Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology > Intro to CNS drugs and Hypnotics > Flashcards

Intro to CNS drugs and Hypnotics Flashcards

1
Q

Areas in BBB not fully developed

A
  1. Area postrema -vomiting

2. Hypothalamus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Early classes of antihistamines

A

diphenhydramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

later classes of antihistamines

A

Levocetirizine -less lipophilic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Dopamine is very polar so it cannot get through the BBB

A

There are receptors that allow molecules tthat are polar to get into the brain by tricking and by making the molecule look like an amino acid . L dopa is tricking the body to incorporate it into CNS… L-dopa decarboxylase , when L dopa enters, it gets decarboxylated to getit in to the BBB .

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

80-90 % of receptors of CNS drugs focus on proteins of what happens in the synapse other will focus on

A

propagation of action potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Epilepsy and local anesthesia are targeted by drugs that

A

Focus on act pot propagation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Treatment of epilepsy , which type of ion channel

A

voltage gatedm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Known influx of sodium, efflux of potassium, influx of chloride

A

depol-Na in
hyper pol-K out
hyper pol -Cl in

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Ligand gated ion channel are expressed in

A

pre and post synaptic neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Two ligand gated ion channels

A
  1. GABA-A receptors

2. Nicotinic receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

GABA-A

A

inhibitory due to it being a chloride ion channel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Nicotinic receptor is

A

excitatory -triggers rerelease of sodium and calcium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Metabotropic receptors have no

A

ion pores

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Metabotropic receptors affect opening of voltage gates channels by two mechanisms

A
  1. Causing the beta gamma subunits to open up (adrenoreceptors)
  2. Second messengers causes opening of voltage gated ion channels. (DAG, cAMP- these activate kinases to phosphorylate the proteins of ion channels.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

IPSP

A

Cl influx

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

EPSP

A

Na Ca influx

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

When affecting how NT are produced and excreted we can use drugs that are

A

analogues to certain molecules - these molecules can either increase secretion, synthesis, storage, release.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

NT are synth in the

A

presynaptic and stored in vesicles that can degranulate using a calcium dependent mechanism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Limitations with NT are

A

releasing more than what is produced (amphetamines over stimulation)

Not all NT that are released bind to receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Ach broken down by

A

Ach-esterase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Ach is recycled by

A

inhibiting Ach esterase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Amino acid derivative to know (excitatory)

A

Glutamate- main excitatory NT in brain– epilepsy drugs block glutamate

Ach -ionotropic ,nicotinic receptors -in flux of Ca Na
and Muscarinic receptor is metabotropic.

23
Q

Receptors for glutamate

A

Two ionotropic which are NMDR, AMPAR.

One metabotropic which is mGluR

24
Q

Amino acid derivative to know (inhibitory)

A

GABA-A -main inhibitory - If stimulated will treat anxiety, insomnia

Glycine

25
Q

GABA-A receptor

A

ionotropic -5 subunits -allows Cl influx

26
Q

Monoamine NT

A

Dopamine
Serotonin
Norepi
Histamine

27
Q

Neuropeptide NT

A 
Substance P
Endorphins 
Somatostatin
Neurotensin
Orexin

*Anandamide- binds to CB1 and CB2 -natural endocannabinoid

28
Q

First drugs used in the 20s, 30s, 40s, had a very narrow therapeutic index. This means there was a narrow range b/t

A

desired effect and toxic dose

29
Q

Used to treat epilepsy as a last resort when other treatments aren’t working?

A

Phenobarbitial

30
Q

Old gen barbiturates

A

Phenobarbital , pentobarbital, thiopental, glutethimide, chloral hydrate

31
Q

Features of benzos

A

benzene ring .. long carbon chain.. halogenated

32
Q

Benzos discussed in class

A

diazepam , chlordiazepoxide, flurazepam,, flunitrazepam..triazolam,, alprazolam

33
Q

New generation or Z hypnotic

A

zolpidem, zalepon, eszopiclone

34
Q

Benzo, barb, Z-hyp, all interact with

A

GABA-A

35
Q

These drugs mimic the effects of melatonin

A

Ramelteon… Tasimelteon

36
Q

Used to treat depression. Partial agonist of serotonin, used as anxiolytic, safer option.

A

Buspirone.

37
Q

These CNS lipophilic molecules go through rapid

A

redistribution –distributed fast to other organs to be excreted from the body

38
Q

Barbituates can

A

self stimulate their own metabolism –due to this , they may effect other drugs such as oral contraceptives.

39
Q

Benzos can also

A

self stimulate their own metabolism, and can form active metabolites . Caution with liver.

40
Q

Easy overdose with

A

barbiturates

41
Q

Speeding up excretion of these molecules such as barbiturates can be done by

A

giving sodium bicarb because the barbiturates are weak acids.

42
Q

Drugs that affect GABA-A don’t bind to

A

GABA-A

43
Q

GABA sub unit for GABA binding is

A

b/t alpha and beta subunit

44
Q

Benzos and Z-hyp bind where

A

to a pocket b/t alpha and gamma subunit. Referred to as benzodiazepine receptors

45
Q

Barbiturates bind to

A

to more lipophilic AA residues within the membrane

46
Q

Antidote to Z-hyp and benzos

A

Flumazeril

47
Q

Name the alpha 1 receptors

A

alpha 1,2,3,5,

48
Q

Benzos bind to which alpha receptors

A

1,2,3,5

49
Q

Z-hyp bind to which alpha receptors

A

1

50
Q

alpha 1 receptor is involved in

A

hypnosis

51
Q

Why is a Z-hyp not used for anesthesia

A

only binds to alpha 1 which is involved in hypnosis

52
Q

Benzos can cause

A

anterograde amnesia - loss of men after given drug

53
Q

Tolerance can come about two ways

A
  1. Pharmokinetic mechanism - body speeds up and speeds up metabolism requiring higher and higher dose.
  2. Pharmodynamic- overstimulation of NT receptors leads to decrease number of receptors, so dose muse be increased to get the same effect.
54
Q

Two orexin receptors antagonist 1.

Mechanism 2.

A

almorexant and suvorexant -1.

These are antagonist of the orexin receptors which is involved the stimulation of wakefulness, so inhibition would give a hypnotic effect.

Pharmacology (20 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions