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Antiepilepsy
(Anticonvulsants)
Presented by:- Shalini N. Barad
Lecturer,
Appasaheb Birnale College of
Pharmacy
 Epilepsy : Epilepsy is chronic convulsive
disorder characterized by sudden loss or
impairment of consciousness, usually but not
always with characteristic body movements
and sometimes with hyper autonomic activity.
 Seizures : Seizures, are symptoms of
disturbed electrical activity in the brain
characterized by episodes of abnormal,
excessive, and synchronous discharge of a
group of neurons within the brain that cause
involuntary movement, sensation, or
thought.
 These are generated from primary or
acquired neurological disturbances of brain
function as a result of an imbalance between
excitatory and inhibitory processes in the
brain.
 Epilepsies have been classified:
 Types of Epilepsy:
1. Grandmal epilepsy /Major epilepsy:
 Characterized by sudden loss of
consciousness and major convulsions with
tonic spasm and clonic jerking of body.
[stiffening (tonic) and movement (clonic)]
 Attacks can occur at any age.
2. A partial (focal) seizure
 happens when unusual electrical activity
affects a small area of the brain.
 When the seizure does not affect
awareness, it is known as a simple partial
seizure.
Absenc
e
Atonic
Classification:
1) Aliphatic carboxylic acid: Valproic acid
2) Benzodiazepines: Clonazepam,
Diazepam,
3) Barbiturate: Phenobarbitone
4) Deoxybarbiturates: Primidone
5) Cyclic GABA analogue: Gabapentin
6) Phenyltriazine: Lamotrigine,
7) Hydantoin: Phenytoin, Fosphenytoin
8) Iminostilbene: Carbamazepine,
Oxcarbazepine
9) Succinimide: Ethosuximide
10) Newer drugs: Vigabatrin, Topiramate,
Tiagabine, Zonisamide, Levetiracetam
1. Phenytoin:
• Molecular Formula: C15H12N2O2
• Structure:
• Chemical Name: 5,5-
diphenylimidazolidine-2,4-dione
• Uses:
1) Phenytoin is a medicine used to treat
epilepsy.
2) It can also be used to treat trigeminal
neuralgia, a type of nerve pain that affect
your face.
3) It comes as tablets that can be chewed or
dissolved in water, capsules and a light
that you swallow.
 Storage and stability: It should store under
ambient temperatures and keep it an from
oxidizing materials and bases.
 Store, below 40 °C preferably between 15
and 30°C.
 Formulations: Tablet, Capsule,
Suspension, Injection.
2. Carbamazepine:
 Molecular Formula: C15H12N2O
 Structure:
 Chemical Name: 5H-dibenzo [b,f]
azepine-5-carboxamide
• Uses:
1) It is used to treat epilepsy.
2) It is used to treat pain associated with
trigeminal neuralgia.
3) It is occasionally used to treat bipolar
disorder when other medicines have not
worked.
• Storage and stability: Store in airtight
containers, below 40°C and, preferably,
between 15°C and 30°C, and away from
light.
• Formulations: Tablet, Syrup, Injection,
Suppositories.
• Brands: Tegretol, Tegretol XR, Epitol.
3. Valproic Acid:
• Molecular Formula: C8H16O2
 Structure:
• Chemical Name: 2-propylpentanoic
acid
• Uses:
• Valproic acid is used to treat bipolar
disorder.
• It's occasionally used to prevent migraine
headaches and can also be used to
epilepsy.
• Storage and stability:
• Store, 15-30°C in a tight container.
• Store below 40°C, prefer between 15-
30°C, unless, otherwise specified by
manufacturer.
• Store, in a tight container protect from
freezing.
• Formulations: Tablet, Tablet, Injection.
4 . Clonazepam:
• Molecular Formula: C15H10CIN303
• Uses:
1) It's used to control seizures or fits due to
epilepsy, involuntary muscle spasms panic
disorder and sometimes restless legs
syndrome.
• Storage and stability: Keep container tightly
closed in a dry and well-ventilated place light-
resistant containers at 25°C, but may be
exposed to temperatures ranging from15-
30°C.
• Formulations: Tablet, Syrup, Injection.
• Brands: Epitril, Rivotril, Cergo MD, Lonazep.
5. Gabapentin:
 Molecular Formula: C₂H₂NO₂
• Structure:
 Chemical Name: 2-(1-(aminomethyl)
cyclohexyl) acetic acid
• Uses:
1) Gabapentin is in a class of medications called
anticonvulsants..
2) It treats seizures by decreasing abnormal
excitement in the brain.
