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Pharm > anticonvulsants 49/50 > Flashcards

anticonvulsants 49/50 Flashcards

1
Q

Phenobarbital (Luminal®)

A

anti epileptic drug: barbiturate, original, cheap, effective

tonic-clonic and partial seizures
potentiation of synaptic inhibition via GABAa receptor

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2
Q

Phenytoin (Dilantin®, Diphenylan®)

A

anti epileptic drug

monotherapy generalized tonic-clonic and partial seizures

Block of voltage gated sodium channels (promote inactive state)

zero-order kinetics

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3
Q

Carbamazepine (Tegretol®, Carbatrol®)

A

anti epileptic drug

Block of voltage gated Na+ channels (promote inactive state)

monotherapy generalized tonic-clonic and partial seizures (also used in manic-depressive patients)

self-induced metabolism, also, metabolism increased by pheonbarb/phenytoin

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4
Q

Ethosuximide (Zarontin®)

A

anti epileptic drug

mono therapy for absence seizures (altered Ca2+ channel function in thalamus)

Block of T-type calcium channels located on the postsynaptic membrane (thalamus)

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5
Q

Valproic acid (Depakote®, Depakene®)

A

anti epileptic drug

monotherapy, tx both absence and tonic-clonic seizures (ALL)

Block of voltage gated Na+ channels (promote inactive state)
AND
Block of T-type calcium channels located on the postsynaptic membrane

increases GABA synthesis

(off-label uses)

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6
Q

Fosphenytoin (Cerebyx®)

A

anti epileptic drug

water-soluble pro-drug of phenytoin used for treating status epileptics (given IV)

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7
Q

Gabapentin (Neurontin®)

A

Newer anti epileptic drug

GABA molecule bound to lipophillic hexane ring (crosses BBB)

DOES NOT actually interact with GABA receptor, but suppress neuronal activity
binds to L-type Ca channels

Adjunctive tx partial +/- genalized secondary seizures; but mostly used for neuropathic pain

**Not metabolized, excreted unchanged in urine (RFTs before tx)

SE: fatigue, ataxia

(similar drug: Pregabalin (Lyrica®))

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8
Q

Oxcarbazepine (Trileptal®)

A

Newer anti epileptic drug

Block of voltage gated Na+ channels (promote inactive state)

monotherapy/adjunctive treatment partial seizures

like carbamazepine, but does not auto induce, but still incr. metabolism of OCTs

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9
Q

Lamotrigine (Lamictal®)

A

Newer anti epileptic drug

Monotherapy and adjunctive treatment partial- and generalized tonic/clonic seizures; LGS. Considered a “broad spectrum” AED

prolong rate of recovery of voltage-gated Na+ channels from inactivation, inhibit Ca to lesser extent

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10
Q

Topiramate (Topomax®)

A

Newer anti epileptic drug

Monotherapy and adjunctive therapy for partial and tonic/clonic seizures, LGS. Considered a “broad spectrum” AED

Inhibit Na channels and AMPA-kainate receptors enhance GABA receptors

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11
Q

Levetiracetam (Keppra®)

A

Newer anti epileptic drug

Adjunctive treatment for partial- and tonic/clonic seizures in adults and myoclonic seizures in children; IV preparation for status epileptics

may prevent presynaptic glutamate release

highest safety margin
highest therapeutic index
3-D “printable” drug

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12
Q

simple partial seizure

A

single site within the cortex
preservation of consciousness, short duration 20 – 60 sec

focal motor (e.g. one side of face may twitch)
Jacksonian (“marching” seizure, e.g. muscle twitching “running” up the arm)
somatosensory (varied responses; smelling sulfur, crawling sensation on skin, narrowing of visual field)
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13
Q

complex partial seizure

A

single site within the cortex
gradual loss of consciousness, 30 sec – 2 min

may begin with simple seizure, hallucination, strong emotions followed by automatisms (lip smacking, hand wringing, etc)

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14
Q

EEG can determine ??

A

type of seizure

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15
Q

Of the ~10 electrodes placed on the head for an EEG:

if only 1-2 electrodes display synchronous activity during seizure, what type ??

all EEG electrodes will display synchronous activity during a ??

