Study Set Content:
and several similar compounds- are
topically active PGF 2a derivatives used in ophthalmology
to treat open-angle glaucoma.
Latanoprost
is FDA approved for treatment of
eyelash hypotrichosis and has shown efficacy in
enhancing eyelash growth after chemotherapy. The drug
is applied in a 0.03% solution to the skin at the base of
the upper lashes
Bimatoprost
is synthesized
mainly by the vascular endothelium and is a powerful
vasodilator and inhibitor of platelet aggregation. It is
used clinically to treat pulmonary hypertension and
portopulmonary hypertension.
Prostacyclin (PGI2, epoprostenol)-
has underisable
properties (aggregation of platelets, vasoconstriction).
thromboxane (TXA 2)
– receptor antagonists and synthesis
inhibitors have been developed for cardiovascular
indications, although these (except for aspirin) have yet
to establish a place in clinical usage.
TXA 2
The metabolism of AA by the 5-, 12-, and 15-
lipoxygenases (LOX) results in the production of:
Hydroperoxyeicosatetraenoic acids (HPETEs),
which rapidly convert to
o Hydroxy derivatives
Hyxyeicosatetraenoic acid
(HETEs) and
o Leukotrienes
The most actively investigated leukotrienes are those
produced by the (blank) present in leukocytes
5-LOX
The most actively investigated leukotrienes are those
produced by the 5-LOX present in leukocytes
(neutrophils, basophils, eosinophils, and monocyte-
macrophages and other inflammatory cells such as mast
cells and dendritic cells.
This pathway is great interest since it is associated with
asthma, anaphylactic shock, and cardiovascular disease.
Stimulation of these cells elevates intracellular Ca 2+ and
releases
arachidonate
Stimulation of these cells elevates intracellular Ca 2+ and
releases arachidonate; incorporation of molecular
oxygenase by
5-LOX,
Stimulation of these cells elevates intracellular Ca 2+ and
releases arachidonate; incorporation of molecular
oxygenase by 5-LOX, in association with
5-LOX-activating
protein (FLAP),
Stimulation of these cells elevates intracellular Ca 2+ and
releases arachidonate; incorporation of molecular
oxygenase by 5-LOX, in association with 5-LOX-activating
protein (FLAP), then yields the unstable epoxide
leukotriene A 4 (LTA4).
These three products,(blank) are called cysteinyl
leukotrienes.
LTC4, D4 , E4 ,
are potent bronchoconstrictors and are
recognized as the primary components of the slow-
reacting substance of anaphylaxis (SRS-A) that is
secreted in asthma and anaphylaxis.
LTC and D4
Specific isozymes of microsomal cytochrome P450
monooxygenases convert AA to hydoxy- or
epoxyeicosatrienic acids.
Specific isozymes of microsomal cytochrome P450
monooxygenases convert AA to hydoxy- or
epoxyeicosatrienic acids.
o The products are
20 HETE
The products are 20-HETE, generated by the CYP
hydroxylases
(CYP3A, 4A, 4F) and the 5,6 8,9-,
11,12-, 14,15- epoxyeicosatrienic acids (EETs),
The products are 20-HETE, generated by the CYP
hydroxylases (CYP3A, 4A, 4F) and the 5,6 8,9-,
11,12-, 14,15- epoxyeicosatrienic acids (EETs),
which arise from the CYP epoxygenase
2J and 2C
