Antiepileptic Drug

PRESENTED BY
PRERNA SURANA
YUKTA MEHTA
SARFA MALICK
Introduction to epilepsy

 Epilepsy is the tendency to have seizures that start in the

brain.
 The brain uses electrical signals to pass messages between
brain cells.
 If these signals are disrupted, this can lead to a seizure.
 Epilepsy is usually diagnosed when someone has had more
than one seizure.
Definition
A disorder in which nerve cell activity in the brain is
disturbed, causing seizures.
 Epilepsy may occur as a result of a genetic disorder or an
acquired brain injury, such as a trauma or stroke.
Symptoms

Usually self-diagnosable
 During a seizure, a person experiences abnormal
behaviour, symptoms and sensations, sometimes including
loss of consciousness.
 There are few symptoms between seizures.
Treatment

Medicines used to treat epilepsy

 Carbamazepine, clobazam, clonazepam, eslicarbazepine,

ethosuximide, gabapentin, lacosamide, lamotrigine,
levetiracetam, oxcarbazepine, perampanel, phenobarbital,
phenytoin, pregabalin, primidone, rufinamide, sodium
valproate, tiagabine, topiramate, vigabatrin and
zonisamide
Antiepileptic

Especially of a drug) used to treat

epilepsy.
“anti-epileptic drugs can block
seizures in most patients”
What does antiepileptic
Means
 A drug or other substance used to prevent or stop seizures
or convulsions.
 Also called anticonvulsant.
Neurology singles
Different between
Antiepileptic and anticonvulsant
Difference

 Antiepileptic and anticonvulsant are both terms that refer

to the same drugs that target different neural pathways to
reduce seizure episodes in people with epilepsy disorders.
 Anticonvulsants are another name for antiepileptic drugs,
which are medications used to treat seizure disorders and
help suppress seizures.
Drugs involved in antiepileptic

 The benzodiazepines most commonly used for treatment

of epilepsy are lorazepam, diazepam, clonazepam, and
clobazam.
 The first 2 drugs are used mainly for emergency treatment
of seizures because of their quick onset of action,
availability in intravenous (IV) forms, and strong
anticonvulsant effects
Classification of Antiepileptic drug
1) Barbiturates

A)Phenobarbitone:
 Phenobarbitone also called phenobarbital or phenobarb
 By the trade name luminal is a medication of the barbiturate type
 It is recommended by the WHO for the treatment of certain types of epilepsy in
developing countries.
Phenobarbitone:
Mechanism of action of Phenobarbitone:

 Phenobarbital acts on GABAA receptors, increasing

synaptic inhibition.
 This has the effect of elevating seizure threshold and
reducing the spread of seizure activity from a seizure
focus.
 Phenobarbital may also inhibit calcium channels, resulting
in a decrease in excitatory transmitter release
Adverse effect of Phenobarbitone:

 Dizziness, drowsiness, excitation, headache, tiredness, loss

of appetite, nausea, or vomiting may occur as your body
adjusts to the medication.
 If any of these effects last or get worse, notify your doctor
or pharmacist promptly.
Uses of Phenobarbitone:

 Phenobarbitone is used to control seizures.

 Phenobarbitone is also used to relieve anxiety.
 It is also used to prevent withdrawal symptoms in people
who are dependent ('addicted'; feel a need to continue
taking the medication) on another barbiturate medication
and are going to stop taking the medication.
2)Deoxybarbiturates:

(1)Primidone:
 Primidone is used alone or with other medications to
control certain types of seizures.
 Primidone is in a class of medications called
anticonvulsants.
 It works by decreasing abnormal electrical activity in
the brain.
Primidone
Mechanism of action of Primidone

 The exact mechanism of primidone's anticonvulsant action

is still unknown after over fifty years.
 It is believed to work via interactions with voltage-gated
sodium channels which inhibit high-frequency repetitive
firing of action potentials.
Adevers effects of Primidone

 Dizziness, drowsiness, excitation, tiredness, headache, loss

of appetite, nausea, or vomiting may occur as your body
adjusts to the medication.
 If any of these effects last or get worse, notify your doctor or
pharmacist promptly.
Uses of Primidone:

 Primidone is used alone or with other medications to

control certain types of seizures.
 Primidone is in a class of medications called
anticonvulsants.
 It works by decreasing abnormal electrical activity in the
brain.
3) Iminostilbene

(1)Carbamazepine:

 Carbamazepine is used to treat certain types of seizures

(epilepsy).
 It is also used to relieve pain due to trigeminal neuralgia
(tic douloureux) and in the treatment of bipolar disorder
(manic-depressive illness).
 Carbamazepine works in the brain and nervous system to
control seizures, pain, and bipolar disorder.
Carbamazepine
Mechanism of action of Carbamazepine:

 Carbamazepine is a sodium channel blocker.

