6. Psychiatric Drugs Flashcards

1
Q

What is the brain used for and consists of?

A
  • Coordination of mental activity
  • Consists of over 100 billion neurons – Neuron: nerve cell
    • Within cell → electrical transmission
    • Between cells → chemical transmission
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2
Q

What can a neuron do? Explain what a neuron is comprised of.

A
  • dentrites - receive info from other cells
  • cell body (soma)
    -axon - carries info away from cell body
  • axon terminal

*Within a neuron, an action potential can be generated and carried from dentrites –> cell body (soma) –> axon –> axon terminal

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3
Q

How do neurons communicate with one another?

A

with a neurotransmitter

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4
Q

What is neurotransmission and when does it occur?

A
  • Occurs by means of specific neurotransmitters at the synapse
    • Neurotransmitter: chemical that is released from the presynaptic neuron in response to an electrical signal
    • Synapse: junction between two neurons
  • A complex process involving neurotransmitter synthesis, storage and release, receptor activation, and neurotransmitter inactivation
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5
Q

Explain the process of neurotransmission. (hint: 4 steps)

A
  1. Synthesis
    • building blocks of a transmitter substance are imported into the terminal where the neurotransmitter is synthesized and packaged into vesicles
  2. Release
    • in response to an action potential, the transmitter is released across the membrane by exocytosis
  3. Receptor action
    • the transmitter crosses the synaptic cleft (presynaptic cleft –> postsynaptic cleft) and binds to a receptor
  4. Inactivation
    - the transmitter is either taken back into the terminal (presynaptic cleft) or inactivated by enzymes in the synaptic cleft
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6
Q

Is it male or females that visit physicians more?

A

Females

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7
Q

Why is there an increased prevalence?

A
  • inc awareness of disorders
  • diagnostic criteria has broadened
  • social behavour
  • less stigmatized in receiving help
  • diet
  • affects of covid
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8
Q

What are Psychiatric Disorders? Which age group do they usually affect?

A
  • A group of medical conditions characterized by alterations in thinking, mood, and/or behaviour
  • Associated with significant distress and impaired functioning over an extended period of time
  • Major economic impact
    • Health care system
      • estimated public and private mental health expenditure: $15.8 Billlion
    • Lost productivity (self and society) –> inc work of absences
      • ex. inc need for community care and hospital care
  • usually affects people in their 20s-30s
    • usually most productive, has burden in job and family wise
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9
Q

What are the causes of psychiatric disorders?

A
  • genetics
  • Neurodevelopmental defects
    • ex. alcoholism, malnutrition
  • Medical conditions
    • ex. infections, strokes
  • psychosocial experiences
    • emotional, physical or sexual abuse
  • Drugs
    • (e.g. substance abuse)
  • Stress
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10
Q

What are the 3 Subclassification of Psychiatric Disorders?

A
  • Mood disorders: depression, bipolar disorder
    • Changes in emotional state
  • Psychotic disorders: schizophrenia
    • Changes in thoughts and perception
  • Anxiety disorders
    • Excessive, persistent worry and/or fear

–> Negative impact on the quality of life!
- relationships, jobs, schooling, day-to-day activities…

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11
Q

What are Psychiatric Drugs used for and their fundamental requirements?

A
  • For treatment of psychiatric disorders
  • Fundamental requirements
    • Act in the central nervous system (the brain)
      • has to cross the blood-brain barrier
        • blood-brain barrier: prevent certain substances from getting in the brain
    • Influence neurotransmission by modulating neurotransmitter action
    • Cause changes in perception, mood, cognition and/or behaviour
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12
Q

4 characteristics of Psychiatric Drugs.

A
  • Do not “cure” → only decrease or relieve symptoms
    • we only know how to decrease symptoms
  • Wide spectrum of therapeutic activity
    • ex. sleep disturbance in depression and anxiety
  • Usually slow onset of therapeutic effects → may take weeks to improve symptoms
  • Often many side effects
    • not selective in their mechanism of action –> target other receptors
      –> more side effects
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13
Q

Explain the PK of Psychiatric Drugs.

A
  • Often administered orally
    • Very lipid soluble –> allow to pass blood-brain barrier and absorb through GI tract
  • Most are metabolised in the liver
  • Generally eliminated from the body by renal excretion (metabolites are water soluble)
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14
Q

What are the classifications of Psychiatric Drugs.

A
  1. Antidepressants: MAOIs, TCAs, SSRIs, SNRIs
  2. Mood stabilizers: lithium, anticonvulsants
  3. Antipsychotics: typical, atypical
  4. Anxiolytics: BZDs, azapirones
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15
Q

What is depression?

A
  • Characterized by feelings of severe despair over an extended period of time
  • Some people experience only a single episode in their lifetime, but most often people have multiple episodes
  • Affects ~8% of the population
  • Nearly twice as prevalent in women
    • may be due to hormonal differences
    • men more likely to seek help and acknowledge their symptoms
  • Average age of onset ~30 years old
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16
Q

What are the symptoms of depression/What is required for you to be considered to have depression?

A
  • need one of these…
    • depressed mood
    • apathy/loss of interest
  • and need 4 of these…
    • weight/appetite changes
    • sleep disturbances
    • fatigue
    • worthlessness
    • executive dysfunction
      • difficulty memorizing and concentrating
    • suicidal ideation
17
Q

What are antidepressants? What is its Theory of Treatment?

A
  • Indicated for the treatment of depression and anxiety disorders
  • Affect serotonin and/or norepinephrine neurotransmission
  • Theory of treatment: Monoamine Hypothesis
    • “Depression is associated with low levels of serotonin and norepinephrine in the brain”

*Please refer to slide 25 for procedure of how it works

18
Q

What are Monoamine Oxidase Inhibitors (MAOIs)?

