Exam 4: NSAIDs/Non-Opioids yo-Part 1 to Aspirin Flashcards Preview

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Flashcards in Exam 4: NSAIDs/Non-Opioids yo-Part 1 to Aspirin Deck (100):
1

Patients who ________ having pain or who have fear and anxiety will perceive more pain.

ANTICIPATE!!!

2

_______: “an unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage”

Pain

3

_______ = absence of pain in response to a stimulus that is normally painful

Analgesia

4

________ = absence of all sensory modalities

Anesthesia

5

2 Types of pain: _______ = non- steroidal anti-inflammatory analgesics (NSAIDS) are most effective.....AND...._________ = opiates (narcotics) are most effective

Dull, aching, inflammatory......AND......Sharp, piercing, lancinations

6

Hey, I don't think I saw this enough...Narcotics are NOT __________.

anti-inflammatory

7

Degrees of Pain & what to use: _____ = Salicylates, NSAIDS most effective...._______ = Salicylates, NSAIDS most effective....________ = opiates are best

Mild...Moderate...Severe

8

Locus of Action...haha that sounds cool: Non-opioid Analgesics- Act primarily at ________ nerve endings...._______ effect mediated centrally... Mechanism: inhibit _________ synthesis

peripheral....Antipyretic...prostaglandin

9

Locus of Action...haha that sounds cool: Opioid Analgesics-Act primarily within ______.....Mechanism: _______ CNS which reduces response to pain (pain reaction)

CNS....depress

10

Locus of Action...haha that sounds cool: ________ (local pain control) = analgesia, anti-inflammatory effects THEREFORE ________, _______ are used; few side effects....All non-opioid analgesics work on the ________
nervous system (as well as CNS)

Periphery...salicyclates and NSAIDs....PNS

11

Locus of Action...haha that sounds cool: ________ = analgesia, anti- inflammatory effects, ANTIPYRETIC effect.....NSAIDS; acetaminophen (Tylenol).....opiates = more side effects

CNS

12

The WAR- NSAIDs VS Opioids- _______ = true analgesics; stop the pain from where it is occurring

NSAIDs

13

The WAR- NSAIDs VS Opioids- ________ = diminish your awareness of pain, so act as analgesics (don’t feel pain)

Opiates

14

The WAR- NSAIDs VS Opioids- NSAIDS inhibit _________ synthesis; they accomplish this by inhibiting the __________ enzyme.

prostaglandin...cyclooxygenase

15

The WAR- NSAIDs VS Opioids- NSAIDs inhibit ________ PG as well as PG associated with _________.

cytoprotective...inflammation

16

What is another name for salicyclics?

Aspirin

17

How many drugs approved by the US are in the NSAIDs family? Whats one example?

22...ibuprofen

18

acetaminophen (Tylenol) = classified as a “__________” analgesic (not NSAID), as it works on COX-___ in the CNS, and is NOT ________.

miscellanious...COX 3...anti-inflammatory

19

What is the grandfather molecule of prostaglandin synthesis?

Arach-id-onic Acid

20

What are the four steps to forming prostaglandins? Where do NSAIDs/Salicyclics intervene?

Arachidonic Acid-->Cyclooxygenase (Salicyclics/NSAIDs inhibit here)-->Endoperoxidases--->Prostaglandins

21

Non-selective NSAIDs are COX-__ & ____ inhibitors.

COX-1 & 2

22

COX-1 leads to ________ prostaglandins which promote _________. ERGO- blocking COX-1 will lead to side effects in the _____, ______, and ______ aggregation.

cytoProtective....homeostasis....stomach, kidneys, platelet

23

What are the three end products of COX-1?

1.Prostacyclin-stomach endothelium 2.Prostaglandin E2-kidneys 3.Thromboxane A2-platelets

24

COX-2 leads to the prostaglandins that are correlated with ________...which is our goal!

inflammation

25

Salicyclates and NSAIDs block which COX(s)?

COX-1 AND COX-2 non selectively

26

COX-___ Regulates the amount of stomach acid produced

COX-1

27

Blocking COX-___ with aspirin or NSAIDS decreases production of protective _______ in the gastric lining = explains side effect of GU ulceration and bleeding

COX-1...mucous

28

COX-___ is the inducible form which is produced when you experience trauma and need inflammatory response for healing

COX-2

29

Drugs that block COX 2 are primarily used for ______.

arthritis

30

COX-___ have no effect on the stomach = leave cytoprotective prostaglandins intact.

COX-2

31

What is THE ONLY COX-2 selective inhibitor on the market?

Celebrex

32

COX-__: Recently discovered (2002), Works in the central nervous system, Suppresses prostaglandin synthesis, No anti-inflammatory effects, this is how acetaminophen (Tylenol) works (pain control but no anti-inflammatory effects)

COX-3

33

COX-3: Works in the ______.

