METOLAZONE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

metolazone (UNII: TZ7V40X7VX) (metolazone - UNII:TZ7V40X7VX)

Available from:

Upstate Pharma, LLC

INN (International Name):

metolazone

Composition:

metolazone 2.5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Upstate's metolazone tablets, USP, are indicated for the treatment of salt and water retention including: - edema accompanying congestive heart failure; - edema accompanying renal diseases, including the nephrotic syndrome and states of diminished renal function. Metolazone tablets, USP, are also indicated for the treatment of hypertension, alone or in combination with other antihypertensive drugs of a different class. MYKROX Tablets, a more rapidly available form of metolazone, are intended for the treatment of new patients with mild to moderate hypertension. A dose titration is necessary if MYKROX Tablets are to be substituted for Upstate's metolazone tablets, USP, in the treatment of hypertension. See package circular for MYKROX Tablets (UCB). The routine use of diuretics in an otherwise healthy woman is inappropriate and exposes mother and fetus to unnecessary hazard. Diuretics do not prevent development of toxemia of pregnancy, and there is no evidence that they are useful in the treatment of developed t

Product summary:

Upstate's metolazone tablets, USP, are shallow biconvex, round tablets, and are available in three strengths: 2½ mg, pink, debossed "643" on one side, and "2½" on reverse side. 5 mg, blue, debossed "644" on one side, and "5" on reverse side. 10 mg, yellow, debossed "645" on one side, and "10" on reverse side. Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [See USP Controlled Room Temperature]. Protect from light. Keep out of the reach of children. For more information about Metolazone Tablets, USP call 1-844-599-CARE (2273).

Authorization status:

New Drug Application Authorized Generic

Summary of Product characteristics

METOLAZONE- METOLAZONE TABLET
UPSTATE PHARMA, LLC
----------
METOLAZONE TABLETS, USP
Rx Only
DO NOT INTERCHANGE
DO NOT INTERCHANGE UPSTATE'S METOLAZONE TABLETS, USP, ZAROXOLYN®
TABLETS, AND OTHER FORMULATIONS OF METOLAZONE THAT SHARE THEIR
SLOW AND INCOMPLETE BIOAVAILABILITY AND ARE NOT THERAPEUTICALLY
EQUIVALENT AT THE SAME DOSES TO MYKROX® TABLETS, A MORE RAPIDLY
AVAILABLE AND COMPLETELY BIOAVAILABLE METOLAZONE PRODUCT.
FORMULATIONS BIOEQUIVALENT TO ZAROXOLYN AND FORMULATIONS
BIOEQUIVALENT TO MYKROX SHOULD NOT BE INTERCHANGED FOR ONE
ANOTHER.
DESCRIPTION
Upstate's metolazone tablets, USP, for oral administration contain
2½, 5, or 10 mg of metolazone, USP, a
diuretic/saluretic/antihypertensive drug of the quinazoline class.
Metolazone has the molecular formula C
H ClN O S, the chemical name 7-chloro-1, 2, 3, 4-
tetrahydro-2-methyl-3-(2-methylphenyl)-4-oxo-6-quinazolinesulfonamide,
and a molecular weight of
365.83. The structural formula is:
Metolazone is only sparingly soluble in water, but more soluble in
plasma, blood, alkali, and organic
solvents.
Inactive Ingredients: Magnesium stearate, microcrystalline cellulose
and dye: 2½ mg-D&C Red No. 33;
5 mg-FD&C Blue No. 2; 10 mg-D&C Yellow No. 10 and FD&C Yellow No. 6.
CLINICAL PHARMACOLOGY
Metolazone is a quinazoline diuretic, with properties generally
similar to the thiazide diuretics. 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 delivery of sodium to
the distal tubular exchange site
results in increased potassium excretion. Metolazone does not inhibit
carbonic anhydrase. 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 severe