Pharm approach to pain Flashcards by Christian Wakim

what are analgesics?

drugs that relieve pain without causing loss of consciousness

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what is secondary hyperalgesia?

pain caused by glutamate stimulation of spinal NMDA receptors

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what are the characteristics of COX1?

expressed in all tissue
responds to physiological stimuli
responds to pathological stimuli (inflammation)

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what is the COX1 pain pathway?

inflammation stimulates AA release
COX1 converts AA to PGE2
PGE2 causes symptoms

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what are the characteristics of COX2?

expressed in some tissue
physiological role in kidney and complements COX1
response to pathological stimuli (inflammation)

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what is the COX2 pain pathway?

inflammation induces COX2 expression
COX2 also converts AA into PGE2
COX2 derived PGE2 amplifies symptoms

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what are the NSAIDs?

ASA
ibuprofen
celecoxib
diclofenac
inomethacin
ketorolac (Toradol)
naproxin (Aleve)

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what is the MOA of most NSAIDs?

inhibits COX1 and COX2

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which NSAID only inhibits COX2?

celecoxib

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what are the adverse reactions of ASA?

GI bleeding
hemostatic defects
toxicity leading to respiratory failure

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what is the toxic dose of ASA?

400-500 mcg/mL

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what is the dose of ASA for antiplatelet or analgesia use?

100 mcg/mL

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what is the dose of ASA for anti-inflammatory use?

150-300 mcg/mL

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what is the dose of ASA for the treatment of rheumatic fever?

250-400 mcg/mL

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what is the progression of ASA toxicity?

salicylates uncouple ox phos in CNS
resp center sees decreased ATP as hypoxemia
hyperventilation causes respiratory alkalosis
organic acids accumulate from Krebs cycle dysfunction
metabolic acidosis becomes life-threatening

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what are the adverse reactions of ibuprofen?

fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed

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what are the adverse reactions of celecoxib?

fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed

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what are the 4 major actions of ASA?

anti-inflammatory
mild to moderate pain relief
fever reduction
prevention of MI or stroke (anti-platelet)

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what are the differences between ASA and other NSAIDs?

other NSAIDs:
reversible
increase the risk of MI and stroke

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how is celecoxib different from ASA and other NSAIDs?

less likely to cause gastric ulceration
no risk of bleeding
increases MI and stroke risk

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what are the contraindications of using NSAIDs?

CKD
gastric/duodenal ulcer
heart failure
uncontrolled HTN
allergy
anticoagulant use

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what are the possible MOAs of acetaminophen?

TRPV1 activator
central PG synthase inhibitor
cannabinoid receptor activator

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what is the major adverse reaction of acetaminophen?

hepatotoxicity due to overdose

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what are the effects of acetaminophen?

suppresses pain and fever

NOT anti-inflammatory

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how do you treat acetaminophen toxicity?

acetylcysteine

who should not take acetaminophen?

people with liver disease | people who take warfarin (increased risk of bleeding)

what is the MOA of opioids?

act on central and peripheral µ, ∂ and k receptors

what is the blackbox warning of morphine?

respiratory depression with/without combining with other drugs

what are the adverse reactions of opioids?

constipation CNS depression hypotension

when are patients at risk for physical opioid dependence?

when used at high doses for > 20 days

what are indications for opioid use?

``` post-op pain obstetric analgesia MI head injury chronic non-cancer pain ```

what are the first-line agents for neuropathic pain?

calcium channel alpha 2 delta ligands SNRIs TCA

what is the MOA of amitriptyline?

TCA | inhibition of NE and 5-HT reuptake

what are the adverse reactions of amitriptyline?

``` dry mouth constipation tachycardia nausea vomiting sedation mental clouding ```

what is the MOA of duloxetine?