A

partial seizure

generalized seizure

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16
Q

if all EEG electrodes display synchronous activity during a seizure

A

generalized seizure

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17
Q

generalized seizure

A

simultaneously in both hemispheres of brain (40% of all seizures)

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18
Q

absence (generalized)

A

sudden loss of consciousness, less than 30 sec

staring and blinking (3/sec)
body may remain active
ADHD, impaired learning

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19
Q

tonic-clonic (grand mal, gen)

A

sudden loss of consciousness, 1.5 to 2.5 min

20 sec of muscle rigidity followed by 1 – 2 min of rhythmic muscle contractions (clonic)

injury when falling during tonic stage, loss of bowel control

20
Q

Phenobarbital (Luminal®) SEs

A

sedation, irritability/hyperactivity (kiddos), rash

*metabolized by CYP2C9, induction of CYP3A4–> inc. metabolism of OCTs and teratogenic

21
Q

anticonvulsant drug MOA

A

reduce neuronal activity

22
Q

drugs that enhance inhibitory effects of GABA

A

Barbs (Phenobarbital and primidone) and benzos (clonazepam, diazepam) increase GABA effects at GABAa

tiagabine: inhibit the re-uptake of GABA
vigabatrin: irreversible inhibitor of the GABA-degrading enzyme GABA transaminase

23
Q

monotherapy will sufficiently control seizures for

A

70% of epileptic pts

24
Q

original seizure tx

A

bromides

25
Q

barb less effective than phenobarbital

SEs??

A

primidone

dizziness, nausea, nystagmus, ataxia (dec. firing)

26
Q

Phenytoin SEs

A

gingival hyperplasia

SJS: only in first few months of tx

interact with warfarin and OCTs and may cause birth defects

27
Q

Carbamazepine SEs

A

Acute: stupor, coma, hyperirritability convulsions

Chronic: drowsiness, vertigo, ataxia, blurred vision. Induces CYP3A4 resulting in increased drug metabolism (e.g. oral contraceptives)

28
Q

benzos can be used for ??

A

adjunctive treatment only of absence seizures and juvenile myoclonic seizures

29
Q

newer AEDs

A

lack serious side effects (less SJS)

do not induce liver enzymes (fewer drug-drug interactions)

less efficacious

mostly approved for adjunctive treatment (combo tx)

30
Q

Lennox-Gustaut syndrome

A

Childhood-onset epilepsy

Severe cognitive dysfunction

Multiple seizure types including atonic or “drop” seizures (cause of injury)

Resistant to drug therapy (tx with Felbamate)

Mortality rates 3 – 7%

ketogenic diet

31
Q

partial seizure tx

(or secondarily
generalized)

A

carbamazepine
phenytoin

alternative: lamotrigine (broad-spec)
valproic acid

32
Q

generalized: absence seizure tx

A

Ethosuximide
Valproic acid*

alternative: Clonazepam

33
Q

generalized: tonic-clonic tx

A

Carbamazepine
Phenytoin
Valproic acid*

alternatives:
Lamotrigine*
Topiramate*

34
Q

Status Epilepticus

A

a series of seizures (any type) where full recovery from one seizure does not occur before onset of next seizure

20% mortality rate

35
Q

Status Epilepticus tx

A

lorazepam IV

IV fosphenytoin (Cerebyx®) (water soluble prodrug of phenytoin-which would irritate veins)

levetiracetam (alternative to fosphenytoin)

phenobarbital and valproic acid (Depacon®)

36
Q

long term use of AEDs may cause

A

osteoporosis:

altered vitamin D metabolism in the liver–>lower bone density

37
Q

AEDs: OCT interactions

safe for preggos??

specifically ??

most common offending drug ??

A

3X higher failure rate of the contraceptive

NO, 2 – 3 fold increase in birth defects

neural tube formation abnormalities resulting in facial and cranial deformities

phenytoin (all AEDs may cause similar birth defects)

38
Q

To reduce the likelihood of neural tube birth defects the patient should be given ???

A

folate (0.4 mg/day) throughout pregnancy

vitamin K (10 mg/day) during last month of gestation to help reduce newborn blood coagulation problems/Vit K deficiencies

39
Q

treating epilepsy with ??? is controversial

A

generic drugs, use brand names

40
Q

teratogenic AED

A

valproic acid

41
Q

for pregnant/soon to be pregnant pts…

A

do not discontinue tx (do not want break thru seizures)

but reduce to mono therapy and monitor drug plasma levels/seizure activity, lowest dose possible is desired

42
Q

ethosuximide SEs

A

Nausea, vomiting, anorexia
CNS drowsiness, lethargy, euphoria
SJS, aplastic anemia

43
Q

Valproic acid SEs

A

GI nausea, anorexia
CNS sedation, ataxia, tremor
Increase in hepatic blood enzymes (40%)
Hepatic toxicity in patients

44
Q

Lamotrigine SEs

A

dizziness, ataxia, blurred vision, nausea

Rash and SJS when used in addition to other AEDs

45
Q

Topiramate SEs

A

Ataxia, fatigue, somnolence, weight loss

Reduces plasma levels of estradiol and oral contraceptives

46
Q

Levetiracetam SEs

A

somnolence, dizziness, asthenia , no drug-drug interactions



Pharm (45 decks)

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