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Pharm, Ass 12 TBL
Antiphsychotics
20
Pharmacology
Graduate
01/22/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Chloropromazine
Definition

[Thorazine]

Typical Anti-Psychotic - low potency;

Inhbits D2 receptor - effective for positive symptoms; Aliphatic side chain - low potency (↓ risk of EPS, ↑ risk of anti-muscarinic effects);

Tx: Huntington's chorea (DA antag);

 

SE: Corneal deposits, ↑ PRL (severe), ↓ INSULIN (impairs glc tolorance), Jaundice, ANTI-DIURETIC, ORTHOSTATIC hypoT, skin rxns (urticaria and dermatitis), EPS;

 

CI: In dementia-related psychosis (↑ mortality in the elderly)

Term
Fluphenazine
Definition

Typical Anti-Psychotic - high potency;

Inhibits D2 receptor - effective for positive symptoms; Piperazine group - ↑ potency (↑ risk of EPS, ↓ anti-muscarinic effects);

 

SE: EPS, ↑ PRL, skin rxns (urticaria and dermatitis)

Term
Thiothixene
Definition

Typical Anti-Psychotic;

Inhibits D2 receptor - effective for positive symptoms; Piperdine ring - ↓ incidence of EPS;

 

SE - ↑ PRL, highly anti-muscarinic

Term
Haloperidol
Definition

[Haldol]

Typical Anti-Psychotic - very high potency;

Inhibits D2 receptor - effective for positive symptoms;

 

Tx: Huntington's chorea (DA antagonism);

 

SE - EPS, ↑ PRL, less orthostatic hypoT than with other typical antipsychotics.

Term
Clozapine
Definition

Atypical Anti-Psychotic;

D2 (low affinity) and 5-HT2A (high affinity) antagonism;

↑ efficacy for Negative Sx (in addition to tx + sx);

 

5HT2A antg limits EPS SE;

SE - BLOOD DYSCRASIAS (w/ leukopenia prodrome), ↑ risk of DM typeII, weight gain/Metabolic Syndrome (esp in kids and adolescents);

Term
Risperidone
Definition

Atypical Anti-Psychotic;

D2 (low affinity) and 5-HT2A (high affinity) antagonism;

↑ efficacy for Negative Sx (in addition to tx + sx);

5HT2A antg limits EPS SE;

 

Tx: only approved agent for CHILDREN and TEENS;

 

SE - ↑ risk of DM typeII, moderate risk metabolic syndrome, ↑ PRL secretion and less/minor orthostatic hypoT;

Term
Olanzapine
Definition

Atypical Anti-Psychotic;

D2 (low affinity) and 5-HT2A (high affinity) antagonism;

↑ efficacy for Negative Sx (in addition to tx + sx);

5HT2A antg limits EPS SE;

 

SE - WEIGHT GAIN, ↑ risk of DM typeII, high risk of Metabolic Syndrome*

Term
Quetiapine
Definition

Atypical Anti-Psychotic;

D2 (low affinity) and 5-HT2A (high affinity) antagonism;

↑ efficacy for Negative Sx (in addition to tx + sx);

5HT2A antg limits EPS SE;

 

SE - ↑ risk of DM typeII, moderate incidence of metabolic syndrome.

No ↑ PRL*

Term
Ziprasidone
Definition

Atypical Anti-Psychotic;

D2 (low affinity), 5-HT2A, 5-H1A, 5HT2C (high affinity) antagonism* (note different than many atypicals);

↑ efficacy for Negative Sx (in addition to tx + sx);

5HT2A antg limits EPS SE;

 

SE - ↑ risk of DM typeII, low incidence of metabolic syndrome

Term
Aripiprazle
Definition

[Abilify];

Atypical Anti-Psychotic;

3MoA: D2 partial agonist, 5-HT2 antagonist, and 5-HT1A partial agonist;

↑ efficacy for Negative symptoms (as well as positives);

 

No effect/possible↓ of PRL levels;

SE - ↑ risk of DM typeII, low incidence of metabolic syndrome;

Term
CNS effects of Anti-Psychotics (6 sites)
Definition

Cortex - ↓ seizure threshold;

Basal ganglia - ↑ DA metabolism + DA blockade (EPS - dystonia, akinesia, parkinsonian syndrome, perioral tremor, neuroleptic malig syndrome,tardive dyskinesia), ↑ Ach turnover;

Limbic - main site of anti-psychotic efx;

Hypothalamus - ↑ PRL;

Brainstem - dec reflexes;

CTZ - protect AGAINST N/V

Term
Endocrine effects of Anti-Psychotics
Definition

Atypicals ↑ risk of Type II DM;

 

↑ PRL secretion (due to inhibition of D2) - Avoid in patients with breast carcinomas. Sustained hyperPRL can cause sexual dysfxn, amenorrhea, gynecomastia, galactorrhea, hypoestrogenism (poss osteopenia);

Term
Cardiovascular effects of Anti-Psychotics
Definition

Direct and indirect effects;

Orthostatic hypotension - esp with chlorpromazine

Term
EPS of of Anti-Psychotics (6)
Definition

Acute dystonia;

Akathesia;

Parkinsonian syndrome;

Neuroleptic Malignant Syndrome;

Perioral tremor;

Tardive dyskinesia

Term
Anti-cholinergic effects of Anti-Psychotics
Definition
Dry mouth; blurred vision; constipation; nasal congestion; orthostatic hypoT
Term
What are the depot antipsychotics and when might their use be considered?
Definition

Prolixin Decanoate, Haldol Decanoate, Risperidal Consta;

 

These formulations are the antipsychotic with a fatty acid complexed to them making them more lipophilic.

Are injected IM where tissue esterases hydrolyze the drug and allow slow release of the active compound;

 

Consider for patients who are non-compliant, have had several relapses, default on oral meds or have poor oral absorption/ideosyncratic pharm rxns.

Term
Misc SE of antipsychotics
Definition

Weight Gain/Metabolic syndrome (esp with clozapine and olanzapine), 

Urticaria/dermatitis (esp with phenothiazines),

Blood dyscrasias (esp with clozpine)

Term
What are some Misc uses for antipsychotic drugs?
Definition

To treat N/V (act on CTZ to ↑ DA and reduce Nausea);

To treat alcoholic hallucinations during detox;

Neuropsychiatric dz marked by movement disorders (Tourette's, HD, intractable hiccups).

Term
How does hemodialysis differ from hemoperfusion and when is each used?
Definition

Hemodialysis: ultrafiltration of the blood. Rquires that the toxin is water-soluble, relatively small, and mostly unbound in plasma.

Used in cases of severe Asprin or severe Theophylline OD.

 

Hemoperfusion involves passing blood through a charcoal cartridge filter to remove drugs bound to plasma proteins.

Used in cases of Carbamazepine, Phenobarbital, Phenytoin, and Theophylline OD*

Term
What Black Box warning accompanies AEDs?
Definition
Increase in suicide risk.
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