CHAPTER 9: Anxiolytic and Hypnotic Drugs

Question 1

states affected by these agents

Answer 1

ANXIETY: feeling tension, nervous, fear reaction to stimulus

SEDATION: loss awareness to environmental stimuli (still awake)

HYPNOSIS: extreme sedation, further CNS depression and sleep

Question 2

GABAergic Neurotransmission

Answer 2

• under stress excitatory neurons in amygdala send signal to areas of brain w feelings of fear/anxiety
  -inhibitory GABA neurons REGULATE these emotions, tranquilize effects

Question 3

GABA-A receptors

Answer 3

• refer to a1 subunit of ligand gated ion channel(hypnosis)
• allow movement/flow of chloride in post synpatic membrane, hyperpolarization

GABA IS THE ENDOGENOUS MOLECULE

Question 4

Anxiolytic, Hypnotic, Sedative purposes

Answer 4

Anxiolytics: prevent tension, fear
Sedatives: calm, make PT unaware to enviro
Hypnotics: cause sleep

Question 5

Benzodiazepines
-where do they act
-low dose/high dose

Answer 5

• act in limbic systemic and RAS (reticular activating system)
• make GABA more effective
• interfere w neuron firing

LOW DOSE: assist anxiety
HIGH DOSE: sedate/hypnosis

Question 6

Benzodiazepines: use

Answer 6

• replaced barbiturates and meprobamate for treating anxiety and insomnia, safer and more effective
• CONTROLLED substances: induce addiction
• end in -lam or -pam

Question 7

Benzodiazepines: MOA

Answer 7

receptor empty: channel closed, no Cl- go thru

GABA binded: channel open, hyperpolarize cell, Cl- go thru

GABA and Benzo: bind to diff sites, benzo betwen alpha and gamma sites, channel open for a LONGER time/greater Cl- entry

Question 8

Benzodiazepines: pharmacokinetics

Answer 8

• absorb from GI
  -peak levels in 30mins-2 hrs
  -lipid soluble, distributes well
  -crosses placenta
• enters breast milk
• metab in liver by CYP3A4, some metab STILL ACTIVE

Question 9

benzodiazepines: duration of action

Answer 9

• short, intermed, and long acting groups
  -long makes active metabolites

Question 10

Benzos: therapeutic actions

Answer 10

• reduce anxiety low doses, inhib neuronal circuits in limbic system (enhance a2 GABAergic)
• sedative/hypnotic at high dose (a1 GABA-A)
• anterograde amnesia: temp impairment of memory (a1 GABA-A)
• anticonvulsant (a1 GABA-A)
• muscle relaxant

Question 11

Benzos: therapeutic uses
- anxiety, panic, amnesia, seizures

Answer 11

anxiety: clonazepam, lorazepam, diazepam (long acting)

panic disorders: alprazolam

amnesia: short acting for anxiety producing procedures (surgeries), midazolam for anterograde amnesia

seizures: clonezapam adjunct therapy
lorazepam, diazepam for status epilepticus (one seizure after another w out rest)

Question 12

benzos: therapeutic uses
- musc and sleep

Answer 12

muscular disorders: diazepam for spasms and spasticity from degenerative disorders (MS or cerebral palsy)

sleep disorders: balance sedative effect w hangover effect when waking up
- short act triazolam for falling asleep problems
intermed temazepam for frequent awakenings/trouble staying asleep

Question 13

Benzos: tolerance and dependance

Answer 13

tolerance: dec responsiveness to repeated dose of the drug
- high dose, prolonged period of time–> dependence can develop
-absurpt discont=withdrawal

Question 14

withdrawal symptoms of benzos

Answer 14

• return of anxiety
• inc rebound insomnia
• restlessness
• agitation, irritability
• nausea and sweating

Question 15

benzo: adverse effects

Answer 15

-drowsy, confusion, sedation, depression, lethargy
HIGH DOSE: ataxia, no fine motor coordination
-cognitive impairment
-gi conditions, cardiovasc problems
-withdrawal
alcohol and CNS depressants enhance sedative/hypno effects