CNS

34

COX-3: Suppresses _______ synthesis

prostaglandin

35

COX-3: NO _______ effects

anti-inflammatory

36

COX-3: This is how __________ (Tylenol) works (pain control but no anti-inflammatory effects)

acetaminophen

37

Non-selective NSAIDs = block both COX-__ and COX-__...MOST NSAIDs in use today (eg. ibuprofen)

COX-1 and COX-2

38

Selective NSAIDS = block COX-__ only....Only one available on U.S. market: _______ (_______) used primarily for arthritis pain.

cele-COX-ib (Celebrex)

39

Remember that acetaminophen (Tylenol) blocks COX-__ but it is NOT categorized as an _____.

COX-3...NSAID

40

What is the abbreviation of Aspirin? What is its pharmalogic class? Comes from extracts of _______.

ASA...salicylate...willow bark

41

What is the most useful salicyclate for analgesia?

Aspirin

42

What is the chemical structure of Aspirin?

AcetylSaliCyclic Acid

43

Most of aspirin’s effects are due to inhibition of __________.

prostaglandin synthesis

44

Prostaglandins are synthesized _______ by inflammatory stimuli.

locally...shop local broooo

45

Prostaglandins sensitize pain ________ to substances such as bradykinin, therefore reduction in _________ = reduction in pain.

receptors....prostaglandins

46

Aspirin is MORE effective if given ______ painful stimuli are experienced

BEFORE!!!!!

47

Aspirin is more effective against _______ pain (caused by inflammation) versus ______ pain (direct irritation of nerve endings)

throbbing...stabbing

48

Kinetics of ASA-Rapidly and completely absorbed from stomach and small intestine, producing peak effect on empty stomach in ___ minutes

30 minutes

49

Kinetics of ASA- Widely distributed; poorly bound to _______

plasma proteins

50

Kinetics of ASA- Hydrolyzed to ________ in GI tract and via _______ effect in liver

salicyclate...FIRST PASS

51

Kinetics of ASA- Conjugated with ______ and ________ acid by liver

glycine...glu-cur-onic acid

52

Kinetics of ASA- Half-life is ______-dependent, small doses = half life of __-__ hours...Higher dose = 15-30 hours

DOSE...small=2-3 hours...higher =15-30 hours

53

Kinetics of ASA- It follows ______ order kinetics.

Zero

54

Kinetics of ASA- May lead to ________ situation if take too much

poisoning

55

Kinetics of ASA- _______ increased by alkalinization with sodium bicarbonate which increases the proportion of the aspirin that is in the ______ form that is therefore excreted

Excretion...ionized

56

Effects of Aspirin-Analgesic:Relieves _____ to _____ pain, not potent enough for intense pain, use an opioid.

mild to moderate

57

Effects of Aspirin-Considered an antipyretic because it inhibits ________ synthesis in the _________....it also induces peripheral ________ and sweating.

prostaglandin synthesis....hypothalamus...dilation

58

Effects of Aspirin-Anti-inflammatory: Prostaglandins are potent vasodilating agents that also increase capillary permeability.....Inhibition causes decreased erythema and _______ of inflamed area

swelling

59

Effects of Aspirin-Anti-inflammatory: Important because almost all dental pain is __________ in nature....High dose aspirin is used to relieve pain and inflammation of ______ too!

inflammatory.....arthritis

60

Effects of Aspirin- the Analgesic dose = dosing used for pain control is NOT ENOUGH for ________ effects!

anti-inflammatory

61

HOW many mg of aspirin is needed for anti-inflammatory effect? What are the 2 side effects of this high of a dose?

3500 mg....stomach ulceration and bleeding

62

Effects of Aspirin-Large/high doses (greater than ___ g per day) – produces _______ effect = excretion of uric acid in urine...At one time, aspirin was used to treat ____ but, Aspirin is no longer used for this purpose

3 g...URICO-SURIC...gout!

63

What analgesic should a person with gout stay away from?

Aspirin...patient takes probenecid (Benemid) to excrete uric acid (stops absorption of uric acid back into bloodstream)...aspirin can ANTAGONIZE these effects

64

Effects of Aspirin:Anti-platelet effect = _________ effect that lasts for the life of the platelet (___-___ days)...Reduces platelet adhesiveness/aggregation by interfering with _________ (____) release = prolongs bleeding time

irreversible....7-10 days...adenosine diphosphate (ADP)

65

Effects of Aspirin: Aspirin inhibits cyclooxygenase which inhibits the formation of __________, which facilitates clotting, so by reducing this, aspirin reduces the risk for _______ and ______! AT about ____ mg/day

thromboxane A2...blood clots and stroke!...81 mg

66

Adverse effects of aspirin ________: dyspepsia, nausea, vomiting, gastric bleeding...WHY?

Gastointestinal..inhibits the COX-1 Cytoprotective enzymes!!

67

Adverse effects of aspirin-Stimulates chemoreceptor ______ zone in the CNS (nausea and vomiting)

trigger

68

Adverse effects of aspirin--Exacerbates ________ ulcers, gastritis, hiatal hernia, reflux disease

PRE-EXISTING

69

Adverse effects of aspirin- What is it called when aspirin inhibits the production of PROTHROMBIN?

