Antiseizure Drugs Flashcards Preview

Pharma > Antiseizure Drugs > Flashcards

Flashcards in Antiseizure Drugs Deck (41):
0

Cyclic ureides

Phenytoin
Fosphenytoin
Phenobarbital
Ethosuximide

1

Phenytoin
Fosphenytoin

Mechanism of action

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

2

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

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

Mechanism of action

3

Phenytoin
Fosphenytoin

Pharmacokinetics

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

4

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

Phenytoin
Fosphenytoin

Pharmacokinetics

5

Phenytoin, Fosphenytoin

Clinical applications

Generalized tonic-clonic seizures, partial seizures

6

Generalized tonic-clonic seizures, partial seizures

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

Clinical applications

7

Phenytoin
Fosphenytoin

Toxicities, Interactions

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

8

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

Phenytoin
Fosphenytoin

Toxicities, Interactions

9

Ethosuximide

Mechanism of action

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

10

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

Ethosuximide

Mechanism of action

11

Ethosuximide

Pharmacokinetics

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

12

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

Ethosuximide

Pharmacokinetics

13

Ethosuximide

Clinical applications

Absence seizures

14

Absence seizures

Ethosuximide

Clinical applications

15

Ethosuximide

Toxicities, Interactions

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

16

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

Ethosuximide

Toxicities, Interactions

17

Tricyclics

Carbamazepine
Oxcarbazepine
Eslicarbazepine acetate

18

Carbamazepine
Oxcarbazepine
Eslicarbazepine acetate

Tricyclics

19

Carbamazepine

Mechanism of action

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

20

Carbamazepine

Pharmacokinetics

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

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

Carbamazepine

Pharmacokinetics

22

Carbamazepine

Clinical applications

Generalized tonic-clonic seizures, partial seizures

23

Carbamazepine

Toxicities, Interactions

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

24

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

Carbamazepine

Toxicities, Interactions

25

GABA derivatives

Gabapenin
Pregabalin
Vigabatrin

26

Vigabatrin

GABA derivative

27

Pregabalin

GABA derivative

28

Gabapenin

GABA derivative

29

Gabapenin
Pregabalin

Mechanism of action

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

30

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

Gabapenin
Pregabalin

Mechanism of action

31

Gabapenin
Pregabalin

Clinical applications

Generalized tonic-clonic seizures, partial seizures, generalized seizures

32

Generalized tonic-clonic seizures, partial seizures, generalized seizures

Gabapenin
Pregabalin

Clinical applications

33

Valproate

Mechanism of action

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

34

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

Valproate

Mechanism of action

35

Valproate

Clinical applications

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

36

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

Valproate

Clinical applications

37

Lamotrigine

Mechanism of action

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

38

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

Lamotrigine

Mechanism of action

39

Lamotrigine

Clinical applications

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

40

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

Lamotrigine

Clinical applications