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Pharma > Antiseizure Drugs > Flashcards

Antiseizure Drugs Flashcards

0
Q

Phenytoin
Fosphenytoin

Mechanism of action

A

Block high-frequency firing of neurons through action on voltage-gated (VG) Na+ Channels, decreases synaptic release of glutamate

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1
Q

Cyclic ureides

A

Phenytoin
Fosphenytoin
Phenobarbital
Ethosuximide

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2
Q

Block high-frequency firing of neurons through action on voltage-gated (VG) Na+ Channels, decreases synaptic release of glutamate

A

Phenytoin (Cyclic ureide)
Fosphenytoin (Cyclic ureide)
Carbamazepine (Tricyclic)

Mechanism of action

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3
Q

Phenytoin
Fosphenytoin

Pharmacokinetics

A

Absorption is formulation dependent, highly bound to plasma proteins, no active metabolites, dose-dependent elimination, t 1/2 12-36 h, fosphenytoin is for IV, IM routes

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4
Q

Absorption is formulation dependent, highly bound to plasma proteins, no active metabolites, dose-dependent elimination, t 1/2 12-36 h, fosphenytoin is for IV, IM routes

A

Phenytoin
Fosphenytoin

Pharmacokinetics

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5
Q

Phenytoin, Fosphenytoin

Clinical applications

A

Generalized tonic-clonic seizures, partial seizures

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6
Q

Generalized tonic-clonic seizures, partial seizures

A

Phenytoin, Fosphenytoin (Cyclic ureides)
Carbamazepine, Oxcarbazepine (Tricyclics)

Clinical applications

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7
Q

Phenytoin
Fosphenytoin

Toxicities, Interactions

A

TOXICITY: Diplopia, ataxia, gingival hyperplasia, hirsutism, neuropathy, INTERACTIONS: Phenobarbital, carbamazepine, isoniazid, felbamate, oxcarbazepine, topiramate, fluoxetine, fluconazole, digoxin, quinidine, cyclosporine, steroids, oral contraceptives, other

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8
Q

TOXICITY: Diplopia, ataxia, gingival hyperplasia, hirsutism, neuropathy, INTERACTIONS: Phenobarbital, carbamazepine, isoniazid, felbamate, oxcarbazepine, topiramate, fluoxetine, fluconazole, digoxin, quinidine, cyclosporine, steroids, oral contraceptives, other

A

Phenytoin
Fosphenytoin

Toxicities, Interactions

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9
Q

Ethosuximide

Mechanism of action

A

Reduces low-threshold Ca2+ currents (T-type)

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10
Q

Reduces low-threshold Ca2+ currents (T-type)

A

Ethosuximide

Mechanism of action

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11
Q

Ethosuximide

Pharmacokinetics

A

Well absorbed orally, with peak levels in 3-7 h, not protein bound, completely metabolized to inactive compounds, t 1/2 typically 40 h

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12
Q

Well absorbed orally, with peak levels in 3-7 h, not protein bound, completely metabolized to inactive compounds, t 1/2 typically 40 h

A

Ethosuximide

Pharmacokinetics

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13
Q

Ethosuximide

Clinical applications

A

Absence seizures

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14
Q

Absence seizures

A

Ethosuximide

Clinical applications

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15
Q

Ethosuximide

Toxicities, Interactions

A

TOXICITY: Nausea, headache, dizziness, hyperactivity, INTERACTIONS: Valproate, phenobarbital, phenytoin, carbamazepine, rifampicin

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16
Q

TOXICITY: Nausea, headache, dizziness, hyperactivity, INTERACTIONS: Valproate, phenobarbital, phenytoin, carbamazepine, rifampicin

A

Ethosuximide

Toxicities, Interactions

17
Q

Tricyclics

A

Carbamazepine
Oxcarbazepine
Eslicarbazepine acetate

18
Q

Carbamazepine
Oxcarbazepine
Eslicarbazepine acetate

A

Tricyclics

19
Q

Carbamazepine

Mechanism of action

A

Block high-frequency firing of neurons through action on voltage-gated (VG) Na+ Channels, decreases synaptic release of glutamate

20
Q

Carbamazepine

Pharmacokinetics

A

Well absorbed orally, with peak levels 6-8 h, no significant protein binding, metabolized in part to active 10-11-epoxide, t 1/2 of parent ranges from 8 to 12 h in treated patiens to 36 h in normal subjects

21
Q

Well absorbed orally, with peak levels 6-8 h, no significant protein binding, metabolized in part to active 10-11-epoxide, t 1/2 of parent ranges from 8 to 12 h in treated patiens to 36 h in normal subjects

A

Carbamazepine

Pharmacokinetics

22
Q

Carbamazepine

Clinical applications

A

Generalized tonic-clonic seizures, partial seizures

23
Q

Carbamazepine

Toxicities, Interactions

A

TOXICITY: Nausea, diplopia, ataxia, hyponatremia, headache, INTERACTIONS: Phenytoin, carbamazepine, valproate, fluoxetine, verapamil, macrolide antibiotics, isoniazid, propoxyphene, danazol, phenobarbital, primidone, many other

24
Q

TOXICITY: Nausea, diplopia, ataxia, hyponatremia, headache, INTERACTIONS: Phenytoin, carbamazepine, valproate, fluoxetine, verapamil, macrolide antibiotics, isoniazid, propoxyphene, danazol, phenobarbital, primidone, many other

A

Carbamazepine

Toxicities, Interactions

25
Q

GABA derivatives

A

Gabapenin
Pregabalin
Vigabatrin

26
Q

Vigabatrin

A

GABA derivative

27
Q

Pregabalin

A

GABA derivative

28
Q

Gabapenin

A

GABA derivative

29
Q

Gabapenin
Pregabalin

Mechanism of action

A

Decreases excitatory transmission by acting on Voltage gated Ca2+ Channels presynaptically (a2g subunit)

30
Q

Decreases excitatory transmission by acting on Voltage gated Ca2+ Channels presynaptically (a2g subunit)

A

Gabapenin
Pregabalin

Mechanism of action

31
Q

Gabapenin
Pregabalin

Clinical applications

A

Generalized tonic-clonic seizures, partial seizures, generalized seizures

32
Q

Generalized tonic-clonic seizures, partial seizures, generalized seizures

A

Gabapenin
Pregabalin

Clinical applications

33
Q

Valproate

Mechanism of action

A

Blocks high-frequency firing of neurons, modifies amino acid metabolism

34
Q

Blocks high-frequency firing of neurons, modifies amino acid metabolism

A

Valproate

Mechanism of action

35
Q

Valproate

Clinical applications

A

Generalized tonic-clonic seizures, partial seizures, generalized seizures, absence seizures, myoclonic seizures

36
Q

Generalized tonic-clonic seizures, partial seizures, generalized seizures, absence seizures, myoclonic seizures

A

Valproate

Clinical applications

37
Q

Lamotrigine

Mechanism of action

A

Prolongs inactivation of voltage gated (VG) Na+ Channels, acts presynaptically on VG Ca2+ Channels, decreasing glutamate release

38
Q

Prolongs inactivation of voltage gated (VG) Na+ Channels, acts presynaptically on VG Ca2+ Channels, decreasing glutamate release

A

Lamotrigine

Mechanism of action

39
Q

Lamotrigine

Clinical applications

A

Generalized tonic-clonic seizures, generalized seizures, partial seizures, absence seizures

40
Q

Generalized tonic-clonic seizures, generalized seizures, partial seizures, absence seizures

A

Lamotrigine

Clinical applications

Pharma (29 decks)

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