ANTISEIZURE DRUGS

SEIZURE 
Is

a finite episodes of brain dysfunction resulting from abnormal discharge of cerebral neurons.  PRIMARY SEIZURES 
SECONDARY

SEIZURES

CLASSIFICATION OF SEIZURE TYPES

PARTIAL SEIZURES Simple partial seizures Complex partial seizures Partial seizures secondarily generalized

CLASSIFICATION OF SEIZURE TYPES GENERALIZED SEIZURES  Generalized tonic-clonic (grand mal) Sz tonic Absence (petit mal) seizures  Tonic/ Atonic Seizures  Clonic & myoclonic seizures  Infantile Spasms  Febrile Seizures  Status Epilepticus .

PRIMARY DRUGS  CARBAMAZEPINE  PHENYTOIN  VALPROIC ACID  PHENOBARBITAL  PRIMIDONE  DIAZEPAM /LORAZEPAM  CLONAZEPAM  ETHOSUXIMIDE .

ADJUNCTIVE DRUGS FELBAMATE LAMOTRIGINE TOPIRAMATE LEVETIRACETAM GABAPENTIN TIAGABINE VIGABATRIN ZONISAMIDE .

clonazepam III MYOCLONIC SEIZURES  Valproic acid. Phenytoin. valproic acid.ANTISEIZURES CLASSIFICATION I. valproic acid II.ABSENCE SEIZURES  Ethosuximide. clonazepam IV. TONIC-CLONIC & PARTIAL SEIZURES TONIC Carbamazepine. ADJUNCT/NEWER ANTICONVULSANTS .

vigabatrin. carbamazepine.phenobarbital gabapentin. lamotrigine  Inhibition of calcium channel function: ethosuximde  Enhancement of GABA action: action: benzodiazepines. tiagabine  Multiple & Complex Mechanism: Valproic Acid .MECHANISM OF ACTION  Inhibition of sodium channels function: function: phenytoin.

Antiarrhymic drug0 Oral.PHENYTOIN         BLOCK SODIUM CHANNELS USE: partial seizures. ethotoin. mephenytoin. generalized tonic-clonic tonicseizures. phenacemide . dose dependent elimination Fosphophytoin. IV highly bound to plasma proteins T ½ 12 -36 hrs Metabolized.

Phenytoin Adverse Effects  nystagmus. mild peripheral neuropathy. sedation. skin rash. megaloblastic anemia fever. gingival hyperplasia & hirsutism. ataxia. fetal hydantoin syndrome . diplopia. coarsening of facial features.

valproate & phenylbutazone: displace phenytoin from binding sites 2. sulfas. phenylbutazone.PHENYTOIN DRUG INTERACTIONS 1. chloramphenicol: inhibits phenytoin metabolism . disulfiram. warfarin. Cimetidine. Sulfonamides. isoniazid. doxycycline.

PHENYTOIN decreases serum levels of: carbamazepine. warfarin . oral contraceptives. pyridoxine. quinidine.PHENYTOIN DRUG INTERACTIONS 3.Barbiturates & carbamazepine. theophylline: enhance phenytoin metabolism 4. theophylline. corticosteroids. chloramphenicol. haloperidol.

idiosyncratic blood dyscrasias. aplastic anemia & agranulocytosis.CARBAMAZEPINE  BLOCK SODIUM CHANNELS  DOC for partial seizures  Generalized tonic-clonic seizures tonic Trigeminal neuralgia  Mania:bipolar disorders  Orally absorbed with slow distribution  Completely metabolized  CAUSE: diplopia & ataxia. leukopenia .

. Carbamazepine increases drug levels : cimetidine.CARBAMAZEPINE DRUG INTERACTIONS 1. oral contraceptives. erythromycin. Decrease carbamazepine levels via increase metabolism: phenytoin. phenytoin. doxycycline. Carbamazepine decreases drug levels :warfarin. Increase carbamazepine levels via metabolism: cimetidine. isoniazid 2. Lithium induces carbamazepine toxicity. haloperidol 4. isoniazid 5. valproic acid 3.

generalized tonictonicclonic seizures  May cause: CNS depression  Tolerance & dependence CI in porphyria disorders  Enhancement .PHENOBARBITAL of inhibitory process  Dimimution of excitatory transmission  USE: partial seizures.

doxycycline. rifampin  Barbiturates decrease serum levels: tricyclics. chloramphenicol. pyridoxine.PHENOBARBITAL DRUG INTERACTIONS phenobarbital levels via metabolism. digitoxin. beta blockers. valproic acid  Decrease phenobarbital levels via increase metabolism. metronidazole. chronic alcohol ingestion. oral contraceptives. acute ethanol ingestion. theophyllline  Increase . warfarin.

