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Anti-Epilepsy Drugs - updated
Pharm Assessment 12
43
Pharmacology
Graduate
01/25/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
What are the Hydantoins?
Definition

Phenytoin

Fosphenytoin

Term
What is the Mechanism of Action of the Hydantoins? (Phenytoin, Fosphenytoin)
Definition

Stabilizes voltage-gated Na channels in inactivated state Blocks Ca channels to lesser extent

(at higher concentrations)

Term
What anti-epilepsy drug inhibits phenytoin metabolism?
Definition
valproate
Term
How does the rate of elimination vary with Phenytoin?
Definition
Dose-dependent Intially First order Later Zero order
Term
What drug does phenytoin compete with for CYP2C9?
Definition
Warfarin
Term
What drugs does Phenytoin reduce?
Definition

Carbamazepine

Oral Contraceptives

Term
What chronic toxicities can present with Phenytoin use in children?
Definition

Gingival hyperplasia

Coarsened facial features

Hirsutism

Term
What is Fosphenytoin?
Definition
Water soluble phosphoester of phenytoin
Term
What was the 1st non-sedative anticonvulsant? What is it used to treat?
Definition

Phenytoin

 

Simple or Complex Partial seizures

Generalized tonic-clonic seizures

Term
What is Fosphenytoin indicated for?
Definition

Acute treatment of Status Epilepticus

 

Partial and generalized tonic-clonic if parenteral route is wanted

Term
What are the Barbiturates used for seizures?
Definition
Phenobarbital
Term
What is Phenobarbital used to treat?
Definition

Partial seizures

Generalized Tonic-clonic

Term
What is the mechanism of the Barbiturates? (Phenobarbital)
Definition

Enhances GABA-A receptor mediated Cl- flux by prolonging opening of channel

 

Blocks AMPA receptors- less extent

 

Block Na and Ca channels - High conc.

Term
What drug interactions does Phenobarbital have?
Definition

Inducer of CYP2B6 and UGTs

 

Enhancing metabolism of many AEDs

 

Reduce effect of Oral Contraceptives

Term
What AED is related to TCAs and is used as a mood-stabilizer for manic depressive disorder?
Definition
Carbamazepine
Term
What is the drug of choice for partial seizures?
Definition

Carbamazepine

 

Also used for generalized tonic-clonic seizures

Term
What is the mechanism of Carbamazepine?
Definition

Inhibition of Na channels

 

Prolongs recovery from inactivated state

Term
How is Carbamazepine metabolized?
Definition

by CYP2C9 and CYP3A4 to an Active metabolite

 

Clearance slow after inital dose, becomes faster with increaseing dose

Term
What are common side effects of Carbamazepine?
Definition

Blood Dyscrasias

Diplopia and ataxia

Term
What drugs decrease Carbamazepine levels?
Definition

Phenytoin

Phenobarbital

Term
What Drugs does Carbamazepine decrease?
Definition

Levels of Valproate, Lamotrigine, Tigabine, Topiramate Haloperidol

 

Efficacy of Oral Contraceptives

Term
What drugs decrease the metabolism of Carbamazepine?
Definition

Propoxyphene

Erythromycin

Cimeticine

Fluoxetine

Isoniazid

Term
What is the drug of choice for Absence seizures?
Definition
Ethosuximide
Term
What drug inhibits the low threshold T-type Ca current in thalamic neurons?
Definition
Ethosuximide
Term
What are the Pharmacokinetics of Ethosuximide?
Definition

Complete absorption from GI

Does not penetrate Fat

Not Protein Bound

Metabolized by hydroxylation

Slow clearance

Term
What drug can decrease the clearance of Ethosuximide if co-administered?
Definition
Valproic Acid
Term
Why is Valproic Acid Effective in the treatment of absence, myoclonic, partial and tonic-clonic seizures?
Definition

Stabilizes inactive Na Channels

 

Decreases Ca current in thalamic neurons

 

Stimulate GABA synthesis + inhibit GABA degradation

Term
What does Valproic Acids inhibition of UGTs cause?
Definition
inhibits its own metabolism
Term
What drugs have reduced metabolism from Valproate's inhibition of CYP2C9?
Definition

Phenobarbital

Phenytoin

Carbamazepine

Term
What Benzodiazepines are used for the treatment of seizures?
Definition

Clonazepam

Diazepam

Lorazepam

Term
What Benzodiazepine is used for absence, myoclonic, and atonic seizures?
Definition
Clonazepam
Term
What is the drug of choice given IV for status epilepticus?
Definition
Diazepam
Term
What Benzodiazepine can be given IV for status epilepticus, and is longer acting than the Drug of Choice for status epilepticus?
Definition
Lorazepam
Term
What is the mechanism of the Benzodiazepines?
Definition
Potentiates GABA-A receptor function by increasing the probability of chloride channel opening
Term
What drug is an analog of GABA, and may increase GABA release? What is it used for?
Definition

Gabapentin

 

Adjunct for partial seizures, neuropathic pain and neuralgia

Term
What anti-seizure drug is used as an adjuct of mono-therapy in refractory partial seizures, with or without secondary generalized tonic-clonic seizures?
Definition
Topiramate
Term
What is the mechanism of Topiramate?
Definition

Inhibits voltage-gated Na channels & decreases Ca current

 

Enhances GABA-A receptor currents

 

Inhibits AMPA-kainate receptors

Term
What AED has broad spectrum activity against infantile spasm, myoclonic, and generalized and atypical absence seizures?
Definition
Zonisamide
Term
Parital, Simple or Complex (with secondarily generalized) 1st choice 2nd Choice
Definition

Carbamazepine

 

Phenytoin, Valproate, Gabapentin, Zonisamide

Term
Generalized tonic-clonic 1st Choice 2nd Choice
Definition

Carbamazepine

 

Phenytoin, Valproate

Term
Absence 1st choice 2nd choice
Definition

Ethosuximide

 

Valproate

Term
Atypical Absence, Myoclonic, Atonic 1st choice 2nd Choice
Definition

Valproate

 

Clonazepam

Term
Status Epilepticus

1st choice
2nd choice
Definition
Diazepam

Lorazepam
Phenytoin
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