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Therapeutics 3 - Spring 2018 > Final - Vanrign Pt 2 > Flashcards

Final - Vanrign Pt 2 Flashcards

1
Q

2 main pathways of action for cocaine

A

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

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2
Q

what drugs can be used for narcolepsy

A

amphetamine
methylphenidate
armodafinil/modafinil
Sodium Oxybate

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3
Q

which stimulant inhibits BOTH DAT and NET

A

methylphenidate

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4
Q

which stimulant is a prodrug of amphetamine and modulates dopamine transport

A

lisdexamphetamine

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5
Q

how do drugs like phentermine for weight loss work?

A

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

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6
Q

Nicotine:

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

A

full agonist

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7
Q

Nicotinic ach receptors are what kind of structure?

A

pentameric

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8
Q

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

A

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

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9
Q

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

A

nicotine patch/gum/e-cig

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10
Q

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

A

varenicline

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11
Q

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

A

bupropion

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12
Q

methylxanthines (like caffeine) are ______ to adenosine receptors

A

antagonists

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13
Q

how does cocaine affect the dopamine transporter

A

it is an antagonist to it in the nucleus accumbens

same as methylphenidate

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14
Q

how does meth/ecstasy/bath salts affect DA

A

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

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15
Q

is cocaine or meth a bigger structure?

A

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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16
Q

Nicotine is inhibitory or excitatory

A

excitatory

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17
Q

amphetamines are contraindicated with antidepressants???

A

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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18
Q

crack or cocaine gets smoked and why?

A

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

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19
Q

bath salt is known as a synthetic ______

A

cathinone

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20
Q

ADEs of Cathinone use (aka bath salts)

A

hyperthermia
paranoid delusion
cardiac arrest
anxiety/violence

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21
Q

PK of alcohol:

peaks in ______ minutes

A

30 - 90

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22
Q

PK of alcohol:

alcohol increase or decrease acid release

A

increase acid release

23
Q

PK of alcohol:

absorption is promoted or slowed by food

A

slowed

24
Q

PK of alcohol:

has zero, 1st, or 2nd order kinetics

A

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

25
Q

PK of alcohol:

what is the rate limiting step of alcohol

A

ADH (aka 1st step)

26
Q

PK of alcohol:

most metabolism is done by what organ

A

liver

27
Q

PK of alcohol:

what two things can be done to get alcohol to acetylaldehyde

A

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

28
Q

PK of alcohol:

acetylaldehyde gets metabolized by ______

A

ALDH (aldehyde dehydrogenase)

29
Q

T or F: acetylaldehyde is an antioxidant

A

false… well guessing so since the molecule is TOXIC!

30
Q

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

A

Fomepizole

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

31
Q

what SNP in ALDH2 reduces activity

A

ALDH2 *2

32
Q

what drug is an irreversible inhibitor of ALDH2

A

disulfiram

33
Q

what happens if you are heterozygous ALDH2*2

A

flushing and increase skin temp

reduced metabolized activity

34
Q

what happens if you are homozygous ALDH2*2

A

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

35
Q

what pharmacological things happen with alcohol at each level:

30 - 60 mg/dL:
60 - 90: 
80 - 120:
100 - 200:
300 - 500:
A

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

36
Q

alcohol causes hypo or hyper thermia

A

hypo

37
Q

alcohol upregulates what CYP enzyme (affects APAP)

A

CYP2E1

38
Q

what are the 3 accepted drugs for treating alcoholism

A

disulfiram
acaprosate
naltrexone

39
Q

FDA approved drugs for txing alcoholism: MOA of Disulfiram?

A

ALDH inhibitor

40
Q

FDA approved drugs for txing alcoholism: MOA of Acamprosate?

A

NMDA receptor antagonist/GABA agonist

41
Q

FDA approved drugs for txing alcoholism: MOA of Naltrexone?

A

opioid receptor antagonist

42
Q

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

A

118G

43
Q

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

A

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

44
Q

heroin is also known as ______

A

diacetylmorphine

aka acetyl groups on pos 3 and pos 6

45
Q

heroin is lipophillic or hydrophillic

A

lipophillic bc acetyl groups soooo cross BBB v well!

46
Q

heroin or morphine is a prodrug?

A

heroin is! heroin gets metabolized into morphine!

47
Q

what plant (other than opium poppy) contains opioids

A

kratom

48
Q

which is more potent? fentanyl or morphine or heroin

A

fentanyl by hella much

49
Q

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

A

remifentanil

acetylfentanyl

50
Q

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

A

amphetamines/marijauna/nicotine

51
Q

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

A

cocaine

52
Q

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

A

alcohol

53
Q

how does methadone work for opioid dependence?

A

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

Therapeutics 3 - Spring 2018 (20 decks)

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