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Levocarnitine

A16A - Other alimentary tract and metabolism products ATC A16AA01 Small molecule approved 1985 Oral Parenteral Natural product

JFDA label: Trian Oral Solution

Indications

Approved

  • Brain Diseases — Encephalopathy
  • Kidney Failure, Chronic — chronic kidney disease
  • Muscle Weakness — Muscle weakness

Off-label

  • Acquired Immunodeficiency Syndrome
  • Acute Kidney Injury
  • Arthritis, Rheumatoid
  • Asthma
  • Atrial Fibrillation
  • Carbon Monoxide Poisoning
  • Cytomegalovirus Infections
  • Diabetes Mellitus, Type 2
  • Gastrointestinal Stromal Tumors
  • HIV Infections
  • Heart Failure
  • Hyperthyroidism
  • Hypotension
  • Lipid Metabolism Disorders
  • Multiple Sclerosis
  • Muscle Cramp
  • Muscular Atrophy, Spinal
  • Neoplasms
  • Non-alcoholic Fatty Liver Disease
  • Pancreatic Neoplasms
  • Poisoning
  • Polycystic Ovary Syndrome
  • Postpoliomyelitis Syndrome
  • Pyelonephritis
  • Renal Insufficiency, Chronic
  • Shock, Septic
  • Spinal Cord Injuries
  • beta-Thalassemia

Contraindications

Source: openFDA

  • None known. Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Gastrointestinal disorders (2)

Not Known Abdominal Cramps · These Include Transient Nausea And Vomiting

General disorders and administration site conditions (1)

Not Known L-Carnitine

Dosing

Source: openFDA

® (levocarnitine) Tablets. Adults: The recommended oral dosage for adults is 990 mg two or three times a day using the 330 mg tablets, depending on clinical response. Infants and children: The recommended oral dosage for infants and children is between 50 and 100 mg/kg/day in divided doses, with a maximum of 3 g/day. Dosage should begin at 50 mg/kg/day. The exact dosage will depend on clinical response. Monitoring should include periodic blood chemistries, vital signs, plasma carnitine concentrations and overall clinical condition. CARNITOR ® (levocarnitine) Oral Solution and CARNITOR ® SF (levocarnitine) Sugar-Free Oral Solution. For oral use only. Not for parenteral use. Adults: The recommended dosage of levocarnitine is 1 to 3 g/day for a 50 kg subject, which is equivalent to 10 to 30 mL/day of CARNITOR ® (levocarnitine) Oral Solution or CARNITOR ® SF (levocarnitine) Sugar-Free Oral Solution. Higher doses should be administered only with caution and only where clinical and biochemical considerations make it seem likely that higher doses will be of benefit. Dosage should start at 1 g/day, (10 mL/day), and be increased slowly while assessing tolerance and therapeutic response. Monitoring should include periodic blood chemistries, vital signs, plasma carnitine concentrations, and overall clinical condition. Infants and children: The recommended dosage of levocarnitine is 50 to 100 mg/kg/day which is equivalent to 0.5 mL/kg/day CARNITOR ® (levocarnitine) Oral Solution or CARNITOR ® SF (levocarnitine) Sugar-Free Oral Solution. Higher doses should be administered only with caution and only where clinical and biochemical considerations make it seem likely that higher doses will be of benefit. Dosage should start at 50 mg/kg/day, and be increased slowly to a maximum of 3 g/day (30 mL/day) while assessing tolerance and therapeutic response. Monitoring should include periodic blood chemistries, vital signs, plasma carnitine concentrations, and overall clinical condition. CARNITOR ® (levocarnitine) Oral Solution or CARNITOR ® SF (levocarnitine) Sugar-Free Oral Solution may be consumed alone or dissolved in drink or other liquid food. Doses should be spaced evenly throughout the day (every three or four hours) preferably during or following meals and should be consumed slowly in order to maximize tolerance.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Hypersensitivity Reactions Serious hypersensitivity reactions, including rash, urticaria, and facial edema have been reported with oral CARNITOR ® . Other serious hypersensitivity reactions, including anaphylaxis, laryngeal edema, and bronchospasm have been reported following intravenous levocarnitine administration, mostly in patients with end stage renal disease undergoing dialysis. Discontinue use of CARNITOR ® and instruct patients to seek medical attention if they experience symptoms suggestive of a hypersensitivity reaction.

Pregnancy & Lactation

Lactation

Caution Hale L3

Levocarnitine and acetyl-l-carnitine (acetlycarnitine) are normal components of human milk that are required for fat metabolism.

Chemistry & Properties

2D structure
FormulaC7H15NO3
Molecular weight161.2 g/mol
IUPAC name(3R)-3-hydroxy-4-(trimethylazaniumyl)butanoate
CAS541-15-1
PubChem CID10917
InChIKeyPHIQHXFUZVPYII-ZCFIWIBFSA-N
logP-1.81 (XLogP -0.2)
Polar surface area60.36 Ų
H-bond acceptors / donors3 / 1
Drug-likeness (QED)0.49
Lipinski violations0
SMILESC[N+](C)(C)C[C@H](O)CC(=O)[O-]

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life3.169 h
Volume of distribution0.62 L/kg
Protein binding-0.8%
BBB penetrantNo

Enzyme interactions

EnzymeRoleDetail
CYP2C19Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OCT(unspecified) (Inhibitor)OCT1 (Inhibitor)OCTN1 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)PEPT (Inhibitor)PEPT1 (Inhibitor)MATE1 (Substrate)MATE2 (Substrate)OAT3 (Substrate)OCT(unspecified) (Substrate)OCT2 (Substrate)OCTN1 (Substrate)OCTN2 (Substrate)P-gp (Substrate)

Drug–drug interactions (2, DDInter)

Interacting drugSeverityManagement
Dicoumarol moderate
Warfarin moderate

Registered Products (4)

BrandForm / strengthPackAgentCitizen (JOD)
Trian Solution for Injection Injection 1 g/5 ml 5 ml pack varies Al Hilal Drug Store 2.820
Trian Oral Solution Solution 1 g/10 ml 10 ampoule Al Hilal Drug Store 3.490
Trian Solution for Injection Injection 1 g/5 ml 5 ml pack varies Al Hilal Drug Store 5.370
Trian Solution for Injection Injection 1 g/5 ml 5 ml pack varies Al Hilal Drug Store 25.440