Autonomic pharmacology pt. 3: Autacoids

Question 1

Leukotrienes are generated from _______ using the enzyme ________.

Answer 1

arachidonic acid, lipooxygenase

Question 2

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

Answer 2

Lungs. Causes bronchoconstriction

Question 3

How is asthma commonly treated?

Answer 3

With leukotriene receptor antagonists.

Question 4

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

Answer 4

GI tract and kidneys

Question 5

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

Answer 5

Kidneys

Question 6

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

Answer 6

MI or thrombotic stroke

Question 7

Why do NSAIDs cause AEs like GI ulceration and bleeding?

Answer 7

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.

Question 8

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

Answer 8

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.

Question 9

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

Answer 9

Yeah

Question 10

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

Answer 10

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

Question 11

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

Answer 11

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

Question 12

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

Answer 12

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

Question 13

What do bradykinins do?

Answer 13

Vasodilation and pain

Question 14

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

Answer 14

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

Question 15

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

Answer 15

Yeah

Question 16

In which organ is the majority of serotonin found?

Answer 16

GI (~80%)

Question 17

What does serotonin do to smooth muscle?

Answer 17

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

Question 18

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

Answer 18

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

Question 19

Where are mast cells located?

Answer 19

Perivascularly and close to nerve endings

Question 20

Can mast cells release cytokines without degranulating?

Answer 20

Yeah

Question 21

Does mast cell degranulation affect all body organs?

Answer 21

Yeah

Question 22

What does nitric oxide do?

Answer 22

Vasodilator

Question 23

Which two cell types have lots of histamine?

Answer 23

Basophils, mast cells

Question 24

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

Answer 24

N-methylhistamine/1,4-methylimidazole acetic acid

Question 25

Why are opioids often given in conjunction with antihistamines?

Answer 25

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

Question 26

What is Cemetidine?

Answer 26

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

Question 27

What's up with H. pylori?

Answer 27

It causes gastritis and likes low pH in GI tract.

Question 28

What do gastrin and acetylcholine do to the stomach?

Answer 28

Increase gastric acid secretion

Question 29

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

Answer 29

depression. They antagonize Ach muscarinic receptors

Question 30

What drug treats carcinoid tumors?

Answer 30

Cyproheptadine

Question 31

H-1 receptor antagonists are also ______ receptor angatonists.

Answer 31

Ach-muscarinic

Question 32

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

Answer 32

leukotriene receptors for phophylactic, beta 2 stimulation for acute attacks

Question 33

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

Answer 33

mastocytosis

Question 34

mast cells releases

Answer 34

phospholipid metabolites

Question 35

arachidonoic acid

Answer 35

the common denominator for

Question 36

PAF is _______ lived

Answer 36

short

Question 37

why did rofecoxib lead to increased risk of MI?

Answer 37

because it inhibits prostacyclin

Question 38

cytotec

Answer 38

protects the GI from NSAID usage

Question 39

considered the key mediators in asthma

Answer 39

leukotrienes

Question 40

montelukast

Answer 40

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

Question 41

Omalizumab

Answer 41

anti-IgE antibody--> neutralized IgE

Question 42

activates nitric oxide synthase

Answer 42

bradykinin

Question 43

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

Answer 43

kininase

Question 44

check for _________________ in patients sensitive to histamine sontaining foods

Answer 44

DOA deficiency

Question 45

N-Methylhistamine

Answer 45

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

Question 46

histamine binds to

Answer 46

H1 and H2 receptor

Question 47

H1 found in

Answer 47

blood vessels

Question 48

H2 found in

Answer 48

exocrine glands, gastric and pariteal glands

Question 49

Benadryl is a

Answer 49

H1 antagonist

Question 50

Hydroxine is a

Answer 50

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

Question 51

D

Answer 51

stands for decongestant

Question 52

H2 receptro stimulation leads to

Answer 52

gastric acid secretion

Question 53

acid pump inhibitor

Answer 53

omeprazole

Question 54

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

Answer 54

vagus nerve

Question 55

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

Answer 55

Carcinoid syndrome:

Question 56

due to cerebrovascular constriction, following acute elevations

Answer 56

Migraines

Question 57

Sleep due to increased amount in the

Answer 57

median raphe nucleus of the pons

Question 58

MIGRAINE agonists like sumatriptan and antimigraine

Answer 58

DILATION FIRST AND THEN CONSTRICTION

Question 59

ondansetron (zofran)

Answer 59

inhibits 5HT3 CNS/gastric

Question 60

Flushing of the face associated with

Answer 60

increased plasma levels

Question 61

ergot alkaloids leads to

Answer 61

vasonconstriction

Question 62

severe, generalized with radiation to neck

Answer 62

meningitis

Question 63

unilaterla or bilateral throbbing

Answer 63

migraine

Question 64

thunderclap, diffuse

Answer 64

subarachnoid hemorrhage

Question 65

migraine headaches occurs more in

Answer 65

woman

Question 66

muscle tension headache uses for tx

Answer 66

acetaminophen/NSAIDs

Question 67

migraine tx.- wake up from sleep feeling refreshed

Answer 67

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

Question 68

cluster headache- wake up from sleep with a headache

Answer 68

indomethacin, prednisone, topiramate