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STEP 1 (2) > Musculoskeletal/Skin/CT- Pharmacology > Flashcards

Musculoskeletal/Skin/CT- Pharmacology Flashcards

1
Q

What breaks down membrane phospholipids to arachidonic acid?

A

phospholipase A2

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2
Q

What drugs prevent the action of phospholipase A2?

A

corticosteroids (e.g. cortisone, hydrocortisone, prednisone,, dexamethasone)

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3
Q

What two things can happen to arachidonic acid?

A

1) lipoxygenase can convert it to 5-HPETE
2) COX1/2 can convert it to the cyclic endoperoxides (prostacyclin (PGI2), prostaglandins, and thromboxane (TXA2))

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4
Q

What drug can inhibit the action of lipoxygenase?

A

Zileuton (used in tx of asthma)

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5
Q

5-HPETE is converted to leuktrienes such as LTC4, LTD4, LTE4, and LTB4. What does LTB4 do?

A

neutrophil chemotaxis

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6
Q

5-HPETE is converted to leuktrienes such as LTC4, LTD4, LTE4, and LTB4. What do LTC4, LTD4, and LTE4 do?

A

increase bronchial tone

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7
Q

What are some leukotriene (mostly LTC4, LTD4, LTE4) receptor anatagonists?

A

Montelukast (asthma tx), Zafirlukast

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8
Q

What drugs inhibit COX1 and COX2?

A

Aspirin (irreversible)

NSAIDs (indomethacin, Ibuprofen, Naproxen, Ketorlac, Diclofenac)

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9
Q

What is an exclusive COX-2 inhibitor?

A

Celecoxib

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10
Q

What does PGI2 do?

A

decrease platelet aggregation and vascular tone (inhibitor= epoprostenol)

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11
Q

What does PGE1 do?

A

decrease vascular tone (inhibitor= alprostadil)

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12
Q

What does PGE2 and PGF2 do?

A

increase uterine tone (inhibitor PGE2= dinoprostone; inhibitor PGF2= carboprost)

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13
Q

What does acetominophen (Tylenol) do?

A

reversibly inhibit COX, mostly in the CNS. Inactivated peripherally

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14
Q

What are the uses of Tylenol?

A

antipyreitc, analgesic, but NOT anti-inflammatory

Viral infections in children (do not use Aspirin; Reyes syndrome)

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15
Q

What are the AEs of acetaminophen?

A

hepatic necrosis in overdose due to accumulation of NAPQI (antidote= N-acetylcysteine)

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16
Q

How does aspirin work?

A

irreversibly inhibits COX1 and COX2 via acetylation, which decreases the synthesis of TXA2 and prostaglandins

17
Q

What effect does aspirin have on BT, PT, and PTT?

A

increased BT

no effect on PT or PTT

18
Q

What are the uses of aspirin?

A

Low dose (less than 300mg/day): decrease platelet agg

Medium dose (300-2400mg/day): antipyretic and analgesic

High dose (2400-4000mg/day): anti-inflammatory

19
Q

What are the AEs of aspirin?

A

gastric ulceration

tinnitus

chronic use can lead to acute renal failure, interstitial nephritis, GI bleeding

Reyes syndrome in children

20
Q

What effect does aspirin have on pH?

A

causes respiratory alkalosis early, but transitions to mixed metabolic acidosis-respiratory alkalosis

21
Q

What advantage does Celecoxib have?

A

it reversibly inhibits specifically COX2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain but spares COX-1, which helps maintain gastric mucosa. Thus, does not have the corrosive effects of other NSAIDs on the GI lining.

Also spares the function of TXA2 (plateley aggregator)

22
Q

What are the main uses of celecoxib?

A

rheumatoid arthritis and osteoarthritis

23
Q

What are the AEs of celecoxib?

A

risk of thrombosis and sulfa allergy

24
Q

What are the AEs of NSAIDs (e.g. Indomethacin, naproxen, ibuprofen)?

A

interstitial nephritis, gastric ulcer, renal ischemia

25
Q

What is Aledronate?

A

a bisphosphonate, a pyrophosphate analog that binds hydroxyapatite in bone, inhibiting osteoclast activity for tx of osteoporosis, hypercalcemia, and Paget disease of bone

26
Q

What are the main AEs of bisphosphonates?

A

corrosive esophagitis, jaw osteonecrosis

27
Q

What is Teriparatide?

A

rcombinant PTH analog given subQ daily to increase osteoblastic activity for tx of osteoporosis

28
Q

What are the drugs used for tx of chronic gout (preventative)?

A

-allopurinol, febuxostat, pegloticase, and probenecid

29
Q

What does allopurinol do?

A

inhibits xanthine oxidase after being converted to alloxanthine, and decreases conversion of xanthine to uric acid

30
Q

What is another use of allopurinol?

A

lymphoma and leukemia to prevent TLS associated urate nephropathy

31
Q

Allopurinol increases the conc of what drugs?

A

azathiopurine and 6-MP (both normally metabolizes by xanthine oxidase)

32
Q

What does feboxustat do?

A

inhibit xanthine oxidase

33
Q

What is Pegloticase?

A

a recombinant uriace that catalyzes the metabolism of uric acid to allantion (a more water soluble product)

34
Q

How does probenecid help in gout tx?

A

it inhibits reabsorption of uric acid in the proximal convoluted tubules (also inhibits secretion of penicillin)

35
Q

How is an acute gout attack tx?

A

NSAIDs, steroids, and colchicine

36
Q

What are the main NSAIDs used for gout tx?

A

indomethacine and naproxen

37
Q

How does colchicine work?

A

It binds and stabilizes tubulin to inhibit microtubules polymerization, impairing neutrophil chemotaxis and degranulation

STEP 1 (2) (16 decks)

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