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Anticonvulsants
Drugs for the treatment and prevention of Epilepsy
20
Pharmacology
Professional
11/09/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Conventional agents
Definition

Phenobarbital

Phenytoin

Carbamazepine

Valproate, Divalproex

Ethosuximide

Benzodiazepines (diazepam, lorazepam, clonazepam)

Term

2nd Generation Anticonvulsants

 

Definition

Felbamate

Lamotrigine

Gabapentin

Pregabalin

Topiramate

Tiagabine

Levetiracetam

Zonisamide

Lacosamide

Rufinamide

Term

Phenobarbital

-mechanism

-primary use

-side effects

Definition

Mechanism:

- enhances GABA effects via ↑ Cl channel opening time

- ↓ Ca2+ channel activity → ↓ excitatory neurotransmitter release


Primary Use:

- generalized tonic-clonic seizures


Side effects:

- enzyme induction → reduced plasma levels of many drugs

- cognitive deficits in children, cleft palates

Term

Phenytoin

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- enhanced sodium channel inactivation


Primary use:

- generalized and partial seizures


Side effects:

- within therapeutic levels:

   ~ gingival hyperplasia

   ~ folate deficiency

   ~ hypertrichosis

   ~ cystic acne


- out of therapeutic levels:

   ~ nystagmus, ataxia, deminished cognitive function

   ~ enzyme induction, protein displacement

   ~ thrombocytopenia

   ~ lupus-like syndrome

   ~ fetal anticonvulsant syndrome


Notes:

- contraindicated in absence seizures


Term

Carbamazepine

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- prolonged recovery of voltage-gated Na channels

 

Primary use:

- partial seizures

- generalized tonic-clonic seizures

- trigeminal neuralgia

 

Side effects:

- N&V

- diplopia

- leukopenia

- thrombocytopenia

- enzyme induction

- neural tube defects

 

Notes:

- autoinduction

- oxycarbazepine is analog of CBZ that is not metabolized to epoxide

Term

Valproate

Divalproex

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- prolonged recovery of voltage-gated Na-channels

- inhibits T-type Ca-channels

- inhibits GABA metabolism and reuptake

- stimulates GABA synthetic enzymes

 

↑ Na-channel inactivation and ↑ [GABA] (net effects)

 

 

Primary Use:

- most major seizure types including absence

 

Side effects:

- weight gain

- hepatotoxicity

- thrombocytopenia

- enzyme inhibition

- fetal anticonvulsant syndrome

- neural tube defects

- metabolic defects

 

Notes:

- caution in patients with diabetes mellitus or gout

Term

Ethosuximide

-mechanism

-primary use

-side effects


Definition

Mechanism:

- blockade of T-type Ca-channels

 

Primary use:

- absence seizures

 

Side effects:

- drowsiness

- GI effects

- mood changes

Term

Benzodiazepines

(Diazepam, lorazepam, clonazepam)

-mechanism

-primary use

-side effects

Definition

Mechanism:

- enhanced GABA binding → increased frequency of Cl channel openings

 

Primary use:

- Status epilepticus and EtOH WD (diazepam and lorazepam)

- akinetic and myoclonic seizures, Lennox-Gastaut (clonazepam)

 

Side effects:

- drowsiness

- abuse

- tolerance

Term

Lamotrigine

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- inhibits sustained repetitive firing of Na-channels

 

Primary use:

- adjunctive for complex partial seizures

 

Side effects:

- Stevens-Johnson syndrome

 

Notes:

- interacts with valproate to increase risk of S-J syndrome

Term

Gabapentin

-mechanism

-primary use

-side effects

Definition

Mechanism:

- binds to α2δ subunit of Ca-channel and decreases Ca2+ influx

 

Primary use:

- adjunctive for complex partial seizures

Term

Pregabalin

-mechanism

-primary use

Definition

Mechanism:

- binds to α2δ subunit of Ca-channel and decreases Ca2+ influx

 

Primary use:

- adjunctive for complex partial seizures

Term

Topiramate

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- inhibition of Na-channels

 

Primary use:

- complex, partial

- generalized tonic-clonic seizures

- Lennox-Gestaut

 

Side effects:

- renal calculi

- oligohydrosis

- glaucoma

 

Notes:

- also used for migraine prophylaxis

Term

Levetiracetam

-mechanism

-primary use


Definition

Mechanism:

- binds selectively to SV2A (synaptic vesicle protein)

- may modify release of glutamate and GABA

 

Primary use:

- adjunctive for complex partial seizures

Term

Zonisamide

-mechanism

-primary use

-side effects


Definition

Mechanism:

- inhibits T-type Ca-channels

 

Primary use:

- adjunctive for complex partial seizures

 

Side effects:

- renal calculi

- oligohydrosis

- rash

Term
Adjunctives for complex-partial seizures
Definition

Gabapentin

Pregabalin

Lamotrigine

Tiagabine

Levetiracetam

Zonisamide

Lacosamide

Term
Enhanced Na+ channel inactivation agents
Definition

Phenytoin

Carbamazepine

Divalproex

Lamotrigine

Zonisamide

Term
Agents reducing current through T-type Ca2+ channels
Definition

Divalproex

Zonisamide

Term
Agents enhancing GABA transmission
Definition

Benzodiazepines

Barbituates

Gabapentin

Divalproex

Term
Agents reducing excitatory neurotransmitter release or receptor blockade
Definition

Phenobarbital

Topiramate

Levetiracetam

Term

Oxcarbazepine

-mechanism

-primary use

-side effects

-notes

Definition

Mechanism:

- prolonged recovery of voltage gated Na-channels

 

Primary use:

- partial seizures

 

Side effects:

- SJS

- N&V

- diplopia

- hyponatremia is worse than carbamazepine

 

Notes:

- reduces blood concentration of oral contraceptives

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