Red/Bolded Parts in PPTs that match Study Guide Flashcards
Study of what the drugs do to the body (i.e. target sites for drugs- receptors, ion channels, enzymes (MAOIs) and carrier proteins/reuptake pumps)
- Pharmacokinetics
- Pharmacodynamics
Pharmacodynamics
There are more than ___ NT in the brain.
- 10
- 30
- 50
- 70
50
___ Risk cannot be rule out
___ Controlled studies show no risk
___ No evidence of risk in humans
___ Absolutely contraindicated in pregnancy
___ Positive evidence of risk
A, B, C, D, X
Match letter to rating.
A: Controlled studies show no risk
B: No evidence of risk in humans
C: Risk cannot be rule out
D: Positive evidence of risk
X: Absolutely contraindicated in pregnancy
o Locus Cerelus: Key center of ___ production
Remember Fight/Flight - concentration, focus, energy, HR, BP, Glucose
- 5HT
- NE
NE
o Ralphe Nuclei: Key center for ___ production
NOTE: 90% of serotonin in found in the GI tract
- 5HT
- NE
5HT
Inhibitory at the postsynaptic neuron
- Acetylcholine (ACh)
- Glutamate = “on”
- Gamma-aminobutyric acid (GABA) = “off”
Gamma-aminobutyric acid (GABA) = “off”
Excitatory at the post-synaptic neuron
- Acetylcholine (ACh)
- Glutamate = “on”
- Gamma-aminobutyric acid (GABA) = “off”
Glutamate = “on”
Involved in learning and memory (brain’s cholinergic neurons play a critical role in dementias)
- Acetylcholine (ACh)
- Glutamate = “on”
- Gamma-aminobutyric acid (GABA) = “off”
Acetylcholine (ACh)
Antipsychotics must occupy more than ___% of D2 receptors to cause EPS
- 20%
- 40%
- 60%
- 80%
80%
- Blockade of DA in this pathway produces increased motor movements
e.g. EPS (Pseudo parkinsonism, Akathisia, dystonia & TD)
- Mesolimbic Pathway
- Mesocortical Pathway
- Tuberoinfundibular Pathway
- Nigrostriatal Pathway
Nigrostriatal Pathway
- Note: Dopamine inhibits prolactin.
- Therefore, blockade of dopamine= ↓DA= ↑ Prolactin
- Mesolimbic Pathway
- Mesocortical Pathway
- Tuberoinfundibular Pathway
- Nigrostriatal Pathway
Tuberoinfundibular Pathway
- Associated with the negative symptoms of Schizophrenia (i.e. cognition, affect, apathy, behavior etc.)
- Mesolimbic Pathway
- Mesocortical Pathway
- Tuberoinfundibular Pathway
- Nigrostriatal Pathway
Mesocortical Pathway
- Associated with positive symptoms of schizophrenia (i.e. hallucinations, delusions etc)
- Mesolimbic Pathway
- Mesocortical Pathway
- Tuberoinfundibular Pathway
- Nigrostriatal Pathway
Mesolimbic Pathway
______in the mesolimbic area
- ↑Dopamine
- ↓Dopamine
- ↓Serotonin
- ↑Dopamine
______ activity in the Mesocortical area
- ↑Dopamine
- ↓Dopamine
- ↓Serotonin
- ↓Dopamine
______ (down regulation) in the frontal cortex
- ↑Dopamine
- ↓Dopamine
- ↓Serotonin
- ↓Serotonin
Antipsychotic _____________ can increase the risk of or re-hospitalization, diabetes, EPS, sedation, seizures, metabolic effects, mortality, and sudden cardiac death.
- polypharmacy
- toxicity
- resistance
polypharmacy
Delusions
Conceptual disorganization
Excitement
Grandiosity
Hostility
Hallucinations
- Negative symptoms
- Positive symptoms
Positive symptoms
Affect (flat, constricted)
Alogia (absence of speech) (
Apathy/Avolition
Attention (poor, lacking)
Anhedonia
Asociality
- Negative symptoms
- Positive symptoms
Negative symptoms
_____ potency
Low EPS= High antiadrenergic, anticholinergic and antihistaminic s/e, more lethal in overdose d/t QTC prolongation
- Low
- High
Low
_____ potency
High EPS= Low antiadrenergic, anticholinergic and antihistaminic s/e
- Low
- High
High
These manage positive symptoms of schizophrenia
- Antidepressants
- Mood stabilizers
- FGAs
- SGAs
FGAs
IM administration in Acute agitation or psychosis
- Seroquel
- Haldol
- Abilify
- Clozapine
Haldol
FGA side effects:
QTC prolongation?
