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Pharmacology > Lecture 9 - Sedative, Hypotics, Anxiolytics, and Antidepressants > Flashcards

Lecture 9 - Sedative, Hypotics, Anxiolytics, and Antidepressants Flashcards

1
Q

Non-rapid eye movement sleep - Stage 1

A
  • Somewhat aware of surroundings
  • short
  • alpha and theta waves
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2
Q

Non-rapid eye movement sleep - Stage 2

A
  • Unaware of surroundings
  • Easily awakened
  • Sleep spindles and K-complex
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3
Q

Non-rapid eye movement sleep - Stages 3 and 4

A
  • Deeper stages of sleep
  • Delta wave (larger waves)
  • important for physcial rest and restoration
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4
Q

Rapid-eye movement sleep

A

-Bursts of rapid eye movement (REM)
- Increased autonomic activity
- Dreaming

AKA paradoxical sleep

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5
Q
A
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6
Q

Define

Dreaming

A

The absence of motor fuction with the excpetion of the eye muscles and the diaphragm, occurs several times during sleep, and predominates towards morning

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7
Q

Describe the EEG patterns observed during the stages of sleep

A
  1. Awake - low voltage, random and fast waves
  2. Drowsy - 8-12 cps, alpha waves (slighty taller and closer together)
  3. Stage 1 - 3-7 cps, theta waves (farther apart)
  4. Stage 2 - 12-14 cps, sleep spindles (very fast clump of waves) and K complexes (one very large wave)
  5. Delta sleep - 1/2 to 2 cps, delta waves (very large waves), about 75 mV
  6. REM sleep - low voltage, random fast sawtooth waves)
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8
Q

Sedative-Hypnotic Drugs

Mechanisms of Action

A
  • Brain activity is highly affected by GABA
  • regulates the chloride channel –> reduces generation of action potentials
  • Most hypnotic drugs bind to specific receptor sites –> increases the inhibitory effects of GABA
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9
Q

Sedative-Hypnotic Drugs

Dosage (Low vs High)

A

Low Dosage - decreased activity of the reticular activation system (RAS), promotes sedation or sleep
High Dosage - depression of CNS, general anaesthesia, death

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10
Q

Classification of Sedatives and Hypnotics

Barbiturate - Effects on sleep cycle

A
  • Increase in stage 2 sleep
  • decrease in slow-wave sleep
  • Supression of REM sleep
  • Altered sleep structure
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11
Q

Classification of Sedatives and Hypnotics

Barbiturate - Effects and uses

A
  • Prolonged use can lead to tolerance and physical dependence
  • Overdose results in extensive cardiovascular and CNS depression –> hypotension and shock
  • No antidote for an overdose
  • No longer recommended as hypnotics
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12
Q

Classification of Sedatives and Hypnotics

Barbiturate - Phenobarbital

A

Death penalty drug

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13
Q

Classification of Sedatives and Hypnotics

Benzodiazepine - Mechanism and sites of action

A
  • Decrease the excitability and functional activity of specific areas of the brain
  • Limbic system, reticular formation, cerebral cortex, spinal cord
  • Do NOT function as general anaesthetics
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14
Q

Classification of Sedatives and Hypnotics

Benzodiazepines - Example drugs

A

Flurazepam, temazepam, triazolam, lorazepam

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15
Q

Classification of Sedatives and Hypnotics

Benzodiazepines - Effects on sleep cycle

A
  • Increased NREM stage 2 and decreased stage 4
  • No suppression of REM
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16
Q

Classification of Sedatives and Hypnotics

Benzodiazepines - Advantages

A
  • No REM rebound
  • Does not induce microsomal metabolizing enzymes
  • Well tolerated
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17
Q

Classification of Sedatives and Hypnotics

Benzodiazepine - Adverse effects

A
  • Drowsiness, confusion
  • Higher doses affect memory
  • Long term usage, abuse, and abrupt termination can cause dependency
  • Avoid during pregnancy
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18
Q

Classification of Sedatives and Hypnotics

Benzodiazepines - Drug interactions

A

Alcohol - coma and permenant brain damage
Cimetidine - inhibits the metabolism of benzos and prolongs the effects

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19
Q

Flumazenil

A
  • Benzodiazepine antagonist
  • may be administered intravenously to reverse depressant effects of the benzo drugs
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20
Q

Why do GABAa Receptors have large diversity?

