Anxiolytics-Sedative-Hypnotics

Question 1

Barbiturates:

Answer 1

Phenobarbital, Pentobarbital, Thiopental

Question 2

Benzodiazepines:

Answer 2

Diazepam, Lorazepam, Triazolam, Alprazolam

Question 3

MOA: Bind to multiple isoforms of GABAA R, increases DURATION of GABA channel opening
A/D (lipid solubility) M (hepatic, slow) E (kidney, tx phenobarbital overdose by raising urinary pH)

Answer 3

Barbiturates:

Phenobarbital, Pentobarbital, Thiopental

Question 4

Clinical Uses: Anxiety – low doses
Hypnosis – induces sleep
Seizure control (tonic-clonic)
Anesthesia induction – (thiopental is very lipid soluble)

Answer 4

Barbiturates:

Phenobarbital, Pentobarbital, Thiopental

Question 5

AE: Hypnotic doses: resp depression in pts w/ pulmonary DZ, CV depression in pts w/ heart failure
Toxic doses: circulatory collapse, reversible depression of all tissue
Big impact on hepatic E activity

Answer 5

Barbiturates:

Phenobarbital, Pentobarbital, Thiopental

Question 6

Pharmacokinetic & dynamic tolerance
Dependenceincreases anxiety, insomnia, CNS excitability, convulsions
Withdrawal sx related to ½ life

Answer 6

Barbiturates:

Phenobarbital, Pentobarbital, Thiopental

Question 7

MOA:Bind to multiple isoforms of GABAA R, increases FREQUENCY of GABA channel opening (allosterically)
A/D (triazolam rapid, lipid solubility), M (hepatic, active metabolites), E (kidneys)

Answer 7

Benzodiazepines:

Diazepam, Lorazepam, Triazolam, Alprazolam

Question 8

Clinical Uses: Anxiety – sedation at low doses
Insomnia – hypnosis like barbs
Seizures – diazepam, lorazepam, clonazepam, nitrazepam (w/o CNS depression)
Muscle relaxation
Anesthetic(diazepam, lorazepam) better quality, more amnesia & anxiolytic, less pain on injection

Answer 8

Benzodiazepines:

Diazepam, Lorazepam, Triazolam, Alprazolam

Question 9

AE: Little impact on hepatic drug-metabolizing E activity

Respiration and CV effects same as barbs

Answer 9

Benzodiazepines:

Diazepam, Lorazepam, Triazolam, Alprazolam

Question 10

Pharmacodynamic tolerance (CNS responsiveness)

Dependence = same as barbs

Answer 10

Benzodiazepines:

Diazepam, Lorazepam, Triazolam, Alprazolam

Question 11

MOA: Benzo binding site antagonist

Answer 11

Flumazenil

Question 12

Clinical Uses; Reverse postanesthetic respiratory depression of benzo anesthetics

Answer 12

Flumazenil

Question 13

Doesn’t block barbs function

Answer 13

Flumazenil

Question 14

MOA: Non-benzo benzo-R agonist, selectively bind certain subtypes of GABAA R

Answer 14

Zolpidem (Ambien)

Question 15

Clinical Uses: Only promote SLEEP, no anxiolytic properties

Answer 15

Zolpidem (Ambien)

Question 16

AE: No residual effects upon waking

Answer 16

Zolpidem (Ambien)

Question 17

Rapid onset, short duration of action, slow tolerance development

Answer 17

Zolpidem (Ambien)

Question 18

MOA: Partial agonist at 5HT1A R + affinity for D2 DA R (no interax with GABA)

Answer 18

Busipirone

Question 19

Clinical Uses:Relieves ANXIETY w/o sedative or hypnotic effects, used for generalized anxiety disorders

Answer 19

Busipirone

Question 20

AE: Anxiolytic effects make take 1 wk, unsuitable for panic disorders

Answer 20

Busipirone

Question 21

No anticonvulsant or muscle relaxant properties, minimal abuse liability, less psychomotor impairment than benzos (drive)

Answer 21

Busipirone

Question 22

MOA: MT1 & MT2 melatonin R agonist at suprachiasmatic nuclei (no interax with GABA)

Answer 22

Ramelton (Rozerem)

Question 23

Clinical Uses: Used for patients who have difficulty falling asleep

Answer 23

Ramelton (Rozerem)

Question 24

AE: Dizziness, drowsiness, fatigue, endocrine

Answer 24

Ramelton (Rozerem)

Question 25

No rebound insomnia, withdrawal sx, or dependence, minimal potential for abuse

Answer 25

Ramelton (Rozerem)