Neuro 6 Flashcards
_________________ drugs do not cause Extra-pyramidal effects at clinically effective doses
“atypical” anti-psychotic
what is the prototype “atypical” antipsychotic drug
clozapine
what is the prototype neuroleptic antipsychotic drug
thorazine
what is psychosis
- denotes a variety of mental disorders 2. presence of delusions 3. various types of hallucinations 4. grossly disorganized thinking
excessive ___________________ plays a role in psychosis
limbic dopaminergic activity
what is the most common type of psychosis
schizophrenia
what are the 2 clusters of behavior seen with schizophrenia
positive symptoms negative symptoms
positive symptoms of schizophrenia are defined as
something that is added to the situation, i.e. something that should not be there
delusions, hallucinations, reality distortions, bizzarre and agitated behavior are all ______________ symptoms seen with schizophrenia
positive
positive symptoms of schizophrenia are mediated by ___________ receptors
D2
what would define schizophrenic negative symptoms
lack of something that should be there
flat affect, emotional/social withdrawal are examples of _____________ symptoms with schizophrenia
negative
what receptor mediates the negative symptoms seen with schizophrenia
5-HT receptor (esp the 5-HT2A)
diminished ____________ or _____________ activity underlies the cognitive impairment and negative symptoms seen with schizophrenia
cortical; hippocampal
_________-_________% of schizophrenics are drug resistant
20-25
in general, anti-psychotic drugs tend to be _________________ antagonists
serotonin
what is the MOA of clozapine
inverse agonist of the 5HT2A receptor and anatagonizes the D2 receptor
which drug will treat the positive and negative symptoms of schizophrenia
clozapine
clozapine has greater affinity for the ____________ receptor over the _________ receptor
5HT2A; D2
what is the normal fx of the 5HT2A receptor
- depolarizes glutamate neurons 2. stabilizes NMDA receptors on the post-synaptic neuron
clozapine main MOA is with the antagonism of serotonin and D2 receptors; however, if also has some blockade effects on __________, _________, and _________ receptors
alpha; muscarinic; H1
clozapine is used in the tx of what d/o’s
- schizophrenia (positive and negative sx) 2. some benefits in tx agitation with alzheimers and parkinsons
general absorption of anti-psychotics
- readily but not complete absorbed 2. significant first pass metabolism
general distribution of anti-psychotics
- highly lipid soluble and protein bound 2. large Vd 3. longer clinical duration of action than indicated by their 1/2 life
general metabolism of anti-psychotics
- almost completely metabolized to by oxidation or demethylation by CYP450 nz in the liver
____________________ is an antipsychotic that may be excreted in the urine weeks after the last dose of chronically administered drug
chlorpromazine
what is the only antipsychotic that has rapid and severe return of symptoms after discontinuation
clozapine
what is the average time for schizophrenic sx return in pts who d/c their meds?
6 months (exception with clozapine)
efficacy of anti-psychotics is driven by ___________ receptor blockade
D2
adverse reactions of anti-psychotics are d/t antagonism at what receptors?
- alpha 2. Muscarinic 3. H1 4. 5-HT2
MOA of typical (neuroleptic) anti-psychotics
act as D2 antagonists w/ primary action at the mesolimbic and mesocortical regions of the brain
D2 receptor blockade in the __________________ and ______________ pathways mediate some of the side-effects of typical (neuroleptic) anti-psychotics
basal ganglia ; tuberoinfundibular
MOA of atypical antipsychotics
mild D2 receptor antagonists combined with serotonin 5-HT2 receptor blockade (5HT2 > D2)
atypical antipsychotics main MOA is on D2 and 5HT2, but they also have high affinity for _____________ & ______________ receptors
5-HT2c & D4
Therapeutic uses of anti-psychotics
- tx of psychoses 2. tx of schizophrenia 3. mood stabilizers (atypical) 4. tourettes 5. ADD 6. antiemetics 7. intracatable hiccups
in schizophrenia tx, _______________ anti-psychotics are only useful with positive sx; however, ___________________ fx in tx of both positive and negative sx
typical; atypical
what are the general s/e of antipsychotics
- severe sedation 2. anti-cholinergic effects 3. parkinsonian like tremors 4. hyperlactinemia 5. Hypotension
why do you get hyperlactinemia with antipsychotic meds
dopamine is the inhibitor of prolactin. The MOA of most antipsychotics fx as dopamine antagonists thus removing the inhibitory effect of dopamine on PRL
MOA of chlorpromazine
blockade of D2 receptors»_space; 5HT2A receptors
clinical applications of chlorpromazine
- schizophrenia (alleviates positive sx) 2. bipolar disorder (manic phase) 3. anti-emesis 4. pruritus
T/F: many anti-depressants are now FDA approved for things outside of depression
TRUE
anti-depressants treat what?
- Psychologic depression: major depressive disorder & dysthymia 2. anxiety disorders (PTSD, OCD, Generalized anxiety d/o, panic d/o, phobias) 3. bipolar disorder (manic depressive dz) 4. chronic pain 5. premenstrual dysphoric disorder 6. smoking cessation 7. eating disorders
________________ is unipolar, often totally disabling, interferes with work, sleep, and eating
major depressive disorder
_____________ less severe the major depressive disorder, involves long term chronic sx that do not disable, but keep a person from functioning at their highest level
dysthymia
__________________ is characterized by cycles of severe highs and gut wrenching lows, often develops into psychotic states
bipolar
_____________________ increase the risk of suicide in pts under the age of 25
anti-depressants
what meds can have discontinuation syndromes
SSRI SNRI TCA MAOI
discontinuation syndrome sx with SSRI, SNRI, and TCAs?
- dizziness and paresthesias beginning 1-2 days after sudden d/c of drug 2. may persist for 1 wk or longer
discontinuation syndrome with MAOIs
delirium like state with psychosis, excitement, and confusion
(general) peak absorption of anti-depressants is at ____________ hours
3-Feb
