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Psychopharm > Drug Mechanisms > Flashcards

Drug Mechanisms Flashcards

1
Q

Mechanism of action of typical antipsychotics

(a) pathway of therapeutic efficacy

A

Antagonism of dopamine D2 receptors

(a) Therapeutic efficacy against positive symptoms due to D2 blockade in mesolimbic dopamine pathway

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2
Q

What side effects does D2 blockade cause by blocking the following pathways

(a) nigrostriatal
(b) tuberoinfundibular
(c) mesocortical

A

Dopmaine pathways

(a) Nigrostriatal blockade => EPS
(b) Tuberoinfundibular blockade => hyperprolactinemia
(c) Mesocortical blockade worsens negative symptoms (alogia, avolition) and cognitive symptoms (poor attention and vigilance)

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3
Q

3 receptors (besides DA) antagonized by typical antipsychotics

A

Anti:

  • histamine-1
  • alpha-adrenergic
  • muscarinic (type of cholinergic)
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4
Q

General mechanism of atypical antipsychotics

A

Antagonism of D2 and 5HT2 receptors

dopamine D2 and serotonin 2A receptors

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5
Q

Describe the effect of the 2 receptors blocked by atypical antipsychotics

A

(i) Blocking D2 in the mesolimbic dopamine pathway = therapeutic effect against positive symptoms (ex: hallucinations, delusions)
(i) Blocking 5HT2A in mesocortical, nigrostriatal, and tuberoinfundibular pathways enhances DA transmission => mitigating ‘typical’ side effects

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6
Q

What receptors do atypical antipsychotics block?

A
  • Therapeutically: D2 blockade
  • Decreased ‘typical’ side effects due to 5HT2A blockade

Also blocks to varying degrees:
muscarinic, alpha-adrenergic, histamine-1

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7
Q

Mechanism of clozapine

A

Atypical antipsychotic

-wide antagonism: 5HT2A, D1, D2, D4, H1, muscarinic, and alpha1

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8
Q

Mechanism of risperidone

A

Atypical antipsychotic

-antagonism: 5HT2A, D2, alpha1

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9
Q

Mechanism of olanzapine

A

Atypical antipsychotic

  • wide antagonism: 5HT2A, D1, D2, D4, H1, muscarinic, and alpha 1 (same as clozapine)
  • among the atypicals, may have efficacy second only to clozapine
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10
Q

Mechanism of quetipaine

A 
Atypical antipsychotic (quetiapine = Seroquel)
-antagonism: 5HT2A, D2, alpha1, alpha2, H1
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11
Q

Mechanism of ziprasidone

A

Atypical antipsychotic
(ziprasidone = Geodon)
-antagonism: 5HT1A, 5HT2A, D2, D3, and monoamine reuptake pumps (NE, 5HT, DA)

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12
Q

Which antipsychotic inhibits monoamine reuptake pumps?

A

Ziprasidone (= Geodon)

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13
Q

Which atypical antipsychotics antagonize muscarinic receptors?

A
  • clozapine

- olanzapine

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14
Q

Mechanism of aripiprazole

A

Aripiprazole (Abilify) = atypical antipsychotic

  • antagonism: 5HT2A
  • partial agonism: D2, 5HT1A
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15
Q

Mechanism of therapeutic action for TCAs

A

Tricyclic Antidepressants proposed mechanism:
antagonism at serotonin (5HT) and NE presynaptic reuptake pumps

-Not fully understood- may involve receptor and downstream secondary messenger transcription changes

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16
Q

Name all the receptors blocked by TCAs

A

Therapeutically block reuptake pumps: 5HT and NE

Block receptors: muscarinic, alpha-adrenergic, H1

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17
Q

Latency period of TCA activity

A

3-4 weeks of administration for therapeutic effect to begin

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18
Q

What is the difference btwn the two groups of TCAs?

A

TCAs grouped into tertiary and secondary amines b/c this predicts side effect profile

Tertiary amines: greater alpha, H1, and muscarinic blockade

Newer, secondary amines: fewer side effects, less sedating, safer in OD

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19
Q

Mechanism of action of MAOIs

A 
Irreversible MAO (monoamine oxidase) inhibitors
-MAO metabolizes monoamines (5HT, DA, and NE) in the presynaptic neuron => MAO inhibition disables momamine degradation
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20
Q

MAO-A vs. MAO-B

(a) Which is blocked by psychiatric drugs?
(b) Which blockade is necessary for therapeutic effect?

A

MAO-A vs. MAO-B

(a) Psychiatric drugs block both
(b) Only MAO-A blockade is necessary for the anti-depressant effect. MAO-A is used to break down tyramine

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21
Q

What other receptors are blocked by MAOIs?

A

MAOIs also block these receptors:

  • alpha1 adrenergic
  • histamine1
22
Q

Mechanism of patch form MAOI?

