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Xipamide
Systematic (IUPAC) name
4-chloro-N-(2,6-dimethylphenyl)-2-hydroxy-5-sulfamoylbenzamide
Identifiers
CAS number 14293-44-8
ATC code C03BA10
PubChem 26618
Chemical data
Formula C 15H15ClN2O4S 
Mol. mass 354.80 g/mol
Pharmacokinetic data
Bioavailability 95%
Protein binding 98%
Metabolism Glucuronide (30%)
Half life 5.8 to 8.2 hours
Excretion Renal (1/3) and biliary (2/3)
Therapeutic considerations
Pregnancy cat. Contraindication
Legal status
Routes Oral

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.

Contents

Mechanism of action

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 renal failure renders xipamide ineffective.[2]

Uses

Xipamide is used for[1][2]

Pharmacokinetics

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 it speak 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

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

Contraindications

Interactions

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Not recommended combinations

  • 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

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

  • NSAIDs can reduce the antihypertensive and diuretic effects. Xipamide increases the neurotoxicity of high doses of salicylates. (Classified as minor.[3 ])

Interactions not included in the product information

References

  1. ^ a b c d e f g Jasek, W, ed (2007) (in German). Austria-Codex. 1 (2007/2008 ed.). Vienna: Österreichischer Apothekerverlag. pp. 600–603. ISBN 3-85200-181-4.  
  2. ^ a b c d e Dinnendahl, V, Fricke, U, ed (2007) (in German). Arzneistoff-Profile. 10 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.  
  3. ^ a b c d e Klopp, T, ed (2007) (in German). Arzneimittel-Interaktionen (2007/2008 ed.). Arbeitsgemeinschaft für Pharmazeutische Information. ISBN 978-3-85200-184-5.  

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