Antipsychotic Drugs Flashcards
Adverse Side Effects of Antipsychotics:
CNS
Endocrine
Autonomic
Other
What falls under these categories?
Under CNS - EPS and NMS
Under Endocrine - Hyperprolactinemia
Under Autonomic - CV and Anticholinergic effects
Under Other: SMS (Sedation, metabolic, seizures)
- *Causes of EPS:**
- *Causes:** Highest incidence with __ potency typical agents like __ and __.
Why? - because it is very ___ and blocks the ___ receptors very easily. EPS is not nearly as bad in __/___ potency agents.
What do you do next? Treat with ____ drug! ___ (for acute dystonia and TD). ____or __ __ (for akathisia).T___ or D____ (which is an antihistamine - benadryl)
Presenation?
ADAPT:
Hours to days:__ __- abrupt onset muscular spasms of the neck, eyes, trunk, extremities
Days to wks: ___ - a subjective feeling of restlessness
Wks to months: ___ - stiffness, tremor, bradykinesia
Months to yrs: __ __ **very common among ___ ___.
TD:
- Late occurring ____ movements
- ___ and ____ movements, such as lip smacking, sucking and puckering as well as facial grimacing
- Irregular movements of the limbs, particularly ____-like movements of the fingers and toes and slow, writhing movements of the trunk
- Relative ___ deficiency secondary to __ __ of ___ receptors!! (know this!)
- Horrible ADE; advanced cases hard to ___
- Worse with typicals and perhaps high dose of ____
What do you do next?
- ____ dose or DC drug
- Usually ___ to newer ___ agent
- ___ use of drugs with central anticholinergic effects
- If above ineffective, can try high dose____
- *Causes of EPS:**
- *Causes:** Highest incidence with high potency typical agents like haloperidol and fluphenazine
Why? - because it is very potent and blocks the D2 receptors very easily. EPS is not nearly as bad in low/atypical potency agents.
What do you do next? Treat with anticholinergic drug! Benzotropine (for acute dystonia and TD). Benzodiazepam or beta blockers (for akathisia). Trihexylphenidyl or Diphenhydramine (which is an antihistamine - benadryl)
Presenation?
ADAPT:
Hours to days: Acute dystonia- abrupt onset muscular spasms of the neck, eyes, trunk, extremities
Days to wks: Akathisia - a subjective feeling of restlessness
Wks to months: Parkinsonism - stiffness, tremor, bradykinesia
Months to yrs: TD **very common among young men
TD:
- Late occurring abnormal movements
- Mouth and tongue movements, such as lip smacking, sucking and puckering as well as facial grimacing
- Irregular movements of the limbs, particularly choreathetoid-like movements of the fingers and toes and slow, writhing movements of the trunk
- Relative cholinergic deficiency secondary to super sensitivity of DA receptors!! (know this!)
- Horrible ADE; advanced cases hard to reverse
- Worse with typicals and perhaps high dose of risperidone
What do you do next?
- Lower dose or DC drug
- Usually switch to newer atypical agent
- Minimize use of drugs with central anticholinergic effects
- If above ineffective, can try high dose benzodiazepam
NMS symptoms:
What do you treat them with?
Malignant FEVER
Myoglobinuria
Fever
Encephalopathy
Vitals unstable
Enzyme levels increased (CK)
Rigidity
Treat with dantrolene, D2 agonist (eg bromocriptine)
Endocrine S/E of antipsychotics:
Hyper____ Symptoms: -
____ dysfunction
- Infertility, decreased ____, impotence
- A____
- G___/G___
- Hypo____/Os___
Drugs - Worse with all ___ and high dose __
Endocrine S/E of antipsychotics:
Hyperprolactemia Symptoms: -
Sexual dysfunction
- Infertility, decreased libido, impotence
- Ammenorhea
- Gynecomastia/Galactorhea
- Hypoestroginism/Osteopenia
Drugs - Worse with all typicals and high dose risperidone
Autonomic Symptoms from Antipsychotics include:
__ and __
CV effects
Anticholinergic effects
___ effects:
Orthostatic h___, impaired ___
QTc prolongation - especially with ____
Overdose of ____ causes bad arrthymias
___ effects:
Dry ___, ___ retention
- Worse with LP ___, __ and __ are wosrt (b/c you have to give more!)
Autonomic Symptoms from Antipsychotics include:
CV and Anticholinergic
CV effects
Anticholinergic effects
CV effects:
Orthostatic hypotension, impaired ejaculation
QTc prolongation - especially with zisprasidone
Overdose of risperidone causes bad arrthymias
Anticholinergic effects:
Dry mouth, urinary retention
- Worse with LP atypicals, olanzapine and clozapine are wosrt (b/c you have to give more!)
