Prevention and treatment of carnitine deficiency in patients with end-stage renal disease (ESRD) who are undergoing dialysis.

Dietary Supplement

Protein binding: None
Metabolism: Hepatic; Major metabolites: Trimethylamine (TMA) and trimethylamine N-oxide (TMAO)
Bioavailability: Oral solution: 15.9% ± 4.9%; Tablet: 15.1% ± 5.3%
Half-life elimination: 17.4 hours
Time to peak: Oral: 3.3 hours
Excretion: Urine (76%, 4% to 8% as unchanged drug); feces (<1%)

Hypersensitivity to levocarnitine or any component of the formulation.

Teratogenic effects were not observed in animal studies. Carnitine is a naturally occurring substance in mammalian metabolism.

In breast-feeding women, use must be weighed against the potential exposure of the infant to increased carnitine intake.

Cardiovascular: Hypertension (intravenous: 18% to 21%), chest pain (intravenous: 15%)
Central nervous system: Headache (intravenous: 37%), dizziness (intravenous: 15% to 18%), paresthesia (intravenous: 12%)
Endocrine & metabolic: Hypercalcemia (intravenous: 6% to 15%)
Gastrointestinal: Diarrhea (intravenous: 35%), abdominal pain (intravenous: 21%), vomiting (intravenous: 21%), nausea (intravenous: 12%)
Hematologic & oncologic: Anemia (intravenous: 5% to 12%)
Infection: Infection (intravenous: 24%)
Neuromuscular & skeletal: Weakness (intravenous: 9% to 12%)
Respiratory: Cough (intravenous: 18%), rhinitis (intravenous: 11%)
Miscellaneous: Accidental injury (intravenous: 12%), fever (intravenous: 6% to 12%)

1. Carnitine deficiency in patients with ESRD requiring dialysis: 10 to 20 mg/kg (dry body weight) after each dialysis session; guide dosage adjustments by trough (predialysis) levocarnitine concentrations. Evaluate clinical response at 3-month intervals and titrate to the lowest effective dose; therapy should be discontinued if no improvement is seen after 9 to 12 months of therapy.
2. Valproic acid toxicity, acute (off-label use): Initial 100 mg/kg as an IV bolus followed by 50 mg/kg (maximum: 3,000 mg) as an IV bolus or intermittent infusion (over 15 to 30 minutes) every 8 hours; continue until ammonia levels are decreasing and clinical improvement is evident; patients may require several days of therapy.

1. Carnitine deficiency in patients with ESRD requiring dialysis: 10 to 20 mg/kg dry body weight after each dialysis session; evaluate clinical response at 3-month intervals and titrate to the lowest effective dose. Therapy should be discontinued if no improvement after 9 to 12 months of therapy.
2. Valproic acid toxicity, acute (off-label use): Dosing based on level of hepatic involvement and should be adjusted based on clinical response or serum level of valproic acid
(1) No hepatotoxicity: 100 mg/kg/day divided every 6 hours until serum ammonia and valproic acid concentrations begin to decrease and clinical improvement is evident (Max daily dose: 3,000 mg/day )
(2) Symptomatic hyperammonemia or hepatotoxicity: Loading dose 100 mg/kg, maximum loading dose: 6 g; followed by 50 mg/kg/dose (up to 3,000 mg/dose) every 8 hours or 15 mg/kg/dose every 4 hours; continue treatment until serum ammonia concentrations begin to decrease and clinical improvement is evident; patients may require several days of therapy.

There are no dosage adjustments provided in the manufacturer’s labeling; dosage adjustments should be determined by levocarnitine levels and clinical response.

There are no dosage adjustments provided in the manufacturer’s labeling.