What Is Metolazone 2.5 Mg Used for
Metolazone
In Meyler's Side Effects of Drugs (Sixteenth Edition), 2016
Organs and systems
Endocrine
Diuresis can precipitate hyperosmolar non-ketotic diabetes mellitus in susceptible individuals and in one case was associated with metolazone [ 3].
Electrolyte balance
Metolazone causes a greater degree of potassium depletion than thiazides [ 4]. In order to avoid serious electrolyte disturbances when metolazone is introduced in patients taking loop diuretics, the metolazone should be given in low doses to start with in hospital, and at the same time the dosage of the loop diuretic should be reduced under careful biochemical monitoring [5,6].
Hematologic
Neutropenia [7] and aplastic anemia [8 ] are rare complications of metolazone.
Liver
Cholestatic liver disease has been attributed to metolazone [ 9].
Pancreas
Acute pancreatitis has occasionally been attributed to metolazone [ 10]. In a 58-year-old woman with severe congestive cardiac failure it was accompanied by hypercalcemia; the symptoms and laboratory abnormalities rapidly resolved on withdrawal of metolazone [11].
Immunologic
Vasculitis has occasionally been attributed to metolazone [ 12,13].
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Metolazone
Khoyi Mohammad , Westfall David , in xPharm: The Comprehensive Pharmacology Reference, 2007
Indications
| Value | Units | Prep. and Route of Admin. | Reference | Comments | |
|---|---|---|---|---|---|
| Hypertension | |||||
| Dosage | 5-20 | mg | Zaroxolyn tablets; oral | Kastrup et al (2003) | Different brands are not bioequivalent and therefore, not interchangeable. |
| Hypertension | |||||
| Dosage | 0.5-1.0 | mg | Mykrox tablets; oral | Kaplan (2002) | Different brands are not bioequivalent and therefore, not interchangeable. |
| Edema | |||||
| Dosage | 5-20 | mg | Zaroxolyn tablets; oral | Kastrup et al (2003), Kaplan (2002) | Metolazone, like other thiazides, potentiates the effect of loop diuretics. |
| Edema | |||||
| Dosage | 0.5-1.0 | mg | Mykrox tablets; oral | Kastrup et al (2003), Kaplan (2002) | Different brands are not bioequivalent and therefore, not interchangeable. Mykrox is rapidly acting and is administered at 0.5 mg, Zaroxolyn is slowly acting and is given in 2.5 or 5.0 mg tablets. |
| Edema | |||||
| Dosage | 2.5-5.0 | mg | Zaroxolyn tablets; oral | Kastrup et al (2003), Kaplan (2002) | Different brands are not bioequivalent and therefore, not interchangeable. Mykrox is rapidly acting and is administered at 0.5 mg, Zaroxolyn is slowly acting and is given in 2.5 or 5.0 mg tablets. |
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Pharmacologic Treatment of Heart Disease
RONN E. TANEL , MARK D. LEVIN , in Pediatric Cardiology, 2006
Metolazone
Indications
Metolazone is used to treat hypertension and symptoms related to fluid retention in patients with congestive heart failure and nephrotic syndrome. Metolazone appears to be particularly effective in patients with impaired renal function. Metolazone is used for refractory cases and may be synergistic with furosemide, resulting in marked diuresis, hypovolemia, and electrolyte abnormalities.
Mechanism of Action
Although metolazone does not have the same structure as the other thiazide diuretics, it increases the excretion of sodium, potassium, and water by inhibiting sodium reabsorption in the distal and proximal convoluted tubule.
Dosage
In adults, metolazone is administered orally in a dose of 2.5–5 mg every 24 hours. For children, the dose is generally 1 mg daily for toddlers and preschool-age children, 2.5 mg for school-age children, and 5 mg for adolescents and young adults.
Metabolism and Half-Life
Metolazone undergoes enterohepatic recirculation and is excreted primarily in the urine. The dose may need to be adjusted for patients with severe hepatic dysfunction or renal impairment. The drug should be used with caution in patients with elevated serum cholesterol levels. Loop diuretics may increase the effect of metolazone, whereas nonsteroidal anti-inflammatory drugs can decrease the efficacy of thiazide diuretics. The half-life of metolazone is dependent on renal function and varies between 6 and 20 hours. The drug is not dialyzable.
Adverse Effects
Side effects of metolazone include electrolyte disturbances, dizziness and orthostatic hypotension, palpitations, headache, fatigue, rash, nausea, vomiting, cough, photosensitivity, and exacerbation or activation of systemic lupus erythematosus. A risk of cross-reaction exists in patients with sulfonamide allergy because of the chemical similarities of the compounds.
Monitoring
Serum electrolytes, including potassium, sodium, chloride, and bicarbonate, should be monitored. In addition, renal function and orthostatic vital signs should be measured on a regular basis.
