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Immunology & Inflammation > Exam 3-McPhail > Flashcards

Exam 3-McPhail Flashcards

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1
Q

Calcineurin/mTOR inhibitors

A

Cyclosporine
FK-506
Rapamycin
Everolimus

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2
Q

Antimetabolites

A

Azathioprine

Mycophenolate

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3
Q

NSAIDs

A

COX/LOX inhibitors

Ibuprofen, naproxen

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4
Q

Mast Cell Stabilizers

A

Cromolyn

Neodocromil

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5
Q

Cyclosporine (Sandimmune, Neoral)

A

produced by fungi (natural)
Inhibits T cell signal transductions like IL2 that would express lymphocytes
Can’t translocate to the nucleus
increases TGF(B)

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6
Q

Forms a complex with cyclophilin A then binds to calcineurin to inhibit calcium stimulated phosphorylation of cytosolic NFAT

A

Cyclosporine

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7
Q

Cyclosporine indications

A

kidney, liver, heart transplants
used in combo with glucocorticoids

RA, psoriasis, Chron’s Disease, Eyes (Restasis)

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8
Q

Cyclosporine side effects

A

High BP, kidney problems, increased risk of infection and cancer because immune system is suppressed, more hair growth, gum hyperplasia, diarrhea, vomit, loss of app.

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9
Q

AVOID while on cyclosporine

A 
contact with people with infectious diseases
immunizations
sunlight--sunburn=inflammation
Grapefruit-inhibits CYP3A4
lots of potential drug interactions
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10
Q

FK-506 (Tacrolimus)

A

produced by bacterium
big macrocycle
Inhibits T cell signal transductions like IL2 that would express lymphocytes
binds to FKBP-12 and then calcineurin+calcium+calmodium

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11
Q

FK-506 side effects

A

High BP, kidney problems, increased risk of infection and cancer because immune system is suppressed, more hair growth, gum hyperplasia, diarrhea, vomit, loss of app.

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12
Q

FK-506 metabolism

A

by CYP3A5

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13
Q

How cyclosporine and FK506 inhibit Tcell activation and proliferation

A

activate other proteins by changing conformation
normally wouldn’t interact with calcineurin
prevent gene transcription

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14
Q

Rapamycin (Sirolimus)

A

polyketide macrocycle produced by bacterium
Binds to FKBP12 and inhibits kinase mTOR
inhibits Tcell activation and prolif downstream of IL2R
so cells still make IL2 but this blocks TCell Response to IL2

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15
Q

Everolimus (zortress)

A

macrocycle used in kidney and liver (not earlier than 30 days after) transplants
identical mechanism of action to rapamycin-FKBP12 and mTOR

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16
Q

Azathioprine (Imuran)

A

antimetabolite that is cleaved to 6-mercatopurine
inhibit DNA biosynthesis, and can inhibit de novo purine biosynthesis
used in kidney transplants and RA

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17
Q

Azathioprine mechanism

A

block the rate limiting enzymes IMPDH, adenylosuccinate synthase, adenylosuccinate lyase
incorporated into DNA as a nucleotide

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18
Q

Mycophenolate mofetil/sodium

A

antimetabolite ester prodrug to increase drug absorption
isolated from fermentation broths of pencillium sp.
inhibits IMPDH, and is more pronounced in lymphocytes

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19
Q

Corticosteroids

A

can bind to different areas, increase genes to fight inflammation and decrease genes that encourage inflammation
diminish production of prostaglandins and leukotrienes by inhibiting COX and PLA2 to decrease arachidonic acid metabolite productions

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20
Q

Arachidonic acid->COX1 & 2

A

->Prostaglandins->initiation of inflammation

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21
Q

Arachidonic acid->5-LO

A

->Leukotrienes->initiation of inflammation

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22
Q

Arachidonic acid->Transcellular biosynthesis

A

->Lipoxins->End inflammation

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23
Q

Arachidonic acid->COX2

A

->5LO->12-epiLipoxins->end inflammation

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24
Q

Eicosanoids

A

produced by cyclooxygenases, lipoxygenases, and cytochrome P450 epoxygenase
don’t need a lot to make a difference in the body

