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Pharm Exam 4 > Antiepileptics/CNS stimulants/Antiparkisonian > Flashcards

Antiepileptics/CNS stimulants/Antiparkisonian Flashcards

1
Q

Term used to designate a group of chronic central nervous system (CNS) disordered characterized by the onset of sudden disturbances of sensory, motor, autonomic, or psychic origin

A

Epilepsy

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2
Q

Goal of epilepsy treatment

A

control seizures with minimal medication related adverse effects

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3
Q

Antiepileptics are dosed based on _____ function

A

renal

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4
Q

Antiepileptics that rely on renal excretion:

A 
Gabapentin
Pregabalin
Levitiracetam
Vigabatrin 
Zonisamide
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5
Q

Principle binding protein for anti epileptic drugs

A

Albumin

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6
Q

Highly protein bound antiepileptics

A

Phenylbutazone
Thyroxine
Salicylates

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7
Q

Antiepileptics that compete for protein binding sites of highly bound antiepileptic drugs, can displace the bound drug and lead to increase in the plasma concentration:

A

Phenytoin
Valproate
Carbamazepine

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8
Q

Enzyme-inducing anti epileptic drugs (7)

A 
PPPCLOT
Phenobarbital
Phenytoin
Primidone
Carbamazepine
Lamotrigine
Oxycarbazepine
Topiramate
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9
Q

Enzyme-inducing anti epileptics affect which cytochrome?

A

p450

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10
Q

Enzyme-inducing anti epileptics and oral contraceptives

A

anti epileptics render oral contraceptives ineffective, higher dose required

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11
Q

Enzyme-inducing anti-epileptics and induction drugs

A 
Increased dose requirements of:
thiopental
propofol
midazolam
ipioids
non-depolarizing neuromuscular blocking drug
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12
Q

Phenytoin is ___% protein bound

A

90%

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13
Q

Phenytoin goal plasma concentration and its metabolism is unique:

A

Control of seizures is usually obtained when plasma concentrations are 10-20 ug/ml
When plasma concentration <10, first order kinetics
When plasma concentrations >10, zero order kinetics (saturated and dose dependent)
PLASMA CONCENTRATION MONITORING

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14
Q

Only agent for which plasma concentration monitoring is recommended due to nonlinear saturation dose kinetics

A

Phenytoin

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15
Q

Na, Ca, Na+Ca, or GABA?

Phenytoin

A

Na+ Ca

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16
Q

Na, Ca, Na+Ca, or GABA?

Carbamazepine

A

Na+ Ca

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17
Q

Na, Ca, Na+Ca, or GABA?

Phenobarbital

A

Ca and GABA

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18
Q

Na, Ca, Na+Ca, or GABA?

Benzodiazepines

A

GABA

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19
Q

Na, Ca, Na+Ca, or GABA?

Ethosuximide

A

Ca Channel

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20
Q

Na, Ca, Na+Ca, or GABA?

Primidone

A

Na

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21
Q

Na, Ca, Na+Ca, or GABA?

Valproate

A

Na + Ca

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22
Q

Na, Ca, Na+Ca, or GABA?

Lamotrigine

A

Na + Ca

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23
Q

Na, Ca, Na+Ca, or GABA?

Zonisamide

A

Na + Ca

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24
Q

Gabapentin acts on what?

A

GABA

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25
Q

Phenobarbital class

A

barbiturates

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26
Q

Phenobarbital is a second line anti epileptic due to _____

A

cognitive and behavioral SE

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27
Q

Phenobarbital SE in adult

A

sedation

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28
Q

Phenobarbital SE in peds

A

hyperactivity

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29
Q

Phenobarbital drug interaction:

A

accelerates interactions with lipid soluble drugs

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30
Q

Phenobarbital prolongs ___ channel opening and limits the spread of seizure activity and increases seizure threshold

