Actions of Folaxin in details
Pharmacology: Folaxin or folacin, is a member of the B vitamin group. It is involved in amino acid metabolism. Folaxin, 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 Folaxin is necessary in the synthesis of DNA, it is essential in the formation of different body cells. Folaxin is necessary for the normal production and maturation of red blood cells. Deficiency of Folaxin results in megaloblastic anemia.
Folaxin 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 Folaxin 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. Folaxin participates in the conversion of homocysteine into methionine. When Folaxin is deficient, homocysteine levels increase, a condition known as homocysteinemia. Folaxin supplementation is considered protective against such disorders. Results of clinical studies suggest that high doses of Folaxin help reduce risk of birth defects, cardiovascular diseases and cancer.
Folaxin 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 Folaxin, 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, Folaxin supplementation becomes important.
How should I take Folaxin?
Dosing
The dose of Folaxin 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 Folaxin. 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.
- For oral dosage form (tablets):
- To prevent deficiency, the amount taken by mouth is based on normal daily recommended intakes:
- For the U.S.
- Adult and teenage males—150 to 400 micrograms (mcg) per day.
- Adult and teenage females—150 to 400 mcg per day.
- Pregnant females—400 to 800 mcg per day.
- Breast-feeding females—260 to 800 mcg per day.
- Children 7 to 10 years of age—100 to 400 mcg per day.
- Children 4 to 6 years of age—75 to 400 mcg per day.
- Children birth to 3 years of age—25 to 100 mcg per day.
- For Canada
- Adult and teenage males—150 to 220 mcg per day.
- Adult and teenage females—145 to 190 mcg per day.
- Pregnant females—445 to 475 mcg per day.
- Breast-feeding females—245 to 275 mcg per day.
- Children 7 to 10 years of age—125 to 180 mcg per day.
- Children 4 to 6 years of age—90 mcg per day.
- Children birth to 3 years of age—50 to 80 mcg per day.
- To treat deficiency:
- Adults, teenagers, and children—Treatment dose is determined by prescriber for each individual based on the severity of deficiency.
- To prevent deficiency, the amount taken by mouth is based on normal daily recommended intakes:
Missed Dose
If you miss a dose of Folaxin, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
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.
Folaxin administration
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.
Folaxin pharmacology
Folaxin 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. Folaxin 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.
Folaxin is absorbed rapidly from the small intestine, primarily from the proximal portion. Naturally occurring conjugated folates are reduced enzymatically to Folaxin in the gastrointestinal tract prior to absorption. Folaxin 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 Folaxin are several times greater than serum levels of the drug. Folaxin 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 Folaxin 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 Folaxin have also been recovered in feces. Folaxin is also excreted in the milk of lactating mothers.
References
- DailyMed. "ASCORBIC ACID; BIOTIN; CYANOCOBALAMIN; DEXPANTHENOL; ERGOCALCIFEROL; FOLIC ACID; NIACINAMIDE; PHYTONADIONE; PYRIDOXINE HYDROCHLORIDE; RIBOFLAVIN 5'-PHOSPHATE SODIUM; THIAMINE HYDROCHLORIDE; VITAMIN A; VITAMIN E: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Folic Acid: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Folic acid: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
