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Midterm Psychopharm > Final psychopharm > Flashcards

Final psychopharm Flashcards

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1
Q

Paliperidone

A

Antipsychotic (Invega sustenna)
Available as a long acting injectable
Active metabolite of risperidone

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2
Q

First generation antipsychotics and risks

A 
TD
dystonia
akathesia
parkinsonism
Metabolic-wt gain, dyslipidemia, hyperglycemia
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3
Q

clozapine facts

A 
highly effective antipsychotic
risk of several side effects
least likely to cause EPS
used more for refractory pts- most effective
CAN CAUSE AGRANULOCYTOSIS
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4
Q

Olanzapine facts

A

Very effective antipsychotic
chemical derivative of clozapine
reduced EPS, superior to Haldol
Weight gain

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5
Q

First gen antipsychotics names

A 
Haloperidol
chlorpromazine (thorazine)
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6
Q

Big concern and side effect seen with risperidone

A

elevated prolactin levels

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7
Q

secondary negative symptoms of schizophrenia

A

Social isolation from paranoia
apathy from depression
neuroleptic induced parkinsonism

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8
Q

First Generation antipsychotic receptors facts

A

65% occupany of striatal D2 receptors is needed for efficacy
Neuro side effects emerge when there is greater than 80% occupancy
High potency conventional agents (haldol and fluvenazine) are highly selective of D2 so they are more likely to cause EPS (dystonia, akathesia, parkinsonism)

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9
Q

akathesia

A

extremely distressing motor restlessness primarily in lower extremities
CAN BE MISTAKEN FOR PSYCHOTIC AGITATION
DOSE DEPENDENT
CAN SWITCH TO A MED THAT IS KNOWN FOR LESS AKATHESIA
Propanolol can be helpful for akathesia

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10
Q

WHAT TO DO WITH AKATHESIA

A

LOWER THE DOSE
POSSIBLE PROPANOLOL
POSSIBLE MIRTAZEPINE (antagonizes serotonin 2A-receptors implicated in pathology of akathesia

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11
Q

Dystonia

A

sustained muscle spasms (anywhere but often neck, tongue, back)
can occur within the first 4 days
dystonia is rare in atypical antipsychotics like quetiapine and clozapine

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12
Q

antipsychotic induced parkinsonism facts

A

tremor, stiffness, gait disturbance
diminished facial expression
most common in high potency first gen antipsychotics

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13
Q

elderly concerns with first gen antipsychotics

A

High risk anticholinergic effects -constipation, dry mouth, blurred vision, urinary retention, memory impairment

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14
Q

TD facts

A

rarely appears right away (less than 6 mo)
Once occurs may be irreversible
Involuntary, choreiform (quick/nonrythmic) movements of mouth tongue and upper extremities.
also possible dystonic form
lifetime risk 50-60%
Lower dose or switch to clozapine
lowering dose or switching may cause withdrawal dyskinesia that may resolve in 6wks
severe cases-tetrabenzine or deep brain stimulation

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15
Q

neuroleptic malignant syndrome facts

A

Rare, potential lethal complication
hyperthermia
rigidity, confusion,diaphoresis
elevated CPK, leucocytosis

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16
Q

clozapine facts

A

tricyclic dibenzodiazepine derivative antipscyhotic
for tx resistant schizophrenia or schizoaffective
tx of SI
binds to all 5 dopamine subtypes, muscarinic, histaminergic, cholinergic, and seritonergic
Also modulates glutamatergic NMDA sensitivity and BDNF

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17
Q

Aripiprazole pharmacodynamics and kinetics facts

A

Abilify
dihydroquinolinone unrelated to other antipsychotics
approved for schizophrenia and bp mania and mixed
partial agonist of D2-30% activity compared to dopamine
high affinity of 5ht1a partial agonist, full agonist 5ht2A
moderate affinity to alpha adrenergic and histamine
CYP 450 2D6 and 3A4
long half life (up to 94 hrs)
2wks needed to achieve steady level after dose initiation or change

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18
Q

What needs to be done with risperidone and paliperidone? And other concerns?

A

requires careful titration to avoid EPS
Monitoring of hyperprolactinemia
metabolic syndromes

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19
Q

Which two antipsychotics are known to have the highest metabolic liability?