A

Patch form = transdermal selegiline
-MAOI that at lower doses is selectively MAO-B inhibitor => MAO-A is still around to metabolize tyramine => lower dietary restrictions when selegiline used at lower dose

23
Q

Which drug is suggested to have the best efficacy for depression among all new antidepressants?

A

Venlafaxine (Effexor)

-SNRI

24
Q

Mechanism of action of SSRIs

A

Selective antagonism of 5HT presynaptic reuptake pumps

25
Q

Site of action of SSRIs

A

Thought to be frontal serotonin projections

26
Q

Latency period of SSRIs

A

Same as TCAs: therapeutic effect begins only after 3-4 weeks of administration

27
Q

Mechanism of mirtazapine

A

Mirtazapine (Remeron) = NaSSA = Noradrenergic and specific serotonergic antidepressant

Dual mechanism

  • antagonism at central alpha2 autoreceptors => disinhibition of NE and 5HT release
  • stimulation of alpha1 somatodendritic receptors on serotonin neurons => boosts 5HT release
28
Q

Name all the receptors that mirtazapine acts on

A

Mirtazapine (Remeron)

  • antagonism of central alpha2
  • stimulation of alpha-1
  • blocks: 5HT2A/2C/3 and H1 receptors
29
Q

Mechanism of trazodone

A

Trazodone = SARI = serotonin antagonist and reuptake inhibitor

-selective antagonism at 5HT presynaptic reuptake pump w/ simultaneous 5HT2A blockade

30
Q

Mechanism of nefazodone

A

Nefazodone = SARI = serotonin antagonism and reuptake inhibitor

  • antagonism of 5HT reuptake pump
  • 5HT2A receptor blockade (to protect against sexual dysfxn as side effect)
31
Q

Mechanism of bupropion

A

Bupropion = Wellbutrin = Noradrenergic and dopamine reuptake inhibitor

-antagonism of presynaptic NE and DA reuptake pumps

32
Q

Mechanism of Vilazodone and vortioxetine

A

Selective serotonin reuptake inhibitor and serotonin partial agonist

33
Q

Mechanism of action of benzos

A

Full agonism of GABA-A receptor by increasing frequency of chloride channel openings

34
Q

Which are the most addictive benzos?

A

High potency, short half-life (b/c rapid onset)

ex: Alprazolam (Xanax) = short half-life and high potency

35
Q

What drugs are helpful in EtOH withdrawal, explain the mechanism

A

Benzos can be used in detox in sedative and alcohol addiction due to cross tolerance w/ alcohol and barbiturates

36
Q

Which benzos are safer in liver disease?

A

Lorazepam (Ativan), Oxazepam (Serax), and temazepam (Restoril) don’t require oxidation in the liver => safer in liver disease

-all 3 are short half-life benzos

37
Q

Mechanism of buspirone

A

Buspirone = nonbenzo anxiolytic
-5HT1A agonist

-unclear mechanism of efficacy against anxiety

38
Q

Mechanism of hydroxyzine

A

Hydroxyzine = nonbenzo anxiolytic

-sedating antihistamine

39
Q

Mechanism of zolpidem

A

Zolpidem (Ambien) = GABAergic

40
Q

Mechanism of zaleplon

A

Zaleplon (Sonata) = GABAergic

-short acting, can dose in middle of the night

41
Q

Mechanism of eszopiclone

A

Eszopiclone (Lunesta) = GABAergic

42
Q

Mechanism of diphenhydramine

A

Diphenhydramine (Benadryl) = sedating antihistamine

43
Q

Mechansim of ramelteon

A

Ramelteon (Rozerem) = melatonin MT1 and MT2 receptor agonists
-thought to normalize circadian rhythms

44
Q

Mechanism of lithium

A

Unknown

-theory that has effect on modulation of secondary messenger systems

45
Q

Lithium clearance

A
  • not metabolized in the liver

- cleared almost entirely by the kidney

46
Q

Carbamazepine mechanism of action

A

Unknown mechanism for its effects in mania

-has effect at Na/K channels, possibly enhances GABA

47
Q

Valproic acid mechanism of action

A

Unknown mechanism for its effects in mania

  • inhibits Na/Ca channels => boosting GABA and decreasing glutamate (not known if this is the mechanism that provides mood stabilization)
  • can be rapidly loaded for quicker therapeutic effect
48
Q

Gabapentin mechanism of action

A

GABAergic

-anticonvulsant mood stabilizer

49
Q

Mechanism of action of the classic CNS stimulants

A

Stimulation of alpha and beta adrenergic receptors => triggers release of DA and NE from presynaptic terminals

50
Q

Mechanism of atomoxetine

A

Atomoxetine = Strattera = novel CNS stimulant

-selective inhibition of presynaptic reuptake of NE

Psychopharm (10 decks)

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