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Barbiturate that is short-acting sedative/anesthetic but has been replaced by Propofol and banned in US d/t lethal injections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
What drug is similar to codeine and metabolized by CYP3A4?
oxycodone (OxyContin)
What drug is similar to codeine but only available in combo with other drugs?
hydrocodone
w/ acetaminophen–> Vicodin
What drug is a mu opioid antagonist that can’t cross BBB, used for opioid-induced constipation?
methylnaltrexone
What drug is a mu opioid agonist that can’t cross BBB, used for acute and chronic diarrhea?
loperamide
Large quantities of this drug (used for a high or alleviate withdrawal sx) can cause?
torsades de pointes d/t QT prolongation
What opioid is safe for use in renal and hepatic insufficiency?
fentanyl
Interaction of opioids with CNS depressants
increased respiratory depression and sedation
Interaction of agonist-antagonist opioids with pure opioids
precipitation of withdrawal reaction
Interaction of opioids with anticholinergic drugs
increased constipation and urinary retention
Interaction of opioids with hypotensive agents
increased hypotension
Interaction of opioids with monoamine oxidase inhibitors
hyperpyrexic (F) coma
What is an ingredient in vaping that is the primary cause of lung injuries and is used as thickening agent?
vitamin E acetate
Does vaping contain nicotine?
yes
What is an orally administered synthetic 9-THC that acts mainly on CB1 and produces analgesia, appetite enhancement, muscle relaxation, psychological effects and hormonal actions?
dronabinol
Dronabinol indications
anorexia in AIDS pts
chemotherapy-induced N/V
off-label: OSA
What is a THC capsule approved for chemo-induced N/V?
nabilone
Adverse effects of THC/marijuana
judgement and coordination–> increase risk for accidents
sedation, bloodshot eyes, depression, dizziness, tachy, hypotension, hallucinations, dry mouth
What kind of pain is cannibis preferred for?
neuropathic and chronic pain
Contraindications for cannabis use
hx psychosis
current or past substance abuse disorder
heart or lung disease
What is CBD useful to treat?
epilepsy
Dravet syndrome (myoclonic seizure)
Lennox-Gastaut syndrome (tonic seizures)
What is the difference between stimulant and non-stimulant meds for ADHD?
stimulants are amphetamine derivatives
Side effects of stimulants
dyspepsia, GI distress
headache
decreased appetite
–> weight loss, reduced growth
insomnia
anxiety
irritability/agression/agitation
elevated BP/HR
Rare effects of stimulants
priapism
seizures
sudden cardiac death
stroke and MI in adults
chemical leukoderma w/ Daytrana patch
What drugs are controlled substances?
stimulants
onset of activity 24 hours
What amphetamine stimulants are immediate release tablets?
dextroamphetamine
dextroamphetamine (adderall)
methamphetamine (desoxyn)
What amphetamine stimulants are immediate release liquid?
dextroamphetamine sulfate (procentra)
What amphetamine stimulants are immediate release capsules?
amphetamine sulfate (evekeo)
What amphetamine stimulants are extended release capsules?
dextroamphetamine (adderall xr)
dextroamphetamine
lisdexamfetamine (vyvanse)
amphetamine mixed salt (mydayis)
What amphetamine stimulants are extended release liquids?
amphetamine (dyanavel xr)
What are methylphenidate-based stimulates that are immediate release tablets?
dexmethylphenidate
methylphenidate (ritalin)
What are methylphenidate-based stimulates that are immediate release liquids?
methylphenidate (methylin)
What are methylphenidate-based stimulates that are sustained tablets?
methylphenidate (ritalin-SR)
What are methylphenidate-based stimulates that are extended release tablets?
methylphenidate HCL (concerta)
methylphenidate ER
What are methylphenidate-based stimulates that are extended release capsules?
methylphenidate (aptensio XR)
dexmethylphenidate hcl (focalin xr)
methylphenidate hcl (metadate cd)
methylphenidate hcl er (ritalin LA)
What are methylphenidate-based stimulates that are extended release transdermal patch?
