Pharm: Pain Meds - Iszard Flashcards

1
Q

what does aspirin irreversibly inhibit?

A

cyclooxygenase 1 AND 2

  • causes decrease in thromboxane (platelets can’t make more)
  • effects persist until cells make more COX (platelet half lie approx 8 days)
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2
Q

what does prostacyclin cause?

A

vasodilation, inhibits platelet aggregation (anti-thrombotic)

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3
Q

what does thromboxane A2 cause?

A

vasoconstriction, promotes platelet aggregation (thrombotic)

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4
Q

what does PGD2, PGE2 cause?

A

vasodilation, increased vascular permeability (inflammation)

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5
Q

expressed in all tissues, all the time

  • prominent role responding to physiologic stimuli
  • also contributes to response of any pathologic stimuli (inflammation)
A

COX-1

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6
Q

induced in “some” tissues, sometimes

  • physiologic role in KIDNEY
  • prominent role is response to any pathological stimuli (inflammation)
A

COX-2

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7
Q

which COX isozyme should especially be avoided in pt with CV risk factors?

A

COX-2

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8
Q

what NSAID is drug of choice for pts at risk of CV complications?

A

naproxen

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9
Q

what are the contraindications for NSAID use?

A
  • chronic kidney dz
  • active duedenal/gastric ulcer
  • CV disease
  • NSAID allergy
  • tx w/ anticoagulants (Warfarin)
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10
Q

what are the major beneficial actions of aspirin?

A
  • suppresses inflammation
  • mild/moderate pain relief
  • fever reduction
  • prevents MI/stroke -> d/t inhibition of COX-1 in platalets
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11
Q

what does aspirin increase the risk of?

A

bleeding in pts taking anticoagulants (d/t antiplatelet effects)

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12
Q

when are adverse outcomes of sodium and water retention seen?

A

pts with advanced, pre-existing renal dysfunction

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13
Q

why should aspirin be avoided in children with chicken pox/influenza?

A

risk of Reye syndrome (swelling of liver and brain)

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14
Q

why should aspirin be avoided in labor/delivery?

A

it can suppress spontaneous uterine contractions, induce premature closure of ductus arteriosus, and intensify uterine bleeding

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15
Q

what is the treatment of hypersensitivity to aspirin?

A

epinephrine

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16
Q

what are the important differences between aspirin and non-aspirin NSAIDs?

A
  • they are REVERSIBLE, so effects decline as blood levels decline
  • suppress platelet aggregation, but increase risk of MI/stroke (so should use lowest dose possible)
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17
Q

indicated for short-term (<5days) management of moderately severe pain

  • usually after surgery
  • NOT for pediatric pts, or minor pain
A

Ketorolac

NOTE: can cause peptic ulcers GI bleed, performation of stomach/intestines

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18
Q

indicated for:

  • moderate/severe RA
  • moderate-severe ankylosing spondylytis
  • moderate-severe osteoarthritis
  • painful bursitis/tendinitis
  • acute gouty arthritis
A

indomethacin

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19
Q

what is the contraindication for indomethacin use?

A

treatment of peri-operative pain in CABG surgery

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20
Q

indicated for:

  • mild-moderate HA pain, menstrual pain
  • minor aches/pains
A

ibuprofen

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21
Q

what are the contraindications for ibuprofen?

A
  • active gastric/duodenal ulcer

- significant hepatic or renal impairment

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22
Q

what are the warnings/precautions for ibuprofen?

A
  • heart failure, HTN
  • GI tract irritation
  • increased risk of renal toxicity
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23
Q

a sterile topical NSAID for opthalmic use

- inhibits intraoperative miosis

A

flurbiprofen

NOTE: contraindicated in pts who are allergic to IBUPROFEN

24
Q

NSAID used for:

  • osteoarthritis
  • RA
  • juvenile RA
A

meloxicam

25
Q

what are the contraindications of meloxicam?

A

hx of asthma, or other allergic-type reactions after taking NSAIDs
- CABG surgery

26
Q

NSAID used for relief of:

  • RA
  • osteoarthritis
  • anylosing spondylytis
  • tendonitis/bursitis
  • acute gout
  • pain
A

naproxen

27
Q

what are the contraindications of naproxen?

A

hx of asthma, urticaria, or other allergic-type rxn after taking NSAID

28
Q

what are the warnings/precautions of naproxen?

A
  • hepatotoxicity
  • thrombotic effects
  • can significantly compromise renal function in geriatric pts
29
Q

what are the warnings/precautions of diclofenac?

A

increased risk of SERIOUS CV thrombotic events, including MI/stroke
- risk may occur early and may increase with duration of use

30
Q

selctively blocks COX-2

  • suppresses inflammation, pain, fever
  • may cause LESS GASTRIC ULCERATION than nonselective inhibitors
  • does NOT inhibit platelet aggregation
A

celecoxib

NOTE: increases risk of MI/stroke, d/t blockade of prostacyclin synthesis in blood vessels

31
Q

suppresses pain and fever, but NOT inflammation

  • inhibition of prostaglandin synthesis in CNS, but not in periphery
  • does NOT impair renal function!
A

acetaminophen

NOTE: inhibits metabolism of warfarin, can increase risk of bleed

32
Q

what does acetaminophen overdose cause?

