3a: Sedative-Hypnotics, Antianxiety, Antidepressants

Question 1

purpose of CNS drugs

Answer 1

to modify the activity of the neurons in the CNS, treat CNS disorders, and change the arousal levels of the CNS

Question 2

neurotransmitters

Answer 2

released by neurons to cause excitation or inhibition to other neurons

Question 3

examples of neurotransmitters in the CNS

Answer 3

ACh, monoamines, amino acids, peptides

Question 4

mechanism of CNS drugs

Answer 4

modification of the synaptic transmission, which is done by altering the quantity of the neurotransmitter

Question 5

two categories of Sedative-Hypnotics

Answer 5

benzodiazepines and nonbenzodiazepines (both used to promote sleep, specifically in short-term situations like hospital stays)

Question 6

benzodiazepines

Answer 6

used for anxiety and promoting sleep, considered safer than barbiturates (nonbenzos), less chance of lethal overdose, and can cause tolerance and physical dependence with long-term use

Question 7

mechanism of benzos

Answer 7

increased inhibition at the CNS synapses that use GABA

Question 8

side effects of benzos

Answer 8

drowsiness, decreased motor performance, hang-over effect, anterograde amnesia

Question 9

suffix for benzos

Answer 9

(-am)

Question 10

nonbenzodiazepines (barbiturates)

Answer 10

used for sleep-hypnosis, CNS depressants, very small therapeutic index, very addictive, not commonly used

Question 11

mechanism of barbiturates

Answer 11

not entirely clear but do bind to GABA receptors

Question 12

side effects of barbiturates

Answer 12

very addictive, drug abuse, hang-over effect

Question 13

suffix for barbiturates

Answer 13

(-al)

Question 14

other compounds that can cause sedation-hypnosis

Answer 14

alcohol, antihistamines, antidepressants, antipsychotics, anticonvulsants, opioid analgesics

Question 15

pharmacokinetics of sedation-hypnosis drugs

Answer 15

very lipid-soluble, administered orally one dose at bedtime, absorbed from the GI tract, distributed uniformly throughout the body, metabolized in the liber, excreted through the kidneys

Question 16

side effects of all sedative-hypnotics

Answer 16

tolerance and dependence, complex motor behaviors (sleep walking, sleep driving, etc.), GI discomfort, dry mouth, sore throat, muscular incoordination

Question 17

indications for anti anxiety drugs

Answer 17

generalized anxiety, social anxiety, panic disorder, OCD, PTSD

Question 18

what is the most common benzo for treating anxiety?

Answer 18

Valium

Question 19

Valium is not good for what population, and why?

Answer 19

not good for the elderly, because it has a long half-life, and they cause sedation, confusion, and memory problems (associated with increased fall risk and hip fractures)

Question 20

what is rebound anxiety (related to benzos)?

Answer 20

removal of benzo that causes anxiety levels to return to pre-treatment levels

Question 21

mechanism of BuSpar

Answer 21

increases the effects of the neurotransmitter serotonin

Question 22

side effects of BuSpar

Answer 22

headache, dizziness, nausea, restlessness, hypothermia, low risk of abuse

Question 23

why are antidepressants an effective way to treat anxiety?

Answer 23

they typically have fewer side effects and lower risk of addiction than anti-anxiety medications

Question 24

examples of antidepressants

Answer 24

Paxil, Effexor, Zoloft

Question 25

indications for beta-blockers

Answer 25

arrhythmias, hypertension, and other cardiac issues (decreases anxiety without the sedation)

Question 26

symptoms of depression

Answer 26

inappropriate disposition, feeling unreasonably sad or discouraged, fluctuating between periods of depression and excessive excitation

Question 27

biological cause of depression

Answer 27

disturbance in CNS neurotransmission involving neurotransmitters serotonin, norepi, dopamine

Question 28

four categories of antidepressants

Answer 28

SSRIs, SNRIs, tricyclics, MAOs

Question 29

what is the key neurotransmitter that helps regulate mood and depression?

Answer 29

serotonin

Question 30

mechanism of SSRIs

Answer 30

block the reuptake of serotonin into the presynaptic terminals (allowing serotonin to stay in the synaptic cleft and exert its effect longer)

Question 31

mechanism of SNRIs

Answer 31

same as SSRIs, but also blocks reuptake of norepinephrine

Question 32

mechanism of tricyclics

Answer 32

block reuptake of all three synapses: serotonin, norepinephrine, and dopamine

Question 33

mechanism of MAO inhibitors

Answer 33

prevents MAO enzyme from breaking down neurotransmitters, therefore keeping neurotransmitters in the synaptic cleft for longer

Question 34

pharmacokinetics of antidepressants

Answer 34

• typically administered orally
• small dosages initially, increased slowly
• metabolized in liver

Question 35

side effects of antidepressants

Answer 35

most common: nausea, vomiting, diarrhea, constipation
less common: anticholinergic, cardiac effects, orthostatic hypotension

Question 36

What is the most serious side effect of SSRIs and SNRIs?

Answer 36

serotonin syndrome

Question 37

mechanism and symptoms of serotonin syndrome

Answer 37

excessive serotonin built up in brain can lead to sweating, restlessness, tremor, clonus, rigidity, progressing to seizures, coma, death

Question 38

what else are antidepressants used to treat?

Answer 38

chronic pain

Question 39

what is the primary drug used to treat bipolar disorder?

Answer 39

lithium

Question 40

side effects of lithium

Answer 40

possible toxicity (since lithium is not metabolized, only excreted in urine)

Question 41

four systems affected by lithium toxicity

Answer 41

CNS, GI, CV, renal

Question 42

rehab implications of antidepressants

Answer 42

• 2-4 week delay from start until effects
• depression may increase during this time
• 1/3 of patients with depression do not respond to meds