(R)-Carnitine
(R)-Carnitine Uses, Dosage, Side Effects, Food Interaction and all others data.
(R)-Carnitine is a naturally occurring substance required in mammalian energy metabolism. It has been shown to facilitate long-chain fatty acid entry into cellular mitochondria, thereby delivering substrate for oxidation and subsequent energy production in the form of Adenosine Tri phosphate or ATP. 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.
(R)-Carnitine is a carrier molecule in the transport of long chain fatty acids across the inner mitochondrial membrane. It also exports acyl groups from subcellular organelles and from cells to urine before they accumulate to toxic concentrations. Lack of carnitine can lead to liver, heart, and muscle problems. Carnitine deficiency is defined biochemically as abnormally low plasma concentrations of free carnitine, less than 20 µmol/L at one week post term and may be associated with low tissue and/or urine concentrations. Further, this condition may be associated with a plasma concentration ratio of acylcarnitine/levocarnitine greater than 0.4 or abnormally elevated concentrations of acylcarnitine in the urine. Only the L isomer of carnitine (sometimes called vitamin BT) affects lipid metabolism. The "vitamin BT" form actually contains D,L-carnitine, which competitively inhibits levocarnitine and can cause deficiency. (R)-Carnitine can be used therapeutically to stimulate gastric and pancreatic secretions and in the treatment of hyperlipoproteinemias.
| Trade Name | (R)-Carnitine |
| Availability | Prescription only |
| Generic | Levocarnitine |
| Levocarnitine Other Names | (R)-Carnitine, Carnitina, Carnitine, L-Carnitine, Levocarnitin, Levocarnitina, Lévocarnitine, Levocarnitine, Levocarnitinum, Vitamin BT |
| Related Drugs | L-Carnitine, Carnitor |
| Type | |
| Formula | C7H15NO3 |
| Weight | Average: 161.1989 Monoisotopic: 161.105193351 |
| Protein binding | None |
| Groups | Approved, Investigational |
| Therapeutic Class | Drugs for muscular energy metabolism |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
The supplemental (R)-Carnitine use is widely established in the management of cardiac ischemia and peripheral arterial disease. It is generally used for cardio protection. It lowers triglyceride levels and increases levels of HDL cholesterol. It is used with benefits in those with primary and secondary carnitine deficiency syndromes. There is also evidence of its use in liver, kidney and immune disorders or in diabetes and Alzheimer's disease. There is little evidence that supplemental (R)-Carnitine boosts energy, increases athletic performance or inhibits obesity. The indications of (R)-Carnitine may be summarized as follows:
- Heart Diseases
- Congestive Heart Failure
- Kidney Disease
- Chronic Fatigue Syndrome
- High Cholesterol
- Intermittent Claudication
- Dementia and memory impairment
- Down Syndrome
- Male infertility
- Hyperthyroidism
(R)-Carnitine is also used to associated treatment for these conditions: Carnitine Deficiency, Congenital carnitine deficiency, Secondary Carnitine deficiency
How (R)-Carnitine works
(R)-Carnitine can be synthesised within the body from the amino acids lysine or methionine. Vitamin C (ascorbic acid) is essential to the synthesis of carnitine. (R)-Carnitine is a carrier molecule in the transport of long chain fatty acids across the inner mitochondrial membrane. It also exports acyl groups from subcellular organelles and from cells to urine before they accumulate to toxic concentrations. Only the L isomer of carnitine (sometimes called vitamin BT) affects lipid metabolism. (R)-Carnitine is handled by several proteins in different pathways including carnitine transporters, carnitine translocases, carnitine acetyltransferases and carnitine palmitoyltransferases.
Dosage
(R)-Carnitine dosage
Tablet-
- 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.Syrup-
- Adults: 10 to 30 ml/day. Dosage should start at 10 ml/day in divided doses, and be increased slowly while assessing tolerance and therapeutic response.
