Antipsychotics

Question 1

2 classes of antipsychotics

Answer 1

Typical or first generation agents
Atypical or second generation agents

Based on their mechanism of action

Question 2

Do need to know clinical uses for

Answer 2

antipsychotics

Site of actions of antipsychotic agents.

Question 3

Typical antipsychotics (6) 
only study blue

Answer 3

Phenothiazines
Butyrophenones
Thioxanthene

Question 4

What are the phenothiazines?

Answer 4

Chlorpromazine
Prochlorperaine
Thioridazine

Question 5

What are the Butyrophenones?

Answer 5

Droperinol

Haloperinol

Question 6

Typical antipsychotics agents are:

Answer 6

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

Question 7

Typical Antipsychotics MOA

CLINICAL USE MOST IMPORTANT TO THE ANESTHESIA PROVIDERS?

Answer 7

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!

Question 8

Not protected by the BBB

Answer 8

Drug does not have to cross the BBB.

Work in CHEMORECEPTOR TRIGGER ZONE

Question 9

Problems with antipsychotics

Answer 9

They attach and agonize multiple other receptors

Question 10

Atypical

Answer 10

NOT USE for anesthesia purpose

Question 11

Atypical created

Answer 11

To decrease incidence of EPS and tardive dyskinesia

Question 12

Atypical share the following characteristics:

Answer 12

Clozapine and Quetiapine, no EPS or Dyskinesia.

Question 13

What is the first atypical agent

Answer 13

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

Question 14

Why called atypical

Answer 14

potent 5-HT 2 antagonists and

WEAK dopamine 2 receptor antagonist

Question 15

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

Answer 15

CLOZAPINE

Question 16

Clozapine is the atypical agent with the most

Answer 16

anticholinergic
sedative
orthostatic hypotensive properties

Question 17

Most antipsychotic drugs are
Pharmacokinetics
Metabolism
Clearance where

Answer 17

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

Question 18

Neurological side effects

Answer 18

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

Question 19

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

Answer 19

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

Question 20

Neurological symptoms 3 types

Answer 20

EPS
TD
Neuroleptic malignant Syndrome (NMS)

Question 21

EPS include:

Symptoms

Answer 21

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

Question 22

Major acute effect that Can cause from one dose of

Answer 22

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

Question 23

***Acute dystonia reaction other

Answer 23

Laryngospasms,
Torticollis
Oculogyric crisis

Question 24

DO not give IV ever

Answer 24

benztropine 1-2mg IM

Question 25

Akathisia

Answer 25

desire to be in constant motion

Question 26

The more dopamine 2 antagonists

Answer 26

greater risk of adverse effects

Question 27

Tardive dyskinesia is

Answer 27

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

Question 28

Does not occur in one dose

Answer 28

TD, does not go Away | No treatments

Question 29

Bucco lingual masticatory

Answer 29

a type of TD

Question 30

NMS

Answer 30

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

Question 31

Malignant hyperthermia associated with anesthesia as well as

Answer 31

Central anticholinergic syndrome may mimic the neuroleptic malignant syndrome,

Question 32

Distinguishing feature is the ability of pa

Answer 32

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

Question 33

Clinical manifestions of NMS (FALTERM)

Answer 33

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

Question 34

Mortality of NMS due to (not important)

Answer 34

``` Ventilatory failure, Cardiac failure Dysrhythmias Renal failure Thromboembolism ```

Question 35

Treatment

Answer 35

``` Lots of volume Coloing Dandrolene Dopamine agonists : Bromicriptine Benzo ```

Question 36

Adverse cardiac effects

Answer 36

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

Question 37

Torsades de pointes most promisent with

Answer 37

Haloperidol IV

Question 38

Agranulocytosis is

Answer 38

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

Question 39

Prolactin levels are ______and why?

Answer 39

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

Question 40

Other side effects of antipsychotics

Answer 40

Gynecomastia Galatorrhea Amenorrhea Sexual dysfunction.

Question 41

As a result of the potential agranulocytosis :

Answer 41

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

Question 42

Classic example for side effects requiring monitoring

Answer 42

CLOZAPINE

Question 43

Droperidol and haldol

Answer 43

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

Question 44

Haloperidol

Answer 44

Laryngospasms, Bronchospams increased depth of respiration

Question 45

Droperinol

Answer 45

Pt most be on EKG because it May prolonged QT

Question 46

Effects of QT are Droperinol

Answer 46

dose dependent

Question 47

Droperinol

Answer 47

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

Question 48

Acceptable in COPD: Droperinol

Answer 48

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

Question 49

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

Answer 49

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

Question 50

• Droperidol prolongs

Answer 50

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

Question 51

• Should not be administered to patients with parkinson’s | disease

Answer 51

Droperinol

Question 52

Can cause QT prolongation

Answer 52

Droperinol | Prolonged QTc in 440msec men and 450msec in women

Question 53

Anesthesia implications | 2 medications to avoid?

Answer 53

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