A

Cl

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31
Q

Drug of choice for Digitalis arrhythmias

A

Phenytoin

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32
Q

Goal plasma concentration of phenytoin

A

10 to 20 ug/ml

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33
Q

Adverse side effects phenytoin

A

nystagmus, diplopia, vertigo, ataxia, neurotoxic effects

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34
Q

Phenytoin induces lipid soluble drugs…

A

carbamazepine, valproid acid, ethosuximide, anticoagulants, corticosteroids

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35
Q

Phenytoin and NMB

A

need higher doses of non-depolarizers

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36
Q

Valproic acid (inhibits/induces) metabolism

A

inhibits

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37
Q

valproic acid and phenytoin

A

Valproic acid slows metabolism of phenytoin

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38
Q

valproic acid and phenobarbital

A

valproic acid causes phenobarbital plasma concentration to increase by 50%

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39
Q

first line treatment for status epilepticus

A

Diazepam

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40
Q

first line treatment for local anesthetic induced seizures

41
Q

Status epilepticus:

A

patient experiences prolonged or rapidly recurring convulsions for 5 minutes or more

42
Q

____ seizure control is associated with improved clinical outcome

43
Q

Diazepam route in status epilepticus

A

IV or rectal

44
Q

Other status epilepticus drugs:

A

fosphenytoin, phenytoin, phenobarbital, valproic acid, levetiracetam, propofol

45
Q

fosphenytoin SE

A

hypotension and prolongation of QT interval

46
Q

Parkinsons Disease (definition)

A

chronically progressive neurodegenerative disease results from the loss of dopaminergic neurons in the substantia migration pars compact region of the basal ganglia

47
Q

Principle inhibitory neurotransmitter in Parkisons

48
Q

Goal of Parkinsons treatment

A

treat debilitating symptoms

49
Q

Does dopamine cross BBB?

50
Q

T/F: Parkinsons medications can slow progression of the disease

A

False, all medications are palliative

51
Q

Parkinsons treatment:

A

administration of levodopa (dopamine precursor) or drugs that mimic dopamines action

52
Q

When pharmacological options fail for parkinsons, next step is

53
Q

Does levodopa cross BBB?

54
Q

Where is levodopa metabolized to dopamine?

A

liver (95%)

55
Q

Levodopa SE:

A

NV, dyskinesia, psychosis, cardiac dysrhythmias, flushing of skin, orthostatic hypotension, RED/BLACK URINE

56
Q

How to minimize levodopa SE:

A

administer with peripheral decarboxylase inhibitor

57
Q

Drugs to avoid in Parkinsons:

A

antipsychotics (butyphenones, phenothiazines)
droperidol
Metoclopramide

58
Q

What vitamins increases metabolism of levodopa

A

Pyridoxine (B6)

59
Q

What drug class improves symptoms of Parkinsons disease?

A

anticholinergics

60
Q

MAO-inhibitors in Parkinsons:

A

increase intra-synaptic time of dopamine

61
Q

Peripheral Carboxylase inhibitors to give with levodopa

A

Carbidopa and Benserazide

62
Q

Monoamine Oxidase Type B enzyme inhibitors (tx of Parkinson’s)

A

Selegiline

63
Q

Catechol-O-Methyltransferase Inhibitors and SE

parkinsons pharmacotherapy

A

Tolcapone: Hepatotoxicity and Rhabdomyolysis
Entacapone: orange urine

64
Q

synthetic dopamine agonists allow you to

A

reduce the dose of levodopa

65
Q

synthetic dopamine agonists SE:

A

Visual & auditory hallucinations, hypotension, dyskinesia
Erythromelalgia- red, edematous, tender extremities
Pulmonary fibrosis and effusions

66
Q

synthetic dopamine agonists (drug names)

A

Bromocriptine & Pergolide (tetracyclic ergot alkaloids)

Pramipexole, Ropinirole & Rotigotine (nonergot alkaloids)

67
Q

Amantadine

A

antiviral (prophylaxis influenza A)
MOA unknown
SE: anticholinergic, ankle edema, lived reticularis

68
Q

Doxapram use

A

temporary measure to maintain ventilation during administration of O2 to patients with COPD who are dependent on the hypoxic drive

69
Q

Doxapram function:

A

centrally active analeptic that selectively increases MV (by increasing TV) by activating the carotid bodies

70
Q

Doxapram and volatile anesthetics:

A

Arousal from the residual effects of inhaled anesthetics follows the administration of doxapram but the effects are transient, nonselective, & not recommended.

