Tìm theo
Dorzolamide
Các tên gọi khác (10 ) :
  • (4S-trans)-4-(ETHYLAMINO)-5,6-dihydro-6-methyl-4H-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
  • (4S,6S)-4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • (4S,trans)-4-(Ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide
  • 4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno[2,3-b]thiopyran-2-sulfonic acid amide
  • 4S,6S-Dorzolamide
  • Dorzolamid
  • Dorzolamida
  • Dorzolamide
  • Dorzolamidum
Thuốc Gốc
Small Molecule
CAS: 120279-96-1
ATC: S01EC03
ĐG : Apotex Inc. , http://www.apotex.com
CTHH: C10H16N2O4S3
PTK: 324.44
Dorzolamide is a carbonic anhydrase (CA) inhibitor. It is used in ophthalmic solutions (Trusopt) to lower intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H16N2O4S3
Phân tử khối
324.44
Monoisotopic mass
324.02721908
InChI
InChI=1S/C10H16N2O4S3/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16)/t6-,8-/m0/s1
InChI Key
InChIKey=IAVUPMFITXYVAF-XPUUQOCRSA-N
IUPAC Name
(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1$l^{6},7-thieno[2,3-b][1$l^{6}]thiopyran-6-sulfonamide
Traditional IUPAC Name
dorzolamide
SMILES
CCN[C@H]1C[C@H](C)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O
Độ tan chảy
283-285 °C
Độ hòa tan
6.99e-01 g/l
logP
-1
logS
-2.7
pKa (strongest acidic)
8.18
pKa (Strongest Basic)
7.14
PSA
106.33 Å2
Refractivity
72.46 m3·mol-1
Polarizability
31.55 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Dorzolamide is topical CA inhibitor that is indicated for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Dorzolamide reduces IOP by approximately 17-23% in patients with elevater IOP.
Cơ Chế Tác Dụng : Dorzolamide is a carbonic anhydrase (CA) inhibitor. It is used in ophthalmic solutions (Trusopt) to lower intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension. Dorzolamide is a sulfonamide and a highly specific carbonic anhydrase II (CA-II) inhibitor, which is the main CA isoenzyme involved in aqueous humor secretion. Inhibition of CA-II 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. Dorzolamide also accumulates in red blood cells as a result of CA-II binding, as CA-II is found predominantly in erythrocytes. However, sufficient CA-II activity remains so that adverse effects due to systemic CA inhibition are not observed.
Dược Động Học :

▧ Protein binding :
~33%
▧ Route of Elimination :
Dorzolamide is primarily excreted unchanged in the urine; the metabolite also is excreted in urine.
▧ Half Life :
4 months
Độc Tính : Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest
Chỉ Định : For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Also used prophylatically for the inhibition of perioperative IOP increase (before neodynium yttrium aluminum garnet laser posterior capsulotomy).
Tương Tác Thuốc :
  • Brinzolamide 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.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Merck
    Sản phẩm biệt dược : Trusopt
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00869
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06969
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07871
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50043906
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0093-7618-33
PharmGKB
http://www.pharmgkb.org/drug/PA164748765
Wikipedia
http://en.wikipedia.org/wiki/Dorzolamide
RxList
http://www.rxlist.com/cgi/generic/dorzolamide.htm
Drugs.com
http://www.drugs.com/cdi/dorzolamide-drops.html
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