クロルタリドン
- 関
- Thiazide diuretics
- 同
- Hygroton
WordNet
- a diuretic (trade names Hygroton and Thalidone) used to control hypertension and conditions that cause edema; effective in lowering blood pressure to prevent heart attacks (同)Hygroton, Thalidone
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2017/01/19 17:56:59」(JST)
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Chlortalidone
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|
Clinical data |
Trade names |
Generic, many tradenames worldwide[1] |
AHFS/Drugs.com |
Consumer Drug Information |
MedlinePlus |
a682342 |
Pregnancy
category |
|
Routes of
administration |
Oral |
ATC code |
C03BA04 (WHO) |
Legal status |
Legal status |
|
Pharmacokinetic data |
Protein binding |
75% |
Biological half-life |
40 hours |
Excretion |
Renal |
Identifiers |
IUPAC name
- (RS)-2-Chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide
|
CAS Number |
77-36-1 Y |
PubChem (CID) |
2732 |
IUPHAR/BPS |
7147 |
DrugBank |
DB00310 Y |
ChemSpider |
2631 Y |
UNII |
Q0MQD1073Q Y |
KEGG |
D00272 Y |
ChEBI |
CHEBI:3654 Y |
ChEMBL |
CHEMBL1055 Y |
ECHA InfoCard |
100.000.930 |
Chemical and physical data |
Formula |
C14H11ClN2O4S |
Molar mass |
338.766 g/mol |
3D model (Jmol) |
Interactive image |
Chirality |
Racemic mixture |
SMILES
-
O=S(=O)(N)c1c(Cl)ccc(c1)C2(O)c3ccccc3C(=O)N2
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InChI
-
InChI=1S/C14H11ClN2O4S/c15-11-6-5-8(7-12(11)22(16,20)21)14(19)10-4-2-1-3-9(10)13(18)17-14/h1-7,19H,(H,17,18)(H2,16,20,21) Y
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Key:JIVPVXMEBJLZRO-UHFFFAOYSA-N Y
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(verify) |
Chlortalidone (INN/BAN) or chlorthalidone (USAN) is a diuretic drug used to treat hypertension, originally marketed as Hygroton in the USA. It is described as a thiazide diuretic (or, rather, a thiazide-like diuretic because it acts similarly to the thiazides but does not contain the benzothiadiazine molecular structure). Compared with other medications of the thiazide class, chlortalidone has the longest duration of action but a similar diuretic effect at maximal therapeutic doses. It is often used in the management of hypertension and edema.
Unlike loop diuretics, chlortalidone efficacy is diminished in patients with certain renal diseases (e.g. chronic renal disease). A clinical trial (ALLHAT) in 2002 compared chlortalidone to doxazosin in the treatment of high-risk hypertensive patients. In this study, only chlortalidone significantly reduced the risk of combined cardiovascular disease events, especially heart failure, when compared with drugs such as doxazosin.[2] Chlortalidone was approved by the FDA in 1960. The ALLHAT study conclusions showed that there was no significant difference in all-cause mortality, fatal heart disease, or non-fatal myocardial infarction when chlortalidone was compared with lisinopril or amlodipine but did show decreased rates of heart failure after 6 years when compared with amlodipine and decreased rates of cerebrovascular disease after 6 years when compared with lisinopril leading the study conclusions to say that thiazide-type diuretics are preferred first-step in antihypertensive therapy.
In terms of activity, chlorothalidone is very similar to hydrochlorothiazide[citation needed] and is used as an independent drug or in combination with other antihypertensive agents for lowering arterial blood pressure, and also as an adjuvant drug for treating edema caused by cardiac insufficiency and renal irregularities, including nephrotic syndrome.
