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Neuropharmacology & Neuroscience > Barbiturates and Benzodiazepines > Flashcards

Barbiturates and Benzodiazepines Flashcards

1
Q

Which compounds fuse to form barbituric acid?

A

Malonic acid and urea

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2
Q

What are all barbiturates derived from?

A

Barbituric acid

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3
Q

What are the three main classes of barbiturates?

A

Long-acting, short-acting and very-short-acting

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4
Q

Which receptor do barbiturates act on?

A

GABAa

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5
Q

What are the effects of barbiturates?

A

Antioxylitic, sedative, relaxant, analgesics and anticonulsant

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6
Q

What are some issues with barbiturates?

A

Pharmacological tolerance and behavioural dependence

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7
Q

Name very-short-acting barbiturates

A

Thiopentone and Sodium Pentothal

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8
Q

Name short-acting barbiturates

A

Pentobarbitone

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9
Q

Name long-acting barbiturates

A

Barbitone and Phenobarbitone

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10
Q

What are the two classes of benzodiazepines

A

Short and long-acting

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11
Q

What makes a short-acting BZ?

A

The metabolite of the drug is inactive

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12
Q

What makes a long-acting BZ?

A

Only the metabolite is active

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13
Q

What are some effects of BZs?

A

Antioxylitic, sedative, relaxant and anticonvulsant

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14
Q

Which is used clinically more commonly out of barbiturates and BZs?

A

BZs have a (relative to barbiturates) high therapeutic index

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15
Q

What are some key issues with BZs?

A

Tolerance and behavioural and physiological dependence

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16
Q

5HTa agonists are useful in treating what?

A

anxiety

17
Q

What are some benefits of using 5HTa agonists as anxiolytics over BZs?

A

They are less effective but result in fewer side effects (little drowsiness, nausea, headache, restlessness)

18
Q

Name a 5HTa agonist

A

Azapirone

19
Q

Name a 5HTa partial agonist

A

Buspirone

20
Q

What do barbiturates and BZs bind to?

A

An allosteric site on GABAa and GABAb

21
Q

What do the drugs do when they bind to GABAa allosteric site?

A

They increase the frequency of the GABA Cl-channel opening

22
Q

What do drugs do when they bind to GABAb?

A

Via GPCR Gi, they inhibit AC and facilitate GABA channels opening

23
Q

Where is the BZ binding site on GABA channels?

A

Between the alpha-1 and gamma-2 subunits

24
Q

Where is the barbiturate binding site on GABA channels?

A

On the top and between alpha-1 and beta-2/3 subunits

25
Q

Where is the GABA binding site?

A

Between the alpha-1 and beta-2/3 subunits, but closer to the membrane

26
Q

Do drugs show GABA subunit selectivity?

A

Yes. This makes them desirable drug targets

27
Q

Drugs targeting alpha-1 subunit usually result in which effects?

A

Sedative effects

28
Q

Drugs targeting alpha-2 subunit usually result in which effects?

A

Anxiolytic effects

29
Q

How do BZs most commonly affect the GABA channels?

A

Increase frequency of opening

30
Q

How do barbiturates most commonly affect the GABA channels?

A

Increase the open time of the channel

31
Q

How does propofol affect GABAergic transmission?

A

It enhances by acting on allosteric sites and acting directly on the main binding site

32
Q

Name a BZ agonist drug

A

Diazepam

33
Q

Name a BZ partial agonist drug

A

Ro 15-1788

34
Q

Name a BZ competitive antagonist

A

Flumazenil

35
Q

Name a BZ partial inverse agonist

A

FG 7142

36
Q

Name a BZ inverse agonist

A

Beta-carbolines

37
Q

How does a BZ agonist induce an effect in the precoupled ON state?

A

Increases GABA receptors affinity which increases the open time of the Cl- channel, which increases the intrinsic agonist

38
Q

How does a BZ inverse agonist induce an effect in the unprecoupled state?

A

Keeps a receptor in the ‘off’ state which reduces the intrinsic efficacy

Neuropharmacology & Neuroscience (10 decks)

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