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BMB W11 > 10-25 L1 Antipsychotic drugs > Flashcards

10-25 L1 Antipsychotic drugs Flashcards

1
Q

What region of the brain is DA found as the neurotransmitter?

A
  • Striatum
  • DA/NE=25
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2
Q

What are the 4 major DA systems in the CNS? Which one is important in Parkinson’s disease?

A
  • Nigrostriatal
  • Mesolimbic
  • Mesocortical
  • Hypothalamic

Nigrostriatal is the most important one.

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3
Q

Which DA system in the CNS is a therapeutic target site of anti-psychotic drugs?

A

-mesolimbic system -mesocortical system

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4
Q

which DA system in the CNS is a site for adverse effects of anti-psychotic drugs?

A

-Hypothalamic -Nigrostriatal

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5
Q

What are the main therapeutic target of a typical antipsychotics?

A

DA systesm (in mesocortical & mesolimbic) pathways via D2 receptor antagonism.

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6
Q

Adverse effects of typical anti-psychotics?

A
  • Motor (EPS) DA systems in nigrostriatel pathways
  • Endocrine DA system in hypothalamic pathyways in D2
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7
Q

Describe the typical anti-psychotics action on other targets (due to lack of specificity for DA receptors) These are not clean drugs that affect only one or two targets.

A

-5-HT receptors muscarinic ACh receptors, alpha1-adrenegeric receptors H1-histamine receptors

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8
Q

Which drugs inhibits the synthesis of both DA & NE? (CARD)

A

-Cocaine (inhibits reuptake) -alpha-methyltyrosine (inhibits TH in both) -Reserpine (inhibits vesicular uptake) -D-Amphetamine (release neurotransmitter)

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9
Q

What is Desipramine’s action on NE and DA receptors?

A

inhibits reuptake in NE neurons (but not DA receptors)

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10
Q

“Typical” anti-psychotics are derivatives of what two basic chemical structures?

A
  • Phenothiazines
    • Chlorpromazine
  • Butyrophenones
    • Haloperidol
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11
Q

What is a prominent side effect of typical anti-psychotics?

A
  • movement disorders
    • EPS (extrapyramidal symptoms)
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12
Q

Name 4 pro-psychotic drugs and their action

A
  • Levodopa: Increases DA content
  • Amphetamine: enhances DA release
  • DA receptor agonist: activates DA receptors
  • Cocaine: Inhibits DA reuptake
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13
Q

Name 3 anti-psychotic drugs and their action

A
  • alpha-Methyltyrosine: inhibits DA synthesis
  • Reserpine: Depletes DA storage
  • DA receptor antagonists: inhibits DA signaling.
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14
Q

Describe the therapeutic lag of anti-psychotics

A
  • drugs reach their molecular targets w/in hours,
  • but therapeutic effects appear only weeks later
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15
Q

Provide examples of typical anti-psychotic drugs (1st generation or traditional antipsychotics)

(3 +5)

A
  • Chlorpromazine (Thorazine)
  • Fluphenazine (Prolixin)
  • Haloperidol (haldol)
  • perphenazine (Trilafon)
  • Prochlorperazine (Compazine)
  • Thioridazine (Mellaril)
  • Trifluoperazine (Stelazine)
  • Thiothixene (Navane)
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16
Q

For typical antipsychotics

  • Which DA recetpro is their therapeutic target?
  • Which DA receptor mediates antidopaminergic side effects
  • Do they interact with other (non-dopaminergic) systems
A
  • Which DA recetpro is their therapeutic target? D2
  • Which DA receptor mediates antidopaminergic side effects? D2
  • Do they interact with other (non-dopaminergic) systems: Yes they definitely do!
17
Q

What are extrapyramidal dopaminergic side effects of typical antipsychotics

A
  • acute dystonia
  • akathisia
  • Parkinsonism
  • Tardive dyskinesia
18
Q

acute dystonia

A

spasm of muscles of face, tongue, neck and back

19
Q

akathisia

A

motor restlessness

20
Q

Parkinsonism

A

Rigidty, tremor shuffling gait

21
Q

Tardive dyskinesia

A
  • oral-facial involuntary movements
  • choriform movement of extremities
  • Tardive= late
22
Q

NMS (Neuroleptic Malignant syndrome)

‘Haldol Hyperthermia’

A
  • Rare (<0.01%) but life threatening
  • Symptoms
    • Hyperthermia
    • Autonomic instability
    • Muscle rigidity
23
Q

What do you do, to treat NMS (Neuroleptic malignant syndrome)

A
  • Withdraw typical antipsychotic (DA receptor antagonist)
  • Cooling, hydration, supportive care
  • Dantrolene (muscle relaxant) for cooling
  • Bromocriptine (DA receptor agonist) b/c we are trying to block off the drug that drought this on.
24
Q

Define the endocrine dopaminergic side effects of typical anti-psychotics?