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25
Arachidonic acid
AA | found in cell membranes, regulates apoptosis
26
anandamide
endocannabinoid that produces mind effects like those of cannabis
27
Phospholipase A2
PLA2 regulated by phosphorylation in the presence of Ca2+ is moved from the cytosol to the membrane of nucleus and ER RESPONSIBLE for the release of AA from membrane phospholipids
28
COX catalyzed rate limiting steps
arachidonic acid -> PGG2 (peroxide) -> PGH2 (reduced to OH)
29
TXA2 - Thromboxines
vasoconstriction, platelet aggregation | in platelets
30
PGI2 - Prostacyclin
vasodilation, decreased platelet aggregation blood vessel walls Ex. Epoprostenol (very spread out)
31
PGD2
erythema, edema, pain, decreased platelet aggregation | in mast cells, brain
32
PGE2
erythema, edema, pain, fever in most cell types ex. Dinoprostone, Carboprost cause abortion
33
PGF2
vasoconstriction in uterus ex. Latanoprost
34
Protanoid Receptor Family
prostaglandins bind to these receptors | relaxant, contractile, inhibitory types
35
COX 1 and 2
PGH2 synthase 1 and 2 major targets of NSAIDs have PGG2 and PGH2 activities membrane bound enzymes on luminal side of ER and both sides of nucleus have 2 active sites: COX and peroxidase active site
36
What COX produce
small but significant amounts of 11R-HPETE, 15R-HPETE, 15S-HPETE oxygenation of polyunsaturated fatty acids into bioactive compounds
37
Actives sites of COX1
Arg120-interacts with carboxylate Ser530-residue acetylated by aspirin Tyr385-abstracts pro-S hydrogen to initiate COX rxn
38
COX 1
always expressed, but can be induced involved in homeostasis active site smaller than COX2
39
COX2
inducible but CNS, kidney have high level endothelial cells, fibroblasts, synovial cells undetectable induced by an inflammatory response active site larger than COX1
40
COX3
dogs, brain, APAP possibly
41
aspirin and COX2
15R-HPETE is produced instead of PGG2
42
NSAIDs general Mech of Action (3)
1. rapid reversible binding followed by irreversible covalent modification (aspirin) 2. rapid reversible competitive inhibition (ibuprofen) 3. rapid, lower affinity competitive inhibition followed by time-dependent transition to high affinity poorly reversible inhibitory mode...
43
Salicylic acid structure
phenol+carboxylic acid
44
Aspirin (ASA) | modified at hydroxyl group
irreversibly acetylates serine 530 in COX active site alters COX2 activity to make epi-lipoxins many uses many side effects (GI) 50-6000 mg daily, interacts with warfarin and methotrexate
45
ASA metabolism
ASA->salicylic acid-> salicyluric acid-inactive gentisic acid-inactive
46
Reye's syndrome
salicylates may worsen existing liver or kidney problems fatal consequenc of chicken pox/flu strains hepatic injury and encephalopathy
47
salicylism
mild, chronic salicylate intoxication no antidote, can do dialysis headache, dizzy, tinnitus, hard to hear, dim vision, confused, lazy feeling, drowsy, sweat, thirst, hyperventilate, N/V/D
48
aspirin hypersensitivity (allergic)
uncommon, more females and middle aged previous chem hypersens, asthma, nasal polyps small doses runny nose, hives, bronchospasm, hypotension treat with epinephrine
49
Salsalate | modified at carboxyl group
2 salicyclic acids together | less GI upset than aspirin, insoluble to stomach absorbed in SI
50
Salicylamide | modified at carboxyl group
salicyl chloride+ammonia not hydrolyzed to salicylic acid less effective anti-inflammatory may be used if sensitive to salicylates
51
Flusenisal and Diflunisal | *5-(p-fluorophenyl) derivatives*
2-5 times effective as aspirin 2 times the duration much lower GI irritation mild-moderate pain in dentist, OA and RA
