Levocarnitine
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
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
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
Levocarnitine and acetyl-l-carnitine (acetlycarnitine) are normal components of human milk that are required for fat metabolism.
Chemistry & Properties
| Formula | C7H15NO3 |
|---|---|
| Molecular weight | 161.2 g/mol |
| IUPAC name | (3R)-3-hydroxy-4-(trimethylazaniumyl)butanoate |
| CAS | 541-15-1 |
| PubChem CID | 10917 |
| InChIKey | PHIQHXFUZVPYII-ZCFIWIBFSA-N |
| logP | -1.81 (XLogP -0.2) |
| Polar surface area | 60.36 Ų |
| H-bond acceptors / donors | 3 / 1 |
| Drug-likeness (QED) | 0.49 |
| Lipinski violations | 0 |
SMILES
C[N+](C)(C)C[C@H](O)CC(=O)[O-]Biology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 3.169 h |
| Volume of distribution | 0.62 L/kg |
| Protein binding | -0.8% |
| BBB penetrant | No |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2C19 | Substrate | — |
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 drug | Severity | Management |
|---|---|---|
| Dicoumarol | moderate | |
| Warfarin | moderate |
Registered Products (4)
| Brand | Form / strength | Pack | Agent | Citizen (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 |