Xipamide
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AHFS/Drugs.com | International Drug Names |
Pregnancy category |
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Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Bioavailability | 95% |
Protein binding | 98% |
Metabolism | glucuronide (30%) |
Elimination half-life | 5.8 to 8.2 hours |
Excretion | kidney (1/3) and bile duct (2/3) |
Identifiers | |
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JSmol) | |
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Xipamide is a sulfonamide
Mechanism of action
Like the structurally related
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
- cardiac oedema caused by decompensation of heart failure
- chronic renal disease (but not with anuria)
- hepatic oedema caused by cirrhosis
- ascites
- lymphoedema
- hypertension in combination with chronic renal disease
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 its peak between the third and sixth hour, and lasts for nearly 24 hours.
One third of the dose is
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
- more than 1/10 of all patients[1]
- ECGabnormities
- 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
- leucopenia
Contraindications
- anuria
- praecoma and coma hepaticum
- hypovolemia, hyponatremia, hypokalemia
- hypercalcemia
- gout
- sulfonamide hypersensitivity
- pregnancy, lactation period[1][2]
Interactions
Not recommended combinations
- Xipamide lowers the renal clearance of )
Combinations requiring special precautions
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 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
- Xipamide can reduce the effect of antidiabetics. (Classified as minor.[3])
Banned use in sport
On 17 July 2012, cyclist
References
- ^ ISBN 978-3-85200-181-4.
- ^ ISBN 978-3-7741-9846-3.
- ^ 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.