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PROSTAGLANDINSPROSTAGLANDINS
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
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.
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.
• 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.
• 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.
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.
CLASSIFICATIO
N OF
PROSTAGLAND
INS
SERIES 1
One double bond-
from Linoleic Acid
SERIES 2
Two double bonds-
from Arachidonic
AcidSERIES 3
Three double bonds-
Eicosa penta-enoic
• 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.
BIOSYNTHESIS OF
PROSTAGLANDINS
GENERAL
FUNCTIONS
OF
PROSTAGLANDINS
Prostaglandins act on an array of cells and have a wide
variety of effects such as:
Vasoconstriction & vasodilation Induce labor pains
Decreases intraocular
pressure by increasing
removal of aqueous
humor from the eye.
Regulate inflammation
CELL GROWTH:
Cell proliferation ( PGE2 )
Stimulates growth of skeletal
muscle (PGF2α)
Acts on thermoregulatory
centre of hypothalamus to
produce fever.
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.
• Sensitize spinal neurons to
pain.
• Cause aggregation or
disaggregation of platelets.
• Regulate calcium movement.
• Regulate hormones
• Brain masculinization (in rats).
SOME OTHER
FUNCTIONS
ARE:
INDICATIONS AND ADVERSE EFFECTS OF
PROSTAGLANDINS
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.
• MISOPROSTOL(GENERIC) - oral 100 and 200 mcg
tablets.
• DINOPROSTONE(PROSTAGLANDIN E2) - vaginal
20mg suppositories ,0.5 mg gel.
• DINOPROST - intra amniotic injection
• LATANOPROSTENOL - topical
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.
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.
• Flushing
• Nausea
• Diarrhoea
• Hypotension
• Headache
• Nasal stuffiness etc.
SOME GENERAL SIDE-
EFFECTS ARE
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PROSTAGLANDINS

  • 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.
  • 8. CLASSIFICATIO N OF PROSTAGLAND INS SERIES 1 One double bond- from Linoleic Acid SERIES 2 Two double bonds- from Arachidonic AcidSERIES 3 Three double bonds- Eicosa penta-enoic
  • 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.
  • 11.
  • 13. Prostaglandins act on an array of cells and have a wide variety of effects such as: Vasoconstriction & vasodilation Induce labor pains
  • 14. Decreases intraocular pressure by increasing removal of aqueous humor from the eye. Regulate inflammation
  • 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:
  • 18. INDICATIONS AND ADVERSE EFFECTS OF PROSTAGLANDINS
  • 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
  • 24.