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1. What are the 6 Safety
general Tolerability
principles of Efficacy
psychopharmaco- Practicality
logical Treatment accessibility
treatment? Treatment compliance
2. Pharmacokinet- How the drug moves in the body. (ex. Where is it absorbed? How and where is it
ics metabolized? Where is it excreted?)
3. Pharmacodynam- What the drug does to the body. (consider mechanism of action)
ics
4. Define First-gen- Referred to as Typical Antipsychotics. Most have strong bond with D2 receptors
eration antipsy- only, cause EPS symptoms faster due to prolonged receptor dissociation, have
chotics more dangerous side effect profiles, have been around longer, more effective
at treating positive symptoms, less expensive. (Ex. Haloperidol, Chlorpromazine,
Thioridazine, Fluphenazine)
5. Define Referred to as Atypical Antipsychotics. Most have a weak bond with D2 receptors
Second-genera- and block serotonin receptors leading to anti-depressive and anxiolytic effects.
tion They cause less EPS due to rapid receptor disassociation which leads to rapid
antipsychotics dopamine neurotransmission. Have less dangerous side effect profiles but can
cause metabolic syndromes, have been around shorter time, more expensive,
more effective at treating negative symptoms but can treat positive symptoms
as well, long-acting injections available for several of these. (Ex. Risperidone,
Clozapine, Quetiapine, Aripiprazole, Ziprasidone)
6. Extra Pyramidal Side effects caused by certain antipsychotic medications, which include: involun-
Symptoms (EPS) tary or uncontrollable movements. tremors. muscle contractions.
7. Tardive dyskine- A neurological disorder characterize by involuntary movement of the face and jaw.
sia
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8. Upregulation Occurs through chronic use of antagonists which causes an increase in the number
of receptors, externalization of receptors, and increased sensitivity of the receptors.
Prolonged use of antagonist -> Up-regulation of receptors -> Sudden withdrawal
of antagonist -> increased number of receptors and increased sensitivity of re-
ceptors *YOU MUST GRADUALLY TAPER A DRUG TO AVOID BINDING TO ALL NEW
RECEPTORS FROM UPREGULATION
9. Down regulation Occurs by chronic exposure of agonists which causes decreased number of recep-
tors, internalization of receptors, and decreased sensitivity of the receptors. Pro-
longed use of agonist -> down-regulation of receptors -> decreased effectiveness
of agonist mediated clinical response.
You have two options:
1 Increase the drug dose OR 2 Switch to another drug(BEST OPTION)
10. Receptor profile The receptors that each drug binds to
(example, risperidone's receptor profile would like...
(a) Blockade of 5HT2A and D2 receptors
(b) High affinity for a1, a2, and H1 receptors)
11. Binding Refers to a drug metabolite or neurotransmitter attaching to a receptor
12. Affinity refers to the "preference" or likelihood of a drug to bind to a certain receptor.
Linked to potency.
13. CYP450 A group of enzymes in the liver that metabolize different drugs. There are six.
14. List the 7 CYP450 (1) CYP1A2
Enzymes (2) CYP2B6
(3) CYP2C9
(4) CYP2C19
(5) CYP2D6
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(6) CYP3A4
(7) CYP2EI
15. CYP2B6 Metabolizes arteminsin, bupropion, cyclophosphamide, efavirenz, ketamine, and
methadone (2B6, there are two psych drugs (bupropion, methadone (keta-
mine...?) and six altogether.
16. CYP1A2 metabolizes AcetAminophen (two As)
17. CYP2C9 metabolizes Warfarin/Coumadin (think warfarin factors 2, C, 9)
18. CYP2C19 metabolizes PPIs, antidepressants, antiplatelet, antifungals, and anticancer drugs
(2C19, two see one, there is only one class of psych drugs that are metabolized,
you ONLY SEE one! antidepressants)
19. CYP2D6 Metabolizes Cardiovascular drugs (2-D echo, echo is a test for heart)
20. CYP3A4 Most common and ambiguous (if not above, then it's this one, a lot of psych drugs
are involved with this one)
21. CYP2EI ETOH (You have to be 21 to drink)
22. CYP450 inhibitors Decreases drug metabolism:
(1) Valproate
(2) Ketoconazole
(3) Isoniazid
(4) Sulfonamides
(5) Chloramphenicol
(6) Amiodarone
(7) All macrolides (think mycins) except azithromycin
(8) Quinidine
(9) Grapefruit juice
23. CYP450 inducers