Antipsychotics

Question 1

What is the dopamine hypothesis?

Answer 1

-blocking of dopamine activity in the CNS can improve psychosis

Question 2

Name 3 Typical Anti-psychotics.

Answer 2

(1st Generation)

1. Haloperidol
2. Chlorpromazine
3. Trifluoperazine

Question 3

What does activation of D2 receptors result in?

Answer 3

• inhibition of adenylyl cyclase

>reduce cAMP

Question 4

Where are the D2 receptors found ?

Answer 4

• Limbic system
• Prefrontal cortex
• Basal ganglia

Question 5

What is the MAIN MOA of Typical Anti-psychotics?

Answer 5

• blockade of D2 receptors

Question 6

What conditions can be treated with Typical Anti-psychotics? (7)

Answer 6

1. Schizophrenia (+)ve symptoms
2. Psychosis
3. Mania
4. OCD
5. Delirium (Haloperidol)
6. Tourette’s Syndrome
7. Huntington’s disease

Question 7

Which pathway do the typical anti-psychotics act on for it to cause motor dysfxn?

Answer 7

• Nigrostriatal Pathway

Question 8

What other NTs are affected by the intake of Typical Anti-psychotics?

Answer 8

1. Serotonin
2. Histamine
3. Epinephrine
4. Ach

Question 9

Which typical anti-psychotic is known to block histamine and alpha-1 receptors MORE than D2 r.?

Answer 9

Chlorpromazine

Question 10

Which typical anti-psychotic blocks the D2 receptors the most?

Answer 10

Haloperidol

Question 11

What are S.Es Typical Antipsychotics when blocking dopamine?

Answer 11

Parkinsonism (rigidity/bradykinesia/resting tremor) 
Hyperprolactinemia
>Amenorrhea 
>Galactorea
>Gynecomastia

Anti-Emetic (esp. Chlorpromezine)

Question 12

What occurs as a result of other receptors being blocked?

Answer 12

1. Ach Blockade> DRY MOUTH and CONSTIPATION
2. A-1 receptors> Hypotension
3. Histamine receptor > sedation and CONSTIPATION

Question 13

What is the pyramidal system?

What occurs if this system is damaged?

Answer 13

• corticospinal system —because it runs through the PYRAMIDS of the medulla
• WEAKNESS when damaged

Question 14

What is the extrapyramidal system responsible for?

Answer 14

-modulation of the movements
- and it involves the Basal Ganglia Nuclei and the associated tracts
> MOVEMENT DISORDERS occur with damage to the extrapyramidal system

Question 15

What are EPS?

Answer 15

-Movement S.Es: Akathisia, Bradykinesia, Tardive dyskinesia, dystonia

Question 16

What is dystonia?

Answer 16

• spasms or stiffness
• occurs within HOURS/days of administering the drug
• jaw is locked/ can’t move arm

Question 17

How to treat dystonia?

Answer 17

Benztropine

-anticholinergic drug; blocks M1 receptors

Question 18

What is the most COMMON EPS with Anti-psychotic drugs?

Answer 18

Akathisia- restlessness, URGE to move

- mistaken for worsening of psychotic condition

Question 19

When does Akathisia usually set in?

Answer 19

• within DAYS

Question 20

How to treat Akathisia?

Answer 20

• lower the dose
• benzodiazepines
• propanolol

Question 21

Which EPS kicks in within WEEKS of drug administration?

Answer 21

• Bradykinesia

drug-induced Parkinsonism

Question 22

How to treat Bradykinesia?

Answer 22

Benztropine

like dystonia- frozen muscles; slow movement

Question 23

What occurs with Tardive Dyskinesia?

Answer 23

Choreoathetosis

• twisting and writhing, irregular MOTIONs
• mouth, tongue, face limbs
• —sets in months/ years after use of drugs
• permanent!

Question 24

Name 3 High potent Typical Antipsychotics.

And why are they of high potency?

Answer 24

• haloperidol
• fluphenazine
• trifluoperazine
• the main s.e: EPS with just 1mg dosage

Question 25

List 2 low potency Typ.Antipsychotics.

Answer 25

1. Chlorpromazine 2. Thioridazine ----need 50-100mg for therapeutic effect

Question 26

What form of S.Es are seen with the low potency drugs?

Answer 26

More NEUROLOGICAL s.es - sedation - dry mouth

Question 27

What is a RARE, dangerous S.E to Typical Antipsychotics?

Answer 27

NMS---Neuroleptic Malignant Syndrome (onset= 7-10 days after administr.) ----watch out for RIGID MUSCLES (EPS) & FEVER

Question 28

What 3 other conditions are seen with NMS?

Answer 28

1. Mental Status Changes (encephalopathy) 2. elevated Creatine Kinase (Muscle Damage) 3. Myoglobinuria> acute renal failure (rhabdomyolysis)

Question 29

How to treat NMS?

Answer 29

- Dantrolene (muscle relaxant) | - bromocriptine (Dopamine Agonist)

Question 30

Which Anti-psychotic is known to PROLONG the QT interval on the ECG? Dangers of prolonged QT?

Answer 30

- IV Haloperidol | - ---Torsades de pointes may turn up

Question 31

Which Typical antipsychotic results in corneal deposits?

Answer 31

- Chlorpromazine | > will ACCELERATE the ageing of the lens

Question 32

Which typical anti-psychotic results in RETINAL deposits? How does it present as?

Answer 32

- Thioridazine | - browning of their vision

Question 33

Main diff. between TYPICAL and ATYPICAL anti-psychotics?

Answer 33

- atypical: LESS EPS s.es

Question 34

Why are second gen. antipsychotics known to reduce psychotic symptoms more efficiently than typical antispsychotics?

Answer 34

- ---d/t its greater Serotonin blocking receptor effect | - increased 5-HT2A receptors activity is said to cause hallucinations

Question 35

WHat are the 2 main s.e of CLOZAPINE?

Answer 35

-bone marrow toxicity >AGRANULOCYTOSIS ....therefore should monitor weekly (then monthly later) -SEIZURES (2-5%)

Question 36

What to do if pt presents with: Amenorrhea, Galactorhea and Gynaecomastia in men?

Answer 36

1. measure prolactin level 2. scan head 3. check med list

Question 37

High rates of Hyperprolactinemia is seen in what drugs?

Answer 37

- Haloperidol - Fluphenazine - RISPERIDONE - PALIPERIDONE

Question 38

What is ARIPIPRAZOLE?

Answer 38

- its a D2 partial AGONIST | - ---less dopamine blockade s.e

Question 39

What is the S.E of ARIPIPRAZOLE?

Answer 39

-akathisia

Question 40

Risks of use of anti-psychotics on elderly?

Answer 40

- STROKE | - THROMBOEMBOLISM