Anticonvulsants (Lauren 🌭) Flashcards
What is the difference between partial/focal and generalized seizures?
Partial/Focal- originates in one area of brain
generalized- involves whole brain
What are the 3 types of partial/focal seizures?
Simple- short, no loss of consciousness
Complex- long
Partial with secondary general- starts in one spot then spreads to whole brain
What are the 4 types of Generalized seizures?
Absence (petit mal)- brief loss of awareness but not consciousness
Tonic-clonic (Grand mal)- initial rigidity, then clonic jerking. Loss of consciousness
Myoclonic- brief spasm
Atonic (no drugs to treat this type)- sudden loss of postural tone, patient falls down
True or False:
Activation of glutamate receptors (NMDA) can lead to seizures
True
true or false:
Blockage of GABA receptors causes seizures
True
Will increasing GABA activity stop seizures?
Yes
What are the mechanisms for increasing GABA activity?
Block GABA re-uptake (GAT inhibitor)- tiagabine
Inhibit GABA metabolism- vigabatrin
Stimulate GABA “A” receptors- benzos and barbs
Bind synaptic vesicular protein- levetiracetem
What are the common targets used to decrease excitatory glutamate activity in seizures?
Voltage gated Na+ and Ca++ channels
If a drug affects calcium channels, what kind of seizure will it help with/
Absence
Do we try to treat seizures with a single drug?
Yes, monotherapy is the goal because all these drugs have so many weird interactions
What are the 2 serious side effects of anticonvulsant drugs?
Teratogenic 👼🏻
Stevens-Johnson Syndrome
Which drug has the highest potential for Stevens Johnson syndrome?
Carbamazepine
Any drugs that block voltage gated Na+ channels have the potential to cause:
Stevens Johnsons Syndrome
What drug is the PROTOTYPE INDUCER of CYP450’s
Phenobarbital
Which drug is the PROTOTYPE INHIBITOR of CYP450s?
Valproic acid
How are most anticonvulsants metabolized?
By CYP450s
The pharmoacokinetics are “messy.” Phenytoin, carbamazepine and phenobarbital induce CYP450s.
Many drug interactions.
Phenytoin (Dilantin) and Fosphenytoin (Cerebyx) are used for what types of seizures?
Partial
Tonic-clonic
NOT ABSENCE
What is the MOA of Phenytoin
Prolongs inactivation of Na+ channels
Decreases glutamate activity
If an anticonvulsant drug acts on Na+ channels, you know it’s going to decrease what
Glutamate activity
How is Phenytoin (and Fosphenytoin) eliminated
At low doses: 1st order kinetics
At therapeutic doses and higher: ZERO order
Why does it matter if Phenytoin is eliminated by zero order kinetics at therapeutic doses?
Small changes in dose can cause BIG CHANGES in plasma levels
Which anticonvulsant can cause gingival hyperplasia?
Phenytoin (Dilantin)
If your patient is on phenytoin and she starts to get a skin rash, what should you do?
Discontinue it becasue there is a risk of SJS!!!
Your patient takes phenytoin for her seizures, and now she wants to get pregnant. What should you tell her?
She should probably stop taking it because its pregnancy category D
What is the drug of choice for partial seizures?
Carbamazepine (Tegretol)
What is a compelling alternative use for Carbamazepine (Tegretol)?
Trigeminal Neuralgia**
Trigeminal nerve is in your cheeks and you chew CARBs with your cheek
What is the MOA of carbamazepine (Tegretol)?
Blocks Na+ channels, decreases glutamate activity
Inhibits NE release and reuptake
What do you need to test your patient for before you put them on Carbamazepine?
HLA-B 1502 gene
High risk of SJS if they have this!!!
What is the MOA of Lamotrigine (Lamictal)?
Inactivation of Na+ channels, decreases glutamate activity
What are the side effects of Lamotrigine (Lamictal)?
Skin rash and Stevens Johnson syndrome
What is the MOA of Topiramate (Topamax)?
Blocks Na+ channels, decreases glutamate activity
What anticonvulsants can help with bipolar disorder for some reason
Carbamazepine ( Tegretol)
Lamotrigine (Lamictal)
Gabapentin
Valproic acid
This is probably not on the test
What are two other things that Topiramate (Topamax) can be sued for other that’s partial and generalized tonic-clonic seizures?
Migraine prevention
Alcohol craving
What is the side effet of Topiramate (Topamax) that you need to know?
Visual stuff: myopia/glaucoma
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