Tìm theo
Azilsartan medoxomil
Các tên gọi khác (5 ) :
  • Azilsartan
  • Azilsartan kamedoxomil
  • Azilsartan medoxomilo
  • Azilsartanum medoxomilum
  • Edarbi
angiotensin receptor antagonists
Thuốc Gốc
Small Molecule
CAS: 147403-03-0
ATC: C09CA09
CTHH: C30H24N4O8
PTK: 568.5336
Azilsartan medoxomil is an angiotensin II receptor antagonist indicated for the treatment of mild to moderate essential hypertension. Azilsartan medoxomil is a prodrug of Azilsartan marketed as "Edarbi" by Takeda. Azilsartan medoxomil has so far been shown to be superior to olmesartan and valsartan in lowering blood pressure.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C30H24N4O8
Phân tử khối
568.5336
Monoisotopic mass
568.159413764
InChI
InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)
InChI Key
InChIKey=QJFSABGVXDWMIW-UHFFFAOYSA-N
IUPAC Name
(5-methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 2-ethoxy-1-({4-[2-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]phenyl}methyl)-1H-1,3-benzodiazole-7-carboxylate
Traditional IUPAC Name
azilsartan medoxomil
SMILES
CCOC1=NC2=C(N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NOC(=O)N1)C(=CC=C2)C(=O)OCC1=C(C)OC(=O)O1
Độ tan chảy
212-214
Độ hòa tan
practically insoluble
logP
6.03
logS
-4.9
pKa (strongest acidic)
9.21
pKa (Strongest Basic)
1.75
PSA
139.57 Å2
Refractivity
149.52 m3·mol-1
Polarizability
57.73 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
7
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
6
Bioavailability
0
MDDR-Like Rule
true
pKa
6.1
Dược Lực Học : Azilsartan medoxomil decreases the pressor effect of angiotensin II. In response, angiotensin I, angiotensin II, and renin are increased while aldosterone is decreased.
Cơ Chế Tác Dụng : Azilsartan medoxomil is an angiotensin II receptor antagonist indicated for the treatment of mild to moderate essential hypertension. Azilsartan medoxomil is a prodrug of Azilsartan marketed as "Edarbi" by Takeda. Azilsartan medoxomil has so far been shown to be superior to olmesartan and valsartan in lowering blood pressure. Azilsartan medoxomil blocks the angiotensin II type 1 receptor preventing angiotensin II from binding and causing vasoconstriction. Azilsartan's ability to remain tightly bound to AT1 receptors for very long periods after drug washout is among its most unusual features.
Dược Động Học :
▧ Absorption :
Azilsartan medoxomil is hydrolyzed to the active metabolite azilsartan in the GI tract. The presence of food does not affect oral absorption of azilsartan medoxomil, and the bioavailability is 60% for azilsartan. Maximum plasma concentrations are reached in 1.5 to 3 hours.
▧ Volume of Distribution :
Azilsartan medoxomil has a Vd of 16L.
▧ Protein binding :
Azilsartan medoxomil is 99% plasma protein bound.
▧ Metabolism :
Azilsartan is metabolized by CYP2C9. CYP2C9 carries out decarboxylation of azilsartan to M-I, and O-dealkylation of azilsartan to M-II. Both M-I and M-II have no pharmacologic activity.
▧ Route of Elimination :
Renal clearance is 2.3 L/minute.
▧ Half Life :
The half-life is 11 hours, and it takes about 5 days to reach steady state concentrations.
▧ Clearance :
Fecal elimination accounts for 55%, urine excretion 42%, and unchanged drug 15%.
Độc Tính : Hypotension and diarrhea are most common.
Chỉ Định : Treatment of hypertension (alone or as an adjunct).
Tương Tác Thuốc :
  • Acetylsalicylic acid Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Amifostine Azilsartan medoxomil used in combintation with amifostine may lead to hypotension.
  • Avanafil Pharmacodynamic synergist- increases effects.
  • Benazepril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Captopril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Celecoxib Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Citric Acid Increases serum potassium.
  • Diclofenac Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Diflunisal Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Enalapril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Etodolac Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Exenatide Pharmacodynamic synergist- increases effects. May also increase hypoglycemic effects by improving insulin sensitivity.
  • Fenoprofen Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Flurbiprofen Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Fosinopril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Ibuprofen Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Indomethacin Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Ketoprofen Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Ketorolac Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Liraglutide Pharmacodynamic synergist- increases effects. May also increase hypoglycemic effects by improving insulin sensitivity.
  • Lisinopril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Lithium Azilsartan medoxomil may increase lithium serum concentrations.
  • Maraviroc Pharmacodynamic synergist- increases effects.
  • Meclofenamic acid Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Mefenamic acid Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Meloxicam Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Moexipril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Nabumetone Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Naproxen Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Nitroglycerin Pharmacodynamic synergist- increases effects.
  • Oxaprozin Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Perindopril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Piroxicam Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Quinapril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Ramipril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
  • Rituximab Azilsartan medoxomil used in combination with rituximab may lead to hypotension.
  • Sulfasalazine Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Sulindac Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Tadalafil Pharmacodynamic synergist- increases effects.
  • Tolmetin Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Trandolapril Pharmacodynamic synergism: dual blockade of renin-angiotensin system. Increases risks of hypotension, hyperkalemia, renal impairment.
Liều Lượng & Cách Dùng : Tablet - Oral - 40 mg
Tablet - Oral - 80 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Takeda
    Sản phẩm biệt dược : Edarbi
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08822
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08865
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64764-844-30
Wikipedia
http://en.wikipedia.org/wiki/Azilsartan
RxList
http://www.rxlist.com/edarbi-drug.htm
Drugs.com
http://www.drugs.com/ingredient/azilsartan-medoxomil.html
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