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PDA Block 2 > Ecosinoids > Flashcards

Ecosinoids Flashcards

1
Q

Alprostadil (impotence and erectile dysfunction)

Prostaglandin

A

PGE1

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2
Q

Alprostadil (impotence and erectile dysfunction)

Site of action

A

corpus cavernosum smooth muscle

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3
Q

Alprostadil (impotence and erectile dysfunction)

Mechanism of Action

A

PGE1 analog thatworks via the EP2/4 receptors to increase cAMP which relaxes trabecular smooth muscle and dilates cavernous arteries leading to entrapment of blood

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4
Q

Alprostadil (impotence and erectile dysfunction)

Receptor

A

EP2 Receptor

PGE1 works on EP2 receptor

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5
Q

Alprostadil (impotence and erectile dysfunction)

Major adverse effect

A

priapism, erection lasting over 6 hours

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6
Q

Two therapuetic uses of Alprostadil

A
  1. Impotence and Erectile Dysfunction when PGE1 acts on EP2 receptor on corpus cavernosum smooth muscle causing an increase in cAMP
  2. Temporary Maintenance of patent ductus arteriosus when PGE1 acts on EP2 receptor on ductus arteriosus smooth muscle leading to increase in cAMP
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7
Q

Alprostadil (maintenance of patent ductus arteriosus)

Prostaglandin

A

PGE1

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8
Q

Alprostadil (maintenance of patent ductus arteriosus)

Site of Action

A

ductus arteriosus smooth muscle

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9
Q

Alprostadil (maintenance of patent ductus arteriosus)

Mechanism of Action

A

PGE1 analog that increases cAMP via EP2 receptor which relaxes ductus arteriosus smooth muscle

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10
Q

Alprostadil (maintenance of patent ductus arteriosus)

Adverse effect

A

apnea

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11
Q

Two therapeutic uses of Bimatoprost

A
  1. glaucoma

2. Eyelash hypotrichosis

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12
Q

Bimatoprost (glaucoma) prostaglandin

A

Prostamide F2a

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13
Q

Bimatoprost (glaucoma) Site of action

A

trabecular and uveoscleral aqueous humor outflow pathways

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14
Q

Bimatoprost (glaucoma) Mechanism of action

A

stimulation of specific Prostamide F2a receptor resulting in changes in genes that remodel cells to increase drainage

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15
Q

Bimatoprost (glaucoma) major adverse effect

A

increase length and number of eyelashes

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16
Q

Bimatoprost (eyelash hypotrichosis) Prostaglandin

A

Prostamide F2a

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17
Q

Bimatoprost (eyelash hypotrchosis) Site of action

A

hair follicles of eye

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18
Q

Bimatoprost (eyelash hypotrichosis) Mechanism of action

A

Stimulation of specific Prostamide F2a receptor causing increase in anagen phase of hair cycle

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19
Q

Two therapeutic uses for Carboprost

A
  1. Pregnancy termination

2. To control postpartum hemorrhage

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20
Q

Carboprost (pregnancy termination) Prostaglandin

A

PGF2a

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21
Q

Carboprost (pregnancy termination) Site of action

A

uterine smooth muscle

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22
Q

Carboprost (pregnancy termination) mechanism of action

A

increase in Ca via FP receptor causing uterine contraction

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23
Q

Carboprost (pregnancy termination) Major adverse effect

A

uterine rupture

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24
Q

Major adverse effect of bimatoprost (eyelash hypotrichosis)

