Peringatan Keamanan

Indapamide overdose symptoms may include but are not limited to nausea, vomiting, gastrointestinal disorders, electrolyte disturbances and weakness.L13982 Other signs of overdose include respiratory depression and severe hypotension.L13982 In cases of overdose, supportive care interventions may be necessary to manage symptoms.L13982 Emesis and gastric lavage may be recommended to empty the stomach; however, patients should be monitored closely for any electrolyte or fluid imbalances.L13982

Indapamide

DB00808

small molecule approved

Deskripsi

The most significant modifiable risk factor for cardiovascular disease and the most prominent contributor to all-cause mortality is hypertension.A204155 Characterized by an office blood pressure of ?140/90, hypertension is pervasive and impacts an estimated 25% of adults globally.A204155 Treatment for hypertension should include a number of lifestyle changes (ie. reduced sodium intake) along with pharmacotherapy - it should be noted that treatment with several antihypertensive agents may be required in order to achieve blood pressure targets.A204155

Thiazide-like diuretics such as indapamide are a valuable tool for the treatment of hypertension and continue to grow in popularity, falling behind only ACE inhibitors in terms of prescription frequency.A204134 When compared to hydrochlorothiazide (another commonly prescribed diuretic), indapamide has been shown to be superior at lowering systolic blood pressure, reducing left ventricular mass index, lowering oxidative stress, inhibiting platelet aggregation, and reducing microalbuminuria associated with diabetes.A204134 Interestingly, unlike thiazide diuretics, several sources suggest that indapamide is not associated with glucose or lipid disturbances.A204134,A204161

Indapamide is characterized by both a methylindoline and a sulfamoyl chlorobenzamide functional group, with the former being largely responsible for the molecule’s lipid solubility.A204158

Struktur Molekul 2D

Berat 365.835
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Indapamide is characterized by biphasic elimination.[A203663] In healthy subjects, indapamide's elimination half-life can range from 13.9 to 18 hours.[A203627,A203519] The long half-life is conducive to once-daily dosing.[A203663]
Volume Distribusi Some sources report an apparent volume of distribution of 25 L for indapamide, while others report a value of approximately 60 L.[A203663,A203519,A204113]
Klirens (Clearance) Indapamide's renal and hepatic clearance values are reported to be 1.71 mL/min and 20-23.4 mL/min, respectively.[A203627]

Absorpsi

The bioavailability of indapamide is virtually complete after an oral dose and is unaffected by food or antacids.A203663,A203519 Indapamide is highly lipid-soluble due to its indoline moiety - a characteristic that likely explains why indapamide’s renal clearance makes up less than 10% of its total systemic clearance.A203627,A203663,A203519 The Tmax occurs approximately 2.3 hours after oral administration.A203663 The Cmax and AUC0-24 values are 263 ng/mL and 2.95 ug/hr/mL, respectively.A203663

Metabolisme

As a result of extensive metabolism in the liver, the majority of indapamide excreted is metabolized, with only 7% remaining unchanged.A203663 In humans, as many as 19 distinct indapamide metabolites may be produced, although not all have been identified.A203627,A203663 There are several metabolic routes through which indapamide may be metabolized, and CYP3A4 is the main enzyme involved in the corresponding hydroxylation, carboxylation, and dehydrogenation reactions.A34415 Indapamide can undergo dehydrogenation to form M5, then oxidation to form M4, then further hydroxylation at the indole moiety to form M2.A17553 These reactions are facilitated by CYP3A4.A17553 Another route of metabolism occurs when indapamide is first hydroxylated to M1 by CYP3A4.A17553 M1 then undergoes dehydrogenation to form M3 and is further oxidized to form M2.A17553 Hydroxylation of indapamide’s indole moiety is thought to form the major metabolite (M1), which is less pharmacologically active compared to its parent compound according to animal studies.A203663 Indapamide may also undergo epoxidation via CYP3A4 to form a reactive epoxide intermediate.A17553 The unstable epoxide intermediate may then undergo dihydroxylation via microsomal epoxide hydrolase to form M6, or glutathione conjugation to form M7.A17553

Rute Eliminasi

An estimated 60-70% of indapamide is eliminated in the urine, while 16-23% is eliminated in the feces.A203627

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. Alcohol may potentiate orthostatic hypotension.
  • 2. Increase consumption of potassium-rich foods. Indapamide my cause potassium depletion leading to hypokalemia.
  • 3. Take with or without food.

