Podcast
Questions and Answers
Which treatment is categorized as a first-generation antipsychotic?
Which treatment is categorized as a first-generation antipsychotic?
What mechanism does a dopamine D2 antagonist primarily target?
What mechanism does a dopamine D2 antagonist primarily target?
What is a common side effect associated with prolonged use of D2 receptor antagonists?
What is a common side effect associated with prolonged use of D2 receptor antagonists?
How do third-generation antipsychotics like aripiprazole function in high levels of mesolimbic dopamine?
How do third-generation antipsychotics like aripiprazole function in high levels of mesolimbic dopamine?
Signup and view all the answers
What percentage of patients do not respond to D2 receptor antagonists?
What percentage of patients do not respond to D2 receptor antagonists?
Signup and view all the answers
What percentage of the human brain is made up of fat?
What percentage of the human brain is made up of fat?
Signup and view all the answers
What is hypofrontality associated with in relation to schizophrenia?
What is hypofrontality associated with in relation to schizophrenia?
Signup and view all the answers
Which of the following factors is NOT linked to an increased incidence of schizophrenia?
Which of the following factors is NOT linked to an increased incidence of schizophrenia?
Signup and view all the answers
What percentage chance does a child have of developing schizophrenia if a parent has the disease?
What percentage chance does a child have of developing schizophrenia if a parent has the disease?
Signup and view all the answers
In what age period does schizophrenia typically begin to occur?
In what age period does schizophrenia typically begin to occur?
Signup and view all the answers
Which of the following symptoms is commonly associated with schizophrenia?
Which of the following symptoms is commonly associated with schizophrenia?
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?
Which area of the brain is noted to show changes in individuals with schizophrenia as indicated by MRI scans?
Signup and view all the answers
Which of the following is considered a significant nutrient found in human brains?
Which of the following is considered a significant nutrient found in human brains?
Signup and view all the answers
What is a potential advantage of having long half-life drugs for schizophrenia patients?
What is a potential advantage of having long half-life drugs for schizophrenia patients?
Signup and view all the answers
What factors need to be measured to determine appropriate dosing of a drug with a long half-life?
What factors need to be measured to determine appropriate dosing of a drug with a long half-life?
Signup and view all the answers
What could be a consequence of having long half-life drugs in the body?
What could be a consequence of having long half-life drugs in the body?
Signup and view all the answers
Which of the following associations is incorrect?
Which of the following associations is incorrect?
Signup and view all the answers
Why is the pharmacokinetic profile essential for a drug's effectiveness?
Why is the pharmacokinetic profile essential for a drug's effectiveness?
Signup and view all the answers
Which of the following is NOT considered a positive symptom of schizophrenia?
Which of the following is NOT considered a positive symptom of schizophrenia?
Signup and view all the answers
Which neurotransmitter imbalance is associated with positive symptoms of schizophrenia?
Which neurotransmitter imbalance is associated with positive symptoms of schizophrenia?
Signup and view all the answers
What role does the blood-brain barrier (BBB) play in the brain's microenvironment?
What role does the blood-brain barrier (BBB) play in the brain's microenvironment?
Signup and view all the answers
How does serotonin mainly influence negative symptoms in schizophrenia?
How does serotonin mainly influence negative symptoms in schizophrenia?
Signup and view all the answers
What is a main characteristic of the specialized transporters in the BBB?
What is a main characteristic of the specialized transporters in the BBB?
Signup and view all the answers
What type of cognitive impairment is commonly seen in schizophrenia?
What type of cognitive impairment is commonly seen in schizophrenia?
Signup and view all the answers
What influences the frequency of drug administration?
What influences the frequency of drug administration?
Signup and view all the answers
Why are schizophrenia symptoms difficult to diagnose?
Why are schizophrenia symptoms difficult to diagnose?
Signup and view all the answers
What does 'steady state' refer to in pharmacokinetics?
What does 'steady state' refer to in pharmacokinetics?
Signup and view all the answers
What does NMDA antagonism lead to in the context of schizophrenia?
What does NMDA antagonism lead to in the context of schizophrenia?
Signup and view all the answers
How are metabolites formed during the metabolism of a drug?
How are metabolites formed during the metabolism of a drug?
Signup and view all the answers
What role does the PFC play in the mesocortical dopamine system in schizophrenia?
What role does the PFC play in the mesocortical dopamine system in schizophrenia?
