Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Year 3 Pharmacology > Pharmacology of Anti-Depressants and Mood Stabilisers > Flashcards

Pharmacology of Anti-Depressants and Mood Stabilisers Flashcards

1
Q

Which drugs easily cross the BBB?

A

Lipophilic drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Uses of anti-depressants?

A

Moderate to severe depression

Dysthymia (AKA persistent depressive disorder, a less severe but more chronic form of depression)

Generalised anxiety disorder

Panic disorder, OCD, PTSD

Premenstrual dysphoric disorder

Bulimia nervosa

Neuropathic pain

i.e: used for more than just depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Classifications of anti-depressant drugs?

A

Monoamine oxidase inhibitors

Monoamine reuptake inhibitors:
• Tricyclics (TCAs)
• Other non-selective reuptake
• Selective serotonin reuptake inhibitors (SSRIs)

Atypical drugs (with post-synaptic receptor effects)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the monoamine neurotransmitters?

A
  1. Noradrenaline
  2. 5-HT
  3. Dopamine

NOTE - these share similar structures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the monoamine hypothesis?

A

Depression results from a functional deficit of monoamine transmitters, part. serotonin (5-HT) and noradrenaline

Drugs that deplete monoamine stores, e.g: reserpine, can induce low mood

This is because the CNS of a depressed patient has reduced monoamine (and metabolite) levels; also, most drugs that treat depression act to increase monoaminergic transmission

NOTE - this is too simplistic and the true mechanism of unknown

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Serotonin projection pathways?

A

Rostral pathway is IMPORTANT for mood, sleep, feeding behaviour and sensory perception

Caudal raphe is important for analgesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Describe transmission at the serotonergic synapse

A

Tryptophan (an amino acid) is converted to 5-OH-tryptophan, by tryptophan hydroxylase; this is then converted to 5-HT by L-AA decarboxylase

5-HT is stored in a vesicle and then released into the synapse, where it can bind to post-synaptic receptors

5-HT is then reabsorbed from the synaptic cleft, via a specific transporter, into the pre-synaptic neurone; MAO (monoamine oxidase) metabolises 5-HT to 5-HIAA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Noradrenaline projection pathway?

A

Locus coeruleus is important from arousal and emotion

Lateral tegmental area

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Describe transmission at the noradrenergic synapse

A

Tyrosine (an amino acid) is converted to DOPA, by tyrosine hydroxylase; this is then converted to dopamine, by L-AA decarboxylase

Dopamine is converted to noradrenaline, by DA β-hydroxylase, which is then stored in a vesicle and released into the synapse

Noradrenaline is reabsorbed into the pre-synaptic neurone, via a specific transporter, and is metabolised by MAO into MHPG

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Examples of MAO inhibitors?

A

Phenelzine

Moclobemide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Mechanism of action of MAO inhibitors?

A

Inhibit MAO-A and B and thus increase the conc. of NT in the pre-synaptic neurone, synaptic cleft and vesicles

MAO inhibition is:
• Irreversible - phenelzine
• Reversible - moclobemide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Side effects of MAO inhibitors?

A
  • ‘Cheese reaction’ and hypertensive crisis
  • Potentiates effects of other drugs, like barbiturates, by decreasing their metabolism
  • Insomnia
  • Postural hypotension
  • Peripheral oedema
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the ‘cheese reaction’?

A

‘Cheese reaction’ - eating too much cheese / gravy can result in inhibition of gut & liver MAO, due to irreversible inhibitors; this prevents breakdown of dietary tyramine

When combined with multiple drugs that potentiate amine transmission, e.g: pseudoephedrine and other anti-depressants, this leads to HYPERTENSIVE CRISIS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Examples of TCAs?

A
  • Imipramine
  • Dosulepin
  • Amitriptyline
  • Lofepramine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Mechanism of action of TCAs?

A

Block the pre-synaptic transporter, preventing reuptake of monoamines (mainly noradrenaline and 5-HT) non-selectively

This increases NT in the synaptic cleft

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Side effects of TCAs?

A 
Anti-cholinergic:
• Blurred vision
• Dry mouth
• Constipation
• Urinary retention

Sedation

Weight gain

CV:
• Postural hypotension
• Tachycardia
• Arrhythmias

If overdose, cardiotoxic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Examples of Selective serotonin reuptake inhibitors (SSRIs)?