 It binds preferentially to voltage-gated sodium channels in
their inactive conformation, which prevents repetitive and
sustained firing of an action potential.
Adverse effect of Carbamazepine:

 difficulty swallowing or breathing.

 headache, new or increased number of seizures, difficulty
concentrating, confusion, weakness, or unsteadiness.
 severe rash with one or more of the following: fever, muscle
or joint aches, red or swollen eyes, blisters or peeling skin,
mouth sores, or swelling of your face or neck.
Uses of Carbamazepine:

 Carbamazepine is used alone or in combination with other

medications to control certain types of seizures in people
with epilepsy.
 Itis also used to treat trigeminal neuralgia (a condition that
causes facial nerve pain).
4) Hydantoin

(1)Phenytoin (diphenylhydantoin):

 Itis anticonvulsant activity was specifically tested in 1938 in the newly

developed electroshock seizure model and till recently it was a major
antiepileptic drug.
 Phenytoin is not a global CNS depressant only mild sedation occurs at
therapeutic doses.
 The most prominent action is abolition of tonic phase of maximal
electroshock seizures with no effect on or prolongation of clinical phase.
 It limits spread of seizure activity
 Threshold for PTZ convulsion is not raised.
 Mechanism of action:
 Phenytoin prevents repetitive detonation of normal brain
cells.
 Phenytoin is believed to protect against seizures by
causing voltage-dependent block of voltage gated sodium
channels.
 This blocks sustained high frequency repetitive firing of
action potentials.
 Adverse effects:
 After prolonged use numerous side effects are produced at therapeutic plasma concentration.
 Over dose toxicity due to higher plasma concentration of phenytoin produce:
1. Cerebellar and vestibular manifestation: ataxia,vertigo,diplopia, nystagmus.
2. Drowsiness,behavioral alterations,mental confusion,hallucinations,disorientation and rigidity.
3. Epigastrie pain,nausea and vomiting
4. Intravenous injection of phenytoin sodium can cause local vascular injury – intimal damage and
thrombosis of the vein – edema and discolouration of the injected limb .
5. Fall in BP and cardiac arrhythmia occur onlyonly iv injection which therefore must be given under
continuous ECG monitoring.
Uses:
1. Phynytoin is used to control seizure (convulsions),including
tonic-clonic(grand mal) and psychomotor (temporal lobe)
seizures, in the treatment of epilepsy.

2. It is also used to prevent and treat seizures that occur during

brain surgery.
5)Succinimide:
(1)Ethosuximide:
 Ethosuximide, sold under the brand name Zarontin among
others, is a medication used to treat absence seizures.
 It may be used by itself or with other antiseizure medications
such as valproic acid.
 Ethosuximide is taken by mouth. Ethosuximide is usually well
tolerated.
Ethosuximide
Mechanism of action of ethosuximide:

 Ethosuximide is in the succinimide family of medications.

 Its mechanism of action is thought to be due to antagonism
of the postsynaptic T-type voltage-gated calcium channel.
 Ethosuximide was approved for medical use in the United
States in 1960.
 It is on the World Health Organization's List of Essential
Medicines.
Adverse effect of ethosuximide:

 nausea.
 vomiting.
 diarrhea.
 stomach pain or cramps.
 loss of appetite.
 weight loss.
 swelling of the tongue.
 overgrowth of the gums.
Uses of ethosuximide:

 Ethosuximide is used to control absence seizures (petit

mal) (a type of seizure in which there is a very short loss
of awareness during which the person may stare straight
ahead or blink his eyes and does not respond to others).
 Ethosuximide is in a class of medications called
anticonvulsants.
6) Benzodiazepam:

 (1) Diazepam:
 Diazepam is used to relieve symptoms of anxiety and
alcohol withdrawal.
 This medicine may also be used to treat certain seizure
disorders and help relax muscles or relieve muscle spasm.
 Diazepam is a benzodiazepin
Diazepam
Mechanism of action of diazepam:

 Diazepam is a benzodiazepine tranquilliser with

anticonvulsant, sedative, muscle relaxant and amnesic
properties 9,10,6. Benzodiazepines, such as diazepam,
bind to receptors in various regions of the brain and spinal
cord.
 Thisbinding increases the inhibitory effects of gamma-
aminobutyric acid (GABA) 9,10,6.
Adverse effects of diazepam:

 Drowsiness ,dizziness, tiredness, blurred vision, or

unsteadiness may occur.
 If any of these effects last or get worse, tell your doctor or
pharmacist promptly.
 Remember that this medication has been prescribed because
your doctor has judged that the benefit to you is greater than
the risk of side effects.
Uses of diazepam:

 Diazepam is a benzodiazepine medicine that has sedative,

anxiety-relieving and muscle-relaxing effects.
 Diazepam: medicine for anxiety, muscle spasms and
seizures - NHS.
7)Aliphatic Carboxylic Acid

(1)Volproate sod [volproic acid]

