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Pharmacology 3 > E1- Anticonvulsants > Flashcards

E1- Anticonvulsants Flashcards

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1
Q

What type of seizure is characterized by:

  • Focal, brief (20-90 sec)
  • Grimacing, focal clonic jerking of an extremity
  • No loss of consciousness
A

Partial simple seizure

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2
Q

What type of seizure is characterized by:

  • Longer (<2 min)
  • Automatic movements
  • Altered or loss of consciousness; hallucinations
A

Partial complex seizure

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3
Q

What type of seizure is characterized by:

  • Tonic-clonic with loss of consciousness
  • Muscle contractions alternating with relaxation
A

Partial with secondary general

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4
Q

What type of seizure is characterized by:

  • Sudden onset, brief
  • Loss of awareness, but not consciousness
A

Absence (petit mal)

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5
Q

What type of seizure is characterized by:

  • Initial tonic rigidity, subsequent tremor, eventual clonic jerking
  • Loss of consciousness
A

Tonic-clonic (grand mal)

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6
Q

What type of seizure is characterized by:

-Brief spasm or rigidity

A

Myoclonic

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7
Q

What type of seizure is characterized by:

-Sudden loss of postural tone, pt can fall down

A

Atonic

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8
Q

What is the general MOA of anticonvulsants?

A

Increase GABA activity or decrease excitatory glutamate activity

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9
Q

Which anticonvulsants inhibit Na+ channels? (6)

A 
Carbamazepine
Phenytoin
Topiramate
Lamotrigine
Valproate
Zonisamide
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10
Q

Which anticonvulsants inhibit Ca2+ channels? (2)

What are their uses?

A

Ethosuximide
Valproate
Absence seizures

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11
Q

Which anticonvulsant inhibits both Na+ and Ca2+ channels?

A

Valproate

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12
Q

What are common SE of anticonvulsants? (4)

A

Teratogenicity
Suicide
Hypersensitivity (SJS)- screen for HLA-B allele, discontinue if develop rash
Failure of contraceptives

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13
Q

What should an OD of an anticonvulsant not be treated with?

A

CNS stimulants

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14
Q

Which anticonvulsant inhibits CYP450s?

A

Valproate

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15
Q

Which anticonvulsants induce CYP450s? (3)

A

Phenytoin
Carbamazepine
Phenobarbital

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16
Q

What is the difference between Phenytoin and Fosphenytoin?

A

Phenytoin (oral)

Fosphenytoin (injectable)

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17
Q

What is the MOA of Phenytoin and Fosphenytoin?

A

Prolongs inactivation of Na+ channels –> decreases glutamate activity

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18
Q

What are the uses of Phenytoin and Fosphenytoin? (2)

A

Partial seizures

Generalized tonic clonic seizures

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19
Q

What is the pharmacokinetics of Phenytoin and Fosphenytoin elimination?

A

Elimination is 1st order at low doses but zero order at therapeutic and higher doses

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20
Q

What are SE specific to Phenytoin and Fosphenytoin? (5)

A 
Nystagmus
Diplopia
Ataxia
Sedation
Gingival hyperplasia
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21
Q

What is the MOA of Carbamazepine?

A

Blocks Na+ channels –> decreases glutamate activity

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22
Q

What is DOC for partial seizures?

A

Carbamazepine

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23
Q

What are uses of Carbamazepine? (4)

A

Partial seizures (DOC)
Generalized tonic-clonic seizures
Bipolar disorder
Trigeminal neuralgia

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24
Q

What are SE specific to Carbamazepine? (6)

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A 
Diplopia
Ataxia
GI upset
Drowsiness
Aplastic anemia Agranulocytosis
25
What is the MOA of Lamotrigine?
Inactivates Na+ channels --> decreases glutamate activity
26
Which anticonvulsant has the highest risk of SJS?
Carbamazepine
27
What are the uses of Lamotrigine? (2)
Partial seizures | Bipolar disorder
28
What are SE specific to Lamotrigine? (5)
``` Dizziness Diplopia Ataxia Somnolence N/V ```
29
What is the MOA of Topiramate?
Blocks Na+ channels --> decreases glutamate activity
30
What are the uses of Topiramate? (2)
Partial tonic-clonic seizures | Generalized tonic-clonic seizures
31
What are SE specific to Topiramate? (2)
Acute myopia | Glaucoma
32
What is the MOA of Levetiracetam?
Binds synaptic vesicular protein SV2A --> decreases glutamate activity and increases GABA release
33
What are uses of Levetiracetam? (3)
Partial seizures Myoclonic seizures Tonic-clonic seizures
34
What is the MOA of Phenobarbital?
Prolongs opening of Cl- channel at GABA receptor
35
What are the uses of Phenobarbital? (2)
Partial seizures | Generalized tonic-clonic seizures
36
What are possible drug interactions of Phenobarbital?
Induces CYP450s (increased metabolism of Phenytoin and Carbamazepine)
37
What is the MOA of Gabapentin?
GABA analog, may increase GABA release
38
What are the uses of Gabapentin? (3)
Adjunct for partial and generalized tonic-clonic seizures Neuropathic pain Bipolar disorder
39
What is the pharmacokinetics regarding Gabapentin elimination?
Elimination is 1st order; excreted unchanged by the kidney
40
What is useful about Gabapentin?
NO drug interactions
41
What is the MOA of Pregabalin?
GABA analog; binds to Ca2+ channels inhibiting excitatory neurotransmitter release
42
What are the uses of Pregabalin? (4)
Generalized anxiety disorder Neuropathic pain Fibromyalgia Post-op pain
43
What anticonvulsants have minimal drug interactions?
Levetiracetam Gabapentin Pregabalin Tiagabine
44
What are SE specific to Pregabalin? (7)
``` Peripheral edema Dizziness Weight gain Xerostomia Ataxia Blurred vision GI upset ```
45
What is the MOA of Tiagabine?
Inhibits reuptake of GABA  enhances GABA activity
46
What is the use of Tiagabine?
Adjunct for partial seizures
47
What is the MOA of Vigabatrin?
Irreversibly inhibits GABA transaminase
48
What are the uses of Vigabatrin? (2)
``` Refractory complex partial seizures Infantile spasm (West’s syndrome) ```
49
What are SE specific to Vigabatrin? (2)
Visual field problems | Retinal damage
50
What is the MOA of Ethosuximide?
Inhibits low-threshold (T-type) Ca2+ channels
51
What is DOC for absence seizures?
Ethosuximide
52
What SE is specific to Ethosuximide?
Hiccup
53
What is the MOA of Valproic acid?
Blocks Ca2+ channels AND Na+ channels
54
What are the uses of Valproic acid? (3)
Absence and general tonic-clonic seizures (“mixed” seizures”) Bipolar disorder Migraine prophylaxis
55
What are SE specific to Valproic acid?
Hepatoxicity | Teratogenic- increase risk of spina bifida
56
What is the MOA of Clonazepam (BZ)?
Stimulates GABA receptor and enhances GABA inhibition
57
What are the uses of Clonazepam (BZ)? (3)
Absence seizures Myoclonic seizures Infantile spasms (West’s syndrome)
58
What is the MOA of Diazepam (BZ) and Lorazepam (BZ)?
Stimulates GABA channel
59
What is the DOC for Status Epilepticus?
Diazepam (BZ) and Lorazepam (BZ)

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