Musculo - Pharmacology Flashcards

1
Q

What does the lipoxygenase pathway of the arachidonic acid pathway yield?

A

Leukotrienes (remember: L for Lipoxygenase and Leukotrienes)

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2
Q

Which arachidonic acid product is a neutrophil chemotactic agent?

A

Leukotriene B4(remember: Neutrophils arrive B4 others)

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3
Q

What effect do leukotrienes C4, D4, and E4 have on the bronchi and the bronchioles?

A

Bronchoconstriction

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4
Q

What effect do leukotrienes C4, D4, and E4 have on the vasculature?

A

Vasoconstriction and increase vascular permeability

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5
Q

What effect does prostacyclin (PGI2) have on platelets?

A

Inhibits platelet aggregation (remember Platelet-Gathering Inhibitor)

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6
Q

What effect does prostacyclin (PGI2) have on the vasculature?

A

Promotes vasodilation

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7
Q

What is the first step of the arachidonic acid pathway?

A

Membrane lipids are converted to arachidonic acid by phospholipase A2

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8
Q

Within the arachidonic acid cascade, what two enzymes use arachidonic acid as their substrate?

A

Lipoxygenase and cyclooxygenase

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9
Q

What drug inhibits the enzyme lipoxygenase?

A

Zileuton

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10
Q

What are the two mechanisms of action of steroids on the arachidonic acid pathway?

A

Steroids inhibit the action of phospholipase and inhibit the synthesis of cyclooxygenases

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11
Q

Cyclooxygenase directly converts arachidonic acid into what category of compounds resulting in what two products?

A

Endoperoxides; prostaglandins G and H

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12
Q

Hydroperoxides are the precursors of what class of arachidonic acid products?

A

Leukotrienes

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13
Q

Endoperoxides are the precursors of what three arachidonic acid products?

A

Prostacyclin, prostaglandins, and thromboxane

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14
Q

List two drugs that inhibit leukotrienes from producing an increase in bronchial tone.

A

Zafirlukast and montelukast

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15
Q

Name three effects of prostacyclin.

A

Prostacyclin decreases platelet aggregation, causes vasodilation and decreases uterine tone

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16
Q

Name four effects of prostaglandins on the body.

A

Prostaglandins cause a decrease in vascular tone, increase in pain, increase in uterine tone, increase in temperature

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17
Q

Zileuton inhibits the conversion of _____ to _____.

A

arachidonic acid to hydroperoxides

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18
Q

Aspirin _____ (reversibly/irreversibly) inhibits cyclooxygenase.

A

Irreversibly

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19
Q

Aspirin causes a decrease in synthesis of what two products?

A

Thromboxane and prostaglandins

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20
Q

At what dose does aspirin cause decreased platelet aggregation?

A

Low-dose; < 300 mg/day

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21
Q

At what dose does aspirin have antipyretic and analgesic properties?

A

Intermediate dose; 300-2400 mg/day

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22
Q

At what dose does aspirin have antiinflammatory properties?

A

High dose; 2400-4000 mg/day

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23
Q

What is a common toxicity of aspirin use?

A

Gastric upset

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24
Q

Chronic use of aspirin can cause what three problems?

A

Acute renal failure, interstitial nephritis, and upper gastrointestinal bleeding

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25
Q

What syndrome can develop in children with viral illnesses who are given aspirin?

A

Reyes syndrome

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26
Q

Name four examples of nonsteroidal antiinflammatory drugs.

A

Ibuprofen, naproxen, indomethacin, and ketorolac

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27
Q

Nonsteroidal antiinflammatory drugs work by reversibly inhibiting what substance?

A

Cyclooxygenase

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28
Q

Do ibuprofen, naproxen, indomethacin, and ketorolac inhibit cyclooxygenase-1, cyclooxygenase-2, or both?

A

Both

29
Q

Nonsteroidal antiinflammatory drugs block the synthesis of what substance?

A

Prostaglandins

30
Q

What are the three effects of administration of nonsteroidal antiinflammatory drugs?

A

They are antipyretics, analgesics, and antiinflammatory agents

31
Q

Which nonsteroidal antiinflammatory drug is used to close a patent ductus arteriosus?

A

Indomethacin

32
Q

What four toxicities are associated with nonsteroidal antiinflammatory drugs?

A

Renal damage, aplastic anemia, gastrointestinal distress, and ulcers

33
Q

How do cyclooxygenase-2 inhibitors differ from other nonsteroidal antiinflammatory drugs?

A

Reversibly inhibit cyclooxygenase-2, found in inflammatory cells and vascular endothelium, mediates inflammation and pain; unlike nonsteroidal antiinflammatory drugs, it spares cyclooxygenase-1

34
Q

Explain the mechanism by which cyclooxygenase-2 inhibitors help maintain the gastric mucosa.

