Drugs used in the treatment of epilepsy Flashcards
At what age can sodium valproate be given?
Valproate can be safely used in children down to 1 month of age.
What kind of seizures can sodium valproate be used for?
Generalised, mixed and partial seizures
When is sodium valproate contraindicated?
Severe hepatic or renal failure
How does sodium valproate work?
Sodium valproate acts by weakly blocking sodium ion channels. It inhibits GABA transaminase, which would deactivate gamma-Aminobutyric Acid (GABA) and may also stimulate GABA synthesis.
Where is valproic acid metabolised?
The liver
75% by the CYP450 system
What is valproic acid at room temperature?
Liquid fatty acid but it can be reacted with a base to form a solid salt.
How does valproic acid affect platelets?
Interferes with platelet aggregation and can cause blood disorders
How many days until valproic acid treatment is effective?
14 days
Can valproic acid be used to treat migraines?
Yes
What effect does phenytoin have on the enzyme intestinal conjugase?
It inhibits intestinal conjugase and this causes folate deficiency.
What is phenytoins half life?
6 - 24hrs
Is phenytoin a CYP450 enzyme inducer or inhibitor?
Inducer
What are the CVS effects of phenytoin?
Hypotension and arrhythmias so should be administered with cardiac monitoring if giving IV.
What effect does phenytoin have on blood glucose?
Phenytoin can cause hyperglycaemia & glycosuria due to insulin inhibition
How protein bound is phenytoin?
Highly protein bound, mainly to albumin
What kind of kinetics does phenytoin undergo?
Phenytoin follows saturatable first order kinetics which converts to zero order kinetics when the enzyme system is overwhelmed.
It has a narrow therapeutic index and blood levels are therefore monitored.
What does SEs does phenytoin toxicity cause?
Toxicity causes blurred vision, mydriasis and brisk tendon reflexes.
What is the oral bioavailability of phenytoin?
Bioavailability is good, but oral absorption is slow, variable & can be only partial.
Volume of distribution is approx 70% of body weight.