関: Thiazide diuretics

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diuretic drug (trade name Naqua) used to treat hypertension (同)Naqua

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/04/16 02:58:44」(JST)

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Trichlormethiazide (INN, currently being sold under the brand names of Achletin, Diu-Hydrin and Triflumen) is a diuretic with properties similar to those of hydrochlorothiazide.^[1] It is usually administered for the treatment of oedema (including that which is associated with heart failure, hepatic cirrhosis and corticosteroid therapy) and hypertension.^[1] In veterinary medicine, trichlormethiazide can be combined with dexamethasone to be used on horses with mild swelling of distal limbs and general bruising.^[2]

As a diuretic (in particular a thiazide), trichlormethiazide encourages water loss from the body.^[1] Trichlormethiazide works by inhibiting Na⁺/Cl⁻ ion reabsorption from the distal tubules of the kidneys.^[1] In addition, trichlormethiazide increases the excretion of potassium.^[1]

Mechanism

Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle. This results in excretion of sodium, chloride and water, and thus acts as a diuretic.^[1] Although trichlormethiazide is used to treat

Synthesis

Trichlormethiazide is 1,1-dioxide 3,4-dihydro-3-(dichlormethyl)-6-chloro-2H-1,2,4-benzothiadiazin-7-sulfonamide.

Trichlormethiazide synthesis:^[3]^[4]^[5]^[6]^[7]^[8]

Synonyms of this drug are esmarin, esmalorid, anatran, carvacron, intromene, sanamirone, methahydrin, naqua, triazide, and others.

References

^ ^a ^b ^c ^d ^e ^f "DrugBank: DB01021 (Trichlormethiazide)". DrugBank. Retrieved 2008-01-23.
^ "Trichlormethiazide and Dexamethasone for veterinary use". Wedgewood Pharmacy. Retrieved 2008-01-24.
^ Scherico Ltd., Br. GB 949373 (1960).
^ G. de Stevens, L.H. Werner, Ger. DE 1147233 (1960).
^ De Stevens, G; Werner, L. H.; Barrett, W. E.; Chart, J. J.; Renzi, A. H. (1960). "The chemistry and pharmacology of hydrotrichlorothiazide". Experientia 16: 113–4. doi:10.1007/bf02158094. PMID 13815073.
^ M.H. Sherlock, N. Sperber, J. Topliss, Experientia, 16, 184 (1960).
^ Scherico Ltd., GB 954023 (1960).
^ W.J. Close, U.S. Patent 3,264,292 (1960).

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1. 原発性（本態性）高血圧患者におけるサイアザイド系利尿薬の使用 use of thiazide diuretics in patients with primary essential hypertension
2. 利尿剤の作用機序 mechanism of action of diuretics
3. 高血圧治療におけるサイアザイド系利尿剤とループ利尿剤の比較 thiazides versus loop diuretics in treatment of hypertension
4. 原発性（本態性）高血圧における薬物療法の選択：推奨 choice of drug therapy in primary essential hypertension recommendations
5. ループ利尿剤およびサイアザイド系利尿剤によって誘発された電解質の合併症の経過 time course of loop and thiazide diuretic induced electrolyte complications

English Journal

A novel compound heterozygous mutation of Gitelman's syndrome in Japan, as diagnosed by an extraordinary response of the fractional excretion rate of chloride in the trichlormethiazide loading test.

Ueda K, Makita N, Kawarazaki H, Fujiwara T, Unuma S, Monkawa T, Hayashi M, Fujita T.SourceDepartment of Nephrology and Endocrinology, University of Tokyo School of Medicine, Japan. koueda-tky@umin.net
Internal medicine (Tokyo, Japan).Intern Med.2012;51(12):1549-53. Epub 2012 Jun 15.
Gitelman's syndrome (GS), an inherited disorder due to loss of function of ion channels and transporters such as Na-Cl co-transporter (NCCT) in distal convoluted tubules, is characterized by hypokalemia, hypomagnesemia, hypocalciuria, metabolic alkalosis and hyperreninemic-hyperaldosteronism. A 39-y
PMID 22728489

Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments.

Watanabe T, Kusuhara H, Watanabe T, Debori Y, Maeda K, Kondo T, Nakayama H, Horita S, Ogilvie BW, Parkinson A, Hu Z, Sugiyama Y.SourceLaboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2011 Jun;39(6):1031-8. Epub 2011 Mar 7.
The present study investigated prediction of the overall renal tubular secretion and hepatic clearances of anionic drugs based on in vitro transport studies. The saturable uptake of eight drugs, most of which were OAT3 substrates (rosuvastatin, pravastatin, pitavastatin, valsartan, olmesartan, trich
PMID 21383204

Japanese Journal

Effect of Pharmaceutical Excipients on the Stability of Trichlormethiazide Tablets under Humid Conditions

Teraoka Reiko,Matsushima Yuki,Sugimoto Isao,Inoue Kana,Morita Shin-ya,Kitagawa Shuji
CHEMICAL & PHARMACEUTICAL BULLETIN 57(12), 1343-1347, 2009
… The stability of trichlormethiazide (TCM) and the drug in the nine products available on the market (the original tablet (B) and 8 generic tablets (G1—G8)) were investigated under humid conditions. …
NAID 130000124532

臨牀研究 furosemide抵抗性浮腫を呈する糖尿病腎症に対するtrichlormethiazideの有用性

志和亜華,水木一仁,河村智一
臨牀と研究 85(6), 934-938, 2008-06
NAID 40016118978

「チアジド系利尿薬」

Trichlormethiazide
Systematic (IUPAC) name
	6-Chloro-3-(dichloromethyl)-1,1-dioxo-3,4-dihydro-2H-benzo[e] [1,2,4]thiadiazine-7-sulfonamide
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	B (D if used to treat pregnancy-induced hypertension);
Routes of; administration	Oral (capsules, tablets, oral solution)
Legal status
Legal status	℞ (Prescription only);
Pharmacokinetic data
Bioavailability	Variably absorbed from GI tract
Excretion	Primarily excreted unchanged in urine
Identifiers
CAS Number	133-67-5
ATC code	C03AA03 (WHO)
PubChem	CID 5560
IUPHAR/BPS	7314
DrugBank	DB01021
ChemSpider	5359
UNII	Q58C92TUN0
KEGG	D00658
ChEMBL	CHEMBL1054
Chemical data
Formula	C8H8Cl3N3O4S2
Molar mass	380.6558 g/mol
(what is this?) (verify)

　　[★]

英: thiazide diuretic, benzothiazide diuretic
同: サイアザイド系利尿薬
関: 利尿薬、利尿薬の作用部位、sodium-chloride symporter inhibitor。ギテルマン症候群

特徴

安価である
有効率が高い
遠位尿細管前半部に作用するらしい
Na⁺とCl^-の共輸送体(NCCT)を阻害→Na⁺,Cl^- の再吸収を阻害する

排泄される電解質の変化

Na↑、K↑、H↑、Ca↓、Mg↑、Cl↑、HCO₃↑、H₂PO₄↑

Ca↓

チアジド系利尿薬の慢性使用により体液量が減少し、近位尿細管での再吸収が亢進するため (GOO.755)　？？

チアジド系利尿薬自体のDCTでの作用による；NCCTを阻害すると細胞内のNa濃度低下、これにより側底膜でのNa⁺-Ca²⁺交換系が亢進することでCa²⁺の再吸収↑ (GOO.755)　→　つまり管腔側から受動的に引き込まれるということ。

K↑、滴定酸↑

ループ利尿薬と同様の機序による (GOO.755)