Interaksi Obat

1808 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Indapamide is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Indapamide is combined with Levodopa.
Risperidone Indapamide may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Indapamide.
Amifostine Indapamide may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Indapamide.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Indapamide.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Indapamide.
Obinutuzumab Indapamide may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Indapamide.
Rituximab Indapamide may increase the hypotensive activities of Rituximab.
Midodrine Midodrine may decrease the antihypertensive activities of Indapamide.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Indapamide.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Indapamide.
Doxapram Doxapram may decrease the antihypertensive activities of Indapamide.
Metaraminol Metaraminol may decrease the antihypertensive activities of Indapamide.
Nicergoline Nicergoline may decrease the antihypertensive activities of Indapamide.
Methoxamine Methoxamine may decrease the antihypertensive activities of Indapamide.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Indapamide.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Indapamide.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Indapamide.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Indapamide.
Naratriptan Naratriptan may decrease the antihypertensive activities of Indapamide.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Indapamide.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Indapamide.
Mephentermine Mephentermine may decrease the antihypertensive activities of Indapamide.
MMDA MMDA may decrease the antihypertensive activities of Indapamide.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Indapamide.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Indapamide.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Indapamide.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Indapamide.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Indapamide.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Indapamide.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Indapamide.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Indapamide.
Periciazine Periciazine may decrease the antihypertensive activities of Indapamide.
Acepromazine Acepromazine may decrease the antihypertensive activities of Indapamide.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Indapamide.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Indapamide.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Indapamide.
Amineptine Amineptine may decrease the antihypertensive activities of Indapamide.
Amibegron Amibegron may decrease the antihypertensive activities of Indapamide.
Naluzotan Naluzotan may decrease the antihypertensive activities of Indapamide.
Solabegron Solabegron may decrease the antihypertensive activities of Indapamide.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Indapamide.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Indapamide.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Indapamide.
Isometheptene Isometheptene may decrease the antihypertensive activities of Indapamide.
Naphazoline Naphazoline may decrease the antihypertensive activities of Indapamide.
Saralasin Saralasin may decrease the antihypertensive activities of Indapamide.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Indapamide.
Cinitapride Cinitapride may decrease the antihypertensive activities of Indapamide.
Tyramine Tyramine may decrease the antihypertensive activities of Indapamide.
Adrafinil Adrafinil may decrease the antihypertensive activities of Indapamide.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Indapamide.
Etilefrine Etilefrine may decrease the antihypertensive activities of Indapamide.
Cirazoline Cirazoline may decrease the antihypertensive activities of Indapamide.
Synephrine Synephrine may decrease the antihypertensive activities of Indapamide.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Indapamide.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Indapamide.
Amitraz Amitraz may decrease the antihypertensive activities of Indapamide.
Medetomidine Medetomidine may decrease the antihypertensive activities of Indapamide.
Xylazine Xylazine may decrease the antihypertensive activities of Indapamide.
Atipamezole Atipamezole may decrease the antihypertensive activities of Indapamide.
Ractopamine Ractopamine may decrease the antihypertensive activities of Indapamide.
Romifidine Romifidine may decrease the antihypertensive activities of Indapamide.
Detomidine Detomidine may decrease the antihypertensive activities of Indapamide.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Indapamide.
Ritobegron Ritobegron may decrease the antihypertensive activities of Indapamide.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Indapamide.
Dopexamine Dopexamine may decrease the antihypertensive activities of Indapamide.
Piclozotan Piclozotan may decrease the antihypertensive activities of Indapamide.
Idazoxan Idazoxan may decrease the antihypertensive activities of Indapamide.
Higenamine Higenamine may decrease the antihypertensive activities of Indapamide.
Reproterol Reproterol may decrease the antihypertensive activities of Indapamide.
Opipramol Opipramol may decrease the antihypertensive activities of Indapamide.
Tramazoline Tramazoline may decrease the antihypertensive activities of Indapamide.
Mephedrone Mephedrone may decrease the antihypertensive activities of Indapamide.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Indapamide.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Indapamide.
Quinupramine Quinupramine may decrease the antihypertensive activities of Indapamide.
Octopamine Octopamine may decrease the antihypertensive activities of Indapamide.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Indapamide.
Fenozolone Fenozolone may decrease the antihypertensive activities of Indapamide.
Norfenefrine Norfenefrine may decrease the antihypertensive activities of Indapamide.
Melitracen Melitracen may decrease the antihypertensive activities of Indapamide.
Oxyfedrine Oxyfedrine may decrease the antihypertensive activities of Indapamide.
Lofepramine Lofepramine may decrease the antihypertensive activities of Indapamide.
Xenon Xenon may decrease the antihypertensive activities of Indapamide.
Iprindole Iprindole may decrease the antihypertensive activities of Indapamide.
Buflomedil Buflomedil may decrease the antihypertensive activities of Indapamide.
Metergoline Metergoline may decrease the antihypertensive activities of Indapamide.
Rimiterol Rimiterol may decrease the antihypertensive activities of Indapamide.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Indapamide.
Methoxyphenamine Methoxyphenamine may decrease the antihypertensive activities of Indapamide.
Tretoquinol Tretoquinol may decrease the antihypertensive activities of Indapamide.
Gepefrine Gepefrine may decrease the antihypertensive activities of Indapamide.
Prenalterol Prenalterol may decrease the antihypertensive activities of Indapamide.
Xamoterol Xamoterol may decrease the antihypertensive activities of Indapamide.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Indapamide.

