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Filicine Actions |
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Pharmacology: Filicine or folacin, is a member of the B vitamin group. It is involved in amino acid metabolism. Filicine, in its reduced form, tetrahydrofolate, participates in many reactions involving one-carbon transfers. It is involved in the conversion of homocysteine to methionine and in the conversion of deoxyuridylate to thymidylate, an essential step required in the synthesis of DNA. As Filicine is necessary in the synthesis of DNA, it is essential in the formation of different body cells. Filicine is necessary for the normal production and maturation of red blood cells. Deficiency of Filicine results in megaloblastic anemia.
Filicine deficiency results in impaired processes of DNA synthesis, cellular replication and cell division. Cells with rapid turnover such as the red blood cells and the epithelial cells of the intestine may be readily affected. Deficiency of Filicine has been associated with birth defects (i.e. neural tube defects, congenital heart defects) certain cancers, blood disorders and higher risk of cardiovascular disorders as a result of homocysteinemia. Filicine participates in the conversion of homocysteine into methionine. When Filicine is deficient, homocysteine levels increase, a condition known as homocysteinemia. Filicine supplementation is considered protective against such disorders. Results of clinical studies suggest that high doses of Filicine help reduce risk of birth defects, cardiovascular diseases and cancer.
Filicine deficiency may result from inadequate dietary intake, impaired intestinal absorption secondary to gastrointestinal diseases, alcoholism and intake of drugs that inhibit folate absorption (i.e. anticonvulsants, phenytoin, oral contraceptives and methotrexate). Dietary deficiency is common in the elderly, malnourished and individuals who do not eat vegetables and fruits. Despite adequate dietary intake of Filicine, relative deficiency may been countered in certain conditions where there are increased requirements for active DNA synthesis (such as in pregnancy, and hematologic disorders). In these circumstances, Filicine supplementation becomes important.
The dose of Filicine 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 Filicine. 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 Filicine, 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.
Filicine 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. Filicine 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.
Filicine is absorbed rapidly from the small intestine, primarily from the proximal portion. Naturally occurring conjugated folates are reduced enzymatically to Filicine in the gastrointestinal tract prior to absorption. Filicine 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 Filicine are several times greater than serum levels of the drug. Filicine 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 Filicine 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 Filicine have also been recovered in feces. Filicine is also excreted in the milk of lactating mothers.
Users | % | ||
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Empty stomach | 2 | 40.0% | |
After food | 2 | 40.0% | |
Before food | 1 | 20.0% |
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Information checked by Dr. Sachin Kumar, MD Pharmacology
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