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Anti-Epileptic Drugs, Treatment of Seizure Disorder, Status Epilepticus,…

- - - - Oldest anticonvulsant (1912)
        
        Disadvantages - Seizures on stopping drug, dangerous in overdose
        
        Uses – status epilepticus when other drugs fail
        
        Neonatal seizures
  - - - Used for atonic, myoclonic seizures
        
        Disadvantage – tolerance, physical dependence
  - - - Use - West’s syndrome – esp assoc with tuberous sclerosis
        
        ADRs- Irreversible retinal dysfunction - visual field defects (30%), psychosis
- - - - MOA - prolongation of Na+ channel inactivation (like phenytoin)
        
        attenuation of Ca2+ mediated T current (like ethosuximide)
        
        inhibits GABA transaminase
        
        inhibits NMDA mediated excitation (repetitive neuronal firing)
      - PK - inhibitor of CYP enzymes
      - Uses - DOC – absence & myoclonic seizures
        
        Very effective – atonic seizures
        
        Also effective for GTCS
        
        Mood stabilizer in mania & bipolar illness
        
        Prophylaxis of migraine
      - DIVALPROEX – sodium valproate + valproic acid
      - ADRs - Drowsiness, ataxia, tremor, alopecia, curling of hair, weight gain (most common)
        
        Fulminant hepatitis (L-carnitine)
        
        Teratogenic - neural tube defects (1-2%), other abnormalities
    - - MOA - prolongation of Na+ channel inactivation & L type Ca2+ channels
        
        enhances GABA
        
        inhibits AMPA receptor
        
        inhibits carbonic anhydrase
      - Uses - Monotherapy for focal & generalized seizures
        
        Lennox-Gastaut syndrome, Dravet’s syndrome, West’s syndrome
        
        bipolar disorder
        
        prophylaxis of migraine
      - ADRs - cognitive defects (26%)
        
        weight loss (85%)
        
        renal calculi (0.5-1.5%)
        
        Oligohydrosis & hyperthermia
        
        Acute myopia & glaucoma
        
        teratogenic – cleft palate
    - - MOA - Blocks voltage gated Na+ channels & Ca2+ channels
        
        Potentiates GABA
        
        Use dependent block of NMDA glutamate receptor
        
        ADRs – aplastic anemia & hepatic failure - Reserved for use in Lennaux Gestaut syndrome & refractory focal seizures
  - - - PK - Poor oral absorption
        
        Different brands are NOT bio-equivalent
        
        Microsomal enzyme inducer – CYP2C, CYP3A & UDPGT - multiple drug interactions
        
        Excretion changes from 1st to zero order kinetics – saturation kinetics - t½ is variable – 12-36 hours
      - Uses - GTCS, focal seizures, status epilepticus
        
        Arrhythmia
        
        promote wound healing (↑collagen synthesis)
      - ADRs - At therapeutic plasma concentrations
        
        Gum hypertrophy, Hirsutism, coarsening of facial features, acne
        
        Hypersensitivity – rash, DLE, lymphadenopathy (pseudolymphoma)
        
        Megaloblastic anemia
        
        Osteomalacia
        
        Hyperglycemia
        
        Cerebellar dysfunction → Nystagmus
        
        Peripheral neuropathy – diminished deep tendon reflexes
        
        Fetal Hydantoin Syndrome
        hypoplastic phalanges, cleft lip & palate, microcephaly
      - ADRs - At toxic plasma concentrations
        
        Cerebellar & vestibular manifestations – ataxia, vertigo, diplopia
        
        Behavioral alteration, confusion, hallucination, rigidity
        
        IV - Local vascular injury, cardiac arrhythmias
      - FOSPHENYTOIN
        
        Water soluble prodrug
        
        Can be given IM & IV (phenytoin – only IV)
        
        Can be injected in saline & glucose (phenytoin cannot be injected in glucose)
        
        Less incidence of cardiac arrhythmias on IV admn
    - - PK - Different brands are NOT bio-equivalent
        
        Substrate & inducer of CYP3A, CYP1A2, CYP2C & UDPGT
      - ADRs – water retention & hyponatremia
        
        Diplopia
        
        rash & SJ syndrome esp in Asians – very common
        
        Teratogenicity
      - Uses - focal seizures, GTCS
        
        trigeminal neuralgia
        
        mania & bipolar illness
    - - MOA - also blocks T-type Ca2+ channels
      - Uses - Monotherapy - GTCS & focal seizures
        
        Absence seizures - Less effective than Ethosuximide & Valproate, but preferred in women who wish to conceive
        
        Lennox-Gastaut syndrome
        - bipolar disorder
      - ADRs – insomnia, ataxia, diplopia, rash, SJ syndrome, DIC
    - - LACOSAMIDE - focal seizures
      - RUFINAMIDE - ADR – shortened QT interval
      - ZONISAMIDE - MOA - Also inhibits Ca2+ ‘T’ current & carbonic anhydrase
        
        used in infantile spasm
        
        ADRs - Renal calculi, oligohydrosis & hyperthermia
    - - MOA - Use-dependent prolongation of inactivated state of Na+ channels
  - - - Ethosuximide
        
        Selective action ONLY on absence seizures – 1st line drug
        
        Valproate preferred if GTCS present along with absence seizures
        
        Also approved for myoclonic seizures
        
        ADRs - Parkinson’s like symptoms, photophobia, leukopenia (irreversible)
    - - Gabapentin, Pregabalin
        
        Structural analogs of GABA
        
        Uses – focal seizures (rarely)
        
        commonly used neuropathic pain, restless leg syndrome, anxiety, fibromyalgia
  - - - ADRs – QT prolongation, blue skin discoloration, retinal & macular abnormalities
        
        3rd line drug for focal seizures
- - - - Most commonly used AED – few side effects & drug interactions
        
        Uses - GTCS in adults & children, focal seizures, myoclonic
  - - - ADR - behavioural changes