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Nervous System > CNS Pharmacology (SUDWEEKS) > Flashcards

CNS Pharmacology (SUDWEEKS) Flashcards

1
Q

Which of the following are “Typical antipsychotics”?

A. Clozapine

B. Olanzapine

C. Phenothiazines

D. Risperidone

A

C. Phenothiazines

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2
Q

Discuss the Dopamine hypothesis:

A

Hyperactive dopamine pathway causes psychosis.

There are “typical antipsychotics” and “atypical antipsychotics” that both are dopamine antagonist

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3
Q

Which of the following are “Typical antipsychotics”?

A. Clozapine

B. Olanzapine

C. Chlorpromazine

D. Risperidone

A

C. Chlorpromazine

note: chlorpromazine is a derivative of phenothiazine

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4
Q

Which of the following is the most widely prescribed “Typical antipsychotics”?

A. Clozapine

B. Olanzapine

C. Haloperidol

D. Risperidone

A

C. Haloperidol

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5
Q

______ is the most widely prescribed “typical antipsychotic”.

A

Haloperidol

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6
Q

“Typical” antipsychotics can cause all of the following EXCEPT:

A. Tardive dyskinesias

B. Parkinson like symptoms

C. Dystonias (spasms)

D. Perioral tremor

E. “Typical” antipsychotics can cause all of the above

A

E. “Typical” antipsychotics can cause all of the above

note: “typical” antipsychotics can cause perioral tremor - “Rabbit syndrome”

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7
Q

Clozapine is an _______.

A. “typical” antipsychotic

B. “atypical” antipsychotic

A

B. “atypical” antipsychotic

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8
Q

Discuss “Typical” vs “Atypical” antipsychotics:

A

Both of them block D2 receptors (dopamine)

“Typical” Antipsychotics:

  • 1st generation dopamine antagonist
  • Eg. Chlorpromazine and Haloperidol
  • Can cause:
    • Tardive dyskinesias
    • Parkinson like symptoms
    • Dystonias (spasms)
    • Perioral tremor “Rabbit syndrome”

“Atypical” Antipsychotics:

  • Newer (2nd generation” D2 antagonist
  • Less likely to develop tardive dyskinesias
  • Eg. Clozapine
  • some also block 5HT-2 receptors
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9
Q

How can you manage the extrapyramidal motor effects of antipsychotics?

A

By using Antimuscarinic drugs

  • ACh and dopamine oppose each other in the basal ganglia, so blocking muscarinic receptors tends to balance out the blocking of the dopamine receptors by the antipsychotic drugs
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10
Q

Discuss Neuroleptic Malignant Syndrome:

A

Neuroleptic Malignant Syndrome

  • A life-threatening neurological disorder that is an adverse rxn to antipsychotic drugs
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11
Q

What is the desired mechanism of action of antipsychotics?

A

Dopamine blockers

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12
Q

What are other adverse effects of antipsychotic use?

A
  • Antimuscarinic symptoms (from the antimuscarinic drugs used to tx antipsychotic drug side effects): constipation, dry mouth, bradycardia
  • Orthostatic hypotension
  • Convulsions
  • Photosensitivity
  • Cardiac arrhythmias (long QT syndrome)
  • Galactorrhea (Dopamine is “PIH” Prolactin Inhibiting Hormone
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13
Q

What are the common side effects of antipsychotic drugs?

A

Extrapyramidal motor effecs

  • Tardive dyskinesias (jerky movements)
  • Parkinson like symptoms
  • Dystonias (spasma)
  • Perioral tremor “Rabbit Syndrome”
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14
Q

_______ are the 3rd most common prescription drugs taken by americans of all ages.

A

Antidepressants

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15
Q

Discuss the difference between Unipolar vs Bipolar depression:

A

Unipolar: mood changes in one direction

  • stress related, not genetic

Bipolar: less common than unipolar

  • hereditary
  • oscillates between manic and depressive
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16
Q

Which of the following is a selective serotonin reuptake inhibitor (SSRI)?

