NABUMETONE tablet film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

NABUMETONE (UNII: LW0TIW155Z) (NABUMETONE - UNII:LW0TIW155Z)

Available from:

Lake Erie Medical DBA Quality Care Products LLC

INN (International Name):

NABUMETONE

Composition:

NABUMETONE 500 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

NABUMETONE - NABUMETONE TABLET, FILM COATED
LAKE ERIE MEDICAL DBA QUALITY CARE PRODUCTS LLC
----------
NABUMETONE 500 MG
DESCRIPTION
Nabumetone is a naphthylalkanone designated chemically as
4-(6-methoxy-2-naphthalenyl)-2-butanone.
It has the following structure:
nabumetone
Nabumetone is a white to off-white crystalline substance with a
molecular weight of 228.3. It is
nonacidic and practically insoluble in water, but soluble in alcohol
and most organic solvents. It has an
n-octanol:phosphate buffer partition coefficient of 2400 at pH 7.4.
Tablets for Oral Administration
Each oval-shaped, film-coated tablet contains 500 mg or 750 mg of
nabumetone. Inactive ingredients
consist of colloidal silicon dioxide, croscarmellose sodium,
hypromellose, magnesium stearate,
microcrystalline cellulose, titanium dioxide, polyethylene glycol 400,
polysorbate 80 and sodium
lauryl sulfate.
CLINICAL PHARMACOLOGY
Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) that
exhibits anti-inflammatory, analgesic
and antipyretic properties in pharmacologic studies. As with other
nonsteroidal anti-inflammatory
agents, its mode of action is not known. However, the ability to
inhibit prostaglandin synthesis may be
involved in the anti-inflammatory effect
Pharmacokinetics
After oral administration, approximately 80% of a radiolabeled dose of
nabumetone is found in the
urine, indicating that nabumetone is well absorbed from the
gastrointestinal tract. Nabumetone itself is
not detected in the plasma because, after absorption, it undergoes
rapid biotransformation to the
principal active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA).
Approximately 35% of a 1000
mg oral dose of nabumetone is converted to 6MNA and 50% is converted
into unidentified metabolites
which are subsequently excreted in the urine. Following oral
administration of nabumetone tablets,
6MNA exhibits pharmacokinetic characteristics that generally follow a
one-compartment model with
first order input and first order elimination.
6MNA is more than 99% bound to plasma