 |
 |
Introduction
Levocarnitine is an amino acid used to treat carnitine
deficiency. Levocarnitine is a vitamin like nutrient related to
vitamins of the B-Group. Another name of Levocarnitine is
vitamin BT (T=Tenebrio). |
Composition
Each tablet contains Levocarnitine USP 330 mg.
Carnitine & Carnitine deficiency
Carnitine is a naturally occurring hydrophilic amino acid
derivative. Dietary source of Levocarnitine are red meat (90%) &
dairy products. Levocarnitine produced endogenously in the kidneys &
liver from lysine & methionine. It plays an essential role in the
transfer of long-chain fatty acids into the mitochondria for
beta-oxidation.
Carnitine deficiency is a metabolic state in which carnitine
concentrations in plasma and tissues are less than the levels
required for normal function of the organs. Biological effects of
low carnitine levels may not be clinically significant until they
reach less than 10-20% of normal. Carnitine deficiency may be
primary or secondary.
Pharmacology
Levocarnitine (Carnitin) is required in mammalian energy metabolism.
It has been shown to facilitate long-chain fatty acid entry into
cellular mitochondria, therefore delivering substrate for oxidation
and subsequent energy production. Carnitine binds acyl residues and
helps in their elimination, decreasing the number of acyl residues
conjugated with coenzyme A (CoA) and increasing the ratio between
free and acylated CoA.
Mechanism
Levocarnitine is essential to transport long chain fatty acids
across the mitochondrial membrane, for subsequent fat breakdown &
energy production.
Pharmacokinetics
Absorption
About 60 to 75% of Levocarnitine from food is absorbed. The
percentage absorbed from supplements appears to be lower. Following
the administration of a dose of Levocarnitine 1,980 milligrams twice
daily, the maximum plasma concentration level (Cmax) was 80
nanomoles per milliliter, and the time to maximum concentration (Tmax)
occurred at 3.3 hours.
Distribution
Following absorption from the intestine, about 25% of Levocarnitine
may be acylated in the intestinal mucosa. Orally administered
Levocarnitine and its acylated metabolite are distributed to most
tissues of the body.
Metabolism and Excretion
Five normal adult male volunteers, administered a dose of
Levocarnitine following 15 days of a high levocarnitine diet and
additional levocarnitine supplement, excreted 58% to 65% of
administered radioactive dose in 5 to 11 days in the urine and
feces. Maximum concentration of Levocarnitine in serum occurred from
2.0 to 4.5 hr after drug administration. Urinary excretion of
levocarnitine was 4% to 8% of the dose. Fecal excretion of total
levocarnitine was less than 1% of total levocarnitine excretion. |
Indications
4Chronic
fatigue syndrome
4Primary
systemic carnitine deficiency
4Congestive
heart failure
4Cardiac
muscle ischemia
4
End stage renal disease (ESRD)
4n
Hyperthyroidism
4
Secondary carnitine deficiency
Dosage and
Administration
Adults: 330 mg 2 or 3 times daily, depending on clinical response.
Infants and Children: 50 to 100 mg/kg/day in divided doses, with a
maximum of 3g/day. Dosage should start at 50mg/kg/day. The exact
dosage will depend on clinical response.
Contraindications
Not known.
Side effects
Generally Levocarnitine is well tolerated. However, few side effects
including abnormal body odor, transient nausea and vomiting,
abdominal cramps and diarrhea may occur.
Precautions
The safety and efficacy of oral Levocarnitine has not been evaluated
in patients with renal insufficiency. Gastrointestinal reactions may
result from too rapid consumption of Levocarnitine. Chronic
administration of high doses of oral Levocarnitine in patients with
severely compromised renal function or in ESRD patients on dialysis
may result in accumulation of the potentially toxic metabolites,
trimethylamine and trimethylamine-N-oxide, since these metabolites
are normally excreted in the urine.
Use in pregnancy and lactation
There are no adequate and well-controlled studies in pregnant women.
This drug should be used during pregnancy only if clearly needed.
Levocarnitine supplementation in nursing mothers has not been
specifically studied.
Drug Interactions
Therapy with valproic acid, the nucleoside analogues didanosine,
zalcitabine and stavudine may produce secondary Levocarnitine
deficiencies. Choline supplementation may lead to increased
Levocarnitine retention.
Carcinogenesis, Mutagenesis,
Impairment of Fertility
Mutagenicity tests performed in Salmonella typhimurium,
Saccharomyces cerevisiae, and Schizosaccharomyces pombe indicate
that Levocarnitine is not mutagenic. No long-term animal studies
have been performed to evaluate the carcinogenic potential of
Levocarnitine.
Over dosage
There have been no reports of toxicity from Levocarnitine over
dosage.
How Supplied
Each box contains 3 strips of 10 tablets.
 |
