Pharm Flashcards
Compare barbiturates vs bezodiazepines
Barbiturates:
- deadly via decreased heart and respirations
- no antidote
- highly addictive
Benzos:
- plateau so not as deadly, though can become deadly with opioids and alcohol
- antidote
- addictive but less so than barbiturates
Xanax
alprazolam
benzo
Ambien
zolpidem
non-benzo
Low-potency benzos with long half-life
diazepam
Valium
diazepam
Low-potency benzos with short half-life
temazepam
High-potency benzos with long half-life
clonazepam
High-potency benzos with short half-life
alprazolam
lorazepam
traizolam
Ativan
lorazepam
What drug accentuates GABA activity by increasing the FREQUENCY of Cl- channel opening in response to GABA?
benzos
local hyperpol–> cell doesn’t fire
Uses for benzos
anxiety
sedative
anticonvulsant
amnesia/anesthesia
–> some anterograde amnesia
skeletal muscle relaxant
alcohol withdrawal
Rohypnol
date-rape drug
benzo
anterograde amnesia
Most common benzo side effect
drowsiness
Who is susceptible/resistant to benzos
susceptible: elderly
resistant: alcoholics, barbiturate abusers
Abrupt d/c of long-term benzo use leads to
rebound insomnia
What benzos also used for insomnia?
triazolam
temazepam
What drug a/w respiratory depression and arrest when used for sedation in non-critical care settings?
IV midazolam (versed)
benzo
What benzo used for preop sedation, general anesthesia, anxiety and amnesia?
midazolam (versed)
What drug is used only for insomnia that is safe in pregnancy?
zolpidem (Ambien)
What drug binds BZ1 receptors of GABAa and is mainly for sleep maintenance?
zolpidem (ambien)
What drug can cause complex sleep behaviors (sex while asleep, sleep-driving, sleep-walking, etc) after taking?
zolpidem (ambien)
What drug is an antagonist of benzo-binding sites on GABAa?
flumazenil
What drug is used to manage benzo overdose and reverse benzo-induced sedation?
flumazenil
What drug is a/w seizures with long-term sedation or concomitant TCA use?
flumazenil
Barbiturate used to control tonic-clonic seizures
phenobarbital (long-acting)
Barbiturate that is short-acting sedative/anesthetic but has been replaced by Propofol and banned in US d/t lethal injections
thiopental
What drugs increase the duration of GABA-gated Cl- channel opening?
barbiturates
hyperpol–>reduce cell firing
Why are barbiturates so deadly?
at high doses, open Cl- channels without need for GABA–> can’t be controlled
CNS depression–> low BP and respiratory rate
What drugs are inducers of CYP450?
barbiturates
–>increase metabolism of drugs
What drug is a non-benzo anxiety med that acts on serotonin receptors and lacks tolerance, dependence and withdrawal?
buspirone
Can you have additive CNS depression with buspirone and other sedative drugs?
no
minimal psychomotor impairment
What drug is used for sleep disorders and activates MT1/2 in SCN in CNS?
ramelteon (melatonin analog)
Can you have abuse, withdrawal or dependency with ramelteon?
no
What drug blocks binding of orexins and is used with difficulty falling asleep?
suvorexant
What drug antagonizes H2 receptors, inhibits reuptake of serotonin and norepi, and is used for sleep maintenance and tmt of resistant MDD?
doxepin
Do antihistamines act on anxiety?
no, only cause sedation
When to use benzos in GAD?
use acutely until SSRIs kick in
reserve for pts without hx abuse disorder
What drug has been shown to reduce anxiety in GAD without risk of dependence?
buspirone
How to treat separation anxiety?
CBT
SSRI
Can you still get constipation and dilated pupils with opioid tolerance?
yes
What are examples of opioid antagonists?
naloxone (narcan)
naltrexone (prevents euphoria, decrease cravings)
What are the 3 major classes of opioid receptors?
mu
kappa
delta
What is the most serious adverse effect of opioids?
respiratory depression
Side effects of opioids
main: resp depression
constipation urinary retention orthostatic hypotension emesis birth defects increase ICP
What G protein receptor is involved in opioid signaling?
Gi
Pure opioid agonists act at what receptors?
mu and kappa
Pentazocine acts on what opioid receptors?
antagonist at mu
agonist at kappa
Butorphanol acts on what opioid receptors?
partial agonist at mu
agonist at kappa
Buprenorphine acts on what opioid receptors?
partial agonist at mu
antagonist at kappa
***used to treat addicts (Subloxone)
What responses does the mu opioid receptor cause?
analgesia (+ kappa) respiratory depression sedation (+ kappa) euphoria physical dependence decreased GI motility/constipation (+kappa)
What responses does the kappa opioid receptor cause?
analgesia
sedation
constipation
Why are oral doses of opioids larger than iv doses?
significant first-pass metabolism
Why give kids less dose of opidoids?
blood brain barrier not fully developed
What responses to opioids are affected with tolerance?
analgesia
euphoria
sedation
respiratory depression
NOT constipation or miosis
Are withdrawal from opioids dangerous/fatal?
NO (3Bs are fatal)
unpleasant so withdraw gradually
Why do you avoid anticholinergic drugs (atropine, antihistamines, TCAs) with opioids?
exacerbate constipation and urinary retention
Triad of opioid overdose
coma
respiratory depression
pinpoint pupils
What opioid is 100x more potent than morphine, has same adverse effects and multiple formulations?
fentanyl
think prince and tom petty
What opioid is more potent than morphine and used for induction and maintenance of anesthesia?
alfentanil
remifentanil
sufentanil
What is an IV opioid with rapid onset and brief duration (used for postop analgesia)?
remifentanil
What opioid used to be used for migraines is in decline d/t short half life (frequent dosing), adverse reactions and toxic metabolite build-up? Also abused by healthcare workers d/t lack of pinpoint pupils (anticholinergic effect)?
meperidine (demerol)
What drug is an NMDA receptor antagonist, similar to morphine, long duration of action but causes disproportionate number of deaths via torsades?
methadone
What drug has higher lipid solubility vs morphine and gives a greater high when injected?
heroin
What drug is used for mod-severe pain, similar SA c/t morphine, reversed by naloxone and more water soluble (can be diluted in smaller volume for injection)?
hydromorphone (Dilaudid)
oxymorphone, levorphanol
What drug is the prototype for moderate-severe opioid agonist, given PO, can be converted to morphine–>analgesia, and formulated alone or with nonopioid analgesics? Also used as cough suppressant.
codeine