Lec #6 Drugs for sleep

Question 1

neurotransmitter that induces somnolence and sleepiness

Answer 1

adenosine

Question 2

sleep

Answer 2

cyclical behavior of reversible unconsciousness and immobility

Question 3

name 3 negative effects of chronic insufficient sleep?

Answer 3

• increased risk of diabetes
• cardiovascular disease
• cancer

Question 4

depressant

Answer 4

drug that reduces neuron activity and arousal

Question 5

2 types of depressants?

Answer 5

• Hypnotic = a drug that induces sleep
• Stimulant = a drug that promotes wakefulness and arousal

Question 6

neurotransmitters that promote wakefulness

Answer 6

• serotonin
  -norepinephrine
  -dopamine
  -histamine
  -orexin

Question 7

action of antihistamine drugs like diphenhydramine (Benadryl) and loratadine (Claritin) on histamine receptors

Answer 7

• some antihistamine drugs like diphenhydramine (Benadryl) block the actions of histamine and promote sleep.
• Newer antihistamines like loratadine (Claritin) don’t cause drowsiness because they are prevented from entering the brain by the blood-brain-barrier

Question 8

what are the 3 components that induce sleepiness?

Answer 8

• increase in adenosine levels
• decrease in levels of orexin and monoamines

Question 9

monoamines

Answer 9

• histamine
• norepinephrine
• dopamine
• serotonin

Question 10

hypnotics

Answer 10

drugs that promote sleep

Question 11

how do hypnotics promote sleep

Answer 11

• reduce activity in the brain involved in consciousness and vigilance
• activate GABA receptors to reduce neuronal activity and promote sleep

Question 12

GABA (gamma-hydroxybutyric)

Answer 12

inhibitory neurotransmitter and body’s mechanism to quiet neurons

Question 13

GABA receptor

Answer 13

ion channel allowing chloride ions to flow into the neuron and hyperpolarize the membrane potential (less likely to fire an action potential)

Question 14

barbiturates (phenobarbitral) action on GABA receptor

Answer 14

• agonists of GABA receptor and cause it to stay open for longer periods of time so that more ions can flow into the cell and hyperpolarize the neuron

Question 15

2 reasons why barbiturates are not safe for patients to take ion their own for insomnia?

Answer 15

• possible to overdose, can be lethal
• can be abused and become addictive

Question 16

benzodiazepines (clonazepam, lorazepam, zopiclone, and zolpidem (Ambien))

Answer 16

natural agonist to the GABA receptor and keep it open more frequently so more chloride ions enter when the benzo is present

Question 17

difference between benzodiazepines and barbiturates

Answer 17

-barbiturates keep the GABA receptor longer, whereas benzodiazepines increase the frequency of GABA channel opening
-benzodiazepines are also safer than barbiturates because we have a method to reverse benzodiazepine poisoning but not barbiturate poisoning.

Question 18

short-term effects of benzodiazepines

Answer 18

• motor and cognitive impairment
• amnesia
• reduce neuronal activity of an autonomic nervous system
• digestion impairment

Question 19

how does consumption of benzodiazepines cause tolerance?

Answer 19

• activate the GABA receptor, the body will decrease the amount of GABA receptor to offset the actions of the drug and require more of the drug to get the same effect

Question 20

how are benzodiazepines addictive?

Answer 20

• Benzodiazepines can be addictive because they indirectly increase the firing of dopamine neurons. They do this in a similar manner to opiates because they also quiet the neurons that normally keep dopamine levels low.
• Instead of binding to mu opiate receptors, benzo’s bind to GABA receptors; however, both drugs will lead to an indirect increase in dopamine.

Question 21

action of ramelteon

Answer 21

melatonin receptor agonist for 2 receptors: MLT1 and MLT2

Question 22

3 ways ramelteon treats insomnia?

Answer 22

• decreases body temperature
• decreases latency to sleep onsent
• latency to persistent sleep

Question 23

parasomnias

Answer 23

sleep disorders that involve abnormal behaviors, movements, or experiences during sleep.

Question 24

which sleep-aid causes parasomnias?

Answer 24

Zolpidem (ambien)- metabolized differently by men and women (prescribed at a lower dose)