Antipsychotic Agents

Question 1

• used to treat psychoses like schizophrenia, mania, senile dementia and behaviour disorders in children
• act by depressing the central nervous system (by decreasing dopamine levels) and by producing sedation without producing sleep

Answer 1

antipsychotic drugs

Question 2

• Antipsychotics are employed to reduce excitation, agitation, agressiveness and
  impulsiveness
• they are also known as antischizophrenic
  drugs or neuroleptic drugs or_________

Answer 2

major tranquilizers

Question 3

1st Generation or Typical Antipsychotics

Answer 3

• phenothiazine derivatives
• butyrophenones
  -thioxanthenes
• miscellaneous

Question 5

Chlorpromazine

Answer 5

Phenothiazine: aliphatic

Question 6

Fluphenazine

Answer 6

Phenothiazine: piperazine

Question 7

Thioridazine

Answer 7

Phenothiazine: piperadines

Question 8

Haloperidol, Droperidol

Answer 8

Butyrophenones

Question 9

Thiothixene

Answer 9

Thioxanthenes

Question 10

Pimozide, Molindone

Answer 10

Miscellaneous

Question 11

Clozapine, Olanzapine, Loxapine, Resperidone, Paliperidone, Quetiapine, Ziprasidone, Amisulpride, Aripiprazole, Molindone

Answer 11

2nd Generation or Atypical Antipsychotics

Question 12

• act exclusively on specific postsynaptic receptors
  and block the postsynaptic dopamine receptors
• positive symptoms of psychosis such as hallucinations,
  delusions, disorganized speech, looseness of association, and bizarre behavior
• chemically constituted by a lipophilic, linearly
  fused tricyclic system having a hydrophilic basic amino alkyl chain

Answer 12

Phenothiazine

Question 13

T or F

Substitution at the second
position of phenothiazine nucleus by electron
withdrawing substituent increases antipsychotic activity

Answer 13

T

Question 14

T or F

Substitution at the 3-position of
phenothiazine nucleus increases
antipsychotic activity than unsubstituted
derivatives but not by substitution at 2-
position.

Answer 14

T

Question 15

T or F

Substitution at 1 and 4 positions of phenothiazine nucleus reduces the antipsychotic activity

Answer 15

T

Question 16

T or F

The phenothiazines produce a lesser degree of central depression than the barbiturates or benzodiazepines.

Answer 16

T

Question 17

is a phenothiazine
derivative and has a chemical formula of 2-chloro-10-[3-(-dimethylamino) propyl] phenothiazine monohydrochloride

Answer 17

Chlorpromazine Hydrochloride

Question 18

synthesized by cyclization of 3- chlorodiphenylamine with sulphur in presence of small amount of iodine as catalyst

Answer 18

Chlorpromazine

Question 19

MOA: block dopamine at D2 receptor
sites in the mesolimbic medullary chemoreceptor trigger zone,areas of the brain
- causes inhibitory post-synaptic effects by
reducing the flow of dopamine as the dopaminergic ion
channels are closed

Answer 19

Chlorpromazine

Question 20

• used in the management of psychotic
  conditions. It also controls excitement, aggression and agitation
• has antiemetic, antipruritic, anti-histaminic and sedative properties

Answer 20

Chlorpromazine

Question 21

T or F

Common side effects of Chlorpromazine:

Extra pyramidal symptoms, hypertension, orthostatic
hypotension, blurred vision, dry mouth, anorexia, nausea,
vomiting, constipation, diarrrhea, weight gain, impotence,
amenorrhea, photosensitivity

Answer 21

T

Question 22

• phenothiazine derivative associated with piperazine
• 3-chloro-10-[3-(4-methyl-1-piperazinyl) phenothiazine
• occurs as maleate and mesylate salts

Answer 22

Prochlorperazine

Question 23

prepared by refluxing 1-(3-chloro propyl)-
4-methylpiperazine with 2-chlorophenothiazine in presence of
sodamide in toluene.

Answer 23

Prochlorperazine

Question 24

• pale yellow colored, viscous liquid
• very slightly soluble in water
• freely soluble in alcohol

Answer 24

Prochlorperazine

Question 26

- an antipsychotic and tranquilizing agent. It is used to treat various psychiatric disorders such as schizophrenia, mania, involution psychoses, senile and tonic psychoses - has antiemetic properties

Answer 26

Prochlorperazine

Question 27

- a fluorinated phenothiazine derivative - possesses a piperazine nucleus -10-[3-(4-methylpiperazin-1-yl)propyl]- 2- trifluoromethyl methylphenothiazine - It is prepared by refluxing 2-trifluoromethyl phenothiazine and 3-(4-methylpiperazinyl) propyl chloride in presence of sodamide as a base

Answer 27

Trifluoperazine

Question 28

- occurs as hydrochloride salt - white to pale yellow, crystalline powder - freely soluble in water - should be protected from light and moisture

Answer 28

Trifluoperazine

Question 29

- used to control psychotic disorders. It is effective to control excessive anxiety, tension, aggressiveness and agitation

Answer 29

Trifluoperazine

Question 30

- fluorinated phenothiazine derivative - 10-[3-(dimethylamino)propyl]-2-(trifluoromethyl) phenothiazine - synthesized by condensing 2-(trifluoromethyl) phenothiazine with (3-chloropropyl) dimethylamine in dry benzene in presence of sodamide

Answer 30

Triflupromazine

Question 31

- occurs hydrochloride salt - white, crystalline powder - freely soluble in water, alcohol - insoluble in ether - used to treat psychotic disorders - has antiemetic properties

Answer 31

Triflupromazine

Question 32

- phenothiazine derivative - 10-[3-(dimethyl amino)-propyl] phenothiazine - prepared by condensing 3-chloro-N, N- dimethylpropylamine with phenothiazine in presence of sodium hydride

Answer 32

Promazine

Question 33

- available as hydrochloride salt - white or slightly yellow crystalline powder - freely soluble in water and chloroform - should be protected from air - has antipsychotic properties - used to control nausea and vomiting

Answer 33

Promazine

Question 34

T or F Intact carbonyl group of butyrophenones is necessary for antipsychotic activity. Replacement of carbonyl group by functional groups such as CH(OH), — CH (X), —O— , —S, —SO2— etc., decreases activity.

Answer 34

T

Question 35

T or F Incorporation of basic nitrogen into 6- membered rings is important for CNS depressant activity.

Answer 35

T

Question 36

- butyrophenone derivative with antipsychotic properties that has also been found as effective in lowering levels of hyperactivity, agitation, and mania - 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4′-fluorobutyrophenone

Answer 36

Haloperidol

Question 37

synthesized by condensing 4-(4-chlorophenyl-4-piperidinol with 4-chloro-4′- fluorobutyrophenone.

Answer 37

Haloperidol

Question 38

MOA: inhibition of the transport mechanism of cerebral monoamines, particularly by blocking the impulse transmission in dopaminergic neurons

Answer 38

Haloperidol

Question 39

- effective in the management of hyperactivity, agitation, and mania - an effective neuroleptic and also possesses antiemetic properties ; it has a marked tendency to provoke extrapyramidal effects and has relatively weak alpha-adrenolytic properties - exhibit hypothermic and anorexiant effects and potentiates the action of barbiturates, general anesthetics, and other CNS depressant drugs

Answer 39

Haloperidol