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Pathopharm Exam 3 > Module 7: Part 3 > Flashcards

Module 7: Part 3 Flashcards

1
Q

What effects do antileptics have on GABA system

A

GABA metabolism
enhancing Cl- influx in response to GABA activation
and influence of GABA release

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2
Q

Effective in TX of gen. tonic-clonic sz’s and partial sz’s
a. Phenobarbital
b. Ethosuximide
c. Clonazepam

A

a. Phenobarbital

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3
Q

antileptic drugs that interact w/GABA (4)

A

Valproate, Gabapentin, Barbiturates, Benzodiazepines

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4
Q

Most widely used antiepileptic bec. of its efficacy, low toxicity and low cost
a) Primidone
b) Phenobarbital
c) Carbamazepine

A

b. Phenobarbital

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5
Q

How is phenobarbital metabolized?
a) mostly conjugated (glucuronidation)
b) only by hepatic microsomal system
c) hepatic microsomal system, but 25% is eliminated unchanged by kidney

A

C. hepatic microsomal system, but about 25% is eliminated unchanged (pH dependent) by kidney

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6
Q

What is Phenobarbital’s MOA for sedation?
a) Ca++ channel inhibition
b) ↑ synaptic inhibition by action on GABA-A receptors
c) inhibits voltage gated Na+ and Ca++ channels

A

b. ↑ synaptic inhibition by action on GABA-A receptors

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7
Q

What is Phenobarbital’s anticonvulsant MOA?

a) Ca++ channel inhibition which ↓ excitatory transmitter release
b) inhibition by action on GABAA receptors
c) None of these are correct

A

a. Ca++ channel inhibition which ↓ excitatory transmitter release

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8
Q

Primidone’s antiseizure efficacy is due both to (SATA)

a) the drug itself
b) increase in Cl- conductance
c) active metabolites
d) inactive metabolites

A

a. the drug itself
c. active metabolites

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9
Q

Metabolized to 2 active metabolites, phenobarbital and phenylethylmalonamide (PEMA)

A

Primidone (Mysoline)

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10
Q

(SATA) Primidone (Mysoline) characteristics

a) well absorbed w/po admin.
b) slightly bound to plasma proteins
c) highly bound to plasma proteins
d) not well absorbed w/po admin
e) has 2 active metabolites
f) 40% of the drug is excreted unchanged

A

a. well absorbed w/po admin.
b. slightly bound to plasma proteins
e. has 2 active metabolites *phenobarbital and phenylethylmalonamide (PEMA)
f. 40% of the drug is excreted unchanged

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11
Q

Used for TX of trigeminal (tic douloureux) and glossopharyngeal neuralgias

a) Oxcarbazepine (Trileptal)
b) Carbamazepine (Tegretol)
c) Ethosuximide (Zarontin)
d) None of these are correct

A

Carbamazepine (Tegretol)

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12
Q

Used to manage pain assoc. w/ MS

a) Primidone (Mysoline)
b) Oxcarbazepine (Trileptal)
c) Ativan
d) None of these are correct

A

d. None of these are correct

correct answer = Carbamazepine (Tegretol) helps manage Multiple Sclerosis pain

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13
Q

T/F
Carbamazepine (Tegretol) is r/t phenobarbital

A

False
Carbamazepine (Tegretol) is related to phenytoin

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14
Q

Carbamazepine (Tegretol)
metabolism

A

Hepatic

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15
Q

Carbamazepine is useful in TX of

a) depression
b) manic-depressive affective d/o
c) schizophrenia

A

b. manic-depressive affective d/o

*(even in lithium carbonate resistant disease)

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16
Q

T/F
Oxcarbazepine is converted to an inactive metabolite (10-hydroxycarbazepine) that is equipotent to carbamazepine

A

False

Oxcarbazepine converted to INACTIVE metabolite (10-hydroxycarbazepine) that is equipotent to carbamazepine

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17
Q

Has anticholinergic activity & may act synergistically with NMB’s

A

Oxcarbazepine (Trileptal)

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18
Q

T/F
Oxcarbazepine is a teratogenic but doesn’t dec. effectiveness of oral contraceptives

A

False

Oxcarbazepine is a teratogenic and DOES decrease effectiveness of oral contraceptives

