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KG - pharmacology 3 > KG - Pharm 3, Exam 1, NSAIDS & DMARDS > Flashcards

KG - Pharm 3, Exam 1, NSAIDS & DMARDS Flashcards

1
Q

clinical signs inflammation?

A
  • erythema, edema, tenderness, pain

- (rubor, calor, tumor, dolor)

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2
Q

three phases inflammation

A
  1. acute inflammation
  2. immune response
  3. chronic inflammation
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3
Q

ASA: moa

A
  • NONSELECTIVE

- IRREVERSIBLE INHIBITOR COX-1 & COX-2

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4
Q

ASA: pharmacokinetics

A
  • organic ACID
  • fast, ORAL absorption
  • HIGH CONCENTRATION IN STOMACH LUMEN (acidic)
  • distribution throughout body - cross placental and BBB
  • binds to plasma proteins
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5
Q

ASA: drug interactions

A

ASA competes w/ the following drugs for binding:
- T3, PEN G, thiopental, bilirubin, phenytoin, naproxen

(causes drug interaction)

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6
Q

ASA: metabolism

A
  • low doses = first order kinetics
  • high doses = zero order kinetics (above 600 mg)
  • RENAL EXCRETION (alkalization of urine promotes excretion)
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7
Q

ASA: pharmacodynamics

A
  • antiinflammatory
  • analgesic
  • antipyretic
  • antiplatelet (irreversible inhibition of platelet COX enzymes)
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8
Q

ASA: uses

A
  • mild/mod pain
  • antipyresis
  • anti-inflammatory
  • MI/thrombosis prophylaxis
  • long term use decr colon CA
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9
Q

ASA: adverse effects

A
  1. respiratory alkalosis

2. THEN, metabolic and respiratory acidosis

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10
Q

ASA: platelet effects

A
  • inhibits platelet aggregation, so incr bleeding time

- effects last 8-10 days

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11
Q

ASA: avoided in pts w/ ___

A
  • hypoprothrombinemia
  • vit K def
  • hemophilia
  • severe hepatic damage
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12
Q

if a pt that takes ASA is going to have surgery, what should he/she do?

A

stop taking ASA AT LEAST ONE WEEK PRIOR to surgery

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13
Q

if a pt that takes ASA is pregnant, what should she do?

A
  • avoid ASA prior to labor
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14
Q

ASA (low dose) & uric acid excretion

A
  • decreases uric acid excretion
  • elevates plasma urate concentration

(1-2 g ASA/day)

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15
Q

ASA (high dose) & uric acid excretion

A
  • enhances uric acid secretion (uricosuria)
  • lowers plasma urate concentration

(over 5 g/day)

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16
Q

ASA: side effects, cardiovascular

A

minimal in reg doses

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17
Q

ASA: side effects, lungs

A

ASPIRIN ASTHMA

- increased leukotriene synthesis

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18
Q

ASA: side effects, GI

A
  • GI upset, gastritis, ulcer, bleeding

- to help, use buffering, food, misoprostol

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19
Q

ASA: side effects, kidneys

A
  • renal damage, acute renal failure, interstitial nephritis
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20
Q

ASA & pregnancy

A
  • NO TERATOGENIC effect

- stop aspirin before labor to prevent bleeding

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21
Q

salicylic acid & irritant effects (NOT ASA)

A
  • destroys epithelial cells, irritant to mucosa
  • used for removal of warts, corns, fungal infections, eczematous dermatitis
  • methyl salicylates = irritating to skin and mucosa (oil of wintergreen)
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22
Q

ASA: avoid in patients w/ ___

A
  • gastric ulcers
  • hepatic damage
  • hypoprothrombinemia
  • vit K def
  • hemophilia
  • hypersensitivity to ASA/salicylates
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23
Q

when should ASA dose be decreased?

A
  • long term therapy w/ oral anticoagulants & hypoglycemic agents (diabetes)
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24
Q

how much for acute salicylate poisoning?