Target Protein

Solute carrier family 12 member 3 SLC12A3
Potassium voltage-gated channel subfamily KQT member 1 KCNQ1

Referensi & Sumber

Synthesis reference: Chunyi Yeh, Yi-Lung Wang, Ya-Sheng Yang, Ya-Ching Chang Chein, "Oral sustained-release pharmaceutical composition of indapamide, production and use thereof." U.S. Patent US20060182803, issued August 17, 2006.
Artikel (PubMed)
  • PMID: 16556441
    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.
  • PMID: 6489195
    Chaffman M, Heel RC, Brogden RN, Speight TM, Avery GS: Indapamide. A review of its pharmacodynamic properties and therapeutic efficacy in hypertension. Drugs. 1984 Sep;28(3):189-235. doi: 10.2165/00003495-198428030-00001.
  • PMID: 10491728
    Bataillard A, Schiavi P, Sassard J: Pharmacological properties of indapamide. Rationale for use in hypertension. Clin Pharmacokinet. 1999;37 Suppl 1:7-12. doi: 10.2165/00003088-199937001-00002.
  • PMID: 4077233
    Thomas JR: A review of 10 years of experience with indapamide as an antihypertensive agent. Hypertension. 1985 Nov-Dec;7(6 Pt 2):II152-6. doi: 10.1161/01.hyp.7.6pt2.ii152.
  • PMID: 19074530
    Sun H, Moore C, Dansette PM, Kumar S, Halpert JR, Yost GS: Dehydrogenation of the indoline-containing drug 4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoylbenzamide (indapamide) by CYP3A4: correlation with in silico predictions. Drug Metab Dispos. 2009 Mar;37(3):672-84. doi: 10.1124/dmd.108.022707. Epub 2008 Dec 12.
  • PMID: 6869203
    Caruso FS, Szabadi RR, Vukovich RA: Pharmacokinetics and clinical pharmacology of indapamide. Am Heart J. 1983 Jul;106(1 Pt 2):212-20. doi: 10.1016/0002-8703(83)90119-9.
  • PMID: 3395370
    Urien S, Riant P, Renouard A, Coulomb B, Rocher I, Tillement JP: Binding of indapamide to serum proteins and erythrocytes. Biochem Pharmacol. 1988 Aug 1;37(15):2963-6. doi: 10.1016/0006-2952(88)90282-1.
  • PMID: 20528637
    Duarte JD, Cooper-DeHoff RM: Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics. Expert Rev Cardiovasc Ther. 2010 Jun;8(6):793-802. doi: 10.1586/erc.10.27.
Menampilkan 8 dari 19 artikel.
Textbook
  • Lukasz Komsta, Monika Waksmundzka-Hajnos, Joseph Sherma (2014). Thin Layer Chromatography in Drug Analysis. Taylor & Francis.

Contoh Produk & Brand

Produk: 99 • International brands: 11
Produk
  • Apo-indapamide 1.25 Mg Tablets
    Tablet • 1.25 mg • Oral • Canada • Generic • Approved
  • Apo-indapamide 2.5mg Tablets
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-perindopril-indapamide
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-perindopril-indapamide
    Tablet • - • Oral • Canada • Generic • Approved
  • Apo-perindopril-indapamide
    Tablet • - • Oral • Canada • Generic • Approved
  • Arcosyl Plus
    Tablet • - • Oral • Canada • Approved
  • Arcosyl Plus
    Tablet • - • Oral • Canada • Approved
  • Arcosyl Plus Ld
    Tablet • - • Oral • Canada • Approved
Menampilkan 8 dari 99 produk.
International Brands
  • Arifon — Servier
  • Bajaten — Merck
  • Fludex — Servier
  • Indamol — Teofarma
  • Ipamix — Visufarma
  • Natrilix — Servier
  • Natrix — Kyoto Yakuhin
  • Noranat — Sandoz
  • Tandix — Azevedos
  • Tertensif — Servier

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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