A

eye redness, itching

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25
Q

dinoprostone therapeutic functions

A
  1. cervical ripening in pregnancy

2. early pregnancy termination

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26
Q

dinoprostone (cervical ripening in pregnancy) prostaglandin

A

PGE2

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27
Q

dinoprostone (cervical ripening in pregnancy) Site of action

A

cervix

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28
Q

dinoprostone (cervical ripening in pregnancy) Mechanism of action

A
  • activation of collagenase via EP4 receptor which increases cAMP
  • relaxes cervical smooth muscle
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29
Q

dinoprostone (cervical ripening in pregnancy) major adverse effect

A

uterine rupture

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30
Q

dinoprostone (early pregnancy termination) prostaglandin

A

PGE2

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31
Q

dinoprostone (early pregnancy termination) Site of action

A

uterine smooth muscle

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32
Q

dinoprostone (early pregnancy termination) Mechanism of action

A

EP1 mediated increase in Ca
OR
EP3 mediated decrease in cAMP

causes uterine contractions

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33
Q

dinoprostone (early pregnancy termination) Major adverse effect

A

uterine rupture

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34
Q

Epoprostenol protaglandin

A

PGI2

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35
Q

Epoprostenol site of action

A

Pulmonary artery smooth muscle

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36
Q

Epoprostenol Mechanism of action

A

increase in cAMP via IP receptor which dilates the pulmonary artery vascular smooth muscle

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37
Q

Epoprostenol major adverse effect

A

GI related and potential drug interations with other hypertensive therapy or anti-platelt therapy

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38
Q

Epoprostenol therapeutic use

A

idiopathic pulmonary arterial hypertension

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39
Q

misoprostol prostaglandin

A

PGE1

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40
Q

misoprostol site of action

A

parietal cell

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41
Q

misoprostol Mechnaism of action

A

PGE1 analog that suppresses gastric acid secretion via decrease in cAMP via EP3 receptor

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42
Q

misoprostol major adverse effect

A

diarrhea

CONTRAINDICATED IN PREGNANCY

43
Q

misoprostol therapeutic use

A

replacement therapy for prevention of ulcers caused by long term administration with NSAIDs

take 4x a day

44
Q

In humans what is the most abundant precursor of ecosinoids

A

arachidonic acid

45
Q

Describe the biosynthesis of ecosinoids- release of arachidonic acid

A
  • Arachidonic acid is the precursor and it is found in very low concentration in the blood bc it is bound to a phospholipid
  • Phospholipase 2 (PLA2) cleaves the Sn-2 ester bond of membrane phospholipids
  • this is Ca dependent
46
Q

How do glucocorticoids suppress PLA2

A

they induce annexin-1 (lipocortin) which suppresses PLA2 activity

47
Q

How many isoforms exist of COX

A

2

48
Q

How many functions does each isoform of COX have

A
  1. oxygenase function and peroxidase function
49
Q

SO there are ______- distinct ______ at _______ distinct __________ on both COX proteins

A

There are two distinct activities at two distinct active sites on BOTH COX proteins

50
Q

2 Actions of COX

A
  1. oxygenates and cyclizes the free arachidonic acid to form
    cyclic endoperoxide PGG2
    - Occurs at cyclooxygenase active site of enzyme
    –  *Site where NSAIDs bind
  2. Peroxidase activity to reduce PGG2
    to PGH2
    -Occurs at peroxidase active site of enzyme
51
Q

Where do NSAIDs bind

A

at the cyclooxygenase active site of the COX enzyme

52
Q

What is the main difference between COX1 and COX2

A

-COX 1 is constitutive it is present in all tissues

  • COX 2 is inducible. It has a promoter region that binds transcription factors. it is commonly seen in inflammation
    • Nf-κB, C/EBP, ERK1/2, MAPK
53
Q

Name the four prostaglandins

A

PGE2
PGD2
PGF2a
PGI2

54
Q

Name the Thromboxane

A

TxA2

55
Q

What are the 3 main things that Arachidonic Acid Can be turned into an what enzyme class makes that happen

A
  1. Leukotrienes when acted upon by 5-lipoxygenases

2. Prostaglandins and Thromboxanes when acted upon by Cyclooxygenases (COX)

56
Q

Lipoxygenases

Also which is the most important and why

A

-family of cytosolic lipoxygenases that catalyze the
oxygenation of fatty acids to corresponding lipid
hydroperoxides
-lipoxygenases differ in specificity for placing the
hydroperoxy group, and tissues differ in the
lipoxygenase(s) they contain
**5-lipoxygenase is the most important because it produces Leukotrienes

