Final: Analgesias/Sedatives Flashcards by Colleen Godfrey

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

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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

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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)

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physical dependence

downregulation of receptors

abstinence syndrome - sudden stop of drug physical symptoms

avoid w/ weaning off

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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”)

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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)

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Opioid ADRs

respiratory depression, hypotension, sedation, dizzy, ^ ICP, urinary retention, euphoria, GI upset, constipation, cough suppression, N/V, miosis

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morphine

strong opioid

think about MI (MONA-B tx)

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fentanyl

strong opioid agonist (duragesic) –> severe pain or need for fast action

100x stronger than morphine

synthetic

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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

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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

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hydromorphone

strong opioid agonist (dilaudid)

slightly less N/V than morphine

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codeine

moderate to strong opioid

similar to morphine, but less analgesia and resp depression

analgesic and antitussive

most likely to cause constipation

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oxycodone

moderate-strong opioid (PO)

used for severe pain (7/10)

Percocet - oxy and acetaminophen

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hydrocodone

moderate-strong

analgesic and antitussive

Vicodin - hydrocodone and acetaminophen

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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