Tìm theo
Brinzolamide
Các tên gọi khác (2) :
  • Azopt
  • Brinzolamide
anti glaucoma agents, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 138890-62-7
ATC: S01EC04
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C12H21N3O5S3
PTK: 383.507
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H21N3O5S3
Phân tử khối
383.507
Monoisotopic mass
383.064332867
InChI
InChI=1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1
InChI Key
InChIKey=HCRKCZRJWPKOAR-JTQLQIEISA-N
IUPAC Name
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1$l^{6},7,2-thieno[3,2-e][1$l^{6},2]thiazine-6-sulfonamide
Traditional IUPAC Name
brinzolamide
SMILES
CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O
Độ tan chảy
131 °C
Độ hòa tan
7.13e-01 g/l
logP
-1.8
logS
-2.7
pKa (strongest acidic)
8.19
pKa (Strongest Basic)
6.78
PSA
118.8 Å2
Refractivity
87.2 m3·mol-1
Polarizability
37.93 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Used in the treatment of glaucoma, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide can decrease intraocular pressure by approximately 16-19% in patients with elevated intraocular pressure.
Cơ Chế Tác Dụng : Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Brinzolamide is a highly specific inhibitor of CA-II, which is the main CA isoenzyme involved in the secretion of aqueous humor. Inhibition of CA in the ciliary process of the eye slows the formation of bicarbonate, and reduces sodium and fluid transport. This results in a reduction in the rate of aqueous humor secretion and the intraocular pressure. Brinzolamide is absorbed systemically following topical ocular administration. Since it has a high affinity for CA-II, brinzolamide binds extensively to red blood cells, where CA-II is primarily found. As sufficient CA-II activity remains, adverse effects resulting from the systemic inhibition of CA by brinzolamide are not observed. The metabolite N-desethyl brinzolamide is also formed. This metabolite binds to CA and accumulates in red blood cells as well. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I (CA-I).
Dược Động Học :
▧ Absorption :
Absorbed into systemic circulation following topical ocular application
▧ Protein binding :
Approximately 60%.
▧ Metabolism :
Ophthalmic
▧ Half Life :
111 days
Chỉ Định : For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Tương Tác Thuốc :
  • Acetazolamide As both brinzolamide and acetazolamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
  • Diclofenamide As both brinzolamide and dichlorphenamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
  • Dorzolamide As both brinzolamide and dorzolamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
  • Methazolamide As both brinzolamide and methazolamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
  • Topiramate As both brinzolamide and topiramate are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
  • Zonisamide As both brinzolamide and zonisamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
Liều Lượng & Cách Dùng : Suspension - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Azopt
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01194
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=68844
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507071
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07760
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00652
ChemSpider
http://www.chemspider.com/Chemical-Structure.62077.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10885
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0065-0275-25
PharmGKB
http://www.pharmgkb.org/drug/PA164744929
Wikipedia
http://en.wikipedia.org/wiki/Brinzolamide
RxList
http://www.rxlist.com/cgi/generic3/brinzolamide.htm
Drugs.com
http://www.drugs.com/cdi/brinzolamide-drops.html
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