Psychopharmacology: Antiepileptics antiseizures anticonvulsants


Classification of AEDs
·         Phenytoin
·         Phenobarbital
·         Primidone
·         Carbamazepine
·         Ethosuximide
·         Valproate (valproic acid)
·         Lamotrigine  
·         Felbamate
·         Topiramate    
·         Gabapentin
·         Tiagabine
·         Vigabatrin
·         Oxycarbazepine
·         Levetiracetam
·         Fosphenytoin
Chemical based classification of Anti-epileptic drugs (AED)

Chemical compound class
Member Drug
Aliphatic carboxylic acid
Sodium valproate
Cyclic GABA analogue
Newer drugs
Vigabatrin , Topiramate,Tiagabine, Levitiracetam, Zonisamide
Newer (Second Generation) Antiepileptic
·         Largely target partial seizures
·         Fewer and less severe drug interactions compared to older drugs
Enhance neurotransmitter release, activation of NMDA subtype Of glutamate receptors, which causes ca influx & neuronal activation.
PHENYTOIN (Dilantin)
·         Oldest nonsedative antiepileptic drug.
·         Fosphenytoin, a more soluble prodrug is used for parenteral use.
·         "Fetal hydantoin syndrome"
·         It alters Na+, Ca2+ and K+ conductances. 
·         Inhibits high frequency repetitive firing.  
·         Alters membrane potentials.
·         Ataxia and nystagmus.
·         Cognitive impairment.
·         Hirsutism
·         Gingival hyperplasia.
·         Coarsening of facial features.
·         Partial seizure
·         Generalized (including tonic-clonic) seizures
·         Contraindicated in absence seizures
·         Nonseizure indications include  
o   Trigeminal neuralgia
o   Manic-depressive disorders
Fetal Hydantoin Syndrome
·         Pre- and postnatal growth deficiency with psychomotor retardation, microcephaly with a ridged metopic suture, hypoplasia of the nails and finger like thumb and hypoplasia of the distal phalanges.
·         Radiological skeletal abnormalities reflect the hypoplasia and fused metopic suture.
·         Cardiac defects and abnormal genitalia.
·         Mechanism of action, similar to phenytoin. Inhibits high frequency repetitive firing
·         Decreases synaptic activity presynaptically.
·         Inh. uptake and release of NE, but not GABA.
·         Potentiates postsynaptic effects of GABA.   Metabolite is active.
·         Auto induction of metabolism.         
·         Nausea and visual disturbances.  
·         Granulocyte suppression.
·         Aplastic anemia.
·         Exacerbates absence seizures.
·         Partial seizure
·         Generalized (including tonic-clonic) seizures
·         Contraindicated in absence seizures
·         Nonseizure indications include  
o   trigeminal neuralgia 
o   manic-depressive disorders

