Flashcards in PHARM - anti-epileptic drugs Deck (63)
Loading flashcards...
1
4 types of AEDs
- Na blockers
- Ca blockers
- GABA agonists
- glutamate antagonists
2
Na blockers
- phenytoin
- carbamazapine
- valproate
- topiramate
- lamotrigine
3
Ca blockers
ethosuximide
4
GABA agonists
- topiramate
- barbs
- benzos
- gabapentin?
5
glutamate antagonists
- topiramate
- lamotrigine
6
absorption is essentially complete for all AEDs except...
gabapentin, which has a saturable transporter at high doses
7
speed of AED absorption
- takes hours
- slowed by food
8
TIs in AEDs
generally good but hard to compare
9
typical cytochrome P-450 enzymes
2C9, 2C19, 3A4
10
some UGTs and what they metabolize
1A9 - valproate
2B7 - valproate, lorazepam
1A4 - lamotrigine
11
what do cytochrome P-450 inducers do?
- increase clearance and decrease steady state concentrations of other drugs
- phenobarbitol, ethosuximide, phenytoin, carbamazepine, tobacco
12
what do cytochrome P-450 inhibitors do?
- decrease clearance and increase steady state concentrations of other drugs
- erythromycin, valproate, fluconasol, trimethoprim, Ca blockers
13
what pharmacokinetic factors change in the elderly?
distribution - more fat, less albumin
metabolism slowed - less hepatic enzyme, less blood flow
excretion - less renal clearance
14
pharmacokinetic factors in pediatrics
neonates - need lower doses, low protein binding and metabolic rate
children - need higher per kg doses, faster metabolism
15
pharmacokinetic factors in pregnancy
- increased volume of distribution
- low serum albumin, but may not affect free drug level
- faster hepatic metabolism
- may need higher AED doses, but not as high as predicted
16
drug of choice for pregnancy
lamotrigine, few side effects
17
AEDs that cause weight gain
gabapentin, valproate, carbamazepine
18
AEDs that cause weight loss
topiramate
19
AEDs associated with PCOS
- carbamazepine
- valproate
20
AEDs associated with osteoporosis
- phenobarbitol
- carbamazepine
- phenytoin
21
phenobarbitol effective for:
all seizure types but absence
22
phenobarbitol mechanism
GABA agonist, opens Cl channels for hyper polarization
23
phenobarbitol metabolism
- PO or IV
- inducer
- hepatic metabolism
- needs to be loaded
- half life 100hrs
24
phenobarbitol toxicity
- hyperactivity in children
- sedation in adults
- joint problems
25
phenytoin used for
- all seizure types except absence
- better for localized and secondary generalized than for primary generalized
26
phenytoin mechanism
blocks voltage gated Na channels
27
phenytoin metabolism
- IV or PO, PO bad in children
- inducer
- zero order kinetics at high doses due to enzyme saturation
- half life 6-24hrs
- hepatic metabolism
28
phenytoin toxicity
- gingival hyperplasia
- ataxia
- osteomalacia
29
benzo used for
- everything
- especially status epilepticus, alcohol seizure and withdrawal
- sedative and anxiolytic
30