Contents
- 1 Mechanism of action
- 2 Banned for some sports
- 3 See also
- 4 References
Mechanism of action
Chlortalidone prevents reabsorption of sodium and chloride by inhibiting the Na+/Cl− symporter in the distal convoluted tubule. Thiazides and related compounds also decrease the glomerular filtration rate, which further reduces the drug's efficacy in patients with kidney impairment (e.g. kidney insufficiency). By increasing the delivery of sodium to the distal renal tubule, chlortalidone indirectly increases potassium excretion via the sodium-potassium exchange mechanism (i.e. apical ROMK/Na channels coupled with basolateral NKATPases). This can result in hypokalemia and hypochloremia as well as a mild metabolic alkalosis; however, the diuretic efficacy of chlortalidone is not affected by the acid-base balance of the patient being treated.
Initially, diuretics lower blood pressure by decreasing cardiac output and reducing plasma and extracellular fluid volume. Eventually, cardiac output returns to normal, and plasma and extracellular fluid volume return to slightly less than normal, but a reduction in peripheral vascular resistance is maintained, thus resulting in an overall lower blood pressure. The reduction in intravascular volume induces an elevation in plasma renin activity and aldosterone secretion, further contributing to the potassium loss associated with thiazide diuretic therapy.
Banned for some sports
Chlortalidone is banned for some sports (including cricket) because it is a diuretic.[3]
See also
References
- ^ drugs.com drugs.com international listing of Chlortalidone Page accessed May 13, 2015
- ^ ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group (18 December 2002). "Major outcomes in high-risk hypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs diuretic: The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT)". JAMA. 288 (23): 2981–97. doi:10.1001/jama.288.23.2981. PMID 12479763.
- ^ http://m.bbc.co.uk/sport/cricket/35185202
Symporter inhibitors
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Na+-Cl− |
- Thiazides: Bendroflumethiazide
- Chlorothiazide
- Cyclopenthiazide
- Cyclothiazide
- Hydrochlorothiazide
- Hydroflumethiazide
- Methyclothiazide
- Polythiazide
- Trichlormethiazide; Others: Chlortalidone (chlorthalidone)
- Metolazone
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Na+-K+-Cl− |
|
Antihypertensives: diuretics (C03)
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|
Sulfonamides
(and etacrynic acid) |
CA inhibitors (at PT) |
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Loop (Na-K-Cl at AL) |
- Furosemide#
- Bumetanide
- Etacrynic acid
- Etozolin
- Muzolimine
- Ozolinone
- Piretanide
- Tienilic acid
- Torasemide
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|
Thiazides (Na-Cl at DCT,
Calcium-sparing) |
- Altizide
- Bendroflumethiazide
- Chlorothiazide
- Cyclopenthiazide
- Cyclothiazide
- Epitizide
- Hydrochlorothiazide#
- Hydroflumethiazide
- Mebutizide
- Methyclothiazide
- Polythiazide
- Trichlormethiazide
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|
Thiazide-likes (primarily DCT) |
- Quinethazone
- Clopamide
- Chlortalidone
- Mefruside
- Clofenamide
- Metolazone
- Meticrane
- Xipamide
- Indapamide
- Clorexolone
- Fenquizone
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|
|
Potassium-sparing (at CD) |
ESC blockers |
- Amiloride#
- Triamterene
- Benzamil
|
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Aldosterone antagonists |
- Spirolactones: Spironolactone#
- Eplerenone
- Potassium canrenoate
- Canrenone
- Non-steroidal: Finerenone
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Osmotic diuretics (PT, DL) |
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Vasopressin receptor inhibitors
(DCT and CD) |
- Vaptans: Conivaptan
- Mozavaptan
- Satavaptan
- Tolvaptan
- Others: Demeclocycline
- Lithium carbonate
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Other |
- Ethanol, Isopropanol, 2M2B
- mercurial diuretics (Chlormerodrin, Mersalyl, Meralluride)
- Theobromine
- Cicletanine
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|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
UpToDate Contents
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English Journal
- Thiazides in advanced chronic kidney disease: time for a randomized controlled trial.
- Sinha AD1, Agarwal R.
- Current opinion in cardiology.Curr Opin Cardiol.2015 Jul;30(4):366-72. doi: 10.1097/HCO.0000000000000188.