A. Amitriptyline

B. Fluoxetine

C. Venlafaxine

D. Duloxetine

E. Bupropion

A

B. Fluoxetine

Amitriptyline = Tricyclic antidepressant (TCAs)

Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)

Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Bupropion = Norepinephrine Reuptake inhibitor

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17
Q

Which of the following is a Norepinephrine reuptake inhibitor?

A. Amitriptyline

B. Fluoxetine

C. Venlafaxine

D. Duloxetine

E. Bupropion

A

E. Bupropion (Wellbutrin)

Amitriptyline = Tricyclic antidepressant (TCAs)

Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)

Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Bupropion = Norepinephrine Reuptake inhibitor

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18
Q

Which of the following is Tricyclic antidepressant (TCAs)?

A. Amitriptyline

B. Fluoxetine

C. Venlafaxine

D. Duloxetine

E. Bupropion

A

A. Amitriptyline

note: it has “tri” in the name

Amitriptyline = Tricyclic antidepressant (TCAs)

Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)

Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Bupropion = Norepinephrine Reuptake inhibitor

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19
Q

Which of the following is a mixed 5-HT and NE reuptake inhibitor (SNRIs)?

A. Amitriptyline

B. Fluoxetine

C. Venlafaxine

D. Duloxetine

E. Bupropion

A

C. Venlafaxine

D. Duloxetine

Amitriptyline = Tricyclic antidepressant (TCAs)

Fluoxetine = Selective Serotonin Reuptake Inhibitor (SSRIs)

Venlafaxine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Duloxetine = mixed 5-HT and NE Reuptake Inhibitors (SNRIs)

Bupropion = Norepinephrine Reuptake inhibitor

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20
Q

Which of the following is a Monoamine Oxidase Inhibitor (MAOIs)?

A. Amitriptyline

B. Fluoxetine

C. Phenelzine

D. Duloxetine

E. Bupropion

A

C. Phenelzine

note: these should not be used together w/ other antidepressant drugs, or w/ autonomic drugs that cause the release of catecholamines or serotonin

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21
Q

All of the following are side effects of SSRIs EXCEPT:

A. Nausea

B. Anorexia

C Insomnia

D. Dry mouth

E. Loss of libido

A

D. Dry mouth

SSRI side effects:

  • Nausea
  • Anorexia
  • Insomnia
  • Loss of libido

TCAs side effects:

  • Initial use:
    • sedation
    • confusion
    • motor impairment
  • Other effects:
    • dry mouth
    • blurred vision
    • urinary retention
    • postural hypotension
    • Ventricular dysrhythmias
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22
Q

List the side effects of TCAs:

A

TCAs side effects

Initial use:

  • sedation
  • confusion
  • motor impairment
  • (these side effects usually wear off in days)

Other effects:

  • dry mouth
  • blurred vision
  • urinary retention
  • postural hypotension
  • continued sedation in some, overdose –> ventricular dysrhythmias
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23
Q

List the side effects for Monoamine receptor antagonist and MAOIs:

A

Monoamine receptor antagonist

  • constipation
  • increased appetite
  • weight gain
  • somnolence

MAOIs

  • hypotension
  • tremors
  • exitement
  • insomnia
  • increased appetite
  • weight gain
  • dry mouth
  • bluurred vision
  • urinary retention
  • Interacts with foods containing tyramine (i.e. cheese and fermented compounds
  • Drug interactions can be life-threatening
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24
Q

Which of the following drugs counteract with tyramine containing foods (i.e. cheese and fermented compounds)?

A. SSRIs

B. Monoamine receptor antagonist

C. TCAs

D. MAOIs

A

D. MAOIs

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25
Q

Which of the following is the most commonly prescribed antidepressants?

