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N926 Pharmacology > Non-Opioid Analgesics > Flashcards

Non-Opioid Analgesics Flashcards

1
Q

NSAIDs MOA

A

Cyclooxygenase (COX) inhibitors
Prevent arachidonic acid binding to COX enzyme
Inhibit prostaglandin biosynthesis
Analgesic, anti-inflammatory, antipyretic

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2
Q

COX-1

A

Cyclooxygenase isoenzyme 1
Renal function maintenance
GI tract mucosal protection
Thromboxane A2 (platelet aggregation)

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3
Q

COX-2

A

Cyclooxygenase isoenzyme 2
Pain mediation
Inflammation
Fever

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4
Q

Non-Selective NSAIDs

A

COX 1 & COX 2 isoenzymes
Limited use in perioperative setting d/t GI toxicity & platelet dysfunction
Delayed bone healing
Toradol (Ketorolac) most commonly used peri-op

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5
Q

Toradol (Ketorolac)

A

Non-selective NSAID
15mg IV or IM Q6H
Decrease dose in elderly patients
Known renal impairment do not administer

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6
Q

COX-2 Inhibitor

A

No platelet aggregation inhibition

Celebrex only available COX 2

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7
Q

Celebrex (Celecoxib)

A

COX-2 inhibitor
Decreased GI toxicity
Increased cardiovascular risk
Commonly given as ERAS protocol (enhanced recovery after surgery)

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8
Q

Celebrex Dose

A

400mg PO pre-op

200mg BID x5 days post-op

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9
Q

NSAIDs PK

A 
Weak acids
Low Vd 0.1-0.3L/kg
Rapid GI absorption
Increased protein binding
Primarily liver metabolism
Eliminated by renal & biliary excretion
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10
Q

NSAIDs SE

A

Impaired platelet function primarily via COX-1
GI complications: Mild ulcers to perforation & bleeding (elderly, H pylori infection, previous ulcer, concomitant use - ASA, anticoagulants, or corticosteroids)
Cardiovascular: Increased MI risk, heart failure, & hypotension
Renal: Na+ excretion, tubular function, interstitial nephritis, & reversible failure
Liver: Transaminase level elevation & liver failure
Pulmonary: ASA exacerbated disease r/t COX-2
Hypersensitivity rare - allergic rhinitis + nasal polyps + asthma = anaphylaxis
Drug-drug interactions: Increased bleeding w/ antiplatelet agents & decreased digoxin/lithium clearance (secondary to prostaglandin inhibition & altered renal flow)

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11
Q

Aspirin ASA

A

Salicylic acid derivative
Irreversible platelet inhibitor - primary use
Overdose S/S: Abdominal pain, N/V, hearing impairment, CNS depression
Higher doses can result in metabolic acidosis, renal failure, CNS changes (agitation, confusion, coma), & hyperventilation w/ respiratory alkalosis
Urine alkalinization increases salicylate elimination

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12
Q

ASA Metabolism

A

Rapidly metabolized - plasma esterases, erythrocytes, & liver

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13
Q

Acetaminophen (Tylenol)

A

Analgesic & antipyretic properties
Central analgesic effect via serotonergic pathway activation & antagonism NMDA, substance P, and nitric oxide pathways
NO anti-inflammatory actions

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14
Q

Acetaminophen Metabolism

A

Metabolized in liver
Chronic usage <2g not associated w/ liver damage
Metabolite N-acetyl-p-benzoquinoeimine leads to liver failure by depleting glutathione (natural antioxidant)
Treatment: Charcoal to remove acetaminophen & acetylcysteine to replace glutathione

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15
Q

Acetaminophen Dose

A

325-650mg Q4-6H
Do not exceed 4,000mg per 24hrs (2,000mg for chronic alcoholics)
Ofirmev IV 1,000mg Q6H

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16
Q

Gabapentin

A

Structural analogue of gamma-aminobutyric-acid (GABA)
Acts on VG Ca2+ channels inhibiting glutamate
Approved as anticonvulsant
Demonstrated some efficacy in neuropathic pain
ERAS protocols - generally accepted as effective in reducing immediate post-op pain & opioid consumption

17
Q

Gabapentin PK

A

Absorption limited to duodenum (small portion)
Antacids impair absorption
Minimal protein binding & excreted w/out significant metabolism

18
Q

Gabapentin Dose

A

Pre-op 1,200mg 1-2hr prior to surgery

600mg Q8H x14 days

19
Q

Gabapentin SE

A 
Sedation
Dizziness
Headache
Visual disturbances
Respiratory depression
Long lasting effects
20
Q

Lidocaine

A 
Amide local anesthetic
Weak base
pKa 7.9
MOA uncertain - VG Na+ channel?
Block polymorphonucelar granulocytes priming
21
Q

Lidocaine PK

A

Blocks nerve transmission
First-pass extraction in the lungs
Metabolized in liver - prolonged in patients under general anesthesia

22
Q

Lidocaine Dose

A

Induction 1.5mg/kg bolus

Infusion 1-2mg/kg/hr

23
Q

Lidocaine Benefits & Concerns

A

Benefits - reduces pain, speeds up bowl function return (laparoscopic cases), improves functional outcomes in prostatectomy thoracic & major spine cases
Concerns - accumulation however given at doses per ERAS protocols serum levels are well below toxicity
Infusion at higher toxicity risk
Monitoring at risk patients is advised

24
Q

Magnesium Sulfate

A

Analgesic properties r/t regulation Ca2+ influx into cells & NMDA receptors in CNS antagonism
↓ opioid consumption & pain
SE: Bradycardia & hypotension
Multi-modal drug NOT sole analgesic

25
Q

Magnesium Sulfate Dose

A

Bolus 30-50mg/kg

Infusion 10mg/kg/hr

26
Q

Capsaicin

A

TRPV1 (transient receptor potential vanilloid) channel agonist
Activation releases high-intensity impulses & substance P
Primary pungent ingredient of chili peppers & botanicals
Topical application for neuralgia & neuropathies
Available OTC in 0.025% 0.075% 0.25% creams & transdermal patches

27
Q

Ketamine

A

NMDA antagonist modulates central sensitization (induced by incision & tissue damage)
Role in preventing opioid-induced hyperalgesia
SE: Psychomimetic, dizziness, blurred vision, N/A

28
Q

Ketamine Dose

A

0.5-1mg/kg prior to surgical incision

29
Q

Dexmedetomidine (Precedex)

A

Acts on locus coeruleus (alertness) located in brain
Selective α2 agonist - blunts sympathetic response
SE: Bradycardia & hypotension

30
Q

Dexmedetomidine Dose

A

0.5-2mcg/kg

Bolus 4mcg up to 16mcg

31
Q

Peripheral Opioids

A

Analgesic effects mediated by peripheral opioid receptors
↓ plasma extravasation, vasodilation, pro-inflammatory neuropeptides, immune mediators, & tissue destruction
Role in arthroplasty & inflammatory bowel disease

32
Q

NSAID Anaphylaxis Risk Factors

A

Allergic rhinitis
Nasal polyps
Asthma
True hypersensitivity rarely occurs

N926 Pharmacology (17 decks)

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