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Analgesics Flashcards

1
Q

Prostaglandins mediate what?

A

Local inflammatory mediators

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2
Q

PGE2 sensitizes what?

A

Nerve endings to the action of bradykinin, histamine, and other chemical mediators

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3
Q

All NSIDs act how?

A

By inhibiting the synthesis of prostaglandins

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4
Q

What are the two conventional NSAIDs?

A

Acetylsalicylic Acid

Celecoxib

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5
Q

What is the “other” NSAID?

A

Acetaminophen

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6
Q

What is the life cycle of platelets?

A

7-10 days

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7
Q

Why is it best to discontinue NSAIDs for 2 weeks before surgery?

A

NSAIDs kill off platelets, so you need to allow them to regenerate before surgery

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8
Q

What dose of ASA is needed for analgesia?

A

160-325mg

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9
Q

What dose of ASA is needed for anti-pyretic?

A

160-325mg

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10
Q

What dose of ASA is needed for anti-inflammatory?

A

325-650mg

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11
Q

What dosing of ASA will kill platelets?

A

80-160mg

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12
Q

How/why does ASA kill platelets?

A

Causes irreversible inhibition of COX-1(TXA2) for the life of the platelets

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13
Q

What two benefits does Acetaminophen have over ASA?

A

No GI effects

Safe in pregnancy

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14
Q

What two disadvantages does Acetaminophen have compared to ASA?

A

No inflammatory control

No platelet inhibition (may not be an advantage…)

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15
Q

What is the MOA of Aspirin?

A

Irreversibly, non-selectively inhibits COX, reducing PG and TXA2 synthesis

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16
Q

What are the two common adverse effects of Aspirin?

A

Bleeding time doubles

Headache

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17
Q

What is the one hypersensitivity reaction to Aspirin?

A

Angioedema

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18
Q

What conditions cause Reye’s Syndrome?

A

A child with a fever from an active viral infection taking Aspirin

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19
Q

What three things occur in Reye’s Syndrome?

A

GI disturbances
Liver Degeneration
Encephalopathy

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20
Q

What is the rate of mortality in Reye’s Syndrome?

A

35%

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21
Q

Reye’s Syndrome can occur in kids up to about what age?

A

15

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22
Q

Aspirin reacts with what three groups of drugs?

A
  1. Ophthalmic/oral NSAIDS and Omega-3s
  2. Aectaminophen and Cyclosporine
  3. Steroids
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23
Q

What is the result of an Aspirin and NSAID/Omega-3 interaction?

A

Hemorrhage risk - additive

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24
Q

What is the result of an Aspirin and Acetaminophen/cyclosporine interaction?

A

Nephrotoxicity - additive

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25
Q

What is the result of an Aspirin and Steroid interaction?

A

GI toxicity - additive

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26
Q

What are the 5 contraindications associated with Aspirin?

A
  1. Hemorrhagic disorders
  2. Pregnancy, esp. 3rd trimester
  3. Corneal denervation/dry eye
  4. NSAID/ASA induced asthma
  5. Chronic GIT inflammation/active peptic ulcer
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27
Q

What are the two indications for Acetaminophen?

A

Mild pain

Fever

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28
Q

What is the MOA of Acetaminophen for the analgesic effect?

A

Inhibits COX and enhances 5-HT release

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29
Q

What is the MOA of Acetaminophen for the antipyretic effect?

A

Acts centrally at the hypothalamus by inhibiting PG synthetase

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30
Q

Acetaminophen only inhibits inflammation where?

A

Centrally - not peripherally

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31
Q

What are the 3 common side effects of Acetaminophen?

A

Nausea
Rash
Headache

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32
Q

What are the 3 serious adverse effects of Acetaminophen?

A

Acute hepatotoxicity
Acute renal tubular necrosis
Chronic analgesic nephropathy

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33
Q

What are the three categories of drugs that interact with Acetaminophen?

