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Anticonvulsant
Anticonvulsant Agents
Question | Answer |
---|---|
Simple Partial other name? | Focal Epilepsy. |
Simple Partial characteristic | No impairment of consciousness - Awake and aware Jerking arm, leg, face then next steps (Jacksonian March) Unexplained fear, sadness, anger, joy Nausea, odd smells, funny feeling stomach |
Complex Partial other name? | Teporal Lope or Psychomotor |
Complex Partial characteristic | Impairment Consciousness - Unaware surrounding Unresponsive w actions that are clumsy not direct: Picking cloths, take off cloths ... May experienced structured hallucinations |
Gerneralized Tonic - Clonic other name | Grand Mal |
Tonic - Clonic characteristics | Loss of consciousness Suddend cry, fall --> muscle jerks --> Suspend breathing, loss of bladder control (temporary) Only few minutes then normal breathing Tense - Clicking |
Absence other name? | Petit Mal |
Absence characteristics | BRIEFLY impairment or loss of consciousness in children (50% out grow) Blank stare for a few second May have rapid blinking, chewing movement Return after seizures |
Atonic other names | Drop attacks |
Atonic Characteristics | Sudden collapse to floor (10s - 1m) Difficult to treat |
Myoclonic | SUDDEN, BRIEF, massive muscle jerks involves whole body Spill what they are holding or fall off chair |
Infantile Spasm other name? | West's Syndrome |
Infantile Characteristics | Children 3 months - 2 years old Sitting - Head forward, arm forward Lying down, kees drawn up, arm, head forward |
Partial Seizure treatment | Carbamazepin Oxcarbamazepin Lamotrigine = DOC Levetiracetam |
Tonic Clonic treatment | Valproic Acid Levetiracetam Lamotrigine |
Absence treatment | Ethosuximide Valproic Acid |
Myoclonic treatment | Valproic Acid / Lamotrigine - Use in children / Adj: Levetiracetam / |
Infantile treatment | Phenobarbital (also used to Febrile but now Diazepam) Vigabatrin (mono therapy) |
Agents are Gaba - T enzyme inhibitor | Vigabatrin, Valproic Acid |
Agents are Gaba reuptake inhibitor | Tiagabine |
Agents enhance Glutamic acid decarboxylase | Vaproic Acid, Gabapentrin |
Agents are Votage-gated Na+ channel Inhibitor | Phenytoin Felbamate Carbamazepine Vaproic Acid Oxycarbazepine Lamotrigine Topipramate Zonisamide - Rufinamide |
Agents are T-Type Ca2+ inhibitor | Zonisamide / Ethosuximdi/ Lamotrigin / Valproic acid |
Agents are N-Type Ca2+ inhibitor (a2d) | Gabapentin, Pregabalin |
Glutamate AMPA receptor antagonist | Phenobarpital Topiramate |
Glutamate NMDA receptor blockage Glycine binding site | Felbamate |
Do not use Absence --> Worsens | Phenytoin Carbamazepine |
Do not use Myoclonic | Carbamazepine |
Phenytoin ADRs dose related | Sedation, Ataxia, Nystagmus, Diplopia (SAND) |
Phenytoin ADRs Non-dose related | Acne Coarseing of facial fetures Gingival Hyperplasia Hirsutism RASH - Stop immediately Purple Glove Syndrome(IV) CYP 450 inducer Osteomalacia - Vit D Hemorrhage - Vit K Megaloblastic Anemia - Folic Acid Intellectual impair |
Phenytoin indication | Oldest non-sedative agent (low dose) 2nd Partial - Tonic-Clonic Sustained control Status Epilepticus |
