Pain Drugs Flashcards
Pain Management Algorithm
- Non-pharmacologic therapy like exercising, PT, sleep hygiene, etc
- Nociceptive pain –> First line = NSAIDs (if active inflam)
or, Neuropathic pain and/or antiepileptic drugs –>
First line = antidepressants (tricyclics, SNRIs) or antiepiletics drugs (gabapentinoids - gabapentin or pregabalin, sodium channel agents - lidocaine, carbamazepine, oxcarbazepine)
- Second and third line = Acetaminophen, Topical agents (NSAIDs, lidocaine, capsaicin), Opioids, neuromodulation
What drug is this toxicity associated
Ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics);
concomitant use associated is with an increased risk of vasospasm leading to cerebral ischemia and/or ischemia of the extremities.
dihydroergotamine
What are ubrogepant and rimegepant?
Nothing bolded for these.
Calcitonin gene-related peptide receptor antagonist for tx of migraine.
Name of 2 drugs that are also antidepressants
- amitriptyline, other TCA
2. duloxetine, other SNRI
Name of 2 drugs that are NMDA antagonists
- ketamine
2. methadone
Name of 2 drugs that are adrenergic agonists
- dexmedetomidine
2. clonidine
What are some topical anti-pain agents?
- Capsaicin: stimulates TRPV1 receptors, desensitizes substance P, mod to poor efficacy for nociceptive and neuropathic pain.
- Camphor: Also desensitizes TRPV1 receptors
- Menthol: stimulates TRPM8 “cold” receptors to cause cool sensation
- Topical NSAIDs
- Topical Na+ channel blocker
Name of the 2 drugs that are AEDs used in neuropathic pain
- pregabalin
2. gabapentin
Name of the 3 drugs that are topical analgesics
- capsaicin, camphor
- menthol
- lidocaine
Name of the 3 drugs that are anti-migraine agents
- sumatriptan
- dihydroergotamine
- (lasmiditan, ubrogepant)
Definition of analgesic
drugs that relieve pain without causing LOC
What drug is an alpha2-adrenergic agonist
used for 1) hypertension and 2) relief of severe epidural pain
administered by continuous infusion through an epidural catheter
highly lipid soluble, escapes to blood to causes hypotension, confusion, dry mouth
Clonidine
What drug is a noncompetitive NMDA receptor antagonist that blocks glutamate.
Sub-anesthetic doses for analgesia, acute and chronic pain. Modulates central sensitization, hyperalgesia and opioid tolerance. Treats complex regional pain syndrome, neuropathic pain.
Causes cataleptic-like state with dissociation from surrounding environment.
ketamine
How is ketamine administered?
IV infusion
Algorithm for neuropathic pain
First line: Ca alpha 2 delta ligands (pregabalin, gabapentin) or SNRIs (duloxetine, venlafaxine) or TCAs (amitriptyline, nortriptyline)
Second line: Other anti-epileptics (valproic acid), opioids, or tramadol
Third line : NMDA antagonists (dextromethorpan), combo of analgesics, or Tizanidine Baclofen
Fourth line: Botulinum toxin injection or consider intrathecal ziconotide
What drug causes
(MOA) Decreased stimulation of the trigeminal system
& is used tx migraine pain without causing vasoconstriction
lasmiditan
What drug has these BLACK BOX WARNINGS
Risk of medication
errors/ingestion by children leads to
overdose and death (respiratory depression)
addiction, abuse, and misuse
interactions with drugs affecting cytochrome P450 isoenzymes
withdrawal syndrome
Increased risk of respiratory depression from concomitant use with benzodiazepines or other CNS depressants
Tramadol
What drug is used for
- Fibromyalgia
- Neuropathic pain associated with diabetic peripheral neuropathy
- Postherpetic neuralgia
- Seizures
Pregabalin
What types of drugs would you use for severe pain
non-opioid analgesics + opioids + adjuncts
adjuncts- called co-analgesics, include TCAs, SNRIs, anticonvulsants, topical anesthetics
What is gabapentin?
Gaba analog like pregabalin, less reliable pharmacokinetics and more sedating
What is the first-line therapy in nociceptive pain
NSAIDs, if an active inflammatory process is present
What is the black box warning for duloxetine?
Increased risk of suicidal thoughts and behaviors.
What is the first-line therapy in neuropathic pain
antidepressants and antiepileptic drugs
What do you give if neuropathic pain is persistent even after first-line therapy
Acetaminophen, Topical agents, Opioids (only when other modes have been used)
Which COX enzyme is induced and which COX enzyme is constituent
COX-1: constiuent
COX-2: induced
What are the other selective 5-HT1B and 5-HT1D agonists, other than Sumatriptan?
multiple others: almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, zolmitriptan… differences are primarily in pharmacokinetics and dosage forms
What drug?
