Final - Vanrign Pt 2 Flashcards by Blade Joneson

2 main pathways of action for cocaine

Increase in catecholamines - by being an antagonist of DAT
and
decrease Na+ transport

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what drugs can be used for narcolepsy

amphetamine
methylphenidate
armodafinil/modafinil
Sodium Oxybate

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which stimulant inhibits BOTH DAT and NET

methylphenidate

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which stimulant is a prodrug of amphetamine and modulates dopamine transport

lisdexamphetamine

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how do drugs like phentermine for weight loss work?

stimulate release of NE and DA in lateral hippocampus aka feeding center of brain

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Nicotine:

full agonist, or partial agonist, or antagonist at nicotinic ach receptors?

full agonist

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Nicotinic ach receptors are what kind of structure?

pentameric

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T or F: Nicotine is degraded by Acetylcholinesterase just like Ach

False - nicotine is not and thus has a long half life than Ach

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what meds can be used for treating nicotine addiction — specifically agonist meds

nicotine patch/gum/e-cig

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what meds can be used for treating nicotine addiction — specifically partial agonist meds

varenicline

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what meds can be used for treating nicotine addiction — specifically antagonist meds

bupropion

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methylxanthines (like caffeine) are ______ to adenosine receptors

antagonists

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how does cocaine affect the dopamine transporter

it is an antagonist to it in the nucleus accumbens

same as methylphenidate

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how does meth/ecstasy/bath salts affect DA

it pushes DA out from vesicles, changes gradient, whihc forces transporter to work in the reverse

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is cocaine or meth a bigger structure?

cocaine - why only an antagonist and doesn’t go inside the cell like meth does to affect vesicle release of DA

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Nicotine is inhibitory or excitatory

excitatory

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amphetamines are contraindicated with antidepressants???

to vanrijn yes because amphetamines are MAOIs too and that is not ok with antidepressants (but who knows if actually applicable)

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crack or cocaine gets smoked and why?

crack does because you add ammonia to make a free base = lower melting temp when free base

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bath salt is known as a synthetic ______

cathinone

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ADEs of Cathinone use (aka bath salts)

hyperthermia
paranoid delusion
cardiac arrest
anxiety/violence

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PK of alcohol:

peaks in ______ minutes

30 - 90

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PK of alcohol:

alcohol increase or decrease acid release

increase acid release

PK of alcohol:

absorption is promoted or slowed by food

slowed

PK of alcohol:

has zero, 1st, or 2nd order kinetics

mainly 0 ( but at end it goes to 1st order)

PK of alcohol: | what is the rate limiting step of alcohol

ADH (aka 1st step)

PK of alcohol: | most metabolism is done by what organ

liver

PK of alcohol: | what two things can be done to get alcohol to acetylaldehyde

ADH (alcohol dehydrogenase) or MEOS (microsomal ethanol oxidizing system) --- only done at high alcohol concentrations

PK of alcohol: | acetylaldehyde gets metabolized by ______

ALDH (aldehyde dehydrogenase)

T or F: acetylaldehyde is an antioxidant

false... well guessing so since the molecule is TOXIC!

what drug is known as an ADH inhibitor and why would you want to use it

Fomepizole use when methanol ingestion/poisoning -- drug given because it prevents acetylaldehyde (a toxic metabolite) from being made

what SNP in ALDH2 reduces activity

ALDH2 *2

what drug is an irreversible inhibitor of ALDH2

disulfiram

what happens if you are heterozygous ALDH2*2

flushing and increase skin temp | reduced metabolized activity

what happens if you are homozygous ALDH2*2

strong!!! hangover alcoholic neuropathy bc neurotoxic acetylaldehyde cant really metabolize acetylaldehyde at all

what pharmacological things happen with alcohol at each level: ``` 30 - 60 mg/dL: 60 - 90: 80 - 120: 100 - 200: 300 - 500: ```

30: euphoria, disinhibition, talkative 60: analgesia 80: CNS stimulation (mood swings, aggression) 100: CNS depression (slurred speech, ataxia) 300: coma/death

alcohol causes hypo or hyper thermia

hypo

alcohol upregulates what CYP enzyme (affects APAP)

CYP2E1

what are the 3 accepted drugs for treating alcoholism

disulfiram acaprosate naltrexone

FDA approved drugs for txing alcoholism: MOA of Disulfiram?

ALDH inhibitor

FDA approved drugs for txing alcoholism: MOA of Acamprosate?

NMDA receptor antagonist/GABA agonist

FDA approved drugs for txing alcoholism: MOA of Naltrexone?

opioid receptor antagonist

what SNP in mu receptor gene causes pts (mainly asians) respond better to naltrexone

118G

what are 3 other drugs (NOT FDA approved tho) for txing alcoholism

topiramate (also NMDA receptor antagonist) Baclofen (GABA(B) receptor agonist) Varenicline (partial nicotinic receptor agonist)

heroin is also known as ______

diacetylmorphine | aka acetyl groups on pos 3 and pos 6

heroin is lipophillic or hydrophillic

lipophillic bc acetyl groups soooo cross BBB v well!

heroin or morphine is a prodrug?

heroin is! heroin gets metabolized into morphine!

what plant (other than opium poppy) contains opioids

kratom

which is more potent? fentanyl or morphine or heroin

fentanyl by hella much

what drugs are typically being added to heroin recently to make the batches more strong

remifentanil | acetylfentanyl

________ drugs can cause low birth wt and premature birth when mom took them when pregnant

amphetamines/marijauna/nicotine

________ can cause lower IQ/decrease developmental learning when mom took them when pregnant

cocaine

________ can cause heart defects, head/face deformities, and mental problems when mom took them when pregnant

alcohol

how does methadone work for opioid dependence?

is a full agonist for mu opioid receptor but acts slowly/leaves slowly soooo no big peaks