Belovich- Antipsychotic medications I Flashcards by Melanie Athens

Main 5 indications for antipsychotics?

Schizophrenia*- most common
Bipolar disorder (plus mood stabilizing effect)
Psychotic depression
Dementia-related psychoses
Drug-induced psychoses

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Though not drug of choice for nonpsychotic patients, Can treat anxiety symptoms in

autism spectrum disorder (risperidone)

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Antipsychotics can improve mood, reduce anxiety, and reduce disturbances

sleep

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some antipsychotics can be used as antiemetics due to antagonism of receptors in the area postrema

dopamine

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What are the 3 antipsychotics used for their antiemetic effects?

Ondansetron (Zofran)
Scopolamine (Transderm Scop)
Dimenhydrinate (Dramamine)

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Histamine receptor antagonism can treat which itchy disease?

Pruritis

(nerve itcthing)

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What are the indications for antipsychotic agents that do not tx some kind of psychosis?

antiemetics

pruritis

preoperative sedatives

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What causes the positive symptoms (hallucinations, delusions) are caused by Hyperactivity of DA in pathway

mesolimbic

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D2R helps alleviate psychotic symptoms

antagonism

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Levodopa, amphetamines, bromocriptine, apomorphine, etc. can schizophrenia psychosis or produce psychosis de novo in some patients. Why?

aggravate; due to increased activity of dopamine receptors

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What is the assumed cause of Negative symptoms (emotional blunting, social withdrawal, lack of motivation) and cognitive impairment of schizophrenia?

DA-receptor hypofunction in the prefrontal cortex

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Presynaptic D1 receptors in the prefrontal cortex thought to modulate activity, which, if impaired, can decrease the activity leading to impaired cognition and working memory.

glutamatergic

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Currently, negative symptoms can/cannot be pharmacologically targeted

cannot

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Which neurotransmitter pathway is affected when a D2R blockade results in:

Alleviates psychotic symptoms

• May induce other behavioral symptoms

mesocorticomesolimbic pathway

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What happens with D2R blockade in nigrostriatal pathway?

Produces motor disturbances by two opposing mechanisms (Extrapyramidal Symptoms and Tardive Dyskinesia)

-imbalance of AcH and DA levels

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Increases prolactin secretion

• Likely responsible for altered metabolism

occur when the D2R is blocked in which dopamine pathway?

D2R blockade tuberoinfundibular pathway

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What causes Parkinsonism like symptoms because of excess acetylcholine signaling relative to dopamine signaling and what dopamine pathway is effected?

The used of antipsychotics that block D2R in the nigrostriatal pathway

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Hyperprolactinemia, caused by D2R blockade in tuberoinfundibular pathway, can lead to which side effects?

increased breast tissue

lactation

gynecomastia

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Antipsychotic drugs have similar/various efficacy

similar

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Most important factor of successfor schizophrenia is spent on a drug

time

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Combination therapy should only be used in patients

refractory

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The main clinical effects of FGA typical antipsychotics is antagonism

D2R

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Potency of typical antipsychotics is with ADRs

correlated

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Atypical (or “second generation”) antipsychotics clincal effects are due to which 2 MOAs?

D2R antagonism and inverse agonism of 5-HT2A

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Why are atypical antipsychotics more commonly presribed?

more efficacious and friendlier ADRs

What are the 3 main classes of typical antipsychotics?

**Phenothiazines** • Chlorpromazine • Fluphenazine **• Thioxanthenes** • Thiothixene **• Butyrophenones** • Haloperidol

What are the 2 antipsychotics in the phenothiazine class (FGA)?

