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CNS Pharma > Slides 4 > Flashcards

Slides 4 Flashcards

1
Q

What are Sedative-Hypnotic drugs?

A

Drugs which cause sedation with concomitant relief of anxiety or encourage sleep.

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2
Q

What is the drug classification of Sedative-Hypnotics?

A

Clinical rather than chemical, because these drugs have diverse chemical structure.

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3
Q

What is the function of a sedative (anxiolytic) agent?

A

Reduces anxiety and exerts a calming effect.

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4
Q

What is the function of a hypnotic agent?

A

Produces drowsiness and encourages the onset and maintenance of sleep.

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5
Q

Which agent involves more pronounced depression of the CNS and how?

A

Hypnotic agents; by increasing the dose.

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6
Q

What are the classifications of Sedative-Hypnotics?

A

1) Benzodiazepines
2) Barbiturates
3) Chloral hydrate

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7
Q

What are some examples of Benzodiazepines?

A

1) Diazepam
2) Chlordiazepoxide
3) Flurazepam
4) Oxazepam
5) Lorazepam
6) Nitrazepam
7) Triazolam
8) Alprazolam

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8
Q

What are some examples of Barbiturates?

A

1) Phenobarbital
2) Pentobarbital
3) Secobarbital
4) Thiopental

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9
Q

What are some new drugs for sleep disorders?

A

1) Zolpidem
2) Zaleplon
3) Eszopiclone

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10
Q

What is an example of a Melatonin receptor agonist (hypnotic)?

A

Ramelteon

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11
Q

What is an example of an Anxiolytic agent?

A

Buspirone

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12
Q

What does the absorption of sedative-hypnotic drugs after oral administration depend on?

A

Lipid solubility (Most are well absorbed)

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13
Q

What does the passage to CNS of sedative-hypnotic drugs depend on?

A

Lipid solubility (Rapid onset of action)

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14
Q

Which sedative-hypnotic drugs are highly lipid soluble?

A

1) Thiopental

2) Triazolam

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15
Q

Can sedative-hypnotic drugs cross the placental barrier? What happens if given before delivery?

A

Yes; they may depress neonatal vital functions

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16
Q

If sedative-hypnotic drugs are given to pregnant women, where can we detect them?

A

In breast milk = depressant effect on the infant

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17
Q

What is the main mechanism of elimination of most sedative-hypnotics?

A

Metabolic transformation

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18
Q

What accounts for the clearance of all benzodiazepines?

A

Hepatic metabolism

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19
Q

What is the path of metabolism for most sedative-hypnotics?

A

Oxidation by cytochrome P450 enzymes (CYP3A4), and subsequently conjugated to glucuronides that are excreted in urine.

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20
Q

Many products of oxidation of benzodiazepines are:

A

Pharmacologically active (some have longer half lives than the parent)

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21
Q

What is the half-life of desmethyldiazepam?

A

> 40 hours

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22
Q

What affects the metabolism of sedative-hypnotics?

A

Inhibitors and inducers of CYPs.

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23
Q

Which drug is conjugated directly?

A

Lorazepam

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24
Q

What is the metabolism pathway of barbiturates?

A

Mainly metabolized by oxidation pathways then conjugated.

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25
Q

Phenobarbital is -% excreted unchanged in urine, and its excretion is increased by:

A

20-30%; alkalinization of urine.

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26
Q

The rate of metabolism is usually __(fast/slow), with

__(long/short) elimination half-lives.

A

Slow; long

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27
Q

What is the half life of Secobarbital and pentobarbital?

A

18 - 48 hours.

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28
Q

What is the half life of Phenobarbital?

A

4-5 days.

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29
Q

Multiple dosing of Secobarbital, pentobarbital, and Phenobarbital can lead to:

A

Cumulative effects

30
Q

Zolpidem, Zaleplon, and Eszopiclone are metabolized to:

A

Inactive metabolites by CYP3A4

31
Q

Which drugs inhibit the metabolism of Zolpidem, Zaleplon, and Eszopiclone?

A

1) Cimetidine

2) Ketoconazole

32
Q

Which drug induces the metabolism of Zolpidem, Zaleplon, and Eszopiclone?

A

Rifampin

33
Q

What is GABA and where is it released from?

A

Inhibitory neurotransmitter; typically released from local interneurons.

34
Q

Where are Interneurons that release GABA found?

A

Throughout the CNS, including the spinal cord.

35
Q

GABA receptors are divided into 2 main types:

A

1) GABAA

2) GABAB

36
Q

IPSPs (inhibitory postsynaptic potentials) in the brain have a fast and a slow component. The fast component is mediated by __ receptors and the slow component by __ receptors

A

GABAA; GABAB

37
Q

GABAA receptors are __ receptors and are selectively permeable to __.

A

ionotropic; Cl-

38
Q

What are GABAA receptors selectively inhibited by?

