches circulation in topical application but due to effective bindnding to erytrocyte carboanhydrases the plasma levels are very low, often lower than 10 ng/ml. Long elimination time in blood; half time about six months. Metabolized by CYPs 3A4 (major enzyme), 2A6, 2C8, 2C9. Brinzolamide and its N-desethyl metabolite is excreted in urine, 20 % as metabolites.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
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