Autonomic pharmacology pt. 3: Autacoids Flashcards

1
Q

Leukotrienes are generated from _______ using the enzyme ________.

A

arachidonic acid, lipooxygenase

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2
Q

In which major organ do leukotrienes bind receptors primarily? What does this cause?

A

Lungs. Causes bronchoconstriction

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3
Q

How is asthma commonly treated?

A

With leukotriene receptor antagonists.

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4
Q

In which organ(s) is/are COX-1 found?

A

GI tract and kidneys

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5
Q

In which organ(s) is/are COX-2 found?

A

Kidneys

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6
Q

What is one AE that inhibition of prostacyclin (PGI2) can cause?

A

MI or thrombotic stroke

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7
Q

Why do NSAIDs cause AEs like GI ulceration and bleeding?

A

They non-selectively inhibit cyclooxygenases 1 and 2. COX-1 produces PGE2 which makes the protective mucosal barrier in the GI tract. COX-1 also produces thromboxane TXA2 which promotes platelet aggregation.

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8
Q

What do prostacyclins like PGI2 do? Which enzyme makes it? Does aspirin affect COX-2?

A

Inhibit platelet aggregation and vasodilate. COX-2 makes it. Aspirin does not affect COX-2 in small doses, and that is the basis for its blood-thinning effects. It inhibits COX-1, preventing TXA2 formation.

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9
Q

Do prostaglandins produced in the kidney help promote healthy renal blood flow?

A

Yeah

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10
Q

What are the two types of histamine receptors? Which one is involved in allergic reactions and therefore is a target of anti-histamines?

A

H-1 and H-2. H-1 is involved in allergic reactions and is a target of diphenhydramine and loratidine.

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11
Q

Can diphenhydramine cross the blood-brain barrier? What is the clinical significance of this?

A

It can because it is lipophilic. It is therefore a sedative because it can bind H-1 receptors in the CNS.

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12
Q

Where are H-2 receptors primarily found? What does stimulation of these receptors do? What drugs target these receptors?

A

Found in the stomach. Stimulation results in parietal cell acid secretion. Drugs target these receptors to treat acid reflux: ranitidine, nizatidine, famotidine.

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13
Q

What do bradykinins do?

A

Vasodilation and pain

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14
Q

What is the relationship between ACE and bradykinins? What do ACE inhibitors do?

A

ACE degrades bradykinins. ACE inhibitors increase endogenous bradykinins and also reduce angiotensin II, resulting in vasodilation.

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15
Q

Does increased serotonin levels in the brain improve mood and sleep?

A

Yeah

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16
Q

In which organ is the majority of serotonin found?

A

GI (~80%)

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17
Q

What does serotonin do to smooth muscle?

A

Constriction (remember serotonin agonist treat migraines in phase 2 - vasodilation)

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18
Q

What two molecules are responsible for symptoms of allergy? What is the Triple response of Lewis?

A

Histamine and kinins causes Triple response of Lewis: heat, itching, swelling, pain (HISP).

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19
Q

Where are mast cells located?

A

Perivascularly and close to nerve endings

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20
Q

Can mast cells release cytokines without degranulating?

A

Yeah

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21
Q

Does mast cell degranulation affect all body organs?

A

Yeah

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22
Q

What does nitric oxide do?

A

Vasodilator

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23
Q

Which two cell types have lots of histamine?

A

Basophils, mast cells

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24
Q

What is measured in a 24-hour urine collection to diagnose systemic mastocytosis?

A

N-methylhistamine/1,4-methylimidazole acetic acid

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25
Q

Why are opioids often given in conjunction with antihistamines?

A

Opiates degranulate mast cells causing histamine release and hypotension, so antihistamines are given.

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26
Q

What is Cemetidine?

A

A H-2 receptor antagonist that treats acid reflux and also inhibits microsomal liver CYP450 resulting in increased estrogen levels –> gynecomastia and psychological problems

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27
Q

What’s up with H. pylori?

