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Pharm III: Exam 1 > Anti-Epileptics > Flashcards

Anti-Epileptics Flashcards

(41 cards)

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1
Q

Definitions
seizure
epilepsy
status epilepticus

A

Seizure
- abnormal neruonal firing in the cortex: physical or sensory manifestation
- an acute neurological event
- diferent types, severity, apperance based on location of firing
- a seizure does NOT = epiliepsy dx.

Epilepsy
- the occurance of 2+ seizures separated by at LEASE 24 hours
- a chronic, recurring disorder with an underlying process

Status Epilepticus
- any seziure last > 5 minutes : this is when neuronal damange can occur
- or any 2 seizures happening without complete recovery or consciousness/recovery of first seizure between

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2
Q

How do you select the proper drug for seizure management

A
  1. identify the underlying cause of the seizure: if its due to hypoglycemia: give dextrose!
  2. type of seizure (tonic-clonic, absence, etc.) guides
  3. MOA of drug: if on multiple: want different MOAs
  4. ADE: of the meds can guide therapy
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3
Q

what are some medications that can worsen seizure
the common ones
& ones to be aware of

A

Common meds to cause/worsen seizures
- meperidine (opioid)
- flumazemil (benzo reversal agent)
- contrast dyes!!
- vaccines
- phenothiazines (anti-psychotics)

Imipenem = can reduce seizure threshold
buproprion = can lower seizure threshold
withdrawl from benzos, alcohol and opioids can worsen seizures

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4
Q

MOA: Sodium channel antagonism

A

MOA
- these AED’s will antagonize the sodium channels: prolonging the inactivity and ability for the Na+ channels to open
- this then reduces the ability of a neuron to fire = decreasing excitabilty and propagation of APs

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5
Q

MOA: Calcium Channel Modulators

A

MOA
- these drugs antagonize the calcium channel (N-type)
- they prevent the channels from releasing Ca+
- if Ca+ cannot be releasd: then there is no ability for the vesicel full of glutamate to fuse to the cleft and release into the synapse
- without the release of glutamate: there can be no excitatory potentiation down the cleft: no depolarizaiton

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6
Q

MOA: drugs that act on GABA

A

GABA: an inhibitory NT

some drugs = enhance GABA: thus inhibiting the ability for an AP to occur, decrease excitability
some drugs = inhibit GABA-transaminase: thus inhibiting the breakdown of GABA: leading to more

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7
Q

what AED (anti-epileptic drugs) can be used for an Absence seizure

A

EL VZ!!

E: ethosuximide (can ONLY be used for absence seizures)
L: Lamotrigine
V: Valproate
Z: Zonisamide

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8
Q

what AED’s must be AVOIDED in myoclonic and absence seizures

A

AVOID the following for absence and myoclonic seizures
- carbamazepine
- oxcarbmazepine
- gabapentin
- tiagabine
- pregabalin

these will all exacerbate the seizure

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9
Q

role of benzodiazepines in seizure control
what is used for status epi. vs. what is used for add-on

A

Reserved for Status Epi.
- Lorazepam
- midazolam
- diazepam

Used for Add-on to gain control with AED
- clonazepam
- clobazam

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10
Q

Benzodiazepines
MOA
Indications (seizure and other)

A

Benzodiazepines: MOA
- bind to post-synaptic GABA A receptors: increase the inhibition that GABA gives

Indications
- Benzos are first line in status epilepticus (lorazepam, midazalam, diazepam)
- can be used for focal or general seizures (clonazepam, clobazam)
- can be used to control Lennox-Gastuat (a seizure syndrome)

Additional Indications
- anxiety, insomnia, ICU sedation, alcohol withdrawl, etc.

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11
Q

Benzodiazepines
side effects
monitoring
Drug interactions

A

Side Effects/ADR
- respiratory depression : in status epi. youll intubate because you’re giving in such high doses
- drowsiness
- ataxia
- hypotension: dose-related, propylene glycol can be given with lorazepam and diazepam to help decrease this effect
- watch for withdrawal symptoms upon abrupt discontinuation: taper off

Monitoring
- watch RR: work of breathing, O2 status
- mental stauts & neuro exam
- BP! wathc for hypotension

Drug Interactions
- no monitoring needed
- watch interactions with otehr CNS depressants (opioids, alcohol,etc.)

