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A SEMINAR ON
ANTICONVULSANT AGENT
SAVITRIBAI PHULE
PUNE UNIVERSITY
M.V.P. SAMAJ’S COLLEGE OF PHARMACY, NASHIK-02
2018-2019
Submitted by
Ms. ANKITA J.GAIDHANE
(PHARMACEUTICAL
CHEMISTRY)
(M. PHARM SEM I)
Guided By
PROF. A.S.JAGDALE
(DEPARTMENT OF
PHARMACEUTICAL CHEMISTRY)
1
CONTENT Introduction
Pathophysiology
Classification
Mechanism of action
Structure activity relationship
Application
Conclusion
References
2
INTRODUCTION
3
 Epilepsy is defined as chronic disorder that caused unprovoked recurrent
seizures.in which there is excessive abnormal brain cell activity .
 The major difference between seizures and epilepsy is that seizure is a term
which represent the single occurance while the epilepsy is the two or more
unprovoked seizures that called as epilepsy.
 Hippocrates at very first who think of that disorder which is occure in brain .
After that berger discovered the stimulation of electroencephalography
 The anticonvulsant activity was discovered by locock(1799-1875) begin to treat
patient in 1912 by phenobarbital by one of the first antiepileptic drug used for
treatment of epilepsy.
4
What is world wide scenario5
Types of seizures6
1. Generalized seizure
 Tonic clonic seizure
 Absence seizure
 Myoclonic seizure
 Atonic seizure
2. Focal seizure
 Simple focal seizure
 Complex focal seizure
 Secondary generalized seizure
Tool to confirm diagnosis
Clinical assessment
1. Patient history
2. Test(blood ,EEG,CT,MRI ,PET scan)
3. Neurological scan
 Id of seizure type
 Clinical evaluation for cause
7
National and community resources
The epilepsy foundation
1. local affiliates
2. websites:www.epilepsyfoundation.org
 Medic alert foundation
 social security administration
 call when there is any emergency mrdical survices on 911
(if the convusive seizure not known last ffrom more than
5 min )
1. If person is injured or pregnant.
2. Do not resume normal breath.
8
GOAL OF TRARTMENT:
 Help person with epilepsy lead full and productive life
Eliminate seizures without producing side effect
9
TYPES OF TREATMENT
 MEDICATION
SURGERY
NON PHARMACOLOGICAL TRATMENT
1. Ketogenic diet
2. Vagus nerve stimulation
3. lifestyle modification
10
Surgery treatment11
OTHER TREATMENT APPROACH
 Behavioural therapy
Biofeedback
Relaxation
 Positive reinforcement
 Cognitive therapy
 Aromatherapy
12
Classification of Anticonvulsant agent13
Barbiturates; Phenobarbitone
Deoxybarbiturates;Primidone
Hydantoin;Phenytoin
Immunostilbene;Carbamazepine
Succinimide;Ethosuximide
Aliphatic carboxlic acid;valproate
Benzodiazepine; Clonazepam, diazepem
Cyclic GABA analogue;Gabapentine
Phenytriezene;Lamotrigine
Newer drugs; Vigabatrine,topiramate. Tiagabine,
levetiracetam
MECHANISM OF ACTION
 VOLTAGE GATED ION CHANNEL
• Voltage gated Na channel-Phenytoin, fosphenytoin
• Voltage gated Ca channel-Ethosuximide
• Voltage gated K channel-Ezogabine
 GABA INHIBITION
• GABAa receptor-Primidone
• GAT-1-GABA transporter-Tiagabine
• GABAa Transaminase- Vigabatrine
14
15
• Synaptic release machinary;levetiracetam
• Ionotropic glutamate receptor;
1. AMPA receptor ; parampanel.
2. Mixed drug; zonisamide, felbamate.
16 VOLTAGE GATED SODIUM CHANNEL
PHENYTOIN:
 Phenytoin is believed to protect against seizures
by causing voltage –dependent Block voltage
gated sodium channel.
 This blocks sustained high frequency repetitive
firing of action potentials
 The primary sites for the action is the appears to be
the motor cortx where spread of seizure activity is

17
STRUCTURE ACTIVITY RELATIONSHIP18
HYDANTOIN DERIVATIVES:
• 5-pheny or other aromatic substitution is essential for activity.
• Alkyl substituted at position 5 may contribute to seduction
• Among other hypnotics 1,3disubstitued hydantoin.Exibit activity against
chemically induced convulsion .while it remain ineffective against
electric shock induced convulsion
Oxazolidinediones derivatives
General structure:
 R1=CH 3
 R2=CH 3
Replacement of the –NH group at position 1 of the
hydantoin system with an oxygen atom yield the oxazolide
2,4-dione system
19
SAR OF OXAZOLDINEDIONE DERIVATIVE20
The nature of substituent on C-5is important ,however
alkyl substituents towards and Antipetitmal activity while
acyl towards Antigrandmal activity
N-Alky substituent doesn’t alter the afford activity clinical
undergo N-Dealkylation in metabolism
3,5,5-trimethdione was first drug introduced specifically
for treating absence seizure it is important as prototype
structure.
