Dosing and uses of Carnitor, carnitine (levocarnitine)
Adult dosage forms and strengths
tablets
- 330mg
- 500mg
capsule
- 250mg
oral solution
- 1g/10mL
injectable solution
- 200mg/mL
Carnitine Deficiency
990 mg PO q8-12hr, up to 3 g/day
50 mg/kg IV bolus, THEN 50 mg/kg over next 24 hr (divided q3-6hr)
End-Stage Renal Disease
Indicated for ESRD in patients on hemodialysis
Initial dose: 10-20 mg/kg IV bolus infused over 2-3 minutes; administer into venous return line after dialysis session
Adjust doses by predialysis levocarnitine concentrations
Downward dose titration may begin as within 3-4 weeks after initiating
Valproic Acid Overdose (Orphan)
For the prevention or treatment of secondary carnitine deficiency in valproic acid toxicity
100 mg/kg IV (not to exceed 6 g/dose) once
May give additional doses of 15 mg/kg IV q4hr infused over 30 min
Recommendations vary; some sources advocate limiting total dose to 3 g/day
Orphan indication sponsor
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
Myopathy (Orphan)
Treatment of zidovudine-induced mitochondrial myopathy
Orphan indication sponsor
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
Rett Syndrome (Orphan)
Acetyl-L-carniticine designated orphan indication for treatment Rett syndrome
Orphan indication sponsor
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
Administration
Consume oral solution slowly, may be mixed with drinks and space doses evenly throughout the day (q3-4hr) preferably during or after meals (may decrease GI distress)
Administer IV bolus slowly over at least 2-3 min
Also sold as a non-pharmacologic health supplement (L-carnitine)
Pediatric dosage forms and strengths
tablets
- 330mg
- 500mg
capsule
- 250mg
oral solution
- 1g/10mL
injectable solution
- 200mg/mL
Carnitine Deficiency
50 mg/kg/day PO divided q8-12hr initially
May increase to 100 mg/kg/day PO divided q8-12hr; not to exceed 3 g/day
IV: 50 mg/kg IV bolus; may repeat 50 mg/kg IV daily if indicated; not to exceed 300 mg/kg
End-Stage Renal Disease
Indicated for ESRD in patients on hemodialysis
Initial dose: 10-20 mg/kg IV bolus infused over 2-3 minutes; administer into venous return line after dialysis session
Adjust doses by predialysis levocarnitine concentrations
Downward dose titration may begin as within 3-4 weeks after initiating
Valproic Acid Overdose (Orphan)
For the prevention or treatment of secondary carnitine deficiency in valproic acid toxicity
Overdose or hyperammonemia: 150-500 mg/kg/day IV; not to exceed 3 g/day or until clinical improvement observed
100 mg/kg/day PO; not to exceed 2 g/day in divided doses
Orphan indication sponsor
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
Rett Syndrome (Orphan)
Acetyl-L-carnitine designated orphan indication for treatment Rett syndrome
Orphan indication sponsor
- sigma-tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd; Gaithersburg, MD 20878
Cardiomyopathy (Orphan)
Treatment of pediatric cardiomyopathy
Orphan indication sponsor
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
Administration
Consume oral solution slowly, may be mixed with drinks and space doses evenly throughout the day (q3-4hr) preferably during or after meals (may decrease GI distress)
Administer IV bolus slowly over at least 2-3 min
Carnitor, carnitine (levocarnitine) adverse (side) effects
Frequency not defined
GI distress
Mild myasthenia in patients with uremia
Hypertension
Headache
Dizziness
Fever
Vomiting
Hypercalcemia
Anemia
Paresthesia
Cough
Tachycardia
Palpitation
Peripheral edema
Vertigo
Rash
Bronchitis
Gastritis
Warnings
Contraindications
None listed by the manufacturer
Cautions
Monitor blood chemistries, plasma carnitine concentration, vital signs
INR may increase in patients receiving warfarin therapy; monitor INR levels following initiation of levocarnitine therapy and after dose adjustments
GI reactions may occur from too rapid consumption of carnitine
Carcinogenic potential unknown
Pregnancy and lactation
Pregnancy category: B
Lactation: not studied, weigh risk/benefit
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Carnitor, carnitine (levocarnitine)
Mechanism of action
Quaternary ammonium compound found in all mammalian tissue (particularly striated muscle)
Important for lipid catabolism; essential for FFA transport from cytosol to mitochondria where they are oxidized
Pharmacokinetics
Bioavailability: 10-20%
Distribution half-life: 0.585 hr
Half-life elimination : 17.4 hr
Peak plasma time: (PO) 3.3 hr
Peak plasma concentration: (PO) 80 umol/L
Protein Bound: None
Total Body Clearance: 4 L/hr
Metabolism: Metabolized to trimethylamine-N-oxide and gamma-butyrobetaine
Excretion: Urine (76%); feces (<1%)