daytrana (methylphenidate transdermal)
What are methylphenidate-based stimulates that are extended release chewable tablets?
methylphenidate hcl (quillichew)
What are methylphenidate-based stimulates that are extended release liquids?
methylphenidate (quillivant xr)
MOA of non-stimulant meds for ADHD
inhibit NE pre-synaptic uptake
agonist of CNS alpha 2 adrenergic receptors
What drugs are useful for patients intolerant of stimulant effects?
non-stimulants
1-4 week onset of activity
nonscheduled
Capsule non-stimulant
atomoxetine (straterra ER)
Non-stimulant meds that are antihypertensives
clonidine ER
guanfacine ER
both tablets
risk of rebound HTN
What are stimulant users at risk of?
future substance abuse
psychosis
Non-IR stimulant with formulation of amphetamine
adzenys XR-ODT
3:1 d to l isomer
qd, dissolves on tongue
Which ADHD stimulant is a pro-drug?
Lisdexamfetamine
Abstinence syndrome
sx that occur with withdrawal of a drug in a dependent person
What classifies drug dependence?
signs and sx caused by withdrawal from chronic use or abrupt lowering of dose
AKA physical dependence
Define designer drug
synthetic derivative of a drug with a slightly modified structure
no major change in action
Describe sensitization
increase in response with repetition of same dose of drug
shifts left vs tolerance shifts right
Most commonly abused prescription depressants
alprazolam (xanax)
zolpidem
zaleplon
Most commonly abused prescription stimulants
adderal
methylphenidate
NMDA antagonist that reduces desire to drink alcohol
acamprosate
What can caffeine be used for?
improve alertness
migraine ha
ha after epidural anesthesia
asthma
ADHD
memory
What drugs are abused but aren’t necessarily adductive?
LSD
PCP/angel dust
Ketamine (special k)
How long does 1 oz of alcohol take to metabolize?
1 hour
so 6oz–> 6 hrs
Drugs for tmt of acute methanol or ethylene glycol poisoning
ethanol
fomepizole
Drugs for prevention of alcohol abuse
acamprosate
disulfiram (antabuse)
naltrexone
Drugs for tmt of acute alcohol withdrawal syndrome
diazepam (valium)
lorazepam (ativan)
oxazepam
thiamine (Vit B1)
Naltrexone MOA
alcohol and opiate dependence
mu opioid antagonist
reduces craving and short-term rate of relapse
Acamprosate MOA
weak NMDA antagonist and GABAa agonist
reduces short and long-term relapse rates
Disulfiram MOA
irreversibly inhibits ADH–> causes extreme discomfort in pts who drink alcohol
Describe Neuroleptic Malignant Syndrome (NMS)
after antipsychotic use (new or increased dose)
can be hours–>30 days until onset of sx
Malignant FEVER: ~Myoglobinuria (muscle damaged, releases myoglobin, can cause acute renal failure) ~Fever ~Encephalopathy ~Vitals unstable ~increased Enzymes, specifically CK ~muscle Rigidity
Tmt for Neuroleptic Malignant Syndrome (NMS)
dantrolene: binds ryanodine receptor, decreases calcium release to relax muscles
bromocriptine (dopamine agonist)
D/C CAUSATIVE AGENT
Typica/First Gen Antipsychotics
Haloperidol Pimozide Trifluoperazine Fluphenazine Thioridazine Chlorpromazine
-azine
What antipsychotic to use in delirium?
