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Human Pharmacy > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

What pathway is responsible for the positive symptoms of schizophrenia?

A

mesolimbic pathway

agitation, delusions, disorganised speech, disorganised thinking, hallucinations, insomnia

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2
Q

What pathway is responsible for the negative symptoms of schizophrenia?

A

mesocortical pathway

apathy, affective flattening, lack of motivation/pleasure (anhedonia), poverty of speech), social isolation

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3
Q

Discuss typical antipsychotics

A

Antagonists of D2 dopamine (R)

They have an equal or greater affinity for D2 receptor over 5HT-2

Higher risk of EPS

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4
Q

Discuss atypical antipsychotics

A

Antagonists, preferred treatment

Greater affinity for 5HT2 > D2 receptor

Some have greater affinity for D3 or D4 receptor

Less risk of EPS

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5
Q

Discuss some time dependent changes seen in neurotransmission with antipsychotics (early, intermediate, late)

A

There will be inc DA synth, release, metabolism = compensatory response

Eventual depol blockage –> inactivation of DA neuron –> reduce release of DA from mesolimbic (dec positive symptoms) and nigrostriatal pathway

Eventual inc in DA receptor number/sensitivity > delayed EPS

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6
Q

What is a permanent adaption seen with antipsychotics?

A

DA receptor upregulation and supersensitivity

–> delayed EPS (tardive dyskinesia)

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7
Q

List some typical antipsychotics

A

Chlorpromazine (one methyl group diff from promethazine)

Haloperidol (chem brace)

Droperidol

Fluphenthixol

Fluphenazine

Thiothixene

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8
Q

What are some receptors blocked by typical antipsychotics?

A

Block D2-R, a1-R, H1-R, 5HT2-R, M-R, D4-R

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9
Q

What will be the effects of an antipsychotic’s D2-R block?

A

EPS, Endocrine (growth hormone dec, prolactin inc)

Antiemetic = block of D2 receptor –> no signals to chemo-sensitive trigger zone due to block of D2-R –> reduced vomiting/nausea

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10
Q

What will be the effects of an antipsychotic’s a1-R block?

A

Alpha1-block = dec BP –> dizziness, hypotension, reflex tachycardia

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11
Q

What will be the effects of an antipsychotic’s H1-R block?

A

Sedation, drowsiness, inc appetite/weight

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12
Q

What will be the effects of an antipsychotic’s M-R block?

A

Dry mouth, urinary retention, dec HR, tachycardia, etc.

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13
Q

What will be the effects of an antipsychotic’s 5HT2R block?

A

Dec EPS, alleviate negative symptoms

Anxiety, insomnia

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14
Q

What will be the effects of an antipsychotic’s D4-R block?

A

Alleviate neg symptoms of schizophrenia, dec EPS

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15
Q

When is parkinsonism commonly seen in patients with antipsychotics?

A

5-30 days = tremors, rigidity, shuffling gait, postural abnormalities

Treat w/ antimusc (benzotropine, diphenhydramine = CAMS)

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16
Q

What movement disorders are commonly observed in people taking antipsychotics?

A

Akathisia
Parkinsonism
Dystonia
Dyskinesia
Tardive dyskinesia

17
Q

What is dystonia?

A

neurological movement disorder causing contraction/spasming of muscles involuntarily

twisting, repetitive, patterned movement

18
Q

What is akathisia?

A

Restlessness and agitation (seen as continuous movements)

19
Q

What is dyskinesia?

A

Difficulty or distortion in performing voluntary movements

20
Q

What is tardive dyskinesia?

A

late/tardy onset of dyskinesia, typically after drug treatment

21
Q

Which typical antipsychotics cause the most EPS? (Why?)

A

Fluphenazine, Haloperidol

Strong D2 blockers

22
Q

Which typical antipsychotics cause the most sedation? (Why?)

A

Chlorpromazine, thioridazine

H1 block

23
Q

Which typical antipsychotics are the anticholinergic? (Why?)

A

Thioridazine

M-R block, very pro arrhythmic

24
Q

Which typical antipsychotics cause the most orthostatic hypotension? (Why?)

A

Chlorpromazine, thioridazine

strong alpha1-block

25
Q

What are the low potency antipsychotics?

A

Chlorpromazine, thioridazine

26
Q

List the relevant atypical antipsychotics

A

Amisulpride/sulpride (D2 blocker)

Risperidone (paliperidone –> major active metabolite)

Clozapine, olanzapine, quetiapine, asenapine

arpiprazole

Ziprasidone

27
Q

Which typical antipsychotics have an equal affinity for 5HT2 and D4?

A

Clozapine

28
Q

What receptors are olanzapine and risperidone selective to?

A

5HT2 > D2

29
Q

What is an important side effect of clozapine and chlorpromazine?

A

blood dyscrasias = neutropenia, severe constipation

30
Q

Which antipsychotics have the most movement disturbances?

A

haloperidol

31
Q

What is a common effect of typical antipsychotics?

A

Sedation, anticholinergic effect (esp clozapine and chlorpromazine)

32
Q

How long are antipsychotics continued on for? Can you stop abruptly?

A

Continued for 12 months at least (aster acute psychotic symptoms)

Can consider change to low dose regimen/gradual withdrawal

All antipsychotics should be tapered slowly

Human Pharmacy (11 decks)

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