Obtain:
baseline EKG
FGA side effects:
Orthostasis
Blockde of?
blockade of α1 receptors
FGA Side Effects:
___________ liver enzymes
- Decreased
- Elevated
Elevated
FGA Side Effects:
EPS consists of these 3 things:
EPS (Akathisia, dystonia, Parkinsonism)
FGA Side Effects:
hyperprolactinemia
(decreased libido, galactorrhea, gynecomastia, impotence, amenorrhea)
FGA Side Effects:
hyperprolactinemia in men
- Men= Gynecomastia, erectile dysfunction, low libido, galactorrhea
- Women = galactorrhea and absence of menses, low libido
- Men= Gynecomastia, erectile dysfunction, low libido, galactorrhea
FGA Side Effects:
hyperprolactinemia in women
- Men= Gynecomastia, erectile dysfunction, low libido, galactorrhea
- Women = galactorrhea and absence of menses, low libido
- Women = galactorrhea and absence of menses, low libido
EPS – due to?
- alpha 1 blockade
- beta 1 blockade
- gamma 1 blockade
- delta 1 blockade
alpha 1 blockade
Tardive dyskinesia:
torticollis definition?
contraction of neck muscles
Tardive dyskinesia is mostly irreversible.
True or false?
True
Risk factors for tardive dyskinesia:
High doses, long duration, old age, women, hx of EPS, substance abuse (heavy smoking), diabetes
-
-Management of tardive dyskinesia:
benztropine (Cogentin); Dose reduction; D/C med; switch to an atypical antipsychotic; Clonazepam, Amantidine, Tetrabenazine.
-
First FDA approved treatment for TD:
- Inderal
- Valbenazine, Ingrezza
- Suboxone
- Tylenol
(Valbenazine, Ingrezza)
Regarding tardive dyskinesia:
-AIMS (Abnormal Involuntary Movement Scale) testing initially then Q3-6 months
-
-Patient Education for tardive dyskinesia:
TD symptoms may initially worsen transiently as medication dosages are lowered.
True or false?
True
Consider switching to clozapine (Clozaril) due to:
(Lowest risk of TD)
TX for akathisia:
- beta-blocker – propranolol
- benztropine (Cogentin)
beta-blocker – propranolol
TX for pseudo-parkinsonism:
- beta-blocker – propranolol
- benztropine (Cogentin)
- benztropine (Cogentin)
Life-threatening idiopathic reaction to antipsychotic medications (more common w/ FGAs)
Neuroleptic malignant syndrome (NMS)
Medical Emergency w/ 20% mortality rate if untreated
what is it?
Neuroleptic malignant syndrome
Per what syndrome?
Clinical features (FALTERED):
Fever
Autonomic instability (BP, HR)
Leukocytosis
Tremor
Elevated CK
Rigidity
Excessive sweating
Delirium
Neuroleptic malignant syndrome
Management of which syndrome?
- D/C medication
- Supportive care (hydration, IV benzos- for relaxation; cooling blankets)
- Administer sodium dantrolene, bromocriptine, amantadine
- ECT can be effective
Neuroleptic malignant syndrome
Do not co-prescribe drugs in efforts to prevent EPS. (Associated w/ high anticholinergic side effects)
True or false?
True
If necessary, anticholinergics should be prescribed at the lowest dose possible.
True or false
True
manage positive and negative symptoms of schizophrenia
Accounts for 80% of total antipsychotics prescribed.
- SGAs (-dones & -pines)
- FGAs
- SGAs (-dones & -pines)
SGAs MOA:
Blocks both dopamine and serotonin receptors
SGAs are used to treat:
acute mania, bipolar disorder and as adjunctive in unipolar depression
SE of SGAs:
obesity, elevated triglycerides, low HDL levels, BP greater than 135/85
Which syndrome is this?
Metabolic syndrome
Regarding SGAs and this SE syndrome:
Obtain baseline and monitor BMI, weight, fasting glucose, waist circumference, BP, HbA1c and fasting lipids
Metabolic syndrome
Regarding SGAs and this SE syndrome:
NOTE: For patients established on SGA medications, _________ labs should be considered.
- daily
- monthly
- quarterly
- yearly
yearly
SGAs SE:
Common with Clozapine, Olanzapine, Quetiapine
Weight gain
SGAs SE:
Least with Aripiprazole, haloperidol, ziprasidone and lurasidone
Weight gain
SGAs and weight gain:
Monitoring: Weight, BMI, waist circumference per guidelines
SGAs and weight gain:
- Management: Switch to weight neutral medication
- May add to regimen: Topiramate, Metformin, Orlistat, Aripiprazole.
H1 receptor antagonism is associated with sedation and weight gain
true or false?
true
SGA meds
Strongest H1 antagonism*
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
quetiapine (Seroquel)
SGA meds
- Causes significant weight gain, sedation and dyslipidemia (strong H1 antagonism)
- Acute agitation IM acts within 15 min
- Monitor for dose-related hyperprolactinemia
- PO/IM/LAI formulation
- Relprevv (Injection)= Monitor 3 hours post injection d/t risk of delirium & sedation syndrome (Post injection syndrome)
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
olanzapine (Zyprexa)
SGA meds
**Greatest prolactin elevation
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
risperidone (Risperdal)
SGA meds
**Weight neutral
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
ziprasidone (Geodon)
SGA meds
- Weight neutral
- Watch for orthostatic hypotension
- Adjunctive tx of depression, bipolar
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
aripiprazole (Abilify)
SGA meds
- Take w/ food
- Approved for bipolar depression
- Low risk for metabolic syndrome
- Use with caution in patients w/ hepatic impairment.
