DARAPRIM pyrimethamine tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

PYRIMETHAMINE (UNII: Z3614QOX8W) (PYRIMETHAMINE - UNII:Z3614QOX8W)

Available from:

Amedra Pharmaceuticals LLC

INN (International Name):

PYRIMETHAMINE

Composition:

PYRIMETHAMINE 25 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

DARAPRIM- PYRIMETHAMINE TABLET
AMEDRA PHARMACEUTICALS LLC
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DARAPRIM
(PYRIMETHAMINE)
25-MG SCORED TABLETS
RX ONLY
PRESCRIBING INFORMATION
DESCRIPTION
DARAPRIM (pyrimethamine) is an antiparasitic compound available in
tablet form for oral
administration. Each scored tablet contains 25 mg pyrimethamine and
the inactive ingredients corn and
potato starch, lactose, and magnesium stearate.
Pyrimethamine, known chemically as
5-(4-chlorophenyl)-6-ethyl-2,4-pyrimidinediamine, has the
following structural formula:
C
H ClN
Mol. Wt. 248.71
CLINICAL PHARMACOLOGY
Pyrimethamine is well absorbed with peak levels occurring between 2 to
6 hours following
administration. It is eliminated slowly and has a plasma half-life of
approximately 96 hours.
Pyrimethamine is 87% bound to human plasma proteins.
MICROBIOLOGY: Pyrimethamine is a folic acid antagonist and the
rationale for its therapeutic action is
based on the differential requirement between host and parasite for
nucleic acid precursors involved in
growth. This activity is highly selective against plasmodia and
_Toxoplasma gondii._
Pyrimethamine possesses blood schizonticidal and some tissue
schizonticidal activity against malaria
parasites of humans. However, the 4-amino-quinoline compounds are more
effective against the
erythrocytic schizonts. It does not destroy gametocytes, but arrests
sporogony in the mosquito.
The action of pyrimethamine against _Toxoplasma gondii_ is greatly
enhanced when used in conjunction
with sulfonamides. This was demonstrated by Eyles and Coleman in the
treatment of experimental
toxoplasmosis in the mouse. Jacobs et al
demonstrated that combination of the 2 drugs effectively
prevented the development of severe uveitis in most rabbits following
the inoculation of the anterior
chamber of the eye with toxoplasma.
INDICATIONS AND USAGE
TREATMENT OF TOXOPLASMOSIS: DARAPRIM is indicated for the treatment of
toxoplasmosis when used
®
12
13
4
1
2
conjointly with a sulfonamide, since synergism exists with this
combination.
TREATMENT OF ACUTE MALA