- PURPOSE OF REVIEW: Chronic kidney disease is common, associated with increased cardiovascular risk, and frequently complicated by hypertension, requiring multiple agents for control. Thiazides are naturally attractive for use in this population; unfortunately, they are classically thought to be inef
- PMID 26049383
- Hydrochlorothiazide is not the most useful nor versatile thiazide diuretic.
- Vongpatanasin W1.
- Current opinion in cardiology.Curr Opin Cardiol.2015 Jul;30(4):361-5. doi: 10.1097/HCO.0000000000000178.
- PURPOSE OF REVIEW: To determine usefulness and versatility of hydrochlorothiazide (HCTZ) relative to other thiazide diuretics in the treatment of hypertension.RECENT FINDINGS: HCTZ was found to be less potent in lowering blood pressure (BP) than other thiazide diuretics, including chlorthalidone (CT
- PMID 26049382
- Refractory Hypertension: Evidence of Heightened Sympathetic Activity as a Cause of Antihypertensive Treatment Failure.
- Dudenbostel T1, Acelajado MC2, Pisoni R2, Li P2, Oparil S2, Calhoun DA2.
- Hypertension.Hypertension.2015 Jul;66(1):126-33. doi: 10.1161/HYPERTENSIONAHA.115.05449. Epub 2015 May 18.
- Refractory hypertension is an extreme phenotype of treatment failure defined as uncontrolled blood pressure in spite of ≥5 classes of antihypertensive agents, including chlorthalidone and a mineralocorticoid receptor antagonist. A prospective evaluation of possible mechanisms of refractory hyperte
- PMID 25987662
- Simultaneous quantification of atenolol and chlorthalidone in human plasma by ultra performance liquid chromatography-tandem mass spectrometry.
- Shah JV1, Patel DP2, Shah PA1, Sanyal M3, Shrivastav PS1.
- Biomedical chromatography : BMC.Biomed Chromatogr.2015 Jun 10. doi: 10.1002/bmc.3537. [Epub ahead of print]
- A simple, sensitive and reproducible ultra performance liquid chromatography-tandem mass spectrometry method has been developed for the simultaneous determination of atenolol, a β-adrenergic receptor-blocker and chlorthalidone, a monosulfonamyl diuretic in human plasma using atenolol-d7 and chlorth
- PMID 26096961
Japanese Journal
- Comparison of the efficacy between hydrochlorothiazide and chlorthalidone on central aortic pressure when added on to candesartan in treatment-naive patients of hypertension
- KWON Beom-June,JANG Sung-Won,CHOI Kyu-Young,KIM Dong-Bin,CHO Eun-Joo,IHM Sang-Hyun,YOUN Ho-Joong,KIM Jae-Hyung
- Hypertension research : clinical and experimental : official journal of the Japanese Society of Hypertension 36(1), 79-84, 2013-01-01
- NAID 10031163289
- A novel software tool for high throughput measurements of interconversion barriers : DCXplorer
- TRAPP Oliver
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 875(1), 42-47, 2008-11-01
- NAID 10028007861
- Outcomes in hypertensive black and nonblack patients treated with chlorthalidone, amlodipine, and lisinopril
- Hydrochlorothaizide versus chlorthalidone. Evidence supporting their interchangeability
Related Links
- Chlortalidone (INN/BAN) or chlorthalidone (USAN) is a diuretic drug used to treat hypertension, originally marketed as Hygroton in the USA. It is described as a thiazide diuretic (or, rather, a thiazide-like diuretic because it acts similarly to the ...
- 24 Nov 2003 ... Hydrochlorothiazide and chlorthalidone have been the 2 most commonly used diuretics in major clinical trials. Treatment guidelines and compendia often consider these 2 drugs interchangeable agents within the class of ...
Related Pictures
★リンクテーブル★
[★]
クロルタリドン、クロルサリドン
- 関
- chlorthalidone、Hygroton
[★]
ハイグロトン
- 関
- chlortalidone、chlorthalidone
[★]
- 英
- chlorthalidone
- 関
-chlorthalidone