Psych: Sleep and Anxiety Disorders Flashcards Preview

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Flashcards in Psych: Sleep and Anxiety Disorders Deck (24)
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1

Barbiturate Drugs?

  • Phenobarbital
  • Thiopental

 

2

Phenobarbital (Luminal)

  • Barbituate – long half life
  • Binds directly to the GABAA receptor
  • Increases the efficacy of endogenous GABA signaling
  • Increases Cl- channel openings --> membrane Hyperpolarization and decreased Excitability
  • Suppresses Reticular activating system --> suppresses Seizures at low levels that do not induce Hypnosis
  • Tx: Tonic-clonic and Partial seizures (preferred Pregnant women)
  • SEx: Sedation, Inducer of CYP450 system

3

Thiopental (Pentothal)

  • GABAergic – short half life
  • Binds directly to the GABAA receptor
  • Increases the efficacy of endogenous GABA signaling
  • Increases Cl- channel openings --> membrane Hyperpolarization and decreased Excitability
  • Suppresses Brainstem Reticular activating system; Sedation, Amnesia, LOC, Reflex suppression
  • Tx: Pre-anesthetic sedative, Adjunct to Local anesthesia, Sedative-hypnotic
  • Hepatic metabolism by CYP450 sys. and Potent CYP450 inducer

4

Benzodiazepines

  • Binds directly to GABAA receptor and increases potency of endogenous GABA signaling
  • Increases Cl- channel openings --> membrane Hyperpolarization and decreased Excitability
  • Suppresses Brainstem Reticular activating system; Sedation, Amnesia, LOC, Reflex suppression
  • Inhibitory neurotransmission --> Anticonvulsant and Muscle relaxant
  • Indirectly activate GABA --> Larger therapeutic index than Barbituates
  • Tx: Sedative-hypnotic, Anxiolytic: short-term management, Status Epilepticus, Prophylaxis against Ethanol withdrawal, Muscle relaxant, Anesthesia induction
  • SEx: Drowsiness, Impaired judgement, Decreased Motor skills
  • Tolerance and High potential for Dependence
  • Concomitmant --> Fatal CNS depression

5

Short half-life Benzodiazepines? ( < 8 hours)

(M O T)

  • Midazolam
  • Oxazepam
  • Triazolam

6

Medium half-life Benzodiazepines? (8 – 16 hours)

(A E L T)

  • Alprazolam
  • Estazolam
  • Lorazepam
  • Temazepam

7

Long half-life Benzodiazepines? ( > 16 hours)

(CCC D F Q)

  • Chlordiazepoxide
  • Clonazepam
  • Clorazepate
  • Diazepam
  • Flurazepam
  • Quazepam

8

Benzodiazepine Drugs? 

(M O T – A E L T – CCC D F Q)

  • Midazolam
  • Oxazepam
  • Triazolam
     
  • Alprazolam
  • Estazolam
  • Lorazepam
  • Temazapam
  • Chlordiazepoxide
  • Clonazepam (also Spasmolytic)
  • Clorazepate
  • Diazepam (also Spasmolytic)
  • Flurazepam
  • Quazepam

9

Non-benzodiazepines?

(E - ZZ)

 

  • Eszopiclone (Lunesta)
  • Zolpidem (Ambien)
  • Zoleplon (Sonata)

10

Eszopiclone (Lunesta)

Zolpidem (Ambien)

Zoleplon (Sonata)

  • GABAergic
  • Nonbenzodiazepine Sedative-hypnotic
  • Selectively stimulates the w1 subtype of GABAA receptor
  • Produces Sedation and Anxiolysis – very little Muscle relaxant or Anticonvulsant activity
  • Tx: Insomnia, Restless leg syndrome
  • SEx: Drowsiness, Dizziness, and Fatigue
  • Additive w/ other CNS depressors

11

Benzodiazapine Antagonist?

  • Flumazenil

12

Flumazenil (Romazicon)

  • Benzodiazepine Analog Antagonist
  • Competitively inhibits the actions of Benzodiazepine
  • Rapidly-reverse Benzodiazepine overdose but MAY precipitate withdrawal Seizures, espcially in Alcoholics or Chronic Benzodiazepine users

13

Ramelteon (Rozerem)

  • Weak Non-benzodiazepine Sedative-hypnotic
  • Selectively Stimulates Melatonin Type 1 and Melatonin Type 2 receptors
  • Melanonin is a hormone secreted by the Pineal gland that regulates the Sleep-wake cycle

14

Buspirone (BuSpar)

  • Selective Partial Agonist of 5-HT1A serotonin receptors
  • Tx: Anxiolytic w/out sedation
  • Cannot be used to treat Benzodiazepine withdrawal
  • SEx: Tachycardia, palpatations, GI distress, Less abuse potential than Benzodiazepines, No rebound anxiety or withdrawal symptoms with Discontinuation
  • Contraindicated w/ Hepatic or Renal impairment
  • Hepatic oxidation to active metabolite
  • Use w/ MAOIs may lead to Hypertensive crisis
  • Cocomitant consumption of Grapefruit joice can lead to markedly increased levels of Buspirone because of inhibition of CYP3A4

15

TCA Sedatives Drugs?

  • Amitryptaline
  • Doxepin

16

Amitryptyline (Elavil)

Doxepin (Sinequan)

  • TCA that Inhibits reuptake of Norepinephrine (++) and Serotonin (+++)
  • Clinical effects not seen for several weeks
  • Also blocks; Anti-H1 (+++), Anti-M1 (++),
    Anti-a1-adrenoceptors (++), and Anti-a2-adrenoceptors receptors --> accounting for Numerous side effects
  • Tx: Clinical Depression, Neuropathic and Chronic Pain, Enuresis, Migraine prophylaxis, ADHD in children
  • SEx: Anti-histamine, Sedation, Weight gain, Secondary amines cause less sedation than Tertiary amines
  • Anticholinergic: Blurred vision, Dry mouth, Urinary retention, Constipation, Agitation, Tachy, Sweating
  • a1-adrenoceptors: Postural HTN, Tachycardia
  • 1A antiarrhythmic properties from Na+ channel blockade
  • Overdose: Coma, Metabolic acidosis, Hyperpyrexia, Cardio Arrhythmias

17

Trazodone (Desyrel)

  • Atypical Antidepressent 5-HT2 Antagonist
  • SEx: Anti-H1 (+++ - sedation), Anti-a1 (+ - Hypotension)
  • Tx: Clinical depression
  • SEx: Sedation (because H1 blockade), rare Hepatic failure
  • CYP3A4 inhibitor
  • More sedating than Nefazodone
  • Priapism

18

Mirtazepine (Remeron)

  • Similar to Trazadone
  • 5-HT2 and 5-HT3 Antagonis and a2 adrenorecptor Antagonist on noradrenergic and serotonergic neurons, increases NE and 5-HT release
  • Powerful H1 blocker --> Very Sedating, Appetitie, Weight gain
  • SEx: Anti-H1 (+++ - sedation), Anti-a1 (0/+ - Hypotension)
  • Minimal effects on Amine reuptake
  • Can also be used in Bullimia Nervosa pts.

19

Gaba-hydroxybutyrate (GHB) (Sodium Oxybate)

20

Valerian

21

Alcohol

22

Melatonin

23

Doxylamine – antihistamines

24

Spasmolytic Drugs?

  • Diazepam
  • Clonazepam
  • Baclofen
  • Tizanidine
  • Dantrolene