USES OF AGENT21
 The main use of anticonvulsant is to treat different types of
seizures .
 Zosenamide gives adjuvant therapy with that of partial
seizure treatment.
 Phenytoin also used in cardiac arrhythmias.
 Some cases of trigeminal and neuralgia response well to
phenytoin.
 The primidone is less toxic than phenobarbital then it is used
to treat vertigo and ataxia.
Conclusion :
Neurobehavioral disorder can profoundly affect the lifes of
people with epilepsy
 In general more frequent and more severe the seizure more likely
the neurobehavioral disorder may developed such as depression
psychosis and epilepsy it can be treated with medication by
identification of cognitive behavioral disorder which can improve
the significant quality life
22
List of drug with its brand name
NAME OF DRUG BRAND NAME
1. Phenytoin Dilantin (20mg)
2. Phenobarbital Luminal, Tedral
3. Ethosuximide Zarotin
4. Primidone Mysoline
5. Leveteracetam Levera(500mg,750mg)
23
CASE STUDY;
Name -Alka m. chalkhor
Age- 23yr
Cause-gentic ,environmental
Dose given:
Phenytoin( iv)
Levera 500mg
Friseum 5mg
Diamox
24
REFERENCES:
Principles of medicinal chemistry by William o. foye ,verges publishing
house, 3rd edition,173-87.
Essentials of medical pharmacology ,K.D.Tripathi by Jaypee brothers
medical publishers ,Eighth edition;
438-51.
 Textbook of medicinal chemistry by V. Algarswamy volume I, Third
edition;304-33.
 A Review article on newer antiepileptic drugs by Satinder aneja and
Suvasini Sharma ,Vol 50;nov15,2013:1033-40
25
Handbook of Drug interaction: A clinical and forensic Guide ,
A.Mozayani and L.P.Raymon,eds,Humana Press,INC,Nanthan
L.Kanous, Barry E.Gidal; 89-103.
CIMS Annual 110, Cimsasia.com,India update-3,37years,Jan-apr
2016-17;180-83.
Epilepsy animation video,you tube,google.com.
https://www.cureepilepsy.org
26
27
28

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Ankita gaidhane ppt

  • 1. A SEMINAR ON ANTICONVULSANT AGENT SAVITRIBAI PHULE PUNE UNIVERSITY M.V.P. SAMAJ’S COLLEGE OF PHARMACY, NASHIK-02 2018-2019 Submitted by Ms. ANKITA J.GAIDHANE (PHARMACEUTICAL CHEMISTRY) (M. PHARM SEM I) Guided By PROF. A.S.JAGDALE (DEPARTMENT OF PHARMACEUTICAL CHEMISTRY) 1
  • 2. CONTENT Introduction Pathophysiology Classification Mechanism of action Structure activity relationship Application Conclusion References 2
  • 4.  Epilepsy is defined as chronic disorder that caused unprovoked recurrent seizures.in which there is excessive abnormal brain cell activity .  The major difference between seizures and epilepsy is that seizure is a term which represent the single occurance while the epilepsy is the two or more unprovoked seizures that called as epilepsy.  Hippocrates at very first who think of that disorder which is occure in brain . After that berger discovered the stimulation of electroencephalography  The anticonvulsant activity was discovered by locock(1799-1875) begin to treat patient in 1912 by phenobarbital by one of the first antiepileptic drug used for treatment of epilepsy. 4
  • 5. What is world wide scenario5
  • 6. Types of seizures6 1. Generalized seizure  Tonic clonic seizure  Absence seizure  Myoclonic seizure  Atonic seizure 2. Focal seizure  Simple focal seizure  Complex focal seizure  Secondary generalized seizure
  • 7. Tool to confirm diagnosis Clinical assessment 1. Patient history 2. Test(blood ,EEG,CT,MRI ,PET scan) 3. Neurological scan  Id of seizure type  Clinical evaluation for cause 7
  • 8. National and community resources The epilepsy foundation 1. local affiliates 2. websites:www.epilepsyfoundation.org  Medic alert foundation  social security administration  call when there is any emergency mrdical survices on 911 (if the convusive seizure not known last ffrom more than 5 min ) 1. If person is injured or pregnant. 2. Do not resume normal breath. 8
  • 9. GOAL OF TRARTMENT:  Help person with epilepsy lead full and productive life Eliminate seizures without producing side effect 9
  • 10. TYPES OF TREATMENT  MEDICATION SURGERY NON PHARMACOLOGICAL TRATMENT 1. Ketogenic diet 2. Vagus nerve stimulation 3. lifestyle modification 10
  • 12. OTHER TREATMENT APPROACH  Behavioural therapy Biofeedback Relaxation  Positive reinforcement  Cognitive therapy  Aromatherapy 12
  • 13. Classification of Anticonvulsant agent13 Barbiturates; Phenobarbitone Deoxybarbiturates;Primidone Hydantoin;Phenytoin Immunostilbene;Carbamazepine Succinimide;Ethosuximide Aliphatic carboxlic acid;valproate Benzodiazepine; Clonazepam, diazepem Cyclic GABA analogue;Gabapentine Phenytriezene;Lamotrigine Newer drugs; Vigabatrine,topiramate. Tiagabine, levetiracetam
  • 14. MECHANISM OF ACTION  VOLTAGE GATED ION CHANNEL • Voltage gated Na channel-Phenytoin, fosphenytoin • Voltage gated Ca channel-Ethosuximide • Voltage gated K channel-Ezogabine  GABA INHIBITION • GABAa receptor-Primidone • GAT-1-GABA transporter-Tiagabine • GABAa Transaminase- Vigabatrine 14
  • 15. 15 • Synaptic release machinary;levetiracetam • Ionotropic glutamate receptor; 1. AMPA receptor ; parampanel. 2. Mixed drug; zonisamide, felbamate.
