MEGESTROL ACETATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

MEGESTROL ACETATE (UNII: TJ2M0FR8ES) (MEGESTROL - UNII:EA6LD1M70M)

Available from:

Par Pharmaceutical, Inc.

INN (International Name):

MEGESTROL ACETATE

Composition:

MEGESTROL ACETATE 20 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Megestrol acetate tablets are indicated for the palliative treatment of advanced carcinoma of the breast or endometrium (ie, recurrent, inoperable, or metastatic disease). It should not be used in lieu of currently accepted procedures such as surgery, radiation, or chemotherapy. History of hypersensitivity to megestrol acetate or any component of the formulation.

Product summary:

Megestrol acetate tablets, 20 mg, are white, round, flat-faced, beveled-edged, bisected, debossed with “Par 289” on one side. They are supplied in bottles of 100’s (NDC #49884-289-01). Megestrol acetate tablets, 40 mg, are white, round, flat-faced, beveled-edged, bisected, debossed with “Par 290” on one side. They are supplied in bottles of 100’s (NDC #49884-290-01), 250’s (NDC #49884-290-04) and 500’s (NDC #49884-290-05). STORAGE Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature]. Protect from temperatures above 40ْC (104ْF). SPECIAL HANDLING Health Hazard Data There is no threshold limit value established by OSHA, NIOSH, or ACGIH. Exposure or “overdose” at levels approaching recommended dosing levels could result in side effects described above (see WARNINGS and ADVERSE REACTIONS). Women at risk of pregnancy should avoid such exposure. Manufactured by: PAR PHARMACEUTICAL Chestnut Ridge, N.Y. 10977

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

MEGESTROL ACETATE- MEGESTROL ACETATE TABLET
PAR PHARMACEUTICAL, INC.
----------
MEGESTROL ACETATE TABLET USP
DESCRIPTION
Megestrol acetate is a synthetic, antineoplastic and progestational
drug. Megestrol
acetate is a white, crystalline solid chemically designated as
17(alpha)-(acetyloxy)-6-
methylpregna-4,6-diene-3,20-dione. Solubility at 37°C in water is 2
mcg per mL, solubility
in plasma is 24 mcg per mL. Its molecular weight is 384.51. The
molecular formula is
C
H
O and the structural formula is represented as follows:
Megestrol acetate is supplied as tablets for oral administration
containing 20 mg and 40
mg megestrol acetate.
Megestrol acetate tablets contain the following inactive ingredients:
acacia spray dried,
colloidal silicon dioxide, corn starch, di-calcium phosphate dihydrate
powder, lactose
hydrous impalpable, magnesium stearate and pregelatinized starch.
CLINICAL PHARMACOLOGY
While the precise mechanism by which megestrol produces its
antineoplastic effects
against endometrial carcinoma is unknown at the present time,
inhibition of pituitary
gonadotropin production and resultant decrease in estrogen secretion
may be factors.
There is evidence to suggest a local effect as a result of the marked
changes brought
about by the direct instillation of progestational agents into the
endometrial cavity. The
antineoplastic action of megestrol acetate on carcinoma of the breast
is effected by
modifying the action of other steroid hormones and by exerting a
direct cytotoxic effect
on tumor cells. In metastatic cancer, hormone receptors may be present
in some
tissues but not others. The receptor mechanism is a cyclic process
whereby estrogen
produced by the ovaries enters the target cell, forms a complex with
cytoplasmic
receptor and is transported into the cell nucleus. There it induces
gene transcription and
24
32
4
leads to the alteration of normal cell functions. Pharmacologic doses
of megestrol
acetate not only decrease the number of hormone-dependent human breast
cancer
cells but also arecapable of modi