Antipsychotic Medications Overview
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Questions and Answers

Which treatment is categorized as a first-generation antipsychotic?

  • Cariprazine
  • Haloperidol (correct)
  • Chlorpromazine (correct)
  • Aripiprazole
  • What mechanism does a dopamine D2 antagonist primarily target?

  • Presynaptic D2 receptors
  • Dopamine reuptake inhibitors
  • Post-synaptic D2 receptors (correct)
  • Serotonin receptors
  • What is a common side effect associated with prolonged use of D2 receptor antagonists?

  • Neuroleptic Malignant Syndrome
  • Weight gain
  • Insomnia
  • Tardive dyskinesia (correct)
  • How do third-generation antipsychotics like aripiprazole function in high levels of mesolimbic dopamine?

    <p>They act as a partial agonist to reduce hyperactivity.</p> Signup and view all the answers

    What percentage of patients do not respond to D2 receptor antagonists?

    <p>30%</p> Signup and view all the answers

    What percentage of the human brain is made up of fat?

    <p>29%</p> Signup and view all the answers

    What is hypofrontality associated with in relation to schizophrenia?

    <p>Depressed prefrontal cortex function</p> Signup and view all the answers

    Which of the following factors is NOT linked to an increased incidence of schizophrenia?

    <p>Excessive adolescent exercise</p> Signup and view all the answers

    What percentage chance does a child have of developing schizophrenia if a parent has the disease?

    <p>10%</p> Signup and view all the answers

    In what age period does schizophrenia typically begin to occur?

    <p>Late teens to early 20s</p> Signup and view all the answers

    Which of the following symptoms is commonly associated with schizophrenia?

    <p>Visual hallucinations</p> Signup and view all the answers

    Which area of the brain is noted to show changes in individuals with schizophrenia as indicated by MRI scans?

    <p>Prefrontal cortex</p> Signup and view all the answers

    Which of the following is considered a significant nutrient found in human brains?

    <p>Omega-3 fatty acid DHA</p> Signup and view all the answers

    What is a potential advantage of having long half-life drugs for schizophrenia patients?

    <p>They may have residual levels in the blood even after stopping.</p> Signup and view all the answers

    What factors need to be measured to determine appropriate dosing of a drug with a long half-life?

    <p>Both parent drug and metabolite levels in the blood.</p> Signup and view all the answers

    What could be a consequence of having long half-life drugs in the body?

    <p>They may require less frequent dosing.</p> Signup and view all the answers

    Which of the following associations is incorrect?

    <p>First pass metabolism involves renal excretion.</p> Signup and view all the answers

    Why is the pharmacokinetic profile essential for a drug's effectiveness?

    <p>It affects both efficacy and the degree of side effects.</p> Signup and view all the answers

    Which of the following is NOT considered a positive symptom of schizophrenia?

    <p>Blunted affect</p> Signup and view all the answers

    Which neurotransmitter imbalance is associated with positive symptoms of schizophrenia?

    <p>Dopamine hyperfunction</p> Signup and view all the answers

    What role does the blood-brain barrier (BBB) play in the brain's microenvironment?

    <p>It protects against circulating toxins while allowing vital nutrients to enter.</p> Signup and view all the answers

    How does serotonin mainly influence negative symptoms in schizophrenia?

    <p>Via modulation of glutamate activity</p> Signup and view all the answers

    What is a main characteristic of the specialized transporters in the BBB?

    <p>They facilitate the transport of both essential molecules and waste products.</p> Signup and view all the answers

    What type of cognitive impairment is commonly seen in schizophrenia?

    <p>Poor attention and memory</p> Signup and view all the answers

    What influences the frequency of drug administration?

    <p>The drug's elimination rate from the body.</p> Signup and view all the answers

    Why are schizophrenia symptoms difficult to diagnose?

    <p>Symptoms vary between individuals</p> Signup and view all the answers

    What does 'steady state' refer to in pharmacokinetics?

    <p>When drug intake equals elimination, keeping blood concentration stable.</p> Signup and view all the answers

    What does NMDA antagonism lead to in the context of schizophrenia?

    <p>Induction of negative symptoms</p> Signup and view all the answers

    How are metabolites formed during the metabolism of a drug?

    <p>Metabolites can be either active or inactive.</p> Signup and view all the answers

    What role does the PFC play in the mesocortical dopamine system in schizophrenia?

    <p>It regulates negative control</p> Signup and view all the answers

    Which of the following statements about drug clearance is true?

    <p>Most drugs are cleared through the kidney and urine.</p> Signup and view all the answers

    Which receptor subtype is predominantly involved in the negative symptom regulation of serotonin?

    <p>5-HT1A</p> Signup and view all the answers

    What behavioral pattern is common among many individuals with schizophrenia regarding smoking?

    <p>They often self-medicate with it</p> Signup and view all the answers

    What is the significance of the half-life (T1/2) in drug dosing?

