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69 Cards in this Set
- Front
- Back
Seizure MOA
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underactivity of GABA or over activity of glutamate transmission
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Kindling
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hyperexcitable state, caused by periodic brief low intensity elecrical stimulation of amygdala or other limbic structures. Caused by inhibiting NMDA
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Partial seizure MOA, what stops them?
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neurons fire at high frequency, reducing ability of Na+ channels to recover from inactivation
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Absence seizure MOA?
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3Hz spike and wave discharge from thalamus. T current voltage gated Ca2+ channels.
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Drugs that prolong Na+ channel inactivation?
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phenytoin, carbamazepine, lamotrigine, valproic acid
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Drugs that block T type Ca2+ current in thalamus?
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ethosuximide, valproic acid
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Drugs that enhance gaba? How?
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phenobarbital and bezodiazepines. Open Cl- channels, hyperpolarize.
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Drugs that induce cytochrome p450?
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phenytoin, carbamazepine, phenobarbital
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Phenytoin/ fosphenytoin MOA, uses?
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block sustained high frequency repetitive firing of neurons by prolonging inactivation of the Na+ channel. Partial seizures and generalized tonic clonic seizures, NOT ABSENCE!
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Phenytoin kinetics?
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Dose dependent, small first order, large zero order. Phenytoin oral, fophenytoin IV. Small therapeutic range. Highly protein bound.
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Drugs that displace phenytoin from protein?
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phenylbutazone, sulfonamides
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Phenytoin prevents metabolism of?
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warfarin
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phenytoin increases metabloism of?
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oral contraceptives
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Phenytoins metabolism is increasedby?
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carbamazepine
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Phenytoin side effects?
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gingival hyperplasia, hirsuitism, abnormal VitD metabolism, Ca2+ absorption inhibition, rash, teratogen
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Carbamazepine MOA?
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blocks Na+ channels and decreases NT release
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Carbamazepine differs from phenytoin how?
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mood stabilizing, used for bipolar
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Carbamazepine DOC for? other uses?
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Partial seizures, also generalized tonic clonic seizures and trigeminal neuralgia.
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Carbamazepine kinetics?
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induces cyp3a4, metabolzes oral contraceptives. Induces own metabolism. Therapeutic range 6-12 microgram
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Carbamazepine increases metabolism of?
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phenytoin, primidone, ethosuximide, valproic acid, clonazepam, haloperidol, oral cont.
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Inhibit carbamazepine metabolism?
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cimetidine, fluoxetine
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Carbamazepine toxicity?
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GI upset, blood dyscrasia, stevens johnsons
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Steven johnsons allele?
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HLA B1502
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Phenobarbital, MOA and uses?
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prolongs chloride channel opening, hyperpolarization. Partial and generalized tonic clonic seizures
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Metabolized to phenobarbital?
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primidone
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Vigabatrin?
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irreversible inhibitor of gaba transaminase, causes visual effects.
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Lamotrigine, MOA and uses?
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inactivates voltage dependent Na+ channels. Partial seizures, absence seizures. Bipolar disorder.
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Lamotrigine toxicity?
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nausea, somnolence, rash. Preg Cat C.
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GABA pentin MOA and uses?
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GABA analog, NOT AGONIST.
Partial, generalized tonic clonic seizures. Neuropathic pain, bipolar, antianxiety. |
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GABA pentin kinetics?
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short T 1/2. Wide dose range. Kidney excretion w/ linear kinetics. Preg CAT C.
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Topiramate MOA?
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blocks voltage gated Na+ channels, enhaces GABAa currents, limits glutamate receptor activation. INHIBITS spread of seizure.
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Topiramate uses?
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partial and generalized tonic clonic seizures. Migraine propylaxis. West's syndrome and lennox getaut.
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Topiramate SE?
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decreases effectvieness of birthcontrol. pre cat C. dizziness, sedation, nervousness, confusion.
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Tiagabine MOA and uses?
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inhibits GABA uptake, partial seizures. Preg CatC
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Absence seizure DOC, drugs MOA?
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ethouximide, reduces low threshold Ca2+ current in thalamus.
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Ethosuximide clearance decreased by?
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valproic acid
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Ethosuximide SE?
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gastric pain, preg cat C
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DOC for absence seizures w/ generalized tonic clonic seizures?
MOA |
valproic acid, blocks high frequency repetitive firing
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Valproic acid uses?
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absence, generalized tc, myoclonic, bipolar, migraines.
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Valproic acid interactions?
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inhibits own metabolism. Inhibits metabolism of phenytoin, carbamazepine, and phenobarbital which causes coma.
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Valproic acid toxicity?
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Hepatotoxicity
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Clonazepam used for?
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absence seizures
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Diazepam/lorazepam used for?
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status epilepticus (IV)
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Drugs that cause steven johnsons?
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Phenytoin, Ethosuximide, Tiagabine
Carbamazepine, Oxcarbazepine, Phenobarbital, primodine Valproic acid, lamotrigine |
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At physiologic pH, local anesthetics exist in what form?
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ionized
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factors that decrease effectiveness of local anesthetics?
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inflammation with acidification
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Epinephrine anesthetic MOA?
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decreases substance P via alpha 2
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Amide anesthetics?
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bupivacaine, lidocaine, prilocaine
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Ester anesthetics?
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benzocaine, cocaine, procaine
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Amide distribution, metabolism?
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Wide distribution. liver cp450
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Ester distribution, metabolism?
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rapid via pseudocholinesterase
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Carbonation
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saturation with CO2, decreases pH to increase cellular concentration.
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Side effects not seen with cocaine?
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negative inotropy, vasodilation/hypotension
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bupivacaine SE?
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broadens QRS
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Prilocaine SE?
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metabolite causes methemoglobinemia, Tx with methylene blue
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ester/PABA SE?
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allergic reaction
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Lidocaine duration of action, uses?
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intermediate, infiltration blocks and epidurals
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Mepivicaine?
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intermediate duration longer than lidocaine. Causes less drowsiness and sedation.
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Bupivacaine duration uses?
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LONG, infiltration blocks and epidural anesthesia
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Ropivicaine?
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S isomer of bupivicaine. Less lipid soluble, cleared via liver and less likely to cause adverse effects.
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TCA MOA and uses?
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inhibit NE and 5HT reuptake. chronic pain and fibromyalgia
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Duloxetine MOA and uses?
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TCA, diabetic peripheral neuropathy and fibromyalgia
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Used for neuropathic pain?
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Gabapentin and pregabalin
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Used for fibromyalgia and shingles pain?
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pregabalin
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Used for trigeminal neuralgia pain?
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carbamazepine
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Muscle relaxant most likely to be abused?
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carisoprodil
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Muscle relaxant used for fibromyalgia?
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cyclobenzaprine
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Topical NSAID?
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diclofenac
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Lidocaine patches?
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local analgesia, especialy for post herpetic neuralgia
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