L-Carnitine (levocarnitine)
Levocarnitine Oral Tablet
Last reviewed · Source: First Databank (FDB) drug data
Overview
Levocarnitine is a naturally occurring amino acid derivative essential for mammalian energy metabolism.
Levocarnitine is the synthetic L-isomer (biologic active form) of D,L-carnitine, a constituent of muscle tissue that plays an essential role in the metabolism of fatty acids. Carnitine is derived from 2 essential amino acids (lysine and methionine); it is synthesized in the liver and kidney, and found primarily in cardiac and skeletal muscle. The main dietary source of carnitine is meat products.
Carnitine acts as a carrier molecule facilitating long-chain fatty acid entry into cellular mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain. In skeletal and cardiac muscle, fatty acids are the main substrate for energy production.
Levocarnitine may promote excretion of excess organic or fatty acids in patients with defects in fatty acid metabolism and/or specific organic acid metabolic disorders that result in accumulation of acyl-coenzyme A (acyl-CoA) esters. In patients with secondary carnitine deficiency, levocarnitine eliminates acyl-CoA compounds by promoting formation of acylcarnitine, which is quickly excreted. Levocarnitine increases plasma levocarnitine concentrations in patients with end-stage renal disease undergoing hemodialysis.
The absolute bioavailability of levocarnitine is about 15-16% following oral administration and correction for endogenous plasma levocarnitine concentrations. Peak plasma concentrations are attained 3.3-3.4 hours following oral administration. The rate and extent of distribution from plasma into erythrocytes appear to be minor or negligible.
Levocarnitine does not appear to bind to plasma proteins or albumin. The drug is metabolized principally to TMAO and gamma-butyrobetaine in the GI tract by bacteria. In healthy adults, approximately 9% of a dose is excreted in urine as levocarnitine (uncorrected for endogenous urinary excretion) following oral administration.
Approximately 58-65% of a dose is excreted (as levocarnitine and metabolites) in the urine and feces 5-11 days following oral administration of the radiolabeled drug to patients receiving a high carnitine diet and additional carnitine supplements for 15 days. About 4-8 and <1% of an administered radiolabeled dose is excreted in the urine as levocarnitine and in the feces as total carnitine, respectively. TMAO is principally excreted in the urine (8-49% of administered radiolabeled dose) and gamma-butyrobetaine is principally excreted in the feces (0.44-45% of administered radiolabeled dose).
Approximately 76% of a dose is excreted in the urine within 24 hours following direct IV injection.
USES: This medication is a diet supplement used to prevent and treat low blood levels of carnitine. Carnitine is a substance made in the body from meat and dairy products. It helps the body use certain chemicals (long-chain fatty acids) for energy and to keep you in good health.
Low blood levels of carnitine may occur in people whose bodies cannot properly use carnitine from their diets, people on dialysis due to serious kidney disease, and people being treated with certain drugs (such as valproic acid, zidovudine). Carnitine levels that are too low can cause liver, heart, and muscle problems. Carnitine comes in 2 forms, this medication (levocarnitine) and D-carnitine.
An over-the-counter product called vitamin Bt contains a mixture of levocarnitine and D-carnitine. Vitamin Bt should not be used to treat serious carnitine deficiency since it can interfere with the body's use of levocarnitine. Do not use levocarnitine to treat serious carnitine deficiency unless prescribed by your doctor.
The form of levocarnitine taken by mouth is not recommended for treating people on dialysis due to serious kidney disease. The injectable form should be used for this treatment. Consult your doctor for details.
Some supplement products have been found to contain possibly harmful impurities/additives. Check with your pharmacist for more details about the brand you use. The FDA has not reviewed this product for safety or effectiveness.
Consult your doctor or pharmacist for more details.
Generic name: levocarnitine
Pronunciation: (lee-voh-KAR-nih-teen)
Drug class: Levocarnitine
Therapeutic class: Electrolyte Balance-Nutritional Products
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on L-Carnitine
Indications
No indications are available for this drug.
Dosing
No dosing information is available for this tab.
Administer levocarnitine orally (as a solution or tablets) or by IV injection or infusion.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects reported with oral levocarnitine therapy include transient nausea and vomiting, abdominal cramps, diarrhea, and body odor.
Common adverse effects reported with IV levocarnitine therapy include transient nausea and vomiting, body odor, and gastritis. Patients on chronic hemodialysis may experience injection site reactions, headache, pain, diarrhea, flu syndrome, pharyngitis, infection, hypertension, vomiting, abdominal pain, hypotension, dizziness, increased cough, chest pain, hypercalcemia, accidental injury, asthenia, nausea, fever, anemia, hypervolemia, paresthesia, rhinitis, or dyspnea.
Seizures were reported in patients, with or without preexisting seizure activity, receiving either oral or IV levocarnitine. Increased seizure frequency and/or severity also has been reported in patients with preexisting seizure activity.
Rare or Very Rare
- Anaphylaxis
- Bronchospastic pulmonary disease
- Laryngeal edema
- Muscle weakness
- Seizure disorder
More Frequent
- Abdominal pain with cramps
- Diarrhea
- Nausea
- Vomiting
Less Frequent
- Body odor
- Gastritis
Rare or Very Rare
- Facial edema
- Skin rash
- Urticaria
Precautions
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Dosage of levocarnitine in pediatric patients <=18 years of age was based on specific patient case record observations rather than on studies that specifically defined age by protocol.
There are no adequate and well controlled studies with levocarnitine use in pregnant women. Animal reproduction studies have not shown any evidence of fetal harm. Use during pregnancy only if clearly needed.
Levocarnitine is distributed into milk in cows; it is not known whether the drug is distributed into human milk. Weigh risks and benefits of use in nursing mothers. The manufacturer recommends to consider discontinuance of nursing or the drug.
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ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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