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