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Anti-Convulsants
Anti-Convulsant info and drugs
39
Pharmacology
Undergraduate 2
02/18/2011

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Term
Convulsion
Definition
Sudden attack of involuntary muscular contractions and relaxations
Term
Seizure
Definition
Abnormal central nervous system electrical activity
Term
Epilepsy
Definition
A group of recurrent disorders of cerebral function characterized by both seizures and convulsions
Term
Neurological disorder affecting the CNS
Definition
Epilepsy
Term
Glutamate
Definition
Excitatory (tells the neuron to fire)
Term
GABA
Definition
Inhibitory (dampens the neuron firing rate)
Term
Action Potential
Definition
Electrical signal that travels down the axon, and is created using sodium ions (Na+) and inhibited by potassium ions (K+)
Term
Seizures occur when _______________
Definition
Excitatory and inhibitory processes dysfunction and abnormal electrical activity occurs (i.e. abnormal action potentials)
Term
Simple Partial (focal) Seizures
Definition
Excessive electrical activity in ONE cerebral hemisphere

-Affects only part of the body

-Key feature: PRESERVATION OF CONSCIOUSNESS
Term
Complex Partial (focal) Seizure
Definition
Excessive electrical activity in ONE cerebral hemisphere

LOSS OF AWARENESS at seizure onset. Person seems dazed/confused and exhibit meaningless behavior.

-Originate in FRONTAL or TEMPORAL lobes
Term
Generalized Seizures
Definition
Excessive electrical activity in BOTH cerebral hemispheres

LOSS OF CONSCIOUSNESS

-Originates in THALAMUS or BRAINSTEM

-Affects whole body, whole brain too
Term
Generalized Seizures: Myoclonic
Definition
Brief shock-like muscle jerks generalized or restricted to part of one extremity
Term
GS: Atonic
Definition
Sudden loss of muscle tone
Term
Tonic Seizures
Definition
Sudden stiffening of the body, arms, or legs
Term
GS: Clonic Seizures
Definition
Rhythmic jerking movements of the arms and legs without a tonic component
Term
GS: Tonic-clonic (grand mal)
Definition
Sudden stiffening followed by rhythmic jerking

Tonic phase followed by Clonic phase
Term
GS: Absence (petit mal)
Definition
Person appears to "blank out"/"Daydreaming"

-Simple absence (primarily affects consciousness only)
-Complex absence
-Atypical absence (including physical symptoms like eye blinking or lip movements)
Term
GS: Status Epilepticus
Definition
A seizure lasting longer than 30 minutes, or 3 seizures without a normal period in between

-May be fatal (i.e. stops person from breathing)

-EMERGENCY INTERVENTION REQUIRED
Term
Incidence of seizure types
Definition
Partial = 51%
Generalized = 38%
Term
1. Are seizures life threatening?

2. What stops the seizures?

3. What happens to breathing?
Definition
1. No

2. Brain

3. May cease for a few seconds
Term
1. Pain related to seizures?

2. Mental capacity after seizures?
Definition
1. No pain during seizures, muscle soreness may occur after

2. May be "different" for a while after seizure
Term
Recurrent seizures that cannot be attributed to any cause are seen in patients with __________
Definition
EPILEPSY
Term
Drug of choice depends on _____________
Definition
TYPE OF SEIZURE
Term
Treatment of seizures
Definition
Try to find a cause (i.e. fever, head trauma, drug abuse)
Term
How many percentage of patients with epilepsy can have their seizures controlled with medication?
Definition
More than 80%
Term
Treatment: Monotherapy with anticonvulsant
Definition
-Increase dose gradually until seizures are controlled or adverse effects become unacceptable

-Multiple therapy may be required
Term
Want to achieve _______________ with therapy
Definition
1. Achieve steady-state kinetics

2. Monitor plasma drug levels

3. Avoid sudden withdrawal
Term
3 MAIN MECHANISMS OF ACTION of Anti-convulsants
Definition
1. Inhibition of voltage-gated SODIUM (Na+)channels to show neuron firing

2. Enhancement of the inhibitory effects of the neurotransmitter GABA

3. Inhibition of CALCIUM channels
Term
Adverse Effects
Definition
THERE ARE MANY!! When treating a patient, need to know TYPE OF SEIZURE and what effects they can TOLERATE
Term
Na+ channal inhibitor: PHENYTOIN (Dilantin, Phenytek)
Definition
First choice for partial and generalized tonic-clonic seizures

AE: GINGIVAL HYPERPLASIA (20-40%) treat by brushing teeth 8 times/day

-Primary reason not prescribed to children
Term
Na+ channel inhibitors: ZONISAMIDE (Zonegran)
Definition
Can be used in INFANTS
Term
Na+ Channel Inhibitor: LIDOCAINE
Definition
Only used when other drugs are refractory for STATUS EPILEPTICUS
Term
Enhancement of GABA inhibition: PHENOBARBITAL (Luminal)
Definition
Second choice for partial or generalized tonic-clonic seizures

-May cure one type of seizure but make another worse
Term
Enhancement of GABA Inhibition: BENZODIAZEPINE
Definition
Diazepam (Valium) - VERY painful to inject
Lorazepam (Ativan) - NOT AS painful to inject
Term
CA2+ Channel Blockers
Definition
Most act presynaptically
Term
Voltage-gated CA2+ Channel Blockers: ETHOSUXIMIDE (Zarontin)
Definition
For absent seizures
Term
Blockade of CA2+ channels: GABAPENTIN (Neurotin)
Definition
For Neuropathies
Term
Other/Unknown MOA: Magnesium chloride
Definition
Used for magnesium deficiency seizures
Term
Other/Unknown MOA: PARALDEHYDE
Definition
Alcohol withdrawal seizures
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