10. Analgesics Flashcards

1
Q

Arachidonic acid is derived from

A

phospholipids in membranes. Enzyme phospholipase

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2
Q

Arachidonic acid can be broken down into two different pathways, what are they

A

cyclooxygenase and lipoxygenase pathway

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3
Q

What are the products of the cyclooxygenase pathway

A

-Prostaglandins and thromboxane

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4
Q

What are the products of the lipoxygenase pathway

A

-5-HETE and leukotrienes

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5
Q

What are the different peripheral analgesics

A
  • Acetaminophen

- NSAIDs

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6
Q

MOA of acetaminophen

A

-Inhibition of cyclooxygenase in different manner from NSAID

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7
Q

Clinical activities of acetaminophen

A
  • Analgesia
  • Antipyretic
  • No anti-inflammatory effects
  • No inhibition of platelet aggregation
  • No inhibition of platelet aggregation
  • no gastric irritation
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8
Q

T/F Acetaminophen crosses the placenta

A

t

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9
Q

Describe the toxicity of acetaminophen

A
  • Acute toxicity with as little as 6 g taken within a short period
  • Metabolite NAPQI binds to liver proteins injuring hepatocytes
  • Hepatotoxicity
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10
Q

How is hepatotoxicity induced by acetaminophen treated

A

gastric lavage

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11
Q

What is the daily max dose for Acetaminophen for adults

A

4 gm

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12
Q

Mechanisms of analgesia for NSAIDs

A
  • inactivation of cyclooxygenase

- Inhibition of bradykinin synthesis

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13
Q

Anti-inflammatory mechanism of NASIADs

A
  • Inactivation of cyclooxygenase
  • Inhibition of WBC migration
  • Inhibition of WBC lysosomal enzyme release
  • Inhibition of phosphodiesterase
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14
Q

Anti-pyretic mechanism of NSAIDs

A

-Inhibition of prostaglandin synthetase in hypothalamus

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15
Q

T/F NSAIDs don’t have a ceiling effect

A

f

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16
Q

Adverse effects of NSAIDs are

A
  • Allergy
  • Anemia
  • Bronchospasm
  • Increased risk of coronary and cerebrovascular thrombotic events
  • GI irritation/bleeding
  • Inhibits platelet aggregation
  • Hepatotoxic
  • Renal toxicity (renal papillary necrosis)
  • Mutagenic
  • Carcinogenic (leukemia possible with indomethacin, phenylbutazone)
  • Fetotoxicity
  • Reye’s syndrome (kids)
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17
Q

Describe the fetotoxic effects of NSAIDs in 1st, 2nd and 3rd trimesters

A

1st
-Teratogenic effects

2nd and 3rd

  • Premature closure of ductus arteriosis
  • Fetal pulmonary hypertension
  • Prolonged gestation
  • Decreased uterine contractions
  • Bleeding at delivery
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18
Q

NSAID drug interactions

A
  • Anticoagulations
  • Triamterene
  • Lithium
  • Phenytoin
  • Valproic acid
  • Digitalis
  • Cyclosporine
  • Fluoroquinolones
  • Imidazole antifungals
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19
Q

T/F NSAIDs should be taken on an empty stomach

A

f

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20
Q

Mixture of NSAIDs with _ increases risk of gastritis

A

alcohol

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21
Q

Contraindications for NSAIDs

A
  • Allergy
  • Alcoholism
  • Asthma
  • Gastritis/ peptic ulcers
  • Pregnant
  • Blood dyscrasia
  • Renal function impairment
  • Psychiatric illness
  • Recent coronary artery bypass graft (CABG)
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22
Q

Indomethacin belongs to what drug category

A

NSAIDs (Indoleacetic acid)

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23
Q

Incidactions for indomethacin

A
  • Osteoarthritis

- Rheumatoid arthritis

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24
Q

Indomethacin shouldn’t be used in what populations

A

pediatric and geriatric and pregnant

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25
Q

Indomethacin may worsen what diseases

A

CNS diseases such as epilepsy and risk of leukemia

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26
Q

What drug class does Nabumetone belong to

A

NSAIDs (Naphthylakanones)

