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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
Benzos CNS effect
Sedation * higher dose - cognitive impairment * amnesia * anticonvulsant - clonazepam KLONOPIN, diazepam VALIUM)
26
Benzos MSK effects
Relaxation - high dose
27
Benzos Cardio effects
DOWN BP | UP HR
28
Benzos Tolerance
Diminished w/ use SAME ALL SEDATIVE-HYPNOTICS *anxiolytic tolerance uncertain *SHORT-TERM USE
29
Benzos Dependence
*Physiological dependence Esp. Barbituates (sche 2-4) *Less w/ benzos (sched 3-4) *MORE w/ high dose/short onsent Taper w/ chronic use
30
Benzos Absorption
*2-4 hours ``` *more rapid: Midazolam VERSED Diazepam VALIUM Alprazolam XANAX Triazolam HALCION ```
31
Benzos Advantages
* safe * antagonist availabe - flumazil ROMAZICON * flatter dose- response curve * no major Cyp interactions * long duration = 1x day
32
Benzo Toxicity
* good - hi T.I. * no ETOH mixing * respiratory - COPD, Obstructive sleep apnea
33
Flumenazil ROMAZICON
* Competitive antagonist * Useful in OD, reverse after surgery * NOT against ETOH, Barbituates * can cause benzo withdrawal s/s * short duration, rapid onset
34
Buspirone BUSPAR | Non-sedative anxiolytic
- 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
Buspirone BUSPAR (Non-sedative anxiolytic) Advantages
no tolerance, dependence, abuse
36
BRAs Mech
Bind to Bz binding site - subset of GABAa (w/ A1 subunit) * NO anxiolytic, anticonvulsant, muscle relaxant * warnings for zolpidem AMBIEN/ezopiclone LUNESTA
37
BRAs List
Zolpidem AMBIEN Eszopiclone LUNESTA Zaleplon SONATA
38
BRAs Advantages
Favorable kinetics (fast acting , short T 1/2) UNFINISHED
39
GABA receptor: Benzos Rxs
``` Diazepam VALIUM Triazolam HALCION Alprazolam XANAX Clonazepam KLONOPIN Midazolam VERSED ```
40
GABA receptor: Benzo Receptor Agonists Rxs
Zolpidem AMBIEN | Eszopiclone LUNESTA
41
GABA receptor: Benzo Receptor Blocker Rxs
Flumazenil ROMAZICON
42
Anxiety Tx Social Phobia
Clonazepam KLONOPIN | Also SSRI, ADs
43
Anxiety Tx Generalized Anxiety Disorder (GAD)
Buspirone BUSPAR Benzodiazepines 1st line: SSRI/SNRI
44
Anxiety Tx Simple Phobia
Buproprion WELLBUTRIN- long term Benzos - short term 1st line - ADDs
45
Anxiety Tx Specific Phobias
Behavioral Therapy
46
Benzo receptors require what subunit?
Gamma
47
Benzo receptors a1 subunit =
Sedation Amnesia
48
Benzo receptors a2/3 subunit =
Anxiolysis Muscle relaxation
49
Benzo receptors a5 subunit =
Cognitive impairment
50
Benzos Respiratory effects
* pulmonary disease - respiratory depression (kids) * NO w/ sleep apnea * Fatalities w/ CNS depressants (ETOH)
51
Benzos Anxiety Tx
* Generalized Anxiety Disorder * situational anxiety ``` Alprazolam XANAX (panic disorders) Diazepam VALIUM ```
52
Benzos Sleep Disorder Tx
Triazolam HALCION
53
Benzos Epilepsy Tx
Clonazepam KLONOPIN | Diazepam VALIUM
54
Benzos Anesthesia Tx
Midazolam VERSED
55
Benzos Neuro disorders - muscle rigidity
Clonazepam KLONOPIN | Diazepam VALIUM
56
Benzo Absorption Rapid CNS entry
More lipophilic *Midazolam VERSED = anesthesia * alprazolam XANAX (ABUSE) * diazepam VALIUM (ABUSE)
57
Benzo metabolism
Many converted to active metabolites EXTEND t1/2 (50-100 hrs) Urinary excretion
58
Benzo use defined by
t 1/2
59
Buspirone (Non-sedative anxiolytic) Disadvantages
*slow to act
60
Buspirone BUSPAR (Non-sedative anxiolytic) Adverse effects
NO w/ MAOIs = UP too much serotonin downstream Hyper cardio, nervousness *prenancy-unknown
61
Hypnotics effect on sleep
Less REM cycles Withdraw = REM rebound *Sleep patterns change with age
62
Sleep disorder Tx
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
Sleep disorder Tx Benzos
*triazolam HALCION Suppress REM/Deep sleep Use= LESS than 3 weeks
64
Rapid onset Benzos
Triazolam HALCION Alprazolam XANAX Diazepam VALIUM
65
Short duration Benzos
Triazolam HALCION | Midazolam VERSED
66
Intermediate Duration Benzos
Alprazolam XANAX
67
Long duration Benzos
Diazepam VALIUM | Clonazepam KLONOPIN
68
BRAs Advantages (vs. Benzos)
*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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