 Valproate (VPA) and its valproic acid, sodium
valproate, and valproate semisodium forms are
medications primarily used to treat epilepsy and
bipolar disorder and prevent migraine headaches.
 They are useful for the prevention of seizures in those
with absence seizures, partial seizures, and generalized
seizures.
Volproate sod (valproic acid)
Mechanism of action of volprote sod:

 Valproic acid exhibits its pharmacologic effects in a couple

of ways, such as by acting on GABA (γ aminobutyric acid)
levels in the CNS, blocking voltage-gated ion channels,
and inhibiting histone deacetylase.
Adevers effects of volprote sod:

 Takingtoo much sodium valproate can lead to

symptoms such as: feeling or being sick (nausea or
vomiting) headaches or feeling dizzy. 
 muscle weakness.
Uses of Volproate sod:

 Sodium valproate is used to treat epilepsy and bipolar

disorder.
 It's occasionally used to prevent migraine headaches.
 This medicine is only available on prescription.
 It comes as capsules, tablets and a liquid that you
swallow.
8)Phenyltriazine

(1)Lamotrigine:
 Lamotrigine is used alone or together with other
medicines to help control certain types of seizures (eg,
partial seizures, tonic-clonic seizures, or Lennox-
Gastaut syndrome) in the treatment of epilepsy. This
medicine cannot cure epilepsy and will only work to
control seizures for as long as you continue to take it
Lamotriagine
Mechanism of action of laminotriagine:

 The mechanism of action for lamotrigine is not entirely

understood.
 Itis a triazine, and research has shown that lamotrigine
selectively binds and inhibits voltage-gated sodium
channels, stabilizing presynaptic neuronal membranes and
inhibiting presynaptic glutamate and aspartate release.
Adverse effects of laminotriagine:

 Blurred vision.
 changes in vision.
 chest pain, discomfort, or tightness.
 clumsiness or unsteadiness.
 decreased urine output.
 dilated neck veins.
 double vision.
 irregular breathing
Uses of laminotriagine:

 All types of lamotrigine tablets (tablets, orally

disintegrating tablets, and chewable tablets) other than the
extended-release tablets are used alone or with other
medications to treat seizures in people who have epilepsy
or Lennox-Gastaut syndrome (a disorder that causes
seizures and often causes developmental delays .
9) Cyclic GABA analogous
(1)Gabapentin:
 Gabapentin works in the brain to prevent seizures and
relieve pain for certain conditions in the nervous
system.
 Itis not used for routine pain caused by minor injuries
or arthritis.
 Gabapentin is an anticonvulsant. This medicine is
available only with your doctor's prescription.
Gabapentin
Mechanism of Gabapentin:

 In vitro, gabapentin modulates the action of the GABA

synthetic enzyme, glutamic acid decarboxylase (GAD) and
the glutamate synthesizing enzyme, branched-chain amino
acid transaminase.
 Results with human and rat brain NMR spectroscopy
indicate that gabapentin increases GABA synthesis.
Adverse effects of Gabapentin:

 Feeling sleepy, tired or dizzy. As your body gets used to gabapentin,

these side effects should wear off. ...
 Feeling sick (nausea) Take gabapentin with or after a meal or
snack. ...
 Being sick (vomiting) ...
 Diarrhoea. ...
 Mood changes. ...
 Swollen arms and legs. ...
 Blurred vision. ...
 Dry mouth.
Uses of Gabapentin:

 Gabapentin is used to:Prevent and control partial seizures.

 Gabapentin can be used in adults and children age 3 and
older who have partial seizures.
 Relieve nerve pain following shingles in adults.
 ...Treat moderate-too-severe primary restless legs
syndrome.
10) Newer Drugs

(1)Vigabatrin:
 Vigabatrin powder is used to control infantile spasms
(a type of seizure that babies and children can have) in
babies 1 month to 2 years of age.
 Vigabatrin is in a class of medications called
anticonvulsants.
 It works by decreasing abnormal electrical activity in
the brain.
Vigabatrin
Mechanism of action of Vigabatrin:

 Vigabatrin was rationally designed to have a specific effect

on brain chemistry by inhibiting the GABA-degrading
enzyme, GABA transaminase, resulting in a widespread
increase in GABA concentrations in the brain.
 The increase in GABA functions as a brake on the
excitatory processes that can initiate seizure activity.
Adeverse effects of Vigabatrin:

 Problems walking or feeling uncoordinated.

Feeling dizzy.
 Shaking (tremors)
 Joint pain.
 Memory problems and not thinking clearly.
 Eye problems (blurry vision, double vision, and eye
movements that you cannot control)
Uses of Vigabatrin:

 Vigabatrin powder is used to control infantile spasms (a

type of seizure that babies and children can have) in babies
1 month to 2 years of age.
 Vigabatrin is in a class of medications called
anticonvulsants.
 It works by decreasing abnormal electrical activity in the
brain