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69 Cards in this Set

  • Front
  • Back
Seizure MOA
underactivity of GABA or over activity of glutamate transmission
Kindling
hyperexcitable state, caused by periodic brief low intensity elecrical stimulation of amygdala or other limbic structures. Caused by inhibiting NMDA
Partial seizure MOA, what stops them?
neurons fire at high frequency, reducing ability of Na+ channels to recover from inactivation
Absence seizure MOA?
3Hz spike and wave discharge from thalamus. T current voltage gated Ca2+ channels.
Drugs that prolong Na+ channel inactivation?
phenytoin, carbamazepine, lamotrigine, valproic acid
Drugs that block T type Ca2+ current in thalamus?
ethosuximide, valproic acid
Drugs that enhance gaba? How?
phenobarbital and bezodiazepines. Open Cl- channels, hyperpolarize.
Drugs that induce cytochrome p450?
phenytoin, carbamazepine, phenobarbital
Phenytoin/ fosphenytoin MOA, uses?
block sustained high frequency repetitive firing of neurons by prolonging inactivation of the Na+ channel. Partial seizures and generalized tonic clonic seizures, NOT ABSENCE!
Phenytoin kinetics?
Dose dependent, small first order, large zero order. Phenytoin oral, fophenytoin IV. Small therapeutic range. Highly protein bound.
Drugs that displace phenytoin from protein?
phenylbutazone, sulfonamides
Phenytoin prevents metabolism of?
warfarin
phenytoin increases metabloism of?
oral contraceptives
Phenytoins metabolism is increasedby?
carbamazepine
Phenytoin side effects?
gingival hyperplasia, hirsuitism, abnormal VitD metabolism, Ca2+ absorption inhibition, rash, teratogen
Carbamazepine MOA?
blocks Na+ channels and decreases NT release
Carbamazepine differs from phenytoin how?
mood stabilizing, used for bipolar
Carbamazepine DOC for? other uses?
Partial seizures, also generalized tonic clonic seizures and trigeminal neuralgia.
Carbamazepine kinetics?
induces cyp3a4, metabolzes oral contraceptives. Induces own metabolism. Therapeutic range 6-12 microgram
Carbamazepine increases metabolism of?
phenytoin, primidone, ethosuximide, valproic acid, clonazepam, haloperidol, oral cont.
Inhibit carbamazepine metabolism?
cimetidine, fluoxetine
Carbamazepine toxicity?
GI upset, blood dyscrasia, stevens johnsons
Steven johnsons allele?
HLA B1502
Phenobarbital, MOA and uses?
prolongs chloride channel opening, hyperpolarization. Partial and generalized tonic clonic seizures
Metabolized to phenobarbital?
primidone
Vigabatrin?
irreversible inhibitor of gaba transaminase, causes visual effects.
Lamotrigine, MOA and uses?
inactivates voltage dependent Na+ channels. Partial seizures, absence seizures. Bipolar disorder.
Lamotrigine toxicity?
nausea, somnolence, rash. Preg Cat C.
GABA pentin MOA and uses?
GABA analog, NOT AGONIST.
Partial, generalized tonic clonic seizures. Neuropathic pain, bipolar, antianxiety.
GABA pentin kinetics?
short T 1/2. Wide dose range. Kidney excretion w/ linear kinetics. Preg CAT C.
Topiramate MOA?
blocks voltage gated Na+ channels, enhaces GABAa currents, limits glutamate receptor activation. INHIBITS spread of seizure.
Topiramate uses?
partial and generalized tonic clonic seizures. Migraine propylaxis. West's syndrome and lennox getaut.
Topiramate SE?
decreases effectvieness of birthcontrol. pre cat C. dizziness, sedation, nervousness, confusion.
Tiagabine MOA and uses?
inhibits GABA uptake, partial seizures. Preg CatC
Absence seizure DOC, drugs MOA?
ethouximide, reduces low threshold Ca2+ current in thalamus.
Ethosuximide clearance decreased by?
valproic acid
Ethosuximide SE?
gastric pain, preg cat C
DOC for absence seizures w/ generalized tonic clonic seizures?
MOA
valproic acid, blocks high frequency repetitive firing
Valproic acid uses?
absence, generalized tc, myoclonic, bipolar, migraines.
Valproic acid interactions?
inhibits own metabolism. Inhibits metabolism of phenytoin, carbamazepine, and phenobarbital which causes coma.
Valproic acid toxicity?
Hepatotoxicity
Clonazepam used for?
absence seizures
Diazepam/lorazepam used for?
status epilepticus (IV)
Drugs that cause steven johnsons?
Phenytoin, Ethosuximide, Tiagabine

Carbamazepine, Oxcarbazepine, Phenobarbital, primodine

Valproic acid, lamotrigine
At physiologic pH, local anesthetics exist in what form?
ionized
factors that decrease effectiveness of local anesthetics?
inflammation with acidification
Epinephrine anesthetic MOA?
decreases substance P via alpha 2
Amide anesthetics?
bupivacaine, lidocaine, prilocaine
Ester anesthetics?
benzocaine, cocaine, procaine
Amide distribution, metabolism?
Wide distribution. liver cp450
Ester distribution, metabolism?
rapid via pseudocholinesterase
Carbonation
saturation with CO2, decreases pH to increase cellular concentration.
Side effects not seen with cocaine?
negative inotropy, vasodilation/hypotension
bupivacaine SE?
broadens QRS
Prilocaine SE?
metabolite causes methemoglobinemia, Tx with methylene blue
ester/PABA SE?
allergic reaction
Lidocaine duration of action, uses?
intermediate, infiltration blocks and epidurals
Mepivicaine?
intermediate duration longer than lidocaine. Causes less drowsiness and sedation.
Bupivacaine duration uses?
LONG, infiltration blocks and epidural anesthesia
Ropivicaine?
S isomer of bupivicaine. Less lipid soluble, cleared via liver and less likely to cause adverse effects.
TCA MOA and uses?
inhibit NE and 5HT reuptake. chronic pain and fibromyalgia
Duloxetine MOA and uses?
TCA, diabetic peripheral neuropathy and fibromyalgia
Used for neuropathic pain?
Gabapentin and pregabalin
Used for fibromyalgia and shingles pain?
pregabalin
Used for trigeminal neuralgia pain?
carbamazepine
Muscle relaxant most likely to be abused?
carisoprodil
Muscle relaxant used for fibromyalgia?
cyclobenzaprine
Topical NSAID?
diclofenac
Lidocaine patches?
local analgesia, especialy for post herpetic neuralgia