A
  • fatal = 20 g aspirin

- for methyl salicylate = 4-5 ml in children

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25
Reye's Syndrome?
- reason why don't give ASA to kids | - cerebral edema in children w/ viral infection
26
DOC for Reye's Syndrome?
acetaminophen
27
Celecoxib: moa
- SELECTIVE, REVERSIBLE COX-2 INHIBITOR
28
celecoxib: side effects
- less gastropathy (but still warning for GI bleed) | - INCREASED RISK CARDIOVASCULAR DISEASE
29
celecoxib: pharmacokinetics
- admin ORALLY
30
celecoxib: contraindications
- GI disease - asthma - breast feeding - pregnancy - renal failure
31
nonspecific reversible inhibitors of COX-1 & COX-2: info
- like ASA, but REVERSIBLE - worst (but potent) = indomethacin - first choice drug = ibuprofen (best side effect profile)
32
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, GI
- pain - bleeding - ulcer - pancreatitis - diarrhea
33
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, CNS
- HA - dizziness - confusion - depression
34
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, lung
- bronchoconstriction
35
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, bone marrow
- agranulocytosis | - aplastic anemia
36
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, kidney
- acute renal failure - interstitial nephritis - nephrotic syndrome
37
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, liver
- enzyme elevation | - hepatitis
38
nonspecific reversible inhibitors of COX-1 & COX-2: toxicities, allergy
- hypersensitivity rxns
39
indomethacin: info
- reduce PMN migration - inhibit phospholipase A - potent AI AR agent - high incidence side effects - USED FOR PATENT DUCTUS ARTERIOSUS (for when full transposition of great vessels)
40
Diclofenac: info
- potent COX inhibitor - decr AA bioavailability - oral absorption, liver metabolism - mostly GI side effects - COMBINE w/ MISOPROSTOL to decrease GI side effects
41
ketorolac: info
- ANALGESIC FOR POSTSURGICAL PAIN - oral, IV, IM admin - after 5 days use, GI side effects - may be combined w/ opiates
42
Ibuprofen: info
- FIRST CHOICE DRUG - lowest incidence side effects - combo w/ ASA decreases effect on platelet aggregation - renal excretion TOXICITY LOW - mostly GI
43
Naproxen: info
- similar to aspirin, ibuprofen - peak levels after 1-2 hrs, LONG HALF LIFE = 13 hrs - excretion = URINE - NOT for pregnant women - bound to plasma proteins (careful w/ Warfarin, hypoglycemic agents) TOXICITY: - mostly GI - gastric bleeding less severe than ASA
44
Piroxicam: info
- inhibits PMN migration, lymphocyte function - decreases oxygen radical production - long half life - LOTS OF GI side effects
45
Nabumetone: info
- prodrug | - long half life
46
Phenylbutazone: info
- POTENT, SERIOUS SIDE EFFECTS | - NOT MARKETED IN US
47
best and cheapest NSAID if person can tolerate it?
ASA
48
why is ACETAMINOPHEN preferred to ASA?
- tolerated better | - lacks side effects ASA has (no platelet effects, no ulcerogenics, no acid-base imbalance)
49
Acetaminophen overdose?
- can cause FATAL HEPATIC NECROSIS | - takes 15-20 g to kill pt
50
Acetaminophen: pharmacokinetics
- oral absorption - liver metabolism - renal excretion - DOSE DEPENDENT FREE RADICAL PRODUCTION (eliminated by GSH)
51
acetaminophen: pharmacodynamics
- antipyretic - analgesic - NO antiinflammatory - NO platelet effects
52
DOC fever in children?
acetaminophen
53
acetaminophen: uses
- mild, mod pain - fever (esp kids) - adjuncts to anti-inflammatory therapy - doesn't influence irate excretion
54
acetaminophen: adverse effects
- skin rash - cross sensitivity w/ salicylates - neutropenia w/ pancytopenia, leukopenia - DOSE-DEPEN FATAL HEPATIC NECROSIS
55
acetaminophen: dose-dependent fatal hepatic necrosis
- 10-15 g can be hepatotoxic, 25 g can be fatal - elevated serum transaminase, lactic acid dehydrogenase are signs of liver damage - hepatotoxicity --> encephalopathy, coma, death - the hydroxylated intermediate metabolite = resp for liver damage - toxicity serious when metabolites > available reduced glutathione in body - CHRONIC ALCOHOL CONSUMPTION INCREASES TOXICITY
56
acetaminophen toxicity: tx?