A. SSRIs

B. Monoamine receptor antagonist

C. TCAs

D. MAOIs

A

A. SSRIs

note: generally have the fewest severe side effects, and high therapeutic index

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26
Q

List other clinical uses for each of the following:

  • TCAs
  • TCAs and SSRIs
  • SSRIs
  • Buproprion
A
  • TCAs for neuropathic pain
  • TCAs and SSRIs for fibromyalgia
  • SSRIs for anxiety disorders
  • SSRIs for ADHD
  • Buproprion (NE uptake blocker) for addiction
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27
Q

Which of the following is a Monoamine receptor antagonist (i.e. alpha2 blocker)?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

B. Mirtazapine

Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors

Mirtazapine: monoamine receptor antagonist (alpha2 blocker)

St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes

Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors

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28
Q

Which of the following is a weak monoamine uptake inhibitor that activates P450 enzymes?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

C. St. John’s wort

Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors

Mirtazapine: monoamine receptor antagonist (alpha2 blocker)

St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes

Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors

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29
Q

Which of the following is thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and also blocks alpha1 receptors?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

A. Trazodone

Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors

Mirtazapine: monoamine receptor antagonist (alpha2 blocker)

St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes

Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors

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30
Q

Which of the following is an S-enantiomer of ketamine (general anesthetic) given as a nasal spray that blocks NMDA receptors?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

D. Esketamine

Trazodone: thought to potentiate 5HT activity (get mixed agonist, antagonist activity) and blocks alpha1 receptors

Mirtazapine: monoamine receptor antagonist (alpha2 blocker)

St. John’s wort: (contain hyperforin) a weak monoamine uptake inhibitor that activates P450 enzymes

Esketamine: S-enantiomer of ketamine (general anesthetic) that blocks NMDA receptors

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31
Q

Which of the following is a newly approved antidepressant?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

D. Esketamine

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32
Q

Which of the following blocks NMDA receptors?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

D. Esketamine

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33
Q

Which of the following is an S-enantiomer of ketamine (general anesthetic)?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

D. Esketamine

note: esketamine is given as a nasal spray

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34
Q

Which of the following has to be taken under doctor’s supervision and is contraindicated in pts w/ hypertension?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

D. Esketamine

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35
Q

Which of the following contains hyperforin?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

C. St. John’s wort

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36
Q

Which of the following get mixed agonist/antagonist activity?

A. Trazodone

B. Mirtazapine

C. St. John’s wort

D. Esketamine

A

A. Trazodone

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37
Q

List 3 drugs used to tx bipolar depression:

A

Lithium, Valproate and Olanzapine

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38
Q

Which of the following is an atypical antipsychotic?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

C. Olanzapine

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39
Q

Which of the following is a mixed dopamine and 5HT2 receptor antagonist?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

C. Olanzapine

40
Q

_______ is a prolactin inhibiting hormone that may lead to galactorrhea.

A

Dopamine

41
Q

Which of the following is an antiepileptic drug?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

B. Valproate

42
Q

Which of the following is an anti-mania or “Mood stabilizing drug”?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

A. Lithium

43
Q

Which of the following is used prophylactically to avoid manic-depressive episodes?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

A. Lithium

Lithium toxicity: nausea, diarrhea, convulsions, coma, hyperreflexia, cardiac arrhythmias, hypotension, thyroid effects, polyuria

  • Dietary Na+ restriction leads to increaed lithium retention in the kidneys and can lead to toxicity
44
Q

Which of the following has a narrow therapeutic index?

A. Lithium

B. Valproate

C. Olanzapine

D. Diazepam

A

A. Lithium

note: careful with lithium toxicity

45
Q

Most ______ work by activating or enhancing chloride channels (GABA-A receptors).

A

Sedative hypnotics

GABA-A receptors also have allosteric binding sites

  • BZ1 site (omega-1)
  • BZ2 site (omega-2)
46
Q

List some uses for sedative hypnotics:

A
  • antianxiety
  • panic disorders
  • sedation
  • anticonvulsants
  • amnesia
  • insomnia
  • skeletal muscle relaxation (particularly baclofen)
47
Q

List some adverse effects of Sedative Hypnotics:

A

Adverse effects

  • ataxia
  • confusion
  • excessive sedation
  • amnesia
  • altered sleep patterns
48
Q

_______ and _______ enhance effect of native GABA on GABA-A receptors (modulators, not direct agonist).

A

Benzodiazepines and Barbiturates

note: barbiturates at higher doses also inhibit AMPA (glutamate) receptors

49
Q

All of the following are classified as Barbiturates EXCEPT:

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

B. Diazepam

Barbiturates = Phenobarbital, Pentobarbital, Thiopental

Benzodiazepines = Diazepam

50
Q

Which of the following is a Benzodiazepine?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

