Brand name: Tegretol, Carbatrol, Potiga

Clinical application: partial seizures primarily generalized convulsive  

PK:slow/erratic * large peak/trough difference * no first pass *food=increase in F * susupesion >higher absorb than tablets *CR and SR=(bid) *highly bound  * major metabolite= epoxide (eliminated in urine) * induces own metabolism*displays diurnal variaition in its serum level with evening levels< than morning levels *no IV*Metabolized=liver

Pro's:Many formulations, minimal cognitive effects . Its safer than others that may become pregnant 

Con's:*can parallel the rise and fall of serum concentration daily

.* Neurosensory Side Effects(diplopia, blurred vision, nystagmus, ataxia, unsteadiness, dizziness and headache (these are the most common @ start of therapy and decrease as the day goes on (may be caused by epoxide) 

* Can cause  hypoatremia (this can decrease serum sodium, ppl feel like they have horrible flu-like symptoms before this) ,

* can cause sedation/nystagmus( when your eys bounce) /memory impairment

*anticholinergic effects (antislud)

* paresthesias (tingling in skin)

*Leukopenia (most common hematologic side effect)

*thrombocytopenia

*aplastic anemia can also occur (fatal in 50%)

*hepatitis

  *cyp3A4 inducer

*rash

*teratogenic

*osteporosis (caused by the fact that Vit D is induced by cyp)

Genetic link with RASH??  *casings can appear in the feces*  can give 1% soina bifida *generic associated with breakthrough seizures when generics have been switched 

Therapeutic considerations:

*Check for side effects

Hypoatremia- feeling like having a terrible flu?

thrombocytopenia- abnormal bleeding?

Leukopenia- feeling sick all the time?

*CBZ rash

genetic component: those from china, thailand, philippines, malaysia, indonesia

*Start low and go slow

*dosing

qid with IR, BID with CR

Brand name:Dilatin

Clinical application:Generalized and convulsive and partial seizures

PK:Complex PK. *absorption complete * goes to brain rapidly and redistributed to other body tissues. Competes for albumin sites with other protein bound drugs.*good F*day-to-day variability with absorption *most liver metaobolized (Cyp 2c9 and 2c19 involved) - CYP and UGT inducer

Pro's:Cheap, good F, can take once a day (clearance)* flexibility in dosing* don't have to titrate up- can take the full dose right away.

Con's:erratic absorption,  unbound monitoring, small dose changes= large changes (changes in gastric Ph- really changes absorption) *unpredictable *renal absorption *hypoalbumininemia *pregnancy *liver disease-alter protein binding, bad iT and CYP, need MVI, osteporosis, some CNS side effects- concentration related( nystagmus, ataxia(drunk like) , confusion, encphalopathy), *rash small changes in dose can result in large increase in serum concentrations-  can do a start low and go slow. * metabolism of phenytoin can saturate even @ low serum concentrations within the therapeutic range * at high concentrations, phneytoin can exacerbate seizures. * gingival hyperplasia can occur *hirsutism and coarse facial features* vit D deficiency/osteomalcia/osteoporosis *carb intolerance *immunologic disturbance *hypothyroid *peripheral neuropathy  * lost of drug interactions inducer of cyp and UGT) *can be increased or decreased depending on meal *complicated dose titiration*induces CYP *high protein binding

Therapeutic considerations:

decreased metabolism if they have liver disease

larger dose per kg body weight in children. *smaller dose per kg body weight in elderly (NONLINEAR PK!)

Brand name:Depakote

Clinical application:primacy generalized seizures, myclonic , atonic, absence

PK: well absorbed* saturable binding to albumin * displays diurnal elimination with lower event serum levels ocrruing more than morning levels. Crosses the placenta and concentrations may be up to 5 times higher in baby blood than mom *metabolized mostly by the liver by gluronidation, beta oxidation and CYP as a minor pathway * polytherapy with inducers can double clearance.