Inhibits production of prothrombin = hypo-prothrombin-emia!!

70

Adverse effects of aspirin-the GI bleeding caused by aspirin is often ______!

painless

71

What is the name of this syndrome??? aspirin contraindicated in children/adolescents with viral infections
(flu, chickenpox)

Reye's syndrome

72

Reye's Syndrome can manifest with fluid in _____ (encephalitis) and ________ = often fatal

brain...hepatotoxicity

73

What do we use instead of aspirin if a child is sick? (most of the time its viral origin!)

Acetaminophen (Tylenol)

74

What is a classic warning sign of Salicyism (toxicity of aspirin)?

Tinnitus

75

Aspirin toxicity- At high doses = _________ = produces _________; then compensatory renal loss of _______, Na and K = leads to respiratory AND _______ acidosis!!!

hyperventilation...respiratory alkalosis..bicarb...metabolic

76

Death from aspirin poisoning is usually ______ and ______ imbalance

acidosis and electrolyte

77

Aspirin toxicity-Usually occurs in overdose ranges from __-___ grams in adults

6-10 grams

78

Allergies to aspirin are pretty rare...Less than __% incidence

1%

79

These are signs of a ________: rash, wheezing, urticaria (hives), angioneurotic edema, anaphylaxis

TRUE aspirin allergy

80

Allergy to aspirin CAN mean a person has __________ to other NSAIDs!

CROSS-sensativity

81

________ are more likely to have hypersensitivity reaction to aspirin (incidence ranges from 5- 15%)...STEEEEEVVVEEEE....THEREFORE ________ is a CONTRAINDICATION for aspirin use.

ASMATICS!!!....Asthma

82

What is the ASPIRIN hypersensitivity TRIAD??

1. Aspirin Hypersensativity 2.ASTHMA 3.Nasal Polyps

83

Mechanism of aspirin allergy...Shift in COX cascade to inhibit
bronchodilating ______.....Shifts to favor unopposed lipoxygenase pathway and formation of ________ (bronchoconstrictors)

PGE2...LEUKOTRIENES

84

Allergic reactions look like _______ attacks = bronchial effects...in fact, in asthmatics, aspirin sensitivity develops over about ____ exposures

asthma...15

85

Cray cray patients- When aspirin is applied directly to oral mucosa, ester in water splits to ______ acid and salicylic acid and makes an "______"

acetic..."aspirin burn"

86

Oral ulcerations = chewing aspirin-containing ____.

gum...whaaaa they make that?!

87

Summary...time to use your memory tricks! What are the 4 contraindications to aspirin?

1.Allergy (bronchal rxn) 2.Chronic Gastritis 3.Gout 4.Anticoagulants

88

Aspirin displaces ______ from plasma proteins and therefore increases risk for a hemmorage.

warfarin

89

When is Aspirin contraindicated in pregnancy? What is the FDA category? BUT _______ aspirin has not been shown to be teratogenic.

The 3rd trimester!....C/D woah!..low dose

90

Aspirin and Prego-Can ______ labor (decreases prostaglandins responsible for uterine contractions)......Increases risk for _______ complications in mother....Risk of premature closing of the ________ in fetus, resulting in pulmonary vasculature abnormalities and pulmonary hypertension in newborn.

prolong (AINT NOBODY GOT TIME FOR THAT!)....BLEEDING....ductus arteriosus

91

Aspirin DOSING-___ mg for cardio-protective...____ mg for full strength dose (during a M.I.)

81 mg...325 mg

92

Aspirin Dosing- ____-____ mg every ___-___ hours UP TO ____ g per DAY!!!

325 - 650 mg...4-6 hours...up to 4 grams per day

93

Aspirin dosing: Children: ___-___ mg/kg/dose every 4-6 hours, up to a total of __ grams per day

10-15...4 g per day

94

Discontinue Aspirin? ______ aspirin therapy (81 mg daily) = NO need to discontinue

LOW DOSE

95

1 single dose of aspirin exerts an effect for a minimum of __ days

4 days

96

Discontinue Aspirin? For highly invasive surgeries, must weigh risk to patient versus bleeding risks...Eg: patients with cardiac stents are on aspirin and antiplatelet drug (Plavix) = discontinue _______ but not _______ before surgery

Plavix...aspirin

97

If patient is taking aspirin because of cardiac history, then __________ before advising the patient to discontinue the drug = benefit must outweigh risks to the patient

consult the patient’s physician!!!!

98

Potential for “________” risks (MI, stroke) if suddenly discontinue the use of aspirin!!

"catastophic"

99

What makes a person on aspirin clot why wouldn't they just bleed out??? _____ AND endothelial cells continue to make ___________.

FIBRIN...thromboxane A2

100

FUN FACTS! Methyl salicylate (oil of wintergreen) – Icy Hot, Ben Gay, Trolamine salicylate - Myoflex, Salicylic acid – Compound W, Magnesium salicylate – Doan’s pills ALL ARE SALICYCLATES used ________.

TOPICALLY