Antipsychotics

Front 1

2 side effects of typical antipsychotics

Back 1

extrapyramidal symptoms (EPS) due to D2 receptor blockage in the nigrostriatal pathway (2) hyperproloactinemia: due to D2 blockage in the tuberoinfundibular system.

Front 2

Mechanism of action of typical antipsychotics

Back 2

blocking dopamine receptors (esp D2) in mesocortical and mesolimbic pathways

Front 3

What other receptors do most typical antipsychotic drugs have affinities for

Back 3

5-HT, histamine, a1 adrenergic and muscarinic receptors (each drug has unique receptor binding profile) (HAMS)

Front 4

two classes of typical antipsychotics/neuroleptics

Back 4

Phenothiazines (chlorpromazine)
Butyrophenones (Haloperidol or Haldol)

Front 5

Atypical antipsychotics are defined by reduced tendency to cause ______ and ______

Back 5

Atypical antipsychotics are defined by reduced tendency to cause EPS and Hyperprolactinemia

Front 6

Atypical antipsychotics are characterized pharmacologically by 2 things. what are they?

Back 6

Weak D2 dopamine receptor blocking. and Serotonin 2A (5HT-2A) receptor antagonism

Front 7

What does activation of presynaptic 5HT receptors on nigrostriatal dopaminergic neurons normally inhibit?

Back 7

dopamine release

Front 8

Where do atypical antipsychotics block D2 receptors (2 places). And what is the result?

Back 8

in the Striatum and in the presynaptic 5-HT2a receptors. The result is more dopamine is released from the nigrostriatal neurons and dopamine neurotransmission is partially rescued, leading to less EPS

Front 9

True or False? Since inhibition of dopamine release by 5HT2A receptors is not as prominent in mesocortical/mesolimbic pathways, antipsychotic effects arenot affect by 5 HT2A receptor antagonism

Back 9

True

Front 10

True or False. for unknown reasons, metabolic syndrome (weight gain 10#, hyperlipidemia, hyperglycemia) is more common with atypical antipsychotics

Back 10

True

Front 11

name 6 atypical antipsychotics

Back 11

clozapine, olanzapine, quetiapine, risperidone, aiprasidone, aripiprazole

Front 12

Name 3 extrapyramidal symptoms due to dopamine receptor blockage

Back 12

Parkinsonism, Tardive dyskinesia (repetitive involuntary choreoathetoid movements of the face, eyelidsetc.., Neuroleptic malignant syndrome (life threatening, result from escessively rapid blockage of postsynaptic dopamine receptors-NEED to give dopamine receptor agonist and/or muscle relaxant)).

Front 13

1. Prototype neuroleptic, inexpensive
2. Many side effects, especially autonomic, because of relatively high muscarinic and a1 receptor blocking activity
3. Highly sedative.

Back 13

Chlorpromazine (Thorazine®)

Front 14

1. Inexpensive, potent, relatively clean drug
with fewer autonomic effects 2. Severe EPS & hyperprolactinemia

Back 14

Haloperidol (Haldol®)

Front 15

1. Less likely to cause EPS (better compliance)
2. Most efficacious among antipsychotics (even effective against negative symptoms)
3. 1-2% of patients may develop agranulocytosis (reduction in the number of WBC): life threatening, mechanism not known
4. Other side effects: weight gain, sedation, hyperlipidemia, lowering seizure threshold
5. Only used for patients resistant to typical antipsychotics (effective for ~30-50% of refractory cases)
6. Strict blood monitoring is mandatory

Back 15

Clozapine (Clozaril®)

Front 16

1. __________ and risperidone are widely regarded as the second most effective atypical antipsychotic drugs (next to clozapine): currently, two most commonly prescribed antipsychotics in the US.
2. Relatively strong anti-histamine receptor (H1) antagonism
3. Side effects: sedation, metabolic syndrome, lowering seizure threshold

Back 16

Olanzapine (Zyprexa ®)

Front 17

- Structurally similar to clozapine
- Strong anti-histamine H1 antagonism (sedation, weight gain).

Back 17

Quetiapine (Seroquel®)

Front 18

1. Most potent D2 receptor blocker among atypical antipsychotics (associated with EPS and hyperprolactinemia at higher dose)
2. Much less potent anti-muscarinic activity

Back 18

Risperidone (Risperdal®)

Front 19

Number 1 atypical antipsychotic drug prescribed because its the most efficacious

Back 19

Clozapine

Front 20

The number 2 atypical antipsychotic drugs prescribed, 2nd most effective

Back 20

Olanzapine and risperidone

Front 21

This drug is not indicated for heart problem patients

Back 21

Zisprasidone

Front 22

Another name for abilify: its a partial agonist for D2, seratonin receptor antagonist

Back 22

Aripiprazole