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Pharmacology II > Osteoarthritis (exam 1) > Flashcards

Osteoarthritis (exam 1) Flashcards

(60 cards)

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1
Q

cardinal features of osteoarthritis

A

progressive cartilage loss
subchrondral thickening
marginal osteophytes

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2
Q

what type of disease is OA

A

degenerative joint disease

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3
Q

osteoarthritic is characterized by

A

degeneration of cartilage that cushions the ends of bones

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4
Q

treatment for osteoarthritis

A

exercise
pain medication

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5
Q

is there a drug that can reverse OA?

A

no

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6
Q

initial drug of choice for OA

A

acetaminophen

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7
Q

what types of medication can be used to treat OA?

A

acetaminophen
NSAIDs
capsaicin
tramadol
glucocorticoids
opioids

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8
Q

when does OA begin and how long does it develop compared to RA?

A

RA: 25-50 yrs; weeks-months

OA: 40 yrs; years

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9
Q

are osteophytes present in RA and OA?

A

ONLY osteoarthritis

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10
Q

is RF present in RA and OA?

A

ONLY rheumatoid arthritis

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11
Q

major sign of RA and OA

A

RA: inflammation
OA: pain

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12
Q

how long does morning stiffness last in RA and OA?

A

RA: over an hour
OA: under 20 minutes

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13
Q

are fatigue, weight loss and anemia present in RA and OA?

A

ONLY rheumatoid arthritis

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14
Q

rheumatoid arthritis is a _____________ response while osteoarthritis is a _______________

A

autoimmune

loss of cartilage matrix

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15
Q

eicosanoids

A

prostaglandins, thromboxanes, leukotrienes
short lives, extremely potent
formed in almost every tissue of the body

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16
Q

COX1 pathway is ___________ and COX2 pathway is ___________

A

constitutive (expressed at all times)

inducible (expressed by inflammatory stimuli)

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17
Q

which COX pathway is NSAID sensitive?

glucocorticoid sensitive?

A

both COX1 and COX2

only COX2

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18
Q

types of prostaglandins in COX-1 pathway

A

stomach - PGE2
Kidneys - PGE2, PGI2
platelets - TxA2
vascular endothelium - PGI2

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19
Q

COX-1 pathway activation leads to ___________ while COX-2 pathway activation leads to _______________

A

physiological homeostasis

inflammation

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20
Q

NSAIDs MOA

A

inhibit the product of eicosanoids by inhibiting the activity of cyclooxygenases

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21
Q

NSAIDs are what type of antagonist?

A

noncompetitive

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22
Q

NSAIDs posses what type of effects?

A

anti-inflammatory
analgesic
antipyretic

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23
Q

aspirin MOA

A

irreversibly acetylates COX1 and COX2

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24
Q

how are NSAIDs antipyretic?

A

PGE2 crosses BBB to increase body temperature

when this is decreased, body temp lowers

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25
chief metabolic products of aspirin
salicyluric acid (glycine conjugate) phenolic glucuronide acyl glucuronide
26
how is aspirin exerted in the urine?
75% - free salicyluric acid 10% - salicylic acid 10% - salicylic phenolic 5% - acyl glucuronide
27
aspirin is contraindicated in
vitamin K deficiency and hemophilia
28
ADRs of aspirin
increase gut irritation gastric distress N/V prolonged bleeding time nephropathy
29
where is aspirin metabolized?
hepatic ER and mitochondria
30
Pharmacokinetics of acetaminophen
extensive 1st pass metabolism in luminal cells of intestine conjugated in liver to form inactive glucuronidated/sulfated metabolites
31
part of acetaminophen is hydroxylated to from
N-acetyl-p-benzoiminoquinoneimine (NAPQI)
32
NAPQI
highly reactive potentially dangerous metabolite that reacts with sulfhydryl groups
33
acetaminophen converts into _________________ which can be therapeutic or toxic doses
toxic intermediate
34
adverse effects of acetaminophen
acute overdoses - fatal liver damage (from NAPQI) renal tubular damage
35
are there adverse effects at normal doses of acetaminophen?
rarely
36
antidote for acetaminophen how it works?
n-acetylcysteine contains sulfhydryl groups which interact with NAPQI and detoxify it
37
MEOS compromises
CYP4502E1 (major) 1A2 3A4
38
why acetaminophen intake can be toxic after alcohol consumption?
increase liver damage due to increased production of NAPQI
39
NSAID nonselective antagonists
piroxicam tolmetin indomethacin ibuprofen naproxen meloxicam
40
most potent nonselective antagonist NSAID to inhibit COX1
piroxicam
41
most potent nonselective antagonist NSAID to inhibit COX2`
meloxicam
42
which nonselective antagonist NSAIDs are more selective at inhibiting COX2 pathway?
meloxicam naproxen
43
celecoxib and parecoxib are what type of antagonist?
reversible selective COX-2
44
how is parecoxib administered?
by injection
45
adverse effects of selective COX-2 antagonists
risk of myocardial infarction and stroke hypertension and edema due to inhibition of PG production in kidney protective effects thrombosis
46
acetaminophen MOA
poor inhibitor of COX1 and COX2 in presence of peroxides inhibits a novel COX splice variant in the brain (COX3)
47
what type of effects does acetaminophen have?
antipyretic and analgesic
48
is acetaminophen an anti inflammatory?
no
49
NAPQI is considered a
BRI biological reactive intermediate
50
acetaminophen undergoes _______________ to form NAPQI
CYP450 oxidation
51
2 classes of DMARDs
traditional biologic
52
traditional DMARDs
MTX leflunomide hydroxychloroquine sulfasalazine cyclophosphamide cyclosporine tacrolimus
53
biologic DMARDs
abatacept etanercept infliximab rituximab tocilizumab
54
methotrexate is the ___________ for DMARD therapy
gold standard
55
treatment and care for osteoarthritis
protecting joints medication and lifestyle changes knee injections knee replacement joint fusion injury corticosteroid injections joint replacement
56
joint replacement are sometimes considered
treatment of last resort
57
inflammasome
multiprotein intracellular complex that detects pathogens and sterile stressors activates highly pro-inflammatory cytokines I-1b and IL-18
58
what is the best characterized inflammasome?
NLRP3
59
what does APAP stand for?
N-acetyl-para-aminophenol
60
acetaminophen is found to inhibit _____________ in the canine brain but its role in humans is not confirmed
COX-1 isoenzyme COX3

Pharmacology II (18 decks)

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