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药品详细

Indapamide (吲达帕胺 )

化学结构式图
中文名
吲达帕胺
英文名
Indapamide
分子式
Not Available
化学名
4-chloro-N-(2-methyl-2,3-dihydro-1H-indol-1-yl)-3-sulfamoylbenzamide
分子量
Average: 365.835
Monoisotopic: 365.060089790
CAS号
26807-65-8
ATC分类
C03B 未知
药物类型
small molecule
阶段
商品名
Apo-Indapamide;Arifon;Bajaten;Cormil;Fludex;Idapamide;Indamol;Ipamix;Lozide;Lozol;Natrilix;Natrix;Noranat;Novo-Indapamide;Nu-Indapamide;Pressurai;Tandix;Tertensif;Veroxil;
同义名
Indapamida [INN-Spanish];Indapamidum [INN-Latin];
基本介绍

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]

生产厂家
  • Actavis elizabeth llc
  • Alphapharm party ltd
  • Cadista pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Sanofi aventis us llc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Dong DL, Wang QH, Yue P, Jiao JD, Gu RM, Yang BF: Indapamide induces apoptosis of GH3 pituitary cells independently of its inhibition of voltage-dependent K+ currents. Eur J Pharmacol. 2006 Apr 24;536(1-2):78-84. Epub 2006 Mar 2. Pubmed
剂型
Form Route Strength
Tablet Oral
规格
Unit description Cost Unit
Indapamide 2.5 mg tablet 0.85 USD tablet
Indapamide 1.25 mg tablet 0.69 USD tablet
Lozide 2.5 mg Tablet 0.55 USD tablet
Apo-Indapamide 2.5 mg Tablet 0.31 USD tablet
Mylan-Indapamide 2.5 mg Tablet 0.31 USD tablet
Novo-Indapamide 2.5 mg Tablet 0.31 USD tablet
Nu-Indapamide 2.5 mg Tablet 0.31 USD tablet
Pms-Indapamide 2.5 mg Tablet 0.31 USD tablet
Apo-Indapamide 1.25 mg Tablet 0.2 USD tablet
Mylan-Indapamide 1.25 mg Tablet 0.2 USD tablet
Pms-Indapamide 1.25 mg Tablet 0.2 USD tablet
化合物类型
Type small molecule
Classes
  • Indoles and Indole Derivatives
  • Benzenesulfonamides
  • Phenethylamines
  • Benzamides
  • Amphetamines
Substructures
  • Carboxylic Acids and Derivatives
  • Indoles and Indole Derivatives
  • Amino Ketones
  • Sulfonyls
  • Benzene and Derivatives
  • Aryl Halides
  • Benzenesulfonamides
  • Halobenzenes
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Sulfonamides
  • Hydrazine Derivatives
  • Benzoyl Derivatives
  • Phenylhydrazines
  • Benzamides
  • Anilines
  • Amphetamines
  • Pyrrolines
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication 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.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Rapidly absorbed from gastrointestinal tract.
Volume of distribution Not Available
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)
Clearance Not Available
Toxicity Side effects include electrolyte imbalance (potassium or salt depletion due to too much fluid loss), nausea, stomach disorders, vomiting, weakness
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00110 Indapamide Pathway SMP00110
理化性质
Properties
State solid
Melting point 161 oC
Experimental Properties
Property Value Source
water solubility 75 mg/L PhysProp
logP 2.2 PhysProp
pKa 8.8 Various sources
Predicted Properties
Property Value Source
water solubility 3.42e-02 g/l ALOGPS
logP 2.52 ALOGPS
logP 2.43 ChemAxon Molconvert
logS -4.03 ALOGPS
pKa 11.69 ChemAxon Molconvert
hydrogen acceptor count 4 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 92.50 ChemAxon Molconvert
rotatable bond count 3 ChemAxon Molconvert
refractivity 103.31 ChemAxon Molconvert
polarizability 36.34 ChemAxon Molconvert
药物相互作用
Drug Interaction
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.
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).
食物相互作用
  • Take without regard to meals. Magnesium, potassium and zinc needs increased.

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