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SRNAPharmacology I > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

2 classes of antipsychotics

A

Typical or first generation agents
Atypical or second generation agents

Based on their mechanism of action

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2
Q

Do need to know clinical uses for

A

antipsychotics

Site of actions of antipsychotic agents.

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3
Q 
Typical antipsychotics (6) 
only study blue
A

Phenothiazines
Butyrophenones
Thioxanthene

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4
Q

What are the phenothiazines?

A

Chlorpromazine
Prochlorperaine
Thioridazine

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5
Q

What are the Butyrophenones?

A

Droperinol

Haloperinol

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6
Q

Typical antipsychotics agents are:

A

dopamine receptor ANTAGONISTS<
primarily dopamine 2 receptor antagonist,
Inactive dopamine neurotransmitter

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7
Q

Typical Antipsychotics MOA

CLINICAL USE MOST IMPORTANT TO THE ANESTHESIA PROVIDERS?

A

Blockade of dopamine2 receptors located in the
chemoreceptor trigger zone (CTZ) of the medulla is responsible for the antiemetic effects of antipsychotics
• This is the clinical use that is most important to the anesthesia provider!

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8
Q

Not protected by the BBB

A

Drug does not have to cross the BBB.

Work in CHEMORECEPTOR TRIGGER ZONE

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9
Q

Problems with antipsychotics

A

They attach and agonize multiple other receptors

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10
Q

Atypical

A

NOT USE for anesthesia purpose

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11
Q

Atypical created

A

To decrease incidence of EPS and tardive dyskinesia

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12
Q

Atypical share the following characteristics:

A

Clozapine and Quetiapine, no EPS or Dyskinesia.

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13
Q

What is the first atypical agent

A 
Clozapine (Clozaril)
Risperidone (risperidal)
Olanzapine (ziprexa)
Quetiapine (seroquel)
Ziprasidone (Geodon)
Aripiprazole (ability)
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14
Q

Why called atypical

A

potent 5-HT 2 antagonists and

WEAK dopamine 2 receptor antagonist

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15
Q

Which is considered to be the atypical agent with the most anticholinergic , sedative and orthostatic hypotensive?

A

CLOZAPINE

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16
Q

Clozapine is the atypical agent with the most

A

anticholinergic
sedative
orthostatic hypotensive properties

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17
Q

Most antipsychotic drugs are
Pharmacokinetics
Metabolism
Clearance where

A 
Metabolized in Liver
Lipophillic (work in the CNS)
Highly protein bound
Cross fetal (do not give to woman pregnant)
Half life all over the place
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18
Q

Neurological side effects

A

EPS and tardive dyskinesia correlates with the dopamine 2 antagonism potency of the antipsychotics agent.

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19
Q

There is a LOWER risk of EPS and TD with _________compared to ______because they are more ________for ________are weaker ________

A

Atypical antipsychotics agents compared to typical antipsychotics agents, atypical are more SELECTIVE for 5-HT2 receptors and are weaker dopamine 2 antagonists

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20
Q

Neurological symptoms 3 types

A

EPS
TD
Neuroleptic malignant Syndrome (NMS)

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21
Q

EPS include:

Symptoms

A

Parkinsonism (parkinson-like state)
Bradykinesia, rigidity, tremor, postural instability and gait shuffling
Take 1 week on long
Responds to Diphenydramin (benadryl) and Benztropine

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22
Q

Major acute effect that Can cause from one dose of

A

Acute dystonia
Cause MUSCLE CONTRACTION UNCONTROLLABLE REPETITIVE and often twisting movements
most likely 1-5 days.

