Flashcards in Epilepsy Drugs Deck (56)
1st line Absence
Blocks thalamic T-type Ca++ channels
GI, Fatigue, headache, urticaria, Steven-Johnson syndrome. EFGHIJ
Benzodiazepines (diazepam, lorazepam) clinical use?
1st line for acute Status epilepticus; Also for eclampsia seizures (MgSO4 is first line)
Increase GABA(A) action
Sedation, Tolerance, Dependence, Respiratory Depression
Phenytoin clinical Use:
First Line Tonic-Clinic. First Line-prophylaxis for Status Epilepticus. Also Treats Simple and Complex Seizures
Increase Na+ channel inactivation; zero-order kinetics
Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, peripheral neuropathy, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome) SLE-Like syndrome, induction of CYP-450, lymphadenopathy, Stevens-Johnson Syndrome, Osteopenia
What do you use for parenteral Use?
Carbamazepine Clinical use?
First line for Simple, Complex, and Tonic-clonic. Also first line for trigeminal neuralgia
increase Na channel inactivation
Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of CYP 450-, SIADH, Stevens-Johnson syndrome.
Valproic Acid clinical use?
First line Tonic-Clonic. Also used to treat Simplex, Complex, Tonic-Clonic, Absense. Also used for myoclonic seizures and bipolar disorder.
Valproic Acid Mech:
Increase Na+ channel inactivation, Increase GABA concentration by inhibiting GABA transaminase
Valproic Acid SE:
GI, distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain, contraindicated in pregnancy.
Gabapentin Clinical use?
Simple, Complex, Tonic-Clonic Seizures. Also used for peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder.
Primarily inhibits high voltage activated Ca++ channels; designed as GABA analog
Phenobarbital clinical use:
Simple, Complex, Tonic-Clonic
Increase GABA (A) action
Sedation, tolerance, dependence, induction of CYP450, cardiorespiratory depression.
What drug is 1t line for neonates?
Topiramate Clinical use:
Simple, Complex, Tonic-Clonic. Also used for migraine prevention.
sedation, mental dulling, kidney stones, weight loss
blocks Na+ channels, increase GABA action
Lamotrigine clinical use:
Simple, Complex, Tonic-Clonic, Absence
Blocks voltage-gated Na+ channels
Stevens-Johnson syndrome (must be titrated slowly)
Levetiracetam clinical use:
Simple, Complex, Tonic-Clonic
Unknown; may modulate GABA and glutamate release
Tiagabine clinical use:
Simple and Complex
increase GABA by inhibiting re-uptake
Vigabatrin clinical use:
Simple and Complex
Increase GABA by irreversibly inhibiting GABA transamination.
What is the presentation of Stevens-Johnson syndrome?
Prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal and sloughing.
What is the first line prophylaxis for Status Elipticus?
What is the first line for for Simple?
What is the first line for acute status epilepticus?
Benzos (diazepam, lorazepam)
First line for Tonic - Clonic?
Phenytoin, Carbamazepine, Valproic Acid
First line for complex?
What are the barbiturates?
Phenobarbital, Pentobarbital, Thiopental, Secobarbital
What is the mech of Barbiturates?
Facilitate GABA(A) action by increasing duration of Cl- channel opening, thus decrease neuron firing (barbiDURATES increase duration).
Barbiturates are contraindicated in what?
What is the clinical use of Barbiturates?
Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)
Toxicity of barbiturates?
Respiratory and cardiovascular depression (can be fatal); CNS dperession (can be exacerbated by EtOH use); dependence; drug interactions (induces CYP450). Overdose treatment is supportive (Assist respiration and maintain BP).
Diazepam, lorazepam, triazolam, temazepam, oxacepam, midazolam, chlordiazepoxide, alprazolam.
mech of benzos?
Faciliate GABA(A) action by increasing (FREQUENCY) of Cl- channel opening. Decrease REM sleep. Most have long half-lives and active metabolites
most have long half lifes, what are the exceptions? what does this indicate?
Triazolam, oxazepam, and midazolam: short acting and therefore have a higher addictive potential.
Clinical use of benzos
Anxiety, spaticity, status epilepticus (lorazepam and diazepam), detoxification (especially alcohol withdrawal -DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)
Dependence, additive CNS depression effects with alcohol. less risk of respiratory depression and coma than with barbiturates.
What is the antidote for benzo toxicity?
Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
What are the nonbenzodiazepine hypnotics?
Zolpidem, Zaleplon, esZopiclone. (All ZZZs put you to sleep)
Act via the BZ1 subtype of the GABA receptor. Effects reversed by flumazenil.
Nonbenzodiazepine clinical use: