Fertihope M

Uses

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

Lycopene is an ingredient found in a variety of supplements and vitamins.

HMG CoA reductase inhibitors mediated decreased level of Coenzyme Q10 in blood, Drug induced Myopathy, Protects body against free radical damage with its antioxidant property, Adjuvant therapy in cardiovascular disease especially in angina and congestive heart failure, Immune system depression, Cognitive decline, Useful in the management of Periodontal Disease

Zinc sulfate is a drug used to replenish low levels of zinc or prevent zinc deficiency, or to test for zinc deficiency.

This medication is a mineral used to treat or prevent low levels of zinc alone and together with oral rehydration therapy (ORT). It is also used as a topical astringent. Zinc Sulfate Injection, USP is indicated for use as a supplement to intravenous solutions given for TPN.

Fertihope M is also used to associated treatment for these conditions: Carnitine Deficiency, Congenital carnitine deficiency, Secondary Carnitine deficiencyNutritional supplementationMigraineDry Eyes, Local itching, Localized pain, Localized swelling, Nutritional supplementation

How Fertihope M works

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

Ubidecarenone is an essential cofactor in the mitochondrial electron transport chain. Its functions are the acceptance of electrons from the complex I and II and this activity is vital for the production of ATP. It acts as a mobile redox agent shuttling electrons and protons in the electron transport chain. Ubidecarenone also presents antioxidant activity in mitochondria and cellular membranes, protecting against peroxidation of lipid membranes as well as inhibiting oxidation of LDL-cholesterol.

Zinc inhibits cAMP-induced, chloride-dependent fluid secretion by inhibiting basolateral potassium (K) channels, in in-vitro studies with rat ileum. This study has also shown the specificity of Zn to cAMP-activated K channels, because zinc did not block the calcium (Ca)-mediated K channels. As this study was not performed in Zn-deficient animals, it provides evidence that Zn is probably effective in the absence of Zn deficiency. Zinc also improves the absorption of water and electrolytes, improves regeneration of the intestinal epithelium, increases the levels of brush border enzymes, and enhances the immune response, allowing for a better clearance of the pathogens.

Dosage

Fertihope M 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.

The recommended dose of Co-enzyme Q10 is:

For Co-enzyme Q10 deficiency:150 mg daily.

For mitochondrial disorders:150-160 mg, or 2 mg/kg/day.

For heart failure in adults:100 mg per day divided into 2 or 3 doses.

For recent myocardial infarction:120 mg daily in 2 divided doses.

For high blood pressure:120-200 mg per day divided into 2 doses.

For isolated systolic hypertension:60 mg twice daily.

For preventing migraine headache:100 mg three times daily.

For Parkinsons disease:300 mg, 600 mg, 1200 mg and 2400 mg per day in 3-4 divided doses.

For infertility in men:200-300 mg per day.

For muscular dystrophy:100 mg per day.

Dividing the total daily dose by taking smaller amounts two or three times a day instead of a large amount all at once can help to reduce side effects.

Side Effects

Generally Levocarnitine is well tolerated. However, few side effects including transient nausea and vomiting, abdominal cramps, and diarrhoea may occur

Coenzyme Q10 is well tolerated and having no significant side effects. Mild gastrointestinal symptoms such as nausea, diarrhea and epigastric distress have been reported.

Toxicity

LD₅₀ > 8g/kg (mouse, oral). Adverse effects include hypertension, fever, tachycardia and seizures.

There have not been reports of adverse events of diet supplementation with ubidecarenone. The normal side effects reported in humans are related to the gastrointestinal tract.

Human : TDLo ( Oral) 45mg/kg/7D-C : Normocytic anemia, pulse rate increase without fall inBP Human: TDLo (oral) 106mg/kg : Hypermotylity, diarrhea Mouse ; LD50 Oral : 245mg/kg Mouse : LD50 : subcutaneous : 781mg/kg

Precaution

The safety and efficacy of oral Levocarnitine has not been evaluated in patients with renal insufficiency. 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 (TMA) and trimethylamine-N-oxide (TMAO), since these metabolites are normally excreted in the urine

Supplemental Coenzyme Q10 may improve beta-cell function and glycemic control in type II diabetics. Therefore, those diabetic patients who do use supplemental Coenzyme Q10 should determine by appropriate monitoring if they need to make any adjustments in their diabetic medications.