A
  • Fluoxetine
  • Citalopram / escitalopram
  • Sertraline
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Mechanism of action of SSRIs?

A

SELECTIVELY inhibit reuptake of serotonin (5-HT), increasing conc. in the synaptic cleft

19
Q

Common side effects of SSRIs?

A

Nausea and headaches (usually improve after the 1st week)

Sweating

Vivid dreams

Worsening of anxiety (initially)

Sexual dysfunction

Hyponatraemia (in the elderly)

Transient increase in self-harm / suicidal ideation in those <25 YEARS

20
Q

Other issues with SSRIs?

A

Discontinuation effects

21
Q

Other monoamine reuptake inhibitors?

A

SNRIs (serotonin & noradrenaline reuptake inhibitors), e.g: venlafaxine, duloxetine

22
Q

Mechanism of action of SNRIs?

A

Block reuptake of monoamines (noradrenaline and 5-HT) into pre-synaptic terminals

23
Q

Side effects of SNRIs?

A

Similar to SSRIs

NOTE - they lack major receptor-blocking action so fewer side effects than TCAs, i.e: less anti-cholinergic and less anti-histaminergic

24
Q

Anti-depressant drugs that are noradrenaline selective?

A

Reboxetine

Maprotiline

Desipramine

Protriptyline

Nortriptyline

25
Anti-depressant drugs that are 5-HT selective?
Venlafaxine Paroxefine Fluvoxamine Sertraline Fluoxetine Citalopram
26
Anti-depressant drugs that are non-selective?
Amitriptyline Imipramine Clomipramine
27
Atypical anti-depressants?
Those with mixed receptor effects: • Mirtazapine (blocks α2, 5-HT2 & 5-HT3) Dopamine uptake inhibitors: • Bupropion
28
Side effects of mirtazapine?
WEIGHT GAIN AND SEDATION NOTE - if given with SSRIs, serotenergic side effects can be blocked
29
Efficacy of anti-depressants?
Most classes have a similar efficacy and most have delayed onset of action (several weeks)
30
When are anti-depressants most useful?
Clearer evidence for benefit in severe depression, i.e: there is a large placebo response in mild depression
31
Cautions in young adults / teenagers with anti-depressants?
Caution due to transient increase in suicide ideation / aggressive ideas
32
Levels of treatment in BPAD?
Acute treatment of symptoms: • To reduce mood in episodes of mania • To raise mood in episodes of depression Long-term treatment: • To stabilise mood and prevent recurrence of both mania and depression, i.e: for prophylaxis
33
Forms of lithium?
Normally given as lithium carbonate NOTE - different forms have different bioavailability, so be careful with doses if the type of lithium salt is changed, i.e: 600mg of lithium carbonate will have a different effect compared to 600mg of lithium citrate
34
Mechanism of action of lithium?
May block phosphatidylinositol pathway (2nd messenger system) OR inhibit glycogen synthase kinase 3β, i.e: uncertain
35
Cautions with lithium?
12 hour post-dose blood levels must be monitored, due to narrow therapeutic index
36
Common side effects of lithium?
Dry mouth / strange taste Polydipsia and polyuria Tremor Hypothyroidism Long-term reduced renal function Nephrogenic diabetes insipidus Weight gain
37
Toxic effects of lithium?
Vomiting and diarrhoea (this is a big issue, as this dehydrates the patients and makes the Li more toxic) Ataxia and coarse tremor Drowsiness Convulsions Coma
38
Uses of lithium?
Mood stabiliser
39
Which anti-convulsants are often used as mood stabilisers?
Valproid acid Lamotrigine Carbamazapine
40
Mechanism of action of anti-convulsants as mood stabilisers?
Unclear (perhaps they block overactive pathways)
41
Side effects of anti-convulsants?
``` Carbamazapine: • Drowsiness • Ataxia • CV effects • Induces liver enzymes ``` Volproate - TERATOGENICITY (neural tube defects); AVOID IN WOMEN OF CHILD-BEARING AGE
42
Which anti-psychotics are often used as mood stabilisers?
Quentiapine, aripiprazole, olanzapine, lurasidone
43
Mechanism of action of anti-psychotics?
Dopamine and 5-HT antagonism
44
Side effects of anti-psychotics?
Sedation Weight gain and metabolic syndrome Extra-pyramidal side effects, esp. with aripiprazole

Year 3 Pharmacology (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions