Kruse- Intro to Drugs of Abuse Sedative-Hypnotics Alcohol Flashcards by Stephen Tulley

Sedatives do what?

-decrease CNS activity, moderate excitement, and calms the recipient

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Hypnotics do what?

-produces drowsiness and facilitates the onset and maintenance of sleep and from which the recipient can be aroused easily

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Where/How do Benzodiazpines work?

Act on ligand gated ion channels aka GABAa receptors
cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects
makes receptor more active in lower concentrations of GABA
so you need BOTH a BENZO and GABA receptor presents

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Where/How do Barbiturates work?

Act on GABAa receptors
cause a wide spectrum of effects: mild sedation to anesthesia
Keep receptor open for longer period of time

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Where do Benzodiazepines distribute?

-CNS, Placenta, and Breast-milk

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How are Benzodiazepines processed?

CYP34A phase 1

- Glucuridation phase 2

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Do Benzodiazepines have a risk of dependence and tolerance?

-yes

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Benzodiazepines examples?

Diazepam (Valium)
alprazolam (Xanax)
lorazepam (Ativan)

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Half life and onset of Chlordiazepoxide? active metabolites?

greater than 100 hours
intermediate onset
yes

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Half life and onset of Diazepam? Active metabolites?

greater than 100 hours
very fast
yes

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Half life and onset of Oxazepam? Active metabolites?

5-14 hours
Slow
none

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Half life and onset Lorazepam? Active metabolites?

10-20 hours
intermediate
none

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Use of Midazolam?

rapid on and rapid off

- dentists use this to induce anesthesia or in other quick surgery settings

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Intermediate to lond acting Benzodiazepines are?

Diazepam
Lorazepam
Clonozepam

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Short acting benzodiazepines are?

Midazolam
Oxazepam
Alprazolam
Temazepam
Triazolam

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How do Barbiturates work?
What are examples?
risk of dependence and tolerance?

binding to GABA a receptor and increase duration of time the channel is actually open
—“arbitals”
yes, risk of both but not all people have risk or dependence. all people build tolerance

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How do Benzodiazepines work?

-Causes GABA receptors to be activated at lower concentrations

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Barbiturates are mostly used for what? examples?

-sleep aids
-Eszopiclone
-Zolpidem
-Zaleplon
“Sleep Ezzy with barbiurates”

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Sedative-hypnotics are used to treat what?

-anxiety, insomnia, epilepsy, siezures, control withdrawals

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Benzo Drugs to treat anxiety?
How high is the theraputic index? What is the antagonist (antidote) to overdose?

What are the disadvantages?

Clonazepam
Lorazepam
Alprazolam
Diazepam
high
Flumazenil treats OD

-disadvantages are dependence risk, CNS depression, SSRIs are preferred for these reasons

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Benzo drugs used for insomnia? side effect?

-Eszopiclone (long half life)
-Zolpidem (2 sustain sleep)
-Zaleplon (both Zol and Zal act rapidly)
EZZy Sleep

-sleep shopping and sleep driving

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Ramelteon is used to treat what?
MOA?
bioavailability?
Metabolized by?

insomnia
agonist at MT1 and MT 2 melatonin receptors
low bioavailability
CYP1A2

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Buspirone is used to treat what?
how long to take affect?
Does it cause sedation, hypnotic, euphoric, etc?
MOA?
Metabolized for?

general anxiety
takes a full week
no it does not
unknown
CYP3A4

What is responsible for breaking down alcohol?

How high is it’s first pass?

How much metabolized per hour?

alcohol dehydrogenase (ADH)
alcohol had zero order kinetics meaning as soon as you start drinking all the enzymes used in its biotransformation are maxed out
7-10gs per hour should take 1 drink per hour

What causes hangovers? pathway? why are fewer asains alcoholics?

- acetaldehyde build up - alcohol--> acetaldehyde-->acetic acid - higher concentration of people with polymorphisms of alcohol dehydrogenase

What is the primary excitatory NT in the CNS? what does alcohol do to it? whats the major inhibitor in the CNS?

