Tìm theo
Indapamide
Các tên gọi khác (5 ) :
  • Indapamid
  • Indapamida
  • Indapamide
  • Indapamidum
  • Metindamide
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 26807-65-8
ATC: C03BA11
ĐG : Actavis Group , http://www.actavis.com
CTHH: C16H16ClN3O3S
PTK: 365.835
A benzamide-sulfonamide-indole. It is called a thiazide-like diuretic but structure is different enough (lacking the thiazo-ring) so it is not clear that the mechanism is comparable. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H16ClN3O3S
Phân tử khối
365.835
Monoisotopic mass
365.06008979
InChI
InChI=1S/C16H16ClN3O3S/c1-10-8-11-4-2-3-5-14(11)20(10)19-16(21)12-6-7-13(17)15(9-12)24(18,22)23/h2-7,9-10H,8H2,1H3,(H,19,21)(H2,18,22,23)
InChI Key
InChIKey=NDDAHWYSQHTHNT-UHFFFAOYSA-N
IUPAC Name
4-chloro-N-(2-methyl-2,3-dihydro-1H-indol-1-yl)-3-sulfamoylbenzamide
Traditional IUPAC Name
indapamide
SMILES
CC1CC2=CC=CC=C2N1NC(=O)C1=CC(=C(Cl)C=C1)S(N)(=O)=O
Độ tan chảy
160-162
Độ hòa tan
75 mg/L
logP
2.2
logS
-4
pKa (strongest acidic)
8.85
pKa (Strongest Basic)
0.097
PSA
92.5 Å2
Refractivity
103.31 m3·mol-1
Polarizability
36.34 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.8
Dược Lực Học : Indapamide is an antihypertensive and a diuretic. It contains both a polar sulfamoyl chlorobenzamide moiety and a lipid- soluble methylindoline moiety. Indapamide bears a structural similarity to the triazide diuretics which are known to decrease vascular smooth muscle reactivity. However, it differs chemically from the thiazides in that it does not possess the thiazide ring system and contains only one sulfonamide group. Indapamide appears to cause vasodilation, probably by inhibiting the passage of calcium and other ions (sodium, potassium) across membranes. This same effect may cause hypokalcemia in susceptible individuals. Indapamide has also been shown to cause uterine myometrial relaxation in experimental animals. Overall, indapamide has an extra-renal antihypertensive action resulting in a decrease in vascular hyperreactivity and a reduction in total peripheral and arteriolar resistance.
Cơ Chế Tác Dụng : A benzamide-sulfonamide-indole. It is called a thiazide-like diuretic but structure is different enough (lacking the thiazo-ring) so it is not clear that the mechanism is comparable. [PubChem] Indapamide blocks the slow component of delayed rectifier potassium current (IKs) without altering the rapid component (IKr) or the inward rectifier current. Specifically it blocks or antagonizes the action the proteins KCNQ1 and KCNE1. Indapamide is also thought to stimulate the synthesis of the vasodilatory hypotensive prostaglandin PGE2.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from gastrointestinal tract.
▧ Protein binding :
71-79%
▧ Metabolism :
Primarily hepatic. Indapamide is an extensively metabolized drug with only about 7+ACU- of the total dose administered, recovered in the urine as unchanged drug during the first 48 hours after administration.
▧ Route of Elimination :
Indapamide is an extensively metabolized drug, with only about 7% of the total dose administered, recovered in the urine as unchanged drug during the first 48 hours after administration.
▧ Half Life :
14 hours (biphasic)
Độc Tính : Side effects include electrolyte imbalance (potassium or salt depletion due to too much fluid loss), nausea, stomach disorders, vomiting, weakness
Chỉ Định : For the treatment of hypertension, alone or in combination with other antihypertensive drugs, as well as for the treatment of salt and fluid retention associated with congestive heart failure or edema from pregnancy (appropriate only in the management of edema of pathologic origin during pregnancy when clearly needed). Also used for the management of edema as a result of various causes.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Deslanoside Possible electrolyte variations and arrhythmias
  • Diazoxide Significant hyperglycemic effect
  • Digitoxin Possible electrolyte variations and arrhythmias
  • Digoxin Possible electrolyte variations and arrhythmias
  • Dofetilide Increased risk of cardiotoxicity and arrhythmias
  • Lithium The thiazide diuretic, indapamide, may increase serum levels of lithium.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trandolapril The thiazide diuretic, Indapamide, may increase the hypotensive effect of Trandolapril. Indapamide may also increase the nephrotoxicity of Trandolapril. Monitor for postural hypotension at initiation of concomitant therapy and renal dysfunction during chronic therapy.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Servier
    Sản phẩm biệt dược : Arifon
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  • Công ty : Teofarma
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  • Công ty : Visufarma
    Sản phẩm biệt dược : Ipamix
  • Công ty : Servier
    Sản phẩm biệt dược : Lozide
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Lozol
  • Công ty : Servier
    Sản phẩm biệt dược : Natrilix
  • Công ty : Kyoto Yakuhin
    Sản phẩm biệt dược : Natrix
  • Công ty : Sandoz
    Sản phẩm biệt dược : Noranat
  • Công ty : Azevedos
    Sản phẩm biệt dược : Tandix
  • Công ty : Servier
    Sản phẩm biệt dược : Tertensif
  • Công ty : Baldacci
    Sản phẩm biệt dược : Veroxil
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00808
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3702
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508626
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00345
ChemSpider
http://www.chemspider.com/Chemical-Structure.3574.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25901
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0339-6494-11
PharmGKB
http://www.pharmgkb.org/drug/PA449975
Wikipedia
http://en.wikipedia.org/wiki/Indapamide
RxList
http://www.rxlist.com/cgi/generic/indap.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/loz1241.shtml
Drugs.com
http://www.drugs.com/cdi/indapamide.html
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