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19
Q

fewer SE’s that carbamazepine

A

Oxcarbazepine (Trileptal)

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20
Q

T/F
Oxcarbazepine (Trileptal) has no microsomal enzyme induction

A

True

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21
Q

Oxcarbazepine (Trileptal) is used to tx

a) epilepsy, mood disorders, anxiety
b) epilepsy and schizophrenia
c) epilepsy only
d) none of these are correct

A

a. epilepsy, mood disorders, anxiety

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22
Q

T/F
Ethosuximide (Zarontin) is a central agent in TX of partial sz’s

A

False
central agent in treating absence seizures

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23
Q

T/F
More effective in mgmt of absence sz’s than trimethadione w/fewer serious S/E

A

True

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24
Q

Ethosuximide (Zarontin)
metabolism and how much is excreted unchanged?

A

metabolized by the liver microsomal system
about 25% is excreted unchanged

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25
Q

Lamotrigine (Lamictal) can not be combined with other drugs to TX gen sz, BP and depression d/t risk of aplastic anemia

A

False

used alone or in combo to TX partial and gen sz’s, bipolar disorder and depression

*aplastic anemia a/w Carbamazepine

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26
Q

Lamotrigine SE’s include

a) ataxia, headaches, rash and joint pain (Stevens-Johnson syndrome)
b) ataxia, headaches, joint pain
c) anxiety, CNS depression and hallucinations

A

a. ataxia, headaches, rash and joint pain (Stevens-Johnson syndrome)

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27
Q

T/F
Lamotrigine’s exact mechanism is clear and acts in part as a Na+ channel agonist decreasing the release of aspartate and glutamate

A

False
Lamotrigine’s exact mechanism UNclear but acts in part as a sodium channel ANtagonist decreasing the release or aspartate and glutamate

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28
Q

How is Lamotrigine (Lamictal)
metabolized

A

metabolized to large extent in liver & hepatic enzyme inducers (ie – phenobarbital, phenytoin, etc) decrease its half-life

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29
Q

Levetiracetam (Keppra) is used to TX

a) partial sz’s in adults only
b) partial sz’s in adults and neuropathic pain
c) gen. sz’s
d) gen. sz’s and neuropathic pain

A

b. partial sz’s in adults and neuropathic pain

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30
Q

T/F
Keppra has high protein binding and moderate liver metabolism

A

False
Keppra has no liver metabolism or protein binding

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31
Q

Levetiracetam (Keppra) S/E (6)

A

headache
anxiety
CNS depression
and initial sedation, depression and hallucinations

*all S/E mostly minor per ppt

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31
Q

Levetiracetam (Keppra) has

a) no major interactions w/other antiepileptics but ineffective when combined with other agents
b) some interactions w/other antiepileptics - useful for mono- or adjunctive therapy
c) no major interactions w/other antiepileptics - useful for mono- or adjunctive therapy
d) None of these are correct

A

c. no major interactions w/other antiepileptics - useful for mono- or adjunctive therapy

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32
Q

Levetiracetam (Keppra) MOA

A

exact mech. unclear but seems to bind to synaptic vesicles decreasing release of neurotransmitters

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33
Q

T/F
Status epilepticus is a medical emergency where pt experiences prolonged/rapidly recurring convulsions for 3 min. or more

A

False

5 min or more

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34
Q

Best Drug therapy for status epilepticus is

a) Diazepam
b) Lorazepam
c) Keppra
d) Fosphenytoin

A

a. Diazepam

  • Lorazepam and Fosphenytoin are also used to TX status epi. but Diazepam is best first choice
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35
Q

Benzo used for status epilepticus and other seizures

A

Lorazepam (Ativan)

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36
Q

T/F
Lorazepam (Ativan) is first choice for TX of status epilepticus

A

False

Diazepam is 1st choice

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37
Q

T/F
Benzo’s like Diazepam & Lorazepam act by interaction w/GABA-B to inc. duration of GABA binding & ↑Cl flux –> hyperpolarization

A

False
act by interaction of GABA- A

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38
Q

Benzo’s: low or high toxicity?

