Final: Analgesias/Sedatives Flashcards
Opioid receptors
receptors –> mu, kappa, delta
mainly bind with the mu receptors, weakly to kappa and do not interact with delta
mu –> analgesia, sedation, euphoria, physical dependence, decreased GI motility (constipation), respiratory depression
tolerance
a larger dose is required to produce the same response –> larger dose to maintain any analgesic/euphoria effects
cellular adaptations from prolonged opioid exposure
leads to overdoses
can develop tolerance to analgesic, euphoric, and respiratory effects (opioid naive will have bigger respiratory effects than an everyday user); no tolerance to constipation and miosis (will always have these)
can develop quickly, as soon as a week
cross tolerance
equivalent dosing (may be different dosing but equiv) leads to the same tolerance
swapping from oxycodone and hydrocodone example (20/30)
same effects
switiching someone with tolerance –> would need a higher amount of the new drug as well (need an equivalent dose)
physical dependence
downregulation of receptors
abstinence syndrome - sudden stop of drug physical symptoms
avoid w/ weaning off
withdrawal symptoms
flu-like symptoms, agitation, seizures, pain, psychosis, yawning(?), goosebumps (“cold turkey”), anorexia, tremor, itching, N/V/D, bone and muscle pain, spasms and kicking motion (“kicking the habit”)
Opioid agonists
most effective analgesics for acute pain, less evidence for chronic (opioid crisis)
mimic the actions of endogenous opioid peptides
anyone on an opioid should also be on bowel regimen
VS - keep eye on BP and RR
BP - opioids cause histamine release which leads to vasodilate and can lower BP enough to bottom someone out
avoid anticholinergics
be careful giving opioids w/ tylenol in them to patients where you wouldn’t want to mask a fever (cellulitis example)
extremes of age are more susceptible to resp depression (elderly and kids)
Opioid ADRs
respiratory depression, hypotension, sedation, dizzy, ^ ICP, urinary retention, euphoria, GI upset, constipation, cough suppression, N/V, miosis
morphine
strong opioid
think about MI (MONA-B tx)
fentanyl
strong opioid agonist (duragesic) –> severe pain or need for fast action
100x stronger than morphine
synthetic
meperidine
strong opioid agonist (demerol)
short action requiring lots of doses
only used really for rigors after surgery
ton of ADRs - toxic metabolites –> toxicity, drug interactions
methadone
PO opioid (strong agonist)
indications: chronic pain (>6months) and tx of heroin addiction
very long half-life and prolonged QT QT –> Vfib
used for DOT for opioid use disorder and pain
hydromorphone
strong opioid agonist (dilaudid)
slightly less N/V than morphine
codeine
moderate to strong opioid
similar to morphine, but less analgesia and resp depression
analgesic and antitussive
most likely to cause constipation
oxycodone
moderate-strong opioid (PO)
used for severe pain (7/10)
Percocet - oxy and acetaminophen
hydrocodone
moderate-strong
analgesic and antitussive
Vicodin - hydrocodone and acetaminophen
Agonist-Antagonist Opioid
antagonize mu, agonize kappa
ceiling??
Buprenorphine
moderate-strong (suboxone)
ag-antag = less analgesia and lower potential for abuse
can still have respiratory depression, but a higher dose (higher ceiling)
Pentazocine
moderate-strong (Talwin)
ag-antag = less analgesia and lower potential for abuse
Naloxone
opioid induced sedation/respiratory depression
antagonizes mu & kappa
short-acting: temporary fix to keep breathing until can put on a drip
methylnatrexone
specifically antagonizes mu receptors in the gut –> no CNS blocking
opioid induced constipation
NSAIDS
1st (COX 1 & 2) vs 2nd (COX 2) gen
contras: bleeding, kidney injury, gastric ulcer
short instances (a few days)
COX 1 = can lead to fluid retention from kidney block
COX 1 v. COX 2
COX 1 - kidney, GI, clotting
(protect against MI/CVA –> “slippery platelets”)
COX 2 - inflammation, vasodilate, fever
Aspirin
1st gen NSAID
life of platelet 7 days, stop a week before surgery
contra: children
ADRs: GI distress, bleeding, renal impairment –> edema, Reye’s syndrome - encephalopathy in kids, hypersensitivity, erectile dysfunction
some evidence for prevention of colon cancer
toxicity –> tinnitus, HA, dizzy, drowsy, confused, hyperventilate (progresses to depression)
Ibuprofen
1st gen, less platelet inhibition and GI bleed than aspirin
adjunct to opioids, well tolerated (less ADRs than aspirin)
Naproxen
??
Ketorolac
IV NSAID –> acute pain
equally effective to opioids, not much anti-inflammatory
same NSAID ADRs
Celecoxib
COX 2 inhibitor
2nd gen NSAID –> doesn’t impact COX 1 = stomach lining, renal function, or platelets
ADR: inc risk of MI/CVA, can cause renal impairment indirectly from vasoconstriction
more expensive
Acetaminophen
selective for the CNS and has minimal effects at peripheral sites (less GI upset ex.)
4 g Qday max (2g max for ETOH) –> overdose can cause fatal liver damage
contra: ETOH abuse
antidote for OD: acetylcysteine PO or IV (PO = awful smell/taste)
Tramadol
Non-opioid centrally acting analgesic
analog of codeine, weak agonist at mu receptor
rare CNS ADRS
Clonidine
Non-opioid centrally acting analgesic
alpha 2 adrenergic agonist, IV for cancer pain
ADRs: hypotension, bradycardia, rebound HTN, dry mouth, dizzy, sedation
Dexmedetomidine
Non-opioid centrally acting analgesic
alpha 2 adrenergic agonist
used to facilitate sedation & analgesia in procedure areas (IV)
benzodiazepines
trigger/potentiates GABA neurotransmitter
limit to CNS depression –> safer than others; IV dosing strict monitoring - cardiac (brady & hypo)
anxiolytic agents (low dose) and hypnotics (higher dose, facilitate sleep)
ADRs: residual hangover drowsy, vivid dreams/nightmares, dependence (phys and psych), tolerance, respiratory depression, teratogenic
caution w/ elderly, withdrawal will kill
benzo examples
Lorazepam (Ativan) – Sedative, Status Epilepticus,
• Diazepam (Valium) – Sedative, Seizures, Muscle Spasms, ETOH Withdrawal..
• Midazolam (Versed) – Anesthesia Induction, procedural, ICU, conscious
sedation
• Alprazolam (Xanax) – Sedative, Anxiety, Panic Disorder
• Temazepam (Restoril)– Insomnia/hypnotic
lorazepam/diazepam
indic: anxiolytic, anti-seizure (status), induction of anesthesia (sometimes)
teach: take only as prescribed, avoid ETOH & opioids
flumazenil
benzo induced hypotension/resp depression
reversal agent for benzos
zolpidem
ambien –> sleep aid, NOT anxiolytic
ER - for both falling asleep and staying asleep
can intensify the effects of other CNS depressants
ramelteon
activates melatonin receptors
well-tolerated and helps w/falling asleep
benzos vs. barbs
benzo = lower abuse potential, less tolerance, lower dependence, reversal agent is available
MOA
benzo - potentiate GABA
barbs - stimulate GABA receptor directly
barbiturates
phenobarbital - sometimes still used for seizures
don’t give these that much anymore
highly addictive, huge ADRs w/ no reversal
