Exam review Flashcards

(53 cards)

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
Benzodiazepines
-increase frequency cof channel opening
26
Barbituates
increase duration of opening chloride channels -directly activate chloride channels at high concentrations
27
Zolpidem
-decrease REM sleep but not slow wave sleep -provides sustained sleep
28
Zalplon
-decrease latency of sleep onset -used for patients who wake early in sleep cycle
29
Eszopiclone
-increase total sleep time -increase 2 NREM sleep -decrease REM at high dose
30
Rebound insomnia
only occurs with zolpidem and zaleplon at high doses
31
anestesia
diazepam, lorazepam, midazolam
32
muscle relaxation
-certain benzodiazepines and meprobamate
33
Buspirone
-anxiety reducing -substrate of Cyp3A4
34
Ramelteon and Tasimelteon
-melatonin agonists -no rebound insomnia or withdrawl effects
35
Orexin receptor antagonists
-Suvorexant+ first approved for insomnia -2 others approved recently
36
Triazolam absorption
absorbed extremly rapidly
37
Sedative hypnotics PK
-hepatic metabolism -microsomal oxidation and conjugated to be excreted in urine
38
Zolpidem PK
-peak levels 1-3 hours
39
Zaleplon PK
-metabolized by hepatic aldehyde oxidase and CYP3A4 -dose adjustment in elderly or liver issues
40
Tolerance
Decreased drug responsivness with repeates exposure, often requiring higher doses
41
Dependenance
-psycological dependance starts as simple behavioral patters -physiological dependence is when drug is need to avoid withdrawal
42
Benzodiazepine for withdrawals
diazepam and chlordiazepoxide
43
treatment for delirium tremens
lorazepam
44
Toxic effects of sedative hypnotics
-CNS depression -amnesia -hangover -elderly
45
Alcohol metabolism
-alcohol dehydrogenase -MEOS -acetyaldehyde dehydrogenase
46
What genetic variation is associated with being protective againist alcohol dependence
deficiency of ALDH2 -ADH1*2
47
Pharmacodynamics of acute alcohol consumption
-sedation, releif of anxiety -decrease in myocardial contractility -vasodilator and hypothermia
48
Short acting benzodiazepines
lorazepam and oxazepam
49
Naltrexone
-long acting opioid antagonist -must be opioid free otherwise otherwise precipitates withdrawal
50
Acamprosate
-weak NMDA receptor antagonist and GABA-A activator -may reduce relapse rates
51
Disulfiram
Inhibits aldehyde dehydrogenase -extreme discomfort after drinking -adhearence is low
52
Methanol poisoning
-absorbed through skin or respiratory tract -slow conversation to toxic metabolites -treat with fomepizole or IV ethanol
53
Ethylene glycol poisoning
-sweet taste -treat with fomepizole or hemodialysis