Kefei Injection

Renal Care Kefei InjectionRenal Care Kefei Injection

COMPOSITION

Each vial of Kefei levocarnitine injection contains 1.0g levocarnitine.

PHARMACOLOGY

Carnitine, like many biologically active molecules, exists in two forms: L-Carnitine and D-Carnitine. These two forms or isomers are mirror images of each other. Only L-Carnitine is the naturally occurring and effective form to treat serious carnitine deficiency. D-Carnitine does not occur in nature and is harmful to the human body in that it inhibits the utilization of L-Carnitine.

TOXICOLOGY

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 levocamitine. In the researches of procreation on mice and rabbit with the human dose of 3.8 times animal body surface area shows that no harm to genitalia or fetus. But, no enough clinical researches had been done on pregnant to demonstrate its safety. The animal researches only foresee human's reaction. Only in needed can this medicine be used.

PHARMACOKINETICS

The plasma concentrations profiles of levocarnitine after a slow 3 minute intravenous bolus dose of 20 mg/kg of Levocarnitine were described by a two compartment model. Following a single i.v. administration, approximately 76% of the levocarnitine dose was excreted in the urine during the 0-24 hour interval. Using plasma concentrations uncorrected for endogenous levocarnitine. the mean distribution half life was 0.585 hours and the mean apparent terminal elimination half life was 17.4 hours.
Total body clearance of levocarnitine (Dose/AUC including endogenous baseline concentrations) was a mean of 4.00 L/h. Levocarnitine was not bound to plasma protein or albumin when tested at any concentration or with any species including the human. Major metabolites found were trimethlyamine N-oxide, and [3H]-y-butyrobetaine, 58% to 65% of the administered radioactive dose was recovered in the urine and feces in 5 to 11 days.

INDICATIONS

For the chronic treatment of long term hemodialysis in renal failure patients which results in secondary carnitine deficiency. In the reported cases, the clinical presentation consisted of myocardiosis, skeletal muscles disease, arrhythmia, hyperlipemia, muscle convulsion in patients of hypotension and hemodialysis.

DOSAGE AND USAGE

The recommended starting dose is 10-20 mg/kg body weight, dissolving in 5-10ml of injection water, as a slow 2-3 minute bolus injection into the venous return line after each dialysis session. Initiation of therapy may be prompted by trough (pre-dialysis) plasma levocarnitine concentrations that are below normal (40-50 µmol/L). Dose adjustments should be guided by trough (pre-dialysis) levocarnitine concentrations, and downward dose adjustments (e.g. to 5 rug/kg after dialysis) may be made as early as the third or fourth week of therapy.

ADVERSE REACTION

Transient nausea and vomiting have been observed. Less frequent adverse reactions are body odor, nausea, and gastritis. An incidence for these reactions is difficult to estimate due to the confounding effects of the underlying pathology. Seizures have been reported to occur in patients, with or without pre-existing seizure activity, receiving either oral or intravenous levocarnitine. In patients with pre-existing seizure activity, an increase in seizure frequency and/or severity has been reported. The table below lists the adverse events that have been reported in two double-blind, placebo-controlled trials in patients on chronic hemodialysis. Events occurring at ~5% are reported without regard to causality.

Body as Whole:

Abdominal pain, Accidental injury, Allergic reaction, Asthenia, Back pain, Chest pain, Fever, Flu syndrome, Headache, Infection, Injection site reaction, Pain.

Cardiovascular:

Arrhythmia, Atrial fibrillation, Cardio-vascular disorder, Electrocardiogram abnormal, Hemorrhage, Hypertension, Hypotension, Palpitations, Tachycardia, Vascular disorder.

Digestive:

Anorexia, Constipation, Diarrhea, Dyspepsia, Gastrointestinal disorder, Melena, Nausea, Stomach atony, Vomiting. Endocrine System, Parathyroid disorder. Hemic/Lymphatic, Anemia.

Metabolic/Nutritional:

Hypercalcemia, Hyperkalemia, Hypervolemia, Peripheral edema, Weight decrease, Weight increase.

Musculo-Skeletal:

Leg cramps, Myalgia.

Nervous:

Anxiety, Depression, Dizziness, Drug dependence, Hypertonia, Insomnia Paresthesia, Vertigo.

Respiratory:

Bronchitis, Cough increase, Dyspnea, Pharyngitis, Respiratory disorder, Rhinitis, Sinusitis, Skin and Appendages, Pruritus, Rash.

Special Senses:

Amblyopia, Eye disorder, Taste perversion.

Urogenital:

Urinary tract infect Kidney failure.

CONTRAINDICATION:

The patient should avoid levocarnitine if allergy to it.

PRECAUTION:

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

PREGNANCY

Reproductive studies have been performed in animals and have revealed no evidence of impaired fertility or harm to the fetus due to Levocarnitine. There are, however, no adequate and well controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

NURSING MOTHERS

Levocarnitine supplementation in nursing mothers has not been specifically studied. In nursing mothers receiving levocarnitine, any risks to the child of excess carnitine intake need to be weighed against the benefits of levocarnitine supplementation to the mother. Consideration may be given to discontinuation of nursing or of levocarnitine treatment.

PEDIATRIC USAGE

See DOSAGE AND ADMINISTRATION.

GERIATRIC USAGE

By now no studies of levocarnitine had been done on geriatric for safety, but the studies forecast that no any special limited condition for geriatric usage.

MEDICINE INTERACTION

From the underlying metabolism, the patient who accepts the Valproic acid treatment needs a higher dose of levocarnitine.

OVER DOSAGE

There have been no reports of toxicity from levocarnitine overdosage. Levocarnitine is easily removed from plasma by dialysis.

HOW SUPPLIED

Kefei (Ievocarnitine for injection) is available in…….... 1gm

Each vial contains

Levocarnitine………………………… 1gm

SHELF LIFE

Kefei levocarnitine injection should not be used beyond the expiry date imprinted on the product package/Label

STORAGE

Store in a cool & dry place, below 20°C. Protect from heat & sunlight. Use immediately after reconstitution