A
  • GABAa recpetors exist as pentamers that form an anion selective channel
  • Possible arrangments of subunits are taken from three different types; alpha, beta, and gamma
    -GABAc receptors are formed from rho-subunits and are insenstitive to benzos and barbiturates
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21
Q

Subunit specific GABAa receptor agonists

Gaboxal

A

Targets benzo-insensitive alpha-4, beta-3, delta receptors
- In late stage clinical development for the treatment of insomnia

22
Q

Subunit specific GABAa receptor agonists

Alpha2/Aplha3 subunit selective agonists

A

Non-sedating anxiolytics

23
Q

Subunit specific GABAa receptor agonists

Alpha5 subunit inverse agonists

A

Memory enhancers

24
Q

Subunit specific GABAa receptor agonists

Zolpidem

A
  • GABAa receptor, alpha-1 subunit-selective compound
  • Short-term treatment of insomnia
25
Q

Classification of Sedatives and Hypnotics

Z-Drugs - Site of action

A

Selectively bind alpha-1 subunit of GABAa receptor

26
Q

Classification of Sedatives and Hypnotics

Z-drugs - Examples

A

Zopiclone, zaleplon, zolpidem

27
Q

Classification of Sedatives and Hypnotics

Z-drugs - Effects

A
  • Increased inhibitory effects of GABA
  • No anticonvulsant muscle relaxing, or anxiolytic effects
  • Cannot be used as general anaesthetics
  • Do not disturb sleep stages
  • Less physical dependence
28
Q

Classification of Sedatives and Hypnotics

Melatonin and Ramelteon

A

Melatonin is a hormone stimulated by a lack of sunlight, 1 hour half life
Ramelteon is a melatonin receptor agonist with a 2.6 hour half life

29
Q

Use

Zolpidem or Zopiclone

A

-Preferred therapy for insomnia

30
Q

Use

Flurazepam or Quazepam

A

For insomnia coupled with anxiety

31
Q

Use

Zaleplon or Ramelton

A

Helps induce sleep

32
Q

Use

Benzodiazepines

33
Q

Anxiolytics

Causes of anxiety

A

Overactive limbic system and situations that are interpreted as threatening or dangerous

34
Q

Anxiolytics

Percent of the US with GAD

35
Q

Antidepressants

What phenotype of mice recapitulates the core symptoms of human major depression?

36
Q

What is the Monoamine Theory of Major Depression?

A

Decreased levels of norepinephrine or seretonin lead to depression

37
Q

Antidepressants

What amino acid is serotonin made from?

A

Tryptophan

38
Q

Antidepressants

Antidepressant drug classes

A
  1. Selective serotonin reuptake inhibitors (SSRIs)
  2. Serotonin-norepinephrine reuptake inhibitors (SNRIs)
  3. Tricyclic antidepressants (TCAs)
  4. Monoamine oxidase inhibitors (MAOIs)
  5. Atypical antidepressants
39
Q

Classification of antidepressants

SSRIs - Mechanism of action

A

Blocks the reuptake of serotonin into the serotonergic nerve endings
- vary in degree of CNS activation (Lexapro - low, Prozac - high, Fluvoxamine - sedating)

40
Q

Classification of antidepressants

SSRIs - Clinical indications

A
  • Preffered therapy for major depression
  • Administered 1-2 times a day
  • No effect on adrenergic, cholinergic, adrenergic, or histamine receptors
  • Some SSRIs can treat anxiety, PTSD, and OCD
41
Q

Classification of antidepressants

SSRIs - Adverse effects

A
  • GI disturbances
  • sexual dysfunction
  • OD leads to serotonin syndrome
42
Q

Classification of antidepressants

SNRIs - Mechanism of action

A

Block the reuptake of norepinephrine and serotonin
- Little effect in blocking cholinergic, adrenergic, or histamine receptors

43
Q

Classification of antidepressants

SNRIs - Adverse effects

A
  • Increased blood pressure, heart rate, and CNS stimulation
  • Sudden discontinuation can lead to discontinuation syndrome
44
Q

Classification of antidepressants

TCAs - Mechanism of action

A

Blocks the reuptake of norepinephrine and serotonin, increased serotonin and NE levels contribute to the antidepressant effect

45
Q

Classification of antidepressants

TCAs - Pharmacological actions

A

Produces varying degrees of sedation, anticholinergic effects, and alpha-adrenergic blockade

46
Q

Classification of antidepressants

MAOIs - Mechanism of action

A

Inhibits or blocks MAOs (inhibit break down of NE, serotonin, and dopamine)

47
Q

Classification of antidepressants

Where is MAO found in the body?

A

MAO-A: Liver, GI tract, brain, other tissues
MAO-B: nervous system, blood platelets

48
Q

Classification of antidepressants

MAOIs - How long does it take to see the full effects?

A

2 to 4 weeks

49
Q

Classification of antidepressants

MAOIs - Dietary restrictions

A
  • Avoid foods containing tyramine (substance that causes the release of ME) such as wine, beer, herring, and some cheeses
  • Avoid sympathetic drugs that treat cold symptoms (broncodilators)
50
Q

Classification of antidepressants

Atypical antidepressants - Bupropion

A
  • NE-dopamine reuptake inhbitor
  • Useful for bipolar disorder
  • Increased dopamine and serotonin levels in the brain
51
Q

Classification of antidepressants

Atypical antidepressants - Mirtazapine

A
  • Acts as a sedative
  • Antagonizes serotonin 5HT2a and SHT2c receptors
52
Q

Classification of antidepressants

Atypical antidepressants - ketamine

A

Unknown mechanism of action

Pharmacology (18 decks)

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