Antipsychotics Flashcards
Which dopamine receptor do typicals antagonise?
D2
Which dopamine receptor do 2nd generation atypicals antagonize? What makes them different from typicals?
D2- Have fast dissociations
They are selective to the meso-limbic area
What other receprors do 2nd generation atypicals antagonize?
5-HT2
What receptors do 3rd generation atypicals antagonize?
Partial agonist-antagnoist of D2 and 5-HT1A
Antagonist of 5-HT2A
When are typical antipsychotics used?
Control active psychosis
Reduce assaultive behavior/agitation
Decanoate for maintenance in non-compliant patients
What is the potency level of haldol?
High
What are the worst side effects from haldol?
High:
- EPS
- Prolactin elevation
Low:
- Anticholinergic
- Orthostasis
- Sedation
- Wt gain
- Cardiac arrythmias
- Seizures
- Hyperglycemia
What is the potency level of thorazine?
Medium
What are the side effects of thorazine?
High
- Anticholinergic
- Orthostasis
- Sedation
- Wt gain
Moderate
- EPS
- Cardiac arrythmias
- Photosensitivity
- Rashes
- Pigmentation
- Glucose intolerance
- Elevated cholesterol
Low
- Seizures
- Blood dyscrasias
In what areas of treatment are atypicals more efficatious then typicals?
Negative symptoms
Cognitive symptoms
How is risperdal’s half life special?
It’s half life is 3 hrs, but it’s metabolite is 24 hrs
What are the side effects of risperdal?
High
- EPS
- Elevated prolactin
Moderate
- Orthostatic hypotension
- Sedation
- Metabolic syndrome
Low
- Anticholinergic
- Seizures
- Priapism
Which two atypicals are more effective than risperdal?
Clozaril
Zyprexa
What is paliperidone?
6-OH-risperidone (active metabolie)
How can you increase the absorptions of paliperidone?
Take it with a high calorie meal
What about paliperidone makes it ideal for patients with hepatic insufficency?
60% us excreted unchanged by the kidney
What are the side effects of paliperidone?
Similar to Risperdal except it may prolong QT
What are the side effects of ziprasidone?
Moderate
- Prolong QT
Low
- Anticholinergic
- Rash
- Seizures
- Elevated prolactin
- EPS
- Weight gain
- Orthostatic hypotension
- Sedation
- Metabolic syndrome
What is a concerning disadvantage about ziprasidone (other than prolonged QT)?
May be activating
In what circumstances should ziprasidone not be prescribed because of the increased risk of prolonged QT?
Bradycardia
Hypokalemia or hypomagnesemia
Other drugs that prolong the QT interval
Congential prolonged QT interval
What is the cut off QT interval for using ziprasidone?
> 500 msec
What is the “gold standard” of antipsychotic pharmacology?
Clozapine
What about clozapine’s MOA makes it “special”?
Exclusive activity on the mesolimbic and mesocortical areas
- Works equally well on postive and negative symptoms
What are the side effects of Clozapine?
High
- Anticholinergic
- Sedation
- Metabolic syndrome
- Orthostasis
Medium
- Agranulocytosis
- Myocaarditis
- Cardiac arrhythmias
- Sialorrhea
- Constipation
Low
- Eosinophilia
- PE
- Hepatitis
Minimal
- EPS
- Prolactin elevation
What are some advantages of clozapine?
Effective for treatment resistant cases
Lowers suicide risk
Effective for treating TD
How many drugs should a patient fail before starting them on clozapine?
2 to 3
How often do you need to get a CBC for patients using clozapine?
1 wk X 6 months the q2wks
Side effects of olanzapine?
High
- Metabolic syndrome
Medium
- Sedation
- Orthostasis
- Anticholinergic
Low
- EPS
- Elevated prolactin
- Cardiac arrhythmias
- Elevated LFTs
- Seizures