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Pharm > Anticonvulsants II > Flashcards

Anticonvulsants II Flashcards

1
Q

What are the general adverse side effects of antiepileptic drugs?

A 
Ataxia
Nystagmus
HA
Depression
Sedation
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2
Q

How are antiepileptic drugs metabolized?

A

hepatic MES system

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3
Q

Abrupt withdrawal of antiepileptic drugs has the potential for what to happen?

A

Inducing seizures

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4
Q

Why do antiepileptics cause a decrease in efficacy of oral contraceptives?

A

Induces cytochrome p450

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5
Q

What is the safest antiepileptic drug to take during pregnancy?

A

Phenobarbital

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6
Q

What is the MOA of hydantoins? (3)

A
  • Blocks and prolongs the inactivated state of voltage-gated Na channels
  • Decreases glutamate release
  • Enhances GABA release
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7
Q

What type of antiepileptic drug is phenytoin?

A

Hydantoin

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8
Q

What type of antiepileptic drug is Fosphenytoin?

A

Hydantoin

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9
Q

What is the major difference between the Hydantoins Phenytoin and fosphenytoin?

A

Fosphenytoin is more soluble prodrug

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10
Q

What are the pharmacokinetics of Hydantoins (absorption, state in blood, what type of elimination)?

A

Variable absorption
Highly bound to protein albumin
Zero order elimination

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11
Q

What type of drugs cause the release of albumin bound hydantoins?

A

Acidic drugs

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12
Q

What is the route of metabolism for Hydantoins?

A

Metabolized in liver by MES system

Induction of p450 enzymes

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13
Q

Can zero order elimination be saturated?

A

yes

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14
Q

At low doses, what is the relationship between plasma concentration, and dose? High doses?

A 
Low = relatively linear
High = Nonlinear
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15
Q

true or false: phenytoin can be used to treat status epilepticus

A

true

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16
Q

What are the idiosyncratic side effects of phenytoin?

A

Gingival hyperplasia
Osteomalacia
Hirsutism

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17
Q

What is fetal hydantoin syndrome?

A

Teratogenic effects like cleft palate,

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18
Q

What are the two drugs that interfere with Phenytoin metabolism?

A

Warfarin

barbiturates (high concentration)

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19
Q

What are the two drugs that increase phenytoin metabolism?

A

Barbituates (low dose)

Carbamazepine

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20
Q

Lower pH can cause the release of phenytoin from albumin. What are the two drugs and one condition that can cause this?

A

ASA
Valproic acid
Renal failure

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21
Q

What is the MA of carbamazepine?

A

Inhibition of voltage gated Na channels

Decreases E release

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22
Q

How is carbamazepine metabolized?

A

Hepatic MES

Potent induce of MES p450s

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23
Q

How well is carbamazepine absorbed?

A

Well absorbed

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24
Q

What is the MOA of oxcarbazepine?

A

Derivative of carbamazepine

Inhibits Na channels and decreases E release

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25
Q

What is the major difference between Oxcarbazepine and carbamazepine?

A

fewer drug interactions

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26
Q

What are the clinical uses of carbamazepine?

A

generalized szs
Partial szs
Trigeminal neuralgia

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27
Q

What are the side effects of carbamazepine?

A

CNS depression
Aplastic anemia
SIADH

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28
Q

What are the three major drug interactions of carbamazepine?

A

Phenytoin
valproate
Phenobarbital

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29
Q

What is the role of carbamazepine in the treatment of bipolar disorder?

A

treats the manic phase

30
Q

What is the MOA of barbiturates?

A

Enhances phasic GABA(A) receptor responses, increasing the opening time of Cl channels

31
Q

What are the primary uses of phenobarbital?

A

Status epilepticus

Neonatal seizures

32
Q

What type of drug is phenobarbital?

A

Barbiturate

33
Q

What type of drug is primidone?

A

Barbiturate

34
Q

What is the MOA of ethosuximide?

A

Blocks presynaptic Ca influx through type T channels (decreases low threshold Ca currents), thereby blocking high frequency firing of neurons

35
Q

How is ethosuximide metabolized?

