METOLAZONE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

METOLAZONE (UNII: TZ7V40X7VX) (METOLAZONE - UNII:TZ7V40X7VX)

Available from:

Sandoz Inc

INN (International Name):

METOLAZONE

Composition:

METOLAZONE 2.5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Metolazone is 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 is 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 Zaroxolyn® tablets and other formulations of metolazone that share its slow and incomplete bioavailability, in the treatment of hypertension. 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 toxemia. Edema during pregnancy may arise from pathologic causes or from the physiologic and mechanical consequence of pregnancy. Metolazone is indicated in pregnancy when edema is due to pathologic causes, just as it is in the absence of pregnancy (see PRECAUTIONS ). Dependent edema in pregnancy resulting from restriction of venous return by the expanded uterus is properly treated through elevation of the lower extremities and use of support hose; use of diuretics to lower intravascular volume in this case is illogical and unnecessary. There is hypervolemia during normal pregnancy which is harmful to neither the fetus nor the mother (in the absence of cardiovascular disease), but which is associated with edema, including generalized edema, in the majority of pregnant women. If this edema produces discomfort, increased recumbency will often provide relief. In rare instances, this edema may cause extreme discomfort which is not relieved by rest. In these cases, a short course of diuretics may be appropriate. Anuria, hepatic coma or precoma, known allergy or hypersensitivity to metolazone.

Product summary:

Metolazone tablets, USP for oral administration are available as: 2.5 mg: Pink, shallow biconvex, modified oval tablets, debossed “E 50” on one side, plain on the other side and supplied as: NDC 0185-5050-01 bottles of 100 NDC 0185-5050-10 bottles of 1000 5 mg: Blue, shallow biconvex, modified oval tablets, debossed “E 55” on one side, plain on the other side and supplied as: NDC 0185-0055-01 bottles of 100 NDC 0185-0055-10 bottles of 1000 10 mg: Yellow, shallow biconvex, modified oval tablets, debossed “E 56” on one side, plain on the other side and supplied as: NDC 0185-5600-01 bottles of 100 NDC 0185-5600-10 bottles of 1000 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light. Dispense contents in a tight, light-resistant container as defined in the USP with a child-resistant closure. Keep out of the reach of children. Zaroxolyn® and Mykrox® are registered trademarks of UCB Manufacturing, Inc., Rochester, NY 14623. Manufactured in India by Sandoz Private Ltd., for Sandoz Inc., Princeton, NJ 08540 46316475 Rev. September 2022

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

METOLAZONE- METOLAZONE TABLET
SANDOZ INC
----------
METOLAZONE TABLETS, USP
RX ONLY
DO NOT LNTERCHANGE:
DO NOT INTERCHANGE ZAROXOLYN TABLETS AND OTHER FORMULATIONS
OF METOLAZONE THAT SHARE ITS 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
Metolazone Tablets, USP for oral administration contain 2.5 mg, 5 mg
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-4-oxo-3-_o_-tolyl-6-quinazolinesulfonamide,
and a molecular
weight of 365.84. The structural formula is:
Metolazone is only sparingly soluble in water, but more soluble in
plasma, blood, alkali,
and organic solvents.
Inactive Ingredients: colloidal silicon dioxide, magnesium stearate,
microcrystalline
cellulose and dye: 2.5 mg - D&C red No. 30 and FD&C blue No. 2; 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
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16
16
3
3
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
wit