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Pharmacology 2 > Anticonvulsants > Flashcards

Anticonvulsants Flashcards

5 questions

1
Q

the clinical manifestation of an abnormal and excessive excitation of a population of neurons

A

seizure

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2
Q

a tendency toward recurrent seizures unprovoked by systemic or neurologic insults

A

epilepsy

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3
Q

occurs with an aura, epileptic cry, loss of consciousness and postural tone, tonic spasm of entire body, synchronous clonic movements, followed by confusion and sleep

A

tonic-clonic (grand mal)

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4
Q

brief loss of consciousness (5-10 secs), with local or widespread clonic movements (minor muscle twitching without loss of postural tone)

A

petit mal (absence)

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5
Q

in which patients do petit mal (absence) occur?

A

children

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6
Q

continuous or repeated attacks, can be grand mal or petit mal

A

status epilepticus

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7
Q

in which 2 acute disorders affecting the brain can status epilepticus occur in?

A

meningitis
encephalitis

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8
Q

individual remains conscious, is limited to certain muscles, specific sensory changes, and autonomic activity; may remain localized or may spread causing progressive symptoms

A

simple partial seizure

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9
Q

which seizure type is associated with Jacksonian Epilepsy?

A

simple partial seizure

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10
Q

impaired consciousness, usually originate in temporal or frontal lobes but spread to broader areas; cause flashbacks and stereotypes movements like chewing

A

complex partial seizures

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11
Q

what does treatment of a partial seizure evolving to a generalized seizure depend on?

A

type of generalized seizure that is triggered

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12
Q

what is more refractory to drug treatment than the common generalized seizures?

A

partial evolving to generalized

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13
Q

what is the pathophysiology of most seizures?

A

unknown etiology

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14
Q

what do antiepileptic drugs treat?

A

symptom of seizure
NOT underlying epileptic condition

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15
Q

what is the goal of antiepileptic drugs?

A

maximize QOL by minimizing seizures and ADRs

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16
Q

which 3 anticonvulsants decrease the excitability of the focus?

A

phenobarbital
primidone
ethosuximide

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17
Q

which 4 anticonvulsants prevent the spread of nervous activity?

A

phenytoin
phenobarbital
carbamazepine
valproate

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18
Q

which 4 anticonvulsants enhance inhibitory mechanisms?

A

phenobarbital
primidone
valproate
benzodiazepines

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19
Q

all anticonvulsants are specific for seizure type, except which one that is used for all types of seizures?

A

valproic acid

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20
Q

what are many anticonvulsants used for?

A

neuropathic pain

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21
Q

very painful, sharp electric-like spasms that usually last a few seconds-mins but can become constant

A

trigeminal neuralgia

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22
Q

what activities can trigger trigeminal neuralgia? (5)

A

brushing teeth
chewing
drinking/eating
lightly touching face
shaving

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23
Q

what is a risk factor for trigeminal neuralgia?

A

age (after 40)

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24
Q

what is the major cause of trigeminal neuralgia?

A

demyelination of the axons of the trigeminal nerve

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25
Q

what are 2 other uses of anticonvulsants?

A

diabetic pain
bipolar disorder

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26
Q

sedation can occur at therapeutic doses of anticonvulsants, except in these meds: (2)

A

phenytoin
valproic acid

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27
Q

why are there potential drug interactions with anticonvulsants?

A

highly protein bound

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28
Q

why do some anticonvulsants reduce antibiotic efficacy?

A

some induce hepatic enzymes

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29
Q

which 2 drug types decrease anticonvulsant absorption?

A

antacids
antihistamines

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30
Q

the first drug developed specifically to treat seizures and is non-sedating

A

phenytoin

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31
Q

what is the drug of choice for generalized tonic-clonic seizures?

A

phenytoin

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32
Q

what are the 4 uses for phenytoin?

A

generalized tonic-clonic seizures
partial seizures
status epilepticus
trigeminal neuralgia

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33
Q

phenytoin is used as a backup treatment for _____

A

trigeminal neuralgia

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34
Q

drug that inhibits reactivation of Na channel and prevents post tetanic potentiation

A

phenytoin

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35
Q

what increases the effectiveness of phenytoin in its MOA?

A

high extracellular K

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36
Q

what does phenytoin do at greater than therapeutic concentrations?

A

interferes with Ca channel and neurotransmitter release

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37
Q

what is special about phenytoin’s elimination?

A

has zero order kinetics at high doses (small increment of dose leads to toxicity)

38
Q

what is the highest protein-bound anticonvulsant?

A

phenytoin (90%)

39
Q

a patient taking phenytoin is experiencing nystagmus, diplopia, thought disorders and sedation. what is their plasma level?

A

20

40
Q

a patient taking phenytoin is experiencing loss of consciousness, confusion, and hyperactivity. what is their plasma level?

A

30

41
Q

a patient is taking phenytoin is experiencing lethargy, stupor, and coma. what is their plasms level?

A

40

42
Q

what are the ADRs of phenytoin?

A

P450 inducer
Hirsutism
Enlarged gums

Teratogenic
Osteomalacia
Intereferes with B12 = megaloblastic anemia

43
Q

what can be used to treat blood dyscrasias side effects of phenytoin?

A

folate

44
Q

what can be used to prevent osteomalacia side effect of phenytoin?

A

vitamin D supplements

45
Q

what is the drug of choice for trigeminal neuralgia?

