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Medicinal Chemistry - Winter > 6 - Antidepressants > Flashcards

6 - Antidepressants Flashcards

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1
Q

What are the 5 types of depression?

A

1) Major depression
2) Chronic depression
3) Atypical depression
4) Bipolar/manic depression
5) Seasonal depression

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2
Q

What is major depression?

A
  • Generally recurring and disabling w/ sx that interrupt a persons ability to work, sleep, study, or eat
  • Usually lasts greater than 2 weeks
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3
Q

What is chronic depression?

A
  • Less severe or disabling
  • Longer lasting sx
  • Characterized by long term “melancholy” or depressive personality
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4
Q

What is atypical depression?

A
  • Characterized as less pervasive sadness

- Can manifest as overeating, oversleeping, sensitivity, or rejection

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5
Q

What is bipolar/manic depression?

A

Oscillates btwn major depressive and mania episodes

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6
Q

What is seasonal depression?

A
  • Result of a reduction in amount of sunlight
  • Common during winter
  • Scandinavian countries most affected
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7
Q

How is a person diagnosed w/ depression?

A
  • Must have 1 of top 2 symptoms and at least 5 other sx which occur daily, and persist for at least 2 weeks
  • Top 2 sx = persistently sad, anxious, or “empty” feelings and loss of pleasure in usual activities
  • Other sx = crying, hopelessness, pessimism, helplessness, fatigue, loss of concentration, sleep problems, change in appetite, suicidal thoughts
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8
Q

What are the causes of depression?

A
  • Genetic
  • Death/abuse
  • Medication
  • Socio
  • Environment
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9
Q

What are the various tx for depression?

A
  • Psychotherapy (talk therapy) – useful when combined w/ drugs
  • Natural alternatives – St. John’s Wort and exercise can help mild depression
  • Electroconvulsive therapy (ECT) – fast and effective solution for major depression or suicidal thoughts
  • Medications – SSRIs, SNRIs, NDRIs, MAOIs, TCAs, and TeCAs
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10
Q

What are sx of serotonin deficiency?

A
  • Anxiety
  • Panic
  • Phobia
  • Obsessive compulsive
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11
Q

What are sx of norepinephrine deficiency?

A
  • Decreased concentration, working memory, and info processing
  • Fatigue
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12
Q

What are sx of dopamine deficiency?

A
  • Cognitive slowing
  • Hypersomnia (excessive sleepiness)
  • Anhedonia (inability to feel pleasure)
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13
Q

What are sx of serotonin and dopamine deficiencies?

A
  • Food craving

- Bulimia

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14
Q

What are sx of dopamine and NE deficiencies?

A
  • Decreased attention

- Psychomotor retardation

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15
Q

What are sx of serotonin, NE, and dopamine deficiencies?

A

Depressed mood

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16
Q

What does it mean when an antidepressant has a high NE/5-HT ratio?

A

The drug is more selective for 5-HT receptor

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17
Q

What is the function of serotonin?

A

Regulates mood, calmness, appetite, cognitions, memory, body temp, sexuality, and BP

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18
Q

Can circulating serotonin cross the BBB?

A

No, but serotonin is derived from tryptophan, and tryptophan can cross the BBB (but must compete w/ other AAs for the active AA transporters)

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19
Q

Is the indole ring of serotonin basic?

A

No

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20
Q

What percentage of tryptopharn consumed is converted to serotonin?

A

5%

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21
Q

Where does biosynthesis of serotonin occur?

A

Primarily in CNS presynaptic neurons and some GI tract cells

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22
Q

What happens to free 5-HT in blood plasma?

A

Rapidly taken up by platelets for storage

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23
Q

What does 5-HT stand for?

A

5-hydroxytryptamine

24
Q

How is serotonin removed from the synaptic cleft?

A
  • Removed by diffusion

- Binds to SERT receptor or 5-HT autoreceptor of serotonergic neuron

25
Q

How is serotonin removed from a serotonergic neuron?

A

MAO inactive metabolites

26
Q

How is serotonin released into a synapse?

A
  • Action potential causes influx of Na+ and Ca+
  • Increase in Ca+ in cytoplasm causes storage vesicles to fuse w/ presynaptic cell membrane, releasing 5-HT into synaptic cleft
27
Q

5-HT reuptake is through the _____ on ______

A

Serotonin transporter (SERT); presynaptic membrane

28
Q

What is the half life of free serotonin in blood? Why?

A

Short (few minutes) b/c of fast metabolism by MAO

29
Q

What is produced from a minor route of 5-HT metabolism? How?

