Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PBL Pharm Block 3 > Pharm 42 - Eicosanoids > Flashcards

Pharm 42 - Eicosanoids Flashcards

1
Q

Aspirin MOA

A

Irreversible inhibits COX-1 and COX-2 by acetylating the active site serine residue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Aspirin clinical applications

A

Mild-to-moderate pain, HA, myalgia, arthralgia, prophylaxis of stroke and MI (@ low doses -> antiplatelet effect)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Aspirin adverse effects

A

GI ulcer/bleeding, Reye’s syndrome, asthma exacerbation, bronchospasm, angioedema; also tinnitus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Aspirin contraindications

A

Hypersensitivity; aspirin-triggered asthma; chickenpox/flu in children/teens (risk of Reye’s syndrome)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Aspirin therapeutic considerations

A

Increases plasma concentration of acetazolamide -> CNS toxicity; Ibuprofen may inhibit antiplatelet effect; may enhance methotrexate toxicity; increased risk of bleeding in anti coagulated pts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

NSAID MOA and classes

A

Inhibit COX-1 and COX-2, decreasing synthesis of eicosanoids and limiting inflammatory response
Includes Proprionic acids, acetic acids, Oxicams, Fenamates, Ketones

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Priopionic Acids (4)

A

Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Acetic Acids (5)

A

Indomethacin, Sulindac, Etodolac, Diclofenac, Keterolac

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Oxicams (1)

A

Prioxicam (duh)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Fenamates (2)

A

Mefenamate, Meclofenamate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Ketones (1)

A

Nabumetone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

NSAID clinical applications

A

Mild-to-moderate pain, F, OA, RA, dysmenorrhea, gout, PDA closure (indomethacin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

NSAID adverse effects

A

GI hemorrhage/ulceration/perforation, nephrotoxicity, Stevens-Johnson syndrome, pseudoporphyria (naproxen); also tinnitus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

NSAID contraindications

A

GI/intracranial bleeding; coagulation defects; asthma, urticaria, or allergic rxn to NSAIDs including ASA (b/c of risk of fatal anaphylaxis); renal insufficiency

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

NSAID therapeutic considerations

A

1) Naproxen has longer T1/2, more potency, and fewer GI effects than ASA
2) Keterolac is used for 3-5 days post-surgery
3) Piroxicam has long T1/2 - dose once daily
4) Nabumetone has greatest COX-2 selectivity
5) Fenamate is less useful than ASA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Acetominophen MOA

A

COX-3 inhibitor in CNS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Acetominophen clinical applications

A

F, mild-to-moderate pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Acetominophen adverse effects

A

Hepatotoxicity, nephrotoxicity; also rash and hypothermia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Acetominophen contraindications

A

Hypersensitivity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Acetominophen therapeutic considerations

A

Insignificant anti-inflammatory effects b/c of weak inhibition of peripheral COX; overdose is LEADING CAUSE OF HEPATIC FAILURE (b/c of modification by CYP40 to reactive metabolite that requires detoxification by glutathione) -> antidote is N-ACETYLCYSTEINE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Celecoxib MOA

A

Selective inhibition of COX-2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Celecoxib clinical applications

A

OA, RA in adults, ankylosing spondylitis, primary dysmenorrhea, acute pain in adults, familial adenomatous polyposis (b/c of some interaction w/ PPAR-delta)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Celecoxib adverse effects

A

MI, ischemic stroke, heart failure, GI bleeding/ulceration/perforation, renal papillary necrosis, exacerbation of asthma; also peripheral edema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Celecoxib contraindications

A

Hypersensitivity to sulfonomides or celecoxib; asthma, urticaria, or allergic rxn to NSAIDs (b/c of risk of fatal anaphylaxis); pain with CABG

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Celecoxib therapeutic considerations

A

Decreased efficacy of ACE inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Glucocorticoid MOA and names (4)

A

Induces lipocortins -> inhibit COX-2 action and prostaglandin biosynthesis
Prednison, Prednisolone, Methylprednisolone, Dexaethasone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Glucocorticoid clinical applications

A

Inflammatory conditions; autoimmune diseases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Glucocorticoid adverse effects

A

Immunosuppression, cataracts, hyperglycemia, hypercortisolism, depression, euphoria, osteoporosis, growth retardation in children, muscle atrophy; topical may cause skin atrophy

29
Q

Glucocorticoid contraindications

A

Systemic fungal infection

30
Q

Zileuton MOA

A

Inhibits 5-lipoxygenase -> decreases leukotriene synthesis

31
Q

Montelukast MOA (and another drug in the class)

A

Cysteinyl leukotriene type-1 receptor antagonistsAlso includes Zafirlukast

32
Q

Zileuton clinical applications

A

Asthma, also ASA-exacerbated respiratory distress (aspirin-sensitive asthma)

33
Q

Zileuton adverse effects

A

Increased liver enzymes; also, urticaria, abdominal discomfort, dizziness, insomnia; occasionally associated with Churg-Strauss

34
Q

Zileuton contraindications

A

Active liver disease, elevated liver enzymes

35
Q

Zileuton therapeutic considerations

A

Avoid concurrent use of dihydroergotamine, ergoloid mesylates, ergonovine, and methylergonovine b/c of increased risk of ergotism (N, V, vasospastic ischemia); pill-form reduces problems with inhaler use in kids (and can also treat other systemic allergies); requires periodic LFTs

