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Step 1 Pharmacology > MSK Pharm > Flashcards

MSK Pharm Flashcards

1
Q

lipoxygenase produces

A

Leukotriens

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2
Q

cyclooxygenase produces

A

Prostacyclin (PGI2), Prostaglandins (PGE2, PGF2alpha), Thromboxane (TXA2)

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3
Q

LTB4 function

A

Neutrophil chemotaxis [PMNs arrive B4 others]

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4
Q

LTC4, D4, and E4

A

BRONCHOCONSTRICTION, vasoconstriction, contraction of smooth muscle, inc. vascular permeability

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5
Q

PGI2

A

Prostacyclin, inhibits platelet aggregation and promotes vasodilation. [Platelet-Gatherin Inhibitor]

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6
Q

What are the intermediates for lipo and cyclooxygenases

A

Hydroperoxides (HPETEs for Lip-), Endoperoxides (PGG2, PGH2 for Cyclo-)

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7
Q

What does Zileuton block

A

lipoxygenase

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8
Q

What does Zafirlukast, montelukast MOA

A

Blocks actions of LTC4,D4,E4

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9
Q

What is the substrate for all oxygenases

A

Arachidonic acid made via. phospholipase A2 from e.g. phosphatidylinositol

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10
Q

PGE2, PGF2alpha actions

A

inc. uterine tone

dec. bronchial tone

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11
Q

TXA2 actions

A

inc. platelet agg.
inc. vascular ton
inc. bronchial tone

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12
Q

Lifetime of platelets

A

Around 7 Days

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13
Q

Dosage range uses for aspirin

A

Low dose <300 is dec. platelet aggregation, intermediate dose 300-240 is antipyretic and analgesic. high dose (2400-4000 mg/day) is anti-inflammatory

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14
Q

Aspirin toxicity

A

Gastric ulceration, tinnitus (CN VIII). Chronic use: acute renal fialure, interstitial nephritis, upper GI bleeding.

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15
Q

Aspirin block of COX

A

irreversible inhibits COX-1 and COX-2.

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16
Q

COX-1 product

A

TXA2, PGI2 (in gut) (Platelet action and Gut Mucosa, hence why aspirin (low Km for COX-1) messes these up)

17
Q

COX-2 product

A

PGI2 in blood vessels (much more than COX-1), this inhibition of PGI2 leads to the CV effects. Also produces prostaglandins in inflammatory cells, vascular endothelium, and mediates inflammation and pain.

18
Q

COX-2 is found where

A

Found in inflammation, not constitutively active like COX-1. Hence why stopping it reduces inflammation. But when you block it’s anticoagulant properties without blocking the procoagulant properties of COX-1, you get an MI!

19
Q

Celecoxib specific moeity

A

Sulfa drug, so sulfa allergy possible.

20
Q

Acetaminophen MOA

A

inhibits reversibly cyclooxygenase mostly in CNS. inactivated peripherally

21
Q

Acetaminophen uses

A

Antipyretic, analgesic, but not anti-inflammatory. Use in children instead of aspirin in viral infection.

22
Q

Acetaminophen toxic metabolite and antidote

A

NAPQI: depletes glutathione and forms toxic adducts in liver.
N-acetylcysteine: regenerates glutathione

23
Q

Bisphosphonates MOA

A

pyrophosphate analogs, binds hydroxyapatite in bone, inhibiting osteoclast activity

24
Q

Bisphosphonates use

A

Osteoporosis, hypercalcemia, Paget disease of bone

25
Q

Bisphosphonate toxicity

A

Corrosive esophagitis (sit upright for 30 minutes afterwards, take with glass of water), osteonecrosis of jaw.

26
Q

Allopurinol MOA

A

inhibits xanthine oxidase

27
Q

Allopurinol uses

A

Gout, prevents tumor lysis associated urate nephropathy in lymphoma and leukemia.

28
Q

Allopurinol drug interacts

A

inc. azathioprine and 6-MP concentrations (both normally inhibited by xanthine oxidase)
Salicylates?

29
Q

Allopurinol and Salicylates

A

Salicylates are ANTIURICOSURIC.?????????????????????

30
Q

Salicylates and diuretics and uric acid metabolism

A

All decreases Tubular secretion of uric acid

31
Q

Febuxostat MOA

A

inhibits xanthine oxidase

32
Q

probenecid

A

inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)

33
Q

Acout drugs used for gout

A

NSAIDs, steroids, golchicine

34
Q

Colchine MOA for gout

A

binds and stabilizes tubulin to inhibit microtubule polymerization, imparing leukocyte chemotaxis and degranulation. Acute and prophylactic value. GI side effects.

35
Q

TNF-alpha inhibitors

A

Etanercept and Inflmixmab,adalimumab

All prevent activation of macrophages and destruction of phagocytosed microbes.

36
Q

Etanercept MOA

A

Fusion protein (receptor for TNF-alpha and IgG1 Fc) that is a TNF decoy receptor. [Etanercept is a TNF decoy reCEPTor]

37
Q

Infliximab, adalimumab MOA

A

anti-TNFalpha monoclonal antibody

38
Q

Etanercept use

A

RA, psoriasis, ankylosing spondylitis

39
Q

Infliximab, adalimumab

A

IBD, RA, ankylosing spondylitis, psoriasis

Step 1 Pharmacology (17 decks)

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