Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHAR 341 - Pharmacology > Prostaglandins and Leukotrienes > Flashcards

Prostaglandins and Leukotrienes Flashcards

1
Q

Synthesis of Prostagladins, Leukotrienes, and Isoprostanes starts with:

A
  • Arachidonic acid (AA) is released from the cell membrane by phospholipase A2, phospholipase C, and diglyceride lipase
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Examples of Prostaglandins

A
  • COX 1 (cyclooxygenase)
  • COX 2
  • LOX (Lipoxygenase)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Expression of COX 1

A
  • expressed constitutively in most cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Expression of COX 2

A
  • indubile

- expression depends on certain stimuli

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Synthesis of Prostagladins

A
  • PGH2 is the precursor of prostaglandins and thromboxanes

- specifc isomerases and synthases for each unique PG

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Synthesis of Leukotrienes

A
  • LOX converts AA to leukotrienes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Prostaglandin PGE2 can bind to which receptors:

A

EP1
EP2
EP3
EP4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Prostaglandin PGD2 can bind to which receptors:

A

DP (1,2)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Prostaglandin PGF2 alpha can bind to which receptors:

A

FP (A,B)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Prostaglandin PGI2 (prostacyclin) can bind to which receptors:

A

IP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Thromboxane TXA2 can bind to which receptors:

A

TP (alpha, beta)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Effects of EP1

A
  • activates GI smooth muscle

- protects against NSAID ulceration in stomach

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Effects of EP2

A
  • facilitates pain transmission (spinal cord)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Effects of EP3

A
  • mediates fever generation
  • inhibits gastric acid secretion
  • protects against NSAID ulceration in intestines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Effects of EP4

A
  • sensitize npciceptors and neurons
  • pro-inflammatory in joint
  • promotes mucus secretion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Effects of DP(1,2)

A
  • bronchoconstriction

- promote sleep induction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Effects of FP(A,B)

A
  • vasoconstriction
  • bronchoconstriction
  • regulation of intraocular pressure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Effects of IP

A
  • vasodilation
  • inhibition of platelet aggregation
  • uterine relaxation
  • sensitize nociceptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Effects of TPAB

A
  • potent vasoconstriction
  • potent brochoconstriction
  • promote platelet aggregation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Leukotriene LTB4 binds to which receptor:

A

BT1,2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Leukotrienes LTC4,D4,E4 bind to which receptor:

A

CystLT1,2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Effects of BT1,2

A
  • chemoattractant (PMNs)

- activates inflammatory cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Effects of CystLT1,2

A
  • chemoattractant (eosinophils)

- potent brochoconstriction (induces bronchial inflammation)

24
Q

Prostaglandin Synthesis Inhibitors

A
  • corticosteroids

- NSAIDs

25
Q

How Corticosteroids inhibit prostaglandin synthesis

A
  • block all the known pathways of PG and LT synthesis

- block phospholipase A2

26
Q

How NSAIDs inhibit prostaglandin synthesis

A
  • block COX (prostaglandin and thromboxane)

- may promote synthesis by LOX of leukotrienes

27
Q

How NSAIDs work as analgesics

A
  • blocks formation of all prostaglandins (PGE2) peripherally (and in the CNS)
28
Q

How NSAIDs work form dysmenorrhea

A
  • increase endometrial synthesis of PGE2 and PGF2 causes the pain
  • block PGE2 synthesis which causes pain
29
Q

How NSAIDs work for Patent Ductus Arterious

A
  • PGE2 keeps the fetal ducts arteriosus open (normally closes at birth)
  • block PGE2 synthesis to get the duct to close
30
Q

Porstaglandin Agonists

A
  • Alprostadil
  • Dinoprostone
  • Misoprostol
31
Q

How Alprostadil works

A
  • PGE1-analogue of PGE2

- vasodilator

32
Q

Therapeutic use of Alprostadil

A
  • maintain the ductus arterosus patent in neonates awaiting cardiac surgery
  • 2nd line treatment for erectile dysfunction
33
Q

How Dioprostone works

A
  • PGE1-derivative

- promotes uterine contractions and cervical ripening

34
Q

Therapeutic uses for Diprostone

A
  • at end of term -> to facilitate delivery

- 1st/2nd trimester -> abortion

35
Q

Adverse effects of Diprostone and Misoprostol

A
  • abdomenal discomfort

- diarrhea

36
Q

How Misoprostol works

A
  • PGE1-derivative
  • cytoprotective at low doses
  • inhibits gastric acid secretion at hig doses
37
Q

Therapeutic uses of Misoprostol

A
  • prevent NSAID induced peptic ulcers

- used with antiprogestins for early abortion

38
Q

Prostaglandin E Analogues

A
  • Lubiprostone
39
Q

How Lubiprostone works

A
  • metabolite of prostaglandin E1 with low systemic absorption
  • activates voltage-dependnet chloride channels on the apical membrane of intestinal epithelial cells
  • increases chloride in intestinal tract which promotes intestinal fluid secretion leading to more rapid transit
40
Q

Therapeutic use of Lubiprostone

A
  • treatment of chronic constipation
41
Q

Adverse effects of Lubiprostone

A
  • vomitting, nausea, abdominal cramping
42
Q

Prostaglandin F Agonist

A
  • Latanprost (PGF2)
43
Q

How Latanprost works

A
  • topically active PGF2 derivative that lowers intraocular pressure
44
Q

Therapeutic use of Latanoprost

A
  • glaucoma
45
Q

Prostaglandin I Agonist

A
  • Prostacyclin (epoprostenol:PGI2)
46
Q

How Prostacyclin works

A
  • powerful vasodilator and inhibitor of platelet aggregation synthesized mainly by the vascular endothelium
  • promotes blood flow
47
Q

Therapeutic use for Prostacyclin

A
  • pulmonary hypertension

- porto-pulmonary hypertension

48
Q

Thromboxane receptor antagonists and synthesis inhibitors

A
  • prevent platelet aggregation and vasocontriction
49
Q

5-lipoxygenase enzyme inhibitors

A
  • Zileuton
50
Q

How Zileuton works

A
  • blocks LT4 synthesis
51
Q

Therapeutic Use for Zileuton

A
  • Asthma
52
Q

Adverse Effects of Zileuton

A
  • elevated liver enzymes, indigestion, abdominal pain, and nausea
  • metabolized by CYP so it can alter metabolism of other drugs
53
Q

Leukotriene-receptor inhibitors

A
  • montelukast
54
Q

How Montelukast works

A
  • competitive antagonist at the CystLT1 receptor
55
Q

Therapeutic uses for Montelukast

A
  • asthma

- allergic rhinitis

PHAR 341 - Pharmacology (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions