8. Antipsychotics - Intro Flash Cards

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Title:	8. Antipsychotics - Intro
Description:	test
Number of Cards:	64
Save Count:	0
Author:	kerenjill
Created:	2008-03-24
Tags:	pharm3
Private	No

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- Question
- Answer
- Side 3

- What is the general term for major mental disorders characterized by derangement of personality and loss of contact w/ reality?
- Psychosis
- What are the symptoms of psychosis?
- Hallucinations and delusions
- What are 3 causes of psychosis?
- -Schizophrenia
  -Drugs
  -Organic brain diseases
- What is schizophrenia?
- Deranged thinking but with intact sensorium
- What are the pos symptoms of schizophrenia?
- -Hallucinations
  -Behavioral disturbances
  -Delusions
- What are the neg symptoms of schizophrenia?
- -Flattened affect
  -Alogia
  -Amotivation
- What is schizophrenia caused by?
- Unknown
- What is the most likely HYPOTHESIS for etiology of schizophrenia?
- Dopamine hypothesis
- What is the DA hypothesis?
- -Excess/hyperactivity of DA in mesolimbic areas of brain
  -Deficient DA in mesocortical areas
- What does Excess/hyperactivity of DA in mesolimbic areas of brain result in?
- Positive symptoms
- What does Deficient DA in mesocortical areas result in?
- Negative symptoms
- What are the 4 dopamine pathways in the brain? What is the function of each?
- -Nigrostriatal - movement
  -Tuberoinfundibular - Prl
  -Mesolimbic - arousal/motivation
  -Mesocortical - cognition and executive function
- What happens to the nigrostriatal pathway in schizophrenia treatment with antipsychotics
- DA blockade leads to parkinsonism symptoms
- What does DA in the tuberoinfundibular pathway normally do?
- Inhibits prolactin secretion
- What does blockade of DA receptors in treatment for Schizophrenia result in?
- Galactorrhea via increased Prl secretion
- What does DA hyperactivity in the mesolimbic pathway result in?
- Positive sx - hallucinations, delusions, behavioral disturbances
- What does decreased dopamine in the mesocortical pathway result in?
- Neg sx - amotivation, social withdrawal, etc.
- What are the 3 main types of DA receptors?
- D1-like
  D2-like
  Autoreceptors
- What are the 2 D1 type receptors?
- D1 and D5
- What is the mechanism of the D1-like receptors?
- Gs stimulates Adenylyl cyclase
- What are the 3 D2 receptors?
- D2, D3, and D4
- What is the mechanism of the D2 type receptors?
- Gi inhibits adenylyl cyclase
- What do most of the antipsychotic drugs act on?
- D2-type receptors
- What are the Dopamine autoreceptors like?
- D2-like
- What is the function of DA autoreceptors?
- To sense DA in the synapse and decrease its synthesis and release
- How do DA autoreceptors affect the actions of drugs that block postsynaptic DA receptors?
- Initially DA release increases from the presynaptic neuron due to autoreceptor blockade by the drug, so it overcomes the D2 receptor block
- When are maximum effects of DA receptor blockers seen?
- When autoreceptor tolerance develops so the DA blockade is effective
- So why is the maximal effect of most antipsychotics delayed?
- Because most antipsychotics block BOTH D2 and autoreceptors
- What do the Atypical antipsychotics block in addition to D2 receptors?
- 5HT-2 receptors
- So what is the mechanism by which all antipsychotic drugs act on DA neuronal function?
- Block D2 receptors (and some block 5HT2 receptors)
- What are 4 important pharmacokinetic properties of antipsychotics?
- -Highly lipophilic
  -High protein binding
  -Large apparent Vd (>TBW)
  -Long half lives
- What is the plasma half life of most antipsychotics?
- Less than a day
- Why can the antipsychotics be detected in patients so many days after administration?
- Because they accumulate in fat so that their effective half lives are much longer than plasma half lives.
- What is the most reliable method of administration of antipsychotics?
- Parenteral
- What is the metabolism of antipsychotics like?
- Complex
- What is the important thing to remember about treating schizophrenia with drugs?
- It is the most common effective therapy but NOT CURATIVE.
- How do the antipsychotic drugs compare in general?
- -SAME mechanism of reducing psychotic behavior
  -WIDELY VARY in potency and incidence of side effects
- What correlates almost linearly with the potency of the antipsychotic drugs?
- Their affinity of binding to D2 receptors
- What were the first 2 antipsychotic drugs that were discovered serendipitously?
- Reserpine and Chlorpromazine
- How does Reserpine work?
- Blocks VMAT transporters so less DA is released
- What is Reserpine more commonly used for than antipsychosis?
- Anti-hypertensive
- So what is the only way that the antipsychotic drugs differ?
- POTENCY
- What is the implication of antipsychotic drugs differing in potency?
- Not all symptoms of schizophrenia are equally well treated
- What class of antipsychotic drugs DO have equal efficacy AND potencies?
- Atypicals - ie Clozapine
- What are the 3 receptor types that Typical Antipsychotics block?
- D2
  Cholinergic muscarinic
  Histamine
- What effect is produced as a result of Histamine receptor blockade?
- Sedation
- When is Sedation more pronounced with the typical antipsychotics?
- After large doses of low potency drugs
- What happens to the sedation effects of typicals over time?
- Tolerance develops
- What is a major side effect of the typicals due to DA rec blockade?
- Extrapyramidal symptoms EPS
- What are the 4 main EPS?
- -Dystonia
  -Parkinsonism
  -Akathesia
  -Tardive dyskinesia
- What is Dystonia? How soon does it develop after starting the drug?
- Spasms of the tongue/face/back and neck - 1-5d
- What is Parkinsonism? How soon does it develop after starting the drug?
- Bradykinesia, masked facies, tremor and rigidity; 5-30 days
- What is Akathesia? How soon does it develop after starting the drug?
- Compulsive, restless movements
  -Weeks to months
- What is Tardive Dyskinesia? How soon does it develop after starting the drug?
- Oral facial movements and lip smacking - a late reaction that develops mo-yrs after starting.
- Which EPS can be treated with Anticholinergic drugs? Which can't?
- CAN treat: Dystonia, Parkinsonism, Akathisia
  
  CAN'T treat: tardive dyskinesia
- What anticholinergic effects can the typical antipsychotics cause?
- Dry mouth
- What are 3 neuroendocrine changes that can be seen due to DA rec blockade?
- -Increasd prolactin/Galactorrhea
  -Gynecomastia
  -Amenorrhea
- What side effect can the typicals produce via a-adrenergic blockade?
- Orthostatic hypotension
- What antipsychotic drug is most toxic to the heart?
- Thioridazine
- What side effect is particulary seen with phenothiazines?
- Decreased seizure threshold
- What is a problem with antipsychotics?
- Weight gain
- What is a side effect of antipsychotics that has potential for FATALITY?
- Neuroleptic Malignant syndrome
- What are 4 symptoms of NMS?
- -Fever
  -Mutism/rigidity
  -Severe EPS
  -Death
- What are 3 components of treatment for Neuroleptic Malignant syndrome?
- -Cooling/rehydration
  -Muscle relaxant - Dantrolene
  -DA agonist - Bromocriptine