AGENTS, CONTROLLING THE FUNCTIONS OF THE CENTRAL NERVOUS SYSTEM - Antiseizure drugs Flashcards

1
Q

The mechanism of action of antiseizure drugs is

A
  • Enhancement of GABAergic (inhibitory) transmission
  • Diminution of excitatory (usually glutamatergic) transmission
  • Modification of ionic conductance
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2
Q

Which antiseizure drugs produces enhancement of GABA-mediated inhibition?

A

Phenobarbital

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3
Q

Indicate an antiseizure drug, which has an impotent effect on the T-type calcium channels in thalamic neurons?

A

Ethosuximide

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4
Q

Which antiseizure drugs produces a voltage-dependent inactivation of sodium channels?

A
  • Lamotrigine
  • Carbamazepin
  • Phenytoin
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5
Q

Indicate an antiseizure drug, inhibiting central effects of excitatory amino acids

A

Lamotrigine

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6
Q

The drug for partial and generalized tonic-clonic seizures is

A
  • Carbamazepine
  • Valproate
  • Phenytoin
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7
Q

Indicate an anti-absence drug

A

Valproate

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8
Q

The drug against myoclonic seizures is

A

Clonazepam

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9
Q

The most effective drug for stopping generalized tonic-clonic status epilepticus in adults is

A

Diazepam

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10
Q

Phenytoin

A

It blocks sodium channels

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11
Q

Phenytoin is used in the treatment of

A

Grand mal epilepsy

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12
Q

Dose-related adverse effect caused by phenytoin is

A

Gingival hyperplasia

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13
Q

Granulocytopenia, gastrointestinal irritation, gingival hyperplasia, and facial hirsutism are possible adverse effects of

A

Phenytoin

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14
Q

The antiseizure drug, which induces hepatic microsomal enzymes, is

A

Phenytoin

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15
Q

The drug of choice for partial seizures is

A

Carbamazepin

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16
Q

The mechanism of action of carbamazepine appears to be similar to that of

A

Phenytoin

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17
Q

Which antiseizure drugs is also effective in treating trigeminal neuralgia?

A

Carbamazepine

18
Q

The most common dose-related adverse effects of carbamazepine are

A

Diplopia, ataxia, and nausea

19
Q

Indicate the drug of choice for status epilepticus in infants and children

A

Phenobarbital sodium

20
Q

Barbiturates are used in the emergency treatment of status epilepticus in infants and children because of

A

They significantly decrease of oxygen utilization by the brain, protecting cerebral edema and ischemia

21
Q

Which antiseizure drugs binds to an allosteric regulatory site on the GABA-BZ receptor, increases the duration of the Cl-channels openings

A

Phenobarbital

22
Q

Adverse effect caused by phenobarbital is

A
  • Physical and phychological dependence
  • Exacerbated petit mal epilepsy
  • Sedation
23
Q

Which antiseizure drugs is a prodrug, metabolized to phenobarbital?

A

Primidone

24
Q

Indicate the antiseizure drug, which is a phenyltriazine derivative

A

Lamotrigine

25
Q

Lamotrigine can be used in the treatment of

A
  • Partial seizures
  • Absence
  • Myoclonic seizures
26
Q

The mechanism of vigabatrin′s action is

A

Inhibition of GABA aminotransferase

27
Q

Indicate an irreversible inhibitor of GABA aminotransferase (GABA-T)

A

Vigabatrin

28
Q

Tiagabine

A

Blocks neuronal and glial reuptake of GABA from synapses

29
Q

The mechanism of both topiramate and felbamate action is

A
  • Reduction of excitatory glutamatergic neurotransmission
  • Inhibition of voltage sensitive Na+ channels
  • Potentiation of GABAergic neuronal transmission
30
Q

The drug of choice in the treatment of petit mal (absence seizures) is

A

Ethosuximide

31
Q

The dose-related adverse effect of ethosuximide is

A
  • Gastrointestinal reactions, such as anorexia, pain, nausea and vomiting
  • Exacerbated grand mal epilepsy
  • Transient lethargy or fatigue
32
Q

Valproate is very effective against

A
  • Absence seizures
  • Myoclonic seizures
  • Generalized tonic-clonic seizures
33
Q

The drug of choice in the treatment of myoclonic seizures is

A

Valproate

34
Q

The reason for preferring ethosuximide to valproate for uncomplicated absence seizures is

A

Valproate′s idiosyncratic hepatotoxicity

35
Q

The mechanism of valproate action is

A
  • Facilitation glutamic acid decarboxylase, the enzyme responsible for GABA synthesis and inhibition of GABAaminotransferase, the enzyme responsible for the breakdown of GABA (enhance GABA accumulation)
  • Inhibition of voltage sensitive Na+ channels
  • Inhibition of low threshold (T-type) Ca2+ channels
36
Q

Indicate the antiseizure drug, which is a sulfonamide derivative, blocking Na+ channels and having additional ability to inhibit T-type Ca2+ channels

A

Zonisamide

37
Q

Indicate the antiseizure drug – a benzodiazepine receptor agonist

A

Lorazepam

38
Q

Which antiseizure drugs acts directly on the GABA receptor-chloride channel complex?

A

Diazepam

39
Q

Benzodiazepine΄s uselfulness is limited by

A

Tolerance

40
Q

A long-acting drug against both absence and myoclonic seizures is

A

Clonazepam

41
Q

Which antiseizure drugs may produce teratogenicity?

A
  • Phenytoin
  • Valproate
  • Topiramate
42
Q

The most dangerous effect of antiseizure drugs after large overdoses is

A

Respiratory depression