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Clinical Pharmacology > Analgesia - APAP, NSAID, Muscle Relaxant > Flashcards

Analgesia - APAP, NSAID, Muscle Relaxant Flashcards

1
Q

NSAID Families

A
  1. Carboxylic Acids
  2. Propionic Acids
  3. Acetic Acid Derivatives
  4. Enolic Acids
  5. Fenamates
  6. Napthylkanones

Paxton: start with Ibuprofen or Naproxen –> enolic acids –> acetic acid

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2
Q

NSAIDs MOA?

A

Inhibit COX1 +/- COX2

1 - regulates most normal cellular processes
2 - expressed during inflammation

Reversibly bind platelets, except ASA

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3
Q

What conditions are NSAIDs indicated?

A
  1. Analgesia
  2. Antipyretic
  3. Dysmenorrhea
  4. Anti-inflammatory (rheum conditions)
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4
Q

Who are NSAIDs contraindicated in?

A

Recent CABG

Pregnancy

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5
Q

NSAIDs are pregnancy category ___ because?

A

Category C

  • early: miscarriage
  • later: fetal renal dysfunction, premature closure of PDA
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6
Q

General side effects/ risks of NSAIDs?

A
  1. GI, CV, Renal
  2. Caution w/HTN, HF, CKD, asthma
  3. May precipitate asthma and anaphylactoid reaction in ASA-sensitive pt (not IgE-mediated)
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7
Q

Describe the GI side effects related to NSAIDs?

A
  • Dyspepsia/gastritis & ulceration/perforation*
  • INC r/o GI bleed w/anti-plt, EtOH, steroids
  • may exacerbate IBD
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8
Q

Describe the CV side effects related to NSAIDs?

A
  • r/o thrombosis [BBW INC r/o CV events]
  • d/c ALL (except ASA) in AMI pt
  • caution w/warfarin
  • reversible plt dysfunction –> INC bleeding time
  • may interfere w/anti-plt effect of ASA (try other analgesics first)
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9
Q

Describe the renal side effects related to NSAIDs?

A
  • DEC efficacy of diuretics (loops/thiazides & ACE/ARB) –> AKI risk
  • INC [Li]
  • nephrotoxicity: fluid retention, AIN, ATN
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10
Q

Who must you avoid NSAIDs in?

A

Pt with high GI and CV risk

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11
Q

Your elderly patient is on diuretics and ACE/ARB. You need to start him on NSAIDs now too. What must you monitor?

A

Monitor renal function and serum K within 7 days of starting the NSAID

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12
Q

Recognize Carboxylic Acids

A
  1. ASA*
  2. Salsalate
  3. Diflunisal
  4. Choline Mag Trisalicylate
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13
Q

Recognize Propionic Acids

A
  1. Ibuprofen*
  2. Naproxen*
  3. Fenoprofen
  4. Ketoprofen
  5. Flurbiprofen
  6. Oxaprozin
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14
Q

Recognize Acetic Acid Derivatives

A
  1. Indomethacin*
  2. Diclofenac*
  3. Ketorolac*
  4. Sulindac
  5. Etodolac
  6. Tolmetin
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15
Q

Recognize Enolic Acids

A
  1. Piroxicam (better CV, worse GI)

2. Meloxicam (worse CV, better GI)

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16
Q

Which NSAID is safest for breastfeeding women? It also has low GI toxicity.

A

Ibuprofen

17
Q

Which NSAID is safest in terms of CV toxicity?

A

Naproxen

18
Q

Which propionic acid has more GI toxicity, ibuprofen or naproxen?

A

Naproxen

19
Q

Which acetic acid is used for PDA closure? Give it to the baby, but don’t give to pregnant women!

A

Indomethacin (IV for PDA closure)

20
Q

What are two side effects of Indomethacin?

A
  • worst GI toxicity

- high r/o thrombosis

21
Q

Acetaminophen max dose

A
  • 1,000 mg/dose

- 4g/day

22
Q

Acetaminophen indications

A
  • Antipyresis

- Mild-mod pain –> IV APAP more robust that PO

23
Q

Acetaminophen MOA

A
  • Not clear
  • Analgesia: Inhibit NO pathway mediated by certain NTs
  • Antipyretic: inhibits endogenous pyrogens
24
Q

Acetaminophen ADRs

A

-Hepatotoxicity (inc glutathione–> acetylimidoquinone)

  • > 3 drinks/day + APAP
  • > 4g/day (50% unintentional, iatrogenic)
  • Additive effect if given with =/> 1 hepatotoxic med (INH, etc)
25
Q

Acetaminophen Hepatotox tx

A

Acetylcysteine- given within 8-10 hr of OD

26
Q

Acetaminophen and Pregnancy

A
  • Category C

- Occasional use is fine for mild-mod pain

27
Q

Prescribing APAP

A

-put max tabs/day in sig to help keep patients from going over 4g/day

28
Q

Cyclobrenzapine

A
  • MOA: near identical to amitriptyline
  • Indications: SHORT-TERM (2-3 wks) muscle spasms–> has most evidence for efficacy
  • Interactions: death with CNS depressants, don’t give 14d of MAOI, seizure reported with tramadol
  • CI in pts with arrhythmia, AMI, HF
  • ADRs: sedation, dizziness, xerostomia quinidine-like effect (QT-prolongation)**
29
Q

Carisoprodol

A
  • MOA: unknown
  • Indication: don’t use according to MISTER Paxton
  • Schedule IV drug
  • Interactions: additive sedation with CNS depressants
  • ADRs: dizziness/sedation, transient quadriplegia, temporary loss of vision**
30
Q

Baclofen

A
  • Indications: SC injury/MS

- Withdrawal sx or worsening spasticity if not tapered over 2 wks

31
Q

Dantrolene

A
  • Spasticity in BS or SC injury
  • Also used for malignant hyperthermia (IV)

ADR: dose-dependent hepatotoxicity

32
Q

You should avoid this acetic acid derivative at all costs, due to toxicity, especially with CV events. What are the other side effects?

A

Diclofenac

CV events; greatest r/o thrombosis

Increased HTX (dili drug) 
Increased GI tox
33
Q

Your patient requires a pain med. Which potent NSAID could you give IV. You must limit IV/IM to less than 5 days otherwise there is increased risk of ____.

A

Ketorolac

AKI > 5d

34
Q

3 drugs to minimize GI side effects of NSAIDs. Which is preferred?

A
  1. Misoprostol
  2. H2Ras (famotidine)
  3. PPIs (omeprazole)**
35
Q

Misoprostol is a progesterone analogue used to prevent gastric ulcers. Know these other two things:

A
  • SE: diarrhea

- Cat X (abortion)

36
Q

What’s the 1 Cox-2 selective NSAID still on market?

A

Celecoxib

37
Q

What’s the main use of Cox-2 inhibitors?

A

Anti-inflammatory for rheum

AE:

  • less GI toxicity
  • nephrotoxicity
38
Q

Which drugs are used for MS, SC injury?

A

Antispastics

  • baclofen
  • dantrolene
39
Q

Which muscle relaxants are used for other msk conditions?

A

Antispasmodics

  • cyclobenzaprine*
  • carisoprodol*
  • metaxalone
  • methocarbamol
  • chlorzoxazone
  • tizanidine
  • orphenadrine

Clinical Pharmacology (54 decks)

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