- NMDA glutamate receptors - alcohol inhibits this - GABA receptor

what is acute alcohol intoxication? what should you do?

- drunk person - monitor breathing and inhaling of vomit - treat w/ glucose and thiamine to prevent korsakoff syndrome

what is chronic alcohol abuse? | how to treat?

- alcoholics | - avoid withdrawal symptoms w/ BENZOs

what are withdrawal symptoms?

-seizures, delirium, and arrhythmias

what treatment does alcohol dependence require?

-psycosocial therapy first and drugs second

what drugs for alcoholism?

-Naltrexone

What is Naltrexone? what is it used for? MOA? what must patients be before starting therapy?

- treatment of alcohol/opiate dependence and reduces craving - mu opioid receptor antagonist (long-acting) - patients must be alcohol and opioid free b/c if not you trigger alcohol withdrawal syndrome

What is Acamprosate? | MOA?

- treat alcohol/opiate - weak NMDA antagonist and GABA receptor agonist mimicking the effects of alcohol in the body - reduces relapse rates

What is Disulfiram? MOA? what must the patient be?

- for alcohol dependence - irreversibly inhibits aldehyde dehydrogenase causing build up of acetaldehyde - makes people feel shitty when they drink - the patient must be highly compliant because they could easily just not take the pill

What are ethanol and Fomepizole used to treat? What is the toxic build up? MOA?

- methanol OD seen with antifreeze, windshield washer fluid, - formaldehyde - ADH has higher affinity for ethanol than it does for methanol. allowing methanol to be cleared form the body unchanged

Do schedule 1 drugs have medical use? addictive? examples?

- no - strong opioids - highest addictive - rohypnol (date rape) Heroin, PCP, MDMA, LSD

Schedule 4 drugs use? addictive? examples

- medical use - least addictive - BENZOs and weak opioids

Are phencyclidine and ketamine addictive?

-no that are rated a 1 on his chart meaning they are not addictive

What receptors do addictive drugs commonly target?

-activate GPCRs | ie opiates, weed, GHB, LSD

BENZOs, Nicotine, and alcohol bind to what receptors?

-ionotropic receptors and ion channels

Are LSD, psilocybin, PCP., and mescaline addictive?

-no

Long term effects of: PCP? LSD?

PCP= irreversible schizophrenia pshchosis LSD= flashbacks and altered perception

The Opioids--- Naloxone, Naltrexone, and Methadone--- inhibit what?

-inhibition of GABA inhibitory neurons

Which of these acts longer? | Naloxone vs Naltrexone

-Naltrexone is the long acting antagonist

Is Methadone a long acting antagonist or agonist?

-agonist

Agitation, HTN, tachycardia, delusions, hallucinations, death, hyperthermia.......What did the patient OD on?

-Amphetamines and cocaine

Slurred speech, drunk behavior, dilated pupils, clammy skin, coma, weak rapid pulse.....what did the patient OD on?

-Barbiturates, BENZOs, alcohol

constricted pupils, clammy skin, nausea, drowsiness, respiratory depression, coma, death.....what did the patient OD on?

-Heroin or other opioids

apathy, irritable, more sleep, disorientation, depression.....what are they withdrawaling from?

-Amphetamines and cocaine

anxiety, insomnia, delirium, tremors, seizures......what are thy withdrawaling from?

-Barbiturates, BENZOs, alcohol

Nausea, chills, cramps, lacrimation, rhinorrhea, yawning, hyperpnea, tremor....what are they withdrawaling from?

-Heroin and other opioids

What are the only two conjugated BENZOs?

- Oxazepam (slow and short acting) | - Lorazepam (intermediate and long acting)

T/F: GABA neurons synapsing on dopamine neurons can shut off the dopamine neurons?

-True

Cocaine blocks

-reuptake of dopamine | = more dopamine in the synapse

Amphetamines works by

-fill up the vesicles keeping dopamine out of the vesicles causing cytoplasmic reverse of dopamine transporter leading to dopamine being pump against its gradient =more dopamine in the synapse

What's a good BENZO to give an addict in order to avoid the dopamine reward pathway?

Oxazepam works because it has a slow onset