A

Acetaminophen/antihitstaminic combos
ASA
Lidocaine Topical

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34
Q

What is the effect of the interaction of Acetaminophen with acetaminophen/antihistaminic combos?

A

Hepatotoxicity - additive

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35
Q

What is the effect of the interaction of Acetaminophen with ASA?

A

Nephropathy - additive

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36
Q

What is the effect of the interaction of acetaminophen with topical lidocaine?

A

Methemoglobinemia - additive

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37
Q

What are the 4 indications for Celecoxib?

A

Arthritis
Ankylosing Spondylitis
Dysmenorrhea
Acute pain

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38
Q

What is the MOA of Celecoxib?

A

Selectively inhibits COX-2 and reduces PG synthesis

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39
Q

What is the common adverse effect of Celecoxib?

A

Headache

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40
Q

What are the 3 cardiovascular black box warnings of Celecoxib?

A

Stroke
Myocardial infarction
Congestive heart failure

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41
Q

What are the 2 GI black box warnings for Celecoxib?

A

Bleed

Ulceration/perforation

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42
Q

Celecoxib contains what moiety?

A

Sulfonamide

43
Q

What are the two drug categories that interact with Celecoxib?

A

NSAIDS (esp Ketorolac)/Corticosteroids

Azoles

44
Q

What is the effect of the interaction of NSAIDs/Corticosteroids with Celecoxib?

A

Hemorrhage

45
Q

What is the effect of the interaction of Celecoxib with Azoles?

A

Impaired metabolism (buildup of celecoxib)

46
Q

What is the contraindication to Celecoxib?

A

Sulfonamide allergy

47
Q

What does neurogenic pain respond best to?

A

Anticonvulsants or antidepressants

48
Q

What type of drug is the drug of choice for severe chronic malignant/nonmalignant pain?

49
Q

What FDA class do narcotics belong to?

50
Q

What is the MOA of Hydrocodone?

A

Inhibit adenylyl cyclase activity
Enhance K+ outflow to hyperpolarize nerves affecting neuronal excitability and muscle tone
Stimulates prolactin and growth hormone release

51
Q

What receptors does Hydrocodone act through?

A

G-protein-coupled Mu, Kappa and delta “opioid” receptors

52
Q

Where does hydrocodone act, centrally or peripherally?

53
Q

What are the 6 common adverse effects of Hydrocodone?

A 
Lightheadedness
Dizziness
Sedation
Miosis
Puritis
Flushing
54
Q

Why might Hydrocodone cause flushing?

A

Histamine release

55
Q

What are the 3 cardiovascular adverse effects of Hydrocodone?

A

Bradycardia
Tachycardia
Orthostatic hypotension

56
Q

What are the 3 CNS adverse effects of Hydrocodone?

A

Drowsiness
Mood changes
Elevated intracranial pressure

57
Q

How long does it take for drowsiness to kick in with hydrocodone use?

A

About 1 week

58
Q

With Hydrocodone use, are mood changes quick to occur, or slow to occur?

A

Quick tolerance

59
Q

With Hydrocodone use, what causes pupillary miosis?

A

Excitatory action on the parasympathetic nerve to the iris sphincter

60
Q

What are the 3 drugs that interact with Hydrocodone?

A

Anticholinergics
Classic Antihistamines
Carbonic Anhydrase Inhibitors

61
Q

What occurs in the interaction of Hydrocodone and Anticholinergics?

A

Constipation/paralytic ileus - additive

62
Q

What occurs in the interaction of Hydrocodone and Classic Antihistamines?

A

CNS depression - additive

63
Q

What occurs in the interaction of Hydrocodone and CAIs?

A

CNS toxicity - additive

64
Q

What is the contraindication for Hydrocodone?

A

Mydriatic procedures - antagonizes

65
Q

What is the Non-Conventional opioid?

66
Q

What is the indication for tramadol?

A

Moderate/severe pain

67
Q

What is the MOA of Tramadol?

