Levocarnitin

Uses

The supplemental Levocarnitin 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 Levocarnitin boosts energy, increases athletic performance or inhibits obesity. The indications of Levocarnitin 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

Levocarnitin is also used to associated treatment for these conditions: Carnitine Deficiency, Congenital carnitine deficiency, Secondary Carnitine deficiency

How Levocarnitin works

Levocarnitin can be synthesised within the body from the amino acids lysine or methionine. Vitamin C (ascorbic acid) is essential to the synthesis of carnitine. Levocarnitin 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. Levocarnitin is handled by several proteins in different pathways including carnitine transporters, carnitine translocases, carnitine acetyltransferases and carnitine palmitoyltransferases.

Dosage

Levocarnitin 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 Levocarnitin 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 Levocarnitin has not been evaluated in patients with renal insufficiency. Chronic administration of high doses of oral Levocarnitin 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

Levocarnitin is categorized by the USFDA as Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women. Supplemental Levocarnitin should be used by pregnant women only if clearly indicated and only under medical supervision. It is not known whether Levocarnitin is excreted in human milk. Supplemental Levocarnitin is not advised for nursing mothers. Those with seizure disorders should only use Levocarnitin under medical advisement and supervision.

Contraindication

There is no known disease or syndrome in which Levocarnitin 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. Levocarnitin 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.

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