haloperidol (haldol)
High potency first gen antipsychotics
Hal Tries to Fly HIGH
Haloperidol
Trifluoperazine
Fluphenazine
more neuro SE like EPS
Low potency first gen antipsychotics
Cheating Thieves are low
Chlorpromazine
Thioridazine
MOA of first gen psychotics
block D2 receptors–> increase CAMP
decrease dopamine, also block these receptors:
muscarinic (ACh)
histamine
alpha-1
SE of first gen anitpsychotics
EPS hyperprolactinemia metabolic syndrome (obesity, DM, hyperlipidemia) antimuscarinic (dry mouth, constipation) antihistamine (sedation) alpha: orthostatic hypotension QT prolongation corneal deposits (chlorpromazine) retinal deposits (thioridazine) NMS
Sx of hyperprolactinemia
galactorrhea
oligomenorrhea
gynecomastia
What antipsychotic causes corneal deposits
chlorpromazine (1st)
What antipsychotic causes retinal deposits
thioridazine (1st)
Describe hours-days sx of EPS
acute dystonia
- ->muscle spasm, rigidity/stiffness
- ->oculogyric crisis
tmt: benztropine (blocks muscarinic receptors to decrease ACh which increases dopamine) and diphenhydramine
Describe days-months sx of EPS
akathisia (restlessness)
–>tmt: propranolol or other B blocker, benztropine, benzos
parkinsonism (bradykinesia)
- -> d/t decreased dopamine
- -> tmt: benztropine, amantadine
Describe months-years sx of EPS
Tardive dyskinesia
–>choreathetosis, smaking gums, etc
tmt: clozapine, valbenazine, deutetrabenazine (VMAT 2 inhibitors)
What is EPS
d/t decreased dopamine, decreased modulation of movement via basal ganglia
Atypical/2nd generation antipsychotics
Aripiprazole Asenapine Clozapine Olanzapine Quetiapine Iloperidone Paliperidone Risperidone Lurasidone Ziprasidone
- idone
- piprazole
- apine
MOA of -idone atypical antipsychotics
block serotonin (2A) and dopamine (D2) receptors
MOA of -piprazole atypical antipsychotics
partial serotonin and dopamine agonist
What drug to use for tmt-resistant schizoprhenia or schizoaffective disorder
clozapine
What drug to use for suicide prevention in schizophrenia
clozapine
universal SE of atypical antipsychotics
prolonged QT
fewer EPS and anticholinergic c/t typical antipsychotics
SE of atypical -apines (antipsychotics)
metabolic syndrome: weight gain, DM, hyperlipidemia
olanzapine
clozapine
O–>obesity
SE of clozapine
2nd gen/atypical antipsychotic:
Agranulocytosis (monitor WBC)
Seizures (dose related)
must watch bone marrow CLOZely with CLOZapine
SE of risperidone
2nd gen/atypical antipsychotic:
hyperprolactinemia
–>galactorrhea, amenorrhea, gynecomastia
Long-acting injectables to treat non-adherence of antipsychotics
Risperidone
Olanzapine
Aripiprazole
Paliperidone
What is the most common drug-induced cause of hyperprolactinemia?
antipsychotics (fluphenzine, haloperidol, risperidone)
Tmt of EPS
benztropine (antimuscarinic)
diphenhydramine (antihistamine)
Tmt of tardive dyskinesia
VMAT 2 inhibitors (-benazine)
Difference between typical and atypical antipsychotics
typical: EPS, side effects, act only on dopamine D2 receptor
atypical: more serotonin (2a) receptor activity vs dopamine, less EPS and anticholinergic effects
What can cause drug rxn w/ eosinophilia and systemic sx (DRESS)?
olanzapine
Cause sedation and anticholinergic SE the most
chlorpromazine
thioridazine
cariprazine
clozapine (other -apines)
Cause orthostatic hypotension SE the most
chlorpromazine
thioridazine
clozapine
cariprazine
Antipsychotic least likely to cause weight gain
ziprasidone
Antidepressant used for nicotine withdrawal
bupropion
Antidepressant used for enuresis/bedwetting
imipramine
Antidepressant used for diabetic peripheral neuropathy
duloxetine
Antidepressant used for fibromyalgia
duloxetine
Antidepressant used for chronic musculoskeletal pain
duloxetine
Antidepressant used for stress incontinence
duloxetine