Lennox-Gastaut | 2-6 years of age Seizure everyday Multiple Seizure |
Fosphenytoin | Injectable prodrug of Phenytoin - DOES not appear Purple Glove Syndrome |
Agents associated with Rash | Phenytoin, Carbamazepin, Lamotrigine |
Phenytoin interaction? | Valproic Acid --> Displace Phenytoin from albumin and inhibit its metabolism |
Rufinamide MOA | Prolong inactive state Na+ channel |
Rufinamide Indication | Adj Lennnox Gastatut Syndrome in patient > 4 YEARS Take with Food --> Bioavailability |
Rufinamide ADRs | Sonolence, Headache, Abormal Vision, Nause Can shorten QT (Avoid Digoxin or Magnesium - shorten PT) |
Carbamazepine MOA | Inhibits voltage gate Na+ channel |
Carbamazepine indication | Partial Seizure - DOC / Trigeminal Neuralgia / Bibolar Disorder (patient non responsive Lithium) |
Carbamazepine contraindication? | Absence and Myoclonic |
Carbamazepin ADRs | # Phenytoin - (S)AND Leukopenia (10%) ADH release - HYPONATREMIA Inducer own metabolism --> Increase dose 1st month RAsh APLASTIC ANEMIA (1:20.000) COGNITIVE IMPAIRMENT (Less Phenytoin but STILL moderate) |
Oxcarbazepine | Prodrug --> MDH active form / Na+ channel HYPONATREMIA more that Carbamazepine LESS CYP450 induction, less drug interaction than Carbamazepine |
Phenobarbital MOA | 1. Bind GABA receptor Enhance GABA 2. Block AMPA |
Phenobarbital Indication | DOC of Infantile and Febrile (but now Diazepin preferred for Febrile) |
Phenobarbital ADRs | SEDATION (than Phenytoin, Carbamazepin) PARADOXICAL HYPERACTIVTY, behavior changes in children INDUCE CYP 450 - Power Associated Vi K - Hemorrhage |
Agents associated with Cognitive Impairment | Phenytoin / Carbamazepine / Phenobarbital - WORST / Topiramate - 2nd/ Tiagabine / |
Primidone | Prodrug --> PHENOBARBITAL + PEMA Less PARADOXICAL HYPERACTIVITY than Phenobarbital CYP450 inducer |
Felbamate MOA | 1. GABA active 2. NMDA 3. Na+ |
Felbamate indication | Comlex partial Adjunct in Lennox-Gastaut |
Felbamate ADRs | Aplastic Anemia Severe Hepatitis (Pull from the market - REstated INFORM CONSENT) |
Felbamate Favorable | Less cognitive effects |
Lamotrigine MOA | Inhibit RELEASE GLUTAMATE Ca2+ Na+ |
Lamotrigine Indication | DOC - PARTIAL SEIZURE / Myoclonic on Children (Valproic Acid - DOC) / BIPOLAR DISORDER |
Lamotrigine ADRS | RASH 10% Interact with Vaproic Acid --> Increase Lamotrigine |
Lamotrigine ADRs Advantage | Little Cognitive impairment |
Topiramate MOA | GABA / AMPA / Na+ |
Topiramate Indication | NOT 1st choice for any Seizure / Adj Lennox Gastaut > 2 YEARS / Migraine Prophylaxis / Piopar Disorder |
Topiramate ADRs | Weight Loss (+ Pheteramine) Nephrolithiasis FLAT EFFECTS (70%) COGNITIVE Worst 2nd |
GABAPENTIN MOA PREGABALIN | DO NOT bind GABA Bind a2d Voltage Ca2+ Channels (type N) |
GABAPENTIN Indication | ADJUNCT Parial and Tonic-clonic (not mono) |
Gabapentin ADRS | Dizziness, Drowsiness, Ataxia, Edema, WEIGHT GAIN |
Gabapentin Advantage | No drugs interaction (# Levetiractam) |
Pregabalin indication | Neuropathic Pain, Fibromyalgia |
Vigabatrin MOA | Inhibit GABA - Transaminase |
Vigabatrin Indication | Mono therapy for INFANTILE |
Vigabatrin ADRs | Concentrically Constricted Visual Fields (1/3 patients) |
