Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharm III > Exam 1 Antipsychotics > Flashcards

Exam 1 Antipsychotics Flashcards

(66 cards)

Start Studying
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

First antipsychotic tx

A

chlorpromazine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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

A

increased in Limbic, decreased in frontal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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apathetic, withdrawn, anti-social, lack of motivation, depressed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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What cognitive impairment do Schizophrenics have

A

distracted, disorganized thought, memory loss

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

D2 distributed where? D4?

A

D2 = limbic region

D4 = cortical

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Prochlorperazine is

A

antipsychotic that is an antiemetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Do antipsychotics have many SE

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

How do you treat EPS?

A

with anticholinergics such as Benztropine (Congentin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Which have more EPS, classical or atypical antipsychotics

A

classical antipsychotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what antipsychotics are least likely to cause TD

A

the atypicals CLOZAPINE and OLANZAPINE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
How do classical antipsychotics work and what receptor occupancy is required
block DA D2 receptors, require 60% R occupancy
26
PK of Classicals?
Oral admin, gut absorption * high first pass, CYP 450 (2D6 and 3A4) metab * 20-35 hr half life * effects persists wks after last administration
27
Chlorpromazine (Thorazine).. class and use
Classical antipsychotic: block DA D2 Receptors *psychosis associated w/ mania & drugs of abuse, pre-anesthetic prochlorperazine = antiemetic
28
Risks of Chlorpromazine (classical Antipsych)
EPS, TD, Neuroleptic malignant syndrome may occur | *but high antichol effects thus lower incidence of EPS
29
SE of chlorpromazine include
sedation, postural hypoTN, blurred vision, constipation, decreased GI motility, inhibition of ejaculation, jaundice DECREASED SEIZURE THRESHOLD *may cause RETINAL DEPOSITS "browning of vision"
30
Fluphenazine (Prolixin).. what type of drug? is similar to? action?
classical antipsychotic similar to Chlorpromazine selective for DA DR R less antichol thus more EPS
31
Haloperidol (Haldol) aka? MOA? use?
Vit H, potent DA DR r blocker *also DA D1, 5HT2, a1 receptors - used in acute situations, injected
32
half life and SE of Haldol
long half life | no anticholinergic activity thus increased EPS
33
Atypical antipsych include
``` Clozapine (Clozaril) Risperidone Olanzapine (Zyprexa) Quetiapine Ziprasidone Aripiprazole (Ability) ```
34
Clozapine (Clozaril) MOA, SE
*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
Olanzapine (Zyprexa): class? is similar to? MOA, use?
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
SE of Olanzapine (Zyprexa)
sedation, ortho hypoTN, wt gain, HYPERGLYCEMIA WITH T2DM
37
Olanzapine (zyprexa) use
improve +/- sx schizo w/o agranulocytosis SE *also used for bipolar when comb with lithium
38
Risperidone (Risperdal) use, MOA
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
SE of Risperidone (Risperdal)
hypoTN, wt gain, insomnia, anxiety, some cardiac (lengthens QTI) *EPS and TD rare bc little effect on DA neurotransmission in nigrostriatal pathway
40
Ziprasidone (Geodon) class? MOA?
atypical antipsychotic | *blocks DA D2 and 5HT2a r
41
activity and use of Ziprasidone (Geodon)
some antidepressant activity (5-HT1a R agonist, inhibition of 5-HT reuptake) Use: TOURETTES, acute mania
42
PK of Ziprasidone (Geodon) | *atypical antipsych used for tourettes and acute mania
oral or IM | CYP3A4 metab
43
SE of Ziprasidone (Geodon)
PROLONGS QTI SEDATION, impairs cog and motor skills may cause hyperPRL (tubuloinfundibular pathway) *decrease seizure threshold
44
Quetiapine (Seroquel) class? similar to? MOA?
atypical antipsychotic similar to clozapine but no agranulocytosis (Olanzapine also no agranulocytosis) MOA: blocks 5HT-2a and D2 rec
45
Use of Quetiapine (Seroquel)? SE?
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
Use of Aripiprazole (Abilify)?
Dopamine system stabilizer - dopaminergic tone low, DA receptors activated - dopaminergic tone high, DA receptors blocked
47
MOA of Aripiprazole (abilify)
Partial agonist for DA D2 and 5-HT1a; antagonist for 5-HT2a *also blocks a1 and histamine r
48
SE, of Aripiprazole (ability)
SE: hypergly, seizures, sedation, orthostatic hypoTN, DECREASES ESOPHAGEAL MOTILITY *no ^PRL, no ^QTI, low EPS :)
49
What is bipolar affective disorder
affects about 2% of the population, genetic component * pt alternate bw manic and deep depression * may be due to lack of GABAergic activity
50
How are bipolar pt normally treated
Lithium &anticonvulsants *often treated with combinations of these drugs and antipsychotics such as OLANZAPINE (ZYPREXA)
51
How does lithium (Li) work
mood stabilizer works by suppression of 2nd messengers (IP3) - may increase ACh, NE, DA
52
PK of Lithium
gut absorption body wide distribution half life 24 hr no metab, kidney excretion
53
effectiveness of Lithium (Li), compliance
calming effect in 60% of pt * poor compliance bc feel sick * extremely toxic in OD
54
How is Lithium reabsorbed and what influence does this have on Na?
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
Is lithium safe? Therapeutic window?
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
SE of Lithium
Hypothyroidism Diabetes Insipidus (Li inhibits ADH, treat with amiloride) *not recommended in pregnancy
57
how do you treat Diabetes insipidus due to Lithium
Amiloride
58
Drug interactions with Lithium include
* 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
Anticonvulsants that are alternatives to Lithium for tx of bipolar include
Valproic Acid (Depakene) Gabapentin (Neurontin) Carbamazepine (Tegretol) Lamotrigine (Lamictal)
60
Valproic Acid (Depakene) MOA and use/efficacy
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
SE of Valproic Acid (Depakene)
*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
Gabapentin (Neurontin) use specifically regarding mood disorders
anticonvulsant GABA analogue used for rapid cycling in bipolar disorder *also neuropathic pain, partial seizures, generalized tonic clonic seizures Preg Cat C
63
Carbamazepine (Tegretol) drug class and mood disorder use?
*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
Carbamazepine (Tegretol) SE?
GI, sedation, CNS toxicity, hematologic rxn, hypersensitivity rahss (risk SJS - toxic epidermal necrolysis, must test human antigen)
65
Lamotrigine (Lamictal) drug class and use?
Anticonvulsant that inhibits Na channels and thus Glutamate neurotransmission *use: prevention of relapse, depressive state following mania and acute mania
66
just as a review, seizures are due to
underactive GABA neurotransmission, and/or over active glutamate *thus anticonvulsants target increasing GABA Neurotransmission and inhibition Glutamate neurotransmission

Pharm III (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions