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N365: Pharmacology in Nursing > Week 6: Anti-Inflammatories > Flashcards

Week 6: Anti-Inflammatories Flashcards

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1
Q

Prototype Drugs for the Anti Inflammatory Category

A
  1. aspirin (Aspirin)
    2. acetaminophen(Tylenol)
    3. indomethacin (Indocin)
    4. ibuprofen (Motrin, Advil, etc.)
    5. celecoxib (Celebrex)
    6. ketorolac (Toradol)
    7. etanercept (Enbrel)
    8. hydroxychloroquine (Plaquenil)
    9. azathioprine (Imuran)
    10. allopurinol (Zyloprim)
    11. colchicine (Colcrys)
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2
Q

Prostaglandins

A

Modulate important components of inflammation: Body Temp increases, Pain Increases, Platelet Aggregation Increases

They are converted from arachidonic acid by cyclooxygenase (COX) enzyme

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3
Q

Chronic Inflammation = ???

A

More prone to blood clotting

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4
Q

COX 1

A

The first kind of COX enzyme that converts arachidonic acid to prostaglandins

HAS PROTECTIVE EFFECTS

Found in all tissues

Decreases stomach acid and increases gastric mucus = protects the stomach

Increases platelet aggregation = may prevent bleeding

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5
Q

COX 2

A

Second kind of COX

A major mediator of bad effects - we want to stop this one

Found mainly in INJURED tissues

increases inflammation

increases pain

causes fever

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6
Q

NSAIDS

A

Non steroidal anti inflammatory

many NSAIDS inhibit prostaglandin synthesis and many do so by targeting both COX 1 and 2

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7
Q

How do NSAIDS cause many adverse effects we see?

A

it blocks COX 1 (the protective effects/good stuff)

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8
Q

Salicylates

A

Class of anti inflammatories - active form

is so irritating it can only be used externally - so it includes Acetylsalicylic acid (Aspirin, ASA)

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9
Q

Prototype drugs for Salicylates

A

Aspirin (Metabolizes into the active metabolite of salicylic acid)

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10
Q

Aspirin is a ___ drug

A

ancient

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11
Q

Aspirin is used for what effects

A

Analgesic

Antipyretic

Anti Inflammatory

Anti Platelet

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12
Q

What is unique about aspirin

A

IRREVERSIBLY INHIBITS COX - good blocking COX 2 but blocks COX 1 which is also bad

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13
Q

What is important to know about clotting after taking aspirin

A

As long as ASA is still lingering it will effect COX thus impacting the life of the platelet as well

Every platelet of any age is effected by ASA, so once a platelet is effected it cannot clot well for the rest of its lifespan

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14
Q

Side effects from ASA are mostly due to what

A

inhibition of COX 1 enzyme

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15
Q

Since salicylic acids can only be sued externally what reason are they commonly used for

A

acne products

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16
Q

Actions of Aspirin

A
  1. Analgesia
  2. Antipyretic
  3. Anti Inflammatory
  4. Gastrointestinal
  5. Anticoagulation
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17
Q

What is the analgesia action of aspirin

A
  1. Effects PERIPHERAL more, not central, by preventing sensitization of pain receptors by inhibiting prostaglandin synthesis !!! - This is the main way ASA works, periphery
  2. Works somewhat centrally on the hypothalamus by modifying pain perception, but the action here is little and also the antipyretic effect takes place here
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18
Q

What is the antipyretic action of Aspirin

A

believed to act directly on heat regulating center in the hypothalamus

decreases fever but not below the set point

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19
Q

What is the anti inflammatory action of aspiring

A

inhibits prostaglandin synthesis (by irreversibly impacting Platelets and COX 1 and 2)

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20
Q

What is the GI action of aspirin

A

local irritation and also stimulation of the vomiting center in brain - since it blocks COX 1 it increases stomach acid and it will cause less mucus so there is a greater irritation risk

Also* if a stomach ulcer occurs you will bleed more from the anticoagulant effect and the acid will irritate flesh

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21
Q

What is the Anticoagulation effect of Aspirin

A

IRREVERSIBLY inhibits platelet aggregation, weakly inhibits prothrombin synthesis, and prolongs bleeding time

MORE LIKELY TO BLEED

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22
Q

Uses for Aspirin

A
  1. Effective in pain from inflammation (due to prostaglandin increases), BUT NOT sharp pain due to sensory nerve stimulation
  2. Anti pyretic effects - peripheral and central inhibition of prostaglandin (pyretic) activity
  3. Anti inflammatory - inhibits prostaglandin activity
  4. Anti platelet - antithrombotic effect by inhibiting thromboxane A2, a prostaglandin that induces platelet aggregation
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23
Q

What is the main reason we use ASA nowadays

A

Its Anti Platelet Effect

It blocks Thromboxane A2 which is a prostaglandin that induces platelet aggregation!