23
Q

***Acute dystonia reaction other

A

Laryngospasms,
Torticollis
Oculogyric crisis

24
Q

DO not give IV ever

A

benztropine 1-2mg IM

25
Q

Akathisia

A

desire to be in constant motion

26
Q

The more dopamine 2 antagonists

A

greater risk of adverse effects

27
Q

Tardive dyskinesia is

A

involuntary movement disorder characterized by RHYTHMICAL, Stereotyped, repetitive, tick like movement of face eyelids, tongue, mouth

CAN affect respiratory muscles and pt may stop breathing

28
Q

Does not occur in one dose

A

TD, does not go Away

No treatments

29
Q

Bucco lingual masticatory

A

a type of TD

30
Q

NMS

A

SERIOUS and potentially fatal complication of antipsychotics
Occur with atypical or typical but typical more likely

31
Q

Malignant hyperthermia associated with anesthesia as well as

A

Central anticholinergic syndrome may mimic the neuroleptic malignant syndrome,

32
Q

Distinguishing feature is the ability of pa

A

nondepolarizing neuromuscular blockers to produce flaccid paralysis in patients experiencing NMS but not in those experiencing malignant HYPERTHERMIA

33
Q

Clinical manifestions of NMS (FALTERM)

A 
Fever
ANS - instability(unstable BP, HR)
Leukocytosis
Tremor
Elevated Enzymes
Hypertonicity
Mental Status changes
34
Q

Mortality of NMS due to (not important)

A 
Ventilatory failure, 
Cardiac failure
Dysrhythmias
Renal failure
Thromboembolism
35
Q

Treatment

A 
Lots of volume
Coloing
Dandrolene
Dopamine agonists : Bromicriptine
Benzo
36
Q

Adverse cardiac effects

A

hypotension
Prolonged QTc , increases risk of sudden cardiac death
Torsades de pointes

37
Q

Torsades de pointes most promisent with

A

Haloperidol IV

38
Q

Agranulocytosis is

A

associated with primarily clozapine only (incidence < 1.3%) and can be life threatening

39
Q

Prolactin levels are ______and why?

A

are increased due to blockade of dopamine receptors and the loss of normal inhibition of prolactin secretion.

40
Q

Other side effects of antipsychotics

A

Gynecomastia
Galatorrhea
Amenorrhea
Sexual dysfunction.

41
Q

As a result of the potential agranulocytosis :

A

Patient must be in a monitoring program (monitor WBC and ANC ,500 Cells) in order to take Clozapine

42
Q

Classic example for side effects requiring monitoring

A

CLOZAPINE

43
Q

Droperidol and haldol

A

Haloperinol longer duration of action and has less alpha adrenergic antagonistic activity.

44
Q

Haloperidol

A

Laryngospasms,
Bronchospams
increased depth of respiration

45
Q

Droperinol

A

Pt most be on EKG because it May prolonged QT

46
Q

Effects of QT are Droperinol

A

dose dependent

47
Q

Droperinol

A

powerful antiemetics agent
DOES NOT PRODUCE AMNESIA
can cause hypotension (alpha 1 antagonists) , decreased PVR

48
Q

Acceptable in COPD: Droperinol

A

Droperidol, when given IV, augments the ventilatory response evoked by arterial hypoxemia, presumably by blocking the action of the inhibitory neurotransmitter dopamine at the carotid body
• For this reason, droperidol may be an acceptable preoperative medication in patients with COPD who depend on carotid body drive to prevent hypoventilation

49
Q

Neuroleptanalgesia
• Fentanyl combined with droperidol is administered for the production of neuroleptanalgesia

• This fixed combination is not associated with enhanced ventilatory depression as compared with either drug alone

A

• Innovar® is a commercially available combination of droperidol and fentanyl in a ratio of 50:1

50
Q

• Droperidol prolongs

A

fentanyl’s duration of action but does not enhance analgesia produced by fentanyl

51
Q

• Should not be administered to patients with parkinson’s

disease

A

Droperinol

52
Q

Can cause QT prolongation

A

Droperinol

Prolonged QTc in 440msec men and 450msec in women

53
Q

Anesthesia implications

2 medications to avoid?

A
  • do not give to parkison patient
  • avoid use of ketamine and meperidine
  • Do not CO-ADMINISTER dopaminergic blockade
  • Use DIRECT acting for vasopressors.

SRNAPharmacology I (29 decks)

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