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NUNA 679 - ANP Pharm > Anxiolytics, Antiepileptics, Antiparkinsonians, & Alzheimer Therapy > Flashcards

Anxiolytics, Antiepileptics, Antiparkinsonians, & Alzheimer Therapy Flashcards

1
Q

What drugs (in addition to SSRIs and SNRIs) are used for chronic anxiety?

A

Buspirone

Benzodiazepines

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2
Q

Name 3 characteristics of buspirone.

A

Partial 5-HT1A agonist
No sedative or anticonvulsant activity
Caution with other serotonergic drugs

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3
Q

Benzodiazepines are a _________ __________ ________ of GABA at the GABA-A receptor which is a __ channel.

A

positive allosteric modulator; chloride

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4
Q

What makes midazolam an ideal benzo for anesthesia?

A

Short-acting (2-6 hours)

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5
Q

What benzos have active metabolites?

A

Diazepam and Flurazepam

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6
Q

Abrupt cessation of benzodiazepines can case _______ after _____ ________.

A

seizures; severe dependence

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7
Q

Name 2 “Z” compounds/novel benzodiazepine receptor agonists.

A

Zopidem

Zaleplon

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8
Q

What is the advantage of “Z” compounds over benzos for sleep?

A

Induce more normal sleep patterns

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9
Q

What is the benzodiazepine receptor antagonist?

A

Flumazenil

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10
Q

2 precautions concerning flumazenil?

A

Can precipitate seizures in patients with prolonged benzo use.
Effects last 30-60 minutes which is shorter than longer-acting benzos; may require repeat doses.

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11
Q

What is the general MOA of antiepileptics?

A

Keeping the cell polarized/hyperpolarized; preventing efflux of negative ions/promoting influx of positive ions. Involves Na+, Ca+, Cl-.

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12
Q

What antiepileptics suppress sodium influx?

A

Phenytoin

Carbamazepine

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13
Q

What antiepileptics decrease Ca influx?

A

Gabapentin

Pregabalin

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14
Q

What 2 antiepileptic classes potentiate GABA activity?

A

Benzos

Barbiturates

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15
Q

Name 3 mixed mechanism AEDs.

A

Valproate sodium
Topiramate
Laomtrigine

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16
Q

Name an AED with an uncertain mechanism.

A

Levetiracetam

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17
Q

What AEDs are associated with idiosyncratic reactions?

A

Phenytoin
Phenobarbital
Valproic acid
Carbamazepine

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18
Q

Name 4 idiosyncratic reactions to AEDs.

A

Hepatotoxicity
Pancreatitis
Exfoliative dermatitis
Blood dyscrasias

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19
Q

What is fosphenytoin?

A

The prodrug of phenytoin; both are indicated for status epiplepticus.

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20
Q

What are 3 key points about phenytoin levels?

A

Narrow therapeutic index - monitor levels
Induces multiple CYPs
Metabolism is variable (polymorphic CYP2C9/19) and easily saturable

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21
Q

Why is phenytoin easily saturable?

A

Nonlinear kinetic metabolism

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22
Q

Name 3 major s/s of phenytoin toxicity

A

CNS depression - nystagmus, diplopia, ataxia
Idiosyncratic reaction - rash, blood dyscrasias, hepatotoxicity
Vesicant - purple glove syndrome

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23
Q

What is the MOA of phenobarbital?

A

Potentiates GABA

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24
Q

Name 4 AEs for phenobarbital.

A

Cognitive dysfunction/respiratory depression
Idiosyncratic reactions - blood dyscrasias, exfoliative dermatitis, hepatotoxicity
Interferes with vitamins D and K metabolism (bleeding)
Birth defects

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25
Q

Why does phenobarbital have so many DDIs?

A

Potent inducer of hepatic enzymes

26
Q

What is the MOA of carbamazepine?

A

Inhibits sodium influx into neuron

27
Q

What are the 2 most notorious AEs of carbamazepine?

A

Hyponatremia
Bone marrow suppression

(Also an inducer of CYPS and subject to idiosyncratic reaction)

28
Q

In addition to idiosyncratic reactions, what are 2 adverse reactions for which valproate is known?

A

HEPATOTOXICITY (monitor LFTs)

The MOST TERATOGENIC AED

29
Q

What effect does valproate have on CYPs?

A

Inhibitor

30
Q

What are some AEs of topiramate? (4)

A

Cognitive impairment
Metabolic acidosis
Weight loss
Kidney stones

31
Q

What is the MOA of gabapentinoids?

A

Binds to alpha-2-delta subunit of voltage-gated Ca2+ channel leading to decreased Ca2+ influx and decreased excitatory neurotransmitter release

32
Q

Which gabapentinoid is used for fibromyalgia and is schedule V for substance abuse?

A

Pregabalin

33
Q

Name 3 AEs of gabapentinoids.