·         Closely related to carbamazepine.
·         With improved toxicity profile.
·         Less potent than carbamazepine.
·         Active metabolite.
·         Mechanism of action, similar to carbamazepine It alters Na+ conductance and inhibits high frequency repetitive firing.
·         Hyponatremia
·         Less hypersensitivity and induction of hepatic enzymes than with carb
·         It is the oldest antiepileptic drug.
·         Although considered one of the safest drugs, it has sedative effects.
·         Many consider them the drugs of choice for seizures only in infant
·         Useful for partial, generalized tonic-clonic seizures, and febrile seizures
·         Inhibits high frequency, repetitive firing of neurons only at high concentrations.
·         Sedation.
·         Cognitive impairment.
·         Behavioral changes.
·         Induction of liver enzymes.
·         May worsen absence and atonic seizures.
·         Metabolized to phenobarbital and phenylethylmalonamide (PEMA), both active metabolites,
·         Effective against partial and generalized tonic-clonic seizures.
·         Absorbed completely, low binding to plasma proteins.
·         Should be started slowly to avoid sedation and Gl problems.
·         Its mechanism of action may be closer to phenytoin than the barbiturates.
·         Same as phenobarbital           
·         Sedation occurs early.
·         Gastrointestinal complaints.
·         Fully ionized at body pH, thus active form is valproate ion.
·         One of a series of carboxylic acids with antiepileptic activity. Its amides and esters are also active.
·         Mechanism of action, similar to phenytoin.
·         ↑↑levels of GABA in brain.
A broad-spectrum anti-seizure drug (effective against most partial and generalized seizures, including myoclonic and absence seizures)
 Non-seizure indications include:
·         Migraine (prophylaxis) 
·         Bipolar disorder
·         Drug of choice for absence seizures
·         High efficacy and safety.
·         Mechanism of action involves reducing low-threshold Ca2+ channel current in thalamus.
 At high concentrations:
·         Inhibits GABA aminotransferase.
Phensuximide = less effective
Methsuximide = more toxic
 A benzodiazepine.
·         Long acting drug with efficacy for absence seizures.
·         One of the most potent antiepileptic agents known.
·         Also effective in some cases of myoclonic seizures.
·         Has been tried in infantile spasms.
·         Doses should start small.
·         Presently use as add-on therapy with valproic acid
·         Almost completely absorbed 
·         T1/2 = 24 hrs
·         Low plasma protein binding
·         Also effective in myoclonic and generalized seizures in childhood and absence attacks.
·         Suppresses sustained rapid firing of neurons and produces a voltage and use dependent inactivation of sodium channels, thus its efficacy in partial seizures.
Blocks repetitive firing of cultured neurons, thus its mechanism may involve blocking of voltage-dependent sodium channels.
·         Somnolence
·         Fatigue
·         Dizziness
·         Cognitive slowing
·         Paresthesia
·         Nervousness
·         Confusion
·         Urolithiasis
·         Sulfonamide derivative
·         T1/2= l - 3 days
·         Effective against partial and generalized tonic-clonic seizures.
·         Mechanism of action involves voltage and use-dependent inactivation of sodium channels (?).
·         May also involve Ca2+ channels.
           Effective against partial seizures but has severe side effects.
 Because of its severe side effects, it has been relegated to a third-line drug used only for refractory cases.

GABAPENTIN (Neurontin)
·         Used as an adjunct in partial and generalized tonic-clonic seizures.
·         Does not induce liver enzymes.
·         Not bound to plasma proteins. 
·         Drug-drug interactions are negligible.   
·         Low potency.
Status Epilepticus
·         Status epilepticus exists when seizures recur within a short period, such that baseline consciousness is not regained between the seizures.
·         They last for at least 30 minutes.
·         Can lead to systemic hypoxia, academia, hyperpyrexia, cardiovascular collapse, and renal shutdown.
·         The most common, generalized tonic-clonic status epilepticus is life threatening and must be treated immediately with concomitant cardiovascular, respiratory and metabolic management.
·         Benzodiazepines       
·         Given I.V.
·         Lorazepam may be longer acting.
·         First line drugs for treating status epilepticus
·         Have muscle relaxant activity.
·         Potentiates GABA function, by increasing the frequency of channel opening.  
·         Treatment of Status Epilepticus in Adults
 Diazepam, i.v. 5-10 mg (1-2 mg/min)
           repeat dose (5-10 mg) every 20-30 min.
 Lorazepam, i.v. 2-6 mg (l mg/min)
           repeat dose (2-6 mg) every 20-30 min.
           Phenytoin, i.v. 15-20 mg/Kg (30-50 mg/min).
           repeat dose (100-150 mg) every 30 min.       
           Phenobarbital, i.v. 10-20 mg/Kg (25-30mg/min).
           repeat dose (120-240 mg) every 20 min.



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item Psychopharmacology: Antiepileptics antiseizures anticonvulsants
Psychopharmacology: Antiepileptics antiseizures anticonvulsants
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