week 2 SUD Flashcards
medication for overdose/reversal of alcohol use
moa
Flumazenil
ANTAGONIST at GABA-BENZODIAZEPINE RECEPTOR
What is the black box warning for Flumazenil?
seizures
specific medical indications for Flumazenil
q
used for benzodiazepine overdose only in inpatient medical settings.
What drugs are useful for relapse prevention/maintenance for alchoholic dependance?
Disulfiram (Antabuse)
Acamprosate (Campral)
What is the MOA of Disulfiram (antabuse)
inhibits aldehyde dehydrogenase
indication- relapse/prevention alchoholism
gives very uncomfortable side effects when used with alchohol
What are the side effects Disulfiram?
black box warning
sweating, nausea, vomiting when used concurrently with alcohol
should never be administered while alcohol intoxication setting.
What are the three benzodiazepines?
Chlordiazepoxide (Librium)
Diazepam (Valium)
Lorazepam (Ativan)
what is the MOA of
chlordiazepoxide (librium)
Diazepam (Valium)
Lorazepam (Ativan)?
bind to the benzodiazepine site on the GABA-A receptor
This increases the frequency of chloride (Cl⁻) channel opening in the presence of GABA
Result: Enhanced inhibitory neurotransmission → sedative, anxiolytic, muscle relaxant, anticonvulsant, and amnestic effects
what class of medications are useful for managing withdrawl symptoms for alcohol dependance?
benzodiazipines
barbiturates
What is the MOA of Phenobarbital
class and use
Bind to GABA-A receptors (same receptor type as benzodiazepines)
But instead of increasing frequency, barbiturates increase the DURATION of chloride channel opening when GABA is present
This leads to prolonged neuronal inhibition and CNS depression
barbiturates- alchohol withdrawl
adverse effects of phenobarbital
CNS depression: sedation, confusion, coma
Respiratory depression: can be fatal in overdose
Dependence and withdrawal (dangerous and potentially life-threatening)
Drug interactions: Induce cytochrome P450 enzymes
Narrow therapeutic index → risky
pharm therapy for overdose of opiods?
Naloxone- (Narcan)
MOA of Naloxone (Narcan) and what is its contradiction?
Mu- opiod receptor antagonist
contradicted in liver failure
may need repeat dosing
What pharm therapies are used for relapse prevention and maintenance in opiod used disorders?
Naltrexone (ReVia)(Mu- antagonist)
Buprenorphine (subutex)( partial agonist)
buprenorphine + naloxone (suboxone) (partial + antagonist)
methadone (agonist)
which opiod therapy drug helps maintain abstenance once opiod free? how?
Naltrexone-
Full opioid receptor antagonist (μ-receptor)
Blocks euphoric and analgesic effects of opioids
How does buprenorphine help in opioid addiction treatment, and why is it safer than full agonists?
MOA: Partial μ-opioid receptor agonist—high affinity but low activity.
Use: Reduces cravings and withdrawal without strong euphoria.
Pearl: Has a ceiling effect on respiratory depression → safer in overdose. Can be prescribed in office-based settings.
What is the purpose of naloxone in Suboxone, and how does this combo medication work?
MOA:
Buprenorphine: partial μ-opioid agonist
Naloxone: full antagonist (inactive orally, active if injected)
Use: Maintenance therapy that deters IV abuse.
Pearl: Naloxone precipitates withdrawal if injected, not when taken as prescribed (sublingually).
Why is methadone effective in opioid maintenance therapy, and what are key risks?
MOA: Full μ-opioid receptor agonist with a long half-life
Use: Prevents withdrawal and cravings in severe OUD, given in specialized clinics
Pearl: Watch for QT prolongation and respiratory depression. Highly effective but has high abuse potential.
what drug is used for opiod withdrawl? and how does it work?
Clonidine
MOA: alpha 2 adrenergic agonist
How does nicotine replacement therapy (NRT) work, and what are the available forms?
MOA: Provides a controlled dose of nicotine to reduce withdrawal and cravings, allowing gradual taper.
Forms: Patches, gum, lozenges, inhalers, nasal spray
Pearl: Combining patch (baseline) + gum/lozenge (prn cravings) is often more effective than monotherapy.
What is the mechanism and benefit of using bupropion for smoking cessation?
MOA: Norepinephrine-dopamine reuptake inhibitor (NDRI)
Reduces nicotine cravings and withdrawal symptoms
Non-nicotine aid with mild stimulant effects
Pearl: Also used in depression; contraindicated in patients with seizure disorders or eating disorders due to seizure risk.
How does varenicline (Chantix) work in nicotine addiction, and what side effects should be monitored?
MOA: Partial agonist at α4β2 nicotinic receptors—stimulates receptor enough to reduce cravings, but blocks nicotine’s reinforcing effect.
Effect: Reduces both withdrawal and the satisfaction of smoking.
Pearl: Watch for neuropsychiatric symptoms (e.g., depression, suicidal ideation), vivid dreams, and nausea.
