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Pharm III > Exam 1 Antipsychotics > Flashcards

Exam 1 Antipsychotics Flashcards

1
Q

What is Schizophrenia

A

neuro-developmental disorder with onset in late adolescence, early adulthood characterized by hallucinations, delusions, disorganized thinking and emotional abnormalities

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2
Q

First antipsychotic tx

A

chlorpromazine

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3
Q

Schizophrenics have increased activity in what pathway? Decreased in what?

A

increased in Limbic, decreased in frontal

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4
Q

Positive sx of Schizophrenia include

A

hallucinations (auditory and visual) and delusions
*disorganized speech and thinking

  • due to over active DA pathways in limbic
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5
Q

Negative sx of Schizophrenia include

A

apathetic, withdrawn, anti-social, lack of motivation, depressed

  • due to under active dopamine pathways in frontal cortex
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6
Q

What cognitive impairment do Schizophrenics have

A

distracted, disorganized thought, memory loss

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7
Q

Hypotheses of Schizo

A

DA and Serotonin hypotheses

  • DA increased can induce psychosis, antipsych block DA R
  • 5-HT mediates DA transmission

other = glutamate (PCP, KEtamine)

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8
Q

What are the 4 DA pathways

A
  1. Mesolimbic: VTA to limbic (emotion)
  2. Mesocortical: VTA to frontal cortex (cognition, emotion)
  3. Nigrostriatal: SN to striatum (motor control)
  4. Tuberoinfundibular: hypothalamus to pituitary (PRL)
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9
Q

What two major classes of antipsychotics are there and major actions?

A

Classical: “neuroleptics”, block DA D2 receptors to target mesolimbic system (+ sx)

Atypical: block 5-HT2a and DA D2 receptors to target mesocortical system (+/- sx)

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10
Q

D2 distributed where? D4?

A

D2 = limbic region

D4 = cortical

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11
Q

Prochlorperazine is

A

antipsychotic that is an antiemetic

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12
Q

What are general effects of antipsychotics? onset?

A

onset 6 wk

  • decrease aggression, restlessness, anxiety
  • slowed psychomotor function, decreased initiation/motivation
  • Reduced spontaneous mvmt
  • Sedation
  • most also block M, alpha adrenergic and Histamine R in brain and periphery
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13
Q

In addition to DA D2 and 5-HT receptors, most (classical and atypical) antipsychotics also block…

A

M, alpha adrenergic and histamine receptors

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14
Q

Do antipsychotics have many SE

A

yes, SE are very common, generally not pleasant thus compliance is poor

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15
Q

SE of antipsychotics include

A
  • decreased seizures threshold (dangerous bc seizures can trigger relapse)
  • endocrine: wt gain, ^PRL
  • Autonomic (antichol (dry mouth, blurred vision, tachy, constipation), alpha adrenergic (hypoTN), Histamine (sedation)
  • dental (xerostomia, bruxism)
  • EPS: PD sx
  • Tardive dyskinesia
  • neuroleptic malignant syndrome
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16
Q

Describe the EPS that are common with antipsychotics

A

Parkinsons like sx - tremor, akathisia (rocking), cogwheel rigiditiy, pacing, dyskinesias

  • antipsychotics (DA receptor antag) also block DA receptors in nigrostriatal pathway –> imbalance of striatal DA & ACh
  • *imbalance of striatal DA and ACh
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17
Q

EPS due to? degree based on? treat with?

A

imbalance of striatal DA & ACh

  • degree of EPS based on anticholinergic activity of drug
  • high antichol activity ie chlorpromazine = lower EPS
  • low antichol activity ie haloperidol = higher deg EPS

*treat with anticholinergics = Benztropine (Congentin)

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18
Q

How do you treat EPS?

A

with anticholinergics such as Benztropine (Congentin)

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19
Q

Which have more EPS, classical or atypical antipsychotics

A

classical antipsychotics

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20
Q

Tardive dyskinesia is present in what percent of pt treated with antipsychotics and what sx does it entail

A

15-25%

  • uncontrollable mouth and facial mvmts, occurs late in dz after LONG term TX
  • difficult to treat, often irreversible; dc antipsychotic
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21
Q

what antipsychotics are least likely to cause TD

A

the atypicals CLOZAPINE and OLANZAPINE

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22
Q

What is neuroleptic malignant syndrome and what is it caused by?

A

life threatening condition char by muscle rigidity, hyperpyrexia, changes in BP and HR
- due to blockage of DA D2 R in striatum and hypothalamus by antipsychotic med

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23
Q

How do you treat neuroleptic malignant syndrome?

A

Dantrolene (dantrium)

  • can also used DA agonists (bromocriptine) to stimulate DA receptors
  • bromocriptine used to treat Parkinsons
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24
Q

What medications do Antipsychotics interact with?

