fbpx
Wikipedia

Xipamide

January 01, 1970

Xipamide is a sulfonamide diuretic drug marketed by Eli Lilly under the trade names Aquaphor (in Germany) and Aquaphoril (in Austria). It is used for the treatment of oedema and hypertension.

Xipamide
Clinical data
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
  • contraindication
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability95%
Protein binding98%
Metabolismglucuronide (30%)
Elimination half-life5.8 to 8.2 hours
Excretionkidney (1/3) and bile duct (2/3)
Identifiers
  • 4-chloro-N-(2,6-dimethylphenyl)-2-hydroxy-5-sulfamoylbenzamide
CAS Number
  • 14293-44-8 Y
PubChem CID
  • 26618
IUPHAR/BPS
  • 7900
ChemSpider
  • 24795 N
UNII
  • 4S9EY0NUEC
KEGG
  • D06341 Y
ChEMBL
  • ChEMBL517199 N
CompTox Dashboard (EPA)
  • DTXSID5023744
ECHA InfoCard100.034.727
Chemical and physical data
FormulaC15H15ClN2O4S
Molar mass354.81 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC1=C(C(=CC=C1)C)NC(=O)C2=CC(=C(C=C2O)Cl)S(=O)(=O)N
  • InChI=1S/C15H15ClN2O4S/c1-8-4-3-5-9(2)14(8)18-15(20)10-6-13(23(17,21)22)11(16)7-12(10)19/h3-7,19H,1-2H3,(H,18,20)(H2,17,21,22) N
  • Key:MTZBBNMLMNBNJL-UHFFFAOYSA-N N
 NY (what is this?)  (verify)

Mechanism of action edit

Like the structurally related thiazide diuretics, xipamide acts on the kidneys to reduce sodium reabsorption in the distal convoluted tubule. This increases the osmolarity in the lumen, causing less water to be reabsorbed by the collecting ducts. This leads to increased urinary output. Unlike the thiazides, xipamide reaches its target from the peritubular side (blood side).[1]

Additionally, it increases the secretion of potassium in the distal tubule and collecting ducts. In high doses it also inhibits the enzyme carbonic anhydrase which leads to increased secretion of bicarbonate and alkalizes the urine.

Unlike with thiazides, only terminal kidney failure renders xipamide ineffective.[2]

Uses edit

Xipamide is used for[1][2]

Pharmacokinetics edit

After oral administration, 20 mg of xipamide are resorbed quickly and reach the peak plasma concentration of 3 mg/L within an hour. The diuretic effect starts about an hour after administration, reaches its peak between the third and sixth hour, and lasts for nearly 24 hours.

One third of the dose is glucuronidized, the rest is excreted directly through the kidney (1/3) and the faeces (2/3). The total plasma clearance is 30-40 mL/min. Xipamide can be filtrated by haemodialysis but not by peritoneal dialysis.[2]

Dosage edit

Initially 40 mg, it can be reduced to 10–20 mg to prevent a relapse.[2]

The lowest effective dose is 5 mg. More than 60 mg have no additional effects.[1]

Adverse effects edit

Contraindications edit

Interactions edit

Not recommended combinations edit

  • Xipamide lowers the renal clearance of lithium which can lead to lithium intoxication.[1] (This interaction is classified as medium.[3])

Combinations requiring special precautions edit

The product information requests special precautions for these combinations:[1]

Interactions not included in the product information edit

Banned use in sport edit

On 17 July 2012, cyclist Fränk Schleck was removed from the Tour de France by his team RadioShack-Nissan after his A-sample returned traces of xipamide.[4]

References edit

  1. ^ a b c d e f g Jasek W, ed. (2007). Austria-Codex (in German). Vol. 1 (2007/2008 ed.). Vienna: Österreichischer Apothekerverlag. pp. 600–603. ISBN 978-3-85200-181-4.
  2. ^ a b c d e Dinnendahl V, Fricke U, eds. (2007). Arzneistoff-Profile (in German). Vol. 10 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.
  3. ^ a b c d e Klopp T, ed. (2007). Arzneimittel-Interaktionen (in German) (2007/2008 ed.). Arbeitsgemeinschaft für Pharmazeutische Information. ISBN 978-3-85200-184-5.
  4. ^ Williams R (17 July 2012). "Frank Schleck tests positive for banned diuretic and is out of Tour". The Guardian. London. Retrieved 2012-07-18.