57
Q

FLAP

A

5 lipoxygenase activating protein

58
Q

5-lipoxygenase inhibitor

A

Zileuton

59
Q

Leukotriene receptor

antagonist

A 
Zafirlukast
-DOES NOT INHIBIT
BIOSYNTHESIS 
-Inhibits the effect of the
CYS-containing
Leukotrienes (LTC4, LTD4, LTE4) 
meaning all except for LTB4
60
Q

Which Leukotrienes increase vascular permeability

A

LTC4 and LTD4

61
Q

Which Leukotrienes cause bronchoconstriction

A

LTC4 and LTD4

62
Q

Which Leukotrienes serve as chemoattractant for neutophils

A

LTB4

63
Q

Which Leukotrienes are increased in allergies and asthma

A

all

64
Q

Zileuton

A

 Inhibits 5-lipoxygenase
leads to  No production of any LTs

-Not appropriate or indicated for the reversal of bronchospasm in acute asthma attacks

65
Q

Zafirlukast

A
  • Cysteinyl leukotriene receptor antagonist

- No effect on LTB4

66
Q

Describe the catabolism of ecosanoids

A

rapidly inactivated

-95% of PGE1 is inactivated in one pass through the lungs

67
Q

Prostaglandins/Thromboxane interact with what type of receptors

A

GPCRs therefore their effects involve secondary messengers

68
Q

Receptor and second messenger

TXA2

A

TP and Ca mobilization

69
Q

Receptor and second messenger

PGF2a

A

FP and Ca mobilization

70
Q

Receptor and second messenger

PGE2

A

EP1/EP3 Ca mobilization

EP2/EP4 increase cAMP

71
Q

Receptor and second messenger

PGI2

A

IP increase cAMP

72
Q

Receptor and second messenger

PGD2

A

DP1 and DP2 increase cAMP

73
Q

Leukotriene  LTB4 causes

A

chemotaxis

Effector system=Increase intracellular
calcium

74
Q

Leuktorienes  LTC4 & LTD4 & LTE4 cause

A

-Bronchoconstriction
-Increase vascular
permeability

Effector system=Increase intracellular
calcium

75
Q

PGE2 and PGI2 and peripheral pain

A
  • act through specific GPCR
  • sensitive pain receptors
  • lead to hyperalgesia
76
Q

How do PGs cause pain

A

they decrease the threshold of pain so that lower levels of other mediators are able to cause pain

sometimes when levels of PGs are high enough they can cause pain alone through a specific GPCR

77
Q

Sequence of events for a fever

A
  1. increased formation of
    cytokines
    2  increases synthesis of PGE2
    in areas of brain associated with temperature control
    3  increases cAMP and
    triggers hypothalamus to elevate body temperature
    4  Hypothalamus regulates the
    set point at which body temperature maintained = fever
78
Q

Ecosinoids in Platelets

A 
-Activation of platelet
membrane PLA
release of arachidonic
acid and its metabolism
to thromboxane by
COX-1 (platelets make thromboxane specifically TXA2)

THEN

-TXA2 induces platelet aggregation
◦   Acts on TP receptor
◦  Increase in intracellular calcium

79
Q

TXA2 induces

A

platelet aggregation
◦   Acts on TP receptor
◦  Increase in intracellular calcium

80
Q

Activation of endothelial membrane PLA2 causes release of arachidonic acid which is then metabolized by COX1 and COX2 into…..

A

Prostacyclin PGI2

81
Q

What does PGI2 do?