A

carbamazepine

46
Q

what are the 3 uses for carbamazepine?

A

trigeminal neuralgia
generalized tonic-clonic seizures
partial seizures

47
Q

drug that inhibits high frequency neuronal firing, inhibits reactivation of Na channels, and inhibits Ca influx

A

carbamazepine

48
Q

what is the half-life of cabamazepine?

A

10-20 hours

49
Q

what are the 5 ADRs of Carbamazepine? PATCH

A

Parkinsonism (involuntary movement)
Aplastic anemia / Agranulocytosis
Teratogenic / Taste disorder
Convulsions / CNS (dizziness, slurred speech, ataxia)
Headache

50
Q

a patient presents with dizziness, diplopia, drowsiness, ataxia, and slurred speech. what are they experiencing?

A

carbamazepine overdose

51
Q

one of the oldest, most effective and least toxic anticonvulsants that is the drug of choice for seizures in infants; particularly febrile

A

phenobarbital

52
Q

what are the 3 uses for phenobarbital?

A

febrile seizure in infants
generalized tonic-clonic
partial seizures

53
Q

drug class that enhances the binding to GABAa receptors, increasing Cl channel openings, which inhibits Ca currents, leading to decreased excitability

A

barbituates

phenobarbital
primidone

54
Q

what is the half life of phenobarbital?

A

50-140 hours

55
Q

what inactivates phenobarbital?

A

liver enzymes

56
Q

phenobarbital decreases the efficacy of what drugs?

A

tetracycline + other antibiotics

57
Q

how can we measure the plasma concentration of phenobarbital and other antiepileptics?

A

saliva

58
Q

what are the 2 uses for primidone?

A

generalized tonic-clonic seizures
complex partial seizures

59
Q

what is the difference between primidone and phenobarbital in their PK?

A

primidone is completely absorbed after oral administration

60
Q

what is the half life of primidone?

A

5-15 hours

61
Q

what are the 5 ADR of phenobarbital and primidone (barbituates)?

A

sedation
depressed cardio/pulm
hepatotoxicity
megaloblastic anemia
osteomalacia

62
Q

phenobarbital is not teratogenic, but enhances teratogenicity of ______when combined

A

phenytoin

63
Q

what are 2 ADR specific to primidone?

A

acute toxicity
acute psychosis in complex partial seizures

64
Q

what is the drug of choice for absence seizures?

A

ethosuximide

65
Q

which drug inhibits Ca channels through T-type Ca channels = reducing oscillatory behavior of thalamic neurons?

A

ethosuximide

66
Q

how can plasma concentration of ethosuximide be measured?

A

saliva

67
Q

what are the 4 ADR of ethosuximide?

A

Gi distress
CNS depression (transient)
bone marrow depression
blood dyscrasias

68
Q

what is the preferred drug in pregnancy?

A

ethosuximide

69
Q

which drug prolongs the activation of Na channel, leading to decreased repetitive neuronal firing, inhibits T-type Ca channels, and increases GABA levels at higher than therapeutic doses?

A

valproic acid

70
Q

what are the 5 uses for valproic acid?

A

absence seizures
tonic-clonic seizures
myoclonic seizures
partial seizures
neuropathic pain

71
Q

what is the half-life of valproic acid?

A

10-15 hours

72
Q

how is valproic acid excreted?

A

in urine

73
Q

what are the 4 ADR of valproic acid? HATS

A

Hepatotoxicity
Abdominal (GI) distress
Teratogenic
Sedation

74
Q

which drug class enhances the binding of GABA to GABAa receptors, increasing the frequency of opening GABA Cl channels? and at higher concentrations, act on Na channels like phenytoin and carbamazepine?

A

benzodiazepines

clonazepam
clorazepate
diazepam
lorazepam

75
Q

what are the 2 uses for clonazepam?

A

“the clone makes the myoclonic absent”
absence seizures
myoclonic seizures

76
Q

what is the use for clorazepate?

A

“the lor is only partially correct”
partial seizures

77
Q

which 2 benzodiazepines can treat status epilepticus?

A

diazepam
lorazepam

78
Q

the major metabolite of clorazepate and diazepam that has anticonvulsant activity

A

desmethyldiazepam

79
Q

what are 2 ADR of benzodiazepines?

A

tolerance w/ 1-6 mo of treatment
hyperactivity in children

80
Q

which drug binds to voltage dependent Ca channels, and has a GABA analogue but does not interact with GABA receptors?

A

gabapentin

81
Q

what are the 3 uses of gabapentin?

A

partial seizures
trigeminal neuralgia
neuropathic pain

82
Q

how is gabapentin excreted?

A

renal, unchanged

83
Q

what are the 2 uses for lamotrigine?

A

partial seizures
bi-polar depression

84
Q

MOA of lamotrigine?

A

acts on Na channels

85
Q

what is the ADR of lamotrigine?

A

“lamotrigine is a lamo and causes SJS”
stevens-johnson syndrome; severe skin rash

86
Q

what drug reduces lamotrigine half life from 24 to 12 hours? why?

A

carbamazepine

induces liver enzymes

87
Q

which drug increases lamotrigine half life up to 60 hours?

A

valproate

88
Q

what is the use for felbamate?

A

partial seizures

89
Q

what is the major ADR of felbamate? what did that lead to?

A

aplastic anemia
bone marrow transplants

90
Q

which drug is only approved for restricted use?

A

felbamate

Pharmacology 2 (22 decks)

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