A

Mu receptor agonist - effect is greater with active metabolite
Weak inhibitor of Ne/5-HT reuptake

68
Q

What does NE stand for?

A

Norepinephrine

69
Q

What is 5-HT?

70
Q

What are the 3 common adverse effects of Tramadol?

A

Headache
Puritis
Flushing

71
Q

What is the CNS adverse effect of Tramadol?

A

Serotonin syndrome

72
Q

What is the cardiovascular adverse effect of Tramadol?

A

Orthostatic hypotension

73
Q

What are the 3 classes of drugs that interact with Tramadol?

A

Anticholinergics
Classic antihistaminics
Azoles

74
Q

Tramadol antagonizes which ACh receptors?

A

Both muscarinic and nicotinic

75
Q

Migraines are what kind of disorder?

A

Neurovascular

76
Q

Up to 1/3 of patients with migraine experience what?

A

Visual aura

77
Q

High levels of what are associated with migraines?

78
Q

What signs are associated with the prodromal phase of a migraine?

A

Arterial vasoconstriction

Release of serotonin

79
Q

What signs are associated with the headache phase of migraines?

A

Cerebral vasodilation

Lower than normal levels of serotonin

80
Q

What is the top prophylactic migrane drug class?

A

Topiramate

81
Q

What are the two classes of abortive drugs for migraines?

A

Triptans

Ergotamines

82
Q

What are the 2 indications for Sumatriptan?

A

Acute migraines

Cluster headaches

83
Q

What is the MOA of Sumatriptan?

A

Selectively activates vascular serotonin 5HT-1 receptors, causing intracranial vasoconstriction
Stimulates neuronal serotonin receptors, decreasing the release of peptides including Substance P and CGRP

84
Q

What is the common adverse effect of Sumatriptan?

85
Q

What is the 1 hypersensitivity to Sumatriptan?

A

Angioedema

86
Q

What are the 2 ocular adverse effects of Sumatriptan?

A

Partial vision loss

Transient/permanent blindness

87
Q

What is the 1 caution for Sumatriptan?

A

Hypertension (it causes vasoconstriction)

88
Q

What are the 2 indications for Ergotamine?

A

Migraine

Cluster headache

89
Q

Ergotamine is structurally similar to what?

A

Biogenic Amines

90
Q

What is the MOA of Ergotamine?

A

Stimulates serotonin receptors producing intracranial vasoconstriction, and inhibition of CN-V pain transmission

91
Q

What is the 1 adverse effect of Ergotamine?

A

Photosensitivity

92
Q

What are the 4 drug types that inhibit ergotamine metabolism?

A

Macrolides
Azoles
Fluoroquinolones
Cyclosporine

93
Q

What happens when tetracyclines interact with Ergotamine?

A

May increase risk of Ergot toxicity

94
Q

What happens with Ergotamine interacts with Timolol?

A

Peripheral vasoconstriction is enhanced

95
Q

What are the 2 indications for Topiramate?

A

Migraine prophylaxis

Seizures

96
Q

What requires a higher dose of Topiramate, migrain prophylaxis, or seizures?

97
Q

What is the MOA of Topiramate?

A

Blocks voltage-gated Na channels
Augments GABA activity
Antagonizes glutamate receptors
Inhibits CAI

98
Q

What are the 5 common adverse effects of Topiramate?

A

Bleeding
Nystagmus
Diplopia
Visual disturbance

99
Q

What are the 5 serious adverse effects of Topiramate?

A 
Angle closure glaucoma
Myopia
Maculopathy
Hemorrhage
Anemia
100
Q

What may occur when Topiramate interacts with CAIs or Steroids?

A

Hypokalemia - additive

101
Q

What may occur when Topiramate interacts with Gluoroquinolones?

A

QT prolongation

102
Q

What may occur when Topiramate interacts with Opioids or classic Antihistamines?

A

Increased risk of CNS depression

103
Q

What is the 1 caution for Topiramate?

A

Hemorrhage

Systemic Pharm (15 decks)

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