- Infants and children: 50 to 100 mg/kg/day which is equivalent to 0.5 ml/kg/day. 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. 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.
Side Effects
Generally (R)-Carnitine is well tolerated. However, few side effects including transient nausea and vomiting, abdominal cramps, and diarrhoea may occur
Toxicity
LD50 > 8g/kg (mouse, oral). Adverse effects include hypertension, fever, tachycardia and seizures.
Precaution
The safety and efficacy of oral (R)-Carnitine has not been evaluated in patients with renal insufficiency. Chronic administration of high doses of oral (R)-Carnitine in patients with severely compromised renal function or in ESRD patients on dialysis may result in accumulation of the potentially toxic metabolites, trimethylamine (TMA) and trimethylamine-N-oxide (TMAO), since these metabolites are normally excreted in the urine
Interaction
Reports of INR increase with the use of warfarin have been observed. It is recommended that INR levels be monitored in patients on warfarin therapy after the initiation of treatment with levocarnitine or after dose adjustments.
Food Interaction
- Take with food. Taking levocarnitine oral solution with meals may reduce gastrointestinal upset such as nausea, vomiting, and cramping.
Volume of Distribution
The steady state volume of distribution (Vss) of an intravenously administered dose, above endogenous baseline levels, was calculated to be 29.0 +/- 7.1L. However this value is predicted to be an underestimate of the true Vss.
Elimination Route
Absolute bioavailability is 15% (tablets or solution). Time to maximum plasma concentration was found to be 3.3 hours.
Half Life
17.4 hours (elimination) following a single intravenous dose.
Clearance
Total body clearance was found to be a mean of 4L/h.
Elimination Route
Following a single intravenous dose, 73.1 +/- 16% of the dose was excreted in the urine during the 0-24 hour interval. Post administration of oral carnitine supplements, in addition to a high carnitine diet, 58-65% of the administered radioactive dose was recovered from urine and feces in 5-11 days.
Pregnancy & Breastfeeding use
(R)-Carnitine is categorized by the USFDA as Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women. Supplemental (R)-Carnitine should be used by pregnant women only if clearly indicated and only under medical supervision. It is not known whether (R)-Carnitine is excreted in human milk. Supplemental (R)-Carnitine is not advised for nursing mothers. Those with seizure disorders should only use (R)-Carnitine under medical advisement and supervision.
Contraindication
There is no known disease or syndrome in which (R)-Carnitine administration is contraindicated. It is contraindicated in patients with hypersensitivity to any of its components.
Acute Overdose
There have been no reports of toxicity from levocarnitine overdosage. (R)-Carnitine is easily removed from plasma by dialysis. The intravenous LD50 of levocarnitine in rats is 5.4 g/kg and the oral LD50 of levocarnitine in mice is 19.2 g/kg. Large doses of levocarnitine may cause diarrhea.
Storage Condition
Tablet: Store in a cool & dry place, protected from light & moisture.
Solution: Store in a cool & dry place, protected from light.
Innovators Monograph
You find simplified version here (R)-Carnitine
(R)-Carnitine contains Levocarnitine see full prescribing information from innovator (R)-Carnitine Monograph, (R)-Carnitine MSDS, (R)-Carnitine FDA label
FAQ
What is (R)-Carnitine used for?
(R)-Carnitine is used to prevent and treat a lack of carnitine. It is used to prevent and treat this condition in patients with kidney disease on dialysis. It is given to people whose body cannot properly use carnitine from their diet.
How safe is (R)-Carnitine?
In one review of (R)-Carnitine safety, doses of approximately 2 grams per day appeared to be safe for long-term use.
How does (R)-Carnitine work?
(R)-Carnitine is a naturally occurring substance that the cells of mammals need to produce energy. It is used to treat carnitine deficiency. (R)-Carnitine is a small protein that binds to and helps transport fatty acids into the mitochondria, the site of energy production within cells.
