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Antipsychotics
Drugs used in the treatment of schizophrenia and other mental health diseases
23
Pharmacology
Professional
11/15/2011

Additional Pharmacology Flashcards

 


 

Cards

Term

1st generation antipsychotics

- low potency

- high potency

Definition

Low potency:

- chlorpromazine

- thioridazine

 

High potency:

- haloperidol

- fluphenazine

Term

2nd generation "atypical" antipsychotics

 

Definition

Clozapine

Quetiapine

Ziprasidone

Paliperidone

Iloperidone

Risperidone

Olanzapine

Aripiprazole

Asenapine

Term

1st generation antipsychotic general properties

-receptor

-treats

-side effects

Definition

Receptor:

- high affinity D2 antagonists

 

Treats:

- positive symptoms 

- minimal effects on negative symptoms

 

Side effects:

- high incidence of extrapyramidal s/e's

- sedation

- elevated prolactin levels

Term

Thioridazine

Chlorpromazine

- class

- side effects

Definition

Class:

- 1G "typical" low potency antipsych meds

 

Side effects:

- autonomic effects

- sedation

Term

Haloperidol

Fluphenazine

- class

- side effects

Definition

Class:

- 1G "typical" high potency antipsych meds

 

Side effects:

- more extrapyramidal s/e's

- less sedation

Term

General features of 2nd generation antipsychotics

 

Definition

First-line therapy

Lower incidence of EP s/e's

Used to treat levodopa-induced

Augmentation of Rx-resistant depression

Effective in patients not receiving benefit from 1G agents

Substituted for 1G agents when signs of tardative dyskinesia appear 

 

Term
Side effects of 2G antipsych medications
Definition

Weight gain + hyperglycemia (compliance issue)

QT prolongation

Sedation

Somnolence, dizziness, constipation, postural hypotension, dry mouth

Mortality risk in dementia-related psychosis

Suicidal risk if indicated for depression

Term

Clozapine

-receptors

-side effects

Definition

Receptors:

- 5-HT2 > D2    (D4 , D3 > D2) antagonist

- H1 antagonist

- α1 antagonist

- M1 antagonist

 

Side effects:

- most effective antipsychotic limited in used due to agranulocytosis

- sedative effects high

Term

Risperidone

-receptors


Definition

Receptors:

- 5-HT2 > D2 antagonists

- H1 antagonists

- α1 antagonists

- M1 antagonists

- selectivity for limbic system (targets D3)

Term

Ziprasidone

-receptors

-uses

Definition

Receptors:

- potent 5-HT2A antagonist >> D2

- high affinity for 5-HT1A , 5-HT1D, and 5-HT2C

- less potent αantagonists

- less affinity for M1 & H1 receptors

 

Uses:

- antipsych

- good anxiolysis and antidepressant

- low potential for impairing cognitive abilities = good in AD

Term

Quetiapine

-receptors

-side effects

Definition

Receptors:

- 5-HT2 > D2 

- H1

- α1 & α2 adrenergic antagonists

 

Side effects:

- possibility of cataracts

Term

Olanzapine

-receptors

-contraindications

Definition

Receptors: (antagonists)

- D1, D2, D4

- 5-HT2, 5-HT3

- H1

- α1

- M1

 

Contraindicated:

- diabetics due to weight gain and hyperglycemic effects

Term

Aripiprazole

-receptors

-uses

Definition

Receptors:

- D2 and 5-HT1A partial agonists

 

Uses:

- antipsych

- good for bipolar disorder

- improved blunted affect

 

**considered 3G antipsych

Term

Asenapine

-receptors

 

Definition

5-HT2A > D2

D3 and D4 antagonists

5-HT6 and 5-HT7 antagonists

α1 & α2 adrenergic antagonists

Term

Iloperidone

-receptors

Definition

5-HT2 > D2 

low/no affinity for other receptors (H1, M1, α1)

Term

Paliperidone

-receptors

Definition

Major active metabolite of risperidone

 

5-HT2 > D2 

α1 and α2

H1

Term

D2 receptor antagonists

-therapeutic effect

-side effect

Definition

Therapeutic effect:

- reduced positive signs of psychosis

 

Side effects:

- extrapyramidal sypmtoms

- elevated prolactin and its effects

Term

Serotonin 5-HT2A 

-therapeutic effect

-side effect

Definition

Therapeutic effect:

- Reduced negative signs of psychosis

- mitigation of EPS

- potentiation of antipsychotic effect on positive signs

 

Side effects:

- sexual disturbances

Term

α1 adrenergic antagonists

-therapeutic effect

-side effect

Definition

Therapeutic effect:

- unknown

 

Side effects:

- postural hypotension

- dizziness

- reflex tachycardia

- potential for drug interactions (esp anti-HTNs)

Term

Muscarinic-cholinergic antagonist effects

-therapeutic

-side effects

Definition

Therapeutic effects:

- mitigation of EPS

 

Side effects:

- blurred vision

- urinary retention

- sinus tachycardia

- memory impairment

- narrow angle glaucoma

Term

H1 antagonist effects

-therapeutic

-side effects

Definition

Therapeutic:

- sedation

 

Side effect:

- sedation

- increased appetite

- weight gain

- hypotension

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