B. Diazepam

51
Q

Which of the following is a long acting Barbiturate used to tx epilepsy?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

A. Phenobarbital

Long acting =Phenobarbital

Intermediate acting = Pentobarbital

Short acting = Thiopental

52
Q

Which of the following is a intermediate acting Barbiturate sometimes used for sleep induction?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

D. Pentobarbital

Long acting =Phenobarbital

Intermediate acting = Pentobarbital

Short acting = Thiopental

53
Q

Which of the following is a short acting Barbiturate used as an induction anesthetic?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

C. Thiopental

Long acting =Phenobarbital

Intermediate acting = Pentobarbital

Short acting = Thiopental

54
Q

Which of the following is used to tx epilepsy?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

A. Phenobarbital

55
Q

Which of the following is used for sleep induction?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

D. Pentobarbital

56
Q

Which of the following is an induction anesthetic?

A. Phenobarbital

B. Diazepam

C. Thiopental

D. Pentobarbital

A

C. Thiopental

57
Q

Which of the following is contraindicated in certain types of porphyria (genetic condition affecting heme synthesis)?

A. MAOIs

B. SSRIs

C. Benzodiazepines

D. Barbiturates

A

D. Barbiturates

58
Q

Which of the following have active metabolites that extends the functional half-life?

A. Metoprolol

B. Clonidine

C. Diazepam

D. Phenobarbital

E. Pentobarbital

A

C. Diazepam

59
Q

Which of the following act on GABA-A receptors (BZ1 receptor site) and has a low risk of dependence?

A. Buspirone

B. Baclofen

C. Chloral Hydrate

D. Zolpidem

E. Flumazenil

A

D. Zolpidem

  • Not anticonvulsant
  • used mainly to tx insomnia

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Chloral Hydrate = used in dentistry for conscious sedation

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

60
Q

Which of the following has a similar action as bezodiazepines but is used as a short acting sleep inducer?

A. Buspirone

B. Baclofen

C. Chloral Hydrate

D. Zolpidem

E. Flumazenil

A

C. Chloral Hydrate

  • used for conscious sedation in dentistry, repetitive doses should not be used
  • can result in serious cardiac toxicities if not controlled

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Chloral Hydrate = used in dentistry for conscious sedation

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

61
Q

Which of the following is a GABA-A antagonist that will reverse sedation from drugs acting at BZ sites?

A. Buspirone

B. Baclofen

C. Chloral Hydrate

D. Zolpidem

E. Flumazenil

A

E. Flumazenil

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Chloral Hydrate = used in dentistry for conscious sedation

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

62
Q

Which of the following is a GABA-B agonist?

A. Buspirone

B. Baclofen

C. Chloral Hydrate

D. Zolpidem

E. Flumazenil

A

B. Baclofen

  • G-protein linked receptor, not an ion channel, activates Gi, leads to decreased cell activity. Sometimes used to treat trigeminal neuralgia

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Chloral Hydrate = used in dentistry for conscious sedation

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

63
Q

Which of the following block H1 receptors in CNS to cause sedation?

A. Buspirone

B. Baclofen

C. Diphenhydramine

D. Zolpidem

E. Flumazenil

A

C. Diphenhydramine

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

Diphenhydramine = H1 receptor blocker

64
Q

Which of the following is a partial agonist at 5-HT1A receptors (NOT GABA)?

A. Buspirone

B. Baclofen

C. Diphenhydramine

D. Zolpidem

E. Flumazenil

A

A. Buspirone

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

Diphenhydramine = H1 receptor blocker

65
Q

Which of the following is not clinically used bc it likely affects multiple targets including GABA-A?

A. Buspirone

B. Baclofen

C. Diphenhydramine

D. Zolpidem

E. Ethanol

A

E. Ethanol

Buspirone = partial agonist at 5-HT1A receptors

Baclofen = GABA-B agonist

Zolpidem = GABA-A agonist (BZ1 recceptor site)

Flumazenil = GABA-A antagonist

Diphenhydramine = H1 receptor blocker

Ethanol = affects multiple targets not clinically used

66
Q

Which of the following is a sedative hypnotic?