A

Hepatic MES

36
Q

What is the major clinical use of ethosuximide?

A

Absence seizures

37
Q

What are the primary drugs to treat petit mal seizures?

A

Ethosuximide

valproic acid

38
Q

What is the MOA of valproic acid?

A

Inhibition of Presynaptic T-type Ca Channels

Inhibition of GABA transaminas

39
Q

What are the two primary adverse effects of valproic acid?

A 
hepatotoxic syndrome
Teratogenic risk (spina bifida)
40
Q

What is the role of valproic acid in bipolar disorder?

A

treats manic phase

41
Q

What is the MOA of benzodiazepines?

A

Potentiates GABA-A responses by increasing the frequency of channel opening

42
Q

What type of drug is diazepam?

A

Benzo

43
Q

What type of drug is lorazepam?

A

Benzo

44
Q

What is the preferred initial agent for status epilepticus?

A

Diazepam

45
Q

What are the limitations of diazepam use?

A

Sedative effects

Tolerance

46
Q

Why must diazepam be followed up by another antiepileptic in the treatment of status epilepticus? What other benzodiazepine can be used to avoid having to use two drugs?

A

Short duration of effect

Lorazepam

47
Q

What is the MOA of gabapentin?

A

Analog of GABA, thereby blocking presynaptic voltage gated Ca channel

48
Q

What are the three major clinical uses of gabapentin?

A
  1. generalized tonic-clonic seizures
  2. Partial seizure
  3. Neuropathic pain
49
Q

What is the MOA of pregabalin?

A

GABA analog, blocking presynaptic Ca channels

50
Q

What are the two drugs discussed that can treat neuropathic pain?

A

gabapentin

carbamazepine

51
Q

What is the MOA of Lamotrigine?

A

Blocks presynaptic Na and Ca channels

52
Q

What is the major adverse effect of Lamotrigine?

A

Steven-Johnson syndrome

53
Q

what are the two major drugs that can interact with Lamotrigine?

A

Valproate

carbamazepine

54
Q

What is Steven-Johnson syndrome?

A

a form of toxic epidermal necrolysis, starting with a sore throat and fever. Caused by hypersensitivity to a drug.

55
Q

What is the MOA of felbamate?

A

Blocks Na channels and Glutamate receptors

56
Q

What is the MOA of topiramate?

A

Blocks Na and Ca channels

Potentiates GABA

57
Q

What is the MOA of tiagabine?

A

Specific inhibitor of GABA reuptake

58
Q

What is spasticity?

A

An exaggerated muscle stretch reflex syndrome that occurs following injury to the CNS

59
Q

What is a spasm?

A

increase in muscle tension seen after certain MS injuries an inflammation

60
Q

What is the cause of spasms/spasticity?

A

hyperexcitability of the neurons or muscle cells

61
Q

What is the goal of pharmacotherapy in treating muscle spams/spasticity?

A

Normalize muscle excitatbility

62
Q

What is the MOA of Baclophen?

A

GABA-B agonist

63
Q

What is the neurotransmitter used in inhibitory interneurons?

A

GABA

64
Q

What is the difference between GABA-A and GABA-B receptors?

A 
A = ionic
B = G protein coupled receptor
65
Q

What is baclofen used for?

A

reduce spasticity of muscles

66
Q

What can diazepam be used for, besides anticonvulsants?

A

treating muscle spasms

67
Q

What are the 5 major cyclic ureides?

A 
Phenytoin
Fosphenytoin
Primidone
Phenobarbital
Ethosuximide
68
Q

What are the two major tricyclic antiepileptics?

A

Carbamazepine

Oxcarbazepine

69
Q

What are the three major benzodiazepine antiepileptics?

A

Diazepam
Lorazepam
Clonazepam

70
Q

What are the three major GABA derivative antiepileptics?

A

Gabapentin
Pregabalin
Vigabatrin

71
Q

What is the MOA of acetazolamide?

A

carbonic hydrase inhibitor

Pharm (73 decks)

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