36
Q

Montelukast clinical applications

A

Chronic asthma, allergic rhinitis, also ASA-exacerbated respiratory distress (aspirin-sensitive asthma)

37
Q

Montelukast adverse effects

A

Allergic granulomatosis angiitis, hepatitis; also, GI distress, hallucinations, agitation; occasionally associated with Churg-Strauss

38
Q

Montelukast contraindications

A

Hypersensitivity

39
Q

Montelukast therapeutic considerations

A

Excreted in breast milk; not indicated for acute asthma attacks, not appropriate as monotherapy for asthma; pill-form reduces problems with inhaler use in kids (and can also treat other systemic allergies)

40
Q

Glucocorticoid therapeutic considerations

A

Does not correct underlying disease, only limits effects of inflammation; requires tapering dosage after chronic use to avoid adrenal insufficiency

41
Q

TNF-Alpha Inhibitors MOA and names (5)

A

1) Enteracept: TNF receptor dimer

2) Infliximab, Adalimumab, Certolizumab, Golimumab: anti-TNF antibodies

42
Q

TNF-Alpha Inhibitors clinical applications

A

1) RA & Ankylosing Spondylitis (E, I, A, G)
2) Juvenile Idiopathic Arthritis (E, A)
3) Crohn’s (I, A, C)
4) Ulcerative Colitis (I)
5) Plaque Psoriasis (E, I, A)
6) Psoriatic Arthritis (E, A, G)

[Key: E=Enteracept, I=Infliximab, A=Adalimumab, C=Certolizumab, G=Golimumab]

43
Q

TNF-Alpha Inhibitors adverse effects

A

Myelosuppression, heart failure, optic neuritis, REACTIVATION OF TB, increased risk of infection/leukemia/lymphoma, demyelination of CNS; also upper respiratory infection, V, abdominal pain

44
Q

TNF-Alpha Inhibitors contraindications

A

Enteracept: sepsis, heart failure
Infliximab: Hypersensitivity

45
Q

TNF-Alpha Inhibitors therapeutic considerations

A

Give pts PPD before starting treatment (and regularly when they’re on the drug); in case of infection, give aggressive antibiotics; Enteracept binds to TNF-Alpha and Beta, the rest bind only to TNF-Alpha

46
Q

Alprostadil MOA

A

PGE1 analogue w/ vasodilator properties

47
Q

Alprostadil clinical applications

A

Maintenance of PDA (in Tetralogy of Fallot, Eisenmenger pulmonary HTN, and aortic valve atresia), erectile dysfunction

48
Q

Alprostadil adverse effects

A

Heart failure, arrhythmias/conduction defects, DIC, disorders of bone development, seizure, priapism, apnea in newborns; also hypotension, penile fibrosis/discomfort

49
Q

Alprostadil contraindications

A

Sickle cell; leukemia/myeloma; neonatal RDS; Anatomical deformation of the penis (and implant/Peyronie’s disease)

50
Q

Misoprostol MOA

A

PGE1 analogue w/ vasodilator properties

51
Q

Misoprostol clinical applications

A

Cytoprotective (increases mucus and bicarb production) and antisecretory (inhibits parietal cells) protection against gastric ulcers in long-term NSAID therapy; PUD; abortifacient (with mifepristone)

52
Q

Misoprostol adverse effects

A

Anemia, cardiac arrhythmia; also GI disturbance

53
Q

Misoprostol contraindications

A

Pregnancy

54
Q

Carboprost MOA

A

PGF2Alpha analogue that stimulates uterine contraction; leuteolytic activity controls fertility

55
Q

Carboprost clinical applications

A

Abortion in 2nd trimester, postpartum hemorrhage

56
Q

Carboprost adverse effects

A

Dystonia, pulmonary edema; also D, HA, F, paresthesia, breast tenderness

57
Q

Carboprost contraindications

A

Acute PID; cardiac, pulmonary, renal, or hepatic disease

58
Q

PGF2Alpha Analogues with Vasodilator Properties (3)

A

Latanoprost, Bimatoprost, Travoprost

59
Q

PGF2Alpha Analogues with Vasodilator Properties clinical applications

A

Ocular HTN; open-angle glaucoma

60
Q

PGF2Alpha Analogues with Vasodilator Properties adverse effects

A

Macular retinal edema; also blurred vision, hyper pigmentation of eyelids/iris

61
Q

PGF2Alpha Analogues with Vasodilator Properties contraindications

A

Hypersensitivity

62
Q

Epoprostenol MOA

A

Prostacyclin analogue that stimulates vasodilation of pulmonary & systemic arterial vasculature; also inhibits platelet aggregation

63
Q

Epoprostenol clinical application

A

Pulmonary HTN

64
Q

Epoprostenol contraindications

A

Supraventricular tachycardia, hemorrhage, thrombocytopenia; also hypotension, rash, GI disturbance, MSK pain, paresthesia, anxiety, flu-like illness

65
Q

Epoprostenol contraindications

A

Heart failure w/ severe L. ventricle dysfunction; chronic use in pts w/ pulmonary edema

66
Q

Anakinra MOA

A

Recombinant IL-1 receptor antagonist

67
Q

Anakinra clinical application

A

RA - reduces bony erosions, by decreasing metalloproteinase release from synovial cells

68
Q

Anakinra adverse effects

A

Neutropenia, increased risk of infection

69
Q

Anakinra contraindications

A

Hypersensitivity to drug OR to E. Coli-derived proteins

PBL Pharm Block 3 (14 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions