Psychopharmacology Exam 2 (part 2)

通報

問題一覧

What is the difference between typical and atypicals related to binding?

Typicals have D2 binding only whereas Atypicals have D2 and 5HT2A binding

Explain the difference between SE of Typicals vs Atypicals

Atypicals have less EPS/TD, DIP, Prolactin, and they dont worsen negative symptoms

Explain how well Typicals work vs Atypicals

There is no difference in efficacy between them

Direct innervation (via the direct pathway) of glutamate pyramidal neurons causes increase of dopamine release in the mesolimbic/mesostriatam leads to what symptoms?

Positive symptoms

Indirect innervation (via the indirect pathway) of glutamate pyramidal neurons in the SN activates a GABA neuron which in turn decreases dopamine in the nigrostriatal pathway leads to what symptoms?

DIP

Indirect innervation (via the indirect pathway) of glutamate pyramidal neurons in the mesocortical pathway (via the VTE) inhibits a GABA neuron which decreases dopamine in the PFC and leads to what symptoms?

Negative/cognitive/affective symptoms

Reduces EPS by increasing Dopamine in the nigrostriatal areas.

5HT2A antagonism

Reduces negative symptoms (via the indirect pathway) by improving dopamine in the prefrontal cortex.

5HT2A antagonism

Has antidepressant effects by increasing dopamine in the ventromedial prefrontal cortex.

5HT2A antagonism

Reduce hyperprolactinaemia.

5HT2A antagonist

Is always inhibitory and can be found pre-synaptically and post-synaptically, and leads to downstream effects that reduce DIP and negative/cognitive symptoms.

5HT1A

D2 antagonism and/or D2 partial agonism are effective in treating?

Mania

D2/5HT2A antagonism, D2/5HT1A partial agonism can cause?

Antidepressant actions

What receptor combo has the most potential for weight gain?

5HT2C + H1

What drug is FDA approved for treating the negative symptoms of schizophrenia?

None

Causes weight gain via decrease in limbic dopaminergic activity, possibly increasing reward-seeking behaviors such as food intake; can also contribute to weight gain via disinhibition of prolactin release from the hypothalamus

D2 antagonism

Causes weight gain via increase in hypothalamic AMP-related kinase activity, which leads to increased appetite; sedative effects may lead to reduction in mobility

H1 antagonism

Not directly correlated with weight gain, but causes diabetes via impairment of glucose tolerance and reduction of insulin secretion from pancreatic beta cells

M3 antagonism

May mitigate weight effects due to serotonin-2C antagonism; may decrease carbohydrate craving

5HT1A partial agonism

Causes weight gain via disinhibition of hypothalamic neuropeptide Y neurons and inhibition of pro-opiomelanocortin neurons; may also influence leptin resistance

5HT2C antagonism

What is unique about the "-pines" (Clozapine, Quetiapine, Olanzapine, Asenapine)?

They are all sedating and cause weight gain as a class, and work on alpha, H1, and M3 receptors

What is the indication for using Clozapine?

Treatment resistant schizophrenia

At what dose do you begin to see the adverse effects of clozapine?

600 mg per day

Why would you not want to give cogentin or benadryl to treat excess salvation (sialorrhea) during clozapine treatment?

The potential for an illeus

What is the preferred treatment for sialorrhea during clozapine treatment?

Atropine

What antipsychotic is the only med known to reduce suicide?

Clozapine

What drug would be contraindicated to give with clozapine and why?

Luvox, because it is a CYP1A2 inhibitor and clozapine is metabolized via CYP1A2 which would cause it to reach dangerous levels

Why is it important to know the smoking status of your patient on clozapine?

Because smoking is an inducer of CYP1A2 which will reduce clozapine levels. When they are admitted to the hospital they will have to quit temporarily and the dose will be decreased, but when they are discharged it is important to increase the dose when they pick up smoking again.

What are the adverse effects of clozapine?

Myocarditis, Agranulocytosis, Seizures, Sedation, Sialorrhea, Weight Gain, Constipation, Orthostatic Hypotension

What does your ANC count need to be to take clozapine?

> 1500

What is the patient lab schedule while on clozapine?

Check ANC weekly for 1st 6 months, then bi-weekly for another 6 months, then every month for the rest of their lives

What should you avoid giving while giving Olanzapine IM and why?

