This document summarizes a seminar on anticonvulsant agents. It discusses the pathophysiology and classification of epilepsy, as well as the mechanisms of action and structure-activity relationships of common anticonvulsant drugs like phenytoin, primidone, and ethosuximide. It also reviews the clinical uses of anticonvulsants to treat different seizure types and neurological conditions. The document concludes that identifying and treating associated neurobehavioral disorders can improve quality of life for people with epilepsy.
INTRODUCTION
DISEASE SPOTLIGHT
CLASSIFICATION OF CONVULSION
MACHANISM OF ANTICONVULSANT
CLASSIFICATION OF ANTICONVULSANT DRUGS
CONTRAINDICATIONS
ADVERSE EFFECTS OF CONVULSANTS
DOSAGE AND DILUTION
NURSES PRECAUTION AND RESPONSIBILITIES
CONCLUSION
INTRODUCTION
DISEASE SPOTLIGHT
CLASSIFICATION OF CONVULSION
MACHANISM OF ANTICONVULSANT
CLASSIFICATION OF ANTICONVULSANT DRUGS
CONTRAINDICATIONS
ADVERSE EFFECTS OF CONVULSANTS
DOSAGE AND DILUTION
NURSES PRECAUTION AND RESPONSIBILITIES
CONCLUSION
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
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Anticonvulsants are drugs that are used to arrest convulsions or seizures caused in epilepsy.
Seizure: associated with abnormal episodic high frequency discharge of impulses by a group of neurons in brain which starts local abnormal discharge & then spray to the other area of brain.
Convulsion: body muscles are contract and release rapidly & repeatedly, resulting in uncontrol shaking of body.
Epilepsy: these are a group of disorder of the CNS characterized by paroxysmal cerebral dysrhythmia, brief episodes (seizure) or disturbance of consciousness with or without characteristic body movements (convulsions).
Sedatives & Hypnotics
Sedatives
➢ It is a drug that reduces excitement and calms the person
➢ A drug that reduces excitement, calms the patient (without inducing sleep)
➢ Sedatives in therapeutic doses are anxiolytic agents
Abstract: Epilepsy is a serious and common chronic neurological disorder characterized by recurrent seizures, which are caused by abnormal synchronized neuronal disorders. It is a relatively common condition (up to 2% of the population) which can affect anyone at any age. Epilepsy can be controlled in a number of ways. The most common way to treat epilepsy is with anti-epileptic drugs. These AEDs can control but not cure epilepsy. Surgery can also be a possible treatment. Curative epilepsy surgery can only be performed in patients in whom the epileptogenic focus can be localized and does not overlap with eloquent brain areas. In the other patients with bilateral or multiple epileptogenic foci, with epilepsy onset in eloquent areas, or with no identifiable epileptogenic focus, treatments such as ketogenic diet, vagus nerve stimulation can be offered. VNS is an available procedure of which the mechanism of action is not understood, but with established efficacy for refractory epilepsy and low incidence of side-effects. The ketogenic diet is a high-fat, moderate protein, low carbohydrate diet used to treat intractable epilepsy, primary in the pediatric population. Hippocampal Deep Brain Stimulation has been used to treat patients with refractory epilepsy. Complementary and Alternative Medicine for epilepsy such as apuncture, aromatherapy, yoga etc may be used for lessening seizures, for alleviating related symptoms and for reducing side effects. Gene therapy aims to utilize viral and non-viral vectors in the delivery of DNA to target areas for the treatment of patients before their disease progresses. Gene therapy has delivered promising results in animal trials and pre-clinical settings and can be used for neurological disorders such as epilepsy.
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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
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
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
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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.
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9. GOAL OF TRARTMENT:
Help person with epilepsy lead full and productive life
Eliminate seizures without producing side effect
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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
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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
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
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
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