Antiseizure Drugs Flashcards
1
Q
Which antiseizure medication is excreted in the urine largely unchanged?
A
Gabapentin
2
Q
Which antiseizure medication is bound to plasma proteins the least?
A
Gabapentin
3
Q
Phenytoin
- Mechanism of Action:
- Pharmacokinetics:
A
-
MECHANISM OF ACTION:
-
Alters Na ion conductance
- Use dependent effect on sodium channels
- Inhibits the generation of repetitive action potentials
-
Alters Na ion conductance
-
PHARMACOKINETICS:
- Dependent upon drug formulation
- Highly protein bound
- Pharmacokinetics are dose-dependent
- Usual therapeutic level – 10 -20 μg/ml
4
Q
What are the **clinical uses **of phenytoin?
A
- Generalized tonic-clonic seizures
-
Partial seizures
- NOT absence seizures
5
Q
Phenytoin
- Drug Interactions
- Toxicity
A
-
Drug interactions
- drugs metabolized by microsomal enzymes
- drugs that are protein bound
-
Toxicity
- CNS (Dose-dependent) – nausea, anorexia, apathy, sedation, ataxia, nystagmus and diplopia.
- Gingival hyperplasia
- Hirsuitism
- Teratogenicity -fetal hydantoin syndrome-cardiac defects, cleft palate
- Hypersensitivity reactions - Rash
6
Q
Which of the toxicities caused by phenytoin is not dose dependent?
A
- gingival hyperplasia
- hypersensitivity reaction (rash)
7
Q
What is fosphenytoin and when is it used?
A
- Water soluble phenytoin analog
- Used IV in status epilepticus
8
Q
Carbamazepine
- **Mechanism of Action **
- Pharmacokinetics
- Clinical Use
A
-
Mechanism of Action (similar to phenytoin)
- blocks Na channels
- does not interact with GABA
-
Pharmacokinetics
- unpredictable absorption
- hepatic enzyme induction
-
Clinical Use
- drug of choice for partial seizures
- contraindicated in absence seizures
9
Q
Carbamazepine
Toxicity
A
Dose related
- diplopia and ataxia
- GI upset
- drowsiness
- rare blood discrasias
-
teratogen
- increased incidence of Spinal Bifida
- risk is less than with valproic acid
10
Q
What is oxcarbazepine?
A
- Newer analog
- Similar in action, but less likely to cause CNS side effects
- Less enzyme induction than carbamazepine
11
Q
Ethosuximide
- **Mechanism of Action **
- **Pharmacokinetics **
A
- **Mechanism of Action **
- Reduces low-threshold (T type) Ca currents in thalamic nuclei
- **Pharmacokinetics **
- Well absorbed after oral administration
-
Not protein bound
- Volume of distribution approximaes total body water
- Liver metabolism (inhibited by valproic acid)
- Long half life
12
Q
What are the side effects/toxicity of ethosuximide?
A
- Gastric distress (dose twice daily)
- Lethargy & fatigue
13
Q
Valproic Acid
- Mechanism of Action
- Pharmacokinetics
A
-
Mechanism of Action
- Blocks repetitive neuronal firing
- May reduce T-type Ca2+ currents
- Increases GABA concentrations
-
Pharmacokinetics
-
Bound to plasma protein
- competes with phenytoin
- Distributes to ECF
- Inhibits metabolism of phenobarbital, phenytoin and carbamazepine
-
Bound to plasma protein
14
Q
Valproic Acid
- Clinical Uses
- Side Effects & Toxicity
A
-
Clinical Use
- Absence seizures
- Absence seizures w/ concomitant-generalized tonic-clonic seizures
- Generalized tonic-clonic seizures and partial seizures
- Myoclonic seizures
-
Side Effects & Toxicity
- GI upset
- weight gain, hair loss
- idiosyncratic hepatotoxicity
- teratogen – spinal bifida
15
Q
What side effects/toxicity caused by valporic acid are not dose-related?
A
- idiosyncratic hepatotoxicity
- teratogenicity