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Block 6
Lecture 2 - Antipsychotics
15
Pharmacology
Graduate
04/18/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Typical vs. Atypical Antipsychotics
Definition

Typical

nD2 receptor blockers
nLess effective against negative symptoms
nSignificant motor side effects (EPS) & hyperprolactinemia
Greater efficacy in treatment resistant groups

 

Atypical

 

n5HT2A & D2 blockers
nMore effective against negative symptoms
nMinimal EPS & hyperprolactinemia
More weight gain
nClozapine is the only atypical that is useful in treatment resistant groups
 
Term

Chlopromazine

Fluphenazine

Haloperidol

Definition

Typical or "First Generation (FGA)" Antipsychotics

 

MOA

nTypical antipsychotics are potent D2 receptor family blockers
nVery effective in treating positive symptoms
nLess effective in treating the negative symptoms

 

Side effects that limit the use

 

nMotor side effects aka extrapyramidal symptoms (EPS) due to blockade of dopamine receptors in the nigrostriatal pathway
nNeuroendocrine side effects due to blockade of dopamine receptors in the tuberoinfundibular pathway

 

EPS Side Effects

 

nAcute EPS
Acute Dystonia – dystonia is just painful contractions of motor muscles. You are freezing in an abnormal posture.
Parkinson’s like symptoms: bradykinesia, rigidity, postural imbalance
Akathisiarestlessness. Restless leg syndrome

nChronic EPS
Tardive dyskinesia
Tardive dystonia

 

Treatment of Acute EPS

 

nAnticholinergic drugs
Procyclidine, orphenadrine
Benzatropine
Benadril

nReduction of the antipsychotic dose

nSwitch to an atypical antipsychotic

 

Chronic EPS: Tardive dyskinesia and dystonia

 

n20% of patients who have been on typical antipsychotics  for long time develop tardive dyskinesia

nThere is NO clear relationship to duration, dose, or class of antipsychotic (phenthiazines vs non phenothiazines)
nTARDIVE”: these symptoms persist even after the drugs have been stopped*

 

Treatment of Tardive dyskinesia and dystonia

 

nNo effective treatment
nPrevention by limiting the use of typical antipsychotics and early recognition of symptoms are important
nIncreasing the dose may temporarily alleviate* the symptoms, while reducing the dose may worsen them
nClozapine improves these symptoms

 

Neuroendocrine SE: Hyperprolactinemia

 

nD2 blockade in the tuberoinfundibular pathway removes dopamine inhibition of prolactin release from the anterior pituitary
n High serum concentrations of prolactin can produce galactorrhea, amenorrhea and infertility in some patients
nUse Smaller doses of typicals or switch to atypicals

 

Other Side Effects

 

nCommon to BOTH typical & atypical antipsychotics
n In addition to blocking D2 receptors, antipsychotics also block other receptors

 

Autonomic and Histaminergic Side Effects

 

nBlockade of muscarinic receptors
dry mouth
difficulty urinating or retention
constipation
blurred vision
confusion
nBlockade of α adrenoceptors
Orthostatic hypotension
nBlockade of H1 histamine receptors
Sedation

 

Other Side Effects (cont.)

 

nCardiac arrythmias
nSeizures
nWeight gain*
Once they took care of the EPS side effects, weight gain was the side effect that came up! If you treat long term, they will get weight gain!!
nIdiopathic:
Neuroleptic malignant syndrome (NMS)
nHyperthermia, muscular contraction. (You can use dantrolene to treat this). Since it is the antipsychotics that are causing this, you might want to give bromocriptine as well!
Hypersensitivity reactions
nYou do see these because they have similar chemical structure that they have developed these neuroleptics from

 

Term

Procyclidine, Orphenadrine

Benzatropine

Benadril

 

Definition

Anticholinergic Drugs

 

Used for the Treatment of ACUTE EPS

Term
Clozapine
Definition

Improves the Chronic EPS symptoms of Tardive Dyskinesia and Dystonia

Term

Haloperidol

 

Definition

Typical Anti-psychotic

nOften used to treat acute schizophrenia
nMOA: Potent D2 blocker
nSide effects typical of “TYPICAL” antipsychotics
EPS
Hyperprolactinemia
To a lesser extent seizures, weight gain
nAdvantages:
Very little sedation*** (Here is was a question!!)
Low anti-muscarinic effects
Very little orthostatic hypotension
Term