* Chlorpromazine * Fluphenazine

What is the FGA antipsychotic in the thioxanthenes class?

thiothixene

What is the FGA antipsychotic in the butyrophenones class?

haloperidol

ANS ADRs due to antipsychotics depends on the .

potency

Neurologic effects, Neuroleptic Malignant Syndrome, and Behavioral Effects are more commone **typicals/atypicals?**

typical antipsychotics

Metabolic ADRs are more common in **typical/atypical** agents

atypical

hyperprolactinemia is more common in **atypical/typical** agents

typical

Which antipsychotic is more likely to cause toxic or allergic reactions?

clozapine

Cardiac toxicity ADRs can occur with **atypicals/typicals/both?**

both

Typical antipsychotics can also act as antagonists for which 3 other receptor types (off target) other than dopamine receptors?

**• 𝛼-adrenergic antagonists** - orthostatic hypotension, light-headedness **• Muscarinic antagonists -** anticholinergic effects, dry mouth, urinary retention • **H1 antagonists** - sedation, weight gain

The following off target effects of typical antipsychotics is due to antagonism of receptors? orthostatic hypotension, light-headedness

a-adregergic

The following off target effects of typical antipsychotics is due to antagonism of receptors? anticholinergic effects, dry mouth, urinary retention

Muscarinic

The following off target effects of typical antipsychotics is due to antagonism of receptors? sedation, weight gain

ADRs of Antipsychotic agents share close relationship with D2R

affinity

Potency governs ADR profiles of antipsychotics and severity more than

efficacy

more potent= higher

affinity

Typicals have a **higher/lower** affinity for D2 receptors

higher

In general, higher potency agents are given at doses, while lower potency agents may dosed

lower; higher

More potent antipsychotics will have **less/more** occurrence of off target ADRs?

less

More potent antipsychotics wil have strong on target ADRs such as :

EPS and TD

Blockade of D2 receptors alters balance

DA/ACh

Relative excess cholinergic influence results in **EPS/TD**?

EPS (excess Ach as compared to DA)

What are the EPS ADRs?

Dystonias (sustained contraction of muscles leading to twisting, distorted postures) * Parkinson-like symptoms * Akathisia (motor restlessness)

**EPS/TD** symptoms are generally reversible?

EPS

Drugs that have **stronger/weaker** anticholinergic activity have a lower risk of developing EPS

stronger as the imbalance of Ach to DA is less

“Neuroleptic” refers to potency typical antipsychotic drugs • High incidence of extrapyramidal side effects at clinically effective doses

high

What type of drugs are effective at treating extrapyramidal symptoms acute dystonia and Parkinsonism?

Antiparkinsonian agents **• Amantadine**, a prodopaminergic drug, increases effective dopamine signaling **• Benztropine**, an anticholinergic drug, can counter the effects of “excess” cholinergic effects • Antimuscarinic effects can occur

Which type of antiparkonsonian agent that is used to combat extrapyramidal symptoms caused by typical antipsychotics should not be used with an Alzheimer's co-morbidity?

**Benztropine**, an anticholinergic drug, can counter the effects of “excess” cholinergic effects

Which Antiparkinsonian agents, effective for acute dystonia and Parkinsonism due to EPS from typical antipsychotics, is a prodopaminergic drug, increases effective dopamine signaling and restores the Ach/DA imbalance?

Amantadine

Which Antiparkinsonian agents is an anticholinergic drug and can counter the effects of “excess” cholinergic activity due to typical antipsychotics?

Benztropine

What non Antiparkinsonian agents is also effective for acute EPS?

Diphenhydramine

Akathesia (restlessness), an EPS symptom, a is more effectively managed with (benzodiazepines) or (ßblockers)

clonazepam propranolol

EPS/TD symptoms are generally irreversible?

Excess and Involuntary movements, bilateral and facial jaw movements, “fly-catching” or “worm-like” tongue movement

Tardive dyskinesia (TD)

TD occurs with **short/long-term** treatment with antipsychotic agents

long-term

Which ADR occurs when Dopaminergic receptors become sensitized due to chronic antagonism? Also, Neuronal response to dopaminergic input overpowers response to cholinergic input cause the symptoms?

Describe the Ach/DA imbalance that caused TD symptoms?

excess dopamine activity compared to Ach activity from sensitization of dopamine receptors

TD is more commonly observed with **high/low** potency agents (esp. haloperidol)

high

What are the 2 types of treatments for Tardive dyskinesia?

