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50 Cards in this Set
- Front
- Back
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almost all antiepileptic drugs, AEDS are associated with CNS depressing or elevating effects?
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depressing (also some tolerance to these effects develops over 7-10 days)
intially pts may feel VERY TIRED, drowsy, ataxic, etc |
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Once you prescribe an AED to a pt, what do you need to monitor?
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serum drug levels must be monitored. therapy is guided by clinical response but drug levels can be useful when toxicity or dosage adjustments are needed. THESE DRUGS HAVE A NARROW THERAPEUTIC INDEX!)
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tell me about carbamazepine and about you're so. carb, auto partial tonic mood D
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-sodium channel bocker
-controlled vs. immediate release dosing -autoinduction (metabolized by CYP 3A4 (need to increase dose after 10 days) -FOR: partial seizures esp complex partial, tonic clonic generalized seizures, mood stabilizers in BPD and is category D |
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what's the cousin of carbamazepine?
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oxycarbazepine!
same MOA and similar structure potential first line for partial + general tonic clonic seizures -role as mood stabilize in bipolar disorder |
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What do you use as a loading dose for phenytoin (dilantin)?
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IV fosphenytoin
water soluble phenytoin (its highly protein bound therefore it WILL cross the BBB) |
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What's the moa OF phenytoin?
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alters calcium uptake, alters na/k pump therefore slowing rate of na+ channel recovert
CA AND NA |
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what's the pharm of phenytoin? describe how to give it.
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-liver metabolism
-loading dose + half life (requires both a loading dose and maintenance dose!) 400 mg (every 2-4 hours) then 300-400 mg either each day to TID (start with 5 mg/kg/day and make frequent adjustments!) -IRRITATING TO VEINS AND TISSUE |
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who do you prescribe phenytoin to?
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AED OF CHOICE for those with generalized type tonic clonic seizures
(for status elepticus, prophylaxis and tx of seizures in neurosurgery) also used for partial seizures |
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phenytoin can worsen what type of seizures?
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absence seizures
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moa of valproic acid?
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affects NA channel and may affect GABA metabolism (may increase levels- remember its inhibitory)
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pharm of valproic acid? (depakene)
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-comes in many forms (divalproex sodium, enteric coated, caps w/sprinkle, tabs, ER, caps, syrup
-liver metabolism + renal excretion -well absorbed although DELAYED BY FOOD and longer to peak w/enteric coated forms |
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use of valproic acid?
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used for diverse AED
1ST LINE FOR GENERALIZED ABSENCE SEIZURES, AND MYOCLONIC SEIZURES (localized muscle twitches) -useful in partial seizures and generalized tonic clonic seizures |
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difference between primidone and phenobarbitol
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barbiturates that bind to receptors to enhance inhibitor effects of GABA on postsynaptic neurons
-increase opening of the Cl- channels -primidone = is metabolized to PB but has a 2nd metabolite that might as well be an active AED. |
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whats the preferred route for primidone/phenobarbitol?
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IV> IM > po (onset is QUICK with IV route!)
-p450 inducer (issues with drug interactions) Its a potent enzyme inducer long half life (can give as a single dose @ bedtime or BID) full therapeutic effects take 2-3 weeks unless loading dose is given |
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which is the oldest AED?
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phenobarbitol and primidone
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what's the first line usage of primidone and phenobarbitol?
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neonatal seizures!
-generalized tonic clonic seizures -partial seizures (NOT used for absence seizures) |
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what drugs are NOT used for absence seizures?
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primidone/phenobarbitol, phenytoin, carbamazepine, oxycarbazepine
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partial seizures?
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carbamazepine and oxycarbazepine
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generalized type tonic clonic?
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phenytoin
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absence seizures
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valproic acid
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primidone and phenobarbitol?
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neonate seizures
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with carbmazepine does it have a black box warning?
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Need frequent CBC monitoring b/c its secondary to cases of aplastic anemia + stevens johnson (rash)
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what are the AE of carbamezepine?
PREGNANCY CATEGORY? |
-BANDS G
blurry vision ataxia -nystagmus -dizziness -stevens johnson (rash) -GI (give larger doses @ bed time to decrease this and titrate over 2-3 weeks to therapeutic range!) CATEGORY d!! |
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what are the drug interactions of carbamezapine?