A

Sedation
Ataxia and vertigo
Peripheral edema

34
Q

Which AEDs are notorious for inducing CYP450? Inhibiting?

A

Carbamazepine, phenytoin, phenobarbital

Valproate

35
Q

Name the two pharmacologic steps to treating status epilepticus.

A

IV benzo

Longer acting AED (phenytoin, fosphenytoin, levetiracetam)

36
Q

What infusions can be initiated for protracted status epilepticus?

A

Propofol or midazolam

37
Q

What is the IV push drug of choice for status epilepticus?

A

Lorazepam (lasts greater than 6 hours)

38
Q

What is the advantage of diazepam for status epilepticus? Disadvantage?

A

Available in rectal gel and intranasal prep (can give without IV access)
Effect usually lasts only 20 minutes

39
Q

What labs should be monitored perioperatively (as indicated) with AED use?

A

CBC, liver function, drug levels

40
Q

What is the mechanism of Parkinson’s disease?

A

Degeneration of DA producing neurons in substantia nigra leading to imbalance of DA and ACh neurotransmitters

41
Q

What Parkinson’s drug increases DA synthesis?

A

L-Dopa/levodopa

42
Q

What Parkinson’s drug inhibits dopa decarboxylase in the periphery?

A

Carbidopa

43
Q

What Parkinson’s drug inhibits COMT in the periphery?

A

Entacapone

44
Q

What Parkinson’s drug inhibits MAOI-B in the CNS?

A

Selegiline

45
Q

What Parkinson’s drug stimulates DA receptors?

A

Ropinirole

46
Q

What Parkinson’s drug promotes DA release?

A

Amantadine

47
Q

What Parkinson’s drug decreases ACh action in the CNS?

A

Trihexyphenidyl

48
Q

For what Parkinson’s patients is levodopa reserved?

A

Greater than 70 years old and advanced disease since drug efficacy decreases with time

49
Q

What Parkinson’s drugs are the 1st choice for mild to moderate disease?

A

DA agonists - ropinirole and pramipexole

Remember ropidop[amine] and the pex!

50
Q

DDIs with pro-dopamine Parkinson’s drugs?

A

DA2 receptor antagonists:
Antipsychotics
Antiemetics (promethazine, droperidol)
Prokinetics (metoclopramide)

51
Q

Name 2 MAO-B inhibitors

A

Selegiline
Rasagiline

(Remember Mao’s B-geline for incredible style)

52
Q

MAO-B DDIs?

A

MANY!

Avoid with opioids/serotonergic drugs d/t risk of serotonin syndrome

53
Q

Name two centrally-acting antimuscarinics

A

Benztropine

Trihexyphenidyl

54
Q

Abrupt withdrawal of levodopa can cause…?

A

Worsening muscle rigidity and interfere with ventilation

55
Q

What drug classes are used to treat cognitive impairment in early to moderate Alzheimer disease?

A

Centrally acting acetylcholinesterase inhibitors (AChE-I)

NMDA type glutamate receptor antagonist

56
Q

Name an NMDA type glutamate receptor antagonist

A

Memantine

57
Q

Name 3 AChE-Is.

A

Galantamine
Donepezil
Rivastigmine

(Remember “gallantly down the river”)

58
Q

What affect can AChE-Is have on a depolarizing NMB?

A

Effects prolonged (Sch)

59
Q

What effect could AChE-Is have on nondepolarizing NMBs?

A

Diminished effects

60
Q

In the PICU, a 76‐year‐old patient with Parkinson’s Disease
begins to show increasing signs of tremor and rigidity. Which of
the following perioperative medications is most likely to have
contributed to the exacerbation of PD symptoms?
A. Ondansetron (Zofran)
B. Haloperidol (Haldol)
C. Fentanyl (Duragesic)
D. Aprepitant (Emend)
E. Glycopyrrolate (Robinul)

A

B

61
Q 
Review Question 2
Which of the following drug/mechanism pair is correctly
matched?
A. Ropinirole/dopa decarboxylase inhibition
B. Trihexyphenidyl/dopamine precursor
C. Flumazenil/ MAOI‐A inhibitor
D. Lorazepam/GABA‐A allosteric agonist
E. Phenytoin/calcium channel antagonist
A

D

62
Q

A 61‐year‐old woman with a history of a seizure disorder is admitted
for an appendectomy. She will receive lorazepam (Ativan) for anxiety
preoperatively. Lorazepam is inactivated by CYP3A4. Which of the
following AEDs is most likely to increase the serum concentration of
lorazepam?
A. Phenytoin (Dilantin)
B. Carbamazepine (Tegretol)
C. Divalproex (Depakote)
D. Topiramate (Topamax)
E. Lamotrigine (Lamictal)

A

C

NUNA 679 - ANP Pharm (9 decks)

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