Tìm theo
Amiloride
Các tên gọi khác (9 ) :
  • 3,5-Diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide
  • Amilorid
  • Amilorida
  • Amiloride
  • Amiloridum
  • Amipramidin
  • Amipramidine
  • Amyloride
  • N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide
Thuốc lợi tiểu
Thuốc Gốc
Small Molecule
CAS: 2016-88-8
ATC: C03DB01
ĐG : Kaiser Foundation Hospital
CTHH: C6H8ClN7O
PTK: 229.627
A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H8ClN7O
Phân tử khối
229.627
Monoisotopic mass
229.04788562
InChI
InChI=1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)
InChI Key
InChIKey=XSDQTOBWRPYKKA-UHFFFAOYSA-N
IUPAC Name
3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
Traditional IUPAC Name
amiloride
SMILES
NC(N)=NC(=O)C1=C(N)N=C(N)C(Cl)=N1
Độ tan chảy
240.5-241.5
Độ hòa tan
Slightly soluble
logP
-0.3
logS
-2.3
pKa (strongest acidic)
16.46
pKa (Strongest Basic)
3.29
PSA
159.29 Å2
Refractivity
56.69 m3·mol-1
Polarizability
19.99 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
8
H Bond Donor Count
4
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
8.7
Dược Lực Học : Amiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.
Cơ Chế Tác Dụng : A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705) Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.
Dược Động Học :
▧ Absorption :
Readily absorbed following oral administration.
▧ Metabolism :
Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.
▧ Route of Elimination :
Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours.
▧ Half Life :
Plasma half-life varies from 6 to 9 hours.
Độc Tính : No data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance.
Chỉ Định : For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
Tương Tác Thuốc :
  • Benazepril Increased risk of hyperkalemia
  • Candesartan Increased risk of hyperkalemia
  • Captopril Increased risk of hyperkalemia
  • Cilazapril Increased risk of hyperkalemia
  • Dihydroquinidine barbiturate Decreases the antiarrhythmic effect of quinidine
  • Enalapril Increased risk of hyperkalemia
  • Eplerenone Increased risk of hyperkalemia. Monitor serum potassium levels during concomitant threapy.
  • Eprosartan Increased risk of hyperkalemia
  • Forasartan Increased risk of hyperkalemia
  • Fosinopril Increased risk of hyperkalemia
  • Irbesartan Increased risk of hyperkalemia
  • Lisinopril Increased risk of hyperkalemia
  • Losartan Increased risk of hyperkalemia
  • Moexipril Increased risk of hyperkalemia
  • Perindopril Increased risk of hyperkalemia
  • Polystyrene sulfonate Risk of alkalosis in renal impairment
  • Potassium Increased risk of hyperkalemia
  • Quinapril Increased risk of hyperkalemia
  • Quinidine Amiloride may decrease the therapeutic effect of quinidine. Monitor for changes in the therapeutic and adverse effects of quinidine if amiloride if initiated, discontinued or dose changed.
  • Quinidine barbiturate Decreases the antiarrhythmic effect of quinidine
  • Ramipril Increased risk of hyperkalemia
  • Saprisartan Increased risk of hyperkalemia
  • Spirapril Increased risk of hyperkalemia
  • Tasosartan Increased risk of hyperkalemia
  • Telmisartan Telmisartan may increase the hyperkalemic effect of Amiloride. Monitor for increased serum potassium concentrations during concomitant therapy.
  • Trandolapril Increased risk of hyperkalemia. Monitor serum potassium levels.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Valsartan Increased risk of hyperkalemia
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Sharp & Dohme
    Sản phẩm biệt dược : Arumil
  • Công ty : Orion
    Sản phẩm biệt dược : Diurex
  • Công ty : Alphapharm
    Sản phẩm biệt dược : Kaluril
  • Công ty : Merck
    Sản phẩm biệt dược : Midamor
  • Công ty : Merck
    Sản phẩm biệt dược : Modamide
  • Sản phẩm biệt dược : Moduret
  • Công ty : Merck
    Sản phẩm biệt dược : Moduretic
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00594
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=16231
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508156
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06821
ChemSpider
http://www.chemspider.com/Chemical-Structure.15403.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=16173
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64980-151-01
PharmGKB
http://www.pharmgkb.org/drug/PA448368
Wikipedia
http://en.wikipedia.org/wiki/Amiloride
RxList
http://www.rxlist.com/cgi/generic2/amilor.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mod1272.shtml
Drugs.com
http://www.drugs.com/cdi/amiloride.html
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