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Year 2 Pharmacology > Anticonvulsants I > Flashcards

Anticonvulsants I Flashcards

1
Q

what is the cause of seizures?

A

abnormally excessive and rhythmic firing of certain populations of hyper-excitable neurons in the brain

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2
Q

seizures are usually characterized by what physical manifestation?

A

convulsions

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3
Q

what are the underlying causes of seizures?

A
  1. CNS injury - altered excitation thresholds
  2. congenital abnormalities within brain
  3. genetic factors
  4. infections, hypoglycemia, hypoxia, toxic metabolites
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4
Q

definition: epilepsy

A

chronic neurological disorder characterized by recurrent seizures

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5
Q

what are the two types of seizures?

A
  1. partial (focal)

2. generalized

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6
Q

what are the subtypes of partial (focal) seizures?

A
  1. simple partial
  2. complex partial
  3. secondarily generalized
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7
Q

what are the subtypes of generalized seizures?

A
  1. tonic-clonic (grand mal)
  2. absence (petit mal)
  3. myoclonic, atonic, clonic, tonic
  4. unclassified
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8
Q

what is the most severe type of seizure?

A

tonic-clonic (grand mal)

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9
Q

what is the most common partial seizure?

A

complex partial

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10
Q

what is the most common generalized seizure?

A

tonic-clonic

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11
Q

is there loss of consciousness with simple partial seizures?

A

no

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12
Q

how does a complex partial seizure spread?

A

from a small area of the brain to other areas that affect alertness and consciousness

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13
Q

is there loss of consciousness with complex partial seizures?

A

altered with potential automatisms

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14
Q

which type of seizures affect the entire brain with global EEG change and bilateral manifestations?

A

generalized

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15
Q

what are the features of a petit mal (absence) seizure?

A
  1. sudden onset and abrupt cessation
  2. brief loss of consciousness
  3. typically seen in children
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16
Q

what are the features of grand mal (tonic-clonic) seizures?

A
  1. tonic spasms and major convulsions of entire body (bilateral)
  2. loss of consciousness
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17
Q

what are the four stages of grand mal (tonic-clonic) seizures?

A
  1. aura
  2. tonic phase
  3. clonic
  4. stuporous state and sleep
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18
Q

what is status epilepticus?

A

continuous or very rapid recurring seizures, usually of the tonic-clonic type - medical emergency and require immediate therapy

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19
Q

what characterizes an atonic seizure? what type of seizure is it?

A
  1. sudden loss of postural tone, often seen in children

2. subtype of generalized seizure

20
Q

what are the three stages of the seizure mechanism?

A
  1. initiation
  2. synchonization of surounding
  3. propagation - recruitment of normal neurons
21
Q

what are the cellular and molecular factors that lead to seizure?

A
  1. excitatory postsynaptic potentials
  2. sodium influx
  3. calcium currents
  4. paroxysmal depolarization
22
Q

what are the cellular and molecular factors that lead to control of seizures?

A
  1. inhibitory postsynaptic potentials
  2. potassium efflux
  3. chloride influx
  4. pumps
  5. low pH
23
Q

what is the goal of antiepileptic drugs?

A

restore normal patterns of electrical activity

24
Q

what are the treatment options for seizures?

A
  1. antiepileptic drugs
  2. surgery
  3. vagus nerve stimulation
25
Q

when is vagus nerve stimulation indicated for seizure treatment?

A

for drug resistant patients with partial seizures

26
Q

what are the anticonvulsant drug classes?

A
  1. cyclic ureides
  2. tricyclics
  3. benzodiazepines
  4. GABA derivatives
  5. “others”
27
Q

what are the cyclic ureide drugs?

A
  1. phenytoin and fosphenytoin
  2. primidone
  3. phenobarbital
  4. ethosuximide
28
Q

what are the tricyclic anticonvulsant drugs?

A
  1. carbamazepine

2. oxcarbazepine

29
Q

what are the benzodiazepine anticonvulsant drugs?

A
  1. diazepam

2. lorazepam

30
Q

what are the GABA derivative anticonvulsant drugs?

A
  1. gabapentin

2. pregablin

31
Q

what are the “other” anticonvulsant drugs?

A
  1. valproic acid
  2. lamotrigine
  3. acetazolamide
  4. tiagabine
  5. topiramate
32
Q

which drugs are typically used for partial seizures?

A
  1. carbamazepine
  2. phenytoin
  3. valproate
33
Q

which drugs are typically used for tonic-clonic seizures?

A
  1. carbamazepine
  2. phenytoin
  3. valproate
34
Q

which drugs are typically used for absence (petit mal) seizures?

A
  1. ethosuximide

2. valproate

35
Q

which drugs are typically used for status epilepticus?

A

diazepam, lorazepam, phenytoin, fosphenytoin

36
Q

what is the MOA for anticonvulsant agents?

A

inhibit firing of certain hyper-excitable cerebral neurons by

  1. decreasing excitatory effects of glutamate and repetitive firing of neurons (block voltage gated sodium channels)
  2. increase inhibitory effects of GABA
  3. alter neuronal activation by altering movement of ions (sodium, calcium) across neuronal membrane
37
Q

what are the presynaptic methods of diminishing glutamate release?

A
  1. inactivation of VG sodium channels
  2. inactivation of VG calcium channels
  3. increase potassium channel opening
38
Q

what are the postsynaptic methods of diminishing glutamate release?

A
  1. blockage of AMPA receptors

2. blockage of NMDA receptors

39
Q

what is the mechanism for anticonvulsive agents that inactivate sodium channels?

A

bind sodium channel in inactive state and keep it inactivated for a prolonged period of time - preventing sodium from entering cell

40
Q

what is the mechanism for anticonvulsive agents that cause reduced activity of calcium channels?

A

reduce calcium influx - decrease NT release and prevent neuronal excitability

41
Q

inactivation of which receptor type is most effective for petit mal seizures?

A

calcium

42
Q

what are the targets for increasing the effect of GABA?

A
  1. inhibit GABA transporters (block GABA reuptake)
  2. inhibit GABA transaminase (block GABA metabolism)
  3. potentiate activation of GABAa receptors
43
Q

what are the general side effects of anticonvulsants?

A

sedation, diplopia, nystagmus, ataxia, GI upset

44
Q

which anticonvulsant is considered safest during pregnancy?

A

phenobarbital

45
Q

valproate and ethosuxamide act on which receptor to decrease seizure activity? which type of seizures are these good for? what is the MOA?

A
  1. calcium channel
  2. petit mal
  3. reduce pacemaker current that underlies thalamic rhythm in spikes and waves seen in absence seizures

Year 2 Pharmacology (70 decks)

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