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12
Q

Carbamazepine
MOA
Uses
Adverse Effects /ADR

A

Carbamazepine: AED (Tegretol)
- fast sodium channel inactivator with active metabolite also inactiving the Na+ channel

Uses
- focal and general seizures (no absence)
- bipolar disorder
- trigeminal neuralgia
- neuropathic pain

ADR
- these are all concentration dependent
- diplopia, drowsiness and sedation
- slgnificant N/V
- leukopenia
- Aplastic anemia
- hyponatermia
- rash: SJS risk
- decreased BMD
- teratogenic

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13
Q

Carbamazepine
Contraindications to Use
Monitoring Parameters
what about metabolism

A

Contraindiciations
- bone mineral density suppression: depression
- use of MAO within 14 days
- using nefaxdone
- using NNRTI (HIV med)
- presence of the HLA-B 1502 gene: if you CANNOT TEST FOR THIS; you CANNOT USE this med

Monitoring
- drug level 4-12mcg/mL
- must screen for HLA-B1502 gene
- monitor CBC: WBC > 2,500 & ANC > 1,000
- Na: keep 135-145

Metabolism
Carbamazepine is an AUTOinducer:meaning it will metabolize itself quicky at 3A4 then over time level out
- increase dose every week until adequte concentration
- starts 3- 5days; ends 21-28 : check levels weekly for first 3-5 weeks

PT. MUST BE ON FOLIC ACID 1-4 MG DOSING IF THEY ARE ON CARBAMAZEPINE

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14
Q

Oxcarbazepine
MOA
Indications

A

MOA
- a prodrug: converted and then its metabolite inactivates fast sodium channels

Indications
- generalized and focal seizures
- can be usd in those not responding to carbamaizepine

Side Effects
- well tolerated
- diplopid, dizzty, somnelence
- rash: watch if they had it to carbamaz. they’ll probs have it here too
- hyponatremia: more likely

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15
Q

Oxcarbazepine
monitoring
metabolism

A

Monitoring
- no therapeudic monitoring needed
- watch neuro exam
- watch sodium levels

Metabolism
- no autoinduction
- this drug can decrease the bioavalibility of estrogen in OCP medications

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16
Q

Ethosuximide
MOA
Indications (specific)
Side Effects
Monitoring

A

Ethosuximide:MOA
- a calcium channel modulator

Indications
only used for absence seizures!!!!! : the first-line medication

Side Effects
- well tolerated
- N/V
- ataxia and sedation
- neutropenic: monitor CBC
- rash
- hepatoxicity

Monitoring
drug levels should be 40-100mcg/mL

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17
Q

Felbamate
MOA
Indications (specific)
Side Effects
Drug Interactions
Contraindication!!

Study These Flashcards
A

Felbamate: MOA
- glutamate activity inhibitor

Indications
- LAST LINE CHOICE: use for pt. who are not responding to other agents

Side Effects (many = hence last line)
- anxiety/insomnia
- nausea
- weight loss
- HA severe
- Aplastic anemia: need to monitor CBC
- Acute liver failure: monitor LFTs

Drug Interactions
- increased CNS depressant with others
- no monitoring of levels needed

Contraindication
- hisotry of blood disorder (dyscrasias)
- history of hepatic dysfunction

18
Q

Gabapentin (neurontin)
MOA
Indications
Side Effects

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A

Gabapentin: MOA
- enhances GABA inhibition activity
- modulates calcium channels

Indications
- used for focal and general seizures (usually adjuct)
- used on elderly
- post-herpetic neuralgia
- neuropathic pain
- diabetic neuropathy

Side Effects
- well tolerated
- sedation/drowsy
- peripheral edema & weight gain
- on withdrawal: anxiety, insomnia, nausea, sweating etc. (syndrome)

Pearls
- no monitoring, contraindications, enzyme issues
- watch in renal: need to renally adjust

19
Q

Lacosamide
MOA
Indications
Side Effects

Study These Flashcards
A

Lacosamide: MOA
- slow sodium channel inactivation

Indications
- can be indicated for those who failed other sodium channel blocking meds (phenytoin)
- focal seziures
- last line salvage in status. epi.