SNRI inhibitor of neuronal 5-HT and NE reuptake weak inhibitor of DA reuptake

what are the adverse reactions of SNRIs?

``` nausea dizziness diaphoresis sexual dysfunction insomnia/agitation hypertension ```

what is the MOA of calcium channel alpha2-delta ligands?

modulates calcium influx at nerve terminals | GABA analog but does NOT bind to GABA receptors

what are the indications for using pregabalin?

diabetic neuropathy postherpetic neuralgia partial seizures fibromyalgia

what are the calcium channel alpha2-delta ligands?

pregabalin | gabapentin

what are the indications for using gabapentin?

``` broad-spectrum anti-seizure activity post-herpetic neuralgia diabetic neuropathy migraine prophylaxis fibromyalgia restless leg syndrome ```

what is the MOA of tramadol?

partial agonist of µ-opioid receptors in CNS | inhibits reuptake of 5-HT and NE

what are the adverse reactions of tramadol?

``` sedation dizziness headache dry mouth constipation ```

what are the indications for using tramadol?

moderate pain * stronger than ASA or acetaminophen * weaker than morphine

what are the serious side effects of tramadol?

seizures in epileptics hypertensive crisis if combine with MAO serotonin syndrome if combined with SSRI, TCA, MAO

what is the MOA of tapentadol?

moderate to strong µ-opioid receptor agonist | blocks reuptake of NE

what is an indication for giving tapentadol?

patients who are not effectively treated with other non-opioids and opioids

what is the MOA of ketamine?

noncompetitive NMDA receptor antagonist

what are the indications for using ketamine?

``` agitation sub-anesthetic doses for analgesia depressive episode procedural sedation refractory status epilepticus ```

what are adverse reactions of ketamine?

psych reactions: agitation confusion hallucinations

what is the MOA of dexmedetomidine?

alpha2-adrenergic agonist for analgesia and sedation

what are the indications for using dexmedetomidine?

short-term sedation in intubated patients sedation prior to procedures administered IV for pain

what are the adverse reactions of dexmedetomidine?

``` hypotension bradycardia nausea dry mouth transient HTN agitation constipation respiratory depression ```

what is the MOA of clonidine?

alpha2-adrenergic agonist used for HTN and relief of severe pain blocks transmission of pain signals

what are the indications for using clonidine?

severe cancer pain in patients not treated effectively with opioid alone

what are the adverse reactions of clonidine?

hypotension confusion dry mouth

what is the MOA of ziconotide?

selective N-type voltage-sensitive calcium channel antagonist on nociceptive afferent neurons prevents transmission of pain signals

what are the indications for using ziconotide?

chronic severe pain in those whom intrathecal administration is warranted and when refractory to other treatments

what are the adverse reactions of ziconotide?

cognitive impairment and psych symptoms

what drugs are contraindicated in pregnancy?

dexmedetomidine clonidine ziconotide

what are the topical anti-pain agents?

``` capsaicin camphor menthol topical NSAIDs topical Na channel blockers ```

what drugs can treat migraines?

sumatriptan lasmiditan ubrogepant dihydroergotamine

what is the MOA of sumatriptan?

selective 5HT1B and 5-HT1D agonist activates receptors on the intracranial blood vessels and sensory nerves of the trigeminal system

what are the adverse reactions to sumatriptan?

``` Torsades MI stroke CNS depression blindness or partial vision loss serotonin syndrome peripheral ischemia ```

what is the MOA of lasmiditan?

high-affinity highly selective 5-HT1F receptor agonist

what are the adverse reactions to lasmiditan?

CNS depression serotonin syndrome can potential toxic effects of other drugs

what is the MOA of ubrogepant?

calcitonin gene-related peptide receptor antagonist

what are the adverse reactions to ubrogepant?

nausea somnolence dry mouth

what is the MOA of dihydroergotamine?

ergot alkaloid binds to serotonin, adrenergic and dopamine receptors

what are the adverse reactions to dihydroergotamine?

do not use with potent CYP3A4 inhibitors --> vasospasm | cardiac fibrosis