Hydrochlorothiazide

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Hydrochlorothiazide
Systematic (IUPAC) name
6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide
Clinical data
Trade namesApo-hydro, Aquazide h, Dichlotride among others, Oretic
AHFS/Drugs.commonograph
MedlinePlusa682571
Pregnancy cat.B (D if used to treat pregnancy-induced hypertension)
Legal status Prescription only
RoutesOral (capsules, tablets, oral solution)
Pharmacokinetic data
BioavailabilityVariably absorbed from GI tract. Bioavailability ~ 70%
Metabolismdoes not undergo significant metabolism (>95% excreted unchanged in urine)[1]
Half-life5.6–14.8 h
ExcretionPrimarily excreted unchanged in urine
Identifiers
CAS number58-93-5 YesY
ATC codeC03AA03
PubChemCID 3639
DrugBankDB00999
ChemSpider3513 YesY
UNII0J48LPH2TH YesY
KEGGD00340 YesY
ChEMBLCHEMBL435 YesY
Chemical data
FormulaC7H8ClN3O4S2 
Mol. mass297.74
 YesY (what is this?)  (verify)
 
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Hydrochlorothiazide
Systematic (IUPAC) name
6-chloro-1,1-dioxo-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide
Clinical data
Trade namesApo-hydro, Aquazide h, Dichlotride among others, Oretic
AHFS/Drugs.commonograph
MedlinePlusa682571
Pregnancy cat.B (D if used to treat pregnancy-induced hypertension)
Legal status Prescription only
RoutesOral (capsules, tablets, oral solution)
Pharmacokinetic data
BioavailabilityVariably absorbed from GI tract. Bioavailability ~ 70%
Metabolismdoes not undergo significant metabolism (>95% excreted unchanged in urine)[1]
Half-life5.6–14.8 h
ExcretionPrimarily excreted unchanged in urine
Identifiers
CAS number58-93-5 YesY
ATC codeC03AA03
PubChemCID 3639
DrugBankDB00999
ChemSpider3513 YesY
UNII0J48LPH2TH YesY
KEGGD00340 YesY
ChEMBLCHEMBL435 YesY
Chemical data
FormulaC7H8ClN3O4S2 
Mol. mass297.74
 YesY (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]

Medical uses[edit]

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.[3]

It is also sometimes used for treatment of hypoparathyroidism,[4] 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.[5]

It is frequently given together with other antihypertensive agents in fixed combination preparations, such as losartan (an angiotensin II receptor antagonist) as hydrochlorothiazide/losartan (Hyzaar in the US).

Adverse effects[edit]

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.[6]

Mechanism of action[edit]

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.[7] Additionally, by other mechanisms, HCTZ is believed to lower peripheral vascular resistance.[8]

Brand names[edit]

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 popular drugs used to treat hypertension such as Diovan HCT, Zestoretic, Ziac, Benicar HCT, Olmy-H, Atacand HCT, and Lotensin HCT, Temax-H and others.

Prohibited use in sport[edit]

Hydrochlorothiazide was detected in the urine of the Russian cyclist Alexandr Kolobnev during the 2011 Tour de France.[9] Kolobnev was the only cyclist to leave the 2011 race in connection with adverse findings at a doping control.[10] 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.[11][12]

See also[edit]

References[edit]

  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. ^ Duarte JD, Cooper-DeHoff RM (June 2010). "Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics". Expert Rev Cardiovasc Ther 8 (6): 793–802. doi:10.1586/erc.10.27. PMC 2904515. PMID 20528637. 
  3. ^ "Hydrochlorothiazide". The American Society of Health-System Pharmacists. Retrieved 3 April 2011. 
  4. ^ Mitchell, Deborah. "Long-Term Follow-Up of Patients with Hypoparathyroidism". J Clin Endocrin Metab. Endocrine Society. Retrieved 19 June 2013. 
  5. ^ Dvorak MM, De Joussineau C, Carter DH et al. (2007). "Thiazide diuretics directly induce osteoblast differentiation and mineralized nodule formation by targeting a NaCl cotransporter in bone". J. Am. Soc. Nephrol. 18 (9): 2509–16. doi:10.1681/ASN.2007030348. PMC 2216427. PMID 17656470. 
  6. ^ Johnson, KK; Green, DL, Rife, JP, Limon, L (February 2005). "Sulfonamide cross-reactivity: fact or fiction?". The Annals of pharmacotherapy 39 (2): 290–301. doi:10.1345/aph.1E350. PMID 15644481. 
  7. ^ Uniformed Services University Pharmacology Note Set #3 2010, Lectures #39 & #40, Eric Marks
  8. ^
    Benazepril hydrochloride 20 mg / Hydrochlorothiazide 25 mg oral tablet

    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

  9. ^ "Tour de France: Alexandr Kolobnev positive for banned diuretic". Velonation. 2011-07-11. Archived from the original on 2011-07-12. Retrieved 2011-07-12. 
  10. ^ "Kolobnev denies knowledge of doping product, says not fired by Katusha". Velonation. 2011-07-12. Archived from the original on 2011-07-12. Retrieved 2011-07-12. 
  11. ^ "Press release: Adverse Analytical Finding for Kolobnev". Union Cycliste Internationale. 2011-07-11. Archived from the original on 2011-07-12. Retrieved 2011-07-12. 
  12. ^ "Kolobnev Tour de France's first doping case". Cycling News (Bath, UK: Future Publishing Limited). 2011-07-11. Archived from the original on 2011-07-12. Retrieved 2011-07-12. 

External links[edit]