A

low

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39
Q

anesthesia adjuvant for its CNS sedative, muscle relaxant, anxiolytic, & amnesic effects

A

Benzodiazepines

40
Q

T/F
Clonazepam (Klonopin) is useful in TX of myoclonic and absence sz’s in adults only

A

False
Useful in TX of myoclonic sz’s in children and absence sz’s

41
Q

Clonazepam is also used in combo w/other drugs to TX (3)

A

akinetic seizures
absence seizures refractory to succinimides or valproic acid (Depakene)
infantile spasms

42
Q

T/F
Clonazepam is used to TX absence sz’s refractory to succinonitrile or valproic acid

A

False
absence seizures refractory to succinimides or valproic acid

43
Q

Useful for TX of infantile sz’s

A

Clonazepam (Klonopin)

44
Q

T/F
Clonazepam is generally added to other RX therapy and used as first-line drug only for myoclonic seizures

A

True

*from stoelting’s

45
Q

Clonazepam (Klonopin) MOA for anti-sz activity

A

benzo-mediated enhancement of GABA-induced inc. in Cl- conductance & enhances hyperpolarization

46
Q

T/F
benzo binding site is not part of the GABAA receptor

A

False

benzo binding site is part of the the GABA-A receptor

47
Q

Clonazepam has

a) inactive metabolites
b) active metabolites
c) your mom’s metabolites
d) a combo of active and inactive metabolites

A

a. inactive metabolites

48
Q

Generalized sz activity may be precipitated if this drug is DC’ed abruptly

A

Clonazepam (Klonopin)

*from Stoelting’s

49
Q

Clonazepam (Klonopin) metabolized by

A

liver

50
Q

T/F
Phenytoin is effective in TX of partial, tonic-clonic sz’s & absence seizures

A

False

Phenytoin is effective in treating all types of partial and tonic-clonic seizures but NOT absence seizures

51
Q

Types of sz’s phenytoin treats

A

partial and tonic-clonic seizures but NOT absence seizures

52
Q

T/F
partial and tonic-clonic seizures but NOT absence seizures1st line TX for absence sz’s

A

False

phenytoin doesn’t TX absence sz’s

53
Q

Phenytoin is metabolized by

A

hepatic microsomal system

53
Q

T/F
Phenytoin is one of the most widely used agents

A

True

54
Q

a Phenytoin prodrug injectable for status epilepticus (5 day max use)

A

Fosphenytoin (Cerebyx)

(5 day max use, only if Phenytoin not usable)

55
Q

T/F
Fosphenytoin is a lipid soluble, phenytoin prodrug injectable used for status epilepticus

A

False
Its water soluble

56
Q

Metabolized to formic acid

A

Fosphenytoin (Cerebyx)
*metabolized to formic acid (small amounts which are slowly eliminated)

57
Q

Effective in TX of partial, generalized and absence sz’s

a) Valproic Acid
b) Carbamazepine
c) Ethosuximide

A

a. Valproic Acid

*Carbamazepine: gen sz, simple & complex partial
*Ethosuximide: absence sz only

58
Q

Valproic Acid (Depakote) MOA

A

probably d/t an ↑ recovery time of voltage activated Na+ channels

59
Q

Is Valproic Acid well absorbed w/po admin?

A

Yes

60
Q

Valproic is (extensively/slightly) protein bound and (extensively/slightly) metabolized–mostly conjugated (glucuronidation).

A

extensively
extensively

61
Q

other uses of Zonisamide besides sz’s (3)

A

obesity, migraines and Parkinson’s disease

62
Q

acts at GABAA receptor to enhance GABA binding and blocks voltage-gated T-type Ca++ channels

A

Zonisamide (Zonegran)

63
Q

Zonisamide S/E’s (4)

A

loss of appetite
anhidrosis
drowsiness
occasional metabolic acidosis (can be severe)

64
Q

T/F
Zonisamide can occasionally cause only mild metabolic acidosis

A

False

Can cause occasional metabolic acidosis but it can be severe

65
Q

Zonisamide metabolism inhibited by

a) ketoconazole & carbamazepine
b) ketoconazole only
c) ketoconazole & carbimazole

A

a. ketoconazole & carbamazepine

66
Q

adjunct for partial seizures, anxiety disorders (panic attacks), and neuropathic pain