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27
Q

Nabumetone is primarily used for

A

osteoarthritis and rheumatoid arthritis and TMJ

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28
Q

Nabumetone is FDA class _

A

C

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29
Q

Other names for indomethacin and Nabumetone are

A

indocin and relafen

30
Q

Primary in dication for piroxicam are

A
  • OA
  • RA
  • Gout
31
Q

Piroxicam may produce what types of symptoms

A

flu like

32
Q

Diclofenac is indicated for

A

primarily arthritis but good for acute dental pain

33
Q

T/F diclofenac has minimal effect on platelets

A

t

34
Q

What risk does diclofenac have

A

risk of bone marrow suppression

35
Q

Diclodenac is FDA class

A

B

36
Q

What drug category does piroxicam fall under

A

NSAID (oxicam)

37
Q

What drug class does diclofenac belong to

A

NSAID (phenylacetic acids)

38
Q

What are the different NSAID propionic acids

A
  • Ibuprofen
  • Fenoprofen
  • Fluribiprofen
  • Ketoprofen
  • Naproxen
  • Oxaprozin
39
Q

Propionic acids are good for treating what kinds of pain

A

acute pain

40
Q

Other names for ibuprofen are

A

motrin and advil

41
Q

Indications for ibuprofen

A

mild to moderate pain

42
Q

What are the doses for ibuprofen for analgesia and inflammation

A
  • Analgesia= 200-400 mg 6hrs

- Anti-inflammation= 600-800mg 6hrs

43
Q

T/F Ibuprofen has been associated with sedation

A

t

44
Q

Other name for fluribprofen is

A

ansaid

45
Q

Issues with flurbiprofen

A
  • *not indicated for routine analgesic use

- Potentially fetotoxic and embryotoxic

46
Q

Other names for naproxen

A

aleve and anaprox

47
Q

Indications for naproxen

A

mild to moderate dental pain

48
Q

Naproxen is associated with _ in young kids

A

rash

49
Q

Avoid what form of naproxen in the elderly

A

Na+ salt form

50
Q

What form of naproxen should be avoided for initial therapy

A

delayed release

51
Q

Etodoloc belongs to what family of NSAIDs

A

pyranocarboxylic acid

52
Q

Other name for etodoloc is .

A

lodine

53
Q

Indications for Etodoloc

A

Mild to moderate pain

54
Q

Etodoloc is associated with abnormal

A

fetal limb development and decreased fertility, testicular atrophy

55
Q

Another name for aspirin is

A

acetylsalicylic acid

56
Q

Other Salicylates are

A

Aspirin and diflunisal

57
Q

All salicylates are associated with _ syndrome

A

reyes

58
Q

Salicylates should be avoided in what population

A

children (avoid in treating fever due to viral illness –> reyes)

59
Q

Diflunisal has a (greater/lesser) effect on platelets compared to ASA

A

lesser

60
Q

Diflunisal shouldn’t be used in combo with

A

acetaminophen

61
Q

Celecoxib is what class of NSAID

A

COX2 inhibitor

62
Q

Celecoxib is indicated for

A

RA and OA ONLY

63
Q

Celecoxib has a (higer/lower) incidence of gi effects

A

lower

64
Q

T/F Celecoxib is indicated for odontogenic pain

A

f

65
Q

Celecoxib puts patients at (increased/decreased) risk of CV events, MI, storke, etc.

A

increased

66
Q

T/F There is cross reactivity between celecoxib and other NSAIDs

A

t

67
Q

FDA classification of celecoxib

A

C

68
Q

Avoid celecoxib in patients with

A
  • CVD
  • daily aspirin use
  • Hypersensitivity
  • Asthmatics
  • Pregnant
69
Q

Metabolize of celecoxib is antagonized by

A

fluconazole and other agents metabolized via cytochrome p450 2C9

70
Q

Prostaglandins are involved in

A

GI mucosal protection (mediate pain, fever and inflammation)

71
Q

Thromboxanes are involved in

A

hemostasis