Brainscape's Knowledge GenomeTM

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


See full index

Pathopharm Final > Eicosanoids > Flashcards

Eicosanoids Flashcards

V: 30-58

1
Q

what is an eicosanoid

A

a diverse group of molecules mainly derived from arachidonic acid

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

what is arachidonic acid produced from

A

membrane phospholipids by the action of phospholipase A2

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

eicosanoids are termed ____________

A

autocrine regulators (local hormones)

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

what are eicosanoids important for regulating

A

many physiologic functions
inflammation, pain perception, blood flow, smooth muscle contraction

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

eicosanoids are implicated in several disease states including (2)

A

rheumatoid arthritis and myocardial infarction

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

eicosanoids include what classes (3)

A

Includes the prostaglandins, thromboxanes, and leukotrienes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

eicosanoids are produced in very ____________ amounds and have ____________ half-lives

A

are produced in very small amounts, and have short half-lives

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

Prostaglandins are ____________ derivatives containing a____________ ring

A

arachidonic acid; cyclopentane

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

prostaglandin class # is related to

A

the number of double bonds in the structure

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

most important prostaglandin series in humans

A

2 series (prostaglandin F2)

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

actions of prostaglandins include (3)

A

inflammation
reproductive (ovulation & uterine contractions)
digestion (inhibit gastric secretions)

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

prostaglandins may have ____________ functions

A

antagonistic

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

some prostaglandins may cause

A

smooth muscle contraction , and some may cause relaxation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

thromboxanes are derivatives of

A

arachidonic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

structurally, thromboxanes contain a ____________ group

A

cyclic ether

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

most prominent thromboxane compound

A

TXA2

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

TXA2 is produced mainly by

A

platelets

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

TXA2 release stimulates….

A

platelet aggregation & vasoconstriction
important mechanism to control hemorrhage

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

leukotriene structure

A

noncyclic (linear) derivatives of arachidonic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

leukotriene name stems from

A

original discovery in leukocytes, and the presence of three conjugated double bonds.

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

what does the subscript # in leukotrienes mean

A

total # of double bonds

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

leukotrienes are known to be components of

A

SRS-A (slow releasing substance of anaphylaxis)

LTC4, LTD4, and LTE4

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

leukotrienes are secreted by

A

mast cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is x5000 more potent with a longer duration, leukotrienes or histamine

A

LEUKOTRIENES!!!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

what do leukotrienes do during inflammation

A

they increase fluid leakage from blood vessels into tissue

(Addtnl fxns: vasoconstriction, bronchoconstriction and edema)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

function of LTB4

A

a potent chemotactic factor, attracting white blood cells to area of inflammation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

other effects of leukotrienes include (3)

A

vasoconstriction, bronchoconstriction and edema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

arachidonic acid cascade

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

low concentration of PG-D2 causes

A

vasodilation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

higher concentration of PG-D2 causes

A

vasoconstriction

(exception: causes only vasoconstriction in the pulmonary circulation).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

PG-D2 contracts what muscle

A

broncial

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

PG-D2 causes secretion of…

A

renin from the renal cortex

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

PG-D2 inhibits

A

platelet aggregation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

PG-Es primarily cause

A

potent vasodilation
(decrease BP & increased flow to most organs, esp heart & kidney)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

PG-Es increase ____________ and can cause ____________

A

Increases local blood flow and can cause erythema.

PG-Erythema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

PG-Es inhibit (2)

A

B lymphocyte proliferation and differentiation to plasma cells

also inhibits expression of IL-1 and T cell proliferation.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

PG-Es relax ____________ muscle

A

bronchial

“PG-E helps you brEEEEathe”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

PG-Es contracts ____________ and ____________ smooth muscle

A

uterine and intestinal smooth muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

PG-Es synthesis is increased in the ____________ during menstruation

A

endometrium

(uterine membranes are disrupted, AA is released, and PG-Es synthesis is stimulated).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

PG-Es sensitizes ____________ pain fibers and causes uterine contractions resulting in ____________

A

afferent; ischemic pain and primary dysmenorrhea.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

what PG causes strong uterine contractions during the last 2 trimesters and can induce delivery

A

PG-Es

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

uterus becomes more sensitive to ____________ as gestation progreses

A

PG-Es

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

PG-Es are particularly abundant in (3)

A

the uterus, menstrual and amniotic fluid.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

what do PG-Es do to body temp

A

Increases body temperature (synthesized in response to pyrogens which increase the synthesis and release of cytokines.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