A
  • Inhibit the enzyme monoamine oxidase, which breaks down monoamines (serotonin and norepinephrine)
    • therefore increase [neurotransmitter] in nerve terminal, available for neurotransmission
  • Must avoid foods and beverages that contain tyramine (e.g. cheese, red wine)
    • Risk of hypertensive crisis due to excessively high levels of norepinephrine
  • Last-line treatment for depression
19
Q

What are foods to avoid and allowed because it has tyramine?

A
  • Foods to avoid:
    • dried, aged, smoked, fermented, fish, and poultry
    • broad bean pods
    • aged cheeses
    • tap and unpasteurized beer
    • marmite and sauerkraut
    • soy products/tofu
  • Foods allowed
    • fresh or processed meat, fish, and poultry
    • all other vegetables
    • processed and cottage cheese, ricotta cheese and yogurt
    • brewer’s and baker’s yeast
20
Q

What do Tricyclic Antidepressants (TCAs) do? What are the side effects?

A
  • Prevent serotonin and norepinephrine reuptake by inhibiting the serotonin transporter (SERT) and the norepinephrine transporter (NET)
    • Increase [neurotransmitter] in synaptic cleft
  • Not very selective
    • High affinity for other additional receptors
  • Many side effects:
    • Anticholinergic effects
      • blurred vision, dried mouth and constipation
    • Orthostatic hypotension
      • dec in BP when a person goes from supine to upright position
    • Sedation, weight gain
    • Cardiac arrhythmia
21
Q

What do Selective Serotonin Reuptake Inhibitors (SSRIs) do? What are the side effects?

A
  • Prevent serotonin reuptake by selectively inhibiting SERT
    • Increase [serotonin] in synaptic cleft
  • Less side effects than TCAs and MAOIs, therefore safer and better tolerated
  • Side effects: nausea, headache, drowsiness, sexual dysfunction
    • minor compared to TCAs
  • First-line treatment for depression – Some approved for use in children
22
Q

What do Serotonin Norepinephrine Reuptake Inhibitors (SNRIs) do? What are the side effects?

A
  • Prevent serotonin and norepinephrine reuptake by selectively inhibiting SERT and NET
    • Increase [neurotransmitter] in synaptic cleft
  • Side effects similar to SSRIs

*same mechanism as TCA, difference is that SNRIs has higher selectivity

23
Q

Conclusion in depressants.

A
  • patients who have mild depression won’t get much benefits from antidepressants –> turn to other firms of treatment instead
  • antidepressants are effective in acute depressive episodes that are moderate to sever but are not effective in mild depression
24
Q

What is Bipolar Disorder?

A
  • Characterized by drastic mood changes – alternating between extreme “highs” (mania) and extreme “lows” (depression)
  • Affects ~1% of the population
  • Average age of onset ~25 years old
25
Q

What are the symptoms of Bipolar Disorder?

A
  • 4 of these required for manic phase
    • high energy
    • higher self esteem
    • racing thoughts
    • very quick talking
    • impulsive behaviour
    • irritability
    • reduced need for sleep
  • depressed phase (as previously said…)
    • lack of concentration
    • low self-esteem
    • suicidal thoughts
    • helplessness
    • loss of interest
    • low energy levels
26
Q

What are mood stabilizers?

A
  • Indicated for the treatment of bipolar disorder
  • Mechanism of action not clearly understood
  • In general more effective in treating mania than depression, therefore often used in combination with antidepressants
    • Antidepressant monotherapy should be avoided in patients with bipolar disorder

*antidepressants should not be used alone for the treatment of bipolar disorder –> can induce manic episodes and cause rapid cycling in moods

27
Q

What is Lithium and what is it used for?

A
  • A small monovalent cation (+1 charge)
  • an effective treatment for reducing the risk of suicide in people with mood disorders
  • Relatively slow onset of action (1-3 weeks)
  • Mechanism of action unclear
    • May alter signal transduction pathways
    • Possibly influence neurotransmitters and receptors
  • Not metabolised; excreted through the kidneys
  • comes in 2 forms: Lithium carbonate and lithium citrate
  • Very low therapeutic index (has narrow margin of safety)
    • Ineffective at blood levels <0.4 mmol/L while toxic when >1.5 mmol/L
    • Must monitor blood levels during treatment
  • Over 80% of patients experience side effects:
    • Tremor (usually in the hands)
    • Weight gain
    • Polyuria (↑ urine), polydipsia (↑ thirst)
    • Hypothyroidism (inc metabolic rate: tired and cold)
    • GI symptoms (vomiting, diarrhea)
28
Q

What are Anticonvulsants used for?

A
  • Only a few anticonvulsants are approved for the treatment of bipolar disorder
  • Specific mechanism unknown
    • Possibly act by reducing neuronal excitability
29
Q

What are the 2 forms Anticonvulsants come in? Explain their mechanism of action.

A
  • Carbamazepine: antagonist of MDA receptor
    • MDA - activated by excitatory neurotransmitter, glutamate. If MDA is blocked –> glutamate cannot bind = dec neuronal excitability
  • Valproic Acid
    • inc GABA transmission in the brain. GABA is the main inhibitory transmitter. It helps stabilize mood by reducing excitability.
30
Q

What is Schizophrenia?

A
  • Characterized by deficits in thought processes, perceptions, and emotional responsiveness
    • most lose contact with reality and don’t even realize it
  • Affects ~1% of the population
  • Typical onset in early adulthood
    • Late teens to early 30s
  • Symptoms classified as “positive” or “negative”