Other side effects of antipsychotics include:
__, __ and __
___ is caused from central histamine-1 blockade (remember, histamine is the alert NT)
Metabolic: worse with __ and ___
Seizures: worse with ___
Other side effects of antipsychotics include:
sedation, metabolic, seizures
sedation is caused from central histamine-1 blockade (remember, histamine is the alert NT)
Metabolic: worse with clozapine and olanzapine
Seizures: worse with clozapine
LP Drugs: bad for __, ___ effects, and o___
HP Drugs: bad for ____
All have pretty bad effect on ___ and s____ (especially ___)
Olanzapine - worst ___ effects
__ and __ - least amount of S/Es
LP Drugs: bad for sedation, cholinergic effects, and orthostasis
HP Drugs: bad for EPS
All have pretty bad effect on metabolism and seizures (especially clozapine)
Olanzapine - worst metabolic effects
Aripiprazole and Ziprasidone - least amount of S/Es
Usages:
Acute Agitation: ___
N&V: ___ and ___
Usages:
Acute Agitation: Haloperidol
N&V: prochlroperazine and Promethazine
Don’t Use the Wrong Injection !
- __ __ IM/IV injection - Used because pt can’t (or won’t) take ___ ___
- ___ ___ (depot) IM injection - Used to address __ issues (or to overcome some weird absorption issues) - Newer agents are very expensive ($1700/month)
Don’t Use the Wrong Injection !
- Immediate release IM/IV injection - Used because pt can’t (or won’t) take oral product
- Sustained release (depot) IM injection - Used to address compliance issues (or to overcome some weird absorption issues) - Newer agents are very expensive ($1700/month)
Anti-emetics
___-receptor blockade in the ___ ___ ___ and peripherally (in stomach) treats nausea and vomiting
Two drugs to know:
- ____ Has high potency ADE (eg, EPS because it is a typical antipsychotic)
- ___ ____ - histamine-1 blocking effects (sedation). Acts like benadryl. Given before surgery!
- *Anti-emetics**
- *DA**-receptor blockade in the chemoreceptor trigger zone and peripherally (in stomach) treats nausea and vomiting
Two drugs to know:
- Prochlorperazine - has high potency ADE (eg, EPS because it is a typical antipsychotic)
- Promethezine - histamine-1 blocking effects (sedation). Acts like benadryl. Given before surgery!
____ is an atypical antipsychotic
- It can cause metabolic S/E like weight gain
- You have to take a special program (dictating who can prescribe, etc.)
WHY? - AGRANULOCYTOSIS!
It can also cause ___
Clonazine is an atypical antipsychotic
- It can cause metabolic S/E like weight gain
- You have to take a special program (dictating who can prescribe, etc.)
WHY? - AGRANULOCYTOSIS!
It can also cause myocarditis
Pharmacodynamics:
Absorbed orally, but some agents have __ pass metabolism, therefore: ___ dose might be << __dose (meaning, ___ dose is required if you give the drug ___)
___ Metabolized (Cyp450) - long/short half-life - some other drugs may ___ their metabolism, but they usually don’t __ metabolism of other drugs - most interactions with other drugs are related to additive pharmacologic actions (eg, both drugs causing sedation of QTc prolongation)
Pharmacodynamics:
Absorbed orally, but some agents have first pass metabolism, therefore: IV dose might be << PO dose (meaning, less dose is required if you give the drug IV)
Hepatically Metabolized (Cyp450) - long half-life - some other drugs may alter their metabolism, but they usually don’t alter metabolism of other drugs - most interactions with other drugs are related to additive pharmacologic actions (eg, both drugs causing sedation of QTc prolongation)
MOA of Antipsychotics
____ receptor blockade
- Antipsychotic action: ___-___ pathway
- EPS - ____ pathway
____ receptor blockage
- This influences DA, NE, glutamate, GABA and ACh
___ have a greater affinity for D2; ____ have a greater affinity or 5HT2A
MOA of Antipsychotics
D2 receptor blockade
- Antipsychotic action: mesolimbic-mesocortical pathway
- EPS - nigrostriatal pathway
5HT2a receptor blockage
- This influences DA, NE, glutamate, GABA and ACh
Typical have a greater affinity for D2; Atypical have a greater affinity or 5HT2A
Typical Antipsychotics
- Effective against ___ Sx
- More ___ S/Es
- Seldom used (except ___)
- In general, D2 blockade + 5HT2a blockade
Potency High - more EPS (___, __ and ___)
Low - more ____ effects - more ___ (___ and __)
Note: Phenothiazine Class: ___ (LP), ____ (LP), ____ (HP), ____ (HP)
Butyrophenones class: ___ (HP)
Typical Antipsychotics
- Effective against positive Sx
- More EPS S/Es
- Seldom used (except haloperidol)
- In general, D2 blockade + 5HT2a blockade
Potency High - more EPS (haloperidol, fluphenazine, trifluoperazine)
Low - more cholinergic effects - more sedation (chloropramezine and thioridazine)
Note: Phenothiazine Class: chlropromezine (LP), thioridazine (LP), fluphenazine (HP), trifluoperazine (HP)
Butyrophenones class: haloperidol (HP)
