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DATB > elm 10.2 > Flashcards

elm 10.2 Flashcards

1
Q

what are some derivatives of barbiturates?

A

amobarbital
pentobarbital
thiopental
phenobarbital

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2
Q

what are some historical uses of barbiturates?

A

anxiolytics
anticonvulsants
sedatives/hypnotics
anaesthetics

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3
Q

barbiturates are positive ____ modulators of ____ receptors - they ____ the open time.

A

allosteric
GABAA
prolong

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4
Q

at higher concentrations, barbiturates can directly _____ the receptor

A

activate

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5
Q

barbiturates may also _____ AMPA receptors, ___ type VSCC (to inhibit ___ release)

A

inhibit
P/Q
NT

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6
Q

thiopental is an ___ agent in general anaesthesia

A

induction

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7
Q

thiopental can also be used in ___ when the seizure hasn’t responded to ___ or ____

A

status epileptus
benzodiazepines
anti-convulsants

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8
Q

benzodiazepines are ______ allosteric modulators of the ____ receptor

A

positive
GABAA

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9
Q

benzodiazepines are used as anxiolytics t or f

A

t

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10
Q

GABA binding sites are formed at the interfaces of _____

A

beta

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11
Q

high affinity BDZ binding requires a ___ subunit

A

gamma2

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12
Q

what are some compounds that enhance GABAA receptor function

A

anxiolytic, sedative, muscle relaxant, amnesic, anticonvulsant

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13
Q

what are some compounds that decrease GABAA receptor function

A

convulsants

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14
Q

flumazenil is a benzodiazepine ____, which competes with agonists for the same binding site, but it is pharmacologically fairly ______. it is used to reverse _____

A

antagonist
inactive
BDZ sedation

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15
Q

benzodiazepine inverse agonists - beta carbolines act at the same site as ______, and they ___ channel opening frequency

A

flunitrazepam
decrease

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16
Q

high affinity is associated with type ____ benzodiazepine binding sites

A

I

17
Q

low affinity is associated with type ____ benzodiazepine binding sites

A

II

18
Q

what are two examples of early anxioselective BDZ ligands?

A

bretazenil
alpidem, ocinaplon

19
Q

what are 4 examples of behavioural tests

A

elevated plus maze
vogel water-lick conflict test
rotorod test
morris water maze

20
Q

what is the strategy for knockout studies

A

eliminate individual subunits from genome and to see if this alters sedative or anxiolytic properties of BDZs

21
Q

which subunit is related to cerebellar expression?

A

alpha 6

22
Q

which subunits are related to perinatally lethal ?

A

beta 3
gamma 2

23
Q

alpha one is type __

A

I

24
Q

alpha 2,3,5 is related to type __

A

II

25
Q

alpha 4,6 is realted to

A

high affinity

26
Q

mutation conserved alpha His to Arg in BDZ site leads to what

A

complete loss of classic BDZ binding

27
Q

knock in is what

A

in vivo replacement of single amino acid in a defined gene

28
Q

sedative, amnesic actions are

A

alpha 1

29
Q

anxiolytic actions are

A

alpha 2

30
Q

alpha 1 selective drugs would give you what

A

sleeping tablets

31
Q

alpha 2 selective drugs give you what

A

anti anxiety without sedation

32
Q

Which of the following barbiturates has been frequently used as an ingredient of lethal injections?

a.	 Amobarbital

b.	 Barbital

c.	 Phenobarbital

d.	 Thiopental
A

d

33
Q

Which subunit of the GABAA receptor contains the primary binding site for the barbiturates?

a.	 Alpha

b.	 Beta

c.	 Delta

d.	 Gamma 2
A

b

34
Q

The main current clinical uses of barbiturates are as:

a.	 Anxiolytics and sedatives

b.	 Anticonvulsants and anaesthetics (induction agents)

c.	 Anxiolytics and anticonvulsants

d.	 Muscle relaxants and anaesthesia (induction agents)
A

b

35
Q

Which alpha subunits confer high affinity binding for diazepam when they form a benzodiazepine binding site with the gamma 2 subunit?

a.	 1,2,3,5

b.	 1,2,4,6

c.	 2,4,5,6

d.	 3,4,5,6
A

a

36
Q

Flumazenil is a _____________ of the GABAA receptor

a.	 negative allosteric modulator

b.	 non-competitive antagonist

c.	 positive allosteric modulator

d.	 silent allosteric modulator
A

d

37
Q

Which residue in alphas 1,2,3,5 confers high affinity binding for diazepam?

a.	 G153

b.	 H105

c.	 R105

d.	 Y90
A

b

38
Q

Which of the following tests can be used to measure the amnesic actions of benzodiazepines?

a.	 Elevated plus maze

b.	 Morris water maze

c.	 Rotorod test

d.	 Vogel water lick conflict test
A

b

DATB (24 decks)

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