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22 Cards in this Set
- Front
- Back
What are the original six anti-epileptic drugs?
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1. Phenobarbital
2. Phenytoin 3. Ethosuximide 4. Diazepam 5. Carbamazepine 6. Valproate |
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What do we know now about the basic targeting of the anti-epileptic drugs?
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Targets neurotransmitters to slow excitatory glutamate transmission or enhance the inhibitory (GABA) transmissions
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2 main problems with phenobarbital?
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Besides sedation
1. Respiratory depression 2. Abuse and addiction potential |
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What is the main difference between Phenytoin vs. Phenobarbital?
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phenytoin inhibits excitation whereas Phenobarbital enhances inhibition
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Which drugs antagonize voltage gated Na channels?
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PHT, CBZ, VAL
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Explain in detail the mechanism of phenytoin and carbamazepine...
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antagonists of voltage-dependent Na channels which blocks depolarization and vesicle fusion and release
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Phenytoin & carbamazepine uses
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Primiary drug carbamazepine for treatment of epilepsy except absence seizures
- more tolerability and efficacy is better with Carbamazepine |
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Complications with phenytoin
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zero order pharmacokinetics- yet does adjustment is difficult
Also... 1. CYP 450 enzymes 2. GINGIVAL HYPERPLASIA 3. HIRSUTISM 4. HYPOCALCEMIA 5. OSTEOPOROSIS |
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Complications with carbamazepine
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1. CYP 450 enzymes
2. LEUKOPENIA 3. NEUTROPENIA 4. THROMBOCYTOPENIA (INFECTIONS, BRUISING) - very narrow therapeutic window which leads to loss of efficacy and induction of seizures |
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Starting carbamazepine needs to be careful for women on what drug and why?
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Women on Oral Contraceptives are cleared faster thus 4x increase risk of pregnancy
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Pt. has heart attack and then was put on anti-coag what problem does carbamazepine do?
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increases clearance of warfarin and causes rapid coagulation
Also increases clearance of statins |
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What causes typical absence seizures?
Drugs to treat it? |
disruption of T-type Ca ion channels
- Ethosuxmide and Valproate |
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Complications with Valproate?
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weight gain
hepatotoxicity |
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Status epilepticus what is DOC?
What if seizure does not stop? |
use benzodiazapam to stop seizure/eeg bursts by GABA-ergic agents that increase inhibition
- Lorazepam/diazepam - if seizure does not stop use fosphenytoin |
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MOA for BZD (benzodiazepines)
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bind to distinct site which potentiates GABA binding and opens Cl channels
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List the new AEDs
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Gabapentin
Lamotrigine Topiramate Tiagabine Oxcarbazepine Levetiracetam Zonisamide Pregabalin |
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Two broadspectrum agents
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Topirimate
Valproic acid |
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Topiramate MOA
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receptor antagonist of glutamate
also a GABAa receptor agonist |
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MOA of tiagabine
MOA of valproate |
- inhibits GABA re-uptake
- Valproate inhibits GABA metabolism |
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Which drugs inhibit conjugation of drugs by UGT enzymes?
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valproate and lamotrigine- causing accumulation of parent drug
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Black box warning are in what two drugs?
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CArbamazepine- Life-threatening
• Allergic reaction (Stevens-Johnson syndrome) • Aplastic anemia LAmotrigine- allergy (steven Johnson syndrome) |
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Which drug is associated with major congenital malformations
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Valproic acid
1. spina bifida 2. Atrial septal defect |