A

Tiagabine (Gabitril)

67
Q

How does Tiagabine inhibit GABA neuronal uptake

A

increases the duration of GABA interaction at receptor zone, thus increasing neuronal inhibition

68
Q

T/F
Tiagabine is highly protein bound and uses hepatic enzyme induction

A

False
no hepatic enzyme induction

69
Q

Tiagabine (Gabitril) major S/E’s (2)

A

confusion and CNS depression without euphoria of benzo’s

70
Q

T/F
Tiagabine S/E of CNS depression is worsened by severe euphoria

A

False

No euphoria w/ CNS depression

71
Q

Tiagabine can trigger sz’s in

a) epileptics
b) non-epileptics
c) children only

A

b. non-epileptics

72
Q

Topiramate treats what type of sz’s? (3)

A

partial
generalized
absence seizures

73
Q

Other uses for Topiramate (besides antiepileptic)

A) bulimia, cluster HAs, tremors
B) bulimia, migraine HAs, ataxia
C) bulimia, migraine HAs, tremors

A

C) bulimia, migraine HAs, tremors

74
Q

structurally a monosaccharide r/t fructose

A

Topiramate (Topamax)

75
Q

Topiramate (Topamax) MoA

A

Inhibits voltage-gated Na+ channels.
Inhibits voltage-gated Ca++ channels.
Enhances GABAA Cl- ion flux
Inhibits glutamate-induced neuronal excitation

76
Q

what effect does Topiramate have on protein binding and hepatic enzymes?

A

little effect on protein binding or hepatic enzymes

77
Q

Major S/E of Topiramate

A

development of kidney stones

78
Q

T/F
Antiepileptic Drug sedative effects maintain a steady state over time

A

False

effects diminish over time

79
Q

T/F
Most antiseizure medications tend to be sedating, without drowsiness

A

False

Most antiseizure medications tend to be sedating, with drowsiness observed

80
Q

other common S/E of antiepileptics are _____ related

A

GI tract

81
Q

Serious adverse effects of Primidone and Phenobarbital (6)

A

rash
leukopenia
thrombocytopenia
lupus
megaloblastic anemia
Osteomalacia

82
Q

Primidone and Phenobarbital S/E’s (8)

A

Sedation
Vertigo
n/v
ataxia
nystagmus
diplopia
feeling of intoxication immediately after ingestion

83
Q

What med causes Hypoprothrombinemia w/hemorrhage in newborns of primidone-treated mothers? What is the treatment?

A

Primidone & Phenobarbital
Vitamin K is effective for treatment or prophylaxis

84
Q

Carbamazepine (Tegretol)
long term S/E’s (3)

A

drowsiness, vertigo, blurred vision

85
Q

causes serious hematological toxicity: aplastic anemia, agranulocytosis

A

Carbamazepine (Tegretol)

86
Q

Carbamazepine acute intoxication S/S (5)

A

stupor
coma
hyperirritability
convulsions
respiratory depression

87
Q

Can cause hiccups

A

Ethosuximide (Zarontin)

88
Q

Ethosuximide GI S/E’s (4)

A

G.I. upset
including n/v
anorexia

89
Q

Ethosuximide (Zarontin) CNS S/E’s (4)

A

drowsiness, euphoria, headache and hiccups

90
Q

t/F
Pt’s taking Ethosuximide can develop tolerance to S/E’s

A

True

91
Q

Ethosuximide hematological disturbances (4)

A

leukopenia, thrombocytopenia and aplastic anemia
*Bone marrow depression may be fatal, although very rare.

92
Q

Ethosuximide skin rxn’s (2)

A

Stevens-Johnson syndrome and exfoliative dermatitis

93
Q

most common S/E w/long-term clonazepam use is (2)

A

lethargy and drowsiness
*tend to diminish over time

94
Q

S/E’s with IV admin of Clonazepam & Diazepam (4)

A

dysarthria, dizziness, hypotonia, respiratory depression

95
Q

IV admin of Clonazepam & Diazepam S/E more likely to occur if

A

other antiseizure meds or other CNS depressants have been previously given

96
Q
A

Pathopharm Exam 3 (18 decks)

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