Pearls
Because loop diuretics may enhance the effects of metolazone, the two drugs are sometimes used together for better diuresis, especially in patients who are refractory to single-diuretic therapy. However, profound hypovolemia may occur.
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M
Carl P. Weiner MD, MBA, FACOG , Catalin Buhimschi MD , in Drugs for Pregnant and Lactating Women (Second Edition), 2009
Metolazone—(Diulo; Metenix; Mykrox; Zaroxolyn)
International Brand Name
Barolyn (Finland); Diondel (Spain); Diulo (Hong Kong, Portugal); Metenix 5 (England); Normelan (Japan); Xuret (England, Ireland)
| ▪ Drug Class | Antihypertensives; Diuretics; Thiazides |
| ▪ Indications | CHF, peripheral edema, hypertension |
| ▪ Mechanism | Inhibits resorption of sodium and chloride in the proximal convoluted tubule |
| ▪ Dosage with Qualifiers |
|
| ▪ Maternal Considerations |
|
| ▪ Fetal Considerations | There are no adequate reports or well-controlled studies in human fetuses. It is unknown whether metolazone crosses the human placenta. Rodent studies are reassuring, revealing no evidence of teratogenicity or IUGR despite the use of doses higher than those used clinically. (See Chlorothiazide.) |
| ▪ Breastfeeding Safety | There are no adequate reports or well-controlled studies in nursing women. Metolazone enters human breast milk, but the kinetics remain to be elucidated. (See Chlorothiazide.) |
| ▪ Drug Interactions |
|
| ▪ References | There are no current relevant references. (See Chlorothiazide.) |
| ▪ Summary |
|
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Six-membered Rings with Two Heteroatoms, and their Fused Carbocyclic Derivatives
G.W. Rewcastle , in Comprehensive Heterocyclic Chemistry III, 2008
8.02.12.2.4 Other activities
Quinethazone 1169 and metolazone 1170 are used medically as diuretics, and alfazosin 1171 , an α1-adrenoreceptor antagonist related to prazosin is used to improve urinary flow rate in the treatment of benign prostatic hyperplasia.
Albaconazole (UR 9825) 1172 <1998JME1869> and fluquinconazole 1173 are used as antifungals, while proquinazid 1174 has high activity against powdery mildew diseases of cereals, grape and apple <2006H(68)561>.
The ascaracide fenazaquin 1175 is active against several spider mite species, while DPC-083 (BMS 561390) 1176 is an anti-HIV reverse transcriptase inhibitor <2000JME2019>. The quinazoline 1177 has recently been identified as a lead compound for the development of selective inhibitors of lymphocyte-specific kinase (Lck) which is involved in T-cell-mediated autoimmune and inflammatory disease <2006JME5671>.
Lastly, tetrodotoxin, the Japanese puffer fish toxin, is a polyhydroxylated reduced 2-aminoquinazoline derivative that has attracted a lot of interest, and a number of asymmetric total syntheses have recently been published <2003JA8798, 2003JA11510, 2004AGE4782, 2005CRV4537>.
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A Worldwide Yearly Survey of New Data in Adverse Drug Reactions
Yekaterina Opsha , in Side Effects of Drugs Annual, 2016
Chlorothiazide
Evaluation of the effectiveness of oral metolazone versus intravenous (IV) chlorothiazide as add-on therapy to loop diuretics in hospitalized patients with ADHF and renal dysfunction is the purpose of the following retrospective cohort study which enrolled 55 patients. The primary endpoint was net urine output (UOP) at 72 h after initiation of thiazide-like diuretics. Safety endpoints included worsening renal function, hypotension, and electrolyte abnormalities. The study reported no difference in median net UOP at 72 h in those receiving metolazone (4828 mL), compared to chlorothiazide (3779 mL, p = 0.16). There was no difference in hypotension, worsening renal function, hyponatremia, or hypokalemia (p = NS for all comparisons). This study is important to consider when evaluating diuretic therapy in addition to loop diuretics considering the cost difference favoring oral metolazone [15c].
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Electrolytes and Diuretics
Christer Svensen , in Pharmacology and Physiology for Anesthesia (Second Edition), 2019
Thiazides
Hydrochlorothiazide, indapamide, and metolazone are organic acids that are both filtered and secreted and inhibit the Na +/Cl− transporter on the luminal membrane of the distal convoluted tubule. Normally, the Na+ that is brought in by the Na+/Cl− cotransporter is exchanged for K+ that returns to blood via backdiffusion. Chloride also returns to blood by such a mechanism, whereas Ca2+ returns by a Ca2+/Na+ antiporter. If the Na+/Cl− cotransporter is inhibited by thiazides, hypokalemia and alkalosis occur. Hypercalcemia can occur as the result of increased activity of the Na+/Ca2+ antiporter (Fig. 42.8).
