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Drugs for Epilepsy

Phenytoin: mechanism of action Selective inhibition of sodium channels, delaying recovery of inactive state
Phenytoin: therapeutic range Narrow therapeutic range (10-20 mcg/dL); above 20 mcg/dL = toxicity
Phenytoin: uses Partial seizures and tonic clonic seizures. Drug of choice for adults and older children
Phenytoin: CNS effects (therapeutic doses) CNS effects are mild
Phenytoin: CNS effects (toxic doses) Nystagmus, sedation, ataxia, diplopia, cognitive impairment
Phenytoin: adverse effects (unique) Gingival hyperplasia, purple glove syndrome, hirsutism
Phenytoin: adverse effects (pregnancy) Teratogenic. Can cause cleft palate, heart malformations, fetal hydantoin syndrome. Decreases synthesis of vitamin K-dependent clotting factors
Phenytoin: adverse effects (reactions) Morbilliform rash, rarely SJS or TEN. FDA recommends testing for HLA-B*1502 in Asian patients
Phenytoin: adverse effects (CV) Cardiac dysrhythmia and hypotension. Contraindicated in patients with heart block
Phenytoin: drug interactions Decreases effects of oral contraceptives, warfarin, glucocorticosteroids
Phenytoin: drug interactions that increase phenytoin levels Diazepam, isoniazid, cimetidine, and alcohol. Also valproic acid
Phenytoin: drug interactions that decreases phenytoin levels Carbamazepine, phenobarbital, and alcohol. Breakthrough seizures can occur
Phenytoin: drug interactions that increases CNS effects Alcohol, barbiturates, CNS depressants
Phenytoin: IV administration uses and adverse effects Used for generalized SE and should be infused slowly because rapid administration can cause cardiovascular collapse
Carbamazepine: mechanism of action Delays recovery of sodium channels from inactivated state
Carbamazepine: uses Partial and tonic-clonic seizures. First choice for partial seizures. Preferred to use in younger children. Also used for bipolar disorder and neuralgia associated with trigeminal and glossopharyngeal nerves
Carbamazepine: adverse effects (CNS) Minimal effect on cognitive function. Preferred over phenytoin or phenobarbital. Administer larger doses at bedtime to reduce adverse CNS effects
Carbamazepine: adverse effects (unique) Induces bone marrow suppression (leukopenia, anemia, thrombocytopenia). Contraindicated in patients with pre-existing hematologic abnormalities
Carbamazepine: adverse effects (pregnancy) Teratogenic, increased risk of spina bifida
Carbamazepine: adverse effects (reactions) Morbilliform rash, photosensitivity, SJS, TEN. FDA recommends testing for HLA-B*1502 in Asian patients
Carbamazepine: adverse effects (renal) Hypoosmolarity due to inhibition of renal excretion of water. Use with caution in patients with heart failure
Carbamazepine: drug interactions Decreases effects of oral contraceptives and warfarin
Carbamazepine: drug interactions that decreases carbamazepine levels Phenytoin and phenobarbital
Carbamazepine: drug interactions and increases carbamazepine levels Grapefruit juice
Valproic acid: mechanism of action Blocks sodium channels, suppresses calcium influx through T-type calcium channels, augment inhibitory influence of GABA
Valproic acid: uses First line drug for all major seizure types. Also used for bipolar disorder and prophylaxis of migraines
Valproic acid: adverse effects (most common) Nausea, vomiting, ingestion
Valproic acid: adverse effects (rare) Hepatotoxicity, pancreatitis
Valproic acid: adverse effects (pregnancy) Teratogenic, NTDs
Valproic acid: adverse effects (other) Rash, weight gain, hair loss, tremor, blood dyscrasia
Valproic acid: drug interactions Topiramate increases risk of hyperammonemia (S/S vomiting, lethargy, altered LOC, altered cognitive function). Valproic acid also increases phenobarbital and phenytoin levels.
Valproic acid: drug interactions that decreases valproic acid levels Carbapenem antibiotics (meropenem and impenem/cilastatin)
Ethosuximide: mechanism of action Inhibits T-type calcium channels
Ethosuximide: pharmacokinetics Does not induce drug-metabolizing enzymes
Ethosuximide: uses Absence seizures
Ethosuximide: adverse effects No significant adverse effects. Drowsiness, dizziness, lethargy with initial treatment (but diminishes with continued use). Nausea and vomiting may occur
Ethosuximide: adverse effects (rare) Systemic lupus erythematosus, leukopenia, aplastic anemia, SJS
Ethosuximide: drug interactions No significant drug interactions
Phenobarbital: mechanism of action Binds to GABA receptors, potentiating effects of GABA
Phenobarbital: uses Partial seizures and tonic-clonic seizures. Also used for daytime sedation and to promote night time sleep
Phenobarbital: adverse effects (CNS) Drowsiness, sedation with initial treatment, depression in adults. Agitation and confusion in elderly. Paradoxical hyperexcitability in children
Phenobarbital: adverse effects (toxic) Nystagmus, ataxia, CNS depression, respiratory depression, death
Phenobarbital: adverse effects (pregnancy) Teratogenic. Decreases vitamin K-dependent clotting factors
Phenobarbital: adverse effects (unique) Increases risk of acute intermittent porphyria. Contraindicated in patients with history of intermittent porphyria. Can also cause physical dependence and disrupts vitamin D metabolism
Phenobarbital: drug interactions Decreases effects of oral contraceptives and warfarin
Phenobarbital: drug interactions that increase phenobarbital levels Valproic acid
Phenobarbital: drug interactions that increase CNS effects Benzodiazepines, opioids, alcohol, other CNS depressants
Gabapentin: mechanism of action Unknown. Probably promotes GABA release
Gabapentin: uses Adjunct to partial seizure therapy. Recommended for mono therapy. Postherpetic neuralgia
Gabapentin: uses (off label) Neuropathic pain, prophylaxis of migraines, fibromyalgia, postmenopausal hot flushes
Gabapentin: adverse effects Somnolence, dizziness, ataxia, fatigue, nystagmus, peripheral edema (but diminishes over continued use)
Gabapentin: adverse effects (pregnancy) Safety not established
Gabapentin: drug interaction No significant drug interactions
Levetiracetam: mechanism of action Unknown but it does not bind to GABA receptors
Levetiracetam: uses 1) Myoclonic seizures in adults and adolescents over 12 2) Partial seizures in adults and children over 4 3) Tonic-clonic seizures in adults and children over 6
Levetiracetam: uses (off label) Migraine, bipolar disorder, new onset of pediatric epilepsy
Levetiracetam: adverse effects Drowsiness, asthenia
Levetiracetam: adverse effects (CNS) Agitation, anxiety, depression, psychosis, hallucinations, depersonalizations
Levetiracetam: adverse effects (pregnancy) Safety not established
Levetiracetam: drug interactions No interactions
Created by: suezy



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