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

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

1
Q

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

A

ANTICIPATE!!!

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2
Q

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

A

Pain

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3
Q

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

A

Analgesia

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4
Q

________ = absence of all sensory modalities

A

Anesthesia

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5
Q

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

A

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

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6
Q

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

A

anti-inflammatory

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7
Q

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

A

Mild…Moderate…Severe

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8
Q

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

A

peripheral….Antipyretic…prostaglandin

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9
Q

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

A

CNS….depress

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10
Q 
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)
A

Periphery…salicyclates and NSAIDs….PNS

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11
Q

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

A

CNS

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12
Q

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

A

NSAIDs

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13
Q

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

A

Opiates

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14
Q

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

A

prostaglandin…cyclooxygenase

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15
Q

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

A

cytoprotective…inflammation

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16
Q

What is another name for salicyclics?

A

Aspirin

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17
Q

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

A

22…ibuprofen

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18
Q

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

A

miscellanious…COX 3…anti-inflammatory

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19
Q

What is the grandfather molecule of prostaglandin synthesis?

A

Arach-id-onic Acid

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20
Q

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

A

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

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21
Q

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

A

COX-1 & 2

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22
Q

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

A

cytoProtective….homeostasis….stomach, kidneys, platelet

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23
Q

What are the three end products of COX-1?

A

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

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24
Q

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

A

inflammation

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25
Q

Salicyclates and NSAIDs block which COX(s)?

A

COX-1 AND COX-2 non selectively

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26
Q

COX-___ Regulates the amount of stomach acid produced

A

COX-1

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27
Q

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

A

COX-1…mucous

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28
Q

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

A

COX-2

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29
Q

Drugs that block COX 2 are primarily used for ______.

A

arthritis

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30
Q

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

A

COX-2

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31
Q

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

A

Celebrex

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32
Q

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)

A

COX-3

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33
Q

COX-3: Works in the ______.

A

CNS

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34
Q

COX-3: Suppresses _______ synthesis

A

prostaglandin

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35
Q

COX-3: NO _______ effects

A

anti-inflammatory

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36
Q

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

A

acetaminophen

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37
Q

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

A

COX-1 and COX-2

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38
Q

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

A

cele-COX-ib (Celebrex)

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39
Q

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

A

COX-3…NSAID

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40
Q

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

A

ASA…salicylate…willow bark

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41
Q

What is the most useful salicyclate for analgesia?

A

Aspirin

42
Q

What is the chemical structure of Aspirin?

A

AcetylSaliCyclic Acid

43
Q

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

A

prostaglandin synthesis

44
Q

Prostaglandins are synthesized _______ by inflammatory stimuli.

A

locally…shop local broooo

45
Q

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

A

receptors….prostaglandins

46
Q

Aspirin is MORE effective if given ______ painful stimuli are experienced

A

BEFORE!!!!!

47
Q

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

A

throbbing…stabbing

48
Q

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

A

30 minutes

49
Q

Kinetics of ASA- Widely distributed; poorly bound to _______

A

plasma proteins

50
Q

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

A

salicyclate…FIRST PASS

51
Q

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

A

glycine…glu-cur-onic acid

52
Q

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

A

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

53
Q

Kinetics of ASA- It follows ______ order kinetics.

A

Zero

54
Q

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

A

poisoning

55
Q

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

A

Excretion…ionized

56
Q

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

A

mild to moderate

57
Q

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

A

prostaglandin synthesis….hypothalamus…dilation

58
Q

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

A

swelling

59
Q

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!

A

inflammatory…..arthritis

60
Q

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

A

anti-inflammatory

61
Q

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

A

3500 mg….stomach ulceration and bleeding

62
Q

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

A

3 g…URICO-SURIC…gout!

63
Q

What analgesic should a person with gout stay away from?

A

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

64
Q

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

A

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

65
Q

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

A

thromboxane A2…blood clots and stroke!…81 mg

66
Q

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

A

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

67
Q

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

A

trigger

68
Q

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

A

PRE-EXISTING

69
Q

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

A

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

70
Q

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

A

painless

71
Q

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

A

Reye’s syndrome

72
Q

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

A

brain…hepatotoxicity

73
Q

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

A

Acetaminophen (Tylenol)

74
Q

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

A

Tinnitus

75
Q

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

A

hyperventilation…respiratory alkalosis..bicarb…metabolic

76
Q

Death from aspirin poisoning is usually ______ and ______ imbalance

A

acidosis and electrolyte

77
Q

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

A

6-10 grams

78
Q

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

A

1%

79
Q

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

A

TRUE aspirin allergy

80
Q

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

A

CROSS-sensativity

81
Q

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

A

ASMATICS!!!….Asthma

82
Q

What is the ASPIRIN hypersensitivity TRIAD??

A
  1. Aspirin Hypersensativity 2.ASTHMA 3.Nasal Polyps
83
Q

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

A

PGE2…LEUKOTRIENES

84
Q

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

A

asthma…15

85
Q

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

A

acetic…“aspirin burn”

86
Q

Oral ulcerations = chewing aspirin-containing ____.

A

gum…whaaaa they make that?!

87
Q

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

A

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

88
Q

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

A

warfarin

89
Q

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

A

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

90
Q

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.

A

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

91
Q

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

A

81 mg…325 mg

92
Q

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

A

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

93
Q

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

A

10-15…4 g per day

94
Q

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

A

LOW DOSE

95
Q

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

A

4 days

96
Q

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

A

Plavix…aspirin

97
Q

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

A

consult the patient’s physician!!!!

98
Q

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

A

“catastophic”

99
Q

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

A

FIBRIN…thromboxane A2

100
Q

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 ________.

A

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Pharmacology (23 decks)

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