**• Drug cessation** • Symptoms may improve but in many cases TD is irreversible and persistent **• VMAT inhibitors** • Reduce amount of DA available to release • (valbenazine and deutetrabenazine)

What are the 2 types of vesicular monoamine transporter inhibitors that are used to combat TD?

valbenazine and deutetrabenazine

What is the MOA of VMAT inhibitors?

Reduce amount of DA available to release because they inhib the vesicular monoamine transporter that packs the synaptic vescicles for release

NMS occurs due to D2R blockade in the and nigrostriatal pathways

NMS is an **on/off** target ADR?

What condtion is being described: * Muscle rigidity (“lead-pipe rigidity”) * Fever * Altered mental status and stupor * Unstable blood pressure, * Myoglobinemia, * Elevated serum creatine kinase * Rare, but fatal in 10-20% of cases if untreated

NMS

Most frequent with high doses of potent agents (a.k.a. “ agents”)

neuroleptic

NMS is **more/less** common in atypical agents

less

What 3 things are considered in the treatment of NMS?

Discontinue use of the antipsychotic agent dantrolene\* bromocriptine\*

What 2 drugs can be used to treat NMS associated with antipsychotic agent?

dantrolene bromocriptine

How long can NMS persist after the offending agent is discontinued?

more than a week

NMS symptom persistence is associated with

mortality

How do we distinguish neurological ADRs (most likely caused by FGAs)?

distinguish by duration of symptoms

and D2R antagonism can result in akinesia, and dysphoria

D1R

“diminished spontaneity,” apathy, withdrawal, appearance of depression

akinesia (negative symptom)

Delirium and psychosis can be induced by **small/large** doses of typical antipsychotics

large

Which population can develop pseudomementia (confusion and disorientation) from taking antipsychotics?

elderly

Blockade of D2Rs in pathway causes hypersecretion of prolactin by pituitary

tuberoinfundibular

can directly induce galactorrhea, and sexual dysfunction or infertility in women and men

Hyperprolactinemia

What is an effective method to treat hyperprolactinemia?

Dosage reduction/cessation (however, keep in therapeutic range)

When switching antipsychotic agents in the case of hyperprolactinemia is not feasible, which 2 drugs can be used?

bromocriptine aripiprazole

Low-potency frequently cause orthostatic hypotension and tachycardia due to off target a-adrenergic effects

phenothiazines

What are the cardiovascular effects of FGA phenothiazines due to off target blockade of adgenergic receptors?

Mean arterial pressure, peripheral resistance, and stroke volume are decreased

Phenothiazine agents (low potency than other FGAs) produce more (H1) and weight gain than other typical antipsychotics due to off target effects.

sedation

Low potency phenothiazines associated with increased serum and hyperglycemia.

triglycerides and hyperglycemia

Chlorpromazine and are the least potent of the phenothiazine class

thioridazine

Which phenothiazine is no longer used due to being associated with torsades de pointes?

• Thioridazine

Which phenothiazine is high potent and has a high potential for EP but Low potential for weight gain, sedation, and orthostasis?

fluphenazine

Which highly potent typical antipsychotic phenothiazine is Commonly used in long-acting injectable formulation for noncompliant patients?

Fluphenazine

What is the most potent and widely used typical antipsychotic?

Haloperidol

Which FGA has Greater incidence of EPS compared to other typical antipsychotics?

haloperidol

Which FGA is described: Greater incidence of EPS compared to other typical antipsychotics * Low potential for orthostasis, weight gain, sedation * Can be used to manage acute psychotic states * Commonly used in long-acting injectable formulation for noncompliant patients

haloperidol

Which highly potent typical commonly used in long-acting injectable formulation for noncompliant patients Can be used to manage acute psychotic states?

haloperidol

Belovich- Antipsychotic medications I Flashcards

(99 cards)