Signup and view all the answers
Which of the following statements about drug clearance is true?
Which of the following statements about drug clearance is true?
Signup and view all the answers
Which receptor subtype is predominantly involved in the negative symptom regulation of serotonin?
Which receptor subtype is predominantly involved in the negative symptom regulation of serotonin?
Signup and view all the answers
What behavioral pattern is common among many individuals with schizophrenia regarding smoking?
What behavioral pattern is common among many individuals with schizophrenia regarding smoking?
Signup and view all the answers
What is the significance of the half-life (T1/2) in drug dosing?
What is the significance of the half-life (T1/2) in drug dosing?
Signup and view all the answers
What is true about Cariprazine's pharmacokinetic profile?
What is true about Cariprazine's pharmacokinetic profile?
Signup and view all the answers
Low levels of dopamine release in the PFC are associated with which type of symptoms?
Low levels of dopamine release in the PFC are associated with which type of symptoms?
Signup and view all the answers
What aspect of glutamate's role in schizophrenia has been observed through pharmacological studies?
What aspect of glutamate's role in schizophrenia has been observed through pharmacological studies?
Signup and view all the answers
Which property of the blood-brain barrier contributes to its selectivity?
Which property of the blood-brain barrier contributes to its selectivity?
Signup and view all the answers
What impact do active metabolites have on the therapeutic effect of a drug?
What impact do active metabolites have on the therapeutic effect of a drug?
Signup and view all the answers
What type of side effects is associated with chlorpromazine, a medication for schizophrenia?
What type of side effects is associated with chlorpromazine, a medication for schizophrenia?
Signup and view all the answers
The principle action of amphetamines in schizophrenia is to:
The principle action of amphetamines in schizophrenia is to:
Signup and view all the answers
What is a common behavioral symptom associated with cognitive impairment in schizophrenia?
What is a common behavioral symptom associated with cognitive impairment in schizophrenia?
Signup and view all the answers
The balance of which neurotransmitters is crucial for understanding schizophrenia's symptoms?
The balance of which neurotransmitters is crucial for understanding schizophrenia's symptoms?
Signup and view all the answers
What effect does a low dose D2 antagonist have in combination with NMDA agonists?
What effect does a low dose D2 antagonist have in combination with NMDA agonists?
Signup and view all the answers
Which drug is an example of a 3rd generation antipsychotic that acts as a dopamine stabilizer?
Which drug is an example of a 3rd generation antipsychotic that acts as a dopamine stabilizer?
Signup and view all the answers
What is the primary role of the cytochrome P-450 enzymes in pharmacokinetics?
What is the primary role of the cytochrome P-450 enzymes in pharmacokinetics?
Signup and view all the answers
How does high protein binding affect a drug's efficacy?
How does high protein binding affect a drug's efficacy?
Signup and view all the answers
What is the primary consequence of first-pass metabolism on drug bioavailability?
What is the primary consequence of first-pass metabolism on drug bioavailability?
Signup and view all the answers
What is the significance of lipophilicity in drug distribution?
What is the significance of lipophilicity in drug distribution?
Signup and view all the answers
Which of the following best describes how dopamine acts in the mesolimbic pathway at high levels?
Which of the following best describes how dopamine acts in the mesolimbic pathway at high levels?
Signup and view all the answers
What is one consequence of a drug's lipophilicity on its pharmacokinetics?
What is one consequence of a drug's lipophilicity on its pharmacokinetics?
Signup and view all the answers
Which drug class primarily targets cognitive symptoms in schizophrenia?
Which drug class primarily targets cognitive symptoms in schizophrenia?
Signup and view all the answers
What role does the Blood-Brain Barrier (BBB) play in pharmacology?
What role does the Blood-Brain Barrier (BBB) play in pharmacology?
Signup and view all the answers
Which type of receptors are D2 partial agonists primarily associated with?
Which type of receptors are D2 partial agonists primarily associated with?
Signup and view all the answers
What aspect of drug distribution can be significantly limited by high protein binding?
What aspect of drug distribution can be significantly limited by high protein binding?
Signup and view all the answers
What impact does grapefruit juice have on drug metabolism?
What impact does grapefruit juice have on drug metabolism?
Signup and view all the answers
What primary factor does NOT affect drug distribution to target tissues?
What primary factor does NOT affect drug distribution to target tissues?
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.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
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.