Drugs for Insomnia Lecture PDF

Question 1

Insomnia definition

Answer 1

Defined as inability to fall or maintains sleep, majority do not have predisposing psychaitric disease but untreated may be risk factor for development of psych problems, can be due to medical conditions, anxiety, or other factors

Question 2

Indication for hypnotic drug uses

Answer 2

Reserved for patients whose insomnia cannot be managed by nondrug means

Question 3

Sleep cycle

Answer 3

• NREM Stage 1 to 4 characterized by growing deeper taking 60-90 min
• Stage 1 aware of surroundings but relaxed
• Stage 2 unaware of surroundings but easily awakened
• Stage 3-4 slow wave sleep important for physical rest and restoration
• REM for 20 minutes, characterized by dreaming and mental restoration, is a state of deep sleep
• Return to NREM

Question 4

Drugs for insomnia are indicated only for short term use because of…

Answer 4

…drug dependent insomnia with rebound insomnia occurring upon discontinuing

Question 5

Barbituates mech of action

Answer 5

• Nonspecific suppression of CNS through binding to GABA receptor complexes at the reticular formation and cerebral cortex causing sedation with no ceiling to amount of CNS depression can produce resulting in death when overdosage
• suppresses REM sleep and increases stage 2 sleep resulting in rebound effect upon discontinuation
• Tolerance develops to sedative hypnotic effects but not to toxic effects making likelihood of overdose dangerous

Question 6

Barbituate therapeutic uses (3)

Answer 6

• Distant 2nd choice to benzodiazepines for relieving insomnia
• low dose for seizure suppression
• induction of anesthesia

Question 7

Barbituate ADR’s (4)

Answer 7

• Respiratory depression
• abuse and overdose
• fetal harm
• hangover effect with residual effects following day

Question 8

Triad of acute barbituate overdosage

Answer 8

• Respiratory depression
• pinpoint pupils
• coma

Question 9

Benzodiazepines function and popular examples (3)

Answer 9

Drug of choice for anziety and insomnia

-Diazepam (valium), lorazepam (ativan), and alprazolam (xanax)

Question 10

Benzodiazepines mech of action

Answer 10

-Decrease functional activity of specific areas of the brain and spinal cord by potentiating activity of inhibitory neurotransmitters in the CNS affecting primarily the limbic system (emotion), reticular formation (sleep and wakefulness), cerebral cortex (stop convulsions and seizures), and spinal cord (decrease skeletal muscle tone in injury)

Question 11

Benzodiazepines therapeutic uses (4)

Answer 11

• Anxiety drug of choice (short term typically while antidepressant is long term)
• insomnia drug of choice
• seizure disorders (diazepam is DOC for status epilepticus)
• Induction of anesthesia

Question 12

Benzodiazepines ADR’s (2)

Answer 12

• CNS depression
• rare respiratory depression if combined with other drugs
• physical dependence

Question 13

Flumazenil (romazicon) function

Answer 13

Competitive benzodiazepine receptor antagonist approved for treatment of benzodiazepine overdosage and for reversing effects of benzos following general anesthesia

Question 14

Flurazepam (dalmane) function

Answer 14

Long acting benzodiazepine for treatment of insomnia, has long half life resulting in hangover effect

Question 15

Temazepam (restoril) function

Answer 15

Short acting hypnotic administered 1-2 hours before bedtime

Question 16

Triazolam (halcion) function

Answer 16

Short acting benzodiazepine that does not usually produce hangover effect and has very short duration of action but can be associated with rebound insomnia, concerns over psychotic type behaviors

Question 17

Zopidem drug class, function

Answer 17

• Benzodiazepine receptor agonists function
• Act rapidly to decrease sleep latency, relatively safe with low potential for tolerance, abuse, or dependence, called the nonbenzo benzo as it acts through a different mechanism but helps treat insomnia

Question 18

Zalepon (sonata) function

Answer 18

same chemical class as zolpidem that is short acting and fast onset only lasting 4 hours for those who take in middle of night if cannot sleep

Question 19

Ramelton (rozerem) drug class, function, and mech of action

Answer 19

• Melatonin receptor agonist
• rapid onset short duration for inducing sleep in patients
• highly selective for melatonin receptors that upon their activation inhibit cAMP activation

Question 20

Suvorexant (belsomra) drug class, mech of action, function

Answer 20

• Orexin receptor antagonoist
• orexin neurons are active during wakefulness and silent during sleep, loss of signaling associated with narcolepsy, blocking peptides allows for deep sleep
• Treatment for sleep onset or maintenance insomnia

Question 21

2 antihistamines currently approved as sleep aids OTC

Answer 21

• diphenhydramine in advil and tylenol pm

- doxylamine

Question 22

Buspar (buspirone) function

Answer 22

A non benzoanxiolytic used for the short term treatment of generalized anxiety as alternative because it does not cause sedation, has no abuse potential, and although takes weeks to peak effects has proven equally effective for short term GAD treatment

Question 23

How to withdraw a patient from barbituates?

Answer 23

Phenobarbital