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Hydrochlorothiazide: Wikis

  

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Hydrochlorothiazide
Systematic (IUPAC) name
6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide
Identifiers
CAS number 58-93-5
ATC code C03AA03
PubChem 3639
ChemSpider 3513
Chemical data
Formula C7H8ClN3O4S2 
Mol. mass 297.74
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability Variably absorbed from GI tract
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
Therapeutic considerations
Pregnancy cat. B (D if used to treat pregnancy-induced hypertension)
Legal status Prescription only
Routes Oral (capsules, tablets, oral solution)
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Hydrochlorothiazide, abbreviated HCTZ, HCT, or HZT, is a first line 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. Hydrochlorothiazide is sold both as a generic drug and under a large number of brand names, including Apo-Hydro, Aquazide H, Dichlotride, Hydrodiuril, HydroSaluric, Microzide, Esidrex, and Oretic.

Hydrochlorothiazide is also used in combination with many popular drugs used to treat hypertension such as Diovan HCT, Zestoretic, Benicar HCT, Atacand HCT, and Lotensin HCT and others.

Contents

Mechanism of action

Hydrochlorothiazide belongs to the thiazide class of diuretics, 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. Thiazides increase the reabsorption of calcium in this segment in a manner unrelated to sodium transport. [2] increases the osmolarity in the lumen, causing less water to be reabsorbed from the collecting ducts. This leads to increased urinary output.

Indications

HCTZ is often used in the treatment of hypertension, congestive heart failure, symptomatic edema and the prevention of kidney stones. It is effective for nephrogenic diabetes insipidus and is also sometimes used for hypercalciuria, Dent's disease and Meniere's disease.

Hypokalemia, an occasional side effect, can be usually prevented by potassium supplements or by combining hydrochlorothiazide with a potassium-sparing diuretic.

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.[3]

Side effects

See also

References

  1. ^ Beermann B, Groschinsky-Grind M, Rosén A. (1976). "Absorption, metabolism, and excretion of hydrochlorothiazide". Clin Pharmacol Ther 19 (5 (Pt 1)): 531–7. 
  2. ^ Uniformed Services University Pharmacology Note Set #3 2010, Lectures #39 & #40, Eric Marks
  3. ^ Dvorak MM, De Joussineau C, Carter DH, et al. (2007). "Thiazide diuretics directly induce osteoblast differentiation and mineralized nodule formation by interacting with a sodium chloride co-transporter in bone". J. Am. Soc. Nephrol. 18 (9): 2509–16. doi:10.1681/ASN.2007030348. PMID 17656470.& PMC 2216427. http://jasn.asnjournals.org/cgi/pmidlookup?view=long&pmid=17656470. 

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