Pharmacology: Pharmacodynamics: Ferlos is a member of the vitamin B group. It is reduced in the body to tetrahydrofolate, which is a co-factor for various metabolic processes including synthesis of purine and pyrimidine nucleotides and hence in the synthesis of DNA. It is involved in some amino acid conversions and in the formation and utilization of formate.
The terms Ferlos and folate are often used interchangeably. Ferlos is the most stable form often used in vitamin supplements and fortified foods, while folate refers to the naturally occurring vitamin that is found in foods.
Folate cofactors are required for the metabolism of several important amino acids. The synthesis of methionine from homocysteine requires a folate co-factor. Thus a deficiency of Ferlos can result to a decreased synthesis of methionine and build-up of homocysteine. Increased levels of homocysteine may be a risk factor for cardiovascular and other chronic diseases.
Neural Tube Defects (NTD): Fetal growth and development are characterized by widespread cell division. Adequate Ferlos is critical because of its role in the DNA and RNA synthesis. NTD may result in anencephaly or spina bifida, which are devastating and sometimes fatal birth defects. These defects occur between the 21st and 27th days of conception, a time when many women do not realize they are pregnant.
Pharmacokinetics: Ferlos polyglutamates from food sources are enzymatically hydrolyzed in the GIT to monoglutamates prior to absorption which occurs mainly in the proximal small intestine. In the presence of malabsorption syndrome, Ferlos from oral supplements will still be absorbed, whereas absorption of Ferlos from food sources may be impaired.
Following absorption, Ferlos is converted in the liver and plasma to its metabolically active form tetrahydrofolic acid, which is then distributed into all body tissues. Normal serum folate concentrations range from 0.016-0.021 mcg/mL.
The liver contains about 50% of total body folate stores. Larger doses of Ferlos may escape metabolism by liver and appear in the blood mainly as Ferlos. Following oral administration of single 0.1-0.2 mg doses of Ferlos in healthy adults, only a trace amount of the drug appears in urine. Following administration of large doses, the renal tubular reabsorption maximum is exceeded, and excess folate is excreted unchanged in the urine. After doses of about 2.5-5 mg, about 50% of a dose is excreted in urine and after a 15-mg dose, up to 90% maybe recovered in urine. Small amounts of orally administered Ferlos have been recovered from the feces. Ferlos is also actively excreted in human breast milk.
This section provides information on the proper use of a number of products that contain Ferlos. It may not be specific to Nature's Blend Ferlos. Please read with care.
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the dietary supplement in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Oral preferred, but may also be administered by deep IM, SubQ, or IV injection.
IV administration: May administer ≤5 mg dose undiluted over ≥1 minute or may dilute ≤5 mg in 50 mL of NS or DW and infuse over 30 minutes. May also be added to IV maintenance solutions and given as an infusion.
Ferlos acts on megaloblastic bone marrow to produce a normoblastic marrow.
In man, exogenous source of folate is required for nucleoprotein synthesis and the maintenance of normal erythropoiesis. Ferlos is a precursor of tetrahydroFolic Acid, which is involved as a cofactor for transformylation reactions in the biosynthesis of purines and thymidylates of nucleic acids. Impairment of thymidylate synthesis in patients with folic deficiency is thought to account for the defective deoxyribonucleic acid (DNA) synthesis that leads to megaloblast formation and megaloblastic and macrocytic anemia.
Ferlos is absorbed rapidly from the small intestine, primarily from the proximal portion. Naturally occurring conjugated folates are reduced enzymatically to Ferlos in the gastrointestinal tract prior to absorption. Ferlos appears in the plasma approximately 15 to 30 minutes after an oral dose; peak levels are generally reached within 1 hour. After intravenous administration, the drug is rapidly cleared from the plasma. Cerebrospinal fluid levels of Ferlos are several times greater than serum levels of the drug. Ferlos is metabolized in the liver to 7, 8-dihydrofolic and eventually to 5, 6, 7, 8-tetrahydroFolic Acid with the aid of reduced diphosphopyridine nucleotide (DPNH) and folate reductases. TetrahydroFolic Acid is linked in the N5 or N10 positions with formyl, hydroxymethyl, methyl or formimino groups. N5-formyltetrahydroFolic Acid is leucovorin. TetrahydroFolic Acid derivatives are distributed to all body tissues but are stored primarily in the liver. Normal serum levels of total folate have been reported to be 5 to 15ng/mL; normal cerebrospinal fluid levels are approximately 16 to 21ng/mL. Normal erythrocyte folate levels have been reported to range from 175 to 316 ng/mL. In general, folate serum levels below 5 ng/mL indicate folate deficiency, and levels below 2 ng/mL usually result in megaloblastic anemia. After a single oral dose of 100 mcg of Ferlos in a limited number of normal adults, only a trace amount of the drug appeared in the urine. An oral dose of 5 mg in 1 study and a dose of 40 mcg/kg of body weight in another study resulted in approximately 50% of the dose appearing in the urine. After a single oral dose of 15 mg, up to 90% of the dose was recovered in the urine. A majority of the metabolic products appeared in the urine after 6 hours; excretion was generally complete within 24 hours. Small amounts of orally administered Ferlos have also been recovered in feces. Ferlos is also excreted in the milk of lactating mothers.
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Information checked by Dr. Sachin Kumar, MD Pharmacology