MOA: N-type voltage sensitive calcium channels located on the nociceptive afferent nerves of the dorsal horn
Intrathecal route, its a peptide
ziconotide
What drug has this clinical application?
Management for severe chronic pain
(in patients requiring intrathecal therapy and who are intolerant or refractory to other therapies, eg:
• systemic analgesics
• adjunctive therapies
• intrathecal morphine)
ziconotide
What drug has this BBW?
severe psychiatric symptoms and neurological impairment may occur
this medication is among those listed for heightened risk of causing significant patient harm when used in error
ziconotide
What is an alpha-2-adrenergic agonist used analgesia and sedation? It is a potent anxiolytic, part of multimodal approach to postoperative pain management
Dexmedetomidine
NOCICEPTIVE PAIN ALGORITHM
mild-mod pain:
topical agents –> acetaminophen/paracetamol (APAP)–> NSAIDs + PPI, or COX-2 inhibitors +/- APAP
mod- to severe pain:
if NSAID risk then use APAP
if no NSAID risk then use NSAIDs + PPI, or COX-2 inhibitors +/- APAP
IF the pain does not go…. then use TCAs (antidepressants, which are amitriptyline or duloxetine)
IF pain is still there, use opioids and add Baclofen or Tizanidine if spasms present
Which COX enzyme plays a physiological role in the kidney
COX-2
Which COX enzyme produces the most erythema, edema, and pain
COX-2
What are the 3 main effects of aspirin
decreases prostaglandin and TXA2 ,
inhibits platelet aggregation,
has antipyretic, analgesic, and anti-inflammatory properties
How many types of aspirin tablets are there?
2
immediate release and extended release capsule
What drug has the following toxicities:
- ulcer
- inc. risk for bleeding
- multiple drug interactions
- inc. risk of Reye syndrome in kids under 18
- increase in serum Cr
aspirin
Aspirin/Salicylate toxicity progresses to..
metabolic acidosis that becomes life-threatening
What are the main functions of nonaspirin NSAIDs
suppress inflammation, pain, and fever like aspirin
What drug has the risks of gastric ulcer, renal impairment, and bleeding like aspirin
nonaspirin NSAIDs
what are the 2 main differences in nonaspirin NSAIDs and aspirin
Nonaspirin NSAIDs:
- are reversible, so effects decline as blood levels decline
- have inc. risk of MI and stroke
therefore use lowest effective dosage for shortest possible time
what are the nonaspirin NSAIDs
ibuprofen, naproxen, coxibs
which drug has this black box warning:
may cause fetal renal dysfunction leading to oligohydramnios, > 30 weeks closure of ductus arterious
inc. risk of MI and stroke, contraindicate in CABG
inc. risk of GI bleeding
ibuprofen
which drug is similar to ibuprofen except that its half life is longer than ibuprofen
naproxen
Which drug selectively blocks COX-2
celecoxib (Celebrex)
which drug DOES NOT inhibit platelet aggregation, so does not have risk of bleeding
celecoxib
what is the off-label use of celecoxib
gout
which drug has the following black box warning:
may cause fetal renal dysfunction leading to oligohydramnios, > 30 weeks closure of ductus arterious
inc. risk of MI and stroke, contraindicate in CABG
serious GI risk, but less with COX-2 selective
celecoxib
which drug is used when NSAID therapy is required but pts are at risk of CV complications
naproxen
names of some commonly used NSAIDs
aspirin, celecoxib, diclofenac, ibuprofen, indomethacin, ketorolac, naproxen
Which drug has the following black box warning:
risk of medication errors and overusage can lead to hepatotoxicity with acute liver failure and death possible
acetaminophen
which drug suppressed pain and fever BUT NOT inflammation
acetaminophen
which drug produces a toxic metabolite when glutathione is depleted
use N-acetylcysteine as an antidote
acetaminophen
What are the toxicities of pregabalin?
Depression, suicidal ideation
Gaba analog like pregabalin, less reliable pharmacokinetics and more sedating
gabapentin
which drug does not cause GI ulcers, does not suppress platelet aggregation, and does not impair renal function
acetaminophen
which drug inhibits metabolism, therefore pt will have inc. risk of bleeding
acetaminophen
What drug is used…?
For fibromyalgia, chronic musculoskeletal pain, neuropathic pain, and chemotherapy induced peripheral neuropathy.
Most benefit when SSRI do not work, for pt with concurrent depression.
duloxetine
MOA of morphine (opioid)
binds to opioid receptors in the CNS
which drug has the following black box warning:
respiratory depression in combination with other drugs, routes of administration
morphine (opioid)
how does morphine (opioids) work
they inhibit the ascending pain pathways and
alter the perception of and response to pain and
cause general CNS depression
What tricyclic antidepressant is used off-label to relieve chronic fatigue syndrome related sleep disturbances and pain among other things?
Amitriptyline
What drug are these black box warning and 1 additional side effect of?
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults.
Anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention)
amitriptyline
