Advanced Pharmacology: CNS drugs
1. Monoamines: dopamine, norepinephrine, serotonin
2. Dopamine: motor control, behavior, walking, sleep, mood, perception
3. Amino acids: GABA and glutamate
4. GABA: gamma aminobutyric acid, major inhibitory neurotransmitter, hyper polar- izes
neurons to treat anxiety, seizures, and insomnia, induce sedation and promote muscle
relaxation. Consists of A and B
5. Glutamate: excitatory neurotransmitter, activate to treat Alzheimer's, inhibit to treat
seizures
6. Schizophrenia, positive symptoms: Hallucinations, delusions, agitation
7. Schizophrenia, negative symptoms: Interpersonal withdrawal, loss of drive,
flattened affect
8. DSMIV criteria: Delusions, hallucinations, disorganized speech, grossly disorga- nized
and catatonic behavior, negative symptoms
9. Typical 1st generation AP MOA: Bind to and antagonize receptors in all central
dopamine pathways
10. Typical AP Pharmacological Effect: Alleviate positive sx only
11. Typical AP example: Haloperidol (Haldol)
12. Typical AP Adverse Effects: EPS, dystopia, tremor, akinesia (absence of mov't),
akathisia (restless), Tardive Dyskinesia, dry mouth, orthostatic hypoten- sion,
constipation, difficulty urinating, sedation, gynecomastia, prolactinemia, am- menorhea,
false positive hcg, weight gain
13. 2nd Generation Atypical APs MOA: Bind to receptors in mesolimbic and
mesocortial dopaminergic pathways (more selective). Greater affinity for dopamine
receptor subtypes found is these areas (d3, d4). Also bind to an antagonize serotonin receptors
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, 14. Atypical APs Pharmacological Effects: Alleviates both positive and negative sx
15. Atypical APs Examples: Clozapine (Clozaril), Olanzipine (Zyprexa), Risper- done
(Risperdal), Quetiapine (Seroquel).
16. Atypical APs Adverse effects: EPS, Anticholinergic effects, weight gain, hyper
salivation with Clozaril and Zyprexa and agranulocytosis with Clozaril
17. Abilify (Aripiprazole): Atypical AP, partial agonist of dopamine and serotonin 5-
HT1a receptor and antagonist activity at 5-HT2a. Has fewer side effects and is indicated
for schizophrenia, bipolar and depression
18. AP Considerations: Interact with any drug that causes CNS depression. Zyprexa
its are 10x more likely to develop or exacerbate DM. Prolongs QT inter- val-unknown if
vasoconstrictors have an effect, obtain CV consult
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10
1. Monoamines: dopamine, norepinephrine, serotonin
2. Dopamine: motor control, behavior, walking, sleep, mood, perception
3. Amino acids: GABA and glutamate
4. GABA: gamma aminobutyric acid, major inhibitory neurotransmitter, hyper polar- izes
neurons to treat anxiety, seizures, and insomnia, induce sedation and promote muscle
relaxation. Consists of A and B
5. Glutamate: excitatory neurotransmitter, activate to treat Alzheimer's, inhibit to treat
seizures
6. Schizophrenia, positive symptoms: Hallucinations, delusions, agitation
7. Schizophrenia, negative symptoms: Interpersonal withdrawal, loss of drive,
flattened affect
8. DSMIV criteria: Delusions, hallucinations, disorganized speech, grossly disorga- nized
and catatonic behavior, negative symptoms
9. Typical 1st generation AP MOA: Bind to and antagonize receptors in all central
dopamine pathways
10. Typical AP Pharmacological Effect: Alleviate positive sx only
11. Typical AP example: Haloperidol (Haldol)
12. Typical AP Adverse Effects: EPS, dystopia, tremor, akinesia (absence of mov't),
akathisia (restless), Tardive Dyskinesia, dry mouth, orthostatic hypoten- sion,
constipation, difficulty urinating, sedation, gynecomastia, prolactinemia, am- menorhea,
false positive hcg, weight gain
13. 2nd Generation Atypical APs MOA: Bind to receptors in mesolimbic and
mesocortial dopaminergic pathways (more selective). Greater affinity for dopamine
receptor subtypes found is these areas (d3, d4). Also bind to an antagonize serotonin receptors
1/
10
, 14. Atypical APs Pharmacological Effects: Alleviates both positive and negative sx
15. Atypical APs Examples: Clozapine (Clozaril), Olanzipine (Zyprexa), Risper- done
(Risperdal), Quetiapine (Seroquel).
16. Atypical APs Adverse effects: EPS, Anticholinergic effects, weight gain, hyper
salivation with Clozaril and Zyprexa and agranulocytosis with Clozaril
17. Abilify (Aripiprazole): Atypical AP, partial agonist of dopamine and serotonin 5-
HT1a receptor and antagonist activity at 5-HT2a. Has fewer side effects and is indicated
for schizophrenia, bipolar and depression
18. AP Considerations: Interact with any drug that causes CNS depression. Zyprexa
its are 10x more likely to develop or exacerbate DM. Prolongs QT inter- val-unknown if
vasoconstrictors have an effect, obtain CV consult
2/
10
