TRIMETHOPRIM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TRIMETHOPRIM (UNII: AN164J8Y0X) (TRIMETHOPRIM - UNII:AN164J8Y0X)

Available from:

Actavis Pharma, Inc.

INN (International Name):

TRIMETHOPRIM

Composition:

TRIMETHOPRIM 100 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TRIMETHOPRIM- TRIMETHOPRIM TABLET
ACTAVIS PHARMA, INC.
REFERENCE LABEL SET ID: A4E9183F-D0EB-4BA7-9204-760B1FD62010
----------
TRIMETHOPRIM TABLETS, USP
RX ONLY
To reduce the development of drug resistant bacteria and maintain the
effectiveness of trimethoprim
tablets, USP and other antibacterial drugs, trimethoprim tablets, USP
should be used only to treat or
prevent infections that are proven or strongly suspected to be caused
by bacteria.
DESCRIPTION
Trimethoprim is a synthetic antibacterial available as 100 mg tablets
for oral administration.
Trimethoprim is 5-[(3,4,5-trimethoxyphenyl)
methyl]-2,4-pyrimidinediamine. It is a white to cream
colored, odorless, bitter compound. The structural formula is
represented below:
C
H N O
M.W. 290.32
Trimethoprim tablets, USP, 100 mg contain the following inactive
ingredients: anhydrous lactose,
colloidal silicon dioxide, magnesium stearate, sodium lauryl sulfate,
sodium starch glycolate and
stearic acid.
CLINICAL PHARMACOLOGY
Trimethoprim is rapidly absorbed following oral administration. It
exists in the blood as unbound,
protein-bound, and metabolized forms. Ten to twenty percent of
trimethoprim is metabolized, primarily
in the liver; the remainder is excreted unchanged in the urine. The
principal metabolites of trimethoprim
are the 1- and 3-oxides and the 3 - and 4 -hydroxy derivatives. The
free form is considered to be the
therapeutically active form. Approximately 44% of trimethoprim is
bound to plasma proteins.
Mean peak serum concentrations of approximately 1 mcg/mL occur 1 to 4
hours after oral administration
of a single 100 mg dose. A single 200 mg dose will result in serum
levels approximately twice as high.
The half-life of trimethoprim ranges from 8 to 10 hours. However,
patients with severely impaired
renal function exhibit an increase in the half-life of trimethoprim,
which requires either dosage regimen
adjustment or not using the drug in such patients (see DOSAGEAND
ADMINISTRATION). During a
13 week study of trimethoprim administered at a daily dosage of