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Pharm II Test 2 > Sedatives and Hypnotics > Flashcards

Sedatives and Hypnotics Flashcards

1
Q

Benzodiazepines- Available Drugs

A

diazepam
furazepam
clordiazepoxide

clonazepam
flunitrazepam

midazolam
alprazolam
triazolam

lorazepam
oxazepam
temazepam

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2
Q

Benzodiazepines- Mech of Action

A

Bind both BZ1 and BZ2
Non-selective agonist
Positive allosteric modulators of GABA receptors
increase frequency of Cl channel opening

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3
Q

Benzodiazepines- Absorption/Distribution

A

Lipid soluble (variable= different rates of absorption, onset, and redistribution)

Good bioavailability (60-100%)

High protein binding

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4
Q

Diazepam, Flurazepam, Clordiazepoxide- Elimination

A

VERY LONG HALF-LIVES
Have active metabolites
Phase I and Phase II metabolism

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5
Q

Clonazepam, Flunitrazepam- Elimination

A

Phase I and Phase II

Intermediate to long half lives

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6
Q

Midazolam, Alprazolam, Triazolam- Elimination

A

SHORT HALF LIVES

Phase I and Phase II

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7
Q

Lorazepam, Oxazepam, Temazepam- Elimination

A

INTERMEDIATE HALF LIVES
Phase II only

PREFERRED IN ELDERLY AND IMPAIRED HEPATIC FUNCTION DUE TO NO PHASE I ELIMINATION

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8
Q

Benzodiazepines- Clinical Use

A

Anxiolytic
Sedation
Some have anticonvulsant effects and are used as muscle relaxant adjuncts to anesthesia.
Short term treatment of insomnia (don’t use trizolam).

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9
Q

Benzodiazepines- Adverse Effects/Contraindications

A

CONFUSION

PARADOXICAL EXCITEMENT IN CHILDREN AND ELDERLY

PARADOXICAL RAGE REACTION
RAPID ONSET, HIGHER DOSE, SHORTER HALF LIFE, LONGER DURATION OF USE, AND HIGHER POTENCY ALL INCREASE SEVERITY OF DEPENDENCE AND WITHDRAWAL

lowerchance of extreme CNS depression and death, drowsiness, ataxia, anterograde amnesia, tolerance and dependence, withdrawals (anxiety, insomnia, irritability, muscle aches, tremor, loss of appetite, nausea, ataxia, hyperreflexia, blurred vision, fatigue; rarely confusion, delirium, psychosis, seizures, catatonia), rebound insomnia

Flunitrazepam- Rohypnol= date rape drug

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10
Q

Benzodiazepines- Drug Rxns

A

cross tolerance with EtOH and other sedative hypnotics

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11
Q

Imidazopyridines- Available Drugs

A

Zolpidem

Zaleplon

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12
Q

Imidazopyridines (Zolpidem, Zaleplon)- Mech of Action

A

Bind only the BZ1 site

Positive allosteric modulators of GABA receptor

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13
Q

Zolpidem- Absorption, Distribution

A

rapidly and completely absorbed PO

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14
Q

Zaleplon- Absorption, Distribution

A

rapidly absorbed

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15
Q

Zolpidem- Elimination

A

liver metabolism

short half-life

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16
Q

Zaleplon- Elimination

A

very short half life- even shorter than Zolpidem

hepatic metabolism

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17
Q

Zaleplon- Clinical Use

A

only for short term use for insomnia

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18
Q

Imidazopyridines (Zolpidem, Zaleplon)- Adverse Effects/Contraindications

A

Habit forming

Headache, dizziness, somnlence, nausea, vomiting, diarrhea, anterograde amnesia, rebound insomnia

sleep driving, sleep eating

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19
Q

Imidazopyridines (Zolpidem, Zaleplon)- Drug Rxns

A

Potentially fatal CNS depression when combined with other CNS depressants

Zaleplon= Metabolism is inhibited by cimetidine, an H2 histamine blocker

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20
Q

Pyrrolopyrazines- Available Drugs

A

Eszopiclone

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21
Q

Pyrrolopyrazines (Eszopiclone)- Mech of Action

A

Bind only the BZ1 site
Positive allosteric modulators of GABA receptor
S(+) isomer of Zopiclone

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22
Q

Pyrrolopyrazines (Eszopiclone)- Absorption, Distribution

A

rapid absorption

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23
Q

Pyrrolopyrazines (Eszopiclone)- Elimination

A

Short half life, but longer than Zolpidem and Zaleplon

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24
Q

Pyrrolopyrazines (Eszopiclone)- Clinical Use

A

sleep disorders (not restricted to short-term use)

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25
Q

Pyrrolopyrazines (Eszopiclone)- Adverse Effects/Contraindications

A

Habit forming

headache, dizziness, somnlence, nausea, vomiting, diarrhea, anterograde amnesia, rebound insomnia

sleep driving, sleep eating

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26
Q

Pyrrolopyrazines (Eszopiclone)- Drug Rxns

A

Cyp 3A4 inhibitor and inducers

Potentially fatal CNS depression when combined with other CNS depressants

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27
Q

Inverse Agonists- Available Drugs

A

Beta Carbanolines

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28
Q

Inverse Agonists (Beta Carbanolines)- Mech of Action

A

Bind same site as Benzos
Act as negative allosteric modulators of GABA receptor
Inverse agonist

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29
Q

Barbiturates- Available Drugs

A

Short-Acting-
Thiopental
Methohexital

Intermediate-
Amobarbital
SEcobarbital
Pentobarbital

Long-
Phenobarbital

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30
Q

Barbiturates- Mech of Action

A

bind sites on GABAa receptor distinct from BZ binding sites

No specificity for GABAa isoforms

Increases duration of Cl channel openings

Can directly open Cl channels at very high doses even in the absence of GABA. Enhances P450 enzymes= enhances its own metabolism, thus requires increasingly higher doses

