PHARM - anti-epileptic drugs Flashcards Preview

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Flashcards in PHARM - anti-epileptic drugs Deck (63)
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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

benzo mechanism

GABA agonist