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Pharmacology LECOM SH > Pharm 42 Eicosanoids > Flashcards

Pharm 42 Eicosanoids Flashcards

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1
Q

Aspirin MOA

A

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

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2
Q

Aspirin clinical applications

A

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

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3
Q

Aspirin adverse effects

A

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

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4
Q

Aspirin contraindications

A

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

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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

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6
Q

NSAID MOA and classes

A

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

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7
Q

Priopionic Acids (4)

A

Ibuprofen, Naproxen, Ketoprofen, Flurbiprofen

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8
Q

Acetic Acids (5)

A

Indomethacin, Sulindac, Etodolac, Diclofenac, Keterolac

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9
Q

Oxicams (1)

A

Prioxicam (duh)

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10
Q

Fenamates (2)

A

Mefenamate, Meclofenamate

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11
Q

Ketones (1)

A

Nabumetone

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12
Q

NSAID clinical applications

A

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

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13
Q

NSAID adverse effects

A

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

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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

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15
Q

NSAID therapeutic considerations

A

1) Naproxen has longer T1/2, more potency, and fewer GI effects than ASA2) Keterolac is used for 3-5 days post-surgery3) Piroxicam has long T1/2 - dose once daily4) Nabumetone has greatest COX-2 selectivity5) Fenamate is less useful than ASA

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16
Q

Acetominophen MOA

A

COX-3 inhibitor in CNS

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17
Q

Acetominophen clinical applications

A

F, mild-to-moderate pain

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18
Q

Acetominophen adverse effects

A

Hepatotoxicity, nephrotoxicity; also rash and hypothermia

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19
Q

Acetominophen contraindications

A

Hypersensitivity

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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

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21
Q

Celecoxib MOA

A

Selective inhibition of COX-2

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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)

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23
Q

Celecoxib adverse effects

A

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

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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

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25
Celecoxib therapeutic considerations
Decreased efficacy of ACE inhibitors
26
Glucocorticoid MOA and names (4)
Induces lipocortins -\> inhibit COX-2 action and prostaglandin biosynthesisPrednison, Prednisolone, Methylprednisolone, Dexaethasone
27
Glucocorticoid clinical applications
Inflammatory conditions; autoimmune diseases
28
Glucocorticoid adverse effects
Immunosuppression, cataracts, hyperglycemia, hypercortisolism, depression, euphoria, osteoporosis, growth retardation in children, muscle atrophy; topical may cause skin atrophy
29
Glucocorticoid contraindications
Systemic fungal infection
30
Zileuton MOA
Inhibits 5-lipoxygenase -\> decreases leukotriene synthesis
31
Montelukast MOA (and another drug in the class)
Cysteinyl leukotriene type-1 receptor antagonistsAlso includes Zafirlukast
32
Zileuton clinical applications
Asthma, also ASA-exacerbated respiratory distress (aspirin-sensitive asthma)
33
Zileuton adverse effects
Increased liver enzymes; also, urticaria, abdominal discomfort, dizziness, insomnia; occasionally associated with Churg-Strauss
34
Zileuton contraindications
Active liver disease, elevated liver enzymes
35
Zileuton therapeutic considerations
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
Montelukast clinical applications
Chronic asthma, allergic rhinitis, also ASA-exacerbated respiratory distress (aspirin-sensitive asthma)
37
Montelukast adverse effects
Allergic granulomatosis angiitis, hepatitis; also, GI distress, hallucinations, agitation; occasionally associated with Churg-Strauss
38
Montelukast contraindications
Hypersensitivity
39
Montelukast therapeutic considerations
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
Glucocorticoid therapeutic considerations
Does not correct underlying disease, only limits effects of inflammation; requires tapering dosage after chronic use to avoid adrenal insufficiency
41
TNF-Alpha Inhibitors MOA and names (5)
1) Enteracept: TNF receptor dimer2) Infliximab, Adalimumab, Certolizumab, Golimumab: anti-TNF antibodies
42
TNF-Alpha Inhibitors clinical applications
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
TNF-Alpha Inhibitors adverse effects
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
TNF-Alpha Inhibitors contraindications
Enteracept: sepsis, heart failureInfliximab: Hypersensitivity
45
TNF-Alpha Inhibitors therapeutic considerations
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
Alprostadil MOA
PGE1 analogue w/ vasodilator properties
47
Alprostadil clinical applications
Maintenance of PDA (in Tetralogy of Fallot, Eisenmenger pulmonary HTN, and aortic valve atresia), erectile dysfunction
48
Alprostadil adverse effects
Heart failure, arrhythmias/conduction defects, DIC, disorders of bone development, seizure, priapism, apnea in newborns; also hypotension, penile fibrosis/discomfort
49
Alprostadil contraindications
Sickle cell; leukemia/myeloma; neonatal RDS; Anatomical deformation of the penis (and implant/Peyronie's disease)
50
Misoprostol MOA
PGE1 analogue w/ vasodilator properties
51
Misoprostol clinical applications
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
Misoprostol adverse effects
Anemia, cardiac arrhythmia; also GI disturbance
53
Misoprostol contraindications
Pregnancy
54
Carboprost MOA
PGF2Alpha analogue that stimulates uterine contraction; leuteolytic activity controls fertility
55
Carboprost clinical applications
Abortion in 2nd trimester, postpartum hemorrhage
56
Carboprost adverse effects
Dystonia, pulmonary edema; also D, HA, F, paresthesia, breast tenderness
57
Carboprost contraindications
Acute PID; cardiac, pulmonary, renal, or hepatic disease
58
PGF2Alpha Analogues with Vasodilator Properties (3)
Latanoprost, Bimatoprost, Travoprost
59
PGF2Alpha Analogues with Vasodilator Properties clinical applications
Ocular HTN; open-angle glaucoma
60
PGF2Alpha Analogues with Vasodilator Properties adverse effects
Macular retinal edema; also blurred vision, hyper pigmentation of eyelids/iris
61
PGF2Alpha Analogues with Vasodilator Properties contraindications
Hypersensitivity
62
Epoprostenol MOA
Prostacyclin analogue that stimulates vasodilation of pulmonary & systemic arterial vasculature; also inhibits platelet aggregation
63
Epoprostenol clinical application
Pulmonary HTN
64
Epoprostenol contraindications
Supraventricular tachycardia, hemorrhage, thrombocytopenia; also hypotension, rash, GI disturbance, MSK pain, paresthesia, anxiety, flu-like illness
65
Epoprostenol contraindications
Heart failure w/ severe L. ventricle dysfunction; chronic use in pts w/ pulmonary edema
66
Anakinra MOA
Recombinant IL-1 receptor antagonist
67
Anakinra clinical application
RA - reduces bony erosions, by decreasing metalloproteinase release from synovial cells
68
Anakinra adverse effects
Neutropenia, increased risk of infection
69
Anakinra contraindications
Hypersensitivity to drug OR to E. Coli-derived proteins

Pharmacology LECOM SH (24 decks)

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