ANTI CONCULSANT - MERGE

SEIZURE

Sudden UNCONTROLLED ELECTRICAL DISTORABNCE in the brain

• due to high fever, Head trauma

Epilepsy

Neurological disorder

• there is multiple/unpredictable seizure

CONVULSION

• contraction/relaxation of the body

  • HAPPEN RAPIDLY/REPEATEDLY

ANTIEPILEPTICS

Acts by altering the sodium neuronal concentrations by promoting sodium efflux and restoration or enhancement of GABA inhibitory neuronal function

INHIBITORY

GABA

• Major —- neurotrasmitter

EXCITATORY

GLUTAMATE

• Major —- neurotransmitter

GLUTAMATE

Attenuation of excitatory neurotransmission

• RESPONSIBLE

Tonic-clonic (grand mal)

- most common, most dramatic, loss of consciousness with tonic-clonic phases

• CBZ, OXC, lamotrigine, VPA, Phenytoin, TPМ

Absence (petit mal)

brief, abrupt and self-limiting loss of consciousness, patient manifest rapid eye-blinking -

• Lamotrigine,VPA, ethosuximide

Myoclonic

- consists of short episodes of muscle contraction which reoccurs after several minutes

Status epilepticus

- seizures are rapidly recurrent without any recovery of consciousness between them

simple partial

HAVE memory after seizure

• (abnormal electrical activity is confined to a single focus on the brain)

• Jacksonian motor epilepsy

complex partial

DONT HAVE memory after seizure

• (sensory and motor system)

• There is an aura, then a confused or bizarre purposeful behavior for 2-3 minutes often with no memory of the event

METHYL

ETHYL

• absence seizure

AROMATIC RING

• grand mal

SAR

• R1 - R2

  • CONTAIN

    • USE

BARBITURATES

used primarily for their sedative/hypnotic activity

• have good activity against grand mal and partial seizures.

Phenobarbital

OLDEST epilepsy medicine still use

• LEAST EXPENSIVE anticonvulsant

Phenobarbital

DOC: STATUS EPILEPTICUS

• CHILD

Diazepam

DOC: STATUS EPILEPTICUS

• ADULT

HYDANTOIN

• PENYTOIN

PENYTOIN

USE: GRAND MAL

• has low water solubility weaker acid than barbituric acid used for all types of seizure except absence produces a low degree of sedation

Gingival HyperPLASIA

Hirsutism Fata hydantoin syndrome

• D

PENYTOIN

• A/E

• PREGNANCY LEVEL

Fosphenytoin (Cerebyx®)

PRODRUG of phentoin

• can use na pang IV

PHOSPHA TASES

Fosphenytoin (Cerebyx®)

• Contain phospate

  • give enzyme that tikal that phosphate

OXAZOLIDINEDIONES

• Trimethadione

Trimethadione

The only oxazolidinedione that is currently available

• seldom used. It is active against absence seizures.

USED na as: RESERVE REFRACTORY

• bec. it toxicity

SUCCINIMIDES

• Ethosuximide (Zarontin)

Ethosuximide (Zarontin)

• Prototypical anticonvulsant for treating absence seizure

• More active and less toxic than trimethadione

  • Calcium T- channel blocker

  • Used for absencе seizures

INCREASE THRESHOLD for seizure

GASTRIC DISTRESS

Ethosuximide (Zarontin)

• A/E

CARBAMAZEPINE (TEGRETOL)

N,N-diacylurea, a urea derivative

USE:

• Generalized tonic clonic

• partial seizure

• Na channel blocker

• TRIGEMINAL NEURALGIA

• DIPLOPIA

• ATAXIA

CARBAMAZEPINE (TEGRETOL)

• A/E

OXCARBAZEPINE (TRILEPTAL)

• N,N-diacylurea

• For partial seizure

monohydroxy compound

OXCARBAZEPINE (TRILEPTAL)

• Major metabolite:

PRIMIDONE

USED: all seizures except absence.

• Prodrug of phenobarbital

VALPROIC ACID

2-propylPentanoic acid

• like many aliphatic carboxylic acids, is active against absence seizures, but crosses the blood-brain barrier poorly

• Hepatotoxic

  • 2,4-dieneVPA

  • 4-epoxy-VPA

• Teratogenic

VALPROIC ACID

• A/E

  • metabolite

FELBAMATE (FELBATOL)

• act by reducing seizure spread, and by raising the seizure threshold.

• Blockade of NMDA Receptors

• only recommended for patients who do not respond adequately to alternative treatments and suffer from severe epileptic symptoms.

Anemia

Liver failure

FELBAMATE (FELBATOL)

• A/E

GABAPENTIN (NEURONTIN)

an analogue of GABA but has no gabaergic activity,

• acts by modulating Ca influx, stimulating GABA biosynthesis, and competes in the synthesis of Lglutamic acid

GABAPENTIN (NEURONTIN)

• Pregabalin - LYRICA

DOC: NEOROPATHIC PAIN

LAMOTRIGINE (LAMICTAL)

USE: Refractory seizure

• Inhibits the release of excitatory neurotransmitters, primarily glutamate, by blocking the voltage dependent sodium channels, thereby stabilizing the presynaptic membrane

• stevens johnson syndrome

• PHENYL TRIA ZINE

LAMOTRIGINE (LAMICTAL)

• A/E

• CONTIANNNN

RILUZOLE (RILUTEK)

• bottle - stopper shape container

Sodium channel blocker with antiglutamate effect

• Placed in a

BENZO THIA ZONE

RILUZOLE (RILUTEK)

• CONTAINN

TIAGABINE (GABITRIL)

blocks GABA reuptake as the major mode of anticonvulsant activity

• ainst partial seizure

GAT 1

TIAGABINE (GABITRIL)

• to inhibit gaba re uptake = transporter

ZONISAMIDE (ZONEGRAN)

blocks calcium T channels

• Partial seizure in adults

TOPIRAMATE (TOPAMAX)

Weak carbonic acid inhibitor

• increases the effect of GABA while serving as an antagonist at kainic acid/AMPA receptors.

• adjunct for partial seizures.

migraine.

Topiramate

• also be used off label in the treatment of