DARAPRIM pyrimethamine tablet

Quốc gia: Hoa Kỳ

Ngôn ngữ: Tiếng Anh

Nguồn: NLM (National Library of Medicine)

Thành phần hoạt chất:

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

Sẵn có từ:

KAISER FOUNDATION HOSPITALS

INN (Tên quốc tế):

PYRIMETHAMINE

Thành phần:

PYRIMETHAMINE 25 mg

Loại thuốc theo toa:

PRESCRIPTION DRUG

Tình trạng ủy quyền:

New Drug Application

Đặc tính sản phẩm

DARAPRIM- PYRIMETHAMINE TABLET
KAISER FOUNDATION HOSPITALS
----------
DARAPRIM
(PYRIMETHAMINE)
25-MG SCORED TABLETS
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
conjointly with a sulfonamide,
®
12
13
4
1
2
since synergism exists with this combination.
TREATMENT OF ACUTE MALARIA
DARAPRIM is also indicated for