Name: | Metolazone |
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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
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Name: | Metolazone |
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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]
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Brand: | Diulo, Zaroxolyn, Mykrox, Metalozone, Microx, Metalazone, Oldren, Metenix, Xuret |
Category: | Diuretics, Sulfamyl, Diuretics, Antihypertensive Agents |
CAS number: | 17560-51-9 |
Indication: | For the treatment of hypertension, alone or in combination with other antihypertensive drugs of a different class. |
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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 |
Food interaction: |
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Drug interaction: |
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