出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/08/08 17:05:11」(JST)
Systematic (IUPAC) name | |
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6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide | |
Clinical data | |
Trade names | Apo-hydro, Aquazide h, Dichlotride among others, Oretic |
AHFS/Drugs.com | monograph |
MedlinePlus | a682571 |
Pregnancy cat. | B (D if used to treat pregnancy-induced hypertension) |
Legal status | ℞ Prescription only |
Routes | Oral (capsules, tablets, oral solution) |
Pharmacokinetic data | |
Bioavailability | Variably absorbed from GI tract. Bioavailability ~ 70% |
Metabolism | does not undergo significant metabolism (>95% excreted unchanged in urine)[1] |
Half-life | 5.6–14.8 h |
Excretion | Primarily excreted unchanged in urine |
Identifiers | |
CAS number | 58-93-5 Y |
ATC code | C03AA03 |
PubChem | CID 3639 |
DrugBank | DB00999 |
ChemSpider | 3513 Y |
UNII | 0J48LPH2TH Y |
KEGG | D00340 Y |
ChEMBL | CHEMBL435 Y |
Chemical data | |
Formula | C7H8ClN3O4S2 |
Mol. mass | 297.74 |
SMILES
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InChI
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Y (what is this?) (verify) |
Hydrochlorothiazide, abbreviated HCTZ, HCT, or HZT, is a diuretic drug of the thiazide class that acts by inhibiting the kidneys' ability to retain water. This reduces the volume of the blood, decreasing blood return to the heart and thus cardiac output and, by other mechanisms, is believed to lower peripheral vascular resistance.[2]
It is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic health system.[3]
Hydrochlorothiazide is frequently used for the treatment of hypertension, congestive heart failure, symptomatic edema, diabetes insipidus, renal tubular acidosis, and the prevention of kidney stones.[4]
Most of the research supporting the use of thiazide diuretics in hypertension was done using chlorthalidone, a different medication in the same class. Some more recent studies have suggested that chlorthalidone might be the more effective thiazide diuretic.[5]
It is also sometimes used for treatment of hypoparathyroidism,[6] hypercalciuria, Dent's disease and Ménière's disease. For diabetes insipidus, the effect of thiazide diuretics is presumably mediated by a hypovolemia-induced increase in proximal sodium and water reabsorption, thereby diminishing water delivery to the ADH-sensitive sites in the collecting tubules and increasing the urine output.
Thiazides are also used in the treatment of osteoporosis. Thiazides decrease mineral bone loss by promoting calcium retention in the kidney, and by directly stimulating osteoblast differentiation and bone mineral formation.[7]
It is frequently given together with other antihypertensive agents in fixed combination preparations, such as losartan (an angiotensin II receptor antagonist) as hydrochlorothiazide/losartan.
These side effects increase with the dose of the medication and are most common at doses of greater than 25 mg per day.
Package inserts, based on case reports and observational studies, have reported that an allergy to a sulfa drug predisposes the patient to cross sensitivity to a thiazide diuretic. A 2005 review of the literature did not find support for this cross-sensitivity.[8]
Hydrochlorothiazide belongs to thiazide class of diuretics. It reduces blood volume by acting on the kidneys to reduce sodium (Na) reabsorption in the distal convoluted tubule. The major site of action in the nephron appears on an electroneutral Na+-Cl− co-transporter by competing for the chloride site on the transporter. By impairing Na transport in the distal convoluted tubule, hydrochlorothiazide induces a natriuresis and concomitant water loss. Thiazides increase the reabsorption of calcium in this segment in a manner unrelated to sodium transport.[9] Additionally, by other mechanisms, HCTZ is believed to lower peripheral vascular resistance.[10]
Hydrochlorothiazide is sold both as a generic drug and under a large number of brand names, including BP Zide 12.5 & 25 (Stadmed), Apo-Hydro, Aquazide H,Dichlotride, Hydrodiuril, HydroSaluric, Hydrochlorot, Microzide, Esidrex, and Oretic.
Hydrochlorothiazide is also used in combination with many other classes of hypertensive drugs such as ACE inhibitors, angiotensin receptor blockers, and beta blockers. These are sold under brand names including Diovan HCT, Zestoretic, Ziac, Benicar HCT, Olmy-H, Atacand HCT, and Lotensin HCT, Temax-H and others.
Hydrochlorothiazide was detected in the urine of the Russian cyclist Alexandr Kolobnev during the 2011 Tour de France.[11] Kolobnev was the only cyclist to leave the 2011 race in connection with adverse findings at a doping control.[12] While hydrochlorothiazide is not itself a performance-enhancing drug, it may be used to mask the use of performance-enhancing drugs, and is classed by the World Anti-Doping Agency as a "specified substance". Kolobnev was subsequently cleared of all charges of intentional doping.[13][14]
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(help)Duarte, JD; Cooper-Dehoff, RM (2010). "Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics". Expert review of cardiovascular therapy 8 (6): 793–802. doi:10.1586/erc.10.27. PMC 2904515. PMID 20528637. NIHMSID: NIHMS215063
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リンク元 | 「利尿薬」「ヒドロクロロチアジド」 |
拡張検索 | 「benzylhydrochlorothiazide」「sodium restriction-hydrochlorothiazide-spironolactone loading test」 |
CATIONS | ANIONS | 尿酸 | 腎血液動態 | |||||||||||||
Na+ | K+ | H+ | Ca2+ | Mg2+ | Cl- | HCO3- | H2PO4- | 急性 | 慢性 | RBF | GFR | FF | TGF | |||
炭酸脱水酵素阻害薬 | 炭酸脱水酵素阻害 | 近位尿細管 |
+ | ++ | - | NC | V | (+) | ++ | ++ | I | - | - | - | NC | + |
浸透圧利尿薬 | 浸透圧 | ヘンレループ |
++ | + | I | + | ++ | + | + | + | + | I | + | NC | - | I |
ループ利尿薬 | Na+-K+-2Cl- symport阻害 | 太い上行脚 |
++ | ++ | + | ++ | ++ | ++ | +(1) | +(1) | + | - | V(+) | NC | V(-) | - |
チアジド系利尿薬 | Na+-Cl-symport阻害 | 遠位尿細管 |
+ | ++ | + | V(-) | V(+) | + | +(1) | +(1) | + | - | NC | V(-) | V(-) | NC |
カリウム保持性利尿薬 | 上皮性ナトリウムチャネル阻害 | 遠位尿細管後部と集合管 |
+ | - | - | - | - | + | (+) | NC | I | - | NC | NC | NC | NC |
アルドステロン受容体拮抗 | 遠位尿細管後部と集合管 |
+ | - | - | I | - | + | (+) | I | I | - | NC | NC | NC | NC |
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