Pro's:Broad spectrum,Works well

Con's:Female of child-bearing age: TERATOGENIC, Menstrual cycle mess ups, Polycystic ovary syndrome, tendency to get more facial hair. Estradial contraindication. Concentration-realted side effects: drowsiness, Postural tremor, confusion (encephalopy), hyperammonemia (high ammonia levels) , can't clot- more bleeding/menstrual cycles, induce parkingsons?* WEIGHT GAIN (since looks liek FA, when you ingest more fat while on VPA-you tend to store it more) *alopecia (loss of hair)  *GI se- na, v,  pacreatitis* inhibit metabolized insulin * min cog impairment *hepatotoxicity (if they feel bad all the time) *PCOS, enzyme inhibitor!

Therapeutic considerations: Nonlinear PK, low fat diet is really all you can do when on VPA, risk factors for hepatotoxicity:highest in neonates under 2, those one enzyme inducing antiepileptic drugs, if those 2-12 have back neurology problems, Non really seen in adults. Consider measuring unbound VPA level in patients with hypoalbuminemia

Brand name:-

Clinical application:neonatal seizures, used in other failed therapy with other AED

PK: Absorbed rapidly and completely regardless of whether if was given orally, intramuscularly, or rectall. Penetrates the brain at a reat comparable with that of phenytoin. Drug affective liver enzymes can alter the phenobarb metabolism, but phenobarbital is not affected by liver blood flow.. linear elimination. cl up in elderly * urine flow dependent *inducer of CYP and UDP glucuronyl transferase *urine flow dependent

Pro's:Available in multiple dorms. most inexpensive AED. Well aborbed

Con's:*CNS side effects are primary factors limiting the use of phenobarb (decreased cognitive function- memory, thinking, ability) . * tolerance develops developts to initial complaints of fatigue , drowsiness, sedation, depression *kids and geriatrics- hyperactivity *megaloblastic anemia *osteomalacia*porphyria and rash *teratogenic * potent ezyme inducer and can increase elimination of any drug metabolized by cyp 450 or UGT. Ethanol increases metab for this *delayed development of intelligence *veryyyyy long half life. *resp depression and hypotension

Therapeutic considerations:*start low and go SLOW. Linear PK , 1 qd, bedtime dosing may minimize CNS depression

Brand name:Neurontin

Clinical application:Partial seizures

PK:Renally eliminated  This drug has no effect on GABA, it was supposed to since it is a gabamimetic drug* displays dose dependent F that appears to vary considerably between individuals. *BE CAREFUL WITH KIDNEY DYSFUNCTION! ) renally elminated unchanged!, This drug is useful but erratic, it is NONlinear *no protein binding?

Pro's:Does not inhibit/induce cyp enzymes/UGT( doesn't interacti with other hepatic drugs (warfarin, theophyllin, oc) . Less CNS effects, broad therapeutic window. Don't have to titrate up, amendable to rapid dose escalation. *has multiple MOA *not metabolized and is excreted unchanged in the kidney

Con's:Effect saturates at higher doses, No parenteral forms. Causes somolence,fatigue, dizziness, ataxia,  stimulates appetite and makes people weight gain, edema. Aggressiveness can happen in kids. Withdrawal= anxiety, insomnia, nausea, sweating, increased pain. The dosing is variable and don't know where to start and where to go its going( its transported by AA transporters).

 
Therapeutic considerations:*although gabapentin and pregablin are derived from gaba, don't really have an effect on GABA

Brand name:Lyrica

Clinical application:partial seizures that have failed initial treatment. Also for chronic neuropathic pain and generalized anxiety

PK:*not dose dependent F. food decreases the rate of absorb but not the F. Eliminated renally, unchanged, not protein bound, no other drug interactions.  

Pro's:specifically for complex partial seizures, min drug interactions, starts working in 1-2 days. This is linear PK , more potent than gabapentin with out the dose-limited GI absorb properties. Min CNS effects and no drug interactions *does not display saturable oral absorption.