  • 16. 16 VOLTAGE GATED SODIUM CHANNEL PHENYTOIN:  Phenytoin is believed to protect against seizures by causing voltage –dependent Block voltage gated sodium channel.  This blocks sustained high frequency repetitive firing of action potentials  The primary sites for the action is the appears to be the motor cortx where spread of seizure activity is
  • 18. STRUCTURE ACTIVITY RELATIONSHIP18 HYDANTOIN DERIVATIVES: • 5-pheny or other aromatic substitution is essential for activity. • Alkyl substituted at position 5 may contribute to seduction • Among other hypnotics 1,3disubstitued hydantoin.Exibit activity against chemically induced convulsion .while it remain ineffective against electric shock induced convulsion
  • 19. Oxazolidinediones derivatives General structure:  R1=CH 3  R2=CH 3 Replacement of the –NH group at position 1 of the hydantoin system with an oxygen atom yield the oxazolide 2,4-dione system 19
  • 20. SAR OF OXAZOLDINEDIONE DERIVATIVE20 The nature of substituent on C-5is important ,however alkyl substituents towards and Antipetitmal activity while acyl towards Antigrandmal activity N-Alky substituent doesn’t alter the afford activity clinical undergo N-Dealkylation in metabolism 3,5,5-trimethdione was first drug introduced specifically for treating absence seizure it is important as prototype structure.
  • 21. USES OF AGENT21  The main use of anticonvulsant is to treat different types of seizures .  Zosenamide gives adjuvant therapy with that of partial seizure treatment.  Phenytoin also used in cardiac arrhythmias.  Some cases of trigeminal and neuralgia response well to phenytoin.  The primidone is less toxic than phenobarbital then it is used to treat vertigo and ataxia.
  • 22. Conclusion : Neurobehavioral disorder can profoundly affect the lifes of people with epilepsy  In general more frequent and more severe the seizure more likely the neurobehavioral disorder may developed such as depression psychosis and epilepsy it can be treated with medication by identification of cognitive behavioral disorder which can improve the significant quality life 22
  • 23. List of drug with its brand name NAME OF DRUG BRAND NAME 1. Phenytoin Dilantin (20mg) 2. Phenobarbital Luminal, Tedral 3. Ethosuximide Zarotin 4. Primidone Mysoline 5. Leveteracetam Levera(500mg,750mg) 23
  • 24. CASE STUDY; Name -Alka m. chalkhor Age- 23yr Cause-gentic ,environmental Dose given: Phenytoin( iv) Levera 500mg Friseum 5mg Diamox 24
  • 25. REFERENCES: Principles of medicinal chemistry by William o. foye ,verges publishing house, 3rd edition,173-87. Essentials of medical pharmacology ,K.D.Tripathi by Jaypee brothers medical publishers ,Eighth edition; 438-51.  Textbook of medicinal chemistry by V. Algarswamy volume I, Third edition;304-33.  A Review article on newer antiepileptic drugs by Satinder aneja and Suvasini Sharma ,Vol 50;nov15,2013:1033-40 25
  • 26. Handbook of Drug interaction: A clinical and forensic Guide , A.Mozayani and L.P.Raymon,eds,Humana Press,INC,Nanthan L.Kanous, Barry E.Gidal; 89-103. CIMS Annual 110, Cimsasia.com,India update-3,37years,Jan-apr 2016-17;180-83. Epilepsy animation video,you tube,google.com. https://www.cureepilepsy.org 26
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