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What is the sequence of events involved in neurotransmission from conduction of an action potential through the neuron and ending with release of a neurotransmitter?
1. initial phase
2. second phase
3. exocytosis
What are the target sites of antiepileptic drugs?
Na+
Ca2+
GABA
What is the general underlying cause of seizures?
excessive neural activity in the cerebral cortex
In general, what is the main goal of drugs that treat seizures?
reduce neuronal activity in the brain to control seizures (↓ AP)
What are the underlying causes of epilepsy?
- Stroke, trauma, meningitis, and hyperthermia
- Drug overdose: haloperidol, lidocaine, and alcohol
- Unknown cause: Idiopathic seizure
What is the diagnosis of epilepsy?
- Electroencephalogram (EEG)
- Computer assisted tomography (CT)
- Magnetic resonance imaging (MRI)
What are the 4 classifications with AED? And in each class give one drug as example on quiz
1. Stabilization of inactive voltage-dependent sodium channels
2. Reduced current through T-type calcium channels
3. Inhibition of excitatory neurotransmitters (Glutamate; EPSPs)
4. Enhancement of inhibitory neurotransmitters (GABA; IPSPs)
1. Stabilization of inactive voltage-dependent sodium channels
Carbamazepine
2. Reduced current through T-type calcium channels
Valproate
3. Inhibition of excitatory neurotransmitters (Glutamate; EPSPs)
Lamotrigine
4. Enhancement of inhibitory neurotransmitters (GABA; IPSPs)
Barbiturates
MOA of phenytoin
Na+ channel blocker
What are the PK factors need to be considered for drug monitoring?
- Volume distribution (Vd)
- Bioavailability (F)
- Salt fraction (S)
- Albumin concentration
- Drug clearance
What are the disease factors need to be considered for drug monitoring?
- Aging
- Disease
- Drug interaction
- Pregnancy
What factors are considered for dose adjustment?
- Liver and renal disease
- Obesity
- Metabolism /Clearance
- Age
On quiz/final exam → test on equation (plug in numbers, memorize equation)
loading dose equation
loading dose equation =
(VD) x (desired serum conc)
(S) x (F)
What is the method to determine Vd?
in vitro