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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
Pyrrolopyrazines (Eszopiclone)- Adverse Effects/Contraindications
Habit forming headache, dizziness, somnlence, nausea, vomiting, diarrhea, anterograde amnesia, rebound insomnia sleep driving, sleep eating
26
Pyrrolopyrazines (Eszopiclone)- Drug Rxns
Cyp 3A4 inhibitor and inducers | Potentially fatal CNS depression when combined with other CNS depressants
27
Inverse Agonists- Available Drugs
Beta Carbanolines
28
Inverse Agonists (Beta Carbanolines)- Mech of Action
Bind same site as Benzos Act as negative allosteric modulators of GABA receptor Inverse agonist
29
Barbiturates- Available Drugs
Short-Acting- Thiopental Methohexital Intermediate- Amobarbital SEcobarbital Pentobarbital Long- Phenobarbital
30
Barbiturates- Mech of Action
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
31
Thiopental, Methohexital- Absorption, Distribution
rapid onset, short duration
32
Thiopental, Methohexital- Elimination
short half life- hours
33
Amobarbital, Secobarbital, Pentobarbital- Elimination
18-48 hours
34
Phenobarbital- Elimination
4-5 day half life
35
Thiopental, Methohexital- Clinical Use
Induction of Anesthesia
36
Phenobarbital- Clinical Use
Epilepsy
37
Barbiturates- Adverse Effects/Contraindications
``` LOW THERAPEUTIC INDEX POTENTIAL TO DEPRESS RESPIRATION DEPENDENCE SEVERE WITHDRAWAL SYMPTOMS TOLERANCE, CROSS TOLERANCE WITH OTHER SEDATIVES ```
38
Barbiturates- Drug Rxns
Can decrease levels of other drugs because of P450 induction
39
Neuroactive Steroids- Mech of Action
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
Ramelteon- Mech of Action
High affinity MT1 and MT2 melatonin agonist No effect on BZ receptors
41
Ramelteon- Absorption, Distribution
Rapid absorption | Moderate protein binding
42
Ramelteon- Elimination
Short half life Extensive first pass metabolism Metaboilzed by CYP 1A2, 2C9, 3A4
43
Ramelteon- Clinical Use
sleep disorders
44
Ramelteon- Adverse Effects/Contraindications
Same as placebo Headache, somnolence, fatigue, dizziness, nausea, exacerbated insomnia Caution in liver disease, sleep apnea, depression, suicidal, elderly. No abuse potential
45
Ramelteon- Drug Rxns
Metabolism may be increased by Rifampin (strong CYP inducer)
46
EtOH- Mech of Action
Precise action unknown | Alter GABA neurotransmission
47
Flumazenil- Mech of Action
Competitive antagonist at BZ1 and BZ2 | Does NOT antagonize at the GABA binding site
48
Flumazenil- Absorption, Distribution
act rapidly
49
Flumazenil- Elimination
Short half-life | Hepatic metabolism
50
Flumazenil- Clinical Use
treat benzo overdose | reverse benzo induced surgical sedation
51
Flumazenil- Adverse Effects/Contraindications
can precipitate withdrawals in someone addicted to benzos
53
TCAs- Available Drugs
Amitriptyline, Doxepin, Imipramine
54
TCAs: Amitriptyline, Doxepin, Imipramine- Clinical Use
Sleep disorders associated with chronic pain syndromes (fibromyalgia)
55
TCAs: Amitriptyline, Doxepin, Imipramine- Adverse Effects/Contraindications
Postural hypotension, cardiotoxicity, confusion with memory dysfunction Contraindicated in elderly
56
Atypical Antidepressants- Available Drugs
Mirtazapine Trazadone Nefazadone
57
Mirtazapine- Mech of Action
Alpha2 antagonist | Blocks presynaptic receptors= increased release of NE and 5-HT
58
Mirtazapine- Clinical Use
anxiolytic, antidepressant | highly sedating at low doses
59
Mirtazapine- Adverse Effects/Contraindications
no sexual dysfunction, nausea, or GI problems
60
Trazadone- Clinical Use
antidepressant, highly sedating= hypnotic
61
Nefazadone- Mech of Action
5-HT2a antagonist | 5-HT reuptake inhibitor
62
Nefazadone- Clinical Use
mildly sedating
63
Nefazadone- Adverse Effects/Contraindications
no sexual dysfunction
64
Antihistamines- Available Drugs
cyclobenzaprine hydroxyzine diphenhydramine
65
Cyclobenzaprine, Hydroxyzine, Diphenhydramine- Mech of Action
H-1 antagonist
66
Cyclobenzaprine, Hydroxyzine, Diphenhydramine- Clinical Use
sleep disorders
67
Non-Prescription Sleep Aids- Available Drugs
Compoz, Nytol, Sleep-Eze, Sominex, Unisom
68
Compoz, Nytol, Sleep-Eze, Sominex, Unisom- Clinical Use
sleep disorders- no more effective than placebo
69
Compoz, Nytol, Sleep-Eze, Sominex, Unisom- Adverse Effects/Contraindications
Produce tolerance and rebound insomnia- removed from shelves (except Unisom)
70
Valeriana officinalis- Mech of Action
EtOH extract | Sesquiterpenes increase GABA release and inhibit GABA breakdown
71
Valeriana officinalis- Clinical Use
Hypnotic
72
Valeriana officinalis- Adverse Effects/Contraindications
no next day hangover
73
Chamomile (Apigenin)- Mech of Action
benzo agonist
74
Chamomile (Apigenin)- Clinical Use
relaxation
75
Kava- Mech of Action
facilitate binding of GABA
76
Kava- Clinical Use
calming
77
Chrysin (passion flower)- Mech of Action
benzo partial agonist
78
Chrysin (passion flower)- Clinical Use
Hypnotic

Pharm II Test 2 (8 decks)

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