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-e-mycin and clarithromycin
-increased metabolic of valproic acid, theophylline, and warfarin MONITOR THOSE SERUM DRUG LEVELS! |
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WHAT ARE THE AE OF oxycarbazepine?
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less than carbamezapine
still have hyponatremia just like tegretol |
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AE of phenytoin?
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ligand:
lethary/fatigue, incorrdination, GINGIVAL HYPERPLASIA (50%), ataxia, nystagmus, drowsiness AND HYPOTENSION - when given IV, chronic effects: endocrine + metabolic, infertility issues in women, hirsutism, osteoporosis since it interferes w/vit D necessary for vitamin D necessary for calcium absorption, osteomalacia, category D! chronic hirsuitisim ,acne coarsening of facial features, folic acid def, hypothyroidism , CHO intolerance |
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what are the drug interaction of phenytoin?
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-other aeds
-pregnancy category D |
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what are the SE of valproic acid?
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most common: tremor (unique!), dizzy, HA, insomnia, blurred vision, diplopia
WHAT. Pg -weight gain (30-40%) -MOST SERIOUS: hepatotoxicity early in the course: black box WARNING! -alopecia and hair changes -thrombocytopenia -pancreatitis (rare) -GI (decrease w/ enteric prep) |
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drug interactions of valproic acid?
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*other AEDs
-pregnancy D (related to spina bifida!) |
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as for primidone and phenobarbitol, what are the AE?
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category D
-CNS depressant (drowsy, somnolence) -impairs cognitive function (may paradoxically stimulate children) -rashes (like the other barbiturate rashes) -PB is an enzyme inducer, might increase elimination of drugs metabolized by hepatic enzymes (accelerates metabolism) -dulling of higher cortical function which may delay intellectual development CIRED |
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what is topiramate useful for?
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partial seizures
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what does topiramate block?
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glutamate neurotransmission, affects na channels and enhances GABA
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what are the AE of topiramate?
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WWAMMP. n
-word finding difficulties (obv not the best drug for kids!) -weight loss (anorexia + nausea) -ataxia (imbalance) -memory impairment -memory difficulties -paresthesias -nephrolithiasis (so drink lots of water bc of kidney stones! bc of their acidotic state! |
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what category and DI are there with topiramate?
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category c
FEWER DI than other AEDs |
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first line for absence seizures??
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ethosuxmide, reduces ca currents in thalamic neurons
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m/c ae OF ETHOSUXIMIDE?
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n&v, anorexia!
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ae OF gabapentin?
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m/c: diplopia, HA, ataxia
-gi upset -BB warning = RASH which appears in 1st 3-4 weeks, require withdrawal! titrate slowly and d/c immediately! |
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monotherapy and adjunctive therapy of partial seizures?
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gapapentin (also for neuropathic pain - diabetic neuropathy, and bipolar disorder)
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adjunct med for partial seizures?
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levetiracetam or keppra (new drug)
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tell me more about levetiracetam.
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well tolerated, asthenia, somnolence, dizziness
-saturable carrier protein -fatigue, dizzi, ataxia (VERY SEDATING) -tremor and nystagmus and edema BETTER TOLERATED! |
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why is levetiracetam so great?
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better tolerated!
no major DI! BUT frequent daily dosing! |
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moa OF tiagabine?
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stop GABA reuptake
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what is tiagabine used for?
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adjunct for partial seizures!
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things to remember about tiagabine:
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po
-half life is 8 hours and is shorteneed when coadministered with PB and carbamazepine |
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AE of tiagabine?
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dts: dizziness, tremor, somnolence just like levetiracetam
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zonisamide moa?
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affects are on calcium and sodium channels. LONG half life well absorbed liver metabolism, renal excretion. iamotrigine increases levels whereas carba and PB decrease levels
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use of zonisamide?
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partial seizures
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AE of zonisamide?
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tell pt to have water
raans: renal calculi in 1%, ataxia, anorexia, nervousness (similar to toperamate), somnolence |
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use of pregalin? (lyrica)
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1) partial seizures (adj)
2) fibromyalgia 3) neuropathic pain 4) DM and postherpetic neuralgia (useful in various areas that are painful!) pregalin reduces the calcium-dependent release of several NT's by modulation of calcium channel function |
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ae of pregalin?
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dddebts. w
1) dosedependent (related to gaba-ergic effects), dry mouth, dizziness 2) edema 3) blurred vision 4) "thinking abnormal" 5) somnolence 6) weight gain! |
