- CNS depressant - calming/tranquilizing effect - ideally minimal effect on motor/mental

- sleep-inducing or promoting - not all hypnotics are sedatives

Exam I - Anxiolytics Flashcards by Kristian Melby

Drug List
GABA receptors
Barbiturates

-phenobarbital

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Drug List
GABA receptors
Benzodiazepines

diazepam
triazolam
aplrazolam
clonazepam
midazolam

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Drug List
GABA receptors
Benzodiazepine Receptor Agonists

zolpidem

- eszopiclone

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Drug List
GABA receptors
Benzodiazipine Receptor Antagonists

-flumazenil

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Drug List

Melatonin Congener

-ramelteon

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Drug List

5-HT1a receptor agonist

-buspirone

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Sedative

Definition

CNS depressant
calming/tranquilizing effect
ideally minimal effect on motor/mental

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Sedative

Drug classes

benzos
barbiturates
alcohol
antipsychotics
antidepressants
antihistamines

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Hypnoptic

Definition

sleep-inducing or promoting

- not all hypnotics are sedatives

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Anxiolytic

Definition

reduce anxiety
not all are sedative
broad umbrella of drugs; “anxiety” heterogeneous

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Sedative-Hypnotics

Graded Dose response

-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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Indications
Panic Disorder
Agoraphobia

1) antidpressants (SSRI)

2) alprazolam (risk of dependence)

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Indications

Social Phobia

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

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Indications

Specific Phobia

psychotx

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Indications

GAD

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

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Barbiturates
Phenobarbitol
Mechanism

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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Barbiturates
Phenobarbitol
ADME

low tx index
linear dose-response
induce CYP enzymes

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Barbiturates
Phenobarbitol
Adverse

dependence/addiction

- low TI: overdose

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Barbiturates
Phenobarbitol
Indications

anesthesia
seizure disorders
rarely used as sedative

Benzodiazepines

Mechanism

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)

Benzodiazepines
Receptor Antagonists
(Flumezanil)
Mechanism

-competitively inhibits BZ receport agonists

Benzodiazepines

Indications/Effects

anterograde amnesia (high dose)
anesthesia (IV adjunct)
anticonvulsant (clonazepam)
skeletal muscle relaxations

Benzodiazepines

Adverse

amnesia
disinhibition
dependence
resp depression
contra’d sleep apnea
rebound anxiety/insomnia

Sleep Disorders

Indications

Triazolam

Epilepsy | Indications

Clonazepam, Diazepam

Anesthesia | Indications

- Midazolam IV | - for amnestic component

Benzodiazepines | ADME

-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

Benzodiazepines | Half Lives

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

Benzodiazepines | Safety Profile

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

Benzodiazepines | Adverse

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

Benzodiazepine Receptor Antagonist Indiciations

- post-surgery anesthesia - OD - short acting

Benzodiazepine Receptor Antagonist Adverse

-can precipitate withdrawal

Buspirone | Mechanism

- 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)

Buspirone | Indications

GAD

Buspirone | ADME

- rapidly absorbed | - several active metabs from first pass

Buspirone | Safety Profile

- no tolerance/dependence/abuse | - no psychomotor agitation

Buspirone | Adverse

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

Hypnotics and REM

- REM decreases with hypnotics | - REM rebound when withdrawn

Sleep and age

- latency to fall asleep - increased number of awakenings - total sleep may or may not change

Melatonin Receptor Agonists Ramelteon Mechanism

-agonist at MT1 and MT2 receptors

Melatonin Receptor Agonists Ramelteon Indications

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

Melatonin Receptor Agonists Ramelteon Adverse

- dizziness | - hyperprolactinemia

``` Z drugs (zolpidem, eszopiclone) indications ```

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

Z drugs | adverse

- tolerance/dependence - suppress REM/"deep sleep" - anterograde amnesia, sleepwalking - dose reduce for hepatic dysfxn - dose reduce for cimetidine - resp depression at high dose

Z drugs | Mechanism

-bind GABA A receptors with a1 subunit

Z drugs | ADME

- short acting | - clearance decreased in elderly, reduce dosage