ブリンゾラミド
ブリンゾラミド (Brinzolamide) is a pharmaceutical product used for the intraocular pressure drop of the open-angle glaucoma patient who is a carbonic anhydrase inhibitor (). Brand name エイゾプト.
 | |
| Material name by the IUPAC glossology | |
|---|---|
| (5R) -5-ethylamino-3-(3-methoxypropyl) - 2,2-dioxo-2λ6,9-dithia- 3-azabicyclo[4.3.0]nona-7,10-diene- 8-sulfonamide | |
| Clinical data | |
| Sale name | Azopt, Befardin |
| Drugs.com | monograph |
| MedlinePlus | a601233 |
| License | EMA: Link、US FDA: Link |
| Fetus degree of risk classification |
|
| Legal regulation |
|
| Dosage method | Ophthalmic |
| Pharmacokinetics data | |
| Bioavailability | Absorbed systemically, but below detectable levels (less than 10 ng/mL) |
| Plasma protein combination | ~60% |
| Half-life | 111 days |
| Excretion | Renal (60%) |
| Identification | |
| CAS number (MeSH) | 138,890-62-7 |
| ATC cord | S01EC04 (WHO) |
| PubChem | CID: 68844 |
| IUPHAR/BPS | 6797 |
| DrugBank | DB01194  |
| ChemSpider | 62077 |
| UNII | 9451Z89515 |
| KEGG | D00652 |
| ChEBI | CHEBI: 3176 |
| ChEMBL | CHEMBL220491 |
| Chemical data | |
| Chemical formula | C12H21N3O5S3 |
| Molecular weight | 383.51 g/mol |
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Table of contents
Effect, effect
Glaucoma, high intraocular pressure symptom
Contraindicated
It is eye drops, but excretion delays in the patients with the serious renal insufficiency, and a side effect might occur because it is absorbed in the body, and I am excreted by kidney.
Side effect
As a result of Japan and overseas clinical trial, a side effect was seen in 20.0% of patients in total and saw fog as a local side effect of eyes, and the inflammation of the cornea, hyperemia, a feeling of alien substance, ache in the eye occurred, and fatigue, a headache, taste abnormality, oligocythemia were recognized as a systemic side effect.
Action mechanism
It is a carbonic anhydrase inhibitor, and ブリンゾラミド strongly inhibits carbonic anhydrase II (CA-II) in particular. There is it in a red blood cell mainly, and the carbonic anhydrase is distributed unevenly to the whole body including eyes. When existing CA-II is inhibited in the ciliary body of eyes, generation of the HCO3- decreases, and active transport of Na+ which is an anti-ion is restrained, and aqueous humor production decreases, and, as a result, an intraocular pressure decreases [1]; [2]: 20.
Pharmacokinetics
Absorption
The recommended dosage frequency is instillation twice a day. After instillation, a part is absorbed to a whole body, but the plasma concentration is lower than a measurement lower limit level because most adhere to an organization and a red blood cell (<10ng/mL). Because unevenness of the absorption factor from gastrointestinal tract is big, and the oral administration increases the side effect, I am not recommended.
Distribution
A plasma protein combination rate of ブリンゾラミド is 60%, but most bind to the red blood cell having a carbonic anhydrase. Because the ブリンゾラミド abundance with the red blood cell is hard to be greatly metabolized, the half-life of ブリンゾラミド from all over the whole blood is very long with 111 days.
Metabolism
Among metabolism things, N-de-エチルブリンゾラミド has carbonic anhydrase (I, II) inhibitory activity. This is a main metabolism thing in the Homo sapiens. The other metabolism thing (N-de-methoxypropyl body and O-demethyl body) does not have activity [2]: 29.
Excretion
60% of ブリンゾラミド are excreted in urine by non-change, but the value of the clearance is not found. But the whole body clearance of the intravenous injection (5 mg/kg) is set of 30.9+-9.1mL/m/kg experimentally [2]: 26. In addition, N-de-エチルブリンゾラミド is detected from all over the urine, and N-de-メトキシプロピルブリンゾラミド, O-de-メチルブリンゾラミド are detected in lower density, too, but these excretion parameters are not demanded.
Medical mixture with timolol
ブリンゾラミド and medical mixture with timolol of sympathetic nerve β receptor blockade are manufactured in the name of アゾルガ. The clinical trial provides the result that is better than the case of ブリンゾラミド or the timolol single agent [3].
Source
- ^ "1% of エイゾプト suspension-related eye drops attached document"(April, 2016). July 21, 2016 reading.
- ^ a b c "エイゾプト suspension-related eye drops 1% interview form (PDF) "(April, 2016). July 21, 2016 reading.
- ^ Croxtall JD, Scott, LJ.[1]. Drugs&Aging 2009, 26 (5): 437-446. doi: 10.2165/00002512-200926050-00007.
- "Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification.." Eye 19 (3): 303–7. (2005). doi: 10.1038/sj.eye.6701470. PMID 15258611.
- "Retinal peripapillary blood flow before and after topical brinzolamide.." Ophthalmologica 218 (6): 390–6. (2004). doi: 10.1159/000080942. PMID 15564757.
- "Effects of brinzolamide on ocular haemodynamics in healthy volunteers.". Br J Ophthalmol 88 (2): 257–62. (2004). doi: 10.1136/bjo.2003.021485. PMC 1771998. It is . PMID 14736787
- "The long-term safety and efficacy of brinzolamide 1.0% (azopt) in patients with primary open-angle glaucoma or ocular hypertension.." Am J Ophthalmol 129 (2): 136–143. (2000). doi: 10.1016/S0002-9394(99) 00343-8. PMID 10682964.
- Product Information: Azopt(R), brinzolamide. Alcon Laboratories, Inc, Fort Worth, TX, 1998b.
- Sall KN, Greff LJ, Johnson-Pratt LR, DeLucca PT, Polis AB, Kolodny AH et al. (2003). "Dorzolamide/timolol combination versus concomitant administration of brimonidine and timolol: six-month comparison of efficacy and tolerability.". Ophthalmology 110 (3): 615-24. doi: 10.1016/S0161-6420(02) 01900-0. It is . PMID 12623832
This article is taken from the Japanese Wikipedia ブリンゾラミド
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