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31
Q

Thiopental, Methohexital- Absorption, Distribution

A

rapid onset, short duration

32
Q

Thiopental, Methohexital- Elimination

A

short half life- hours

33
Q

Amobarbital, Secobarbital, Pentobarbital- Elimination

A

18-48 hours

34
Q

Phenobarbital- Elimination

A

4-5 day half life

35
Q

Thiopental, Methohexital- Clinical Use

A

Induction of Anesthesia

36
Q

Phenobarbital- Clinical Use

37
Q

Barbiturates- Adverse Effects/Contraindications

A 
LOW THERAPEUTIC INDEX
POTENTIAL TO DEPRESS RESPIRATION
DEPENDENCE
SEVERE WITHDRAWAL SYMPTOMS
TOLERANCE, CROSS TOLERANCE WITH OTHER SEDATIVES
38
Q

Barbiturates- Drug Rxns

A

Can decrease levels of other drugs because of P450 induction

39
Q

Neuroactive Steroids- Mech of Action

A

Bind sites on GABAa receptor distinct from BZ binding sites, increase teh effects of GABA

Can directly open Cl channels at very high doses

40
Q

Ramelteon- Mech of Action

A

High affinity MT1 and MT2 melatonin agonist

No effect on BZ receptors

41
Q

Ramelteon- Absorption, Distribution

A

Rapid absorption

Moderate protein binding

42
Q

Ramelteon- Elimination

A

Short half life
Extensive first pass metabolism
Metaboilzed by CYP 1A2, 2C9, 3A4

43
Q

Ramelteon- Clinical Use

A

sleep disorders

44
Q

Ramelteon- Adverse Effects/Contraindications

A

Same as placebo
Headache, somnolence, fatigue, dizziness, nausea, exacerbated insomnia
Caution in liver disease, sleep apnea, depression, suicidal, elderly.
No abuse potential

45
Q

Ramelteon- Drug Rxns

A

Metabolism may be increased by Rifampin (strong CYP inducer)

46
Q

EtOH- Mech of Action

A

Precise action unknown

Alter GABA neurotransmission

47
Q

Flumazenil- Mech of Action

A

Competitive antagonist at BZ1 and BZ2

Does NOT antagonize at the GABA binding site

48
Q

Flumazenil- Absorption, Distribution

A

act rapidly

49
Q

Flumazenil- Elimination

A

Short half-life

Hepatic metabolism

50
Q

Flumazenil- Clinical Use

A

treat benzo overdose

reverse benzo induced surgical sedation

51
Q

Flumazenil- Adverse Effects/Contraindications

A

can precipitate withdrawals in someone addicted to benzos

53
Q

TCAs- Available Drugs

A

Amitriptyline,
Doxepin,
Imipramine

54
Q

TCAs: Amitriptyline, Doxepin, Imipramine- Clinical Use

A

Sleep disorders associated with chronic pain syndromes (fibromyalgia)

55
Q

TCAs: Amitriptyline, Doxepin, Imipramine- Adverse Effects/Contraindications

A

Postural hypotension, cardiotoxicity, confusion with memory dysfunction

Contraindicated in elderly

56
Q

Atypical Antidepressants- Available Drugs

A

Mirtazapine
Trazadone
Nefazadone

57
Q

Mirtazapine- Mech of Action

A

Alpha2 antagonist

Blocks presynaptic receptors= increased release of NE and 5-HT

58
Q

Mirtazapine- Clinical Use

A

anxiolytic, antidepressant

highly sedating at low doses

59
Q

Mirtazapine- Adverse Effects/Contraindications

A

no sexual dysfunction, nausea, or GI problems

60
Q

Trazadone- Clinical Use

A

antidepressant, highly sedating= hypnotic

61
Q

Nefazadone- Mech of Action

A

5-HT2a antagonist

5-HT reuptake inhibitor

62
Q

Nefazadone- Clinical Use

A

mildly sedating

63
Q

Nefazadone- Adverse Effects/Contraindications

A

no sexual dysfunction

64
Q

Antihistamines- Available Drugs

A

cyclobenzaprine
hydroxyzine
diphenhydramine

65
Q

Cyclobenzaprine, Hydroxyzine, Diphenhydramine- Mech of Action

A

H-1 antagonist

66
Q

Cyclobenzaprine, Hydroxyzine, Diphenhydramine- Clinical Use

A

sleep disorders

67
Q

Non-Prescription Sleep Aids- Available Drugs

A

Compoz, Nytol, Sleep-Eze, Sominex, Unisom

68
Q

Compoz, Nytol, Sleep-Eze, Sominex, Unisom- Clinical Use

A

sleep disorders- no more effective than placebo

69
Q

Compoz, Nytol, Sleep-Eze, Sominex, Unisom- Adverse Effects/Contraindications

A

Produce tolerance and rebound insomnia- removed from shelves (except Unisom)

70
Q

Valeriana officinalis- Mech of Action

A

EtOH extract

Sesquiterpenes increase GABA release and inhibit GABA breakdown

71
Q

Valeriana officinalis- Clinical Use

72
Q

Valeriana officinalis- Adverse Effects/Contraindications

A

no next day hangover

73
Q

Chamomile (Apigenin)- Mech of Action

A

benzo agonist

74
Q

Chamomile (Apigenin)- Clinical Use

A

relaxation

75
Q

Kava- Mech of Action

A

facilitate binding of GABA

76
Q

Kava- Clinical Use

77
Q

Chrysin (passion flower)- Mech of Action

A

benzo partial agonist

78
Q

Chrysin (passion flower)- Clinical Use

Pharm II Test 2 (8 decks)

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