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Midterm Psychopharm > Final psychopharm > Flashcards

Final psychopharm Flashcards

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
Q

focalin

A

primary active form of MPH d-threo isomer available in immediate and extended release
10mg of MPH is equivalent to 5mg of d-MPH

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26
Q

Daytrana

A

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

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27
Q

Quillivant

A

AKA MEROS
oral suspension MPH
may be useful for children who cant tolerate pills or experience skin reactions to the patch

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28
Q

Amphetamine forms

A

dextroamphetamine (dex;dexadrine)
Mixed amphetamine salts (MAS;Adderall)
Lisdexamphetaminedimesylate (Vyvance;LDX)

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29
Q

DEX facts

A

Behavioral effects peak in 1 to 2 hrs

half life 4-6hrs

30
Q

MAS/Adderall contains

A

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
Q

LDX/vyvanse

A

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
Q

Melatonin

A

Hormone secreted by the pineal gland helps regulate circadian rythms
concerning side effects: Migraines, nightmares, aggression

33
Q

stimulants interactions and side effects

A

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
Q

ATMX/atomoxetine

A

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
Q

side effects of ATMX/Strattera

A

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
Q

clonidine facts

A

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
Q

clonidine side effects

A 
abrupt withdrawal- rebound htn
extreme caution with beta or ca channel blockers
(ok with stimulants)
sedation
dry mouth
vivid dreams
depression
confusion
38
Q

Guanfacine facts

A

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
Q

guanfacine adverse effects

A

sedation
irritability
depression

40
Q

buproprion facts

A

modulates NE and Dopamine

often used in pts with ADHD and comorbidities

41
Q

buproprion side effects

A

more stimulating than other antidepressants-irritability
exacerbate tics
drug induced seizures
irritability during marijuana withdrawal

42
Q

TCA’s for ADHD

A

effective but less robust than stimulants

may be useful in comorbid anxiety, depression, tics, depression but potential cardiotoxicity

43
Q

Modafinil facts

A 
novel stimulant distinct from amphetamine
approved for narcolepsy
activates hypothalamic regions
not for kids
SJS
potential to exacerbate mania
44
Q

Meds for sedation in ETOH withdrawl

A

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
Q

DT facts

A 
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
Q

Wernickie’s encephalopathy facts

A 
opthalmoplegia
ataxia
mental disturbance
nystagmus
disorientation
exhaustion/lethargy
dehydration
47
Q

fetal alcohol spectrum disorder signs

A 
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
Q

GAD critera

A 
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
Q

Alzheimers

A

disease cause by destruction of acetylchoine releasing neurons
(ACH-remember autonomic, contraction, hippocampus)

50
Q

ACH

A

Autonomic-PSNS-bradycardia, gi motility,salivation, sexual arousal
Contraction-Muscle
Hippocampus-learning, memory, awakeness, attention

51
Q

What can risperidone do?

A

Cause markedly elevated serum prolactin levels (due to dopamine blockade)

52
Q

what are young pt’s at risk for with first gen antipsychotics

A

Dystonia during the first week

53
Q

cognitive dysfunction in schizophrenia

A

decline of attention, memory and executive functions. Not very responsive to antipsychotic agents

54
Q

what do you look for in antipsychotic induced parkinsonism?

A

Tremor and rigidity along with diminished facial expression that can be mistaken for depression. Gait disturbance.

55
Q

Anticholinergic agents in the elderly concern?

A

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
Q

TD s/s and risk factors

A

Old age
greater than 6 mo first generation neuroleptic exposure
Hx of parkinsonian side effects
DM

risk is reduced with 2nd gen antipsychotics

57
Q

NMS s/s

A

Rigidity/fever/ALOC - TRIAD

(gradually evolves in the following order)
confusion
rigidity
diaphoresis
mutism
autonomic instability (HR, BP, sweating)
hyperthermia
elevated cpk
58
Q

two 2nd gen antipsychotics with few or no cardiac effects

A

Olanzapine and aripiprazole

59
Q

clozapine, risperidone, quetiapine, ziprasidone, iloperidone can cause what?

A

alpha adrenergic side effects-Orthostatic hypotension so they need careful dose titrations
clozapine causes more tachycardia and hypotension than others.

60
Q

consider intervention when antipsychotic metabolic changes of ?

A

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
Q

Quetiapine has high affinity for what receptors? Metabolized by?

A

5HT2a, A1 and A2 adrenergic, Histaminergic
CYP3A4
short half life (6hrs) still usually prescribed once daily

62
Q

ziprasidone facts

A

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
Q

Aripiprazole mech of action and facts

A

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
Q

Iloperdone facts

A

Finapt
High affinity for d2 and 5th2a
tx of schizophrenia
titrate slowly for orthostatic hypotension

65
Q

Lurasidone facts

A

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
Q

serious side effects from clozapine and ?

A

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
Q

ziprazidone and iloperidone caution

A

significantly effect cardiac conduction so should not be combined with low potency phenothiazines or antiarrhythmics

68
Q

Memantine facts

A

Normalizes levels of glutamate(neurotransmitter involved in learning and memory- glutamate in excessive quantities contributes to neurodegeneration)

NMDA antagonist

69
Q

Cholinesterase inhibitors for AD

A

Donazepil (aricept)
Rivastigmine
Galantamine

70
Q

Tx for frontotemporal dementia and what to avoid

A

SSRI’s for tx of symptoms

Antipsychotics and mood stabilizers sparingly

Avoid cholinesterase inhibitors and memantine- may exacerbate neuropsych sx

71
Q

Tx of vascular dementia

A

control of vascular risk factors-high cholesterol, HTN, inactivity, DM, etoh,
cigarettes and hyperhomocystinemia

Midterm Psychopharm (2 decks)

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