Metolazone

Indications
 Oral
Hypertension
Adult: Initially, 1.25 mg daily, adjusted after 3-4 wk 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.
Contraindications
 Anuria; hepatic coma or pre-coma. Pregnancy.
Warnings / 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.
Adverse Reactions
 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.
Overdose Reactions
 Symptoms: Orthostatic hypotension, dizziness, drowsiness, syncope, haemoconcentration and haemodynamic changes due to plasma volume depletion. Management: Symptomatic and supportive.
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.
See Below for More metolazone Drug Interactions
Food Interactions
 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.
Mechanism of Actions
 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 min.
Duration: ≤24 hr.
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 hr (elimination half-life).
Administration
 Should be taken with food. (Take after breakfast.)
ATC Classification
 C03BA08 - metolazone ; Belongs to the class of low-ceiling sulfonamide diuretics.
Available As
  • Metolazone 10 mg
  • Metolazone 2.5 mg
  • Metolazone 5 mg

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