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Pharm Test 2 > Anti-anxiety > Flashcards

Anti-anxiety Flashcards

1
Q

GABA receptor :
Barbituates

Rxs

A

Phenobarbital

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2
Q

Melatonin congener

A

Ramelteon ROZEREM

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3
Q

5-HT1a receptor agonist
(a1, a2, D2)

Rx

A

Non-sedative anxiolytic:

*Buspirone BUSPAR

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4
Q

Sedative hypnotics

Graded-dose response

A

Low dose - anxiolytic sedative

High dose - sleep/hypnosis

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5
Q

Benzos vs older (alcohol, barbituates, chloral hydrate)

A

Benzos = safer

Older - linear dose response curve

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6
Q

Anxiety Tx

Panic disorder

A

Antidepressants

Alprazolam XANAX

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7
Q

Anxiety Tx

Agoraphobia

A

Alprazolam, XANAX

ADDs

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8
Q

Sedative drugs

A
  • **BARBITUATES
  • **BENZODIAZEPINES
  • Antipsycs
  • Antidepressants
  • Antihistimines
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9
Q

GABAa Receptor

A
  • major inhibitory neurotrans in brain

* binding sites vary among drugs, some different from GABA site

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10
Q

Barbituates

Rx

A

Phenobarbital
Schedule III/IV

*many are sched II
ABUSE POTENTIAL FOR ALL

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11
Q

Barbituates + older

Mechanism

A

Up DURATION Gaba -mediated Cl flux

  • neuronal inhbition
  • at higher concentrations - DIRECTLY OPEN Gaba a Cl channel
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12
Q

Barbituates + older

Absorption

A

Phenobarb - longer

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13
Q

Barbituates + older

S.E.

A

High dose - CNS /respiratory depression

*Low T.E. - OD

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14
Q

Bartituates + older

Drug interactions

A

*+ ETOH = CNS depression

  • INDUCE Cyp enzymes
  • Dependence, addiction
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15
Q

Barbituates + Older sedatives

Uses

A
  • rarely used today
  • Anesthesia
  • seizures = Phenobarbital
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16
Q

Anxiety Tx

Social phobia

A

Clonazepam KLONOPIN

ADDs, B-blockers

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17
Q

Anxiety Tx

Generalized Anxiety Disorder

A

1st line - ADD

  • Buspirone BUSPAR
  • Benzos = short-term relief
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18
Q

Axiolytic

A

CUT ANXIETY

*not all anxiolytics are sedatives, treated w/ non-sedatives

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19
Q

Sedative-hypnotics

A
  • CNS depressants
  • sedative = calming effect
  • ideally - minimal effect on motor function or mental status
  • some hypnotics are NOT sedative
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20
Q

Benzos

Rx list

A
  • Alprazolam XANAX
  • Clonazepam KLONOPIN
  • Diazepam VALIUM
  • Midazolam VERSED
  • Triazolam HALCION
  • Rohypnol - date rape drug
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21
Q

Benzos

Receptor mechanism

A

Bind to Gaba a
Facilitate GABA Cl influx
NO DIRECT OPENING - need GABA present

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22
Q

Benzos

Full agonists

A

NOT DIRECT, NEED GABA
Diazepam VALIUM
Alprazolam XANAX
Zolpidem AMBIEN

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23
Q

Benzos

Inverse agonist

A

INHIBIT GABA OPENING
Experimental drugs
-induce anxiety, seizure

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24
Q

Bezos

Antagonists

A

Flumazenil

*Compete with full ags (benzo) + hypnotics (zolpidem AMBIEN) + inverse ags

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25
Q

Benzos

CNS effect

A

Sedation

  • higher dose - cognitive impairment
  • amnesia
  • anticonvulsant - clonazepam KLONOPIN, diazepam VALIUM)
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26
Q

Benzos

MSK effects

A

Relaxation - high dose

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27
Q

Benzos

Cardio effects

A

DOWN BP

UP HR

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28
Q

Benzos

Tolerance

A

Diminished w/ use
SAME ALL SEDATIVE-HYPNOTICS
*anxiolytic tolerance uncertain
*SHORT-TERM USE

29
Q

Benzos

Dependence

A

*Physiological dependence
Esp. Barbituates (sche 2-4)
*Less w/ benzos (sched 3-4)
*MORE w/ high dose/short onsent

Taper w/ chronic use

30
Q

Benzos

Absorption

A

*2-4 hours

*more rapid:
Midazolam  VERSED
Diazepam VALIUM
Alprazolam XANAX
Triazolam HALCION
31
Q

Benzos

Advantages

A
  • safe
  • antagonist availabe - flumazil ROMAZICON
  • flatter dose- response curve
  • no major Cyp interactions
  • long duration = 1x day
32
Q

Benzo

Toxicity

A
  • good - hi T.I.
  • no ETOH mixing
  • respiratory - COPD, Obstructive sleep apnea
33
Q

Flumenazil ROMAZICON

A
  • Competitive antagonist
  • Useful in OD, reverse after surgery
  • NOT against ETOH, Barbituates
  • can cause benzo withdrawal s/s
  • short duration, rapid onset
34
Q

