Metolazone
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| Clinical data | |
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| Trade names | Zaroxolyn |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682345 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | ~65% |
| Metabolism | kidney (minimal) |
| Biological half-life | 14 hours |
| Excretion | primarily urine |
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| ECHA InfoCard | 100.037.748 |
| Chemical and physical data | |
| Formula | C16H16ClN3O3S |
| Molar mass | 365.835 g/mol |
| 3D model (Jmol) | |
| Melting point | 260 °C (500 °F) |
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Metolazone is a thiazide-like diuretic marketed under the brand names Zytanix from Zydus Cadila, Zaroxolyn, and Mykrox. It is primarily used to treat congestive heart failure and high blood pressure. Metolazone indirectly decreases the amount of water reabsorbed into the bloodstream by the kidney, so that blood volume decreases and urine volume increases. This lowers blood pressure and prevents excess fluid accumulation in heart failure. Metolazone is sometimes used together with loop diuretics such as furosemide or bumetanide, but these highly effective combinations can lead to dehydration and electrolyte abnormalities.
Metolazone was developed in the 1970s. Its creator, Indian born chemist Dr. Bola Vithal Shetty has been active in helping the U.S. Food and Drug Administration review drug applications, and in the development of new medicines. Metolazone quickly gained popularity due to its lower renal toxicity compared to other diuretics (especially thiazides) in patients with renal insufficiency.
Metolazone is a quinazoline, a derivative of the similar diuretic quinethazone, as well as a sulfonamide. It is related to analogs of 1,2,4-benzothiadizine-1,1-dioxide (benzothiadiazine). These drugs are called benzothiadiazides, or thiazides for short. Chemically, metolazone is not a substituted benzothiadiazine, and therefore is not technically a thiazide. However, since metolazone, as well as other drugs like indapamide, act on the same target as thiazides and behave in a similar pharmacologic fashion, they are considered "thiazide-like diuretics". Therefore, they are often included in the thiazide diuretics despite not being thiazides themselves.
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