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Pharmacokinetics
Studies how the body acts on the drug
Pharmacodynamics
Studies how the drug acts on the body
First-generation antipsychotic
- first developed in the 1950s, first available treatment for psychosis
- aka typical antipsychotics
- increased risk for EPS, Tardive dyskinesia
- d2 blocker
- Currently 11 FDA-approved and commerically available FGAs
- Most common differences between individual FGAs are their potency and side effects
- examples include Thorazine (chlorpromazine), Haldol (haloperidol), Prolixin (fluphenazine),
perphenazine (Trilafon
,Second-generation antipsychotic
- examples include Abilify (aripiprazole), Seroquel (quetiapine), Zyprexa (olanzapine), Risperdal
(risperidone), Clozaril (clozapine)
- lower risk of EPS symptoms compared to 1st gen
- higher risk of metabolic side effects
- serotonin-dopamine receptor antagonists
- AKA atypical antipsychotics
EPS
Involuntary movements that occur as a side effect to certina medications. AKA drug induced
movement disorder. May include tardive dyskinesia, dystonic reactions, parkinsons-like
symptoms, akathesia, NMD, akinesia
- Can be acute or chronic
- related to suppression of D2 dopamine receptors in the nigrostriatal pathway
Tardive dyskinesia
- characterized by involuntary movments in the face and body
- often induced by long-term use of anitpsychotic drugs
- can be associated with use of other medication types (antidepressants, lithium,
antihistamines)
- more common with 1st gen antipsychotics
- movements may include: writhing, mouth puckering, tongue rolling, lip smacking, pill rolling,
tongue protrusion
,Upregulation
Refers to the activiation of the nervous system. Is the process by which a cell increases its
response to a subtance or signal from outside the cell to carry out a specific response
downregulation
Refers to state of calm/relation within nervous system. Characterized by a decreased response
by a cell to a molecule or neurotransmitter.
Receptor Profiles
FGA - Primarily D2 antagonism. Also antagonize M2, H1, and a1 receptors
SGA - 5-HT2A & D2 antagonism. Rapid D2 dissociation. 5HT2A agonism. Also antagonizes M2,
H1, 5HT2C, and a1 receptors
Binding
When a neurotransmitter binds to a receptor on a receiving cell, it causes ion channels to open
or close.
Affinity
The property of a drug that describes its ability to bind to a receptor
Constant
Unique for each drug-receptor pair as it is dependent on each of their structures
, CYP450
- membrane-bound hemoproteins that play a pivotal role in the detoxification of xenobiotics,
cellular metabolism, and homeostatis
-Inhibitition or induction of CYP enzymes is a major mechanism underlying drug-drug
interactions
- A CYP450 inhibitor prevents or reduces work by CYP450 enzymes = decreased drug
metabolism and increased risk for toxicity
- A CYP450 inducer increases rate of hepatic metabolism = decreased serum concentation of
other drugs metabolized by the same hepatic isoenzyme
Grapefruit juice is an inhibtior, which can increase serum levels of certain drugs
Dopamine Pathways
- mesolimbic (positive sx)
- mesocortical (negative sx)
- nigrostriatal (EPS)
- tuberoinfundibular (prolactin)
Metabolic Syndrome
cluster of conditions that incerase risk for T2DM and cardiovascular disease (obesity, HTN, high
triglycerides, low HDL, insulin resistance)
-increased risk for metabolic syndrome found with some antipsychotic medications, primarily
SGA
High Potency vs Low Potency