Pain Meds Flashcards by Kara Albright

Which group of pain meds inhibit COX?

NSAIDs

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What inflammatory mediator causes inflammation–>pain?

prostaglandins

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What does COX 1 and 2 do?

use arachidonic acid to produce prostaglandins during inflammation

physiologic role in renal function

COX 1 in all tissues, COX2 induced

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What drug irreversibly binds COX 1 and 2 to decrease prostaglandin and thromboxane A2?

aspirin

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What to use aspirin for?

pain
fever
inflammation
stroke
MI prevention (via - Cox1 in platelets)

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Side effects of aspirin

ulcer

bleeding risk

multiple drug interactions

Reye syndrome in kids with flu or chicken pox

increased serum creatinine d/t loss of prostaglandin effects in kidneys

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What drug reversibly binds COX 1 and 2 to decrease prostaglandin synthesis?

ibuprofen

pain, fever, inflammation

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What is the difference between naproxen and ibuprofen?

same MOA

naproxen has longer half-life (2 vs 12 hours)

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Side effects of ibuprofen

fetal renal dysfunction–> oligohydraminos after 20 weeks

closure of ductus arteriosus after 30 weeks

increased risk MI and stroke
–> DONT USE IN CABG

increased risk of GI bleeding

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What drug inhibits prostaglandin synthesis via COX2?

celecoxib

pain, arthritis, dysmenorrhea

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Side effects of celecoxib

fetal renal dysfunction–> oligohydraminos after 20 weeks

closure of ductus arteriosus after 30 weeks

increased risk MI and stroke
–> DONT USE IN CABG

increased risk of GI bleeding (less with COX2 vs 1 and 2)

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Why do you take aspirin 2 hours before other NSAIDS?

non-aspirin NSAIDS interfere with antiplatelet effects–> decrease protection against MI and stroke

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Why d/c high dose aspirin 1 week before surgery/pregnancy?

increase risk of bleeding with warfarin, heparin, other anticoagulants

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MOA of non-aspirin NSAIDS

inhibit COX1 and 2

pain, fever, inflammation

increased risk gastric ulcer, renal impairment, bleeding

different from aspirin:

reversible effects
increases risk of MI/CVA

use lowest effective dose for shortest possible time

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Coxibs vs aspirin or non-aspirin NSAIDs

less gastric ulceration

selectively blocks COX2

doesn’t inhibit platelet aggregation–> no risk for bleeding

increased risk MI and stroke

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Commonly used NSAIDs

aspirin
celecoxib (celebrex)
diclofenac
ibuprofen (motrin)
indomethacin
ketorolac (toradol)
naproxen (aleve, naprosyn)

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What NSAID is recommended is a patient has cardiovascular risk?

naproxen

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Contraindications for NSAIDs

CKD
gastric or duodenal ulcer
heart failure
uncontrolled HTN
allergy
ongoing anticoagulant tmt

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When to use acetaminophen

pain and fever

DOES NOT treat inflammation

Side effects of acetaminophen

med error/overdosing–> hepatotoxicity (depletes glutathione)

no GI, bleeding or renal risk

Suspected MOA of acetaminophen

activate descending serotonergic inhibitor pathways in CNS

tmt for acetaminophen toxicity

acetylcysteine

substitutes depleted glutathione

Increased risk of bleeding with acetaminophen and ____

warfarin

inhibits its metabolism

First line agents for neuropathic pain

calcium channel ligands

serotonin-norepi reuptake inhibitor (SNRI)

tricyclic antidepressant

amitriptyline

tricyclic antidepressant (inhibits NE and 5-HT reuptake) treat neuropathic pain

Side effects of amitriptyline

SI in kids and ya anticholinergic effects increased bleeding risk

duloxetine

inhibitor of 5-HT and NE reuptake weak dopamine reuptake inhibitor treat neuropathic pain with concurrent depression

Side effects of duloxetine

SI (main) N, dizziness, sweating, sexual dysfunction, insomnia/agitation, increased BP

pregabalin (Lyrica)

binds a2s subunit of CNS calcium channels (NOT GABA) to decrease excitatory AP neuropathic pain a/w DM neuropathy, postherpatic neuralgia, fibromyalgia, partial seizures gabapentin similar

Second line tmt for neuropathic pain

antiepileptic opioid tramadol

Second line for nociceptive pain

weak opioid, nonopioid and adjuvant (TCA, SNRI, anticonvulsant)

Third line for nociceptive pain

strong opioid, nonopioid and adjuvant (TCA, SNRI, anticonvulsant)

Third line for nociceptive pain

strong opioid, nonopioid and adjuvant (TCA, SNRI, anticonvulsant)

tramadol

partial u-opiate receptor agonist block NE and 5-HT reuptake severe pain, premature ejaculation, RLS

Side effects of tramadol

overdose/death via respiratory depression with med error addiction, abuse interact with CYP450 drugs increase respiratory depression with use with benzo, other CNS depressants

What to use for patients not effectively treated with opioids or non-opioids in neuropathic pain?

tapentadol mod-strong opioid agonist, blocks NE reuptake

Third/Fourth line tmt for neuropathic pain

3: NMDA antagonist, analgesic combo, baclofen/tizanidine 4: botox, intrathecal ziconotide

ketamine

noncompetitive NMDA receptor antagonist dissociation/anesthesia, analgesia

dexmedetomidine

selective alpha 2 agonist in brainstem -- inhibit NE release sedation, pain

clonidine

alpha 2 agonist for HTN and severe pain

ziconotide

N voltage calcium channel on dorsal horn afferent nerves--> block excitation to reduce sensitivity to pain

Side effects of ziconotide

severe psych sx, neuro impairment increased risk for patient harm when used in error

When to use ziconotide

only for chronic severe pain given intrathecal when refractory to other treatments

lasmiditan

5-HT receptor agonist decrease stimulation of trigeminal system, treat migraine

ubrogepant

calcitonin antagonist treat migraine with or without aura

dihydroergotamine

ergot alkaloid migraine cluster headaches orthostatic hypotension pelvic congestion with pain

Side effects of dihydroergotamine

contraindicated with potent inhibitors of CYP3A4 cerebral ischemia ischemia of extremities