2. WHAT ARE
PROSTAGLANDINS?
Any of a group of
hormone like
substances
produced in various
tissues that are
derived from amino
acids and mediate a
range of
physiological
functions, such as
3. HISTORY
• Prostaglandins were
discovered in the 1930's.
• Ulf von Euler found that
seminal fluid and seminal
vesicles from most animals
including man contain a
substance which causes
contraction of the smooth
muscle of the uterus.
• He named this new
substance prostaglandin
since they were originally
thought to be secreted by
the prostate gland.
4. In 1945, Bergström met physiologist Ulf von
Euler who was conducting research on
prostaglandins.
Together, they conducted research on how
prostaglandins are formed.
During the 1950's, Bergström with the use of
Lyman Craig’s countercurrent extraction device
he was able to deduce the chemical structures of
prostaglandins. He also discovered that
prostaglandins are formed by the conversion of
unsaturated fatty acids.
5. • In the 1960's, following his successful
researches, he teamed-up with Samuelsson
in conducting further researches on
prostaglandins. Together, they worked on
how prostaglandins are formed and
metabolized.
• In the early 1960's, Vane created upgrades
in the procedure known as biological assay
or bioassay. By the use of this method, he
learned that prostaglandins are produced by
many tissues and organs and not just by the
prostate.
6. • In another study conducted in 1969, he found
the methods by which aspirin alleviates pain
and reduces inflammation. Vane also
discovered the existence of prostacyclin which
was found to be of great importance in
dissolving blood clots.
• Sune K. Bergström, Bengt I. Samuelsson and
John R. Vane were awarded the Nobel Prize in
Physiology or Medicine of 1982 for their
discoveries concerning prostaglandins and
related biologically active substances.
7. CHEMICAL STRUCTURE
• All prostaglandins are
considered to be
derived from the 20 C
cyclic saturated fatty
acid, prostanoic acid.
• The five carbon ring is
saturated.
• All naturally occurring
PGs have an alpha-
oriented OH group at
C15.
9. • Naturally occurring PGs belong to 2 series.
• PGs are not stored; precursor fatty acids are
stored in membrane as phospholipids.
• Arachidonic acid is released by the action of
phospholipase A2 on phospholipids.
• Synthesis is catalysed by prostaglandins H
synthase(PGHS).It contains two separate
enzymes (cyclo-oxygenase & peroxidase).
• PGG2 and PGH2 are formed as intermediates
during synthesis of other PGs.
15. CELL GROWTH:
Cell proliferation ( PGE2 )
Stimulates growth of skeletal
muscle (PGF2α)
Acts on thermoregulatory
centre of hypothalamus to
produce fever.
16. Acts on mesangial cells
(specialised smooth muscle
cells) in the glomerulus of the
kidney to increase glomerular
filtration rate.
Acts on parietal cells in the
stomach wall to inhibit acid
secretion.
17. • Sensitize spinal neurons to
pain.
• Cause aggregation or
disaggregation of platelets.
• Regulate calcium movement.
• Regulate hormones
• Brain masculinization (in rats).
SOME OTHER
FUNCTIONS
ARE:
19. INDICATIONS
There are different indications for each drug,some
are listed below:
• ALPROSTADIL - penile injection 5,10,20,40mcg sterile
powder for reconstitution.
• BIMATOPROST (LUMIGAN) - ophthalmic drops
0.03% solution.
• EPOPROSTENOL(PROSTACYCLIN) - intravenous
0.5,1.5mg powder to reconstitute.
• ILOPROST (VENTAVIS) - inhalation 10mcg/ml
solution.
20. • MISOPROSTOL(GENERIC) - oral 100 and 200 mcg
tablets.
• DINOPROSTONE(PROSTAGLANDIN E2) - vaginal
20mg suppositories ,0.5 mg gel.
• DINOPROST - intra amniotic injection
• LATANOPROSTENOL - topical
21. ADVERSE EFFECTS
EFFECTS ON GIT SYSTEM:
• Longitudinal muscle is contracted by PGE2,circular
muscle is contracted strongly by PGF2 alpha and
weakly by PGI 2.
• Administration of PGE2 results in colicky cramps.
• Misoprostol causes abdominal discomfort and
occasional diarrhoea.
EFFECTS ON FEMALE REPRODUCTIVE
SYSTEM:
• TXA2,low concentrations of PGE2 contracts uterine
muscle.
• Disturbed menses is also seen sometimes.
22. EFFECT ON MALE REPRODUCTIVE
SYSTEM:
• Prostaglandins causes pain in penis if
taken in excess.
EFFECTS ON CARDIOVASCULAR SYSTEM:
• In most vascular beds PGE2;PGFI2 and
PGD2 elicit vasodilation and drop in blood
pressure.
• PGE2 can cause vasoconstriction through
activation of EP1 and EP3 receptors.
• LTC4 and LTD4 results in hypotension.
23. • Flushing
• Nausea
• Diarrhoea
• Hypotension
• Headache
• Nasal stuffiness etc.
SOME GENERAL SIDE-
EFFECTS ARE