A

Clozapine

Olanzapine

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20
Q

clozapine class and action

A 
tricyclic dibenzodiazepine derivative
binds to several CNS receptors
FDA approved for schizophrenia, schizoaffective, SI
peak plasma levels reached in 2 hrs
CYP 1A2, 3A4, 2D6
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21
Q

clozapine lab requirements

A

To initiate clozapine:
wbc’s at least 3500
ANC at least 2000
weekly cbc x 6mo then biweekly for 6 mo, then monthly if they stay stable

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22
Q

additional cardiac and neuro possible side effects with clozapine

A

myocarditis, cardiomyopathy (0,01-0,2%) present like flu like illness, cp, reduced ejection fraction, elevated CPK, T wave changes
Seizures- 5-10%- usually caused by rapid dose escalation or increased plasma concentrations
Obesity, DM(markedly reduced insulin sensitivity), dyslipidemia

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23
Q

Methylphenidate

A

IR- behavioral effects peak at 1-2 hrs
Dissipate within 3-5
More rapidly absorbed and peaks sooner than Ritalin(similar pharmacokinetic profile)
equal racemic mixture of d,l-threo-MPH

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24
Q

concerta

A

racemic mixture of d,l-threo-MPH 50/50 (essentially methylphenidate)- osmotic release oral system (OROS) labeled for 12 hrs of coverage
instead of Methylphenidate 3x daily

