M pharm 1st year

1. Anti epileptics
Submitted to : DR. RJ.Mandade sir. Submitted by: jamdade sonali lala
Pharmacology department M pharm 1st year pharmacology.
Sudhakar Rao Naik institute of pharmacy pusad

2. Content
 Introduction
 Pathophysiology
 Dignosis
 classification of anti epileptic drug
 Pharmacology of phenytoin
 Referance

3. Epilepsy
 It is a brain disorder.
In which the normal
pattern of Neuronal
activity become
distrubed .abnormal
neurohumoral
transmission.(neurolo
gical disorder.)

4. Epilepsy causes(symptoms)
 Seizures
 Strange sensation ,emotoin And behaviour
 Convulsions
 Muscle spasm
 Loss of consciousness
 Proxymal attacks
 These are all due to the Excitation of Cerebral neuron .
 Seizures are generated in The epileptogenIc centre of the brain .
 Involve the shaking and involuntary Contraction of the body
 Occurs due to any toxins,trauma ,hyperthermia ,medical overdose or discontinuous of medications.

5. Why epilepsy occurs
 Children: birth trauma, infection-meningitis Congenital Abnormalities
 Middle age: Alcohol, infection head injury And drug like cocaine , low blood
sugar, low oxygen,low boold Na+ and low ca+ .
 Elderly : stroke, Tumors etc .

6. Types of seizures Or epilepsy
 Generalised seizures:
 Absence seizures(petitmal ):mostly in children,loss of consciousness
blinking of eyelid and jerking of the entire body
Last for 30 sec
 tonic clonic seizures(grandmal): sequence of tonic spasm and clonic jerking of All
Muscle
last for 2 to 5 min.
 Partial seizures: In which neuronal discharge Are abnormal to A particular area or localises area in the brain.
Last for 20 to 60 sec.
 simple seizures: Small part of The brain. Causes twiching Or change in sensation
 Complex seizures:Confuse unable to respond For up to minute .
 Secondary generalised: Spread one part of brain To the whole brain.( Local to general )

7. Pathophysiology
 Neurons are inter connected In a complex network . Each individual neuron is linked With
Hundred of other neuron Via synapses.
 Neurons discharge electrical current And neurotransmitter are Release at synaptic Level and
permit inter communication.
 Neurotransmitter are of two types : inhibitory neurotransmitter And excitatory neurotransmitter.
 Inhibitory neurotransmiter( GABA): Act on ion channel And increase chloride outflow and decrease
the Chances of action potentials formation
 Excitatory neurotransmitter (aspartate,glutamate):Aspartate and glutamate allows the Na and Ca
influx Which paves Way for action potentials Formation .
 In this manner information id conveyed Transmitted and processed through out the CNS . Seizures
occurs due to the imbalance between The above inhibition and excitation .
 A normal neuron discharge respectivel.at low baseline frequency if neuron are
damaged,injured,suffer a chemical Metabolic insult The changes in discharge pattern develop.
 During epilepsy regular low frequency discharge Are replaced by Bursts of highfrequency
Discharge followed by Period of inactivity
 A single neuron Discharge in an abnormal manner Is usually not clinically significant .But when a
whole population of neuron Discharge Synchronously Is an abnormal manner ,epileseizures is
precipitate .this abnormal discharge May remain localised Or it may spread To adjcent area

8.  Abormalities in ion channel (Na+,K,Ca+) Or decreaseD INT activity inactivation
of INT activity .
 ⬇️
 incrased the ENT activity
 ⬇️
 Rythamic and repetative Hypersynochronous Discharge of neuron .
 ⬇️
 seizures focus
 ⬇️
 seizures
 ⬇️
Repetitive seizures
⬇️
Epilepsy.

9. Diagnosis
 Neurological examination : doctor test for behaviour , motor abilities ,mental
function and other symptoms.
 Medical history
 Genetic history
 (EEG ) electroencephalogram : track electrical signal From the brain .
 CT scan ,MRI scan : Used to detedthe abnormalities in brain (tumours , cysts,
bleeding.

10. Treatment: Antiepileptic drugs.
 Classification of antiepileptic agents

11. Pharmacology of phenytoin
 Phenytoin is a hydantoin derivative .
 In 1908 Phenytoin (5,5-diphenylhydantoin) was
first synthesized as a barbiturate derivative in
germany by professor heinrich Biltz (1865-
1943)and subsequently resynthesized by an
american chemist of the pharmaceutical company
parke-Davis in 1923 in Detroit.
 Brand name : Dilantin Dilantin 125,Phenytek.
:

13. Pharmacokinetic of phenytoin
 Absorption: well absorbed when given orally ,howeve,it is also
Available as iv for emergency.
 Distribution: 80 to 90% Protein bound
 Biotransformation :Induces liver enzymes. Metabolise by the liver ti
inactive metabolite .
 Excretion: Excreted in urine On glucoronide conjugate.Plasma half
life Approx 20hrs.
 Dose: 300 to 400 mg/ day .

14. Uses
 Phenytoin is used to control seizures including tonic clonic and temporal lobe
seizures in the treatment of epilepsy .
 It is also used to prevent and treat seizures that occurs during brain surgery.
 It is also used in cardiac arrhythmias .

15. Adverse Effect
Phenytoin
1. Pregnancy Vertigo,drowsiness
 Hypertrophy of gum or hirsutism Vomiting ,nausea
 Edema Ataxia
 Neurological Hallucinations ,epigatric pain
 Yellow discoloured lim
 Thrombosis when injected iv. Fall in BP and
 Osteomalacia Cardiac arrhythmias
 Inhibit insulin
 Neutropenia

16. Drug interaction
 Phenobarbitone competitively inhibits phenytoin metabolism and drug like
chloramphenicol,isoniazide,cimetidine ,and warfarin inhibit the phenytoin
metabolism and can precipitate its toxicity .
 Carbamazepine and phenytoin increase each other’s metabolism.
 Phenytoin induces microsomal enzymes and increase degradation of
steroids,digoxin,doxycycline,theophylin.
 Sucralfate binds phenytoin in gastrointestinal tract and decrease its absorption.
 Contraindication of phenytoin:
 Cardiac diseases
 Diabetis mellitus
 Pregnancy
 Seriouse hepatic disease,

17. Reference
 Text book of pathology By Harsh Mohan
 K. D tripathi
 Wilson book of medicinal chemistry
 Slideshare ppt