A

Antichol: ^SE (dry mouth, urinary retention, constipation)

Sedative-hyp: ^sedation

TCA: ^seizures, cardiac effect

Drugs that induce CYP450s (carbamazepine, cimetidine)

Smoking (bc induces CYP450)

Unpredictable with antihypertensives due to alpha blockade (^hypoTN)

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25
Q

How do classical antipsychotics work and what receptor occupancy is required

A

block DA D2 receptors, require 60% R occupancy

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26
Q

PK of Classicals?

A

Oral admin, gut absorption

  • high first pass, CYP 450 (2D6 and 3A4) metab
  • 20-35 hr half life
  • effects persists wks after last administration
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27
Q

Chlorpromazine (Thorazine).. class and use

A

Classical antipsychotic: block DA D2 Receptors

*psychosis associated w/ mania & drugs of abuse, pre-anesthetic

prochlorperazine = antiemetic

28
Q

Risks of Chlorpromazine (classical Antipsych)

A

EPS, TD, Neuroleptic malignant syndrome may occur

*but high antichol effects thus lower incidence of EPS

29
Q

SE of chlorpromazine include

A

sedation, postural hypoTN, blurred vision, constipation, decreased GI motility, inhibition of ejaculation, jaundice
DECREASED SEIZURE THRESHOLD
*may cause RETINAL DEPOSITS “browning of vision”

30
Q

Fluphenazine (Prolixin).. what type of drug? is similar to? action?

A

classical antipsychotic
similar to Chlorpromazine
selective for DA DR R
less antichol thus more EPS

31
Q

Haloperidol (Haldol) aka? MOA? use?

A

Vit H, potent DA DR r blocker
*also DA D1, 5HT2, a1 receptors

  • used in acute situations, injected
32
Q

half life and SE of Haldol

A

long half life

no anticholinergic activity thus increased EPS

33
Q

Atypical antipsych include

A 
Clozapine (Clozaril)
Risperidone
Olanzapine (Zyprexa)
Quetiapine
Ziprasidone
Aripiprazole (Ability)
34
Q

Clozapine (Clozaril) MOA, SE

A

blocks 5-HT2a and DA D4 receptors, some affinity DA D2

SE: hypersalivation, sedation, postural hypoTN, tachy, wt gain
*EPS and tardive dyskinesia rare
*rapid relapse if dc abruptly
Drug of LAST CHOICE due to AGRANULOCYTOSIS (monitor WBC)

35
Q

Olanzapine (Zyprexa): class? is similar to? MOA, use?

A

Atypcial antipsychotic –>
Similar to clozapine, but NO agranulocytosis
Blocks 5-HT2a R and DA D4, D2
*improves +/- sx schizophrenia, also used for bipolar disorder
*some antichol activity, EPS rare

36
Q

SE of Olanzapine (Zyprexa)

A

sedation, ortho hypoTN, wt gain, HYPERGLYCEMIA WITH T2DM

37
Q

Olanzapine (zyprexa) use

A

improve +/- sx schizo w/o agranulocytosis SE

*also used for bipolar when comb with lithium

38
Q

Risperidone (Risperdal) use, MOA

A

FIRST LINE drug for psychosis

  • improves +/- sx
  • blocks 5-HT2a and DA D2 rec
  • no sig effect on DA neurotransmission in Nigrostriatal pathway (thus TD or EPS rare)
39
Q

SE of Risperidone (Risperdal)

A

hypoTN, wt gain, insomnia, anxiety, some cardiac (lengthens QTI)

*EPS and TD rare bc little effect on DA neurotransmission in nigrostriatal pathway

40
Q

Ziprasidone (Geodon) class? MOA?

A

atypical antipsychotic

*blocks DA D2 and 5HT2a r

41
Q

activity and use of Ziprasidone (Geodon)

A

some antidepressant activity (5-HT1a R agonist, inhibition of 5-HT reuptake)

Use: TOURETTES, acute mania

42
Q

PK of Ziprasidone (Geodon)

*atypical antipsych used for tourettes and acute mania

A

oral or IM

CYP3A4 metab

43
Q

SE of Ziprasidone (Geodon)

A

PROLONGS QTI
SEDATION, impairs cog and motor skills
may cause hyperPRL (tubuloinfundibular pathway)
*decrease seizure threshold

44
Q

Quetiapine (Seroquel) class? similar to? MOA?

A

atypical antipsychotic
similar to clozapine but no agranulocytosis (Olanzapine also no agranulocytosis)

MOA: blocks 5HT-2a and D2 rec

45
Q

Use of Quetiapine (Seroquel)? SE?

A

promote sleep onset and maintenance

*SE: very sedating, dizzy, constipation, xerostomia, ortho hypoTN, wt gain, few EPS, does not elevate PRL (Ziprasidone elevates PRL)

46
Q

Use of Aripiprazole (Abilify)?