3) It relieves the pain of Postherpetic neuralgia
by changing the way the bodypain.
• Storage and stability: Keep container tightly
closed in a dry and well-ventilated Store 25°C,
excursions permitted between 15°C to 30°C,
store oral solution refrigerator to 8°C.
• Formulations: Tablet, Oral solution, Capsule,
Injection.
• Brands: FusePaq Fanatrex, Gabarone,
Gralise, Neurontin.
6. Topiramate
 Storage Condition :Store protected from
light, at a temperature not exceeding 30°C.
 Uses: Used in the treatment of:
(1) Alcohol dependency.
(ii)Epilepsy, primary generalized tonic-clonic
seizures.
(iii) Grand mal generalized tonic-clonic seizure.
(iv) Migraine.
(v) Mood disorders.
(vi) Partial-onset seizures.
 Pharmaceutical Formulations :
(i) Topiramate Tablet I.P.
(ii) Topiramate Capsule,
 Brand Names: Topamax, Trokendi XR,
Qsymia, Topex, Epitop, Topamate, Nextop
and Qudexy.
7. Vigabatrin
 Uses:
1) It is used as adjunctive therapy in the
treatment of refractory complex partial
seizures in children (2 years age) and old
age persons.
2) Also used in the treatment of infantile
spasms in patients between 1 month and 2
years of age for whom the potential benefits
outweigh the risk of vision loss.
 Storage: Store protected from moisture, at a
temperature not exceeding 30°C.
 Pharmaceutical Formulations:
1) Vigabatrin Tablet
2) Vigabatrin Powder, for solution
3) Vigabatrin Powder
 Brand Names: Sabril, Vigadrone.
8. Lamotrigine
 Uses:
1. For the following seizure types in patients >2
years of age: partial seizures, primary
generalized tonic-clonic seizures, and
generalized seizures.
2. For the maintenance treatment of bipolar 1
disorder, delaying the time to moodepisodes
in adults at least 18 years or older which may
include
Mania
Hypomania
Depression
Mixed episodes
 Storage: Store protected from moisture, at a
 Pharmaceutical Formulations:
1) Lamotrigine Dispersible Tablets LP.
2) Lamotrigine prolong-release Tablets
LP.
 Brand Name: Lamictal.
Antiepilepsy

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Antiepilepsy

  • 1. Antiepilepsy (Anticonvulsants) Presented by:- Shalini N. Barad Lecturer, Appasaheb Birnale College of Pharmacy
  • 2.
  • 3.  Epilepsy : Epilepsy is chronic convulsive disorder characterized by sudden loss or impairment of consciousness, usually but not always with characteristic body movements and sometimes with hyper autonomic activity.
  • 4.
  • 5.
  • 6.  Seizures : Seizures, are symptoms of disturbed electrical activity in the brain characterized by episodes of abnormal, excessive, and synchronous discharge of a group of neurons within the brain that cause involuntary movement, sensation, or thought.  These are generated from primary or acquired neurological disturbances of brain function as a result of an imbalance between excitatory and inhibitory processes in the brain.
  • 7.  Epilepsies have been classified:
  • 8.
  • 9.  Types of Epilepsy: 1. Grandmal epilepsy /Major epilepsy:  Characterized by sudden loss of consciousness and major convulsions with tonic spasm and clonic jerking of body. [stiffening (tonic) and movement (clonic)]  Attacks can occur at any age. 2. A partial (focal) seizure  happens when unusual electrical activity affects a small area of the brain.  When the seizure does not affect awareness, it is known as a simple partial seizure.
  • 10.
  • 12. Classification: 1) Aliphatic carboxylic acid: Valproic acid 2) Benzodiazepines: Clonazepam, Diazepam, 3) Barbiturate: Phenobarbitone 4) Deoxybarbiturates: Primidone 5) Cyclic GABA analogue: Gabapentin 6) Phenyltriazine: Lamotrigine, 7) Hydantoin: Phenytoin, Fosphenytoin 8) Iminostilbene: Carbamazepine, Oxcarbazepine 9) Succinimide: Ethosuximide 10) Newer drugs: Vigabatrin, Topiramate, Tiagabine, Zonisamide, Levetiracetam
  • 13. 1. Phenytoin: • Molecular Formula: C15H12N2O2 • Structure: • Chemical Name: 5,5- diphenylimidazolidine-2,4-dione
  • 14. • Uses: 1) Phenytoin is a medicine used to treat epilepsy. 2) It can also be used to treat trigeminal neuralgia, a type of nerve pain that affect your face. 3) It comes as tablets that can be chewed or dissolved in water, capsules and a light that you swallow.  Storage and stability: It should store under ambient temperatures and keep it an from oxidizing materials and bases.  Store, below 40 °C preferably between 15 and 30°C.  Formulations: Tablet, Capsule, Suspension, Injection.
