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PDSA > Block 5 Jones > Flashcards

Block 5 Jones Flashcards

1
Q

how is histamine produced?

A

L-histidine is decarboxylated by histidine decarboxylase

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2
Q

where is most histidine stored

A

mast cells

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3
Q

describe the 4 receptor subtypes of histidine, including their post-receptor mechanism and where they’re found

A

H1 - smooth muscle, endothelium, brain; Gq coupled (IP3 and DAG increase)

H2 - gastric mucosa, cardiac muscle, mast cells, brain; Gs coupled, increase cAMP

H3 - presynaptic autoreceptors and heteroreceptors, brain, myenteric plexus; Gi coupled (decrease cAMP)

H4 - eosinophils, neutrophils, CD4s; Gi coupled (decrease cAMP)

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4
Q

H1 receptors are similar to _____ and H2 receptors are similar to ______

A

muscarinic

serotonergic

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5
Q

H1 stimulation leads to ______ and inhibition leads to ______

A 
stimulation = arousal
inhibition = sedation
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6
Q

H2 receptor antagonists are used for

A

blocking histamine release from ECL cells, which decreases the stimulation and subsequent release of protons into the stomach
- this decreases stomach acid in treatment of GERD/acid reflux and peptic ulcers

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7
Q

IgE binds to _______ on mast cells

A

FC-epsilon-R1 receptors

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8
Q

____ receptors have very important chemotactic effects on eosinophils and mast cells

A

H4

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9
Q

____ receptors in the vestibular system send stimuli to the vomiting center to generate motion sickness

A

H1

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10
Q

contrast 1st and 2nd generation histamine antagonists

A

1st - better sedative effects and have better MR affinity and BBB permeability

2nd - are substrates for P-glycoprotein and are rapidly effluxed; less MR affinity

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11
Q

2nd generation H1 antagonists are used for

A

seasonal allergies

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12
Q

H2 receptor antagonists are used exclusively for

A

stomach acid reducers due to their MOA

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13
Q

give examples of H2 receptor antagonists

A

Axid (nizatidine)
Pepcid (famotidine)
Tagamet (cimetidine)
Zantac (ranitidine)

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14
Q

deficiency in _______ results in depression

A

serotonin

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15
Q

serotonin is synthesized from ______ by hydroxylation of the indole followed by decarboxylation of the amino acid

A

L-tryptophan

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16
Q

which serotonin receptor is not GPCR coupled

A

5-HT3

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17
Q

where are 5-HT3 receptors located?

A

in the GIT and the VC and CTZ, allowing them to participate in the vomiting reflex

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18
Q

the release of serotonin by EC cells from the gut stimulates EPANs via _______, which are ligand gated ion channels that signal the VC

A

5-HT3

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19
Q

stimulating which receptors will cause a response in IPANs?

A

5-HT1P

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20
Q

what happens when IPANs are activated?

A

it activates the enteric neurons responsible for peristaltic and secretory reflex activity

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21
Q

5-HT4 receptors are heteroreceptors with ______ feedback; they release ____ which causes…

A

positive

Gs

enhanced release

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22
Q

antiemetics that target 5HT receptors target which one?

A

5-HT3

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23
Q

what disease state do partial agonists of 5-HT4 treat?

A

IBS-C

24
Q

treatment of depression is done by…

A

enhancement of endogenous 5HT postsynaptic activity by inhibition of pre-synaptic reuptake via SERT inhibitors
- SSRIs = sleective serotonin reuptake inhibitors

25
Q

what kind of lipase removes AA from the membrane?

A

PLA2

26
Q

identify the three forms of PLA2 that play a role in removing AA from the membrane.

A

cPLA2 - cytosolic, calcium dependent, does most of the actual removal
sPLA2 - secretory (inducible), calcium dependent, can be induced when you need lots of AA
iPLA2 - independent; most of the AA removed by it is put back in the membrane

27
Q

what are the 4 pathways by which AA is oxygenated?

A

COX
LOX
CYP450

nonenzymatically - isoeicosanoid

28
Q

which COX enzyme provides for “housekeeping” functions

A

COX1

29
Q

what kind of inducers can “induce” COX2

A

shear stress
growth factors
tumor promoters
cytokines

30
Q

due to the nature of its main producers, ____ is the main source of prostanoids in inflammation and cancer

A

COX2

31
Q

ibuprofen inhibits

A

COX1 and COX2 - non selective

32
Q

Celecoxib, diclofenac, and meloxicam inhibit

A

COX 2 selectively

33
Q

Aspirin inhibits

A

both COX 1 and 2 irreversibly

34
Q

What are the COX metabolites

A

prostaglandins
prostacyclins
thromboxanes

35
Q

what is PGI2 used for

A

smooth muscle relaxation effects to maintain the ductus arteriosus in patients

36
Q

PGE2 and PGF2-alpha are used to

A

induce labor

37
Q

latanoprost is

A

topically active PGF2-alpha used to treat glaucoma/ocular hypertension

38
Q

PGI2 is used by _____ as a _____

A

vascular endothelium

powerful vasodilator (inhibits platelet aggregation)

39
Q

what is the MoA of thromboxane (TXA2)

A

stimulates platelet aggregation and vasoconstriction

40
Q

why is PGE2 special?

A

its effects on platelet aggregation are dose-dependent

  • low concentrations = enhance
  • high concentrations = inhibit
41
Q

5LOX gives rise to…

A

leukotrienes

42
Q

four approaches to anti-leukotriene drugs are

A

1 - inhibit 5 LOX
2 - cysteinyl leukotriene receptor antagonists
3 - FLAP (5-lox activating protein) inhibitors
4 - PLA2 inhibitors (which block all AA derivatives)

43
Q

alpha-melanocyte stimulating hormone (alpha-MSH) is released when

A

ACTH levels are very high. it results in stimulation of synthesis and distribution of melanin
- this is why addison’s diease often results in hyperpigmentation

44
Q

secretion of the mineralocorticoid aldosterone is primarily under the influence of

A

angiotensin 2

45
Q

glucocorticoids are made in the

A

zona fasciculata

46
Q

all GCs are highly _____

A

lipophilic

47
Q

what is the main GC?

A

cortisol

48
Q

what is the effect of GC on serum glucose levels

A

increase

49
Q

how do GCs affect inflammation and the immune system

A

inhibit the functions of immune cells and suppress release of pro-inflammatory cytokines and PGs

50
Q

glucocorticoid receptors are found

A

on the nuclear membrane because they’re part of the nuclear receptor family of TFs

51
Q

______ is the most important mineralocorticoid in humans

A

aldosterone

52
Q

where is aldosterone synthesized?

A

zona glomerulosa of the adrenal gland

53
Q

_____ is used in the treatment of adrenocortical insufficiency (AKA _______). the MOA is…

A

fludrocortisone

Addison’s Disease

is an MR with non-selective GR agonist acitivity

54
Q

spironolactone is used in the treatment of

A

hyperaldosteronism

55
Q

what is Cushing’s disease

A

a pituitary disorder

is caused by excessive ACTH

causes secondary dysfunction of the adrenal glands

PDSA (6 decks)

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