Con's:weight gain (causes a LOT), peripheral edema, have 2-3 times a day. Schedule V drugs  since can cause some euphoria in some patients*(drowsiness, dizziness, blurry vision) All the side effects with gabapentin cept worse. *narrower therapeutic range than Gabapentin

Brand name: Lamictal

Clinical application:Useful as both adjunctive treatemt. In patients with partial seizures and as monotherapy. This appears to have comparable effectiveness with more traditional AED's. May be useful alternative for primary generalized seizures types such as absence and as adjunctive therapy for primary GTC seizures.

PK:Completely and rapidly absorbed with a F of 98% . Food does not significantly affect absorption. It is also absorbed following recetal administration. *clearance is higher in children and lower in older adults compared to younger adults * hepatic disease can influence this drug (therefore susceptible to drug interactions) * if on VPA, you need LESS of lamotrigine since its an inhibitor! * small autoinduction can occur* half protein bound *clearance of drug goes way down during placebo week!!!*half life can increase with dialyses and renal failure

Pro's:100% oral absorption, no PK interactions, minimal cognitive impairment, wgt neutral*broad spectrum AED- efficacy with partial seizures and several types of generalized seizures. * doesn't inhibit/induce other AED's (modest UGT induction)  * may be useful in evalutation of drug interactions*well tolerated in children and elderly and doesn't cause weight gain.

Con's: Induced by CBZ, PHT, PB * inihibited by VPA *modest sedation* occasional HA and insomnia. Adverse effects more common when given with other AED's. Can cause rash- first part of therapy. More serious rashes with VPA.  *incidence is higher in children than adults. OC will induce UGT, therefore need more lamotrigine to work. No established therapeutic range. increased MCM. Can cause rash if you take VPA too. *VPA inhibits the metabolism of lamotrigine * noestablished therapeutic range

Therapeutic considerations: Lamotrigine rash risk factors:

if you go to fast for titration( start slow, go slow), concomitatnt VPA, in children

Brand name: Topamax

Clinical application:partial seizures, tonic-clonic, HA 

MOA: Block sodium channels

PK: excreted into the urine unchanged, 80% F, low protein binding *RENALLY ELIMINATED * Inhibits CYP 2C19, INDUCTION of cyp 3A4 (dose dependent)

Pro's: First line drug to partial and generalized seizures. Multiple MOA, category D. Very efficacious. This also treats headaches!

Con's:Lowers effectives of OC @ high doses (cyp 3A4 induction) (pregnancy category C) renal stones and weight loss. CNS effects- abnormal thinking, the "topiramate stun", memory loss, confusion, hard to think in general- you can see these cognitive effects in really low doses (they are themost common) .* psychosis in rare occasions* hard to find words * nephrolysis *metabolic acidosis * anorexia

Therapeutic considerations:

Brand name:Zonegran

Clinical application:partial seizures, primary generalized 

PK: cyp 3A4n metab

Pro's: no inhibition/drug induction. Long half life (less frequent dosing) and moderate weight loss. Multiple MOA, no known effects on other metabolized drugs 

Con's: Can cause cognitive impairment: sedation, anorexia, HA, agitation, depression= most common CNS May cause rash slowly titrate. Increase the use of Headaches. This causes renal stones, RASH- if a person had history of kidney stone= bad. Long half life- have to go low and go slow. Really don't know a lot about that pregnancy. This can cause depression. *solnolence, dizziness, anorexia, ha, na, agitation, word find difficulty.renal stones, avoid with patients allergical to sulfa

Therapeutic considerations: might be induced by other AEDS. Drugs that inhibit CYP 3A4 may reduce zns clearance and raise serum levels. Avoid with people  with renal failure

Brand name: Keppra

Clinical application:Approved for myclonic seizures and adjunct to generalized seizures in patients with ididopathic generalized epilepsy

PK:Renally eliminated. *absorption is rapid and complete following oral admin. * no cyp450 nor UGT

Pro's: Linear, rapid complete absorbption, low incidence of drug-drug interaction, weight neutral. No rash or wgt gain. Only modest sedation, fatigue, coordination.  This is first line therapy. * novel MOA*initial dose may be effective * appears well tolerated 

Con's:May causes psychosis and irritibility/ despression *does not appear to cause rash. *some animal studies have shown that it may prevent epilepsy *expect age related reduction * clearance higher in children * liver diseases- should receive less  because a decrease in clearance  *children and yound adults-agitation, irritibility, somnolence/lethary are most frequent reported CNS side effects *sedation * may cause behavioral problems * dose adjustment for those qith renal disease. * no established therapeutic range

Therapeutic considerations:

Brand name: Trileptal

Clinical application:Used as a first line therapy for partial seizures. Also dor generalized convulsize seizures. 

