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521-Pharmacology > Exam review > Flashcards

Exam review Flashcards

1
Q

MOR Specificity

A

endorphins>enkephalins>dynorphins

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2
Q

DOR specificity

A

enkephalins

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3
Q

KOR Specificity

A

dynorphins

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4
Q

key features: structure of opioid receptor

A

–extracellular and intracellular loops: ligand binding and signaling
-intracellular C terminus including phosphorylation sites
-extracellular N-terminus including glycosylation sites

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5
Q

Opioids ascending pathway

A

-block release of excitatory NTs by blocking Ca channels
-enhance K channels causing hyperpolarization
-as a result, opioid block the release glutamate and substance P

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6
Q

Opioids in descending pathway

A

-enhance pain relief by reducing the release of GABA

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7
Q

DOR Opioid receptor

A

-agonist can have analgesic effect
-serious side effects

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8
Q

KOR opioid receptos

A

-analgesia
psychotomimetic effects

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9
Q

Opioid Receptor Signaling

A

1)Agonist binds
2) G protein binds
3) Arrestin recruitment, signaling and internalization
4) recycling or degradation

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10
Q

oxycodone metabolism

A

-3A4 -noroxycodone
-2D6-oxymorphone

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11
Q

Methadone metabolism

A

-3A4, 2B6, 2D6
-excreted in urine and bile

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12
Q

Buprenorphine

A

-partial mu agonist, antagonist

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13
Q

Embeda

A

morphine + naltrexone

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14
Q

Talwin

A

Pentazocin+Naloxone

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15
Q

Targiniq

A

Oxycodone+Naloxone

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16
Q

Simple partial

A

preserved consciosness

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17
Q

complex partial

A

impaired consciusness

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18
Q

absence seizure

A

staring and cessation of ongoing activities

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19
Q

myoclonic seizure

A

breif shock like contraction

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20
Q

tonic clonic seizure

A

sustained contraction, relaxation

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21
Q

GABA-B

A

-metabotropic(G-protein coupled)
-produces slow and prolonged inhibitory signals

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22
Q

Na Channel AEDs

A

1) Phenytoin
2) Carbamazepine
3) Lamotrigrine
4) Lacosamide
5) Zonisamide

23
Q

Na fast inactivation

A

phenytoin and carbamzepine

24
Q

Na slow inactivation

A

lacosamide, lamotrigine, valproate, zonisamide

25
Q

Benzodiazepines

A

-increase frequency cof channel opening

26
Q

Barbituates

A

increase duration of opening chloride channels
-directly activate chloride channels at high concentrations

27
Q

Zolpidem

A

-decrease REM sleep but not slow wave sleep
-provides sustained sleep

28
Q

Zalplon

A

-decrease latency of sleep onset
-used for patients who wake early in sleep cycle

29
Q

Eszopiclone

A

-increase total sleep time
-increase 2 NREM sleep
-decrease REM at high dose

30
Q

Rebound insomnia

A

only occurs with zolpidem and zaleplon at high doses

31
Q

anestesia

A

diazepam, lorazepam, midazolam

32
Q

muscle relaxation

A

-certain benzodiazepines and meprobamate

33
Q

Buspirone

A

-anxiety reducing
-substrate of Cyp3A4

34
Q

Ramelteon and Tasimelteon

A

-melatonin agonists
-no rebound insomnia or withdrawl effects

35
Q

Orexin receptor antagonists

A

-Suvorexant+ first approved for insomnia
-2 others approved recently

36
Q

Triazolam absorption

A

absorbed extremly rapidly

37
Q

Sedative hypnotics PK

A

-hepatic metabolism
-microsomal oxidation and conjugated to be excreted in urine

38
Q

Zolpidem PK

A

-peak levels 1-3 hours

39
Q

Zaleplon PK

A

-metabolized by hepatic aldehyde oxidase and CYP3A4
-dose adjustment in elderly or liver issues

40
Q

Tolerance

A

Decreased drug responsivness with repeates exposure, often requiring higher doses

41
Q

Dependenance

A

-psycological dependance starts as simple behavioral patters
-physiological dependence is when drug is need to avoid withdrawal

42
Q

Benzodiazepine for withdrawals

A

diazepam and chlordiazepoxide

43
Q

treatment for delirium tremens

A

lorazepam

44
Q

Toxic effects of sedative hypnotics

A

-CNS depression
-amnesia
-hangover
-elderly

45
Q

Alcohol metabolism

A

-alcohol dehydrogenase
-MEOS
-acetyaldehyde dehydrogenase

46
Q

What genetic variation is associated with being protective againist alcohol dependence

A

deficiency of ALDH2
-ADH1*2

47
Q

Pharmacodynamics of acute alcohol consumption

A

-sedation, releif of anxiety
-decrease in myocardial contractility
-vasodilator and hypothermia

48
Q

Short acting benzodiazepines

A

lorazepam and oxazepam

49
Q

Naltrexone

A

-long acting opioid antagonist
-must be opioid free otherwise otherwise precipitates withdrawal

50
Q

Acamprosate

A

-weak NMDA receptor antagonist and GABA-A activator
-may reduce relapse rates

51
Q

Disulfiram

A

Inhibits aldehyde dehydrogenase
-extreme discomfort after drinking
-adhearence is low

52
Q

Methanol poisoning

A

-absorbed through skin or respiratory tract
-slow conversation to toxic metabolites
-treat with fomepizole or IV ethanol

53
Q

Ethylene glycol poisoning

A

-sweet taste
-treat with fomepizole or hemodialysis

521-Pharmacology (11 decks)

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