Clinical uses of thiazides are hypertension and heart failure. Their effects are improved by Na+ restriction and attenuated by low GFR. Adverse effects are allergies, alkalosis, hypokalemia, hyperuricemia, hypovolemia, hyperglycemia, hyperlipidemia, hypercalcemia, and sexual dysfunction.
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Cardiovascular System
Mark Kester PhD , ... Kent E. Vrana PhD , in Elsevier's Integrated Review Pharmacology (Second Edition), 2012
Thiazides, Loop Diuretics, and Potassium-Sparing Drugs
Thiazides include hydrochlorothiazide, chlorthalidone, metolazone, indapamide. Examples of loop diuretics are furosemide and bumetanide. K +-sparing drugs are spironolactone, triamterene, and amiloride.
An initial strategy for managing hypertension is often to alter volumetric excess through dietary restriction of Na+. Diuretics (see Chapter 9) essentially capitalize on sodium restriction because these drugs facilitate sodium excretion. Diuretics are often included in antihypertensive treatment regimens.
In hypertension management, diuretics initially decrease blood volume by facilitating Na+ excretion, hence reducing extracellular fluid volume; however, antihypertensive effects are maintained even after excess Na+ has been diuresed. It has been speculated that high plasma sodium concentrations increase vessel rigidity; thus antihypertensive effects are maintained because low plasma sodium indirectly induces vasodilation.
According to JNC-VII, thiazide diuretics are the first-line antihypertensive for most patients. These drugs are particularly effective antihypertensives for patients of African ancestry and the elderly. Note, however, that with the exception of metolazone, thiazides are not effective at low glomerular filtration rates; therefore loop diuretics are preferred when kidney function is compromised. In addition, thiazides are often not first-line choices for diabetic patients or patients with hyperlipidemia because the drugs may exacerbate these conditions. Often, K+-sparing diuretics (amiloride and triamterene) are used in combination with thiazides to offset K+ loss.
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Diuretics and Invasive Fluid Management Strategies
Jack F. Price , in Heart Failure in the Child and Young Adult, 2018
Thiazide Diuretics
Thiazides (hydrochlorothiazide, chlorothiazide, and metolazone) are less potent than loop diuretics. Their role should be viewed as an adjunct to further augment urine output in patients already treated with a loop diuretic. They act as inhibitors of the sodium–chloride (Na +/Cl−) cotransporter in the distal convoluted tubule, inhibiting reabsorption of sodium and chloride and increasing their urinary excretion (Fig. 38.3). Oral absorption is variable, with a peak effect of chlorothiazide when given intravenously occurring in ∼30 min [13]. The duration of effect is about 6–12 h for hydrochlorothiazide and chlorothiazide. Metolazone oral absorption is also unpredictable and its duration of action is longer, generally reported to be 12–24 h. Metolazone is not structurally a thiazide but it has thiazide-like activity in the distal tubule [13]. It has a long half-life (2 days) and may be synergistic with the other thiazides [28].
Figure 38.3. Diagram demonstrates the passive sodium transport into the tubular cell via the Na+/Cl− membrane carrier and the active sodium transport out of the cell via the Na+/K+ adenosine triphosphatase (ATPase) pump; (i) thiazide diuretics block the passive sodium transport into the cell.
From M.K. Von der Vorst, J.E. Kist, A.J. van der Heijden, J. Burggraaf, Diuretics in pediatrics: current knowledge and future practice, Pediatr. Drugs 8 (2006) 245–264.Read full chapter
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Cardiovascular Pharmacology
Roman M. Sniecinski , ... Jerrold H. Levy , in Cardiothoracic Critical Care, 2007
Thiazide Diuretics.
Thiazides diuretics (e.g., chlorothiazide, hydrochlorothiazide, metolazone) inhibit sodium and chloride reabsorption in the distal nephron. Thiazide diuretics promote potassium and magnesium excretion but, unlike loop diuretics, inhibit calcium excretion. Thiazide diuretics are less potent than loop diuretics and are ineffective when the glomerular filtration rate falls below about 30 ml/min. 58 Thiazide diuretics are used in the treatment of hypertension and mild heart failure. All thiazide diuretics are administered orally except chlorothiazide, which is also available for intravenous use. Thiazide diuretics are formulated with other agents such as ACE inhibitors for the treatment of hypertension. In the cardiothoracic ICU, thiazides, particularly metolazone, are occasionally useful as cotreatment in patients who are refractory to loop diuretics. Metolazone has a long duration of action (12 to 24 hours) and is slightly more efficacious than other thiazide diuretics because it has an additional diuretic effect in the proximal nephron. Adverse effects of thiazides include excessive clinical effects (hypovolemia, hyponatremia, hypokalemia, hypochloremic metabolic alkalosis), hyperuricemia, hyperlipidemia, hyperglycemia, photosensitivity, and allergic skin rashes.
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What Is Metolazone 2.5 Mg Used for
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