- antidote = N-acetylcysteine (Mucomyst) 10-12 hrs after intoxication - gastric emptying - forced diuresis - hemodialysis
57
gold salts: info
- inhibit phagocytosis - uncouple oxidative phosphorylation & inhibit cellular respiration - stabilize lysosomal membranes and inhibit actions of lysosomal enzymes - prevent PG synthesis - SUPPRESS CELLULAR IMMUNITY
58
gold salts: toxicity
- BONE MARROW DAMAGE - dermatitis - ENTEROCOLITIS - jaundice - peripheral neuropathy
59
penicillamine: info
- chelating drug in RA (and Wilson's)
60
penacillamine: toxicity
- high incidence adverse runs - pruritus, rash, alteration in taste - thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia - proteinuria, hypoalbuminuria, nephrotic syndrome - lupus-like dz, pemphigus, Goodpasture's, MG - PTs over 65 HAVE HIGHEST RISK
61
hydroxychloroquine: info
- has antihistaminic, anticholinesterase, and anti protease properties - inhibits PG synthesis - inhibits biosynthesis of mucopolysaccharide - inhibits response to phagocytosis - stabilizes lysosomes - reacts w/ nucleic acids and tissue proteins
62
hydroxychloroquine: toxicity
- pruritus - hemolysis (G6PD def) - ototoxicity - retinopathy - peripheral neuropathy
63
sulfasalazine: info
- used to treat RA - less toxic than penacillamine - salicylate + sulfa properties
64
sulfasalazine: toxicity
- GI - rash - hepatitis/blood dyscrasias = rare - -> monitor hepatitis & bone barrow suppression first 2-3 wks during first few months tx then less afterward
65
Infliximab: info
- CHIMERIC monoclonal antibody targeted against TNF alpha - for Crohn's & RA - combined w/ methotrexate - admin = IV
66
Infliximab: adverse rxn
- HA | - infusion rxns
67
infliximab: contraindications
- pregnancy - breast feeding - children - infections
68
Rituximab: info
- CHIMERIC monoclonal antibody - binds to CD20, a B-LYMPHOCYTE DIFFERENTIATION ANTIGEN on lymphocytes - CD20 antigen expressed on > 90% NHL b cells --> used to treat NHL - admin = IV
69
adalimumab: info
- recombinant human monoclonal antibody - 100% HUMAN PEPTIDE SEQUENCES - specific for TNF alpha - approved for mono therapy of RA - admin = SUB q - half life 8-10 days
70
adalimumab: adverse effects
- rash - flu-like symptoms - fatigue - HA - pruritus - N/V
71
etanercept: info
- DIMERIC FUSION PROTEIN produced by RECOMBINANT DNA technology - consists of extracellular binding portion of human TNF RECEPTOR - admin = SUB Q
72
etanercept: adverse effects
- injection site rxn - infection - increased incidence antibody formation
73
etanercept: contraindication
- bone marrow suppression - breast-feeding - children - DM - infection - sepsis - vaccination - varicella
74
Abatacept: info
- HUMAN FUSION PROTEIN as costimulatory or second signal blocker of T cell activation - competes w/ CD28 for CD 80/86 binding - disturbs progressive joint destruction in RA - may affect host defenses against infection and malignancy - admin = IV - half life = 13 days
75
leflunomide: info
- inhibits DHODH - enzyme in de novo pyrimidine synthesis - 2nd moa = inhibition of cytokine GF receptor associated tyrosine kinase activity - INHIBITS INDUCTION OF COX-2 - admin = oral
76
leflunomide: adverse effects
- GI - anorexia - oral ulceration - elevated hepatic enzmyes
77
leflunomide: contraindications
- pregnancy - breast feeding - hepatic/renal failure
78
mycophenolate mofetil: info
- PRODRUG FOR immunosuppresive agent MPA - INHIBITS LYMPHOCYTE PURINE SYNTHESIS - admin = oral or IV
79
mycophenolate mofetil: adverse effects
- D/G, GI bleed
80
mycophenolate mofetil: contraindications
- active GI dz - diarrhea - pregnancy - breast feeding - infections
81
anakinra: info
- recombinant, non glysosylated form of HUMAN INTERLEUKIN-1 RECEPTOR ANTAGONIST - for RA - renal elimination
82
anakinra: contraindication
- breast feeding - children - hypersensitivity rxn - renal dz
83
tofacitinib: info
- INHIBITS JAK 1 & JAK 3 (JAK 2) - for adults w/ mod to severe RA, w/ intolerance or inadequate response to methotrexate - serious infections and malignancies may precipitate - half life = 3 hrs

KG - pharmacology 3 (11 decks)

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