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Pharm Spring Exam 1 > Exam I - Anxiolytics > Flashcards

Exam I - Anxiolytics Flashcards

1
Q

Drug List
GABA receptors
Barbiturates

A

-phenobarbital

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2
Q

Drug List
GABA receptors
Benzodiazepines

A
  • diazepam
  • triazolam
  • aplrazolam
  • clonazepam
  • midazolam
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3
Q

Drug List
GABA receptors
Benzodiazepine Receptor Agonists

A
  • zolpidem

- eszopiclone

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4
Q

Drug List
GABA receptors
Benzodiazipine Receptor Antagonists

A

-flumazenil

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5
Q

Drug List

Melatonin Congener

A

-ramelteon

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6
Q

Drug List

5-HT1a receptor agonist

A

-buspirone

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7
Q

Sedative

Definition

A
  • CNS depressant
  • calming/tranquilizing effect
  • ideally minimal effect on motor/mental
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8
Q

Sedative

Drug classes

A
  • benzos
  • barbiturates
  • alcohol
  • antipsychotics
  • antidepressants
  • antihistamines
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9
Q

Hypnoptic

Definition

A
  • sleep-inducing or promoting

- not all hypnotics are sedatives

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10
Q

Anxiolytic

Definition

A
  • reduce anxiety
  • not all are sedative
  • broad umbrella of drugs; “anxiety” heterogeneous
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11
Q

Sedative-Hypnotics

Graded Dose response

A

-low dose anxiolytic/sedative
-high dose hypnotic
-very high dose coma, anesthesia, death
-linear relationship for traditional drugs (e.g. barbs)
-benzos are safer, non-linear; proportionately VERY high dose needed
for coma/anesthesia/death

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12
Q

Indications
Panic Disorder
Agoraphobia

A

1) antidpressants (SSRI)

2) alprazolam (risk of dependence)

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13
Q

Indications

Social Phobia

A

1) psychotx
2) SSRI
3) clonazepam
4) Beta blockers (tremors)

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14
Q

Indications

Specific Phobia

A

psychotx

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15
Q

Indications

GAD

A

1) benzos (alprazolam, diazepam)
2) buspirone
3) antidepressants

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16
Q

Barbiturates
Phenobarbitol
Mechanism

A
  • binds GABA A receptor
  • increased Cl- flux
  • hyperpolarizes neuron, inhibits
  • suppresses glutamate transmission to AMPA receptors
  • directly open Cl- channel at HIGH concentrations (toxicity)
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17
Q

Barbiturates
Phenobarbitol
ADME

A
  • low tx index
  • linear dose-response
  • induce CYP enzymes
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18
Q

Barbiturates
Phenobarbitol
Adverse

A
  • dependence/addiction

- low TI: overdose

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19
Q

Barbiturates
Phenobarbitol
Indications

A
  • anesthesia
  • seizure disorders
  • rarely used as sedative
20
Q

Benzodiazepines

Mechanism

A
  • bind GABA A recepotors
  • facilitate GABA-mediated Cl- influx
  • do NOT have direct effect on Cl- channels
  • specificity for GABA receptors
  • full agonists (except zolpidem, which is specific for a1 subunit)
21
Q

Benzodiazepines
Receptor Antagonists
(Flumezanil)
Mechanism

A

-competitively inhibits BZ receport agonists

22
Q

Benzodiazepines

Indications/Effects

A
  • anterograde amnesia (high dose)
  • anesthesia (IV adjunct)
  • anticonvulsant (clonazepam)
  • skeletal muscle relaxations
23
Q

Benzodiazepines

Adverse

A
  • amnesia
  • disinhibition
  • dependence
  • resp depression
  • contra’d sleep apnea
  • rebound anxiety/insomnia
24
Q

Sleep Disorders

Indications

A

Triazolam

25
Q

Epilepsy

Indications

A

Clonazepam, Diazepam

26
Q

Anesthesia

Indications

A
  • Midazolam IV

- for amnestic component

27
Q

Benzodiazepines

ADME

A

-slow absorption
-midazolam, diazepam, aplrazolam, triazolam
more quickly absorbed
-metab’d to active metabolites by CYP3A4
-many metabolites have half life > 50 hrs
-conjugated to inactive glucuronides for renal exretion

28
Q

Benzodiazepines

Half Lives

A

long >12: diazepam, clonazepam
medium 6-12: alprazolam
short <6: triazolam, midazolam

29
Q

Benzodiazepines

Safety Profile

A
  • relatively safe (high tx index, flatter dose-response)
  • flumazenil for OD antagonism
  • no/low drug-drug interactions
  • long duration (one dose daily)
30
Q

Benzodiazepines

Adverse

A
  • addiction
  • tolerance
  • dependence (rebound insomnia/anxiety)
  • anterograde amnesia
  • weight gain, nausea, headache, light-headedness
  • potentiate EtOH CNS depression
31
Q

Benzodiazepine
Receptor Antagonist
Indiciations

A
  • post-surgery anesthesia
  • OD
  • short acting
32
Q

Benzodiazepine
Receptor Antagonist
Adverse

A

-can precipitate withdrawal

33
Q

Buspirone

Mechanism

A
  • non-sedative anxiolytic
  • partial agonist at CNS 5-HT1a receptors
  • minor effects at a1, a2, D2 receptors
  • efficacy takes 1+ weeks (not useful in acute anxiety)
34
Q

Buspirone

Indications

A

GAD

35
Q

Buspirone

ADME

A
  • rapidly absorbed

- several active metabs from first pass

36
Q

Buspirone

Safety Profile

A
  • no tolerance/dependence/abuse

- no psychomotor agitation

37
Q

Buspirone

Adverse

A

-chest pain, tachycardia, palps, dizziness,
nervousness, tinnitus, GI problems
-contra’d MAOIs

38
Q

Hypnotics and REM

A
  • REM decreases with hypnotics

- REM rebound when withdrawn

39
Q

Sleep and age

A
  • latency to fall asleep
  • increased number of awakenings
  • total sleep may or may not change
40
Q

Melatonin Receptor Agonists
Ramelteon
Mechanism

A

-agonist at MT1 and MT2 receptors

41
Q

Melatonin Receptor Agonists
Ramelteon
Indications

A

-insomia, delayed sleep onset, circadian rhythm d/o

42
Q

Melatonin Receptor Agonists
Ramelteon
Adverse

A
  • dizziness

- hyperprolactinemia

43
Q 
Z drugs (zolpidem, eszopiclone)
indications
A

-short-term (<3 wks) sleep d/o tx

44
Q

Z drugs

adverse

A
  • tolerance/dependence
  • suppress REM/”deep sleep”
  • anterograde amnesia, sleepwalking
  • dose reduce for hepatic dysfxn
  • dose reduce for cimetidine
  • resp depression at high dose
45
Q

Z drugs

Mechanism

A

-bind GABA A receptors with a1 subunit

46
Q

Z drugs

ADME

A
  • short acting

- clearance decreased in elderly, reduce dosage

Pharm Spring Exam 1 (8 decks)

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