Benzos r/t excess sedation

What receptors does clozapine have the highest affinity for and what can this cause?

H1, alpha 1, M1, M3; anticholinergic actions, orthostatic hypotension, sedation, and weight gain

What risk category are the following in relation to clozapine: sedation, weight gain, and EPS

Sedation = high Weight gain = high EPS = low

What receptors does olanzapine have the highest affinity for and what does that result in?

5HT2C, H1, and M3; Antidepressant actions, weight gain ++, and sedation

Explain the EPS/TD risk profile of olanzapine

Lower risk overall but still higher than clozapine

What is the binding profile of quetiapine and what symptoms does that cause?

5HT2A, 5HT1A, NRI, 5HT2C, H1, M1 and M3, alpha 2; it causes Antidepressant actions, sedation, and weight gain

What is the favored antipsychotic drug for Parkinson's psychosis and why?

Quetiapine because it has a low risk for EPS

Discuss the adverse effects of quetiapine r/t sedation, weight gain, and EPS

Sedation: high Weight gain: high EPS: low

What is the dose to achieve a hypnotic effect with quetiapine?

50 mg

What is the dose to acheive a antidepressant effect with quetiapine?

300 mg

What is the dose that is required to achieve an antipsychotic effect with quetiapine?

800 mg

What is the only "-pine" that comes in SL, Buccal, or Patch?

Asenapine

What is the most common complaint about taking Asenapine?

It tastes bad and can cause numbness and tingling of the mouth and tongue

What patient populations can Asenapine treat?

Schizophrenics, Bipolar, and Child/Adolescents

What is the binding affinity of asenapine and what symptoms does that cause?

5HT2C, 5HT1A, 5HT1B, 5HT1D, 5HT7, alpha 2, and H1; Antidepressant actions, sedation, and weight gain

Discuss the adverse effects of aspenpine r/t: sedation, weight gain, and EPS

Sedation: high Weight gain: moderate EPS: moderate

Which of the "-dones and an -rone" must be taken with food?

Ziprasidone (Geodon), Lurasidone (Latuda), Lumateperone (Caplyta)

What are the doses for risperidone where it behaves like a atypical and when it behaves like a typical antipsychoic?

< 6 mg = atypical behavior > 6 mg = typical behavior

What are the binding affinities for risperidone and what does this cause?

5HT2A and alpha 1; causes hyperprolactemia, sedation, and orthostatic hypotension

What are the side effect profiles of risperidone r/t: sedation, weight gain, and EPS?

Sedation = medium Weight gain = high EPS = high

What are the major risks and benefits of paliperidone?

Risk: Hyperprolactemia Benefit: Less sedating

Discuss the binding affinty profile of paliperidone and what that causes?

5HT2A and alpha 2; hyperprolactemia, low sedation, mood stabilizer

What causes paliperidone to be more sustained release allowing for daily dosing?

It is not metabolized by the liver but extreted in the urine

Discuss the side effect profile of paliperidone r/t: sedation, weight gain, EPS

Sedation: moderate Weight gain: moderate EPS: high

Why does ziprasidone require twice daily dosing?

Because it must be taken with 500 calories of food for a total of 1000 calories per day

What is a major S/E we are worried about with ziprasidone?

Prolonged QT

Discuss the binding profile of ziprasidone and what that causes?

5HT2C, 5HT1A, 5HT1B, 5HT1D, 5HT7, alpha 2; Antidepressant effects, low weight gain, low sedation

Discuss the S/E profile of ziprasidone r/t: sedation, weight gain, EPS

Sedation: moderate Weight gain: low EPS: high

What about iloperiodes binding profile causes orthostatic hypotension and sedation?

Potent alpha 1 antagonism

In order to avoid orthostatic hypotension in iloperidone what treatment plan is used?

Titrate slowly over several days to avoid orthostatic hypotension

How often is iloperidone given?

Twice a day

Patients that are sensitive to the motor S/E of antipsychotics should consider taking?

Iloperidone

This drug is taken daily with 350 calories of food daily?

Lurasidone

Discuss the S/E profile of lurasidone r/t: Sedation, Weight Gain, EPS

Sedation: moderate Weight Gain: low EPS: moderate

What is lurasidone a substrate for, and what inducers and inhibitors to watch out for?