A. Methocarbamol

B. Carisoprodol

C. Cyclobenzaprine

D. Two of the above

E. All of the above

A

E. All of the above

note: all of these answer choices are sedative hypnotics that have less described mechanisms of action

67
Q

Discuss Epilepsy:

A

Epilepsy

  • Seizures - inappropriate and excessive activity of CNS neurons
  • Partial seizures are limited to one side of the brain at onset
  • 2 types of generalized seizures:
    • Tonic-clonic (grand mal)
    • Absence (petit mal)
68
Q

Discuss the mechanisms of action for Antiepileptics?

A

Antiepileptics

  • NaV+ channels antagonist
  • Ca2+ channel antagonist
  • Glutatmate receptor antagonist (AMPA, NMDA)
  • Cl- channel agonists
69
Q

All of the following are mechanisms of action for Antiepileptics EXCEPT:

A. NaV+ channel antagonist

B. Ca2+ channel antagonist

C. Cl- channel antagonist

D. Cl- channel agonist

A

C. Cl- channel antagonist

70
Q

Which of the following is an antiepileptic drug w/ a mechanism of action at the GABA-A receptor modulator?

A. Clonidine

B. Zolpidem

C. Phenobarbital

D. Flumazenil

E. All of the above

A

C. Phenobarbital

71
Q

Discuss Phenobarbital:

  • What is Phenobarbital used to tx?
  • What is the mechanism of action?
  • What are the adverse effects of Phenobarbital?
A

Phenobarbital

  • Antiepileptic
  • GABA-A modulators
  • Adverse effects:
    • induction of liver enzymes —> a lot of potential for drug/drug interactions
    • sedation
    • hepatic toxicity
    • Osteomalacia
    • Respiratory depression
72
Q

Which of the following has a lot of potential for drug/drug interactions due to the induction of liver enzymes?

A. Clonidine

B. Zolpidem

C. Phenobarbital

D. Flumazenil

E. All of the above

A

C. Phenobarbital

73
Q

Which of the following is a NaV+ antagonist used to tx epilepsy?

A. Clonidine

B. Zolpidem

C. Phenobarbital

D. Flumazenil

E. Phenytoin

A

E. Phenytoin

74
Q

Discuss Phenytoin:

  • What type of drug is Phenytoin?
  • What is the mechanism of action for Phenytoin?
  • Sometimes also used for _______.
  • Why is Phenytoin dangerous?
  • What are adverse effects of Phenytoin?
A

Phenytoin

  • Antiepileptic
  • NaV+ antagonist
  • Sometimes also used for trigeminal neuralgia
  • Phenytoin is dangerous bc it is often eliminated by “Zero-order kinetics”
    • this means their is a potential for overdose
  • Adverse effects:
    • Gingival hyperplasia
    • can get drug/drug interactions from liver metabolism
75
Q

Which of the following is eliminated by “Zero-order kinetics” w/ a potential for overdose?

A. Phenytoin

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

A. Phenytoin

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

Phenytoin = NaV+ antagonist

76
Q

Which of the following may cause gingival hyperplasia?

A. Phenytoin

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

A. Phenytoin

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

Phenytoin = NaV+ antagonist

77
Q

Which of the following is a NaV+ antagonist used to tx epilepsy?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

D. Carbamazepine

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

78
Q

Which of the following is a GABA-A receptor modulator used to tx epilepsy?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

B. Phenobarbital

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

79
Q

Which of the following antiepileptic drugs is metabolized to phenobarbital and has acute systemic and CNS toxicity that tend to limit its use?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

C. Primidone

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

80
Q

Which of the following antiepileptics is approved as adjunct for partial seizures but is actually used more to treat neuralgia than epilepsy?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

E. Gabapentin

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

81
Q

Which of the following is thought to increase GABA and block NaV+ and CaV++?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Primidone

D. Carbamazepine

E. Gabapentin

A

A. Valproic acid (Valproate)

Ethosuximide = block CaV2+ for absence seizures

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

82
Q

Which of the following is thought to block CaV2+ and is FFDA approved as adjunct for absence seizures?