People are less likely to develop blood clots - daily ASA to prevent clots that cause MI/DVT - inhibits TXA-2 to stop platelets

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24
Q

It is important to know what about the excretion of ASA

A

IT IS EFFECTED BY URINE PH - if someone overdosed on it we could modify their urine pH to increase secretion

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25
Q

What are the ADRs of ASA like

A

widespread- many different effects - most are GI

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26
Q

What are the various ADRs of Aspirin

A
  1. Most are GI* - NOT an allergy but could be a SE - epigastric distress, NV, ulceration
  2. Respiratory - respiratory stimulation, due to increased O2 consumption - resp stimulation NOT usually a problem only seen taking too much
  3. CV - large doses cause peripheral vasodilation - NOT common due to low doses
  4. Allergic - low, but can cause asthma, angioedema, and urticaria
  5. Blood - Anemia, Thrombocytopenia, Coagulation Effects - iron deficiency with bleeding, low platelets and bone marrow depression (effects platelet fxn more than numbers), increases cap. permeability and increases bleeding time
  6. CNS - tremors, HA, vertigo, tinnitus, diplopia, agitation, can be ototoxic
  7. Metabolism effects
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27
Q

What is rare but can occur with too much aspiring

A

hepatic and renal toxicity

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28
Q

Why do we never give children with flu like illnesses aspirin?

A

Risk for Reyes Syndrome - potentially fatal swelling in brain and liver along with hypoglycemia

If there is a flu like viral illness, ASA weill leave them prone to Reyes Syndrome

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29
Q

What does it mean that ASA can be ototoxic

A

impacts 8th cranial nerve and too much is toxic to the ears

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30
Q

What is typical dosage for ASA in adults?

A

81 mg daily or 325 PO once

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31
Q

What is an important prototype drug that is non-antiflammatory analgesic, non opioid that is grouped with anti inflammatories and NSAIDS

A

acetaminophen (Tylenol, Tempra)

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32
Q

acetaminophen (Tylenol, Tempra)

A

a non anti inflammatory and non opioid analgesic - it can be used for its ANTIPYRETIC and ANALGESIC effects (same as Aspirin but without the anti inflammation)

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33
Q

acetaminophen is similar in use to ___ but what sets them apart

A

it is similar to NSAIDS but has NO anti inflammatory effects and NO effect on platelet aggregation

So it is good for bringing down mild to moderate pain and bringing fever down without bleeding

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34
Q

What is the action of acetaminophen

A

uncertain but it has both central and peripheral action - the central action is more important in this case compared to peripheral because it acts centrally more on perception of pain as compared to ASA

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35
Q

ADRs of Acetaminophen

A

Surprisingly free of ADRs at therapeutic doses (less or equal to 4g/day)

Large doses are extremely toxic to the liver - gets press because of liver failure

Chronic use can cause kidney damage (every day)

Many drugs have acetaminophen in it so keep that in mind when taking drugs to prevent overdose

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36
Q

____ is often used in similar instances with aspiring, but has fewer SE and now has an IV formulation (Ofirmev)

A

acetaminophen

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37
Q

What is the antidote to acetaminophen

A

acetylcysteine (Mucomyst)

sulforous compound that is a liquid and smells like rotten eggs- needs to be given cont. in precise intervals

Given with 8 hours of ingestion - 3 bags first over 1 hour, second over 4 hours, and third over 16 hours

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38
Q

What is important to know about Tylenol no 1-4

A

This is the brand name a company uses to show combinations of tylenol with codeine

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39
Q

Combination drugs containing acetaminophen have what suffix

A

-CET

ex: Percocet, Roxicet, etc

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40
Q

acetaminophen can be toxic to both ___ and ___

A

liver and kidneys

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41
Q

Other than ASA, what are other important NSAID prototype drugs to know

A

indomethacin (Indocin)