Clozapine (CLOZARIL)

Olazapine (ZYPREXA)

Risperidone (RISPERDAL)

Quetiapine (SEROQUEL)

Ziprasidone (GEODON)

Aripiprazole (ABILIFY)

Definition
Atypical Antipsychotics
Use
nTreatment with atypical antipsychotics is standard in LONG-term treatment of schizophrenia
nThis class of antipsychotic drugs were developed because they have
Better efficacy against negative symptoms*
Less motor (EPS) and neuroendocrine side effects
MOA

nBlock 5HT2A receptors
nBlock D2 family of receptors and also the D1 family receptors
Side Effects
nMinimal EPS & neuroendocrine side effects***
Risperidone & Olanzapine have some of these effects at HIGH doses
nAnti cholinergic effects
nAnti α-adrenergic effects
nAnti histaminergic effects
nCardiac arrythmias (Clozapine, Ziprasidone)***
Out of the whole list of drugs, these 2 drugs are very notable!
nSeizures (Clozapine, Olanzapine)
nWeight gain*
nNeuroleptic malignant syndrome (NMS)
nHypersensitivity reactions
Weight Gain

nSlightly more with atypicals. Less of a problem with the newest atypicals (Ziprasidone & Aripiprazole)
nIrrespective of the antipsychotic, schizophrenics have higher incidence of weight gain, unfavorable lipid profile, diabetes mellitus and a higher percentage of smokers
Term

Clozapine

(CLOZARIL)

 

 

Definition
nRESTRICTED use due to fatal neutropenia***
nUsed ONLY if a patient
Is unresponsive to two other neuroleptics
Has tardive dyskinesia or severe EPS

nCareful monitoring, CBC is mandatory
Patient has to be registered and drug dispensed only after the white cell count has been found to be normal
A white cell count is then performed every week for 4 months, and regularly thereafter
n Instead of causing dry mouth, this drug  causes hyper salivation***
Term

Olanzeprine

(ZYPREXA)

Definition
nMost commonly used atypical during an acute PSYCHOTIC break***
Overall slightly superior to haloperidol*

nSide effects
Minimal effective dose is 10 mg. Incidences of EPS increase at doses > 25-30 mg
Weight gain*** more than the other antipsychotics
- Seizures
Term

Risperidone

(RISPERIDAL)

Definition
nMost commonly prescribed antipsychotic next to Olanzapine and Haloperidol for acute psychoses
Blocks 5-HT2A receptors with high affinity
Blocks D2  receptors with affinity similar to most ’typical' antipsychotics

SIDE EFFECTS: At doses higher than 8 mg

EPS 
Hyperprolactinemia
Weight gain*
nIt has a TREMENDOUS effect on Weight Gain! You need to have a lot of food ready once they take this drug!! They feel like eating after this drug!!
Term

Quetiapine

(SEROQUEL)

Definition
Commonly used to treat psychoses in Parkinson’s disease
Less potential for exacerbating Parkinson's because it blocks D1, D4 & 5HT2A receptors not D2 receptors
n
Side effects that are slightly more prominent
Somnolence/Sedation***
Postural hypotension
Term

Aripiprazole

(ABILIFY)

Definition
nNewer generation atypical
In addition to blocking 5HT2A it is a partial agonist at 5HT1A & D2 receptors. Also blocks serotonin reuptake moderately
nRecently approved as an adjunct in the treatment of depression*
nMinimal weight gain***
Term

Ziprasidone

(GEODON)

Definition
nNewer generation atypical similar to Aripiprazole
nPotential for Cardiac arrhythmia*** in patients with baseline risk factors
Elderly
Preexisting cardiac disease
Taking diuretics or medication that prolong QT interval
Term
Resiperidone & Olanzapine SE
Definition

Risperidone & Olanzapine have some of these EPS and Neuroendocrine effects at HIGH doses
Term
Clozapine & Ziprasidone SE
Definition
nCardiac arrythmias (Clozapine, Ziprasidone)***
Out of the whole list of drugs, these 2 drugs are very notable!
Term
Clozapine & Olanzapine SE
Definition
nSeizures (Clozapine, Olanzapine)
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