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Year 2 Pharmacology > Anticonvulsants II > Flashcards

Anticonvulsants II Flashcards

1
Q

what are the hydantoin antiseizure drugs?

A

phenytoin and fosphenytoin

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2
Q

which hydantoin antiseizure drug is more soluble and used for parenteral use?

A

fosphenytoin

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3
Q

where is phenytoin metabolized? by what system?

A

liver - MES system

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4
Q

how is phenytoin excreted?

A

urine

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5
Q

elimination of phenytoin follows what kinetics?

A

dose-dependent (zero order)

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6
Q

what is the MOA of phenytoin?

A
  1. blocks and prolongs inactivated state of voltage gated sodium channels
  2. enhances release of GABA
  3. prevents seizure progagation
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7
Q

what are the clinical uses for phenytoin?

A

generalized tonic-clonic, partial, status epilepticus

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8
Q

what are the dose related side effects of phenytoin?

A

sedation, ataxia, nystagmus, diplopia, cardiac dysrhythmias

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9
Q

what are the idiosyncratic side effects of phenytoin?

A

gingival hyperplasia

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10
Q

which drug interactions decrease phenytoin metabolism?

A

barbiturates (high), warfarin

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11
Q

which drug interactions increase phenytoin metabolism?

A

barbiturates (low), carbamazepine

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12
Q

which drug interactions displace the protein binding of phenytoin?

A

salicylates, valproic acid, kidney failure

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13
Q

which drug class is carbamazepine?

A

tricyclic

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14
Q

what is the MOA of carbamazepine?

A

inhibition of voltage gated sodium channels (same as phenytoin)

blocks high frequency firing of neurons and decreases synaptic release of glutamate

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15
Q

what is oxacarbazepine?

A

antiseizure drug similar to carbamazepine - shorter half life but active metabolite has longer duration and fewer drug interactions

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16
Q

what are the clinical uses of carbamazepine?

A

general clonic-tonic (grand mal), partial seizures, TRIGEMINAL NEURALGIA

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17
Q

how is carbamazepine metabolized?

A

hepatic MES - induces p450s to upregulate its own metabolism

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18
Q

what is the drug of choice for trigeminal neuralgia?

A

carbamazepine

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19
Q

carbamazepine has drug interactions with which other drugs?

A

phenytoin, valproate, phenobarbital

20
Q

what is the MOA of the phenobarbital?

A

enhances phasic GABAa receptor responses - increased opening time of chloride channel

21
Q

what are the side effects of cabamazepine?

A

syndrome of inappropriate ADH secretion - fluid retention and hyponatremia

22
Q

what is the main clinical use for phenobarbital?

A

status epilepticus

23
Q

what is primidone?

A

metabolized by liver (MES) to phenobarbital and phenyl ethyl malonic acid (PEMA)

24
Q

what is the MOA of ethosuximide?

A

blocks presynaptic T type calcium channels (blocks high frequency firing of neurons)

25
Q

what are the clinical uses for ethosuximide?

A

absence seizures (petit mal)

26
Q

what are the drugs of choice for petit mal (absence) seizures?

A

ethosuximide, valproic acid

27
Q

what is the MOA of valproic acid?

A
  1. inhibition of presynaptic T type calcium channels - blocks neuronal firign
  2. inhibition of GABA transaminase
28
Q

what is the main clinical use of vvalproic acid?

A

absence (petit mal) seizures

29
Q

what is the main adverse event of valproic acid?

A

hepatotoxic syndrome, teratogenic risk

30
Q

what are the preferred initial agents for status epilepticus?

A

diazepam (valium) or lorazepam (longer acting)

31
Q

what is the MOA of diazepam?

A

potentiates GABAa responses by increasing frequency of channel opening

32
Q

what is the main clinical use of diazepam?

A

status epilepticus

33
Q

what are the use limitations of diazepam?

A
  1. sedative

2. tolerance

34
Q

which drugs apart from diazepam and lorazepam can be used as antiepilepsy drugs?

A

clonazepam, nitrazepam, clorazepate

35
Q

what is the MOA of gabapentin?

A

blocks presynaptic voltage gated calcium channels - decreaes excitatory transmission

36
Q

what are the clinical uses for gabapentin?

A
  1. generalied tonic-clonic (grand mal)
  2. partial seizures
  3. neuropathic pain - postherpetic neuralgia and fibromyalgia
37
Q

what is pregabalin?

A

similar to gabapentin, GABA analog

38
Q

what is the MOA of lamotrigine?

A

blocks presynaptic voltage gated sodium and calcium channels

39
Q

what are the clinical uses for lamotrigine?

A
  1. partial
  2. grand mal
  3. petit mal
40
Q

what is the main adverse effect of lamotrigine?

A

steven johnson syndrome - severe blistering / necrosis of skin

41
Q

what are the “other” newer agents of anticonvulsants?

A
  1. felbamate
  2. topiramate
  3. tiagabine
42
Q

definition: spasticity

A

exaggerated muscle stretch reflex syndrome that occurs following injury to CNS

43
Q

definition: spasm

A

increase in muscle tension seen after certain musculoskeletal injuries and inflammation

44
Q

what is the MOA of diazepam as a muscle relaxant?

A

increases inhibitory actions of GABA on alpha motor neurons in spinal cord

45
Q

what is the MOA of baclofen as a muscle relaxant?

A

GABAb receptor agonist - increased potassium conductance, hyperpolarization, reduction in calcium influx, reduction in excitatory transmitter release

46
Q

which drug treats spasms associated with excess exertion, MS, cerebral palsy, injury?

A

diazepam

47
Q

which drug reduces spasticity with MS, spinal, and brain injury?

A

baclofen

Year 2 Pharmacology (70 decks)

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