Ibuprofen (motrin, advil)

celecoxib (Celebrex)

ketorolac

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42
Q

What is the prototype NSAID that is an indole analog

A

indomethacin (Indocin)

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43
Q

What is the action for indomethacin (Indocin)

A

potent inhibitor of prostaglandin synthesis

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44
Q

ADRs of Indomethacin (Indocin)

A

GI (like most NSAIDS) - anorexia, NV, peptic ulcer, and hemorrhage

Headache

Dizziness

Tinnitus

Skin rash

Edema

Rarely - Bone marrow depression

Aggravates psych disturbances, parkinsons, and epilepsy

OCULAR CHANGES (retinal and corneal)

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45
Q

What is the unique side effect of indomethacin as compared to other NSAIDS

A

the headache - it is a distinct frontal headache (can be severe)

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46
Q

When is indomethacin given instead of ASA or a different NSAID

A

only in specific inflammatory conditions - not given for HA, pain, fever as a replacement to ASA or acetaminophen - but shares some mechanisms with the 2

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47
Q

What is important to know about what NSAIDs can hide

A

Can mask signs and symptoms of infection by decreasing fever redness and swelling

48
Q

___ to ___ of indomethacin patients have a SE, and __% will have to discontinue the drug due to the headache or a rash

A

1/2-1/3; 20%

49
Q

Indomethacin must be given with….

A

food milk or an antacid to slow absorption and decrease SE

50
Q

What is a unique use for indomethacin that is not as an NSAID

A

it can be given IV to close patent ductus arteriosus in preterm infants

51
Q

What is the prototype drug for NSAIDs that is a propionic derivative

A

ibuprofen (Motrin, Advil, etc)

52
Q

Action of ibuprofen

A

exact mode is unknown

Does inhibit synthesis and/or release of prostaglandin

53
Q

ibuprofen absorption has to be done

A

orally

54
Q

ADRs of Ibuprofen

A

NV, Diarrhea, Constipation, Heartburn - GI effects

Skin eruptions, pruritis, dizziness, blurred vision, fluid retention

55
Q

NSAIDS have an effect on blood flow to the kidneys so…

A

even one dose of an NSAID can decrease blood to kidney which leads to fluid retention and increased BP and then a HA potentially

56
Q

Ibuprofen can be toxic to …

A

the kidneys

57
Q

___ NSAIDS should be considered before oral NSAIDs and why?

A

Topical NSAIDS - they cause less ADRs and dont take as long as oral NSAIDs

58
Q

Give what with NSAIDs like ibuprofen to decrease GI symptoms

A

Food

59
Q

ALL NSAIDS except ___ and ___ can interfere with platelet function and prolong bleeding time - this effect is reversible in nearly every NSAID (except ___)

A

Salycylates and celecoxib; Aspirin

60
Q

When is ibuprofen contraindicated

A

in patients with a hx of ASA induced bronchospasm, or those with symptoms of asthma, rhinitis, nasal polyps, angioedema, urticaria

61
Q

If visual difficulties with ibuprofen occur…

A

stop the drug and have a complete eye exam done

62
Q

Caldolor

A

a new IV form of ibuprofen rarely used

63
Q

What is the class effect for NSAIDs

A

potential increased risk for cardiovascular events - increases thrombotic events, MI, CVAs, and heart failure

64
Q

What is a 2nd generation NSAID

A

a COX 2 inhibitor - it is an NSID that only blocks COX 2 rather than both COX 1 and 2

It is great for chronic pain and arthritis conditions

65
Q

Prototype COX-2 Inhibitor; 2nd Generation NSAID

A

celecoxib (Celebrex)

66
Q

Action of celecoxib

A

selectively inhibits COX-2 (an isoform of cyclooxygenase)

67
Q

ADRs of celecoxib

A

abdominal pain, diarrhea, dyspepsia -LOT LESS GI EFFECTS

renal toxicity, fluid retention, edema

  • STILL has kidney, HTN, and fluid volume concerns like other NSAIDs
68
Q

What is nice about using a COX-2 Inhibitor like celecoxib rather than a 1st generation NSAID

A

Since it only impacts the bad COX, there is less bleeding since no interference with platelet function and less GI effects since it doesnt inhibit acid inhibition

69
Q

When is celecoxib contraindicated

A

in persons allergic to sulfonamides (contains a sulfur molecule) - not a common issue