A

It causes gastritis and likes low pH in GI tract.

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28
Q

What do gastrin and acetylcholine do to the stomach?

A

Increase gastric acid secretion

29
Q

Selective serotonin reuptake inhibitors (SSRIs) can be used to treat _______. They also antagonize ________ receptors.

A

depression. They antagonize Ach muscarinic receptors

30
Q

What drug treats carcinoid tumors?

A

Cyproheptadine

31
Q

H-1 receptor antagonists are also ______ receptor angatonists.

A

Ach-muscarinic

32
Q

Prophylactic treatment of asthma involves blocking ______ receptors whereas treatment of an acute attack involves stimulating _______ receptors.

A

leukotriene receptors for phophylactic, beta 2 stimulation for acute attacks

33
Q

contain more mast cells and have a higher chance of developing release of histmaine from them

A

mastocytosis

34
Q

mast cells releases

A

phospholipid metabolites

35
Q

arachidonoic acid

A

the common denominator for

36
Q

PAF is _______ lived

A

short

37
Q

why did rofecoxib lead to increased risk of MI?

A

because it inhibits prostacyclin

38
Q

cytotec

A

protects the GI from NSAID usage

39
Q

considered the key mediators in asthma

A

leukotrienes

40
Q

montelukast

A

one of the most potent tx of asthma by blocking the leukotriene receptor

41
Q

Omalizumab

A

anti-IgE antibody–> neutralized IgE

42
Q

activates nitric oxide synthase

A

bradykinin

43
Q

converting enzyme–> converts angiotensin I to angiotensing II and it is a potent vasoconstrictor

A

kininase

44
Q

check for _________________ in patients sensitive to histamine sontaining foods

A

DOA deficiency

45
Q

N-Methylhistamine

A

measured in a 24hr urine (cold) to diagnose systemic mastocytosis

46
Q

histamine binds to

A

H1 and H2 receptor

47
Q

H1 found in

A

blood vessels

48
Q

H2 found in

A

exocrine glands, gastric and pariteal glands

49
Q

Benadryl is a

A

H1 antagonist

50
Q

Hydroxine is a

A

H1 antagonist but also it is anxiolytic and augmene morphine analgesia (vasodilation and hypotension)

51
Q

D

A

stands for decongestant

52
Q

H2 receptro stimulation leads to

A

gastric acid secretion

53
Q

acid pump inhibitor

A

omeprazole

54
Q

Blockage of H2 receptors decreases gastric acid secretion also in response to gastrin and acetylcholine secreted from the

A

vagus nerve

55
Q

flushing, hypotension, diarrhea, and right heart failure (serotonin is inactivated in the lung and does not affect the left side of the heart)

A

Carcinoid syndrome:

56
Q

due to cerebrovascular constriction, following acute elevations

A

Migraines

57
Q

Sleep due to increased amount in the

A

median raphe nucleus of the pons

58
Q

MIGRAINE agonists like sumatriptan and antimigraine

A

DILATION FIRST AND THEN CONSTRICTION

59
Q

ondansetron (zofran)

A

inhibits 5HT3 CNS/gastric

60
Q

Flushing of the face associated with

A

increased plasma levels

61
Q

ergot alkaloids leads to

A

vasonconstriction

62
Q

severe, generalized with radiation to neck

A

meningitis

63
Q

unilaterla or bilateral throbbing

A

migraine

64
Q

thunderclap, diffuse

A

subarachnoid hemorrhage

65
Q

migraine headaches occurs more in

A

woman

66
Q

muscle tension headache uses for tx

A

acetaminophen/NSAIDs

67
Q

migraine tx.- wake up from sleep feeling refreshed

A

erenumab- calcitoning gene related peptide receptor antagonist
ergotamine, sumatripne (abortive)

68
Q

cluster headache- wake up from sleep with a headache

A

indomethacin, prednisone, topiramate