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INS > Drug therapy of epilepsy > Flashcards

Drug therapy of epilepsy Flashcards

1
Q

Simple partial seizure

A

focal, 20-60 sec, consciousness preserved

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2
Q

Complex partial seizure

A

focal, 30-120 sec, impaired consciousness

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3
Q

Partial seizures can become _____ and include tonic-clonic activity

A

secondarily generalized

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4
Q

Absence seizure

A

generalized, < 30 sec; loss of awareness, staring, unresponsiveness

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5
Q

Myoclonic seizure

A

generalized, ~ 1 sec single or multiple muscle spasms

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6
Q

Tonic-clonic seizure

A

generalized, 1-3 min; loss of consciousness, muscle rigidity followed by alternating periods of contraction and relaxation

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7
Q

Status epilepticus

A

continuous generalized convulsive activity

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8
Q

List four general strategies to inhibit neuronal activity in seizures

A
  1. Inhibit Na+ channels
  2. Inhibit Ca++ channels
  3. Potentiate the inhibitory effect of GABA ( Positive modulators of GABAA receptors, GABA uptake inhibitors, GABA-T inhibitors)
  4. Inhibit the excitatory effect of glutamate (NMDA receptor antagonists, AMPA/KA receptor antagonists)
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9
Q

All antiseizure drugs come with a black box warning for ______ regardless of indication

A

suicidal ideation

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10
Q

_______ is a barbiturate commonly used to treat epilepsy; _______ is a barbiturate used for rapid induction of anesthesia

A

Phenobarbital

Thiopental

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11
Q

Unlike benzodiazepines, barbiturates can produce ______ and depress ____

A

surgical anesthesia, depress respiratory rate and rhythm

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12
Q

Barbiturates are classic CYP ____

A

inducers- leads to tolerance, drug interactions

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13
Q

List common adverse reactions to barbiturates

A

Depress REM sleep
Rebound insomnia, anxiety, seizures
Paradoxical excitement in children and elderly patients
Can worsen pain perception- not to be used for analgesia
Allergic skin reactions
Pregnancy Risk D
Blood dyscrasias

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14
Q

Phenobarbital is generally effective in all seizures except ____

A

absence

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15
Q

Describe the mechanism of action of phenobarbital

A

Main site of action is the GABAA receptor; increases the duration of GABA-induced Cl- channel openings; inhibits the spread of seizure activity and ↑ the threshold for stimulation of the motor cortex

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16
Q

List side effects of phenobarbital

A

CNS, pulmonary depression, bronchospasm, rash/ derm

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17
Q

Phenytoin is used for what kinds of seizures?

A

prophylaxis of complex partial seizures and generalized tonic-clonic seizures

18
Q

______ is a prodrug of phenytoin used IM/ IV for _______

A

Fosphenytoin, for status epilepticus

19
Q

Describe the mechanism of action of phenytoin

A

Main effect is preferential binding to the inactivated state of voltage-activated Na+ channels (use-dependent block); inhibits sustained repetitive neuronal firing
Also decreases the release of glutamate and enhances release of GABA through actions at other ion channels (T-type Ca++ channels, K+ channels)

20
Q

Phenytoin has NO effect on _________

A

seizure threshold

21
Q

Because of variable hepatic metabolism, ______ is one of few drugs for which metabolic capacity can be saturated within therapeutic concentrations leading to ________ kinetics

A

Phenytoin

zero order

22
Q

Gingival hyperplasia is a side effect that is somewhat unique to _______

A

Phenytoin

23
Q

_______ is a drug used for partial seizures and tonic clonic seizures that is preferred over phenobarbital in children because it has fewer behavioral/ alertness side effects

A

Carbamazepine

24
Q

Describe the mechanism of action of carbamazepine

A

use-dependent block of voltage-activated Na+ channels; inhibits sustained repetitive neuronal firing

25
Q

Carbamazepine has some adverse reactions that are not seen with other anti-epilepsy drugs:

A 
CV changes
(also does have CNS, heme, GI, derm side effects common to anti-epilepsy drugs)
26
Q

Metabolism of _______ can be affected by the HLA-B*1502 allele, which is common in _____ populations

A

carbamazepine

South Asian

27
Q

Describe the mechanism of action of valproic acid

A

Several sites of action:
1) prolongs Na+ channel inactivation,

2) inhibits T-type Ca++ channels in thalamic relay neurons,
3) increases brain concentrations of GABA by a) stimulating glutamate decarboxylase (converts glutamate to GABA) and b) inhibiting enzymes (GABA-T, SSA-DH) that metabolize GABA

28
Q

_______ is effective for all types of seizures and is also used in acute mania, bipolar disorder, migraine prophylaxis

A

Valproic acid

29
Q

Valproic acid ______ CYPs and UGT

A

inhibits

other drugs are CYP inducers

30
Q

The DOC for absence seizures is ______ but this drug should not be used as monotherapy for mixed epilepsy because ______________

A

ethosuximide

increases frequency of tonic-clonic seizures

31
Q

_______ and ________ are GABA analogs that do not bind to GABA receptors but do increase brain GABA concentration

A

Gabapentin, pregabalin

32
Q

List uses of gabapentin

A

adjunctive therapy for partial seizures
TX of painful neuropathies
monotherapy for refractory partial seizures, TX of spasticity in MS, and TX of tremor

33
Q

Describe the mechanism of action of gabapentin (and pregabalin)

A

Binds N-type Ca++ channels, decreasing Ca++ entry during action potentials, and resulting in decreased synaptic release of neurotransmitters, including glutamate

34
Q

List adverse reactions to gabapentin

A

drowsiness, dizziness, ataxia, fatigue, nystagmus, tremor, xerostomia, gingivitis, gingival hemorrhage, dyspepsia, constipation

35
Q

List adverse reactions to pregabalin

A

dizziness, somnolence, ataxia, xerostomia, peripheral edema

36
Q

List precautions for treatment with pregabalin

A

taper to DC
adjust dose for renal insufficiency
angioedema

37
Q

Describe treatment options for partial and tonic-clonic seizures

A

DOC: valproic acid, carbamazepine, phenytoin
Alternates: phenobarbital, lamotrigine, topiramate
Adjuncts: gabapentin, pregabalin, vigabatrin, tiagabine, zonisamide

38
Q

Describe treatment options for absence seizures

A

DOC: ethosuximide, valproic acid
Alternates: clonazepam

39
Q

Describe treatment options for myoclonic seizures

A

DOC: valproic acid
Alternates: clonazepam, lamotrigine
Adjuncts: felbamate

40
Q

Describe treatment options for status epilepticus

A

DOC: IV lorazepam, IV diazepam, IV fosphenytoin
Alternates: phenobarbital, general anesthetics

INS (21 decks)

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