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.

Warfarin: Supplemental Coenzyme Q10 may decrease the effectiveness of Warfarin.

Statins: The statin drugs are known to decrease Coenzyme Q10 levels in humans.

Doxorubicin: Coenzyme Q10 may increase the cardiotoxicity of doxorubicin.

Antidiabetic medications: Coenzyme Q10 may improve glycemic control in some type II diabetics. If this were to occur, antidiabetic medications might need appropriate adjusting

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.

Ubidecarenone is distributed to the various tissues of the body and it is able to enter the brain. In preclinical studies with intravenous administration of ubidecarenone, it is reported a volume of distribution of 20.4 L/kg which reflects its ability to penetrate extensively into organs and tissues. AS a general rule, tissues with high-energy requirements or metabolic activity tend to presents higher amounts of ubidecarenone, these organs can be heart, kidney, liver and muscle.

After absorption zinc is bound to protein metallothionein in the intestines. Zinc is widely distributed throughout the body. It is primarily stored in RBCs, WBCs, muscles, bones, Skin, Kidneys, Liver, Pancreas, retina, and prostate.

Elimination Route

Absolute bioavailability is 15% (tablets or solution). Time to maximum plasma concentration was found to be 3.3 hours.

Ubidecarenone is absorbed from the small intestine into the lymphatics and then it can enter the blood. The hydrophobicity and large molecular weight limit its absorption making it very poor and variable depending on the food intake and the number of lipids presented in the food. The absorption is lower in the presence of an empty stomach and greater in presence of high lipid food diet. The daily dosage of ubidecarenone presents the reach of maximal serum concentration by reaching a plateau after three weeks. The pharmacokinetic properties may vary between different brands but studies have reported an AUC of 11.51 mcg h/ml and a Cmax of 0.32 mcg/ml at a time of 7.9 h.

Approximately 20 to 30% of dietary zinc is absorbed, primarily from the duodenum and ileum. The amount absorbed is dependent on the bioavailability from food. Zinc is the most bioavailable from red meat and oysters. Phytates may impair absorption by chelation and formation of insoluble complexes at an alkaline pH. After absorption, zinc is bound in the intestine to the protein metallothionein. Endogenous zinc can be reabsorbed in the ileum and colon, creating an enteropancreatic circulation of zinc.

Half Life

17.4 hours (elimination) following a single intravenous dose.

The pharmacokinetic properties may vary between different brands but studies have reported a half-life of ubidecarenone of 21.7 h.

3 hours

Clearance

Total body clearance was found to be a mean of 4L/h.

In preclinical studies with intravenous administration of ubidecarenone, it is reported a total clearance of 1.18 ml h/kg which was indicative of a prolonged elimination.

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.

The main elimination route of ubidecarenone is through the bile. After its oral administration, over 60% of the dose is excreted in the feces in the form of unchanged ubidecarenone and a small fraction of the metabolites. In the urine, ubidecarenone is bound to saposin B protein and represents only 8.3% of the total administered dose.

Primarily fecal (approximately 90%); to a lesser extent in the urine and in perspiration.

Pregnancy & Breastfeeding use

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

Because of lack of information on long-term safety, pregnant women and nursing mothers should avoid Coenzyme Q10.

Contraindication

There is no known disease or syndrome in which Levocarnitine administration is contraindicated. It is contraindicated in patients with hypersensitivity to any of its components.

Patients with a known hypersensitivity to any component of this product

Acute Overdose

There have been no reports of toxicity from levocarnitine overdosage. Levocarnitine 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.

Store in a cool & dry place, protect from light & moisture. Keep out of the reach of children.

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