A

hepatic necrosis, from accumulation of toxic metabolite that forms when glutathione is depleted

33
Q

how is acetaminophen overdose treated?

A

acetylcysteine know this!

34
Q

what causes hepatic cell death in acetaminophen overdose?

A

an alternate metabolic route causes buildup of toxic products when glutathione is depleted

35
Q

what is the preferred end product of acetaminophen metabolism?

A

Ac-mercapturate

36
Q

pain relievers, with independent analgesic effects as well as ability to relieve depressive sx assoc w/chronic pain (MOA unknown)

A

TCA’s

  • duloxetine, venlafaxine used to treat neuropathic pain
  • WARNING: suicidality
37
Q

what are the 4 specific indications for pregabalin?

A
  1. neuropathic pain assoc w/diabetic neuropathy
  2. postherpetic neuralgia
  3. adjunctive therapy for partial seizures
  4. fibromyalgia first drug approved for it! but benefits are modest and fade
38
Q

broad-spectrum anti-seizure med

- 80% of prescriptions written for post-herpetic neuralgia, diabetic neurophathy, migraines, fibromyalgia, RLS

A

gabapentin

NOTE: alcohol, opioids and benzo’s may intensify depressant effects

39
Q

widely used for moderate/severe pain

  • codeine analog (blocks NE and 5HT)
  • more effective than codeine when combined w/aspirin or acetaminophen
  • less effective than morphine
A

tramadol

40
Q

what are the serious side effects of tramadol?

A
  1. seizures in epileptics
  2. can precipitate HTN crisis if combined w/MAOI
  3. serotonin syndrome if combined w/SSRI, TCA, MAOI
41
Q

what drug is reserved for patients who are not effectively treated w/other non-opioids and opioids?

A

tapentadol

  • moderate opioid agonist, similar to oycodone
  • causes less constipation than traditional opioids
42
Q

NMDA-antagonist used to

  • start/maintain anesthesia
  • post-operative pain
  • common psychological side effects (agitation, confusion)
A

ketamine

NOTE: has tendency to elevate BP

43
Q

a2-adrenergic agonist used for analgesia and sedation

  • short-term sedation in critically ill pts who were intubated
  • sedation prior to/during surgery
  • administered via IV
A

dexmedetomidine

NOTE: pregnancy category C, adverse effects on development

44
Q

a2-adrenergic agonist used for:

  • HTN (enhances hypotensive/depressant effects)
  • relief of severe pain (approved for treating severe cancer pain)
A

clonidine

NOTE: pregnancy category C, adverse effects on development

45
Q

what is the administration route of clonidine?

A

continuous infusion through epidural catheter KNOW this

46
Q

selective antagonist at N-type voltage gated Ca-channels on nociceptive neurons

  • prevents transmission of pain signals from periphery to brain
  • indicated only for CHRONIC SEVERE pain
A

ziconotide

NOTE: has adverse CNS effects that generally resolve w/in 2 weeks of drug discontinuation

47
Q

what is the administration route for ziconotide?

A

intrathecal (injection into spinal canal)

48
Q

prototype for agonist-antagonist opioids used to treat mild/moderate pain
- produces analgesia, sedation, respiratory depression

A

pentazocine

49
Q

how can toxicity of pentazocine be reversed?

A

higher levels of naloxone

50
Q

prototype for agonist/antagonist opioids used to treat mild/moderate pain

  • produces analgesia, sedation, respiratory depression
  • usually given IM or IV
  • primarily used to treat addicts
  • binds very tightly to receptors and cannot be readily reversed by naloxone
A

butorphanol

NOTE: prolongs QT interval, increasing cardiac work -> contraindicated in MI

51
Q

what is the treatment method of choice for using butorphanol for migraines?

A

nasal spray

52
Q

what is the drug of choice for terminating ongoing migraine attacks?
- well tolerated at usual doses, can cause N/V, weakness in legs, myalgia, numbness/tingling of fingers/toes

A

ergotamine

NOTE: pregnancy category X

53
Q

less effective than sumatriptan for terminating ongoing migraine atack, but has lower incidence of recurrence
- does NOT cause N/V, but DIARRHEA is prominent

A

dihydroergotamine

54
Q

5HT agonists, first-line drugs for terminating migraine attacks

  • relieved headache and assoc sx: nausea, neck pain, photophobia, phonophobia
  • rapid onset of effects (15min after subQ or intranasal)
A

sumatriptan

55
Q

what should sumatriptan NOT be combined with?

A
  • ergot alkaloids (ergotamine, dihydroergotamine)

- MAOI, SSRI, SNRI