PG-E increases ____________ and triggers the ____________ to ↑ body temp

A

cAMP; hypothalamus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

the hypothalamus increases body temperature by ____________ and decreasing ____________

A

promoting heat generation; heat loss

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

PG-Es can sensitize pain receptors to simulation and cause

A

hyperalgesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

PG-E GI effects

A

Inhibits gastric acid secretion and increases GI mucus secretion; these are important cytoprotective properties.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

PG-F2 constricts

A

pulmonary vessels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

PG-F2 contracts (3)

A

bronchial muscle (may cause intense bronchoconstriction in asthmatics).

uterine and GI muscles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

PG-F2 stimulates movement of ____________ and ____________ into ____________

A

water; electrolytes; intestinal lumen (may result in watery diarrhea).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

where is PG-F2 most abundant (3)

A

uterus, menstrual and amniotic fluid.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

PG-F2 acts on

A

uterine and intestinal smooth muscle similar to PG-E

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

which PG increases uterine tone more PG-E or PG-D

A

PG-F2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

formation of disproportionately large amounts of PG-F2 is thought to be responsible for

A

uterine hypercontractility in dysmenorrhea.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

what PG is prostacyclin

A

PG-I₂

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

function of PG-I₂

A

Potently inhibits platelet aggregation and causes hypotension.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

PG-I₂ causes vaso____________

A

dilation (relaxes vascular smooth muscle).

59
Q

PG-I₂ has ____________ effects as PG-E and PG-Fs on uterine tone

A

opposite

60
Q

PG-I₂ is abundant in

A

uterine, umbilical and fetal vasculature

61
Q

plays a role in ensuring adequate blood flow and a patent ductus arteriosus

A

PG-I₂

62
Q

PG-I₂ has ____________ properties

A

cytoprotectant

63
Q

TX-A₂ functions (3)

A

potently stimulates platelet aggregation.
potent vasoconstriction.
potent bronchoconstriction.

64
Q

LT-B₄ functions (3)

A

potent leukocyte chemotaxis (induces adherence, degranulation, and formation of oxygen radicals in neutrophils).

can cause hyperalgesia.

stimulates B-cell proliferation.

65
Q

LT-C₄ and LT-D₄ functions (2)

A

potent bronchoconstrictors.

increase microvascular permeability, plasma exudation, and mucus secretion.

66
Q

HPETE and HETE roles

A

Roles are largely unknown

67
Q

how are HPETE and HETE formed

A

from action of lipoxygenase on arachidonic acid.

68
Q

precursors for leukotriene biosynthesis

A

HPETE and HETE

69
Q

12-HPETE may function as

A

a neurotransmitter

70
Q

12-HETE stimulates…

A

migration of aortic smooth muscle cells and may promote cardiac vessel thickening after endothelium damage caused by angioplasty.

71
Q

12-HETE also appears to act as

A

a chemoattractant

72
Q

prostaglandins can be used for ____________ in obstetrics

A

1st and 2nd trimester abortions

Stimulates uterine contractions and can terminate pregnancy.

73
Q

how is hemabate administered

A

IM

74
Q

how is dinoprostone (Prepidil) administered

A

intravaginally

IV appears to be too toxic - diarrhea, vomiting, bronchoconstriction, hyperthermia, etc.

75
Q

prostaglandin use in obstetrics

A

Used to ripen an unfavorable cervix in pregnant patients at or near term with a medical need for the induction of labor

76
Q

PGs cause local cervical effects such as

A

softening and dilating the cervix

77
Q

PG-Es probably produce effects on the cervix by (2)

A

increasing proteoglycan and altering biophysical properties of collagen

78
Q

collagenase may be secreted in response to

A

PG-E₂

79
Q

collagen degradation is performed by

A

collagenase

80
Q

how is dinoprostone (Prepidil Gel) administered

A

endocervically (through an endocervical catheter).

81
Q

carboprost use in obstetrics

A

to control postpartum uterine atony and hemorrhage

promote uterine contraction after C-section or other uterine surgery

82
Q

use of prostaglandins in pediatrics

A

Maintain patency of ductus arteriosus in infants with congenital heart defects who depend upon a patent ductus for survival

83
Q

what defects require the patency of the ductus arteriosus

A

transposition of the great vessels and pulmonary artery stenosis

84
Q

infants with transposition of the great vessels and pulmonary artery stenosis…

A

have restricted pulmonary and systemic blood flow and may be cyanotic.

85
Q

IV infusion of ____________ can be used for pediatric cardiac defects until surgery can be performed

A

alprostadil

86
Q

Vasodilation with penile injection of____________ increases blood flow and causes an erection.

