this ppt highlights physiology and pharmacology of prostaglandins and other lipid derived autacoids with illustrations...for better understanding....

1. DR.V. SATHYA NARAYANAN M.D
PROFESSOR OF PHARMACOLOGY
SRM MEDICAL COLLEGE
CHENNAI, INDIA

2.  Derivatives of 20 Carbon atom
polyunsaturated essential fatty acids
 Derived from cell membrane phospholipids
 Most universally distributed autacoids
 Prostaglandins - PGs
 Leukotrienes - LTs
 Thromboxanes – TXs

4.  Derivatives of prostanoic acid
 Synthesized locally
 in response to appropriate
stimuli
 Like injury, infection

7.  Vasodilatation, fall in BP
 Contraction of uterus, softening of
cervix
 Dilatation of bronchi
 Decreases acid secretion, increases
mucus secretion
 Increases peristalsis of intestines

12.  kidney - Natriuresis, vasodilatation, renin
release
 Pyrogenic
 Sensitize afferent nerves to noxious stimuli
 Release ant.pituitary hormones, steroids,
insulin
 metabolism - Antilipolytic, insulin like
action

16.  Vasodilatation
 Contraction of uterus, softening of cervix
 Constriction of bronchi
 Spasmogenic on intestines
 Release gonadotropins, prolactin

21.  Vasodilatation, fall in BP
 Inhibit platelet aggregation
 Dilate bronchi, inhibit histamine release
 Dec. acid secretion

28.  Weak spasmogenic
 Kidney - Natriuresis, vasodilatation, renin
release
 Sensitize afferent nerves to noxious stimuli

31.  Vasoconstriction
 Platelet aggregation
 Constriction of bronchi

35.  Facilitate fertilization
 PGs mediate initiation and
progression of labour
 Dysmenorrhoea associated With
Increased PGs

42.  Mediate vasodilatation and exudation
at the site of inflammation
 PGI2- regulation of local vascular tone
 Maintaining patency of ductus
arteriosus
 Prevent platelet aggregation (PGI2),
Promote aggregation – TX A2

49.  Mediate pyrogen induced fever,
malaise
 Algesic in inflammation
 Facilitate aqueous humour drainage
 GLAUCOMA

52.  Imbalance cause asthma
 Involved in mediating fluid loss in
toxin induced diarrhea
 Antiulcerogenic and natural ulcer
protective
 Role in the Growth of polyp, cancer
of colon
 Intrarenal regulators of renal blood
flow

59.  DP – affinity for PGD2
 EP - affinity for PGE2
 FP – affinity for PGF2alpha
 IP – affinity for PGI2
 TP – affinity for TXA2
 All are G-protein coupled receptors
 Some act through cAMP and others via IP3

62.  RESTRICTED BECAUSE OF
 Limited availability
 Short lasting action
 Cost
 Side effects

64.  SYNTHETIC PROSTAGLANDINS ARE USED
Because they are
 more stable
 Long acting
 more specific

66.  EXOGENOUS PG F2 α
 Intra amniotic injection
 INDICATIONS
termination of pregnancy ( midterm),
Induction of labor

72. synthetic PGE2 analog
10 times more potent than dinoprost
PREPARATIONS-
 Vaginal gel, vaginal tab, cervical gel,
 i.v inj, Oral tablet
 Uses: cervical ripening, induction of
labour
termination of pregnancy (midterm) –
dinoprostone 20 mg suppository +
gemeprost 1mg vaginal pessary

85.  15methyl PGF2 alpha
 Prolonged action
 INDICATIONS :
1. to arrest Post Partum Hemorrhage –
alternative to ergometrine & oxytocin
2. midterm abortion
3. Cervical ripening
 DOSAGE :
0.25 mg deep i.m

91. PGE1
 INDICATIONS
 Medical termination of pregnancy
 1st
tri - 1mg pessary
2nd
tri – 1mg pessary every 3 hours ( max -5)
 To soften the cervix in 1st
trimester

95.  Synthetic PGE1
 Indications :
 Keep the patency of D.A in children with
Congenital Heart Disease
 Prevent platelet aggregation
 Peripheral vascular disease
 Impotence

101.  Synthetic PGE1 analogue
 Actions :inhibits gastric acid secretion
cytoprotective
 IND : peptic ulcer
prophylaxis of NSAID induced ulcers.
 DOSE :400mg twice daily
 ADR : diarrhoea
 C/I : pregnancy (abortion)

107.  ACTIONS : inhibits platelet aggregation
vasodilatation
 INDICATIONS :cardiac bypass
 to prevent
hemoperfusion platelet
hemodialysis aggregation
 primary pulmonary hypertension
 Has to be given intravenously

111.  Long acting PGF2 α derivative
 Eye Drops to be put into conjunctival sac
 1st
choice drugs in wide angle Glaucoma

115.  Nausea, vomiting
 Watery diarrhoea
 Uterine cramps
 Vaginal bleeding
 Flushing
 Shivering, fever
 Hypotension, tachycardia

125.  LTC4,LTD4,LTE4  SRS – A of anaphylaxis
 Mediate inflammation
 LTC4, LTD4 are the most important
mediators of allergic asthma
 Abdominal colic in anaphylaxis
 Contribute pain of inflammation
 LT receptor antagonists – Montelukast,
Zafirlukast

132.  Synthesized by - platelets,WBC, kidney,
- vascular endothelial cells
ACTIONS : vasodilation, Chemotaxis
aggregation of WBC & degranulation
BP
Broncho constriction
Platelet aggregation
Vasular permeability
ulcerogenic

133.  Pain and Inflammation
 Bronchial asthma
 Anaphylactic shock
 Hemostasis and thrombosis
 Implantation of embryos
 Parturition

134.  GINKGOLIDE B
 Stroke
 Intermittent claudication
 Sepsis
 MI
 Shock
 Asthma
 Contraceptive
 Alprazolam, triazolam

142.  Abortion
 Induction of labour
 Cervical priming
 Post Partum Hemorrhage
 Peptic ulcer
 Glaucoma
 To maintain patency of ductus arteriosus
 To avoid platelet damage
 Peripheral vascular disease