A

Cyclooxygenase-2 inhibitors do not affect the cyclooxygenase-1 enzymes that produce the prostaglandins that protect the gastric mucosa

35
Q

What are the two clinical indications for using cyclooxygenase-2 inhibitors?

A

To treat rheumatoid arthritis and osteoarthritis

36
Q

Individuals with an allergy to _____ should avoid taking cyclooxygenase-2 inhibitors.

A

Sulpha

37
Q

There is an increased risk of _____ when taking cyclooxygenase-2 inhibitors.

A

Thrombosis

38
Q

Acetaminophen reversibly inhibits what substance in the central nervous system?

A

Cyclooxygenase

39
Q

Acetaminophen has antipyretic and analgesic activities but lacks what other property that is common to nonsteroidal antiinflammatory drugs?

A

Antiinflammatory properties

40
Q

What are the physiologic effects of an acetaminophen overdose?

A

Hepatic necrosis

41
Q

Acetaminophens metabolite depletes what reducing substance in hepatic cells?

A

Glutathione

42
Q

What is the antidote to acetaminophen toxicity?

A

N-acetylcysteine; regenerates glutathione depleted by acetaminophen overdose

43
Q

True or False? Acetaminophen has antiinflammatory activity.

A

False; acetaminophen is an nonsteroidal antiinflammatory drug without antiinflammatory activity

44
Q

Aspirin is a Nonsteroidal Antiinflammatory Drug with what additional activity?

A

Antiplatelet activity

45
Q

Name four bisphosphonates.

A

Etidronate, pamidronate, alendronate, and risedronate

46
Q

What is the mechanism of action of bisphosphonates?

A

Inhibit osteoclastic activity

47
Q

Name three clinical indications for use of bisphosphonates.

A

Malignancy-associated hypercalcemia, Pagets disease of bone, postmenopausal osteoporosis

48
Q

Name the three major toxicities of bisphosphonates.

A

Corrosive esophagitis, nausea, and diarrhea

49
Q

Is colchicine used to treat chronic gout or acute gout?

A

Acute gout

50
Q

Which medication used for gout depolymerizes microtubules, thereby impairing leukocyte chemotaxis and degranulation?

A

Colchicine

51
Q

Colchicine has adverse effects related to which organ system, especially when taken orally?

A

The gastrointestinal system

52
Q

Which medication is used more often to treat acute gout because it causes less toxicity than colchicine?

A

Indomethacin

53
Q

Is probenecid used to treat chronic gout or acute gout?

A

Chronic gout

54
Q

Which medication for gout inhibits the reabsorption of uric acid and the secretion of penicillin?

A

Probenecid

55
Q

Is allopurinol used to treat chronic gout or acute gout?

A

Chronic gout

56
Q

Which treatment for gout inhibits xanthine oxidase, which decreases the conversion of xanthine oxidase into uric acid?

A

Allopurinol

57
Q

Which treatment for gout inhibits xanthine oxidase and is used to prevent tumor-lysis-associated urate nephropathy in individuals with lymphomas and leukemias?

A

Allopurinol

58
Q

Allopurinol causes increased serum levels of which drugs if taken concurrently?

A

Azathioprine and 6-MP; both normally metabolized by xanthine oxidase, which is inhibited by allopurinol

59
Q

What drug should not be used to treat gout?

A

Salicylates, which depress uric acid clearance

60
Q

What substance is converted to uric acid for excretion from the body? What are the intermediates?

A

Purines; hypoxanthine and xanthine

61
Q

Which two reactions are inhibited by allopurinol and catalyzed by xanthine oxidase?

A

Conversion of hypoxanthine to xanthine and conversion of xanthine to uric acid

62
Q

Which two drugs inhibit the tubular reabsorption of uric acid?

A

Probenecid and high-dose salicylates

63
Q

Which two drugs inhibit the tubular secretion of uric acid?

A

Diuretics and low-dose salicylates

64
Q

List three clinical uses for etanercept.

A

Rheumatoid arthritis, psoriasis, and ankylosing spondylitis

65
Q

A patient with Crohn’s disease presents for treatment with infliximab. What infection does the physician worry about reactivating?

A

Latent tuberculosis

66
Q

List three clinical uses for infliximab.

A

Crohn’s disease, rheumatoid arthritis, and ankylosing spondylitis

67
Q

Name the drug with the following mechanism: directly binds tumor necrosis factor receptor sites.

A

Adalimumab

68
Q

List three clinical uses for adalimumab.

A

Rheumatoid arthritis, psoriasis, and ankylosing spondylitis

69
Q

Name the drug with the following mechanism: recombinant form of human tumor necrosis factor receptor that binds tumor necrosis factor.

A

Etanercept (remember: EtanerCEPT is a TNF decoy reCEPTor)