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Psychology- Pharm > Sedatives/Hypnotics > Flashcards

Sedatives/Hypnotics Flashcards

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1
Q

What determines the effect of a sedative/hypnotic?

A

Dose

Increasing dose –> increased sedation up to coma/death

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2
Q

Which class of sedatives tapers off in effect with dose?

A

Benzodiazepines

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3
Q

Which class of sedatives continues to increase sedative effects with dosage?

A

Barbiturates

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4
Q

What type of receptors are GABA-A receptors?

A

Ionotropic

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5
Q

How do GABA A receptors work?

A

GABA binding increases the chloride channel opening, leading to an inhibitory post-synaptic potential, hyperpolarization and decreased neuron firing

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6
Q

Which GABA receptor is bound by sedative hypnotics?

A

GABA-A - they modulate the receptor

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7
Q

Describe the basic structure of the GABA-A receptor

A

5 subunits assemble to form a hetero-pentameric glycoprotein receptor

7 polypeptide classes –> multiple isoforms
Each polypeptide has 4 transmembrane loops

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8
Q

WHat three isoforms of the gaba polypeptide are required to form a functional GABA-a receptor?

A

alpha, beta and gamma

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9
Q

What is the composition of the most common GABA-a receptor?

A

two alpha
two beta
one gamma

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10
Q

Which GABA-a subunit isoform determines ability to be modulated by benzos, imidazopyradine and pyrrolopyrazines?

A

alpha subunit isoform

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11
Q

WHich interface is the pharmacore that binds the GABA

A

alpha/beta interface

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12
Q

Which is the allosteric modulatory site responsible for binding benzodiazapines, imidizopyridines and pyrrolopyrazines?

A

alpha/gamma

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13
Q

Which sites are bound by benzodiazepines?

A

BZ1 (alpha1) and BZ2 (alpha2)

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14
Q

What type of ligands are benzodiazepines and non-benzodiazepine agonists?

A

Positive allosteric modulators- they require GABA binding as well for the receptor to open the chloride channel

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15
Q

Do benzodiazepines increase frequency or duration of Cl- channel opening?

A

Increase frequency

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16
Q

How do barbiturates affect chloride channel opening?

A

Increase duration

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17
Q

Where do neuroactive steroids bind on GABA-A receptors? What is their effect?

A

They bind receptors not containing BZ1 or BZ2 receptor sites

They can facilitate or attenuate GABAergic transmission depending on structure

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18
Q

WHat do we have to be concerned with when mixing ethanol and barbiturates/benzos?

A

Ethanol can potentiate the effects of other GABAa receptor modulators

They target a very different part of the receptor -> potentiation of effects

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19
Q

Which class of drugs is safer- benzodiazepines or barbiturates?

A

Benzodiazepines- their dose effects taper out with limited capacity for producing potentially fatal CNS depression

Concerns only with polypharmacy and other respiratory problems

20
Q

Describe the protein binding of benzos in the blood

A

very good: 60-100%.

Potentially knocked off by other highly protein bound drugs

21
Q

Describe the metabolism of benzodiazepines:

A

Phase I: oxidation by P450 family CYP3A4 and CYP2C19

Phase II: Conjugation –> urinary excretion

22
Q

Which three benzodiazepines are metabolized directly by phase II?

A

LOT;

Lorazepam
Oxazepam
Temazepam

23
Q

Why does it take so long for the sedative effects of a benzodiazepine to wear off?

A

Long half lives

Long half lives of active metabolite

24
Q

What are common side effects of benzodiazepines?

A

drowsiness, ataxia, amnesia

25
Q

What puts you at risk for psychological dependence on benzodiazepines?

A

Long-term use, high doses

26
Q

What two effects of benzodiazepines do not develop tolerance?

A

Anxiolytic and muscle relaxant effects do not develop tolerance

27
Q

How does a drug’s half life affect its risk of tolerance and dependence?

A

Shorter half life –> increased risk

28
Q

How does a drug’s time to onset affect its risk of tolerance and dependence?

A

Shorter time to onset –> increased risk

Route of administration can have a major effect

29
Q

How does a drug’s potency affect its risk of tolerance and dependence?

A

HIgher potency, higher risk

30
Q

How does a drug’s dose affect its risk of tolerance and dependence?

A

increased dose, increased risk

31
Q

How does a drug’s length of time taken affect its risk of tolerance and dependence?

A

Longer time, greater risk

32
Q

Name three BZ1 site-selective non-benzodiazepines.

A

Zolpidem
Zaleplon
Eszopiclone

33
Q

Which two BZ1 site-selective benzos are imidazopyridines?

A

Zolpidem

Zaleplom

34
Q

Which BZ1 site-selective drug is a pyrrolopyrazine?

A

Eszopiclone

35
Q

What is the risk of dependence of BZ1 site-specific agonists compared to benzos?

Are they habit forming?

A

Decreased risk of tolerance

Long term use –> habit forming

36
Q

Can overdose with BZ1 site specific agonists be lethal?

A

Overdose does not produce dangerous CNS depression but can be lethal when taken with other CNS depressants

37
Q

What are weird/dangerous side effects associated with BZ1 site-specific agonists?

A

Sleep-driving and sleep-eating

38
Q

What is the metabolism of the three BZ-1 specific agonists?

A

Phase I and II in the liver

39
Q

What are the comparative half lives of the BZ-1 specific agonists?

A

short (1-3 hours) for the immidazopryidines

Longer (6 hours) for the pyrrolopyrazine (Eszopiclone)

40
Q

Name the three barbiturates

A

Phenobarbital
Methohexital
Thiopental

41
Q

What is the MOA of barbiturates?

A

Binds to ionotropic GABA-a receptors at regions distinct from BZ1 and BZ2 sites

Likely binds to lipophilic portions of the beta subunits

42
Q

Differentiate low dose from high dose barbiturate binding effects

A

Low dose: binding increases duration of Cl- channel opening

High dose; directly activates chloride channel opening, independent of GABA –> no ceiling effect of CNS depression

43
Q

Compare the half-lives of phenobarbital, thiopental and methohexital

A

Thiopental and methohexital- short acting

Phenobarbital- long acting

44
Q

Describe the withdrawal associated with barbiturate use

A

Discontinuation after repeated use may lead to life-threatening withdrawal that is very difficult to treat

45
Q

What are the clinical uses of barbiturates?

A

Limited..

46
Q

How does Ramelteon work?

A

Melatonin agonist - selectively binds to MT1 and MT2 melatonin receptors

Psychology- Pharm (7 decks)

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