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Metolazone information from DrugsUpdate  

See Available Brands of Metolazone in India

P - Contraindicated in pregnancy
L - Caution when used during lactation
FI - Food *

Metolazone is a thiazide diuretic (or, rather, a thiazide-like diuretic because it acts similarly to the thiazides but does not contain the benzothiadiazine molecular structure) marketed under the brand names 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.

Pharmacodynamics

Pharmacokinetics

Metolazone is a thiazide-like diuretic. It inhibits reabsorption of sodium in the distal tubules resulting in increased excretion of sodium and water, as well as potassium and hydrogen ions.

Onset
Approx 60 minutes

Duration

≤24 hours

Absorption
Incompletely absorbed from the GI tract (oral).

Distribution
Crosses the placenta and enters breast milk. Protein-binding: 95%.

Metabolism
Not metabolised to a substantial extent.

Excretion
Via urine (80-95% unchanged); via bile and some undergo enterohepatic recycling; 6-20 hours (elimination half-life).

Metolazone Indications / Metolazone Uses

Information Not Available

Metolazone Adverse Reactions / Metolazone Side Effects

Chest pain, palpitation, necrotising angiitis, orthostatic hypotension, syncope, venous thrombosis, vertigo, volume depletion; depression, dizziness, chills, drowsiness, fatigue, restlessness, headache, lightheadedness; petechiae, photosensitivity, hypersensitivity reactions; gout attacks, electrolyte disturbances; abdominal bloating, diarrhoea, abdominal pain, anorexia, constipation, epigastric distress, nausea, xerostomia, pancreatitis, vomiting; impotence; aplastic anaemia, thrombocytopenia, haemoconcentration, leukopenia; cholestatic jaundice, hepatitis; joint pain, muscle cramps, weakness, neuropathy, paraesthesia; blurred vision; increased BUN, glucosuria.

Potentially Fatal: Stevens-Johnson syndrome, toxic epidermal necrolysis.

Precautions

Information Not Available

Special Precautions

Pre-diabetes or DM; gout; SLE; hepatic and renal impairment; hypercholesterolaemia. Correct electrolyte disturbances prior to therapy. Risk of cross-sensitivity with sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides and loop diuretics. Lactation.

Other Drug Interactions

Hypotensive and nephrotoxic effects of ACE inhibitors may be enhanced. Absorption may be reduced with bile acid sequestrants. Hyperglycaemic effect may be enhanced with diazoxide. May increase serum concentration and QTc-prolonging effect of dofetilide. May reduce lithium excretion. Hypotensive effect may be increased with alcohol.

Potentially Fatal: Increased risk of nephrotoxicity with ciclosporin. Severe electrolyte disturbances may occur with furosemide.

Other Interactions

Food Interaction
Photosensitisation may occur with dong quai, St John's wort. Hypertension may be exacerbated with ephedra, yohimbe, ginseng. Antihypertensive effect may be increased with garlic. Avoid natural licorice.

Dosage

Oral
Hypertension
Adult: Initially, 1.25 mg daily, adjusted after 3-4 weeks according to response. Usual dose: 2.5-5 mg daily, either alone or with other antihypertensives. Maintenance dose: 5 mg on alternate days. Formulations with enhanced bioavailability: 0.5-1 mg daily.
Elderly: Initially, 2.5 mg/day or every other day.

Oral
Oedema
Adult: 5-10 mg daily, increased if necessary to 20 mg daily. Max: 80 mg in 24 hr.
Elderly: Initially, 2.5 mg/day or every other day.

Food(before/after)

Should be taken with food. (Take after breakfast.)

List of Contraindications

Metolazone and Pregnancy

Contraindicated in pregnancy

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

If used in pregnancy-induced hypertension.

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Metolazone and Lactation

Caution when used during lactation

Metolazone and Children

Not recommended for use in children

Metolazone and Geriatic

Clinical studies of Metolazone did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Metolazone and Other Contraindications

Anuria; hepatic coma or pre-coma. Pregnancy

Storage

Information Not Available

Lab interference

Information Not Available

Metolazone brands in India:

Diurem Lazon Mela Metadure Metolactone Metoral Metoz Zytanix

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