Tìm theo
Acetazolamide
Các tên gọi khác (14 ) :
  • 2-acetylamino-1,3,4-Thiadiazole-5-sulfonamide
  • 5-ACETAMIDO-1,3,4-thiadiazole-2-sulfonamide
  • 5-acetylamino-1,3,4-Thiadiazole-2-sulfonamide
  • Acetazolamid
  • Acetazolamida
  • Acétazolamide
  • Acetazolamidum
  • Defiltran
  • Diacarb
  • Diamox
  • Diluran
  • Glaupax
  • N-[5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide
  • N-[5-(Aminosulfonyl)-1,3,5-thiadiazol-2-yl]acetamide
Thuốc dùng điều trị mắt, tai mũi họng
Thuốc Gốc
Small Molecule
CAS: 59-66-5
ATC: S01EC01
ĐG : American Cyanamid Co.
CTHH: C4H6N4O3S2
PTK: 222.245
One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C4H6N4O3S2
Phân tử khối
222.245
Monoisotopic mass
221.988131458
InChI
InChI=1S/C4H6N4O3S2/c1-2(9)6-3-7-8-4(12-3)13(5,10)11/h1H3,(H2,5,10,11)(H,6,7,9)
InChI Key
InChIKey=BZKPWHYZMXOIDC-UHFFFAOYSA-N
IUPAC Name
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
Traditional IUPAC Name
acetazolamide
SMILES
CC(=O)NC1=NN=C(S1)S(N)(=O)=O
Độ tan chảy
260.5 °C
Độ hòa tan
980 mg/L (at 30 °C)
logP
-0.26
logS
-2.36
pKa (strongest acidic)
6.93
pKa (Strongest Basic)
-3.3
PSA
115.04 Å2
Refractivity
47.36 m3·mol-1
Polarizability
19.16 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
7.2
Dược Lực Học : Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. Acetazolamide is not a mercurial diuretic. Rather, it is a nonbacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides.
Cơ Chế Tác Dụng : One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) The anticonvulsant activity of Acetazolamide may depend on a direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.
Dược Động Học :

▧ Protein binding :
98%
▧ Half Life :
3 to 9 hours
Chỉ Định : For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
Tương Tác Thuốc :
  • Acetylsalicylic acid Acetylsalicylic acid at high dose increases the effect of the carbonic anhydrase inhibitor, acetazolamide.
  • Bismuth Subsalicylate The salicylate, bismuth subsalicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, acetazolamide.
  • Brinzolamide 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.
  • Cyclosporine Acetazolamide may increase the effect and toxicity of cyclosporine.
  • Memantine Possible increased levels of memantine
  • Tobramycin Increased risk of nephrotoxicity
  • Topiramate Additive renal carbonic anhydrase inhibition may occur increasing the risk of crystaluria and renal calculi. Increased risk of nephrolithiasis. Consider altnerate therapy.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Triprolidine The CNS depressants, Triprolidine and Acetazolamide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Medphano
    Sản phẩm biệt dược : Acemit
  • Công ty : Acme
    Sản phẩm biệt dược : Acemox
  • Công ty : Akorn
    Sản phẩm biệt dược : Acetak
  • Công ty : Micro Vision
    Sản phẩm biệt dược : Acetamide
  • Công ty : Pfoshen
    Sản phẩm biệt dược : Acetazolamax
  • Công ty : Intas
    Sản phẩm biệt dược : Avva
  • Công ty : Ethical
    Sản phẩm biệt dược : Azm
  • Công ty : New Chemical
    Sản phẩm biệt dược : Azol
  • Sản phẩm biệt dược : Azomid
  • Công ty : Edol
    Sản phẩm biệt dược : Carbinib
  • Công ty : CSP
    Sản phẩm biệt dược : Défiltran
  • Công ty :
    Sản phẩm biệt dược : Defiltran
  • Công ty : Raymos
    Sản phẩm biệt dược : Diabo
  • Công ty : Polpharma
    Sản phẩm biệt dược : Diacarb
  • Công ty : Sanofi Aventis
    Sản phẩm biệt dược : Diamox
  • Công ty : Goldshield
    Sản phẩm biệt dược : Diamox Depot
  • Công ty :
    Sản phẩm biệt dược : Diamox Sequels
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Diazomid
  • Công ty : Zentiva
    Sản phẩm biệt dược : Diluran
  • Công ty : Polpharma
    Sản phẩm biệt dược : Diuramid
  • Công ty : Chiesi
    Sản phẩm biệt dược : Edemox
  • Công ty : Phebra
    Sản phẩm biệt dược : Glaumox
  • Công ty : Omnivision
    Sản phẩm biệt dược : Glaupax
  • Công ty : Phebra
    Sản phẩm biệt dược : Glupax
  • Công ty : Teva
    Sản phẩm biệt dược : Huma-Zolamide
  • Công ty : FDC
    Sản phẩm biệt dược : Iopar-SR
  • Công ty : Pharmaland
    Sản phẩm biệt dược : Medene
  • Công ty : Acromax
    Sản phẩm biệt dược : Oculten
  • Công ty : Santen
    Sản phẩm biệt dược : Ödemin
  • Công ty : Taro
    Sản phẩm biệt dược : Uramox
  • Công ty : Vista Pharma
    Sản phẩm biệt dược : Zolmide
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00819
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=1986
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504493
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06805
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00218
ChemSpider
http://www.chemspider.com/Chemical-Structure.1909.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10880
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0513-02
PharmGKB
http://www.pharmgkb.org/drug/PA448018
Wikipedia
http://en.wikipedia.org/wiki/Acetazolamide
RxList
http://www.rxlist.com/cgi/generic/aceta.htm
Drugs.com
http://www.drugs.com/cdi/acetazolamide.html
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