Tìm theo
Methazolamide
Các tên gọi khác (5 ) :
  • Metazolamida
  • Methazolamid
  • Méthazolamide
  • Methazolamidum
  • SID26747005
Thuốc Gốc
Small Molecule
CAS: 554-57-4
ATC: S01EC05
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C5H8N4O3S2
PTK: 236.272
A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C5H8N4O3S2
Phân tử khối
236.272
Monoisotopic mass
236.003781522
InChI
InChI=1S/C5H8N4O3S2/c1-3(10)7-4-9(2)8-5(13-4)14(6,11)12/h1-2H3,(H2,6,11,12)/b7-4-
InChI Key
InChIKey=FLOSMHQXBMRNHR-DAXSKMNVSA-N
IUPAC Name
N-[(2Z)-3-methyl-5-sulfamoyl-2,3-dihydro-1,3,4-thiadiazol-2-ylidene]acetamide
Traditional IUPAC Name
methazolamide
SMILES
CN1N=C(S\C1=N/C(C)=O)S(N)(=O)=O
Độ tan chảy
213.5 °C
Độ hòa tan
3500 mg/L
logP
0.13
logS
-1.83
pKa (strongest acidic)
10.06
pKa (Strongest Basic)
-3.6
PSA
105.19 Å2
Refractivity
51.3 m3·mol-1
Polarizability
21.17 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
7.30
Dược Lực Học : Methazolamide is topical carbonic anhydrase inhibitor. Methazolamide is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Methazolamide is a sulfonamide derivative; however, it does not have any clinically significant antimicrobial properties. Although methazolamide achieves a high concentration in the cerebrospinal fluid, it is not-considered an effective anticonvulsant. Methazolamide has a weak and transient diuretic effect, therefore use results in an increase in urinary volume, with excretion of sodium, potassium and chloride.
Cơ Chế Tác Dụng : A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem] Methazolamide is a potent inhibitor of carbonic anhydrase. 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.
Dược Động Học :
▧ Absorption :
Methazolamide is well absorbed from the gastrointestinal tract.
▧ Volume of Distribution :
* 17 to 23 L
▧ Protein binding :
55%
▧ Half Life :
14 hours
Độc Tính : Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur in the case of an overdose.
Chỉ Định : For treatment of chronic open-angle glaucoma and acute angle-closure glaucoma
Tương Tác Thuốc :
  • Acetylsalicylic acid Acetylsalicylic acid at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Bismuth Subsalicylate The salicylate, bismuth subsalicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Brinzolamide 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.
  • Magnesium salicylate The salicylate, magnesium salicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Memantine Possible increased levels of memantine
  • Salicylate-sodium The salicylate, salicylate-sodium, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Salsalate The salicylate, salsalate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trisalicylate-choline The salicylate, trisalicylate-choline, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Teva
    Sản phẩm biệt dược : Methazolamide
  • Sản phẩm biệt dược : Naptazane
  • Công ty : Fera
    Sản phẩm biệt dược : Neptazane
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00703
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4100
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506393
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07764
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00655
ChemSpider
http://www.chemspider.com/Chemical-Structure.3958.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10881
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-1072-01
PharmGKB
http://www.pharmgkb.org/drug/PA450413
Wikipedia
http://en.wikipedia.org/wiki/Methazolamide
RxList
http://www.rxlist.com/cgi/generic2/methaz.htm
Drugs.com
http://www.drugs.com/cdi/methazolamide.html
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