A

-PGI2 is formed when endothelial membrane PLA2 releases arachidonic acid which is then metabolized by COX 1 and COX2 into PGI2 (Prostacyclin)

  • PGI2 inhibits platelet aggregation
  • It stimulates IP receptors and INCREASES cAMP

-PGI2 causes vasodilation via IP receptors and INCREASES cAMP

82
Q

What synthesizes PGI2

A

endothelial cells (to inhibit platelet aggregation)

83
Q

Role of PGI2 in uterus

A
  • early pregnancy-keeps uterus in quiescent state

- relaxation via IP receptors and increases cAMP

84
Q

Role of PGE2 in uterus

A
  • initiation and progression of labor
  • induces uterine contractility via EP1/EP3 mediated increase in calcium
  • Mediates cervical ripening via EP2/Ep4 mediated increase in cAMP
85
Q

Role of PGF2a in uterus

A

-contracts uterus during labor via FP receptor mediated increase in Ca

86
Q

How does pregnancy influence COX

A

Pregnancy induces COX1 and COX2 which increase PGI2, PGE2, and PGF2a

87
Q

Effect of PGF2a on the non-pregnant uterus

A

contributes to symptoms of primary dysmenorrhea (cramps)

disruption of the uterine membrane during mensration releases AA increasing PG synthesis via COX 1 and COX2

88
Q

What two prostaglandins are vasodilators

A

PGE2 and PGI2

But in some cases PGE2 is a vasoconstrictor when it acts on a different receptor (EP1/EP3) which increases Ca and inhibits cAMP

89
Q

What are two vasoconstrictors

A

PGF2a and TXA2

90
Q

Prostaglandins in the kidneys

A

PGE2 and PGI2 increase renal blood flow and promote diuresis and natriuresis

91
Q

Which os the following COX1 or COX2 is more important in disease in the kidney

A

COX2 (there is constituitive expression of COX2 in the macula densa cells, an there is a relationship between COX2 and PG mediated renin release)

92
Q

Describe the role of PGs in blood pressure regulation

A

LOCALLY produced vasodilator PGs tend to predominate.

  • PGE2 acts through EP4 (and EP2) to increase cAMP
  • PGI2 acts through IP to increase cAMP
  • they serve to counteract the effect of circulating vasoconstrictor autocoids (like angtiotensinII)

-they work to maintain blood flow to vital organs like the kidney, and increase Na and H2o excretion

93
Q

How do prostaglandins influcence Na and H2 excretion

A

increase

94
Q

During fetal life, the ductus arteriosus is

A

a normal structure that
allows most of the blood leaving the right ventricle to bypass the pulmonary circulation and pass into the descending aorta.

95
Q

what maintains patency of the ductus arteriosus during fetal life (keeps it open)

A

PGs specifically PGE2.

it causes relaxation via the EP4 receptor (cAMP) and COX2

96
Q

Function of Leukotrienes

A

bronchoconstriction and chemotaxis

97
Q

Which COX is important in synthesis of cytoprotective PGs (PGs that protect lining of GI system)

A

COX1

98
Q

Which PGs inhibit gastric acid secretion, and via which receptors

A

PGE2 (EP2/4) and PGI2)

99
Q

Role of PGs in gastric ulceration

A

they suppress gastric ulceration

100
Q

Name two reasons for why Prostaglandins have limited therapeutic use

A
  1. Significant adverse effects-PGs do so many different things all over the body there is great potential for adverse effects
  2. Short Half Lives in circulation-PG analogs that have chemical structures that prevent metabolism by 15-OH dehydrogenase and Delta 13-PG reductase have been developed
101
Q

Carboprost (control postpartum hemorrhage) prostaglandin

A

PGF2a

102
Q

Carboprost (control of postpartum hemorrhage) Site of Action

A

uterine smooth muscle

103
Q

Carboprost (control of postpartum hemorrhage) mechanism of Action

A

increase in Ca via FP receptor causing uterine contraction

104
Q

Carboprost (control of postpartum hemorrhage)

adverse reaction

A

uterine rupture

PDA Block 2 (13 decks)

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