71
Q

SE of Doxapram/CNS stimulation:

A 
Hypertension
Tachycardia,
Cardiac dysrhythmias 
Vomiting
Increased body temperature
72
Q

Stimulation produced by Doxapram is similar to that produced by a PaO2 of ___ mm/Hg acting on the carotid bodies

73
Q

Methylxanthines (list of drugs)

A

Caffeine
Theophylline
Theobromine

74
Q

Methylxanthines clinical uses:

A

Primary apnea of prematurity by stimulating medullary respiratory centers by increasing the sensitivity of these centers to carbon dioxide

75
Q

Methylxanthines MOA:

A

Stimulate the CNS
Produce diuresis
Increase myocardial contractility
Relax smooth muscle, especially those in the airways

76
Q

Caffeine clinical uses

A

Neonates apnea of prematurity
Post-dural headache
Common cold

77
Q

Methylphenidate:

A

mild CNS stimulant related to amphetamine

used for tx of ADHD and narcolepsy

78
Q

Methylphenidate SE:

A

Hypertension, tachycardia, priapism, seizures, & serious cardiovascular events such as sudden cardiac death, stroke, & myocardial infarction have been described in patients treated with methylphenidate

79
Q

Baclofen is an agonist at the

A

GABA-B receptor

80
Q

How does Baclofen work?

A

centrally acting muscle relaxant
suppresses neuronal transmission in cerebral cortex
inhibits excitatory impulses at the spinal cord level

81
Q

What is baclofen used for?

A

to treat spastic movements in patients with cerebral palsy and spinal cord injuries
to treat central neuropathic pain

82
Q

How is baclofen excreted?

A

kidneys (80%)

83
Q

Baclofen SE:

A

sedation, confusion, skeletal muscle weakness

84
Q

Baclofen and General Anesthesia:

A

Brady, hypotension, delayed awakening

85
Q

Sudden withdraw from Baclofen:

A

multi-organ system failure, tachycardia, hallucinations

86
Q

Do you modify dose of baclofen in renal failure?

87
Q

Does baclofen work at neuromuscular junction?

88
Q

Cocaine as a CNS stimulant

A

inhibits NE and dopamine reuptake

89
Q

Cocaine has high abuse potential due to

A

euphoric effects caused by inhibition of catecholamine uptake, especially dopamine

90
Q

Chronic cocaine use leads to:

A

cardiomyopathy, HTN, MIs, aortic dissection, psychosis

91
Q

Chronic cocaine use and dopamine:

A

dopaminergic dysfunction due to dopamine depkletion

92
Q

How is cocaine metabolized?

A

plasma esterases

93
Q

cocaine and GA:

A

exaggerated cardiac stimulating effects

94
Q

How does cocaine affect O2 demand?

A

increases O2 demand

95
Q

Dantrolene MOA

A

binds to ryanodine calcium channel and reduces Ca efflux from the sarcoplasmic reticulum, counteracting the abnormal intracellular Ca levels accompanying MH

direct action on excitation-contraction coupling
decreases the amount of calcium released by sarcoplasmic reticulum

96
Q

Does dantrolene work at NMJ?

97
Q

T/F: Dantrolene produces skeletal muscle relaxation

98
Q

Dantrolene SE

A

liver dysfunction/hepatotoxicity

99
Q

Dantrolene Dose

A

2.5 mg/kg IV until symptoms subside

or cumulative dose of 10 mg/kg IV reached

Pharm Exam 4 (3 decks)

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