A
  • Melatonin
  • 5-HT is acetylated by 5-HT n-acetyltransferase to N-acetylserotonin, which is converted to melatonin y 5-hydroxyindole-O-methyltransferase (HIOMT)
30
Q

Can melatonin cross the BBB?

A

Yes b/c not charged

31
Q

What regulates the production of melatonin?

A

Light in the retina inhibits production

32
Q

How is melatonin metabolized? Where does this take place?

A
  • Melatonin is oxidized at position 6, followed by conjugation w/ sulfate
  • Occurs in CNS
33
Q

Do melatonin metabolites posses pharmacological properties?

A

Yes

34
Q

What are the 2 main methods to modulate the effects of serotonin?

A
  • Increase or decrease amount of serotonin (biosynthesis, release into synapse, metabolism, diffusion, reuptake)
  • Agonism or antagonism of serotonin receptor
35
Q

What are the 4 main classes of antidepressants?

A

1) Tricyclic antidepressants and tetracyclic
2) Selective serotonin reuptake inhibitors
3) Selective norepinephrine reuptake inhibitors
4) Monoamine oxidase inhibitors

36
Q

What happens to the ring angles when chlorpromazine is converted to amitriptyline and then imipramine? What does this cause?

A
  • Alpha angle is decreased in amitriptyline, and the beta and gamma angles are introduced in imipramine
  • This causes decreased affinity for dopamine receptor, allowing TCAs to have no dopamine antagonism; and increased affinity for NE and serotonin reuptake transporters
37
Q

How do TCAs work?

A

By competitively inhibiting serotonin or NE reuptake (generally more selective for NE transporter)

38
Q

What almost always happens when a terminal methyl group is attached to an N or O?

A

N or O will be demethylated

39
Q

Which type of amine on a TCA elicits the most selectivity for the serotonin transporter?

A

Tertiary

40
Q

Which type of amine on a TCA elicits the most selectivity for the NE transporter?

A

Secondary

41
Q

For SSRIs, the _____ group probably explains selectivity

A

Electron withdrawing

42
Q

What type of antidepressants are venlafaxine and duloxetine?

A

SSNRIs

43
Q

What are paroxetine and citalopram? What are their indications?

A
  • Potent and most specific SSRIs

- Used in tx of major depression, OCD, PTSD, and panic disorders

44
Q

What are atomoxetine and reboxetine? Why? What are their indications?

A
  • Selective NE reuptake inhibitors
  • Lack a strong electron withdrawer on the phenyl ring (such as fluorine), decreasing serotonin selectivity
  • Atomoxetine used for ADHD and reboxitine for depression
45
Q

What do TCAs inhibit?

A

Serotonin, norepinephrine, and dopamine

46
Q

What part of the serotonin transporter do TCAs and SSRIs interact w/?

A

Asp-98

47
Q

For SSRIs, the ____ residue appears to be determining factor in SSRI potency

A

Ser-438

48
Q

What is the primary effect of MDMA?

A
  • Openness
  • Euphoria
  • Empathy
  • Love
49
Q

What is MDMA believed to cause?

A

Serotonin vesicles to release serotonin into synapses

50
Q

What can acute toxicity of MDMA lead to?

A

Hyperthermic syndrome, dehydration and hyperpyrexia

51
Q

What are SSRIs the most commonly used drugs in depression therapy?

A
  • Fewer adverse side effects and less toxicity than TCAs and MAOIs
  • Don’t exhibit food-interaction toxicity, unlike MAOIs
  • Diminished anticholinergic effect, unlike TCAs
52
Q

What are some discontinuation sx of SSRIs?

A
  • After taking SSRIs for more than 6 weeks, w/in 3 days of discontinuation experience flu-like sx, insomnia, nausea
  • Can occur when switching SSRIs
53
Q

When is serotonin syndrome a concern?

A

When combining SSRIs and MAOIs

54
Q

What are some agents that can cause/induce serotonin toxicity?

A
  • Tryptophan or 5-HTP (increase serotonin production)
  • Amphetamines, MDMA (increase serotonin release)
  • SSRIs, cocaine, TCAs (inhibit serotonin re-uptake)
  • MAOIs (inhibit serotonin metabolism)
55
Q

What are common structural features of all TCAs?

A
  • Terminal secondary or tertiary nitrogen (protonatable)
  • 2 aromatic rings, attached by middle ring
  • Around 4 atom distance from protonatable nitrogen and aromatic ring

Medicinal Chemistry - Winter (15 decks)

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