Tiagabine MOA | Inhibits GABA reuptake |
Tiagabine Indication | ADJUNCT partial seizure |
Tiagabin ADRs | More GABA --> Cognitive impairment |
Levetiracetam MOA | Bind to SV2A protein on synaptcic Vesicles / Metabolize = Hydrolysis --> Not CYP450 --> no drug interaction |
Levetiracetam Indication | 1ST for Partial and Tonic-Clonic |
Levetiracetam most Favorable | Less cognitive effects / NO DRUGS INTERACTION |
Ethosuximide MOA | Ca2+ T Type |
Ethosuximide Indiation | DOC Absence (Vaproic also) |
Ethosuximide ADRs | GASTRIC DISTRESS (40%) - Pain N/V: Slowly increase dose to prevent / Ataxia, Rash, hepatoxicity, lupus - like, Drowsiness |
Zonisamide MOA | Ca2+ T Type Na+ |
Zonisamide Indication | Absence (Ca2+) Actually Broad Spectrum |
Zonisamide ADRs | Dizziness, Somlonance / Nephrolithiasis (Topipramate) / weigh loss (Big agent is Topiramate) / RARE OLIGOHYDROSIS , Hyperthermia , Heat Stroke , |
Zonisamide contraindication | Sufonamide Hypersensity |
Benzodiazepines (Clonazepam) MOA | GABA - Frequency |
Clonazepam Indication | 2nd line Absence, Myoclonic, Atonic |
Clonazepam ADR's | SEDATION / TACHYPHYLASIS (rapid tolerance 1-6 months) / PARADOXICAL HYPERACTIVITY |
Diazepam Indication | DOC Febrile STATUS EPILEPTICUS (not chronic treatment) |
Why Diazepam could use for status epilepticus (emergency) | High Lipophilicy fast to brain |
Why Diazepam associated with return seizure | High lipophilicy fast to brain then fast redistribute to tissue stuck there --> reduce concentration |
How to stop return seizure with Diazepam treatment | Combine Phenytoin or Fosphenytoin or Phenobarbital |
Lorazepam | Sometimes IV instead Diazepam - Action prolong, less Lipophilic --> not quick redistribution |
Valproic Acid MOA | GABA-Transaminase Na+ + Mildly Ca+ Stimulate Glutamic Acid Decarboxylase |
Valproic Acid Indication | - 1st Atonic, Myoclonic, Tonic-Clonic - DOC Absences - Migraine prophylaxis - Bipolar Disorder (Broad spectrum) |
Valproic Acid ADRs | GI DISTRESS (N/V) SEVERE idiosyncratic (individual) HEPATOXIC (high risk for thow , 2 YO) WEIGH GAIN (BIG PROBLEM) Minimal Cognitive (BIG ADVANCE) Teratogenic - Spinal bidifa ALOPECIA; PICOS |
Agents have more than 2 MOAs | Felbamate Lamotrigine Topiramate Vaproic Acid |
Anticonvulsant agents most weigh gain ? | VALPROIC ACID Gabapentin |
Valproic Acid Big Problem? | Weight Gain |
Valproic Acid big advance? | Less Cognitive |
Which agent have ALOPECIA (different hair color) | Valproic Acid |
Which agent have PCOS (Polycystic Ovary Syndrome) | Valproic Acid |
Which Agent have pancreatitis | Valproic Acid |
Which agent have own metabolism | Carbamazepin Valproic Acid |
Which agent displace phenytoin from plasma | Valproic Acid |
Which agent inhibits Metabolism of Phenobarbital, Phenytoin (CYP 2C9 subtrates) | Valproic Acid |
Which agent double plasma concentration of Lamotrigine --> Rash | Valproic Acid |
Which AEDs have 40% Gastric Distress as side effects? | Ethosuximide |
Which AEDs caused irreversible concentrically constricted visual fields? | Vigabatrin |
Which AEDs cause hyponatremia | Carbamazepine Oxcarbazepine |
which agent inhibit CYP 450 | Valproic Acid |