70
Q

Why is celecoxib the preferred 2nd generation NSAID over the first ever one, rofecoxib (Vioxx)

A

Vioxx was the first COX2 inhibitor made, but there is a higher incidence of cardiac issues and MI, and the company his this fact from the FDA

celecoxib has similar cardiac concerns but is used carefully and did not hide this fact

71
Q

What did the investigation into vioxx reveal

A

that ALL NSAIDs, except ASA, have risk for clots and MI concerns

72
Q

What is a prototype NSAID that is basically a parenteral form of ibuprofen

A

ketorolac (formerly known as Toradol)

73
Q

Action of ketorolac

A

inhibits prostaglandin synthesis !!! (inhibits cyclooxygenase, which decreases prost. synthesis and activity)

May also inhibit effects of other substances that sensitize pain receptors

74
Q

ADRs of ketorolac

A

CNS - drowsiness, sedation, dizziness, HA, sweating

CV - edema, HTN, dysrhythmias !!!!!!!

GI - nausea, GI pain, diarrhea, peptic ulceration

Other - decreased platelet adhesion, hyperkalemia, pain at injection site

NO KIDNEY PROBLEMS WITH THIS NSAID SINCE ITS ONLY USED IN SHORT TERM PAIN NOT LONGER TERM (long term could cause renal issues though)

75
Q

ketorolac is used for short term management of pain which is about how many days ?

A

up to 5 days

*this means rather than in rheumatoid conditions it is better in post operative and musculoskeletal conditions - so it can be given instead of morphine

76
Q

What can be used post op equivalent to morphine but without narcotic effects

A

ketorolac

77
Q

___ is a short term parenteral NSAID

A

ketorolac (not used orally)

78
Q

etanercept (Enbrel)

A

anti inflammatory
TNF (tumor necrosis factor) block
Anti Rheumatic
Biologic (meaning it looks at bio mechanisms not compounds adding or taking away)

79
Q

Why does entanercept (Enbrel) count as an anti inflammatory

A

it is a TNF blocker and TNF causes inflammation so blocking it will help lower inflammation

80
Q

Action of etanercept (Enbrel)

A

Suppresses inflammation by neutralizing TNF

Binds with TNF and prevents interactions with its normal receptors

In a long term inflammatory conditions this will decrease in drastically - before this it was symptom treatment but this can target the reason behind the inflammation

81
Q

How is absorption of etanercept done (route)

A

subcutaneous injection

82
Q

ADRs of etanercept (Enbrel)

A

injection site rxns - common - SIGNIFICANT concern regarding increased risk of infection (whole body drug –> systemic effects on immune system –> increased infection)

RARE: CNS disorders like mult. sclerosis, some hematologic disorders

83
Q

What is a big problem for using etanercept

A

very expensive - 1 year is 15000

but is v worth it to young people in chronic pain

84
Q

Why must CXR and TB skin tests and assessment for infection done before giving entanercept

A

people need skin tests and CXR because TB can lurk and blossom once immune system issues occur from taking this TNF blocker - we have to stop if infections develop

85
Q

What is important to know about “Me 2 Drugs”

A

they are drug copies that try to block inflammation in various ways, but can be helpful if one drug doesnt work since another might

ex: enteracept - copies: humira, cimzia, orencia, actemra (all work in different ways)

86
Q

hydroxychloroquin (Plaquenil)

A

An ANTIMALARIAL DRUG but ALSO used for inflammatory conditions

87
Q

Action of hydroxycloroquine (Plaquenil)

A

unknown for its anti inflammatory effect. May involve suppression of antigen responsible for hypersensitivity rxns causing malaria symptom development (interaction with DNA for malaria)

88
Q

ADRs of hyroxycloroquine (Plaquenil)

A

GI Upset (especially nausea)

Mild and transient HA

bone marrow depression

dermatitis, rashl, pruritus

alopecia

OCULAR ISSUES (retinal toxicity, photophobia, blurry vision, abnormal distant and peripheral visual fields)

89
Q

What is the biggest ADR concern when taking hydroxychloroquine (Plaquenil)

A

Ocular issues –> IT IS IRREVERSIBVLE

Progression will stop if drug is stopped but eye damage isnt as big of an issue as people originally thought but remember eye damage is irreversible still

