Levetiracetam

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Dosage-adjustment-in-renal-failure 5 Pharmacokinetics 6 Adverse-effects 7 Drug-interactions 8 Mechanism-of-action 9 More General Terms 10 Additional Terms 11 Internet Database 12 References

Introduction

• Tradename: Keppra.

Indications

• adjunctive agent for partial seizures
• adjunctive agent for generalized seizures [4]
• effective for myoclonic seizures [5]
• bipolar disorder (unlabeled use)
• neuropathic pain (unlabeled use)

• Pregnancy category: C

Dosage

• start 500 mg PO BID
• may increase every 3 days
• maximum 3000 mg/day
• pediatrics: start 10 mg/kg/day; maximum 30 mg/kg/day

• Tabs: 250, 500, 750 (tablets may be crushed)
• Solution: 100 mg/mL (480 mL)

Dosage-adjustment-in-renal-failure

• creatinine clearance 50-80 mL/min: 500-1000 mg BID
• creatinine clearance 30-50 mL/min: 250-750 mg BID
• creatinine clearance < 30 mL/min: 250-500 mg BID
• ESRD: 500-1000 mg/day, supplemental dose of 250-500 mg after dialysis

Pharmacokinetics

• bioavailability 100%, food may delay absorption
• peak effect 1 hour
• protein binding < 10%
• elimination 1/2life 608 hours
• excreted in urine 66% as unchanged drug

Adverse-effects

• common (> 10%)

• behavioral symptoms (13% {adults}, 38% {children})
• somnolence (15-23%)
• headache (14%)
• vomiting (15%), anorexia (13%)
• weakness (9-15%)
• cough (2-11%)
• irritability
• depression

• less common (1-10%)

• facial edema, nervousness, dizziness, ataxia, vertigo, confusion, paresthesia, diplopia, conjunctivitis, pharyngitis, asthma leukopenia ( neutropenia), albuminuria

• uncommon (< 1%)

• alopecia, thrombocytopenia, pancytopenia
• 3-fold increased risk of suicide [6]
  

• drug adverse effects of anticonvulsants

Drug-interactions

• none with other anticonvulsants

Mechanism-of-action

• inhibition of votage-dependent N-type Ca+2 channels
• inhibition of inhibitory GABA-ergic activity
• diminishes delayed rectifier K+ current
• binds synaptic proteins which modulate neurotransmitter release ( SV2A)

More General Terms

• anticonvulsant

Additional Terms

• seizure; epileptic seizure
• Synaptic vesicle glycoprotein 2A (SV2A, KIAA0736, PSEC0174)

Internet Database

PubChem: 441341
PubChem: 5284583
PubChem: 59708

References

1. Prescriber's Letter 7(5):28, May 2000
2. Kaiser Permanente Northern California, Drug update, 9/2000
3. Lexi-Comp, Drug Information 2005
4. Berkovic SF et al, Placebo-controlled study of levetiracetam in idiopathic generalized epilepsy. Neurology 2007, 69:1751 PMID: [1]
5. Medical Knowledge Self Assessment Program (MKSAP) 15, American College of Physicians, Philadelphia 2009
6. Andersohn F et al, Use of antiepileptic drugs in epilepsy and the risk of self-harm or suicidal behavior Neurology 2010;75:335-340 <PubMed> PMID: [2] <Internet> [3]

levetiracetam (Keppra, Etiracetam)