January 01, 1970
xipamide, sulfonamide, diuretic, drug, marketed, lilly, under, trade, names, aquaphor, germany, aquaphoril, austria, used, treatment, oedema, hypertension, clinical, dataahfs, drugs, cominternational, drug, namespregnancycategorycontraindicationroutes, ofadmin. Xipamide is a sulfonamide diuretic drug marketed by Eli Lilly under the trade names Aquaphor in Germany and Aquaphoril in Austria It is used for the treatment of oedema and hypertension XipamideClinical dataAHFS Drugs comInternational Drug NamesPregnancycategorycontraindicationRoutes ofadministrationBy mouthATC codeC03BA10 WHO Legal statusLegal statusIn general Prescription only Pharmacokinetic dataBioavailability95 Protein binding98 Metabolismglucuronide 30 Elimination half life5 8 to 8 2 hoursExcretionkidney 1 3 and bile duct 2 3 IdentifiersIUPAC name 4 chloro N 2 6 dimethylphenyl 2 hydroxy 5 sulfamoylbenzamideCAS Number14293 44 8 YPubChem CID26618IUPHAR BPS7900ChemSpider24795 NUNII4S9EY0NUECKEGGD06341 YChEMBLChEMBL517199 NCompTox Dashboard EPA DTXSID5023744ECHA InfoCard100 034 727Chemical and physical dataFormulaC 15H 15Cl N 2O 4SMolar mass354 81 g mol 13D model JSmol Interactive imageSMILES CC1 C C CC C1 C NC O C2 CC C C C2O Cl S O O NInChI InChI 1S C15H15ClN2O4S c1 8 4 3 5 9 2 14 8 18 15 20 10 6 13 23 17 21 22 11 16 7 12 10 19 h3 7 19H 1 2H3 H 18 20 H2 17 21 22 NKey MTZBBNMLMNBNJL UHFFFAOYSA N N N Y what is this verify Contents 1 Mechanism of action 2 Uses 3 Pharmacokinetics 4 Dosage 5 Adverse effects 6 Contraindications 7 Interactions 7 1 Not recommended combinations 7 2 Combinations requiring special precautions 7 3 Interactions not included in the product information 8 Banned use in sport 9 ReferencesMechanism of action editLike the structurally related thiazide diuretics xipamide acts on the kidneys to reduce sodium reabsorption in the distal convoluted tubule This increases the osmolarity in the lumen causing less water to be reabsorbed by the collecting ducts This leads to increased urinary output Unlike the thiazides xipamide reaches its target from the peritubular side blood side 1 Additionally it increases the secretion of potassium in the distal tubule and collecting ducts In high doses it also inhibits the enzyme carbonic anhydrase which leads to increased secretion of bicarbonate and alkalizes the urine Unlike with thiazides only terminal kidney failure renders xipamide ineffective 2 Uses editXipamide is used for 1 2 cardiac oedema caused by decompensation of heart failure renal oedema chronic renal disease but not with anuria hepatic oedema caused by cirrhosis ascites lymphoedema hypertension in combination with chronic renal diseasePharmacokinetics editAfter oral administration 20 mg of xipamide are resorbed quickly and reach the peak plasma concentration of 3 mg L within an hour The diuretic effect starts about an hour after administration reaches its peak between the third and sixth hour and lasts for nearly 24 hours One third of the dose is glucuronidized the rest is excreted directly through the kidney 1 3 and the faeces 2 3 The total plasma clearance is 30 40 mL min Xipamide can be filtrated by haemodialysis but not by peritoneal dialysis 2 Dosage editInitially 40 mg it can be reduced to 10 20 mg to prevent a relapse 2 The lowest effective dose is 5 mg More than 60 mg have no additional effects 1 Adverse effects editmore than 1 10 of all patients 1 hypokalaemia which can lead to nausea muscular weakness or cramps and ECG abnormities 1 100 to 1 10 hyponatraemia which can lead to headache nausea drowsiness or confusion orthostatic hypotension initially increase of urea uric acid and creatinine which can lead to a gout attack in predisposed patients 1 1000 to 1 10 000 allergic reactions of the skin hyperlipidaemia less than 1 10 000 haemorrhagic pancreatitis acute interstitial nephritis thrombocytopenia leucopeniaContraindications editanuria praecoma and coma hepaticum hypovolemia hyponatremia hypokalemia hypercalcemia gout sulfonamide hypersensitivity pregnancy lactation period 1 2 Interactions editNot recommended combinations edit Xipamide lowers the renal clearance of lithium which can lead to lithium intoxication 1 This interaction is classified as medium 3 Combinations requiring special precautions edit The product information requests special precautions for these combinations 1 The antihypertensive effect can be increased by ACE inhibitors barbiturates phenothiazines tricyclic antidepressants alcohol etc Classified as minor 3 NSAIDs can reduce the antihypertensive and diuretic effects Xipamide increases the neurotoxicity of high doses of salicylates Classified as minor 3 Toxicity of cardiac glycosides is increased due to hypokalemia and hypomagnesemia Classified as minor 3 Antiarrhythmic agents classes Ia and III phenothiazines and other antipsychotics increase the risk of torsades de pointes due to hypokalemia Interactions not included in the product information edit Xipamide can reduce the effect of antidiabetics Classified as minor 3 Banned use in sport editOn 17 July 2012 cyclist Frank Schleck was removed from the Tour de France by his team RadioShack Nissan after his A sample returned traces of xipamide 4 References edit a b c d e f g Jasek W ed 2007 Austria Codex in German Vol 1 2007 2008 ed Vienna Osterreichischer Apothekerverlag pp 600 603 ISBN 978 3 85200 181 4 a b c d e Dinnendahl V Fricke U eds 2007 Arzneistoff Profile in German Vol 10 21 ed Eschborn Germany Govi Pharmazeutischer Verlag ISBN 978 3 7741 9846 3 a b c d e Klopp T ed 2007 Arzneimittel Interaktionen in German 2007 2008 ed Arbeitsgemeinschaft fur Pharmazeutische Information ISBN 978 3 85200 184 5 Williams R 17 July 2012 Frank Schleck tests positive for banned diuretic and is out of Tour The Guardian London Retrieved 2012 07 18 Retrieved from https en wikipedia org w index php title Xipamide amp oldid 1190944982, wikipedia, wiki, book, books, library,

article

, read, download, free, free download, mp3, video, mp4, 3gp, jpg, jpeg, gif, png, picture, music, song, movie, book, game, games.