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
lurasidone (Latuda)
SGA meds
- Used to treat refractory schizophrenia (i.e., treatment resistant)
- Only antipsychotic shown to decrease SI risk
- Less likely to cause TD
- Weight gain is most prominent
- More anticholinergic s/e- tachycardia, constipation etc.
- Hypersalivation (sialorrhea) occurs in 30-80%
- Chew sugarless gum
- Place towel over pillow especially if nocturnal sialorrhea is a problem
- Med: Glycopyrrolate (Robinul) -fewer Anticholinergic side effects)
- Benztropine, Artane etc.
- Agranulocytosis (highest first 3 months of treatment)= Monitor WBC and Absolute neutrophil count (ANC)
- **Perform WBC/ANC weekly for first 6 months of treatment and can decrease frequency there-after
- D/C med if ANC is <1.5 (1500)
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
clozapine (Clozaril)
SGA meds
Used in Parkinson’s related psychosis (newer med)
- quetiapine (Seroquel)
- olanzapine (Zyprexa)
- risperidone (Risperdal)
- ziprasidone (Geodon)
- aripiprazole (Abilify)
- lurasidone (Latuda)
- clozapine (Clozaril)
- Pimavanserin/Nuplazid
Pimavanserin/Nuplazid
_________ induces CYP1A2 enzymes and lowers the levels of certain antipsychotic medications.
- Drinking
- Smoking
- Exercising
Smoking
Haldol and Prolixin use _________ oil – watch for allergic reactions in patients sensitive to it
- olive
- chili
- grapeseed
- sesame
sesame oil
Increased risk of death when used in the elderly and those with dementia related psychosis.
What drug class?
Antipsychotics
Antipsychotics can be used for tx of agitation or psychosis in patients with dementia when symptoms are severe, dangerous and cause significant distress to the patient.
-
Antipsychotics are associated with an increased risk of falls and non-vertebral fractures in patients 65+.
True or false?
True
No antipsychotic medication is approved in patients with dementia.
True or false
True
Mood Disorders
Neurotransmitters/Monoamine hypothesis:
Depression = ↓Serotonin; ↓Dopamine; ↓NE
Monoamine Hypothesis:
Deficient brain 5HT and/or NE results in depression
-
Target symptoms for antidepressants:
Depressed mood, sleep/rest distress, anxiety, irritability, impaired concentration/memory, appetite disturbances, agitation, anhedonia, impaired energy/motivation.
Classes of antidepressants:
SSRI, SNRI, NDRI, SPARI, TCA, MAOI
Maintenance therapy for antidepressants:
- 2-4 months
- 6-13 months
- 8-14 months
- 3-7 months
6-13 months
Factors affecting drug choice of antidepressants
Cost, patient symptoms, previous treatment of patient or family member, side effect profile, comorbid conditions, risk of suicide.
Top distressing side effects of ADs
Sexual dysfunctions, sleep disturbance, weight gain
Meds to avoid in patients with SI
- SSRIs
- TCAs, benzos
- MAOIs
- SNRIs, benzos
TCAs, benzos etc
Adverse effects of ADs
- Sexual Dysfunction
o Highest with SSRI/SNRIs
o Impaired sexual motivation, desire, arousal, and orgasm affecting men and women
o Highest with Venlafaxine and SSRIs
o Lowest with Bupropion, trazodone, nefazodone, mirtazapine
o Management
First line- switch to bupropion (Wellbutrin)
Use of phosphodiesterase -5 inhibitors such as sildenafil (Viagra) or tadalafil (Cialis)
Sexual dysfunction and ADs are highest with:
- MAOIs
- SSRIs/SNRIs
- TCAs
- NDRIs
SSRIs/SNRIs
Sexual dysfunction and ADs are highest with:
- Venlafaxine and SSRIs
- Bupropion, trazodone, nefazodone, mirtazapine
Venlafaxine and SSRIs
Sexual dysfunction and ADs are lowest with:
- Venlafaxine and SSRIs
- Bupropion, trazodone, nefazodone, mirtazapine
- Bupropion, trazodone, nefazodone, mirtazapine
First line management of sexual dysfunction in ADs
- switch to acetaminophen (Tylenol)
- switch to bupropion (Wellbutrin)
- switch to alprazolam (Xanax)
- switch to bupropion (Wellbutrin)
Use of phosphodiesterase -5 inhibitors such as sildenafil (Viagra) or tadalafil (Cialis) can be used to treat sexual dysfunction in ADs
-
Serotonin Syndrome
o S=Shivering
o H=Hyperreflexia/Myoclonic jerks
o I = Increased Temp (Fever)
o V= Vitals Instability (↑↓BP; ↑RR; ↑HR)
o E= Encephalopathy (Confusion)
o R= Restlessness
o S= Sweating (Diaphoresis)
-