Pharmacology Psychosis Sgas

Front 1

Contrast FGA and SGA drugs

Back 1

-SGAs have much less D2 receptor blocking activity and much more 5HT2 receptor blockign activity
-5HT2 neurons in the brain mudlate dopaminergic transmission
-SGAs hav a higher D4 receptor affinity
-D4 not presence in the tuberoinfundibular or nigrostriatal pathways so lower incidence of neurological side effects

Front 2

What are the SGAs?

Back 2

Clozapine
Risperidone
Olanzapine
Paliperidone
LY2140023

Front 3

What is the prototype atypical antipsychotic? What type of symptoms are treated?

Back 3

Clozapine
Both negative and positive symptoms and some refractory patients

Front 4

Describe what receptors clozapine affects

Back 4

-Blocks the mesolimbic dopaminergic tract without blocking the nigrostriatal dopaminergic tract.
-No extrapyramidal effects and no tardive dyskinesia
-Blocks D3, D4, and 5HT2 receptors
-Low affinity for D2 receptors
-No prolactin elevating effects and little effect to increase dopamine receptor number or affinity
-Alpha1 and H1 blocking activity
-Some anticholinergic effects

Front 5

What are the side effects of clozapine?

Back 5

-Agranulocytosis (greater in the first 6 months)
-High incidence of seizures (dose dependent)
-Gastric and cardiac effects
-Sialorrhea
-Weight gain

Front 6

How is clozapine administered?

Back 6

Orally

Front 7

What is risperidone effective for?

Back 7

Treatment of psychotic disorders including acute and chronic schizophrenic psychoses.
-Both negative and positive symptoms

Front 8

Describe the mechanism of action for risperidone

Back 8

-Blocks D2 receptors with much less afinity than halperidol but greater than clozapine
-Blocks 5HT2 receptors

-Blocking D2 receptors -> helps treat positive symptoms
-5HT2 blockage in mesocortical tract -> decreases negative symptoms

Front 9

Describe the side effects of risperidone

Back 9

-Extrapyramidal symptoms at high doses (mostly avoided at therapeutic doses)
-No agranulocytosis
-Low seizure frequency
-Low alpha 1 (hypotensive) and H1 (sedative) block
-Some anticholinergic effects)
-Least likely to cause weight gain

Front 10

Describe the administration and elimination of risperidone

Back 10

-Oral
-Completely absorbed from GI tract
-Metabolized by P450IID in liver
-Metabolites and original drug excrted in urine
-Reduction of dosage level is indicated in patients with hepatic or renal disease

Front 11

Describe the effectiveness of olanzapine

Back 11

At least as effective as risperidone
-Better than haloperidol at negative symptoms and at least as good for positive symptoms

Front 12

Describe the mechanism of action for olanzapine

Back 12

-Blocks dopamine D2 (much less affinity than typical drugs)
-Blocks D4 receptors
-Blocks 5HT2 drugs
-Twice as active against serotonergic receptors as against dopaminergic D2 receptors

Front 13

Describe the side effects of olanzapine

Back 13

-Better than risperidone at not causing extrapyramidal side effects
-Decreased in incidence of tardive dyskinesia, but it can still occur
-No prolactin secretion increase
-No agranulocytosis
-Sedation by H2 block
-Large weigh gain

Front 14

Describe LY2140023

Back 14

mGlu receptor agonist