A. Valproic acid (Valproate)

B. Phenobarbital

C. Ethosuximide

D. Carbamazepine

E. Gabapentin

A

C. Ethosuximide

Ethosuximide = block CaV2+ for absence seizures

Valproic acid (Valproate) = GABA agonist, NaV+ and CaV2+ antagonist

Phenobarbital = GABA-A

Primidone = metabolized to phenobarbital

Carbamazepine = NaV+ antagonist

Gabapentin = unkown mechanism of action

83
Q

Which of the following is FDA approved as adjunct for absence seizures?

A.Ethosuximide

B. Phenobarbital

C. Phenytoin

D. Carbamazepine

E. Gabapentin

A

A.Ethosuximide

84
Q

Discuss Parkinson’s Disease:

A

Parkinson’s Disease

  • Characterized by progressive hypokinesia
    • loss of voluntary movement
  • Tremor at rest
    • involuntary hyperkinesia
    • “Pill rolling”
    • tends to disappear w/ voluntary movement
  • Progresses to muscle rigidity
    • Patients have “Off” and “On” phases
  • Can lead to cognitive impairment
85
Q

__________ is characterized by a defect in the signaling pathways of the basal ganglia.

A

Parkinson’s Disease

86
Q

Parkinson’s disease is characterized by a defect in the signaling pathways of the ______.

A

basal ganglia

87
Q

Discuss Parkinson’s disease tx strategies?

A

Parkinson’s tx strategies

  • increase dopamine receptor activation in basal ganglia
  • block muscarinic receptors in the basal ganglia
  • block NMDA glutamate receptors
88
Q

In Parkinson’s disease there is a loss of DA cells in the ______.

A

substantia nigra

  • leads to less GABAergic (inhibitory) stimulation of the thalamus
  • Get increased excitatory output to the motor cortex
89
Q

Which of the following is transported past BBB and converted into dopamine to tx Parkinson’s?

A. Carbidopa

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

B. Levodopa

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

90
Q

Which of the following is a dopa decarboxylase inhibitor?

A. Carbidopa

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

A. Carbidopa

note: Carbipoa is used in conjunction w/ L-Dopa

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

91
Q

Which of the following does NOT pass BBB, keeps L-Dipa from being converted into dopamine in periphery and reduces side effect?

A. Carbidopa

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

A. Carbidopa

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

92
Q

Which of the following block catecholamine O-methyl transferase (COMT), which prevents breakdown of dopamine in CNS?

A. Carbidopa

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

D. Tolcapone

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

93
Q

Which of the following is a DA receptor agonist used to tx Parkinson’s?

A. Selegiline

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

C. Pramipexole

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

94
Q

Which of the following blocks monoamine oxidase type B (MAO-B), which prevents breakdown of dopamine in CNS?

A. Clonidine

B. Levodopa

C. Pramipexole

D. Tolcapone

E. Rasagiline

A

E. Rasagiline

Carbipoba = dopa decarboxylase inhibitor

Levodopa = (L-Dopa), transported pass BBB converted to dopamine

Pramipexole = DA receptor agonist

Tolcapone = block catecholamine O-methyl transferase (COMT)

Rasagiline = blocks monoamine oxidase type B (MAO-B)

Selegiline = similar mechanism to rasagiline

95
Q

Which of the following blocks H1 histamine receptors and is used to tx extra-pyramidal side-effects?

A. Amantadine

B. Diphenhydramine

C. Benzotropine

D. Selegiline

A

B. Diphenhydramine

96
Q

Which of the following is an anticholinergic drug used to tx parkinson’s?

A. Amantadine

B. Diphenhydramine

C. Benzotropine

D. Selegiline

A

C. Benzotropine

97
Q

Which of the following blocks the NMDA receptor and was previously used as an antiflu medication?

A. Amantadine

B. Diphenhydramine

C. Benzotropine

D. Selegiline

A

A. Amantadine

Amantadine = blocks NMDA receptor (Parkinson’s tx)

Diphenhydramine = blocks H1 receptor

Benzotropine = anticholinergic (tx parkinson’s)

Nervous System (7 decks)

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