A

Dopamine system stabilizer

  • dopaminergic tone low, DA receptors activated
  • dopaminergic tone high, DA receptors blocked
47
Q

MOA of Aripiprazole (abilify)

A

Partial agonist for DA D2 and 5-HT1a; antagonist for 5-HT2a

*also blocks a1 and histamine r

48
Q

SE, of Aripiprazole (ability)

A

SE: hypergly, seizures, sedation, orthostatic hypoTN, DECREASES ESOPHAGEAL MOTILITY

*no ^PRL, no ^QTI, low EPS :)

49
Q

What is bipolar affective disorder

A

affects about 2% of the population, genetic component

  • pt alternate bw manic and deep depression
  • may be due to lack of GABAergic activity
50
Q

How are bipolar pt normally treated

A

Lithium &anticonvulsants

*often treated with combinations of these drugs and antipsychotics such as OLANZAPINE (ZYPREXA)

51
Q

How does lithium (Li) work

A

mood stabilizer works by suppression of 2nd messengers (IP3) - may increase ACh, NE, DA

52
Q

PK of Lithium

A

gut absorption
body wide distribution
half life 24 hr
no metab, kidney excretion

53
Q

effectiveness of Lithium (Li), compliance

A

calming effect in 60% of pt

  • poor compliance bc feel sick
  • extremely toxic in OD
54
Q

How is Lithium reabsorbed and what influence does this have on Na?

A

Reabsorbed in PT of kidney

Competes w Na for reabs:

  • high Na = increased Li abs = toxicity
  • high Na = decreased Li abs = increased Li excretions
  • increased Li = decreased Na absorption = hypoNa
55
Q

Is lithium safe? Therapeutic window?

A

Small therapeutic window (optimal plasma concentrations 0.6-1.2 mEq/L)

  • Plasma > 2mEq/L: N, diarrhea, anorexia, muscle weakness, HA, tremor, confusion, memory impairment
  • Plasma > 2.5 mEq/L: confusion, seizures, renal failure, cardiac arrhythmia, coma, death
56
Q

SE of Lithium

A

Hypothyroidism
Diabetes Insipidus (Li inhibits ADH, treat with amiloride)
*not recommended in pregnancy

57
Q

how do you treat Diabetes insipidus due to Lithium

A

Amiloride

58
Q

Drug interactions with Lithium include

A
  • Antidep: mania may increase
  • Diuretics (alter Na excretion), can alter Li clearance
  • NSAIDs increase Li toxicity, decrease clearnace, increase Li uptake
  • Na: high Na reduces Li concentration; high Li may lead to decreased Na reabsorption and hypoNa

BZ and antipsychotics are safe

59
Q

Anticonvulsants that are alternatives to Lithium for tx of bipolar include

A

Valproic Acid (Depakene)
Gabapentin (Neurontin)
Carbamazepine (Tegretol)
Lamotrigine (Lamictal)

60
Q

Valproic Acid (Depakene) MOA and use/efficacy

A

Unknown MOA
*used for Rapid cycling manic/depressive phases, efficacy in some pt who do not respond to lithium (just as or more effective than lithium), rapid onset

61
Q

SE of Valproic Acid (Depakene)

A

*remember, used for rapid cycling in bipolar and is also an anticonvulsant

  • GI, sedation, liver enzyme induction, wt gain, surgical bleeeding (dental)
  • Teratogenic (anticonvulsants are generally not safe in pregnancy
62
Q

Gabapentin (Neurontin) use specifically regarding mood disorders

A

anticonvulsant GABA analogue used for rapid cycling in bipolar disorder

*also neuropathic pain, partial seizures, generalized tonic clonic seizures

Preg Cat C

63
Q

Carbamazepine (Tegretol) drug class and mood disorder use?

A

*used for REFRACTORY bipolar disorder when combined with Li

Anticonvulsant DOC for partial seizures, wide used for generalized seizures, trigeminal neuralgia inhibits Na channels thus inhibits Glutamate neurotransmission

64
Q

Carbamazepine (Tegretol) SE?

A

GI, sedation, CNS toxicity, hematologic rxn, hypersensitivity rahss (risk SJS - toxic epidermal necrolysis, must test human antigen)

65
Q

Lamotrigine (Lamictal) drug class and use?

A

Anticonvulsant that inhibits Na channels and thus Glutamate neurotransmission
*use: prevention of relapse, depressive state following mania and acute mania

66
Q

just as a review, seizures are due to

A

underactive GABA neurotransmission, and/or over active glutamate

*thus anticonvulsants target increasing GABA Neurotransmission and inhibition Glutamate neurotransmission

Pharm III (9 decks)

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