GIT upset.PRIMIDONE  Metabolized to:  PHENOBARBITAL  PHENYLETHYLMALONAMIDE(PEMA)  Mechanism of action similar to phenytoin  May cause sedation. ataxia. megaloblastic anemia  CI: porphyria. hypersensitivity . vertigo.

behavioral & mood changes.VIGABATRIN  Inhibits GABA transaminase  Partial seizures & WEST syndrome  In patients unresponsive to conventional drugs  Rapid absorption  T ½ 6 -8 hrs  CAUSES: drowsiness. visual field defect . weight gain.

LAMOTRIGINE  Inhibits sodium channels  Partial seizures  Absense seizures  Completely absorbed  T ½ of 24 hours  Broad therapeutic profile  CAUSES: hypersensitivity rxns. life threatening skin disorders. diplopia. dizziness. hematotoxicity . ataxia. headache.

FELBAMATE  MOA is unknown  For partial seizures  Broad therapeutic profile  For intractable cases  T ½ is 20 hrs  CAUSES: severe hypersensitivity aplastic anemia. hepatotoxicity  Increase plasma phenytoin & valproic acid  Decrease carbamazepine levels rxs .

GABAPENTIN alters GABA metabolism. headache & tremor  MOA: . its nonsynaptic release or its reuptake by GABA transporters  Also binds to the 2 subunit of voltage sensitive calcium channels  FOR PARTIAL & GENERALIZED SEIZURES  SATURABLE ABSORPTION CAUSE: somnolence. dizziness. ataxia.

weight loss . blocks voltage dependent sodium channels  Similar to phenytoin with lower side effects & simpler pharmacokinetics  Risk of teratogenesis  Sedation. renal stones. mental dulling.TOPIRAMATE  Complex action: GABA effect.

difficulty in concentration. tremor. psychosis .TIAGABINE  Nicotinic acid derivative  GABA uptake inhibitor in both neurons & glia  Partial seizures  Dizziness.

ETHOSUXIMIDE        DOC for absense seizures Effect on calcium channels( reduce low threshold (T type) currents Inhibits NA/K/ ATPase. depresses the cerebral metabolic rate & inhibits GABA aminotransferase Absorption is complete Completely metabolized CAUSES. gastric distress. lethargy & headache DI: valproic acid inhibits its metabolixm .

VALPROIC ACID  On partial seizures sodium channel effects  Increased levels of GABA inhibits GABA transaminase & succinic semialdehyde dehydrogenase  Sodium channel blockade .

MIGRAINE PROPHYLAXIS 7. PARTIAL SEIZURES 6. BIPOLAR DISORDER  CLINICAL . ABSENCE SEIZURES 2.VALPROIC ACID USES: 1. ATONIC ATTACKS 5. MYOCLONIC SEIZURES 3. GENERALIZED TONIC-CLONIC TYPE TONICOF SEIZURES 4.

increase in appetite & hair loss.  SPINA BIFIDA . weight gain.VALPROIC ACID  Well absorbed. hepatotoxicity. vomiting. thrombocytopenia. fine tremors. ppc within 2 hrs  Bioavailability > 80%  T ½ is 9 -18 hrs  CAUSES: nausea. sedation uncommon. pain & heart burn.

VALPROIC DRUG INTERACTIONS  Decrease valproic acid levels from increase metabolism with carbamazepine  Increase valproic acid levels with antacid (increase absorption)  salicylates (displacements from binding sites)  When used with clonazepam may precipitate absence status .

BENZODIAZEPINES  Diazepam. lorazepam. clonazepam. Nitrazepam. widely distributed  Extensively metabolized with many active metabolites  May cause sedation. tolerance  DIAZEPAM: DOC for status epilepticus . clorazepate. clobazam  Well absorbed.

STATUS EPILPETICUS  DIAZEPAM  LORAZEPAM  PHENYTOIN  PHENOBARBITAL .

100 TOXIC LEVEL (ug/mL) >8 >20 > 40 > 100 > 100 .12 10 .20 10 .40 50 -100 50 .EFFECTIVE PLASMA LEVELS DRUG Carbamzepine Phenytoin Phenobarbital Ethosuximide Valproic Acid Effective Level(ug/m 4 .

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