CYP3A4. Inducers: Tegretol, St John's Wort; Inhibitors: Grapefruit

Must be taken with food - no calorie specification however. Dosed daily, and may be used as an antidepressant.

Lumateperone

Because there is a wide gap between the binding affinities of D2 and 5HT2A in lumateperone with stronger binding favoring 5HT2A, what are the resulting effects?

EPS: low Prolactin: low Sedation: high

Blocks serotonin 2A receptors, causing enhancement of dopamine release in certain brain regions and thus reducing motor side effects and possibly improving cognitive and affective symptoms

Lumateperone

-Blocks postsynaptic dopamine 2 receptors, reducing positive symptoms of psychosis and stabilizing affective symptoms -Binds as a partial agonist at presynaptic D2 receptors

Lumateperone

-Binds to D1 receptors, with preclinical data showing D1-dependent activation of AMPA receptors leading to activation of the mTOR pathway, a mechanism that has been associated with antidepressant effects -Also has affinity for the serotonin reuptake pump (SERT, serotonin transporter)

Lumateperone

What are the major S/E and benefits of the "-pips and a -rip" (Apripiprazole, Brexpiprazole, and Cariprazine)?

High risk of akathesia, but not sedating, low weight gain and prolactin level

What is the binding affinity profile of the "-pips and a -rip" (Apripiprazole, Brexpiprazole, and Cariprazine)?

D2 & 5HT1A partial agonists

What is the binding profile of aripiprazole, and what does that result in?

5HT7, 5HT1A partial agonist; high akathesia, antidepressant actions, low sedation, low weight gain, and low EPS

What drug has less akathesia than abilify but is more sedating?

Brexpiprazole

What is the binding affinitiy profile for brexpiprazole, and what does that result in?

5HT7, 5TH1A partial agonist, alpha 1; anxyolitic, antidepressant, low weight gain, low sedation, and moderate EPS

This drug is very forgiving once steady state is reached due to a long active metabolite, so you must titrate very slowly!

Cariprazine

Discuss the binding affinity of cariprazine, and what that results in?

High D3 partial agonist and 5HT1A partial agonist; antidepressant actions that can treat negative symptoms of schizophrenia, bipolar mixed features, depression, and substance use. Also has low sedation and weight gain, and moderate EPS.

-Only “antipsychotic” that has NO action on dopamine receptors -Selective 5HT2A antagonist (inverse agonist)

Pimavanserin

What is the drug of choice for Parkinson's psychosis?

Pimavanserin or Quetiapine

Patho Renal

Patho Renal

Pathophysiology

Pathophysiology

Two Clean Queens · 34問 · 2年前

Patho Immunology

Patho Immunology

34問 • 2年前

Patho Hematology

Patho Hematology

Two Clean Queens · 76問 · 2年前

Patho Hematology 2

Patho Hematology 2

76問 • 2年前

Patho Respiratory

Patho Respiratory

Two Clean Queens · 54問 · 2年前

Patho Respiratory 2

Patho Respiratory 2

54問 • 2年前

Patho Cardiovascular

Patho Cardiovascular

Two Clean Queens · 56問 · 2年前

Patho Cardiovascular 2

Patho Cardiovascular 2

56問 • 2年前

Two Clean Queens · 52問 · 2年前

Patho MSK

Patho MSK

52問 • 2年前

Two Clean Queens · 35問 · 2年前

Patho Acid Base

Patho Acid Base

35問 • 2年前

Two Clean Queens · 10問 · 2年前

Renal 2

Renal 2

10問 • 2年前

Two Clean Queens · 43問 · 2年前

Fluid Balance

Fluid Balance

43問 • 2年前

Patho Endocrine

Patho Endocrine

Two Clean Queens · 42問 · 2年前

Patho Endocrine 2

Patho Endocrine 2

42問 • 2年前

Two Clean Queens · 58問 · 2年前

Infections

Infections

58問 • 2年前

Two Clean Queens · 31問 · 2年前

Patho Shock

Patho Shock

31問 • 2年前

Two Clean Queens · 18問 · 2年前

GI 2

GI 2

18問 • 2年前

Two Clean Queens · 54問 · 2年前

Cancer

Cancer

54問 • 2年前