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PubChem
Name: Metolazone
PubChem Compound ID: 11957638
Description: A quinazoline-sulfonamide that is considered a thiazide-like diuretic which is long-acting so useful in chronic RENAL FAILURE. It also tends to lower BLOOD PRESSURE and increase POTASSIUM loss.
Molecular formula: C16H16ClN3O3S
Molecular weight: 365.835 g/mol
Synonyms:
EU-0100833
DrugBank
Identification
Name: Metolazone
Name (isomeric): DB00524
Drug Type: small molecule
Description: A quinazoline-sulfonamide that is considered a thiazide-like diuretic which is long-acting so useful in chronic RENAL FAILURE. It also tends to lower BLOOD PRESSURE and increase POTASSIUM loss.
Synonyms:
Metolazona [INN-Spanish]; Metolazonum [INN-Latin]
Brand: Diulo, Zaroxolyn, Mykrox, Metalozone, Microx, Metalazone, Oldren, Metenix, Xuret
Category: Diuretics, Sulfamyl, Diuretics, Antihypertensive Agents
CAS number: 17560-51-9
Pharmacology
Indication: For the treatment of hypertension, alone or in combination with other antihypertensive drugs of a different class.
Pharmacology:
Metolazone is a quinazoline diuretic, with properties generally similar to the thiazide diuretics. A proximal action of metolazone has been shown in humans by increased excretion of phosphate and magnesium ions and by a markedly increased fractional excretion of sodium in patients with severely compromised glomerular filtration. This action has bee...
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Mechanism of Action:
The actions of metolazone result from interference with the renal tubular mechanism of electrolyte reabsorption. Metolazone acts primarily to inhibit sodium reabsorption at the cortical diluting site and to a lesser extent in the proximal convoluted tubule. Sodium and chloride ions are excreted in approximately equivalent amounts. The increased del...
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Absorption: Peak blood levels are obtained within 2 to 4 hours of oral administration. The rate and extent of absorption are formulation dependent.
Protein binding: 50-70% bound to erythrocytes, up to 33% bound to plasma proteins, 2-5% of the drug in circulation is unbound
Biotransformation: Not substantially metabolized. 70-95% is excreted unchanged in urine via glomerular filtration and active tubular secretion. Undergoes enterohepatic recycling.
Route of elimination: Most of the drug is excreted in the unconverted form in the urine.
Half Life: Approximately 14 hours.
Toxicity: Symptoms of overdose include difficulty breathing, dizziness, dizziness on standing up, drowsiness, fainting, irritation of the stomach and intestines, and lethargy leading to coma.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food to reduce gastric irritation.
Drug interaction:
DigitoxinPossible electrolyte variations and arrhythmias
DeslanosidePossible electrolyte variations and arrhythmias
DofetilideIncreased risk of cardiotoxicity and arrhythmias
LithiumThe thiazide diuretic, metolazone, may increase serum levels of lithium.
DigoxinPossible electrolyte variations and arrhythmias
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Targets