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7/28/2019 Antiseizure Agents & Effects
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ANTISEIZURE AGENTS & EFFECTS
Group 3
Munyadi, Muneeslaxmi
Singh, Ruby
Austin, Nissy
Khader Basha
Augustus, Joel
Jayabalan, Jerusha
Darapastham Finny1
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Topic Outlines
Introduction
Drugs Overview
Data Collection
Q & A
Conclusion
2
3-7
8-11
12-15
16-21
22
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INTRODUCTION
What is seizure ?
Seizure results from abnormal neuronal discharge in the CNS
produced by either focal or generalized disturbances of brain
tissue.
Seizure results in abnormal phenomena of
motor (convulsion), sensory, autonomic, or psychic origin
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INTRODUCTION
Etiology & Mechanism
1. Activity of voltage-gated ion channels ( Na+, K+ & Ca++ channels)
2. Inhibitory (GABA) neurotransmission
3. Excitatory neurotransmission (Glutamate receptors)
4. Alteration of extracellular ion concentration (Potassium, calcium).
4
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INTRODUCTION
Types of Seizure
A. Partial Seizure B. Generalized Seizure
The discharge begins locally,
often remains localized.Produce relatively simple
symptoms w/o loss of
Consciousness.
Involve the whole brain,
including the reticular system,producing abnormal electrical
activity throughout both
hemispheres. Immediate loss
of consciousness5
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INTRODUCTION
Antiseizure Agents
They are a diverse group of pharmaceuticals used in the
treatment of epileptic seizures.
The nerve-calming qualities of some of these drugs can alsohelp quiet the burning, stabbing or shooting pain often
caused by nerve damage.
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INTRODUCTION
MOA of Antiseizure
Agents
1. Prolong inactivation of voltage-dependent Na+ channels in a use-
dependent fashion.
2. the effectiveness of inhibitory GABA transmission via the GABAA
receptor.
3. Inhibition of Ca++ currents through T-type Ca++ channels.
4. Inhibition of excitatory glutamate transmission via ionotropic
receptors. 7
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DRUGS OVERVIEW
1. Nicotine
Nicotine is taken by smoking or chewing tobacco.
Nicotine's mood-altering effects are different by report: in
particular it is both a stimulant and a relaxant. Release ofglucose from the liver and epinephrine (adrenaline) from the
adrenal medulla, it causes stimulation.
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DRUGS OVERVIEW
2. Phenobarbital
Phenobarbital is in a class of medications called barbiturates
which is used to control seizures. It is also used to prevent
withdrawal symptoms in people who are dependent onanother barbiturate medication and are going to stop taking
the medication.
It works by slowing activity in the brain.9
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DRUGS OVERVIEW
3. Phenytoin
Phenytoin is in a class of medications called anticonvulsants.
It is used to control certain type of seizures, and to treat and
prevent seizures that may begin during or after surgery tothe brain or nervous system.
It works by decreasing abnormal electrical activity in the
brain.10
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DRUGS OVERVIEW
4. Diazepam
Diazepam belongs to a group called benzodiazepines.
Diazepam is used to relieve anxiety, muscle spasms, andseizures and to control agitation caused by alcohol
withdrawal.
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DATA COLLECTION
(Group 1)
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DRUGS
EFFECTS
ONSET OF
ACTION
DURATION
OF ACTIONSEIZURE SLEEP AROUSAL
Nicotine +++ - +++ 20 secs 20 mins
Phenobarbital
+ Nicotine
++ - ++ 1 min 20 secs 1 min
Nicotine +
Phenobarbital
+ - + 15 secs 8 mins
Nicotine +
Phenytoin
++ - +++ 12 secs 12 mins
Nicotine +
Diazepam
++ - ++ 10 secs 15 mins
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DATA COLLECTION
(Group 2)
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DRUGS
EFFECTS
ONSET OF
ACTION
DURATION
OF ACTIONSEIZURE SLEEP AROUSAL
Nicotine + ++ +++ 13 mins 19 mins
Phenobarbital
+ Nicotine
+ + + 15 mins 25 mins
Nicotine +
Phenobarbital
+++ ++ ++ 15 mins 17 mins
Nicotine +
Phenytoin
++ ++ ++ 15 mins 17 mins
Nicotine +
Diazepam
++ ++ ++ 7 mins 10 mins
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DATA COLLECTION
(Group 3)
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DRUGS
EFFECTS
ONSET OF
ACTION
DURATION
OF ACTIONSEIZURE SLEEP AROUSAL
Nicotine + - +++ Immediate 7 mins
Phenobarbital
+ Nicotine
+ - ++ Immediate 1 min
Nicotine +
Phenobarbital
+ - ++ 30 secs 3 mins
Nicotine +
Phenytoin
+ - +++ 25 secs 2 mins
Nicotine +
Diazepam
+ - ++ 15 secs 2 mins
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DATA COLLECTION
(Group 4)
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DRUGS
EFFECTS
ONSET OF
ACTION
DURATION
OF ACTIONSEIZURE SLEEP AROUSAL
Nicotine + ++ ++ 1-3 mins 7-8 mins
Phenobarbital
+ Nicotine
++ ++ + Immediate 5-7 mins
Nicotine +
Phenobarbital
- - +++ 1-2 mins 5 mins
Nicotine +
Phenytoin
+ - +++ 40 secs 2 mins
Nicotine +
Diazepam
+ - +++ 30 secs 2 mins
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Q & A
1. Drug of choice for status
epilepticus in children and
adults?