A

Convulsants:

1) Picrotoxin
2) Bicuculline

39
Q

GABAB receptors are __ receptors and are selectively activated by __.

A

Metabotropic; Antispastic drug Baclofen

40
Q

GABAB receptors are coupled to __ that either inhibit __ or activate __.

A

G proteins; Ca2+ channels; K+ channels

41
Q

Which drugs bind GABAA receptors in neuronal membranes in CNS? What do they do?

A

1) Benzodiazepines
2) Barbiturates
3) Zolpidem
4) Zaleplon
5) Eszopiclone
6) Many other drugs;
Enhance effects, NOT agonists.

42
Q

Which drug’s binding site is different from all the other?

A

Barbiturates

43
Q

Where does the binding of benzodiazepines and the newer hypnotic drugs such as zolpidem occur?

A

A single site between α and γ subunits, facilitating the process of chloride ion channel opening.

44
Q

Which drug can bind at the same site as benzodiazepines and the newer hypnotic drugs such as zolpidem?

A

The benzodiazepine antagonist Flumazenil can reverse the hypnotic effects of zolpidem

45
Q

What do Barbiturates do?

A

Depress the actions of the excitatory neurotransmitters (glutamic acid), and exert nonsynaptic membrane effects.

46
Q

Why do we rarely use barbiturates?

A

They’re less selective than BDZs, and have a more pronounced central depressant action and a low margin of safety.

47
Q

What does Flumazenil do?

A

Blocks the action of benzodiazepines, eszopiclone, zaleplon, and zolpidem; but NOT barbiturates, meprobamate, or ethanol.

48
Q

What do β-Carbolins do?

A

1) Negative allosteric modulators (inverse agonists) of GABA-receptor function = anxiety and seizures.
2) Block the effects of BDZs.

49
Q

What are the organ system effects of sedative-hypnotic drugs?

A

1) Sedation
2) Hypnosis
3) Anesthesia
4) Anticonvulsant effects
5) Muscle relaxants
6) Respiratory depression
7) Cardiovascular depression

50
Q

How does sedation occur?

A

By depressant action on psychomotor and cognitive functions.

51
Q

What is sedation?

A

Calming effect with concomitant reduction of anxiety (at relatively low doses).

52
Q

Which drugs induce hypnosis?

A

All of the sedative-hypnotics induce sleep if enough doses are given.

53
Q

What happens if you use sedative-hypnotics for more than 1-2 weeks?

A

Tolerance to their effects on sleep patterns.

54
Q

What are the properties of Thiopental and methohexital?

A

1) Very lipid soluble
2) Penetrate brain tissue rapidly after IV administration
3) Useful for induction of anesthesia

55
Q

Why do Thiopental and methohexital have short durations of action?

A

Because of rapid tissue redistribution

56
Q

What can be used IV in anesthesia in combination with other drugs?

A

Benzodiazepines

57
Q

If benzodiazepines are used at large doses, what can happen and how can it be cured?

A

Postanesthetic respiratory depression (long t½ and active metabolites); Flumazenil

58
Q

How do sedatives-hypnotics have anticonvulsant effects?

A

By inhibiting the development and spread of epileptiform electrical activity in the CNS.

59
Q

What is the selectivity that happens with the anticonvulsant action of sedative-hypnotics?

A

It is not associated with marked CNS depression, but psychomotor function may be impaired.

60
Q

Which drugs are sufficiently selective to be used as

anticonvulsants (acutely)?

A

Several benzodiazepines:

1) Clonazepam
2) Nitrazepam
3) Lorazepam
4) Diazepam

61
Q

Which drug is effective in the management of generalized tonic-clonic seizures (long-term
use)?

A

Phenobarbital

62
Q

Which drugs lack anticonvulsant activity and why?

A

1) Zolpidem
2) Zaleplon
3) Eszopiclone;
Because of more selective binding to GABAA
receptor isoforms than that of benzodiazepines.

63
Q

Which drugs exert inhibitory effects on polysynaptic reflexes?

A

1) Meprobamate

2) Benzodiazepines

64
Q

Which drugs DON’T produce muscle relaxation?

A

1) Zolpidem
2) Zaleplon
3) Eszopiclone

65
Q

Respiratory depression is __, and can be:

A

Dose-related; the cause of death with overdose.

66
Q

Sedative-hypnotics, even at therapeutic doses, can produce significant respiratory depression in which patients?

A

Patients with pulmonary diseases.

67
Q

Respiratory effects are more marked after __ administration.

A

IV

68
Q

How can sedative-hypnotics depress the CVS?

A

By depressing the medullary vasomotor center in:

1) Hypovolemic states
2) When cardiac function is impaired

69
Q

What happens in the CVS with sedative-hypnotics overdose?

A

Myocardial contractility and

vascular tone may be depressed = circulatory collapse.

70
Q

Cardiovascular effects are more marked after __ administration.

A

IV

CNS Pharma (7 decks)

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