PK:  Completely absorbed, inactivated by glucuronide conjufation and eliminated by the kidneys* no autoinduction- there is a reduction reaction involved tp MHD (cyp 2c19 inhibited, cyp 3A4 UGT induced) . *linear PK*children appear to have more rapid clearance 

Pro's:comparable efficacy to carbazepine, VPA, phenytoin. Better tolerated then phenytoin for monotherapy. Can give to BID, no autoinduction. First line drug for partial seizures. 

Con's:Many Ade's( dizziness, na, HA, diarrhea, vomiting, URTI, constipation, dyspepsia, ataxia, nervourness, tremor ), can cause rash (less than carbazepine), Dizziness more in edlerly, and hypoatremia - sodium loss(coma).Lowers effectiveness of oral contraceptives. Enzyme inducer (CYP 3A4). Not good for older adults. * decreases the F of OC *can incresase the conc of pehnytoin 

Therapeutic considerations: dose reduction for those with renal impairment * careful for those taking sodiumhypoatremia.

Eslicarbazepine- this is the S entantiomer of oxcarbazepine (that is the parent drug) ( need less in renal impaired adults) - No significant interactions with other AED's- may increase conc of phenytoin and reduce effect of oral contraceptives- low incidence of hypoatremia= same common SE. not associated with changes in total cholesterol. No effect on BW

Brand name:Vimpat

Clinical application:

PK:Rapidly and almost completely absorbed after oral administration. Food does not affect its bioavailability. Linear relationship between daily doses and serum concentrations . No adjustment for the kids or the elderly. Moderate hepatic and renal impairment have been shown to increase *dimethylation is the major metabolic pathway *low protein binding * no significant CYP induction/inhibition

Pro's:absorption not affected by food. Cause enzyme inhibition/induction. Excellent F. Minimal SES, no rash or change in body weight * there is an IV form for short-term (safe, well tolerated, easy to administer. Does not affect the serum level of other ARD's and it minimally affected by enzyme-incuding AED's *novel MOA

Con's:Monitor renal function. Dose-related adverse effects(esp with other sodium channel blocking drugs) . Expensive*the most frequent side effects of lacosamide are dose related* dizziness, nausea, diplopia, abnormal coordination, ataxia, vomiting, and nystagmus. This drug also can causea small increase in the medial PR interval on the ECG * substrated of cyp2c19 *it is a controlled substance

Therapeutic considerations:

Brand name:

Clinical application:First line for infantile spasm, refractory partial epilepsy

MOA: Irreversible inihibitor of the GABA transaminase- enzyme responsible for the metab of gaba

PK: rapid, complete absorption, no metab and unchance in urine, no protein binding, via renal excretion

Pro's:Works well 

Con's:premenant vision loss= BAD. (increase risk with dose)  For a child with infintile spasm * dosage adjustment for renal elmination *may aggravate seizures (absence, myclonic) *might incrase psychiatric effects in those who already had issues *wgt gain/edema, peripheral neuropathy, solmnolence, fatigue *treat with high doses of drug for infantile spasms *induces Cyp 2C 

Therapeutic considerations:

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PK: 30% unchanged in the urine, need to adjust for renal function. Does not induce/inhibit Cyp or UGT

Pro's:

Con's:Shouldn't use with alcohol. Drosieness, dizziness, blurred vision, tremor, fatigue, gait disturbance, QT interval changes. Urinary retention! 3 times a day. This one is relatively new. 

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