A

alprostadil

87
Q

misoprostol can cause cytoprotection of the stomach in patients on ____________ with a hx of ____________

A

NSAIDS; peptic ulcer

(Misoprostol used orally)

88
Q

PG-I₂ is used to ____________ in dialysis machines

A

prevent platelet aggregation

89
Q

synthetic oral PG-E₁ analog

A

misoprostol

90
Q

misoprostol absorption and metabolism

A

Rapidly absorbed and de-esterified to active misoprostol acid.

91
Q

Used orally to prevent ulcers in patients on chronic NSAID treatment.

A

misoprostol

92
Q

May prevent renal failure due to NSAIDS.

A

misoprostol

93
Q

side effects of misoprostol

A

transient diarrhea

94
Q

misoprostol side effects vs other prostaglandins

A

well-tolerated (less vomiting, fever, diarrhea than PG-E2, PG-F2α , or 15-methyl PG-F2α so is preferred by some over these for obstetric use).

95
Q

misoprostol can be given intravaginally to induce

A

abortion

96
Q

misoprostol is contraindicated in

A

pregnant patients (due to its abortifacient effects, it may cause miscarriage which may be incomplete).

97
Q

dinoprostone is a ____________ (class)

A

synthetic PG-E₂ analog

98
Q

dinoprostone is administered as a vaginal suppository to

A

terminate pregnancy and evacuate uterine contents after intrauterine fetal death

99
Q

dinoprostone vaginal dosing

A

20 mg is inserted intravaginally and repeated Q 3-5 hr until abortion occurs.

Should not be used for more than 2 days.

100
Q

dinoprostone (prepidil gel) when administered intrauterine is used to

A

ripen the cervix and facilitate labor.

101
Q

dinoprostone (cervidil) dosing

A

a 10 mg vaginal insert that releases 0.3 mg/hr over 12 hr. It is removed after onset of labor or 12 hr after insertion.

102
Q

side effects of dinoprostone

A

stimulates smooth muscle of GI tract causing vomiting and diarrhea (give antiemetic and antidiarrheal); transient fever.

103
Q

carboprost tromethamine (Hemabate) class

A

Synthetic derivative - 15-methyl-PG-F2α with oxytocic properties, used to induce abortion.

104
Q

what prolongs the duration of action of carboprost (hemabate)

A

15-methyl group prolongs the duration of action.

105
Q

carboprost (Hemabate) dosing

A

0.25 mg given IM when uterine contents haven’t been eliminated but membranes are ruptured, then can give up to 0.5 mg at 2 hr intervals.

Given repeatedly up to a total dose of 2.6 mg normally needed to cause abortion.

106
Q

other uses for carboprost (Hemabate)

A

control post partum hemorrhage

107
Q

large doses of carboprost/hemabate may cause

A

hypertension by constricting vascular smooth muscle.

107
Q

side effects of carboprost (hemabate)

A

vomiting, nausea, diarrhea (stimulates smooth muscle of GI so give antiemetic, antidiarrheal); transient pyrexia.

108
Q

alprostadil class

A

Naturally occurring form of PG-E₁

109
Q

alprostadil use in infants with congenital heart defects

A

Used to temporarily maintain a patent ductus arteriosus in infants with congenital heart defects.

Smooth muscle of the ductus arteriosus is especially sensitive to alprostadil which dilates it.

110
Q

how is alprostadil administered

A

by continuous IV infusion since is rapidly metabolized by one pass through the lungs.

111
Q

alprostadil neonatal effects

A

Apnea occurs in 10 - 12% of neonates (most often in neonates weighing less than 2 kg) usually in the first hour of IV infusion.

Important to monitor respiratory status.

112
Q

side effects of alprostadil

A

fever, flushing, hypotension, bradycardia, seizures, diarrhea, and rarely cardiac arrest.

113
Q

alprostadil penile injection class

A

Naturally occurring form of PG-E₁

114
Q

how is alprostadil penile injection administered

A

Intracavernosal (penile) injection used for impotence (inject into the corpora cavernosa)

115
Q

alprostadil penile injection mechanism of action

A

Relaxes the trabecular smooth muscle and dilates cavernosal arterioles (increases cavernal blood flow) leads to expansion of lacunar spaces and entrapment of blood.

116
Q

alprostadil dosing

A

Injected 20 min before sex; produces an erection within 5-20 min lasting 1 - 3 hours.

Use no more than 3 times a week, at least 24 hr between each use.