    <p>It indicates how frequently to administer the drug.</p> Signup and view all the answers

    What is true about Cariprazine's pharmacokinetic profile?

    <p>It has an active metabolite with a longer half-life than the parent drug.</p> Signup and view all the answers

    Low levels of dopamine release in the PFC are associated with which type of symptoms?

    <p>Cognitive symptoms</p> Signup and view all the answers

    What aspect of glutamate's role in schizophrenia has been observed through pharmacological studies?

    <p>Glutamate dysfunction is associated with various symptom types</p> Signup and view all the answers

    Which property of the blood-brain barrier contributes to its selectivity?

    <p>It allows only small lipid-soluble drugs to pass.</p> Signup and view all the answers

    What impact do active metabolites have on the therapeutic effect of a drug?

    <p>They can contribute to either therapeutic effects or side effects.</p> Signup and view all the answers

    What type of side effects is associated with chlorpromazine, a medication for schizophrenia?

    <p>Reduced positive symptoms</p> Signup and view all the answers

    The principle action of amphetamines in schizophrenia is to:

    <p>Augment dopamine levels</p> Signup and view all the answers

    What is a common behavioral symptom associated with cognitive impairment in schizophrenia?

    <p>Difficulties with abstract thinking</p> Signup and view all the answers

    The balance of which neurotransmitters is crucial for understanding schizophrenia's symptoms?

    <p>Dopamine, serotonin, and glutamate</p> Signup and view all the answers

    What effect does a low dose D2 antagonist have in combination with NMDA agonists?

    <p>It decreases dopamine in the mesolimbic pathway.</p> Signup and view all the answers

    Which drug is an example of a 3rd generation antipsychotic that acts as a dopamine stabilizer?

    <p>Cariprazine</p> Signup and view all the answers

    What is the primary role of the cytochrome P-450 enzymes in pharmacokinetics?

    <p>They metabolize drugs in the liver.</p> Signup and view all the answers

    How does high protein binding affect a drug's efficacy?

    <p>It reduces the amount of free drug available.</p> Signup and view all the answers

    What is the primary consequence of first-pass metabolism on drug bioavailability?

    <p>It decreases the amount of drug entering systemic circulation.</p> Signup and view all the answers

    What is the significance of lipophilicity in drug distribution?

    <p>It affects how easily the drug crosses lipid membranes.</p> Signup and view all the answers

    Which of the following best describes how dopamine acts in the mesolimbic pathway at high levels?

    <p>As an antagonist competing with dopamine for the receptors.</p> Signup and view all the answers

    What is one consequence of a drug's lipophilicity on its pharmacokinetics?

    <p>It facilitates passive diffusion across membranes.</p> Signup and view all the answers

    Which drug class primarily targets cognitive symptoms in schizophrenia?

    <p>Atypical antipsychotics</p> Signup and view all the answers

    What role does the Blood-Brain Barrier (BBB) play in pharmacology?

    <p>It regulates the substances that can enter the brain.</p> Signup and view all the answers

    Which type of receptors are D2 partial agonists primarily associated with?

    <p>Dopamine receptors</p> Signup and view all the answers

    What aspect of drug distribution can be significantly limited by high protein binding?

    <p>Clinical efficacy of the drug</p> Signup and view all the answers

    What impact does grapefruit juice have on drug metabolism?

    <p>It inhibits cytochrome P-450 enzymes.</p> Signup and view all the answers

    What primary factor does NOT affect drug distribution to target tissues?

    <p>Chemical stability</p> Signup and view all the answers

    Study Notes

    Human Brain Nutrition Facts

    • DHA, a vital omega-3 fatty acid, is concentrated in human brains.
    • The brain is approximately 29% fat and 20% protein.
    • It's a good source of vitamin C and iron.

    Schizophrenia Symptoms

    • National Institute of Health considers schizophrenia a chronic, severe mental disorder affecting thoughts, feelings, and behaviours.
    • Individuals may be withdrawn, consumed with their own thoughts and delusions.
    • Typically emerges in the early 20s, disrupting peak productive years.
    • Approximately 30% of those diagnosed are institutionalized at some point.
    • MRI scans reveal smaller brains with larger ventricles (empty space) in affected individuals.
    • Prefrontal cortex function can be depressed, leading to issues with executive function, response inhibition, and problem-solving skills.

    Environmental Factors Associated with Schizophrenia (Incorrect Association)

    • Excessive adolescent exercise is NOT an environmental factor linked to schizophrenia. Other factors (e.g., adolescence cannabis smoking, prenatal malnutrition, urban birth, C-sections, children of dry cleaners) have more substantial associations.

    Schizophrenia and Month of Birth

    • Risk of schizophrenia may be slightly higher for individuals born in certain months.
    • Risk appears lowest around the months of early January through early February and slowly increases and peaks around early September through late October.

