Antipsychotics Flashcards by Kyra Porter

positive symptoms of schizophrenia

“presence of what shouldn’t be”:

*hallucinations
*delusions
*thought disorders

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negative symptoms of schizophrenia

“lack of what should be”:

*losing interest and motivation in life and activities (e.g. relationships, sex)
*social inattentiveness
*affective flattening
*poverty of speech/content of speech
*poor self care, loss of persistence in school/work

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typical antipsychotics - overview

*first generation
*effective against positive symptoms only
*more EPS
*seldom used (except haloperidol)
*MOA: D2 blockade > 5-HT2A blockade

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atypical antipsychotics - overview

*second generation
*effective against positive AND negative symptoms
*less EPS
*used frequently
*MOA: 5-HT2A > D2 blockade

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general MOA of typical antipsychotics

D2 blockade > 5-HT2A (serotonin) blockade

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general MOA of atypical antipsychotics

5-HT2A (serotonin) blockade > D2 blockade

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phenothiazines

*a class of typical antipsychotics
*example = chlorpromazine (Thorazine) (low potency)

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butyrophenones

*a class of typical antipsychotics
*example = haloperidol (Haldol) (high potency)

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chlorpromazine - drug class

LP phenothiazine (typical/first generation antipsychotic)

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important atypical antipsychotics

*Clozapine (Clorazil)
*Risperidone (Risperdal)
*Olanzapine (Zyprexa)
*Quetiapine (Seroquel)
*Ziprasidone (Geodon)
*Aripiprazole (Ablify)
*Paliperidone (Invega)

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clozapine - drug class

atypical antipsychotic

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risperidone - drug class

atypical antipsychotic

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olanzapine - drug class

atypical antipsychotic

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quetiapine - drug class

atypical antipsychotic

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ziprasidone - drug class

atypical antipsychotic

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aripiprazole - drug class

atypical antipsychotic

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paliperidone - drug class

atypical antipsychotic

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pharmacokinetics/dynamics of atypical antipsychotics

*absorbed orally, but some have first pass metabolism (IV dose might be < PO dose)
*most have large Vd (very lipid soluble)
*hepatically metabolized (CP450)

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mechanism for adverse drug effects of antipsychotics: loss of accommodation, dry mouth, difficulty urinating, constipation

*mechanism = muscarinic cholinoceptor blockade (anticholinergic effects)

*system causing the symptoms = autonomic nervous system

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mechanism for adverse drug effects of antipsychotics: orthostatic hypotension, impotence, failure to ejaculate

*mechanism = alpha-adrenoceptor blockade

*system causing the symptoms: autonomic nervous system

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mechanism for adverse drug effects of antipsychotics: Parkinson’s syndrome, akathisia, dystonias

*mechanism = dopamine receptor blockade

*system causing the symptoms = central nervous system

mechanism for adverse drug effects of antipsychotics: tardive dyskinesia

*mechanism = supersensitivity of dopamine receptors

*system causing the symptoms = central nervous system

mechanism for adverse drug effects of antipsychotics: toxic-confusional state

*mechanism = muscarinic blockade (anticholinergic effects)

*system causing the symptoms = central nervous system

mechanism for adverse drug effects of antipsychotics: amenorrhea-galactorrhea, infertility, impotence

*mechanism = dopamine-receptor blockade resulting in hyperprolactinemia

*system causing the symptoms = endocrine system

mechanism for adverse drug effects of antipsychotics: weight gain

*mechanism = possibly combined H1 and 5-HT2A blockade

akithisia

*a subjective feeling of restlessness *one of the extrapyramidal symptoms (EPS) associated with antipsychotics

acute dystonic reactions

*abrupt onset muscular spasms of the neck, eyes, trunk, extremities *one of the extrapyramidal symptoms (EPS) associated with antipsychotics

parkinsonism

*stiffness, tremor, bradykinesia *one of the extrapyramidal symptoms (EPS) associated with antipsychotics

extrapyramidal symptoms

*akithisia (restless/can't sit still) *acute dystonic reactions *parkinsonism

cause of extrapyramidal symptoms (EPS)

*associated with use of antipsychotics *highest incidence with high potency typical agents (haloperidol)

MOA of extrapyramidal symptoms (EPS)

*D2 blockade + imbalance with M1 (Ach)

treatment for extrapyramidal symptoms (EPS)

*treat with ANTICHOLINERGIC drug -benztropine -trihexyphenidyl -diphenhydramine** *do NOT give levodopa

tardive dyskinesia (TD)

*a horrible adverse drug effect associated with antipsychotics *late-occurring abnormal movements: -mouth and tongue movements (lip smacking, sucking and puckering, facial grimacing) -irregular movements of the limbs (choreoathetoid-like movements of the fingers and toes; slow, writing movements of the trunk) *relative cholinergic deficiency secondary to SUPERSENSITIVITY OF DOPAMINE RECEPTORS

MOA of tardive dyskinesia

*relative cholinergic deficiency secondary to supersensitivity of DA receptors *occurs after long-term use with antipsychotics (esp typicals)

tardive dyskinesia - treatment

*discontinue the drug (switch to newer atypical agent) *can try high dose benzos *VMAT inhibitors (block the uptake of dopamine into synaptic vesicles)

neuroleptic malignant syndrome (NMS)

*ADE associated with antipsychotics *fever, rigidity, mental status changes, and autonomic instability *from DA blockade *TX: bromocriptine (DA agonist); DANTROLENE (a muscle relaxant)

treatment for neuroleptic malignant syndrome (NMS)

*bromocriptine (DA agonist) *dantrolene (a muscle relaxant)

other neurologic ADEs of antipsychotics

*seizures (decreases seizure threshold) - esp with clozapine *sedation (from central histamine-1 blockade)

hyperprolactinemia

*ADE of antipsychotics *s/s: sexual dysfunction (decreased libido, infertility, impotence), amenorrhea, gynecomastia / galactorrhea, hypoestrogenism / osteopenia

general drugs that cause hyperprolactinemia

*all typical antipsychotics *risperidone *paliperidone

cardiovascular effects associated with antipsychotics

*alpha-1 blockade: orthostatic hypotension (reflex tachycardia) & impaired ejaculation *QTc prolongation (be careful adding to other QTc drugs)

metabolic effects associated with antipsychotics

*weight gain *diabetes mellitus *dyslipidemia

ADEs of clozapine

*agranulocytosis *myocarditis (note - minimal EPS)

clozapine - unique facts

*minimal EPS and high efficacy *causes AGRANULOCYTOSIS & MYOCARDITIS **REQUIRES A SPECIAL PROGRAM (REMS) dictating who can prescribe it and frequency of CBC monitoring

ADEs of aripiprazole - general

probably the LEAST ADEs of all of the antipsychotics (used alot)

ADEs of clozapine - general

probably the MOST ADEs of all of the atypical antipsychotics (worst tolerated)

ADEs of olanzipine

*metabolic ADEs - weight gain, glucose abnormalities, and hyperlipidemia

ADEs of ziprasidone

*QTc prolongation

prochlorperazine

*antiemetic (treat nausea and vomiting) *MOA: DA-receptor blockade in the chemoreceptor trigger zone and in stomach *has high-potency ADEs (especially extrapyramidal symptoms - EPS)

promethazine

*antiemetic (treats nausea and vomiting) *MOA: DA-receptor blockade in the chemoreceptor trigger zone and in stomach *ADE = sedation (potent histamine-1 blocking effects)

antipsychotic drug used for acute agitation

haloperidol

drugs used for nausea and vomiting

*prochlorperazine *promethazine