117
Q

side effects of alprostadil penile injections

A

priapism (erection lasting 6 hr; requires medical attention), bleeding at injection site, penile pain; penile fibrosis

118
Q

EDEX

A

another injection therapy. It is a slightly different formulation of the prostaglandin in Caverject, is cheaper, and is injected with a smaller needle. It is injected 10 min to 2 hr before sex.

119
Q

MUSE

A

an alprostadil suppository. Alprostadil in gel form is delivered through an applicator inserted into the tip of the penis. It is applied 5 to 10 min before sex and can be used twice a day. Erections can last an hour.

120
Q

t/f sildenafil is an eicosanoid

A

FALSE

121
Q

sildenafil mechanism of action

A

acts by inhibiting Phosphodiesterase type 5, which is responsible for the breakdown of cGMP produced in response to nitric oxide.

This cGMP is responsible for relaxation of smooth muscle cells and increasing blood flow in the corpus cavernosum.

122
Q

PDE5 is also found in

A

blood vessels in the lungs

123
Q

PDE5 inhibitors are used for

A

pulmonary HTN

124
Q

T/F sildenafil is completely specific for PDE5

A

false! side effects may be due to other PDE inhibition

PDE6 in retina and inhibition may alter vision and cause blindness – d/c at least 1 week prior to surgery

125
Q

epoprostenol class

A

PG-I₂ anaglow

126
Q

Orphan drug for replacement of heparin in some hemodialysis patients.

A

epoprostenol

127
Q

prevents platelet aggregation in dialysis machines

A

epoprostenol

128
Q

what is epoprostenol used for long-term

A

long-term treatment of primary pulmonary hypertension (potent pulmonary vasodilator).

129
Q

other PG-I₂ analogues for pulmonary HTN and raynaud’s

A

Iloprost (Ventavis), Treprostanil (Remodulin)

inhalational and parenteral forms available

130
Q

Prostaglandin analogs for glaucoma and ocular hypertension

A
  • Latanoprost (Xalatan)
  • Bimatoprost (Latisse)
  • Travoprost (Ibza)
  • Tafluprost (Zioptan)
131
Q

Latanoprost (Xalatan)

A
  • PG-F2α analog
  • ophthalmic solution (QD) for elevated intraocular pressure
  • selective agonist at FP type prostaglandin receptor, which in the eye increases the outflow of aqueous humor
132
Q

Latanoprost (Xalatan)
is a a (selective/non-selective) agonist at the ____ receptor, which in the eye…

A

selective
FP type prostaglandin
increases the outflow of aqueous humor

133
Q

Montelukast (Singulair)
drug class

A

Leukotriene receptor antagonist (LTRA)

134
Q

Montelukast (Singulair) binds to ____ receptors, which are located…

A
  • cysteinyl leukotriene (CysLT1)
  • bronchiole airway tissue (and other areas)
135
Q

T/F
The CysLT1 receptor is solely located in bronchiole airway tissue.

A

False
other locations as well
but
Montelukast (Singulair) binds here

136
Q

Montelukast (Singulair)
moA

A
  • Binds to cysteinyl leukotriene receptors (CysLT1) in bronchiole airway tissue
  • Blocks LT-D4 action on bronchiole tissue (bronchoconstriction, airway edema, & inflammatory responses)
  • anti-asthmatic
137
Q

Can Montelukast (Singulair) be used for asthma?

A
  • Yes; anti-asthmatic
  • Blocks LT-D4 @ bronchiole tissue, which would normally cause bronchoconstriction, airway edema, and inflammatory responses
138
Q

Which Leukotriene receptor antagonists (LTRA) are only available PO?

A

Montelukast (Singulair)
Zamfirlukast (Accolate)

139
Q

T/F
Montelukast (Singulair) & Zamfirlukast (Accolate) are Leukotriene receptor antagonists that act by a different mechanism.

A

False
same mechanism

140
Q

T/F
Zileuton, Montelukast, & Zamfirlukast are all leukotriene receptor antagonists.

A

False
Leukotriene modifiers:
1) leukotriene receptor antagonists
2) leukotriene inhibitors (zileuton)

141
Q

Arachidonic acid is converted to leukotrienes via the ____ pathway

A

5-lipoxygenase

142
Q

Zileuton (ZyFlo)
moA

A
  • 5-lipoxygenase inhibitor
  • inhibits arachadonic acid → leukotrienes (B4, C4, D4, E4)
  • prophylactic & chronic asthma
143
Q

When can Zileuton (ZyFlo) be used for asthma?

A

prophylactic and chronic treatment

Pathopharm Final (8 decks)

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