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Chapter 16:Anticonvulsants
DH206: PharmacologyLisa Mayo, RDH, BSDH
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
BOARD DRUGS
Drugs most commonly used for both Gen & Partial Seizures1) Barbiurates (Phenobarbital)2) Phenytoin(Dilantin)3) Carbamazepine (Tegretol)4) Valproic acid (Depakene)5) Primidone (Mysoline)6) Levetiracetam (Keppra)7) Topiramate (Topomax)8) Zonisamide (Zonegram)
Drugs most commonly use for Partial Seizures1) Felbamate (Felbatol)2) Gabapentin (Neurontin)3) Tiagabine (Gabitril)4) Lamotrigine (Lamictal)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
BOARD DRUGS
Drugs most commonly used for Absence Seizures (petit mal)1) Ethosuximide (Zarontin)2) Trimethadione (Tridione)3) Benzodiazepines: Diazepam(Valium),
Clonazepam(Klonopin), Lorazepam(Ativan) Drugs most commonly use for Status Epilepticus
1) Lorazepam(Ativan)2) Diazepam(Valium)3) Phenytoin (Dilantin)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
BOARD DRUGS
Drugs most commonly used for Epileptic Seizures Absence Seizures
1) Ethosuximide (Zarotin)2) Valproic acid (Depakene)3) Lamotigine (Lamictal)
Gen Tonic-Clonic Seizures1) Phenytoin(Dilantin)2) Valproic acid (Depakene)3) Carbamazepine (Tegretol)4) Lamotigine (Lamictal) & Topiramate(Topomax) used on kids a lot (newer
drugs) Partial Seizures
1) Phenytoin(Dilantin)2) Valproic acid (Depakene)3) Carbamazepine (Tegretol)4) Lamotigine (Lamictal) & Topiramate(Topomax)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
1. Seizure Types2. Epilepsy3. First-generation drug4. Second-generation drugs
Outline
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Seizure Types for Review
Generalized Seizures Partial Seizures
Brain Affects both hemispheres Affects 1 hemisphere
Types Absence (last <20sec)Tonic-Clonic (last 1-2min)
SimpleComplex
Consciousness Loses consciousness Does NOT lose consciousness
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Epilepsy
Epilepsy Common CNS disorder: 1:200 people Repeated reoccurrence of seizures Multiple etiologies
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Anti-Epileptic Drug Therapy
Treatment or control of seizures depends on types of seizures the patient experiences Drugs for tonic-clonic not always effective for absence
Adverse Side Effects1) Teratogenic2) P-450 enzyme inducers3) GI
Drugs used for seizures also are used in tx of:1) Anxiety disorders2) Bipolar3) Migraine4) Neuropathic pain
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
First-Generation Drugs
FIRST GENERATION
DRUGS
SEZIURES USED TO TX
ACTION
Phenobarbital(Luminal) All except Absence Enhance GABA
Phenytoin(Dilantin) All except Absence Block Na channels
Carbamazepine(Tegretol)
All seizures Block Na channels
Oxcarbazepine(Trileptal)
All seizures Block Na channels
Valproic Acid(Depakene)
All seizures Block Na channelsEnhance GABA
Ethosuximide(Zarotin) Absence (generalized) Block Ca channels
Clonazepam(Klonopin) Myoclonic in kids Benzo: Enhance GABA
Lorazepam(Ativan) Status epilepticus Benzo: Enhance GABA
ALERTKNOW THIS FOR TESTS & BOARDS
INSTEAD P.197
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Phenobarbital(Luminal) 1st anti-epileptic drug developed Use declining with newer drugs on the market GABA
Phenytoin(Dilantin) 1st line drug for all seizures EXCEPT absence Widely used 1st non-sedating drug Narrow TI Adverse reactions: gingival enlargement, tetratogenic,
vitamin deficiency (D & Folate)
First Generation Drugs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Carbamazepine(Tegretol) Also used for bipolar, trigeminal neuralgia Adverse effects: severe blood disorders which can lead
to gingival bleeding & agranulocytosis Blood lab tests needed for dental tx! Metabolized by P450 enzyme system – drug
interactions
Oxcarbazepine(Trileptal) Similar to Tegretol with less side effects
First Generation Drugs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Valproic Acid(Depakene) Many adverse effects
Inhibit platelet aggregation: increase bleeding times
3 BLACK BOX WARNINGS1)Severe, fatal hepatoxic rxns <2yrs2)Tetratogenic: Pregnancy category D
(neural tube defects)3)Life-threatening pancreatitis
First Generation Drugs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
First Generation Drugs
Ethosuximide (Zarontin) Drug of choice for absence seizures Adverse effects
Leukopenia (↓ WBC) Gingival enlargement Hiccups
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Second-Generation Drugs Newer drugs Less side effects because more specific sites of action
SECOND GENERATION DRUGS
Levetiracetam(Keppra)
Tiagabine(Gabitril)
Lamotrigine(Lamictal)
Gabapentin(Neurotin)
Pregabalin(Lyrica)
Felbamate(Felbatol)
Topiramate(Topamax)
Zonisamide(Zonegran)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Second-Generation Drugs
Felbamate(Felbatol)Gabapentin(Neurontin)
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Felbamate(Felbatol) Action: Block Na & Ca channels Drug used when patient unresponsive to other
anticonvulsants Use ONLY when benefits would outweigh the adverse
effects
Gabapentin(Neurotin) Only used for partial seizures Action: Blocks Ca channels One major advantage over the other anticonvulsants:
does not affect hepatic microsomal enzymes, little drug interactions
Second-Generation Drugs
Not in your book but need to know Both been on boards in recent yrs
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
All of the following drugs are anticonvulsants EXCEPT which one?a. Gabapentin(Neurontin)b. Carbamazepine(Tegretol)c. Phenytoin(Dilantin)d. Nifedipine(Procardia)e. Diazepam(Valium)f. Valproic acid(Depakene)
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
All of the following drugs are anticonvulsants EXCEPT which one?a. Gabapentin(Neurontin)b. Carbamazepine(Tegretol)c. Phenytoin(Dilantin)d. Nifedipine(Procardia) CCBe. Diazepam(Valium)f. Valproic acid(Depakene)
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Which of the following anti-epileptic drugs decreases doxycycline levels?a. Primidoneb. Levetiracetamc. Phenytoin(Dilantin)d. Valproic acid(Depakene)
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Which of the following anti-epileptic drugs decreases doxycycline levels?a. Primidoneb. Levetiracetamc. Phenytoin(Dilantin)d. Valproic acid(Depakene)
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Which of the following anti-epileptic drugs increases incidence of gingival enlargement?a. Phenobarbitalb. Lamotriginec. Carmazepined. Phenytoine. Depakenef. Ethosuximide
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Which of the following anti-epileptic drugs increases incidence of gingival enlargement?a. Phenobarbitalb. Lamotriginec. Carmazepined. Phenytoine. Depakenef. Ethosuximide
NBQ
Copyright © 2011, 2007 Mosby, Inc., an affiliate of Elsevier. All rights reserved.
Which of the following anti-epileptic drugs can also be used in the treatment of trigeminal neuralgia?a. Phenobarbitalb. Lamotriginec. Carmazepined. Phenytoine. Tegretolf. Primidone
NBQ