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Pharmacology > Final: Analgesias/Sedatives > Flashcards

Final: Analgesias/Sedatives Flashcards

1
Q

Opioid receptors

A

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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2
Q

tolerance

A

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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3
Q

cross tolerance

A

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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4
Q

physical dependence

A

downregulation of receptors

abstinence syndrome - sudden stop of drug physical symptoms

avoid w/ weaning off

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5
Q

withdrawal symptoms

A

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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6
Q

Opioid agonists

A

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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7
Q

Opioid ADRs

A

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

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8
Q

morphine

A

strong opioid

think about MI (MONA-B tx)

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9
Q

fentanyl

A

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

100x stronger than morphine

synthetic

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10
Q

meperidine

A

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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11
Q

methadone

A

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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12
Q

hydromorphone

A

strong opioid agonist (dilaudid)

slightly less N/V than morphine

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13
Q

codeine

A

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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14
Q

oxycodone

A

moderate-strong opioid (PO)

used for severe pain (7/10)

Percocet - oxy and acetaminophen

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15
Q

hydrocodone

A

moderate-strong

analgesic and antitussive

Vicodin - hydrocodone and acetaminophen

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16
Q

Agonist-Antagonist Opioid

A

antagonize mu, agonize kappa

ceiling??

17
Q

Buprenorphine

A

moderate-strong (suboxone)

ag-antag = less analgesia and lower potential for abuse

can still have respiratory depression, but a higher dose (higher ceiling)

18
Q

Pentazocine

A

moderate-strong (Talwin)

ag-antag = less analgesia and lower potential for abuse

19
Q

Naloxone

A

opioid induced sedation/respiratory depression

antagonizes mu & kappa

short-acting: temporary fix to keep breathing until can put on a drip

20
Q

methylnatrexone

A

specifically antagonizes mu receptors in the gut –> no CNS blocking

opioid induced constipation

21
Q

NSAIDS

A

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

22
Q

COX 1 v. COX 2

A

COX 1 - kidney, GI, clotting
(protect against MI/CVA –> “slippery platelets”)

COX 2 - inflammation, vasodilate, fever

23
Q

Aspirin

A

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)

24
Q

Ibuprofen

A

1st gen, less platelet inhibition and GI bleed than aspirin

adjunct to opioids, well tolerated (less ADRs than aspirin)

25
Q

Naproxen

A

??

26
Q

Ketorolac

A

IV NSAID –> acute pain

equally effective to opioids, not much anti-inflammatory

same NSAID ADRs

27
Q

Celecoxib

A

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

28
Q

Acetaminophen

A

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)

29
Q

Tramadol

A

Non-opioid centrally acting analgesic

analog of codeine, weak agonist at mu receptor

rare CNS ADRS

30
Q

Clonidine

A

Non-opioid centrally acting analgesic

alpha 2 adrenergic agonist, IV for cancer pain

ADRs: hypotension, bradycardia, rebound HTN, dry mouth, dizzy, sedation

31
Q

Dexmedetomidine

A

Non-opioid centrally acting analgesic

alpha 2 adrenergic agonist

used to facilitate sedation & analgesia in procedure areas (IV)

32
Q

benzodiazepines

A

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

33
Q

benzo examples

A

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

34
Q

lorazepam/diazepam

A

indic: anxiolytic, anti-seizure (status), induction of anesthesia (sometimes)

teach: take only as prescribed, avoid ETOH & opioids

35
Q

flumazenil

A

benzo induced hypotension/resp depression

reversal agent for benzos

36
Q

zolpidem

A

ambien –> sleep aid, NOT anxiolytic

ER - for both falling asleep and staying asleep

can intensify the effects of other CNS depressants

37
Q

ramelteon

A

activates melatonin receptors

well-tolerated and helps w/falling asleep

38
Q

benzos vs. barbs

A

benzo = lower abuse potential, less tolerance, lower dependence, reversal agent is available

MOA
benzo - potentiate GABA
barbs - stimulate GABA receptor directly

39
Q

barbiturates

A

phenobarbital - sometimes still used for seizures

don’t give these that much anymore

highly addictive, huge ADRs w/ no reversal

Pharmacology (12 decks)

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