The general principles of management & the initial agents used in
the pediatric patients remain same as for adults.
Differences between adults and childrena. Etiology of status epilepticus in children differ from adults
b. Prognosis of status epilepticus is better in children than
adults.
c. Refractory of status epilepticus in children seems more
similar to that in adults16
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Q & A
17
Medications class Available routes Adverse effects Advantages Disadvantages
Lorazepam
Intravenous
Rectal
Sublingual
Intramuscular
Respiratory depression
Hypotension
Decreased level of
conciousness
Prepared agent
Longer duration of action
May have least respiratory
depression of its class
Slightly longer delay in
brain uptake
Need for refrigeration
Diazepam
Intravenous
Rectal(gel form)
Intra muscular
Respiratory depression
Hypotension
Decreased level ofconciousness
Slightly faster onset of
action
Rectal examination isdone in children
Short DOA
Second line drug is
needed
Midazolam
Intravenous
intramuscular
Respiratory depression
Hypotension
Decreased level of
conciousness
Additional intramuscular
route
Short DOA
additional drug is needed
Phenytoin
intavenous Hypotension
QT prolongationPurple glove syndrome
Low cost Adverse effect profile
Fosphenytoin
Intravenous
Intramuscular
Hypotension
Cardiac arrythmias
Possibly fewer adverse
effects
Expensive
Phenobarbital
Intravenous Respiratory depression
Hypotension
Decreased level of
conciousness
Long acting Long half life
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Q & A
1. Drug of choice for status
epilepticus in children and
adults?
Initial drug of choice is : IN CHILDREN
Lorazepam iv 0.05-0.1mg/kgOrDiazepam iv 0.2-0.5mg/kg
Initial drug of choice is : IN ADULTS
Lorazepam iv 0.10.15 mg/kg OrDiazepam iv 0.3 mg/kg ,0.50.7
mg/kg recta18
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Q & A
2. Give the drugs used to
treat seizures. MOA
tabulation and specific uses
Carbamazepine
Phenobarbital
Phenytoin Primidone
Valproic acid
Lamotrigine
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Q & A
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DRUGS MOA SPECIFIC USES
Carbamazepine (Tegretol) Carbamazepine stabilizes the
inactivated Na channels. This leaves
the affected cells less excitable until
the drug dissociates.
Treating trigeminal neuralgia (a
condition that causes facial nerve
pain).
Phenobarbital (Luminal) The primary action of phenobarbital isto enhance the inhibitory actions of
(GABA) on neurons .
Prevent withdrawal symptoms inpeople who are dependent on another
barbiturate medication and are going
to stop taking the medication.
Phenytoin (Dilantin) Block Na channels, therefore limit
repetitive firing of action potentials.
Prevent seizures that may begin
during or after surgery to the brain or
nervous system.
Primidone (Mysoline) Stimulate or increase the action at the
GABA receptor.
Treatment of tremors, specifically,
essential tremor (ET), the most
common movement disorder.
Valproic Acid (Depakote) Blocks Na channels, augment the
action of GAD, , it restricts GABA-T .
Treat bipolar disorder. It is also used to
prevent migraine headaches .
Lamotrigine (Lamictal) Inhibit release of glutamate andaspartate evoked by the Na-channel Treat bipolar disorder.
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Q & A
3. MOA of nicotine
Nicotine binds to nicotinic acetylcholine receptors channels
open depolarization activate Ca channel dopamine
release epinephrine release = vasoconstriction, BP,blood sugar, rate.
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CONCLUSION
Nicotine diminishes the anticonvulsant activity of antiseizure drugs.
The combination of both nicotine and antiseizure drugs should be
carefully considered as a cause of therapeutic failure in epileptic
patients.
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SEE YOU ALL IN 2ND SEMESTER
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