What are the common side effects of (R)-Carnitine?
The common side effects of (R)-Carnitine are upset stomach, nausea, vomiting, diarrhea, headache, muscle pain/weakness, swelling of hands/lower legs/feet, tingling skin, or body odor ("fishy" smell) may occur. If any of these effects persist or worsen, contact your doctor or pharmacist promptly.
Is (R)-Carnitine safe during pregnancy?
Use is not recommended unless clearly needed. Stopping treatment in a pregnant woman with primary systemic carnitine deficiency may carry serious consequences; the risk of stopping treatment may outweigh the theoretical risks to the fetus of continuing.
Is (R)-Carnitine safe during breastfeeding?
Taking (R)-Carnitine is possibly safe in breast-feeding women when taken by mouth in the amounts recommended. Small amounts of (R)-Carnitine have been given to infants in breast milk and formula with no reported side effects.
Can I drink alcohol with (R)-Carnitine?
You had better stay away from alcohol in any form while you are on this (R)-Carnitine and for three days afterward. Read labels carefully and avoid even small amounts of alcohol, as found, for instance, in cough syrups.
When should I take (R)-Carnitine?
Take (R)-Carnitine with or just after meals.
How often should I take (R)-Carnitine?
(R)-Carnitine should be taken at evenly spaced intervals every 3 or 4 hours.
How long does (R)-Carnitine take to work?
(R)-Carnitine levels increase rapidly after i.v. administration (500 mg) to healthy volunteers declining to baseline after 12 h; (R)-Carnitine levels increase more slowly, reach a peak in 30–60 min, and decline to baseline within 24 h.
Should I take (R)-Carnitine on an empty stomach?
(R)-Carnitine supplements are therefore likely to be much better absorbed on an empty stomach.
What is the half life of (R)-Carnitine?
Using plasma concentrations uncorrected for endogenous (R)-Carnitine, the mean distribution half life was 0.585 hours and the mean apparent terminal elimination half life was 17.4 hours.
How long can I take (R)-Carnitine?
(R)-Carnitine is likely safe when taken for up to 12 months.
Is it safe to take (R)-Carnitine everyday?
Doses of 2 grams or less per day seem to be well tolerated and safe for most people. Tentative evidence suggests (R)-Carnitine supplements might increase your risk of atherosclerosis.
Who should not take (R)-Carnitine?
Do not take (R)-Carnitine if you are allergic to it. Seek immediate medical attention if you notice any symptoms such as skin rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, breathing difficulty, etc.
What happens if I miss a dose?
Oral forms: If you missed a dose of (R)-Carnitine, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Do not take two doses together to make up for a missed dose.
Injection: Since (R)-Carnitine is given in the hospital setting by a qualified healthcare professional, the likelihood of missing a dose is very low.
What happens if I overdose on (R)-Carnitine?
Oral forms: Never take more than the prescribed dose of (R)-Carnitine. If you suspect that you might have taken an overdose of this medicine, seek immediate medical help.
Injection: Since (R)-Carnitine is administered by a healthcare professional, the chances of overdose are very less. However, your doctor will take measures if an overdose is suspected
Can (R)-Carnitine affect my kidneys?
(R)-Carnitine is excreted from the kidneys. If you have kidney problems this medicine may accumulate in your kidneys and leads to serious side effects. Your doctor may adjust the dose of this medicine based on your clinical condition. (R)-Carnitine is not recommended for use if you have severe kidney problems.
Does (R)-Carnitine cause fatty liver?
Firstly, reduced levels of (R)-Carnitine may lower fatty acid oxidation and be a contributing factor in the accumulation of liver fat.
Does (R)-Carnitine cause heart disease?
(R)-Carnitine can absolutely cause heart disease - but only if you have the gut microbes needed to break it down.
Can (R)-Carnitine raise blood pressure?
(R)-Carnitine shown strong correlations between insulin resistance and increased blood pressure.
