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Phar300 > lect 10 benzodiazepines and Cannabinoids > Flashcards

lect 10 benzodiazepines and Cannabinoids Flashcards

1
Q

major compund in marijuana

A

THC and CBD

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2
Q

cannabinoids therapeutic effects for?

A

chronic pain in adults and chemotherapy induced nausea

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3
Q

cannabinoids receptors and where

A

CB1 IN BRAIN CB2 IN IMMUNE SYSTEM

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4
Q

made in the body and natural ligand for cannabinoids receceptors

A

endocannabinoids

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5
Q

compounds of endocanna.

A

anandamine AEA, 2-AG

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6
Q

plant derived cannabinoid and coumpounds

A

phytocannabinoid, THC and CBD

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7
Q

made in lab cannabinoids and compound

A

synthetic cannabinoid, mimics of THC

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8
Q

pharmacodynamics of cannabinoids on transmitters

A

presynaptic inhibition of transmitters release

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9
Q

pharmacodynamics of AEA AND 2-AG at CB1 receptor

A

AEA AND 2-AG synthesized post synaptically, act presynaptically on CB1, increase potassium intake decreases calcium, hyperpolarization and inhibition of transmitters release pre synapt. less post synapt stimulation

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10
Q

Distribution cannabinoids

A

extracellular water, lipid soluble so stored in fat and bind serum proteins

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11
Q

Metabolism cannabinoids

A

Mainly in liver

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12
Q

excretion cannabinoids

A

Metabolites in saliva and sweat, largely in urine, some by liver to small intestine (feces)

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13
Q

cannabinoids act on which pathway for addiction

A

reward pathway in brain

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14
Q

schizophrenic brain has elevated levels of what

A

dopamine

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15
Q

first effective neuroleptic (antipsychotic) drug

A

chlorpromazine

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16
Q

amphetamine and cocaine users have more chances of developing what and why

A

have more chance of schizophrenia due to blockage of dopamine reuptake

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17
Q

How does chlorpromazine work

A

Block d2 receptors preventing activation by dopamine

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18
Q

pathways affected by antipsychotic drugs

A

mesolimbic and mesocortical pathway

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19
Q

increased dopamine effects on mesolimbic

A

dellusions, hallucinations

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20
Q

increased dopamine effects on mesocortical

A

intellectual impairement and defective cognitive abilities

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21
Q

downside of chlorpromazine

A

not very selective and had side effects, acted on histamine and 5-HT receptors

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22
Q

how does monoamine oxidase inhibitors work

A

inhibits the metabolism of neurotransm. by monoamine oxidase in presynapt and synapse. increases levels of excitory neurotransm. at synapse and post synapse

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23
Q

tricyclic antidepressants?

A

block 5-ht and noradrenalin reuptake transporter. so increase of neurotrans at synapse and post synapse

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24
Q

side effects of tricyclic antidepre.

A

block adrenergic, histamine and cholinergic receptors so affects vascular system (effects on SNS), produces sedation, affects GI tract and vision

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25
Q

selective serotonin reuptake inhibitors

A

interferes reuptake of serotonin by blocking 5-HT reuptake transporters. increase of neutrans at synapse and post synapse

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26
Q

how many 5-HT receptors and what type of receptor

A

15 and all over the place, GCPRS BUT 5-HT3 ligand gated ion channel

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27
Q

Most common SSRI and potency

A

Fluoxetine (Prozac) high potency of inhibiting reuptake 5-HT compared to other drugs blocking reuptake of NA

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28
Q

Atypical 5-Ht + NA reuptake inhibittor

A

they affect neurotransmitters in unique ways

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29
Q

seasonal depression treatment

A

exposure to a light source that emits the same wavelengths as sun

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30
Q

what are benzodiazepines used for

A

anxiety

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31
Q

true or false? anxiety is an adaptive system

A

True

32
Q

what anxiety is not normal

A

anxiety that goes past an effective point and triggered by normal situations in life

33
Q

what is anxiety states

A

combination of physical and mental manifestations. Are attacks or persisting state.

