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Folinic acid
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| Systematic (IUPAC) name | |
| 2-[4-[(2-amino-5-formyl-4-oxo-5,6,7,8- tetrahydro-1H-pteridin-6-yl)methylamino] benzoyl]aminopentanedioic acid |
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| Identifiers | |
| CAS number | |
| ATC code | V03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C20H23N7O7 |
| Mol. mass | 473. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 44 g/mol |
| Pharmacokinetic data | |
| Bioavailability | Dose dependent:
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| Protein binding | ~15% |
| Metabolism | ? |
| Half life | 6. For other uses of the words gram or gramme see Gram (disambiguation. The mole (symbol mol) is a unit of Amount of substance: it is an SI base unit, and almost the only unit to be used to measure this In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity 2 hours |
| Excretion | Urinary |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Intravenous, oral |
Folinic acid (INN) or leucovorin (USAN), generally administered as calcium folinate (or leucovorin calcium), is an adjuvant used in cancer chemotherapy involving the drug methotrexate. Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during For a topic outline on this subject see List of basic Australia topics. The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. An International Nonproprietary Name ( INN; also known as rINN, for recommended International Nonproprietary Name or pINN for proposed __FORCETOC__The Union of South American Nations (Unión de Naciones Suramericanas - UNASUR, União de Nações Sul-Americanas - UNASUL, Unie van Zuid-Amerikaanse Naties Cancer (medical term Malignant Neoplasm) is a class of Diseases in which a group of cells display uncontrolled Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. It is also used in synergistic combination with the chemotherapy agent 5-fluorouracil. Synergy (from the Greek el-Latn syn-ergo, el συνεργός meaning working together is the term used to describe a situation where the final outcome Fluorouracil (5-FU or f5U is a Pyrimidine analog, which is used as a drug in the treatment of Cancer.
Folinic acid is not folic acid. Folic acid (also known as Vitamin M and Folacin) and Folate (the Anionic form are forms of the water-soluble Vitamin B9
Contents |
Mechanism of action
Folinic acid is a 5-formyl derivative of tetrahydrofolic acid. Folic acid (also known as Vitamin M and Folacin) and Folate (the Anionic form are forms of the water-soluble Vitamin B9 It is readily converted to other reduced folic acid derivatives (e. g. tetrahydrofolate), and thus has vitamin activity which is equivalent to folic acid. However, since it does not require the action of dihydrofolate reductase for its conversion, its function as a vitamin is unaffected by inhibition of this enzyme by drugs such as methotrexate. Dihydrofolate reductase, or DHFR, reduces Dihydrofolic acid to Tetrahydrofolic acid, using NADPH as Electron donor, which can be converted Enzyme inhibitors are Molecules that bind to Enzymes and decrease their activity.
Folinic acid, therefore, allows for some purine/pyrimidine synthesis to occur in the presence of dihydrofolate reductase inhibition, so that some normal DNA replication and RNA transcription processes can proceed. Purine ( 1) is a heterocyclic Aromatic Organic compound, consisting of a Pyrimidine ring fused to an Imidazole ring Pyrimidine is a Heterocyclic Aromatic Organic compound similar to Benzene and Pyridine, containing two Nitrogen Atoms Deoxyribonucleic acid ( DNA) is a Nucleic acid that contains the genetic instructions used in the development and functioning of all known Ribonucleic acid ( RNA) is a Nucleic acid that consists of a long chain of Nucleotide units
Therapeutic use
Folinic acid is administered at the appropriate time following methotrexate as part of a total chemotherapeutic plan, where it may "rescue" bone marrow and gastrointestinal mucosa cells from methotrexate. Bone marrow is the flexible tissue found in the hollow interior of Bones In adults marrow in large bones produces new Blood cells It constitutes 4% of There is no apparent effect on preexisting methotrexate-induced nephrotoxicity. Nephrotoxicity (from Greek nephros "kidney" is a Poisonous effect of some substances both Toxic chemicals and Medication, on the Kidney [1]
While not specifically an antidote for methotrexate, folinic acid may also be useful in the treatment of acute methotrexate overdose. Different dosing protocols are used, but folinic acid should be re-dosed until the methotrexate level is less than 5 x 10-8 M [2]
Folinic acid is also used in combination with the chemotherapy agent 5-fluorouracil in treating colon cancer. Fluorouracil (5-FU or f5U is a Pyrimidine analog, which is used as a drug in the treatment of Cancer. Colorectal cancer, also called colon cancer or large bowel cancer, includes Cancerous growths in the colon, Rectum and In this case, folinic acid is not used for "rescue" purposes; rather, it enhances the effect of 5-fluorouracil on inhibiting thymidylate synthase. Fluorouracil (5-FU or f5U is a Pyrimidine analog, which is used as a drug in the treatment of Cancer. Thymidylate synthetase ( is the enzyme used to generate
Folinic acid is also sometimes used to prevent toxic effects of high doses of antimicrobial dihydrofolate reductase inhibitors such as trimethoprim and pyrimethamine. An antimicrobial is a substance that kills or inhibits the growth of Microbes such as Bacteria, Fungi, or Viruses. Trimethoprim ( INN) (traɪˈmɛθəprɪm is a bacteriostatic Antibiotic mainly used in the Prophylaxis and treatment of Urinary tract infections Pyrimethamine ( Daraprim) is a Medication used for Protozoal infections
Note on administration
Folinic acid should not be administered intrathecally. Intrathecal is an adjetive that refers to something that happens inside of the spinal canal This may produce severe adverse effects or even death. [3]
References
- ^ Therapeutic Information Resources Australia (2004). Calcium Folinate (Systemic) in AUSDI: Australian Drug Information for the Health Care Professional. Castle Hill: Therapeutic Information Resources Australia.
- ^ www. cancercare. on. ca/pdfdrugs/leucovo. pdf
- ^ Jardine, LF et al (1996). "Intrathecal Leucovorin After Intrathecal Methotrexate Overdose". J Pediatr Hematol Oncol 18 (3): 302–304. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 8689347.
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