Side Effects
- dizzy, diplopia, N/V, HA
- increased LFTs : monitor
- PR interval prolongation: EKG

due to prolonged PR: caution use in those with 2nd or 3rd degree heart block

20
Q

Lamotrigine
MOA
Indications
Side Effects

Study These Flashcards
A

Lamotragine: MOA
- fast sodium channel inactivation

Indications
- absence seizures
- focal, tonic-clonic and general
- bipolar disorder too

Side Effects
- drowsy, HA, diplopia, insomnia, etc.
- Rash: within 3-4 weeks and can progress to SJS
- rash seen more commonly with concurrent use of valproic acid + lamotragine

Drug Intercations
- lamotragine decreases the levogresterol component in OCPS
- ethinyl estradiol impacts lamotragine
- if used with carbamaziepine: CNS effects

21
Q

Levetiracetam (Keppra)
MOA
Indications
Side Effects
Elimination

Study These Flashcards
A

Levetiracetam: MOA
- modulates synaptic vescile protien

Indications
- focal & general: very good with seizures treatment and preventing

Side Effects
- sedation, dizzy, depression
- hallucinations: agitation and psychosis if underlying psych. disease

Metabolism
- renally eliminated: adjust as needed

22
Q

Phenobarbital
MOA
Indications
Side Effects

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A

Phenobarbital: MOA
- fast sodum channel inactivator

Indications
- general or focal seizures

SIde Effects
- ataxia, droswy, sedation (significant!)
- hyperactivity in some pt.
- osteoporosis
- rash
- blood disorders: agranulocytosis, thrombocyotpenia, megaloblastic anemia

23
Q

Phenobarbital
Contraindications
Monitoring levels
Drug Interactions

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A

Contraindications
- hepatic dysfunction
- airway issues/dyspena
- history of sedative/hyponotic abiuse
- nephritic pt.

Monitoring
goal 15-40 mcg/mL
- CBC
- neuro exam

Drug Interactions
- strong CYP - 3A4 inducer: speeds up metabolism of lots of meds
- ethanol will increase metabolism of pehnobarb.
- cimetidine will decrease metabolism

24
Q

Phenytoin (Dilantin)
MOA
Indications
SE (by level) and general

Study These Flashcards
A

Phenytoin: MOA
- fast sodum channel inhibitor

Indications
- status epi: use
- focal or general seizures

Side Effects: depend on concentration
- all: dizzy, diplopia, drowsy sedation
- normal levels 10-20
- > 20 = nystagmus
- > 30 = ateral nystagmus and ataxia
- > 40 = decreased mentation
- > 100 = death

other SE
- anemia
- gingival hyperplasia
- hirsutism
- lymphadenopathy
- osteporosis
- rash
- hepatotoxic
- teratogenic