34
Q

extreme state of anxiety disorder

A

Panic disorder

35
Q

Core structure of benzodiazepines

A

1-4benzodiazepine

36
Q

major effects of benzo. (6)

A

anti-anxiety(hippocampus amygdalla), induce sleep(celebral cortex), anticonvulsant(cerebellum hippocampus), muscle relaxant(spinal cord cerebellum), impair memory formation(amnesia hippocampus cerebral cortex), abuse potential(midbrain dopamine)

37
Q

lethal to therapeutic window ratio of benzo

A

1000 so safe

38
Q

first benzo drug widely used

A

Diazepam

39
Q

what do stage fright people use instead

A

beta receptors blockers in ANS to prevent palpitations

40
Q

benzo drugs acts on which receptors

A

GABA A receptors

41
Q

first benzo in 1960

A

chlordiazepoxide

42
Q

pharmacodynamic of GABA neurotrans.

A

bind to its 2 binding sites on receptor (2 gaba). Channel opens and influx of Cl- ions. hyperpolarization and inhibitory post synaptic potential. inhibits many neurotrans like 5-HT, dopamine, noradrenaline which leads to effects of benzo like antianxiety and sedation

43
Q

pharmacodynamic of benzo

A

allosteric binding site (BDZ) on receptors different to gaba binding site. Facilitates binding of gaba to its site creating greater influx of chloride. so increases gaba activity gabaergic inhibition. binding by itself does nothing.

44
Q

true or false? different drugs act on same location of gaba receptor

A

False.

45
Q

GABA A subtypes and subunit

A

5 alpha subunits, each account for different effects of benzo and two subunits (synaptic and extrasynaptic)

46
Q

two main categories of subunit of gaba a receptors

A

synaptic (subsynaptic) alpha 1-3 and extrasynaptic alpha 4-6

47
Q

Gaba A receptor responsible for phasic inhibition

A

subsynaptic (synaptic) response

48
Q

true or false? Major site of action of benzo happens on extrasynaptic receptors

A

False. its synaptic

49
Q

tonic inhibition occurs where

A

Extrasynaptic receptor

50
Q

benzo effect on dose response curve

A

shifts curve to the left, use of benzo leads to higher effects with lower dose of gaba

51
Q

barbiturates effect on gaba

A

channel is open longer. Can open channel by itself so more powerful but more dangerous than benzo

52
Q

diffence between benzo and barb.

A

benzo: affects frequency, no direct action, safer and selective
barb: affect duration, direct action, not selective not safe

53
Q

which is easier to overdose benzo or barb

A

barb, benzo level off as concentration gets higher, barb is straight line so very lethal

54
Q

alpha unit of gaba a for sedation

A

alpha 1

55
Q

alpha unit of gaba a for anxiety

A

alpha 2

56
Q

dose response curve for agonist and antigonist of benzo binding site BDZ

A

agonist shifts to left and antagonist to right

57
Q

type of inverse agonists

A

beta-carbolines

58
Q

which will shift dose response curve more to right for benzo effects

A

inverse agonists

59
Q

GABA + benzo antagonist = ?

A

no effect normal curve, only block BDZ but not gaba

60
Q

GABA + benzo inverse agonist =?

A

reduced effects of gaba

61
Q

gaba + benzo agonist = ?

A

more effects of gaba

62
Q

new drugs acting on GABAergic transmition and act on different sites than benzo

A

Zolpidem

63
Q

drugs that act on GABA B receptor

A

presynaptic, G-coupled K channel in spinal cord for muscle relaxation

64
Q

absorption of benzo

A

highly absorbed orally, highly lipid soluble, goes quick to brain and peak in 1 hour

65
Q

metabolism of benzo

A

metabolized by CYP3A AND CYP2C19, have active intermediate with long half lives.
ex: diazepam or chlodiazepoxide metabolized into nordiazepam and the oxazepam

66
Q

half lives of benzo

A

very long because are converted to multiple intermediates

67
Q

old people and benzo dose

A

since low metabolism, careful doses to not overdose

68
Q

toxicity of benzo

A

low when alone, but high if combined with cns depressants

69
Q

name of benzo antagonist

A

flumazenil

70
Q

how does tolerance to benzo have an effect on tthee body

A

tolerance will cause changes reuptake of neurotrans, uptake of gaba

71
Q

withdrawal symptomps of benzo and duration (5)

A

anxiety, hallucinations, loss of coordination, restless leg syndrome, (seizures,coma, death). last a week

72
Q

withdrawal on REM sleep

A

benzo suppressed REM but withdrawal causes REM rebound so many nightmares

73
Q

insomnia treatment

A

short half life benzo

74
Q

non benzo drug for sedation

A

zolpidem

75
Q

How does Zolpidem work

A

only binds to a1, treats insomnia without changing REM sleep. binds next to BDZ site

Phar300 (18 decks)

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