  • 15. 2. Carbamazepine:  Molecular Formula: C15H12N2O  Structure:  Chemical Name: 5H-dibenzo [b,f] azepine-5-carboxamide
  • 16. • Uses: 1) It is used to treat epilepsy. 2) It is used to treat pain associated with trigeminal neuralgia. 3) It is occasionally used to treat bipolar disorder when other medicines have not worked. • Storage and stability: Store in airtight containers, below 40°C and, preferably, between 15°C and 30°C, and away from light. • Formulations: Tablet, Syrup, Injection, Suppositories. • Brands: Tegretol, Tegretol XR, Epitol.
  • 17. 3. Valproic Acid: • Molecular Formula: C8H16O2  Structure: • Chemical Name: 2-propylpentanoic acid
  • 18. • Uses: • Valproic acid is used to treat bipolar disorder. • It's occasionally used to prevent migraine headaches and can also be used to epilepsy. • Storage and stability: • Store, 15-30°C in a tight container. • Store below 40°C, prefer between 15- 30°C, unless, otherwise specified by manufacturer. • Store, in a tight container protect from freezing. • Formulations: Tablet, Tablet, Injection.
  • 19. 4 . Clonazepam: • Molecular Formula: C15H10CIN303 • Uses: 1) It's used to control seizures or fits due to epilepsy, involuntary muscle spasms panic disorder and sometimes restless legs syndrome. • Storage and stability: Keep container tightly closed in a dry and well-ventilated place light- resistant containers at 25°C, but may be exposed to temperatures ranging from15- 30°C. • Formulations: Tablet, Syrup, Injection. • Brands: Epitril, Rivotril, Cergo MD, Lonazep.
  • 20. 5. Gabapentin:  Molecular Formula: C₂H₂NO₂ • Structure:  Chemical Name: 2-(1-(aminomethyl) cyclohexyl) acetic acid
  • 21. • Uses: 1) Gabapentin is in a class of medications called anticonvulsants.. 2) It treats seizures by decreasing abnormal excitement in the brain. 3) It relieves the pain of Postherpetic neuralgia by changing the way the bodypain. • Storage and stability: Keep container tightly closed in a dry and well-ventilated Store 25°C, excursions permitted between 15°C to 30°C, store oral solution refrigerator to 8°C. • Formulations: Tablet, Oral solution, Capsule, Injection. • Brands: FusePaq Fanatrex, Gabarone, Gralise, Neurontin.
  • 22. 6. Topiramate  Storage Condition :Store protected from light, at a temperature not exceeding 30°C.  Uses: Used in the treatment of: (1) Alcohol dependency. (ii)Epilepsy, primary generalized tonic-clonic seizures. (iii) Grand mal generalized tonic-clonic seizure. (iv) Migraine. (v) Mood disorders. (vi) Partial-onset seizures.
  • 23.  Pharmaceutical Formulations : (i) Topiramate Tablet I.P. (ii) Topiramate Capsule,  Brand Names: Topamax, Trokendi XR, Qsymia, Topex, Epitop, Topamate, Nextop and Qudexy.
  • 24. 7. Vigabatrin  Uses: 1) It is used as adjunctive therapy in the treatment of refractory complex partial seizures in children (2 years age) and old age persons. 2) Also used in the treatment of infantile spasms in patients between 1 month and 2 years of age for whom the potential benefits outweigh the risk of vision loss.  Storage: Store protected from moisture, at a temperature not exceeding 30°C.
  • 25.  Pharmaceutical Formulations: 1) Vigabatrin Tablet 2) Vigabatrin Powder, for solution 3) Vigabatrin Powder  Brand Names: Sabril, Vigadrone.
  • 26. 8. Lamotrigine  Uses: 1. For the following seizure types in patients >2 years of age: partial seizures, primary generalized tonic-clonic seizures, and generalized seizures. 2. For the maintenance treatment of bipolar 1 disorder, delaying the time to moodepisodes in adults at least 18 years or older which may include Mania Hypomania Depression Mixed episodes  Storage: Store protected from moisture, at a
  • 27.  Pharmaceutical Formulations: 1) Lamotrigine Dispersible Tablets LP. 2) Lamotrigine prolong-release Tablets LP.  Brand Name: Lamictal.