52
Mesalamine | nitrogen containing salicylate
IBS | delayed release, doesn't inhibit COX because not acetate group
53
Sulfasalazine | nitrogen containing salicylate
IBS joined mesalamine and sulfapyridine by diazo link bacteria in bowel cleave the link sulfapyridine inactive but causes side effects like Stevens-Johnson syndrome
54
Olsalazine | nitrogen containing salicylate
IBS | two mesalamines by diazo link
55
Indomethacin | indole-3-acetic acid derivative
potent antiinflam/pyretic drug Actions directly on immune cells cause headache, vertigo, confusion, liver probs not popular time dependent functionally irreversible inhibitor of COX high affinity for COX1 because of 2-methyl group tyrosine385 interacts with aromatic ring
56
Sulindac | arylacetic and arylpropionic acid derivative
``` no Nitrogen like indomethacin sulfoxide increased potency and solubility prodrug, sulfoxide->sulfide active less severe side effects COX1 but some COX2 ```
57
Ketorolac | arylacetic and arylpropionic acid derivative
more potent analgesic, modest antiinflam high COX1 affinity, produces PGE2 use limited to 5 days because of severe side effects
58
Tolmetin Sodium | arylacetic and arylpropionic acid derivative
comparable to ketorolac and sulindac, high COX1 affinity | less frequent side effects but can produce rare anaphylactic shock
59
Diclofenac | arylacetic and arylpropionic acid derivative
substitured acetic acid as selective for COX2 as celecoxib binds to COX2 inverted with carboxylate to TYR and SER
60
Etodoloc | arylacetic and arylpropionic acid derivative
as selective for COX2 as celecoxib | side effects less severe but do have CNS effects because of INDOLE group
61
arylpropionic acid analogs
3 carbon acids all have alpha methyl group, chiral center S=active R=inactive but R->S in body administered as racemates usually nonselective COX inhibitors
62
Ibuprofen | arylpropionic acid analog
racemate, pain and inflammation, GI upset take with food RA and OA, pain, period pain cardiovascular risk not ok for before artery bypass surgery GI risk ulcers and bleeding
63
Naproxen | arylpropionic acid analog
R isomer is toxic so must be only S
64
Meloxicam | enolic acid
RA and OA | hydroxyl group of eneol interacts with TYR and SER of COX2
65
Piroxicam | enolic acid
RA and OA | nonselective and extremely long half life (slow onset)
66
Celecoxib | diaryl hehterocyclic compound
selective COX2 inhibitor | risk of cardiovascular events
67
N-arylanthranilic acid | The Fenamates
mefanamic acid, less than 7 days flufenamic acid-7 times potent as ^^ meclofenamic acid-25 time potent^^ and 150 times aspirin
68
APAP | p-aminophenol derivative
not an NSAID, COX3 not antiinflam but yes antipyretic and analgesic acute overdose normal pathway saturated and depletes GSH(glutathione), reversed with acetylcystine
69
Zileuton | LOX inhibitor
inhibits 5-LOX that converts AA to 5-HPETE | asthma, 2.5 hr half life
70
Zafirleukast | LOX inhibitor
inhibits cys-leukotriene receptor LTD4 asthma interacts with warfarin
71
Montelukast
inhibits cys-leukotriene receptor LTD4 | asthma and allergic rhinitis, ok in kids
72
Cromolyn | Mast Cell Stabilizers
inhibits Cl- channels which may inhibit Ca2+ availability and prevent mast cells from bursting given by inhalation for asthma ok for all ages
73
Nedocromil | Mast Cell Stabilizers
more effective than cromolyn | ok for 12 yo+
74
Olapatidine
antiallergy for eyes | prevent release of histamine and other mediator by preventing calcium influx into mast cells

Immunology & Inflammation (3 decks)

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