    Genetic and Environmental Factors in Schizophrenia

    • Genetic predisposition plays a role; a family history of schizophrenia increases the risk of developing the condition by 10%.
    • Environmental factors such as late winter/early spring birth, infections, vitamin D deficiency, urban pollution, prenatal malnutrition, and smoking are also linked to schizophrenia.
    • Not all factors have a clear and definitive effect, and more work is needed to assess causal linkages.

    Schizophrenia Symptoms: Categories

    • Symptoms grouped into three categories:
    • Positive symptoms: include hallucinations, delusions, illogical thinking, and disorganized speech.
    • Negative symptoms: characterized by loss of normal pleasures, blunted affect, and social withdrawal.
    • Cognitive impairment: involves difficulties with attention, learning, memory, and abstract thinking.
    • Individual experiences vary, making diagnosis challenging. Symptoms can fluctuate over time.

    Range of Symptoms and Associated Brain Sites

    • Mesolimbic and mesocortical neuronal circuits are associated with different symptoms of schizophrenia.
    • Positive symptoms typically correlate with activity in the mesolimbic circuit, while negative symptoms and cognitive issues are linked to the mesocortical circuit.
    • Emotions can be absent or inappropriate.

    Biochemistry of Schizophrenia (Dopamine)

    • Dopamine dysfunction, alongside other neurotransmitters, plays a significant role in schizophrenia.
    • Early pharmacology studies using amphetamines and levodopa demonstrated the relation between dopamine and schizophrenia.
    • Chlorpromazine, a dopamine antagonist, effectively reduces schizophrenia positive symptoms.

    Biochemistry of Schizophrenia (Glutamate)

    • NMDA antagonists exacerbate schizophrenia symptoms.
    • Hypoactivation in the mesocortical dopamine system is linked to negative symptoms due to low local glutamate/NMDA activity.

    Biochemistry of Schizophrenia (Serotonin)

    • Serotonin modulates dopamine and glutamate, and affects primarily negative symptoms
    • 5-HT1A, an inhibitory receptor, is activated by some anti-psychotics, and 5-HT2A, an excitatory receptor, may contribute to hypofrontality.

    Biochemistry of Schizophrenia: Acetylcholine

    • Nicotinic acetylcholine receptors (nACh), particularly α7, are involved in cognitive functions.
    • Schizophrenic patients have decreased nACh receptor levels and increased rates of smoking.
    • Nicotine may be a form of self-medication for some schizophrenics.

    Drug Inducing Schizophrenia-like Symptoms

    • Drugs interfering with dopamine reuptake can induce symptoms similar to schizophrenia, likely related to mesolimbic dopamine hyperfunction.

    Classical Treatments of Schizophrenia

    • First-generation antipsychotics (dopamine D2 antagonists) were initially the primary treatment.
    • Approximately 30% of patients don't respond effectively to these drugs, necessitating research into other options.
    • Tardive dyskinesia and other side effects are possible.

    Third-Generation Treatments of Schizophrenia

    • 3rd generation antipsychotics feature partial D2 dopamine agonists (e.g., aripiprazole).
    • These drugs reduce hyperactivity in mesolimbic dopamine circuits, but partially activate the hypoactivity in mesocortical Dopamine circuits

    Pharmacodynamics

    • Pharmacodynamics refers to how drugs impact the body.

    Biodistribution: Blood-Brain Barrier

    • The blood-brain barrier hinders the entry of many substances into the brain and requires specialized transporters.

    Metabolism

    • Drugs are broken down in the body, often by enzymes in the liver.
    • Metabolites can be inactive or active; some active metabolites have different (or similar) effects compared to the original drug.

    Excretion

    • Eliminating drugs and their metabolites from the body, typically via the kidneys, occurs through excretion.

    Steady-State

    • A period where drug concentration in the bloodstream remains relatively constant due to balanced intake and elimination.
    • Steady-state must be reached to accurately determine efficacy.

    Cariprazine (Vraylar)

    • Cariprazine is a third-generation atypical antipsychotic. It acts as a partial agonist at dopamine D2 receptors and as antagonists at other receptors (e.g., 5-HT2A).
    • It has good oral bioavailability, rapidly crosses the blood-brain barrier, and has a relatively long half-life, which makes it useful for patients who may miss doses.

    Summary

    • Schizophrenia is a complex neurological disease with heterogeneous presentation and unknown cause.
    • While dopamine plays a pivotal role, other neurotransmitters are also involved.
    • Genetic and environmental factors contribute to a predisposition and can impact the course of the disorder.
    • Both first and third-generation pharmacologic therapies are employed, although significant challenges and side effects remain.

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    Schizophrenia Lecture Notes PDF

    Description

    Test your knowledge on antipsychotic medications with this quiz. It covers first-generation and third-generation antipsychotics, their mechanisms of action, common side effects, and treatment responses. Perfect for students of psychology and psychiatry.

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