Buspirone BUSPAR

Non-sedative anxiolytic

A
  • partial agonist CNS 5HT 1a receptor
  • no sedative, hypnotic, antiseziure, euphoric effecs
  • NOT for ACUTE anxiety, need 1 week
  • NOT for panic disorder
  • GOOD for GAD
35
Q

Buspirone BUSPAR
(Non-sedative anxiolytic)

Advantages

A

no tolerance, dependence, abuse

36
Q

BRAs

Mech

A

Bind to Bz binding site

  • subset of GABAa (w/ A1 subunit)
  • NO anxiolytic, anticonvulsant, muscle relaxant
  • warnings for zolpidem AMBIEN/ezopiclone LUNESTA
37
Q

BRAs

List

A

Zolpidem AMBIEN
Eszopiclone LUNESTA
Zaleplon SONATA

38
Q

BRAs

Advantages

A

Favorable kinetics (fast acting , short T 1/2)

UNFINISHED

39
Q

GABA receptor:
Benzos

Rxs

A 
Diazepam VALIUM
Triazolam HALCION
Alprazolam XANAX
Clonazepam KLONOPIN
Midazolam VERSED
40
Q

GABA receptor:
Benzo Receptor Agonists

Rxs

A

Zolpidem AMBIEN

Eszopiclone LUNESTA

41
Q

GABA receptor:
Benzo Receptor Blocker

Rxs

A

Flumazenil ROMAZICON

42
Q

Anxiety Tx

Social Phobia

A

Clonazepam KLONOPIN

Also SSRI, ADs

43
Q

Anxiety Tx

Generalized Anxiety Disorder (GAD)

A

Buspirone BUSPAR
Benzodiazepines

1st line: SSRI/SNRI

44
Q

Anxiety Tx

Simple Phobia

A

Buproprion WELLBUTRIN- long term
Benzos - short term

1st line - ADDs

45
Q

Anxiety Tx

Specific Phobias

A

Behavioral Therapy

46
Q

Benzo receptors require what subunit?

47
Q

Benzo receptors

a1 subunit =

A

Sedation

Amnesia

48
Q

Benzo receptors

a2/3 subunit =

A

Anxiolysis

Muscle relaxation

49
Q

Benzo receptors

a5 subunit =

A

Cognitive impairment

50
Q

Benzos

Respiratory effects

A
  • pulmonary disease - respiratory depression (kids)
  • NO w/ sleep apnea
  • Fatalities w/ CNS depressants (ETOH)
51
Q

Benzos

Anxiety Tx

A
  • Generalized Anxiety Disorder
  • situational anxiety
Alprazolam XANAX (panic disorders)
Diazepam VALIUM
52
Q

Benzos

Sleep Disorder Tx

A

Triazolam HALCION

53
Q

Benzos

Epilepsy Tx

A

Clonazepam KLONOPIN

Diazepam VALIUM

54
Q

Benzos

Anesthesia Tx

A

Midazolam VERSED

55
Q

Benzos

Neuro disorders - muscle rigidity

A

Clonazepam KLONOPIN

Diazepam VALIUM

56
Q

Benzo Absorption

Rapid CNS entry

A

More lipophilic

*Midazolam VERSED = anesthesia

  • alprazolam XANAX (ABUSE)
  • diazepam VALIUM (ABUSE)
57
Q

Benzo metabolism

A

Many converted to active metabolites

EXTEND t1/2 (50-100 hrs)

Urinary excretion

58
Q

Benzo use defined by

59
Q

Buspirone
(Non-sedative anxiolytic)

Disadvantages

A

*slow to act

60
Q

Buspirone BUSPAR
(Non-sedative anxiolytic)

Adverse effects

A

NO w/ MAOIs = UP too much serotonin downstream

Hyper cardio, nervousness

*prenancy-unknown

61
Q

Hypnotics effect on sleep

A

Less REM cycles
Withdraw = REM rebound

*Sleep patterns change with age

62
Q

Sleep disorder Tx

A

Ramelteon ROZAREM

  • MT1 + MT2 receptors
  • FDA approved - long term use
  • no sleep stage change/suppression

Antihistimines
Old sedative hypnotic (not today)
Benzos
BRAs (z drugs)

63
Q

Sleep disorder Tx

Benzos

A

*triazolam HALCION

Suppress REM/Deep sleep
Use= LESS than 3 weeks

64
Q

Rapid onset Benzos

A

Triazolam HALCION
Alprazolam XANAX
Diazepam VALIUM

65
Q

Short duration Benzos

A

Triazolam HALCION

Midazolam VERSED

66
Q

Intermediate Duration Benzos

A

Alprazolam XANAX

67
Q

Long duration Benzos

A

Diazepam VALIUM

Clonazepam KLONOPIN

68
Q

BRAs

Advantages (vs. Benzos)

A

*rapid onset, short t1/2
*Less REM suppression
*Less tolerance
eszopiclone LUNESTA= long term!
*Less dependence/abuse
Zolpidem AMBIEN = sched 4

Pharm Test 2 (13 decks)

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