What is the change in level and outcome

PGC

A
  • prolatin (increase): increased lactation gynecomastia
  • Gonadotropins (decrease): inhibits ovulation, menses
  • Corticotropins (decrease): decreases adrenal corticosteroid secretion
25
Q

Atypical antipsychotics carry an increased risk for what disease?

A

type II diabetes

26
Q

Huntington’s chorea

mirror image of parkinson’s disease

  • genetic
  • presentation
  • cause
  • treatment
A
  • genetic: autosomal dominant, triplet repeat disease
  • Presentation: progressive chorea, dementia; incurable
  • Cause: Degeneration of striatal neurons
  • Treatment: halperidol (a DA receptor antagonist; which would exascerabte PD)
27
Q

Parkinsons Disease (PD)

vs.

Huntington’s disease (HD)

A
  • PD: underactivity in nigrostriatal pathways
  • HD: overactivity in nigrostratal dopamine pathways
28
Q

atypical (newer) anti-psychotic drugs differ from typical antipsychotic drugs by:

5 points

Atypical: full range of targets (and full mechanism) is unclear

A
  • chemcial structure
  • less EPS side effects (D2) **movement disorders
  • Few other (non-motor) DA side effects (e.g. endocrine)
  • Effective in some patietns who fail to respond to typicals. may be better than typicals for neg. symptoms
  • Less potent at D2 than many typicals: must be working also at other targets (5-HTreceptors? D4? alpha1? cholinergic?)
29
Q

Examples of atypical drugs

(5+3)

CORA-Q

A
  • Aripirazole (Abilify)
  • Clozapine (Clozaril)
  • Olanzapine (Zyprexa)
  • Risperidone (Risperdal)
  • Quetiapine (Seroquel)
  • ziprasidone (geodon)
  • asenapine (saphris)
  • palperidone (invega)
30
Q

What is the advantage of atypical vs typical?

A
  • Atypical have a wider window
    • adverse and therapeutic dosage wider apart
    • Has a higher Therapeutic index for EPS (than for typicals)
  • typical have a narrower window
    • adverse vs therapeutic close together
31
Q

List some advese affects for the prototype antipsychotics

A
  • typicals
    • EPS (increase)
    • Metabolic abnormalities (no change)
  • atypicals
    • EPS (some or no change)
    • Metabolic abnormalities (change)
32
Q

What is a major side effect of clozapine?

A
  • causes agranulocytosis (1-2% of patients genetic)
    • basophils and esoniphils thus greater risk of infections in these pts
    • also think what would happen in the immune compromised
  • thus testing is essential
33
Q

List the clinical problems with typical and atypical drugs

Both drugs: poor pt compliance

A
  • Typical
    • EPS (e.g. tardive dyskinesia)
    • Hyperprolactinemia
    • Neuroleptic malignant syndrome (NMS)
  • Atypical
    • Weight gain
    • metabolic problems
    • risk of type 2 diabetes
    • other adverse effects (vary drug to drug)
    • Notably higher risks in elderly and pediatric patients
34
Q

Cardiometabolic risk of atypical antipsychotics in youth

What two drugs increase in weight change and LDLchol change?

What drug do you see a change in glucose and insulin?

A
  • Olanzapine & Aripiprazole
  • Olanzapine
35
Q

Atypical antipsychotics have much less _ _ and much more _ _ than typical antipsychotics.

A

Atypical antipsychotics have much less extrapyramidal toxicity risk** and much more **metabolic toxicity risk than typical antipychotics.

36
Q

Typical and atypical have what similarities?

A
  • all drugs are lipid soluble
  • have large Vd
  • well-absorbed orally
  • cross BBB well
  • long t1/2
  • once/day dosing
37
Q

What is a solution to compliance (which is a big issue in this pt population)?

A
  • depot drugs (hydrophobic derivatives, given by IM injection)
  • t1/2= 1-6 weeks
38
Q

What is a significant risk in this pt population (that you perscribe antipsychotic drugs for )

A
  • suicide is a significant risk in this pt population
  • (but suicide by acute overdose of antipsychotic drugs is very difficult and very rare).

BMB W11 (9 decks)

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