90
Q

How does dose vary for hydroxychloroquine

A

it varies whether it is being given as an antimalarial or antirheumatic

91
Q

When taking hydrochloroquine it is important to do what yearly if at high risk or every 5 years if low risk

A

an eye exam

92
Q

hydroxychloroquine is not an effective treatment for what

A

COVID-19

93
Q

What is a prototype drug that is an immunosuppressive but also an anti inflammatory

A

azathioprine (Imuran)

94
Q

azathioprine (Imuran)

A

super strong immunosuppressant - sometimes used for inflammation, but ADR risk is high so it is not a common anti inflammatory anymore

95
Q

Action of azathioprine (Imuran)

A

inhibits cell proliferation by interfering with synthesis of DNA and RNA

can act as an anti inflammatory because it inhibits responses of cells like lymphocytes or macrophages as a result of immunosuppression

affects purine metabolism - less important

96
Q

ADRs of azathioprine (Imuran)

A

bone marrow depression

GI - NV, anorexia, jaundice

alopecia

hemorrhagic

cystitis

increased incidence of infection

neoplasm risk

VERY SERIOUS CONDITIONS CAN OCCUR - even high incidence of cancer due to immunosuppression

97
Q

What must be carefully considered before using azathioprine (Imuran)? What is an important use of azathioprine still used nowadays?

A

severity of adverse effects should be considered carefully - smaller doses can be given if used with allopurinol

Often still used with organ transplants to decrease rejection nowadays!

98
Q

The historical use of azathioprine is what

A

historical use for inflammatory prevention because of being a powerful immunosuppressant

99
Q

Gout

A

a distinct inflammatory condition in the same family as other forms of arthritis

often characterized by increases of uric acid in bloodstream which can precipitate in the joints

very common still - young middle aged men

a form of arthritis

100
Q

Most common area for gout

A

the great toe

101
Q

2 Important Anti Gout Medications

A

allopurinol

colchicine

102
Q

alopurinol (Zyloprim, Lopurin)

A

anti gout medication

inhibits production of uric acid

“prevents inflammation from gout”

103
Q

Action of allopurinol (Zyloprim, Lopurin)

A

interrupts process of purine degradation BEFORE URIC ACID IS FORMED

interrupted before uric acid production is complete by inhibiting xanthine oxidase

104
Q

ADRs of allopurinol

A

most common - DRUG RASHES

bone marrow depression, reversible hepatotoxicity, drowsiness

DOES have some liver effects though

can have serious impacts but many can take this med for years before having problems

105
Q

What is important to consider if taking allopurinol with an anticoagulant

A

allopurinol has effects on the liver and interferes with clotting factors - risk for bleeding

106
Q

What is important to think about when taking allopurinol?

A
  1. use with care with anticoagulants
  2. high fluid intake necessary
107
Q

What is febuxostat (Uloric) in reference to allopurinol

A

It is a new drug and first selective xanthine oxidase inhibitor that is NOT a purine analog

more potent than allopurinol BUT still inhibits the production of uric acid likle allopurinol

108
Q

colchicine (Colcrys)

A

specifically an anti gout anti inflammatory for gout

109
Q

colchicine has nothing to do with…

A

URIC ACID

110
Q

Action of colchicine

A

decreases inflammation in response to uric acid deposition into joints - very specific to gout but there is some interest in heart disease

111
Q

Can colchicine be used as a general anti inflammatory

A

NO it does not work on other inflammatory conditions since it is specific to uric acid deposition related inflammation

112
Q

ADRs of Colchicine

A

prolonged use = bone marrow depression, agranulocytosis, peripheral neuritis, aplastic anemia, acute poisoning

rare = cell depression - often only in short term use

given too quickly = acute poisoning –> bleeding and loss of fluids

113
Q

Is colchicine a first line treatment for gout

A

not it is a second line treatment for gout attack - we use NSAIDs and Steroids first nowadays

114
Q

Even __ doses of colchicine may prevent gout attacks

A

low

115
Q

what is the take home message about colchicine

A

it is specific to the inflammation caused by gout but does not effect the uric acid it just prevent deposition

can be used for chronic gout management and some heart disease use

116
Q

What is the big difference between allopurinol and colchicine

A

allopurinol = decreases uric acid

colchicine = does not impact uric acid, prevents deposition and inflammation

117
Q

probenecid

A

drug that increases uric acid excretion - sometimes used instead of allopurinol

N365: Pharmacology in Nursing (15 decks)

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