25
Phenytoin Concentration and plasma monitoring difference between free and bound
Concentration Considerations - **phenytoin will be 95% bound to the plamsa albumin protein** - but there is a nonlinear relationship between dose and concentration - as the dose increases, the body can no longer metabolize it as fast, so you get increased serum concentrations once fully saturated in its bound to plasam form - **small chages in dose of phenytoin can lead to large changes in serum concentration** Monitoring - **monitor tough levels (before next dose)** - TOTAL phenyotoin (bound and unbound) = 10-20 - FREE phenyotoin (unbound) = 1-2 TOTAl levels: can be falsely low in those with low albumin: seems ok but when you do the free levle you see there SO much unbound (thus active) that you get bad SE
26
Equation for Free and Total Phenyotinin levels
check a free level in - hypoalbuminemia - reanl failure - pregnant - critically ill - babies - those with lots of protein bound drugs For Hypoalbuminemia adjusted = TOTAL concentration/ (0.2 x albumin) + 0.1 For CrCl < 10 adjusted = TOTAL concentration/ (0.1 x albumin) + 0.1 if calculating both: dose ajust base on whichever one is worse
27
Phenytoin drug interactions contraindications to IV phenytoin
Phenytoin Drug INteractions **major substart at 2C9 and 19** induces 3A4 highly preotien bound drug: so drug interactions can occur with other drugs that are highly bound as well Contraindication to IV Phenyotoin - sinus brday - SA block - 2nd and 3rd degree heart block
28
Pregabalin MOA Indications
Pregabalin: MOA - calcium channel modulator Indications - focal seizure adjuct - fibromyaliga - postherpetic nerualgia - neuropathic pain - **controlled substance** Side effets - dizzy, sedation, dry mouth, blurry vision - **peripheal edema & weight gain** - wihtdrawl syndrome possible Pearls - renally eliminated: dose - no drug interactions or monitoring
29
Tiabaine MOA Indications Side Effects Drug Interactions
MOA - enhances GABA Indication - add on for focal seizures SIde Effects - dizzy - sonolence - slow thinking - CNs depressant Drug Interactions - **major CYP 3A4** substarte: watch with inducers/inhibitors
30
Toperimate MOA Indications Side Effects Drug Indications
Toperimate: MOA - fast sodium channel inactivtion - enhances GABA activity - inhibits glutamate activity Indications - focal and general seziures - migraine prophylaxis Side Effects - ataxia, dizzy, drowsy - **acute angle glaucoma** - ** renal calculi** Contraindications - with extended release: no alcohol within 6 hours; risk of metabolic acidosis if taking metformin Drug Interactions - increases etrogen clearance - carbamazepine, phenytoin and valporate can decrease toperimate concentrations
31
Valproic Acid Types MOA Indications
Valproic Acid: Types - **immediate release med: Depakene** - delayed release: stavzor - IV: valproate sodium - enteric coated - **bioavaiblity between formulations varies** MOA - fast sodium channel inactivation Indications - for all seizures - migraine prophylaxis - mania - diabetic neuropathy
32
Valproic Acid Side Effects Monitoring Contraindications
**Teratogenic** Side Effects - nausea, drowsy - **tremor** - acute hepatotoxicity - acute pancreatitis - osteperosis - weight gain Monitoring **trough: 50-100** Contraindications - hepatic dz. pt. - **urea cycle disorders** - mitochondrail disorders - pregnant pt.
33
Valproic Acid Drug Interactions
Drug Interactions - **highly protein bound drug**: watch interaction with phenytoin! - **oral contraceptives increase clearance of valproic acid** - **valproic acid levels can be decreases by carbapenems** - additive effects of CNS depressants
34
Vigabatrin MOA Indications Side Effects
Vigabatrin: MOA - GABA transaminase Indications - **only for REFRACTORY foacl onset seizures** - you NEED to D/C this med in anyone with subclinical benefits Side Effects - convulsions - dizzy - HA - weight gain - **permanent vision loss and blindness** DOES HAPPEN
35
Vigabatrin Monitoring Parameters
Monitoring - vision assessment: at baseline, before 4 weeks of administeration, then every 3 months AND 3-6 months after d/c med no monitoring of levels no contraindications
36
Zonisamide MOA Indications Side Effects Contraindications
Zonisamide: MOA - sodum and calcium channels Indications - foacl onset seizures Side Effects - dizzy, somnolence - metabolic acidosis - oligohydrosis - paresthesias - renal calculi Contraindications **SULFONAMIDE ALLERGY!!**
37
Cost Issues with AEDs
- rx. can be made for BRAND NAME only if necessary : since sometimes the bioavalibility varies and pt. can be sensitive
38
Drug Levels to Know waht two drugs clearance from the body are increased with OCP use
Carbamazpine ; 4-12 Ethosuximide: 40-100 phenobarbital: 15-40 phenyotoin: 10-20 (total) 1-2 bound valproic acid: 50-100 OCP use: increases clearance of valproic acid and lamotrigine
39
Teratogencity which meds are how much folic acid
Valproic Acid Carbamazpine these have risk of neural tube defects and hypospadias Barbituates (phenobarb) & phenytoin - heart defects, cleft lipe and others **women of childbearing age = MUST take 1-4 mg of folic acid daily** if on these (or any AED) med
40
Osteoporosis and malacia with AEDs
chronic AED use = increased risk phenyotoin, phenobarbital, carbamazepine, valproic acid add cacium and Vit D after 6montsh of therapy to decrease risk
41
D/C medications of AED how is it done
**AED withdrawal can be considered for those meeting ALL THE FOLLOWING CRITERIA!!!** - extended period of seizure free (2 years if absence, 5 years if others) - normal neuro exam - normal IQ - normal EEG - single type of seizure dx. how to D/c - slow taper over 1-3 months - 60% chance they will remain seizure free

Pharm III: Exam 1 (6 decks)

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