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25
focalin
primary active form of MPH d-threo isomer available in immediate and extended release 10mg of MPH is equivalent to 5mg of d-MPH
26
Daytrana
MPH through the skin via transdermal system effects within 2 hrs and 3 hrs after removal doesnt do first pass metabolism so lower doses may be needed than oral doses Good for pts' who can't tolerate PO
27
Quillivant
AKA MEROS oral suspension MPH may be useful for children who cant tolerate pills or experience skin reactions to the patch
28
Amphetamine forms
dextroamphetamine (dex;dexadrine) Mixed amphetamine salts (MAS;Adderall) Lisdexamphetaminedimesylate (Vyvance;LDX)
29
DEX facts
Behavioral effects peak in 1 to 2 hrs | half life 4-6hrs
30
MAS/Adderall contains
equal portions of 4 amphetamine salts the 2 isomers have different pharmacodynamic properties some pts with ADHD preferentially respond to one isomer over another. efficacy of MAS is well established in youth and adults extended release delivers immediate release then 4 hrs later delayed release
31
LDX/vyvanse
amphetamine prodrug lysine(amino acid) linked to d-amphetamine prodrug is metabolically hydrolyzed in the body to release d-amphetamine to reduce abuse liability.
32
Melatonin
Hormone secreted by the pineal gland helps regulate circadian rythms concerning side effects: Migraines, nightmares, aggression
33
stimulants interactions and side effects
Monitor with simpathomimetic (pseudoephedrine) and TCA's MAOIs contraindicated with stimulants nausea, dry mouth, difficulty falling asleep, obsessiveness, rebound phenomena, anxiety, irritability, dysphoria, wt loss
34
ATMX/atomoxetine
Strattera unscheduled blocks NE reuptake- increasing synaptic NE increases dopamine in the frontal lobes cmax occurs 1-2 hrs plasma half life 4-5 hrs,CNS affects over 24 hrs metabolized cyp2d6 If pt taking other 2d6 meds like fluoxetine, paroxetine, quinidine may need lower doses of ATMX 0.5-1.4mg/kg/d early response up to 10 wks for full effects may be good for pt's with substance abuse issues
35
side effects of ATMX/Strattera
children- decreased appetite, dyspepsia, dizzyness adults- dry mouth, insomnia, nausea, decreased appetite, constipation, dizzyness, decreased libido, sweating, difficulty attaining or maintaining erection. watch for any signs of hepatitis or si
36
clonidine facts
alpha adrenergic agonist primarily used for HTN extended delivery (Kapvay) approved for ADHD youth 6-17 less effective than stimulants but good for traumatized children, ODD and ADHD, and ADHD sleep disturbances
37
clonidine side effects
``` abrupt withdrawal- rebound htn extreme caution with beta or ca channel blockers (ok with stimulants) sedation dry mouth vivid dreams depression confusion ```
38
Guanfacine facts
most selective alpha 2 adrenergic agonist mimics binding of NE in the PFC possible less sedation than clonidine and longer duration of action milder CV profile
39
guanfacine adverse effects
sedation irritability depression
40
buproprion facts
modulates NE and Dopamine | often used in pts with ADHD and comorbidities
41
buproprion side effects
more stimulating than other antidepressants-irritability exacerbate tics drug induced seizures irritability during marijuana withdrawal
42
TCA's for ADHD
effective but less robust than stimulants | may be useful in comorbid anxiety, depression, tics, depression but potential cardiotoxicity
43
Modafinil facts
``` novel stimulant distinct from amphetamine approved for narcolepsy activates hypothalamic regions not for kids SJS potential to exacerbate mania ```
44
Meds for sedation in ETOH withdrawl
Diazepam 10-20mg every 1-2 hrs until sedation achieved Chlordiazepoxide 50-100mg Lorazepam -shorter acting for elderly or liver disease phenobarbitol to augment benzo's and prevent ICU admit
45
DT facts
``` Generally occurs 24-72 hrs after abstinence disorientation (person, place, time) tremor hyperactivity fever marked wakefullness increased autonomic tone hallucinations can last 2-3 days can resolve with sleep prognosis good with meds can cause convulsions, coma, death ```
46
Wernickie's encephalopathy facts
``` opthalmoplegia ataxia mental disturbance nystagmus disorientation exhaustion/lethargy dehydration ```
47
fetal alcohol spectrum disorder signs
``` epicanthal folds (upside v down folds) flat nasal bridge small upper lip smooth philtrum (above upper lip) railroad track ears small palpebral fissures (eyes) ```
48
GAD critera
``` EGADS. Im so MISERA-ble Excessive General Anxiety Daily (most days) Six months ``` ``` 3 or more: Muscle tention Irritability Sleep disturbance Energy Restlessness Attention ```
49
Alzheimers
disease cause by destruction of acetylchoine releasing neurons (ACH-remember autonomic, contraction, hippocampus)
50
ACH
Autonomic-PSNS-bradycardia, gi motility,salivation, sexual arousal Contraction-Muscle Hippocampus-learning, memory, awakeness, attention
51
What can risperidone do?
Cause markedly elevated serum prolactin levels (due to dopamine blockade)
52
what are young pt's at risk for with first gen antipsychotics
Dystonia during the first week
53
cognitive dysfunction in schizophrenia
decline of attention, memory and executive functions. Not very responsive to antipsychotic agents
54
what do you look for in antipsychotic induced parkinsonism?
Tremor and rigidity along with diminished facial expression that can be mistaken for depression. Gait disturbance.
55
Anticholinergic agents in the elderly concern?
constipation, dry mouth, dental caries, blurred vision, urinary retention, memory impairment =DRY LT use in elderly should be avoided. Chlorpromazine and clozapine ++++ Quetiapine ++ Perphenazine ++
56
TD s/s and risk factors
Old age greater than 6 mo first generation neuroleptic exposure Hx of parkinsonian side effects DM risk is reduced with 2nd gen antipsychotics
57
NMS s/s
Rigidity/fever/ALOC - TRIAD ``` (gradually evolves in the following order) confusion rigidity diaphoresis mutism autonomic instability (HR, BP, sweating) hyperthermia elevated cpk ```
58
two 2nd gen antipsychotics with few or no cardiac effects
Olanzapine and aripiprazole
59
clozapine, risperidone, quetiapine, ziprasidone, iloperidone can cause what?
alpha adrenergic side effects-Orthostatic hypotension so they need careful dose titrations clozapine causes more tachycardia and hypotension than others.
60
consider intervention when antipsychotic metabolic changes of ?
5% wt gain 1 point increase in BMI 1 in or greater waist circumference criteria met for metabolic syndrome (obesity, triglycerides 150>, HDL <40men <50 women, BP 130/85>, fasting blood glucose 100>
61
Quetiapine has high affinity for what receptors? Metabolized by?
5HT2a, A1 and A2 adrenergic, Histaminergic CYP3A4 short half life (6hrs) still usually prescribed once daily
62
ziprasidone facts
differs from other antipsychotics with moderate reuptake of serotonin and norepiephrine(noradrenaline) Absorption greatly increased with a meal within 1 hr and decreases half life known for not causing wt gain, normalizing lipids and lowering prolactin levels monitor cardiac risk factors
63
Aripiprazole mech of action and facts
Partial agonist of D2(so not associated with eps) affinity to sertonergic, histaminergic and alpha 1 adrenergic receptors CYP2D6 and 3A4 75-94 hr half life. Needs two weeks to achieve steady state drug levels following a dose change. known for less prolactin elevation(good choice for a pt with other antipsychotic induced hyperprolactinemia), less akathesia, less need for tx of eps
64
Iloperdone facts
Finapt High affinity for d2 and 5th2a tx of schizophrenia titrate slowly for orthostatic hypotension
65
Lurasidone facts
Latuda High affinity for D2 and 5ht2a Half life of 18hrs absorption increased with food-must take with 350 cal can increase prolactin levels, eps (including akathesia)
66
serious side effects from clozapine and ?
fluvoxamine and erythromycin- Obtundation and CV effects drugs that induce hepatic metabolism (like carbamazepine and phenobarb, phenytoin) can lower antipsychotic concentrations and can cause loss of therapeutic efficacy.
67
ziprazidone and iloperidone caution
significantly effect cardiac conduction so should not be combined with low potency phenothiazines or antiarrhythmics
68
Memantine facts
Normalizes levels of glutamate(neurotransmitter involved in learning and memory- glutamate in excessive quantities contributes to neurodegeneration) NMDA antagonist
69
Cholinesterase inhibitors for AD
Donazepil (aricept) Rivastigmine Galantamine
70
Tx for frontotemporal dementia and what to avoid
SSRI's for tx of symptoms Antipsychotics and mood stabilizers sparingly Avoid cholinesterase inhibitors and memantine- may exacerbate neuropsych sx
71
Tx of vascular dementia
control of vascular risk factors-high cholesterol, HTN, inactivity, DM, etoh, cigarettes and hyperhomocystinemia

Midterm Psychopharm (2 decks)

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