CNS Depressants

Question 1

Pons and Medulla important for

Answer 1

respiration control

cardiovascular function

Question 2

Reticular formation important for

Answer 2

control of consciousness, arousal and alertness

Question 3

Selective Depressants

Answer 3

Sedative-hypnotics

Benzodiazepines
Barbiturates
Ethanol

Question 4

Non-selective Depressants

Answer 4

Anti-histamines

Opioid analgesics

Question 5

Sedative anxiolytics

Answer 5

calming effect or sedation with relief of anxiety at relatively low doses

Question 6

Hypnotics

Answer 6

produce drowsiness and/or encourage onset and maintenance of state of sleep

Question 7

What brain region is most affected with anxiety?

Answer 7

limbic system

hippocampus
amygdala
pre-frontal cortex

Question 8

Sedative Hypnotic Benzo’s (4)

Answer 8

Flurazepam
Temazepam
Triazolam
Midazolam

Question 9

Anxiolytic Benzo’s (5)

Answer 9

Alprazolam
CLorazepate
Diazepam
Lorazepam
Oxazepam

Question 10

Z Drugs (3)

sleep inducers

Answer 10

Zolpidem
Zaleplon
Eszopiclone

Question 11

Linear slope Drugs

what occurs?

Answer 11

barbiturates
alcohol

as dose increases, effects increase all the way up to potentially coma

not as safe

Question 12

Non-linear slope drugs

what occurs?

Answer 12

benzodiazepines
hypnotics (newer)

plateau occurs with increasing dose

SAFER

Question 13

Sedative-Hypnotics Therapeutic Uses

Answer 13

Relief of - anxiety, insomnia

Sedation/amnesia - medical/surgical procedures

Epilepsy/Seizure tx

Withdrawal tx

Muscle relaxation

Question 14

Benzodiazepines ending?

Answer 14

-epam

Question 15

Benzodiazepine Pharmacokinetics

Metabolism occurs mainly where?

Answer 15

Good absorption ORALLY

Metabolized by the LIVER - (CYP3A4)

Question 16

Benzo’s with rapid metabolism, short duration, less cumulative effects (2)

Why?

Answer 16

Lorazepam
Oxazepam

CONVERTED TO INACTIVE GLUCURONIDES - metabolites have no activity

Question 17

Benzo’s with short duration and weakly active metabolites (2)

Answer 17

Alprazolam

Triazolam

Question 18

Influence of age on metabolism of benzo’s

Affects what pharmacokinetic values (2)?

Answer 18

Elderly have DECREASED PHASE I METABOLISM

Slows hepatic processing

Vd increases
Ve decreases

Question 19

Which two benzo’s have AGE-INDEPENDENT elimination?

Answer 19

Oxazepam

Lorazepam

Question 20

Mechanism of action of benzodiazepins

Answer 20

Potentiate effects of GABA-A receptors

Increase frequency of OPENING/CONDUCTANCE of CHLORIDE ION CHANNELS

leads to HYPERPOLARIZATION – decreased neuronal firing

Question 21

Benzodiazepine Side effects/Toxicity

Answer 21

RESPIRATORY DEPRESSION - can be lethal if combined with other depressants

ANTEROGRADE AMNESIA

TOLERANCE - 12 to 14 days

DEPENDENCE - physical and psychological

WITHDRAWAL

Question 22

Withdrawal effects cause?

How to dissipate?

Answer 22

all of the effects that were being suppressed by the drug return more intensely

taper off drugs slowly

Question 23

5 contraindications of benzo’s

Answer 23

pregnancy
elderly
substance abuser
sleep disorders
when alertness is required

Question 24

Major Drug INteraction of Benzo’s

Answer 24

ADDITIVE CNS DEPRESSION - when combined with other CNS depressants

Question 25

Benzo's Major Therapeutic Uses (2)

Answer 25

Anxiolytic | Sedative/Hypnotic

Question 26

Flumenazil - type of drug? MOA Clinical use

Answer 26

BENZODIAZEPINE ANTAGONIST Competitive inhibitor of BZ RECEPTOR Counteract benzo overdose

Question 27

Eszopiclone Zolpidem type of drug? MOA? Clinical use

Answer 27

Newer SEDATIVES Bind selectively to BZ RECEPTOR ON GABA-A receptor and act as AGONISTS Used primarily for INSOMNIA

Question 28

Barbiturates (3)

Answer 28

Pentobarbital Phenobarbital Thiopental

Question 29

Barbiturates Clinical Uses

Answer 29

Anesthesia - thiopental Anticonvulsant - phenobarbital Medically induced coma - pentobarbital

Question 30

Barbiturates Pharmacokinetics

Answer 30

absorption/distribution varies with lipid solubility SLOW LIVER METABOLISM Little kidney excretion Duration is DEPENDENT ON METABOLISM - except thiopental

Question 31

Barbiturates MOA

Answer 31

increase DURATION OF GABA-GATED CHLORIDE CHANNEL OPENING Hyperpolarization - neuronal inhibition occurs

Question 32

Ramelteon type of drug? MOA? Clinical use?

Answer 32

SEDATIVE MELATONIN RECEPTOR AGONIST - MT1 and MT2 receptors minimal abuse liability

Question 33

Buspirone type of drug? MOA? CLinical use?

Answer 33

NON-SEDATING anxiolytic PARTIAL 5HT-1a AGONIST - reduces neuronal excitability and firing frequency, also decreases 5-HT release anti-anxiety for individuals who need more motor skills for work

Question 34

Beta blocker important for reducing MANIFESTATIONS of anxiety

Answer 34

Propanolol

Question 35

Antihistamines (2)

Answer 35

Hydroxyzine | Dyphenhydramine