Fludarabinefosfaat - PCH
Fludarabinefosfaat - PCH Uses, Dosage, Side Effects, Food Interaction and all others data.
Fludarabinefosfaat - PCH phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis leading to cell death. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.
Fludarabinefosfaat - PCH is a chemotherapy drug used in the treatment of chronic lymphocytic leukemia. It acts at DNA polymerase alpha, ribonucleotide reductase and DNA primase, results in the inhibition of DNA synthesis, and destroys the cancer cells.
Trade Name | Fludarabinefosfaat - PCH |
Availability | Prescription only |
Generic | Fludarabine |
Fludarabine Other Names | Fludarabina, Fludarabine, Fludarabinum |
Related Drugs | Venclexta, prednisone, methotrexate, dexamethasone, triamcinolone, Decadron, rituximab, carboplatin, fluorouracil, Rituxan |
Type | |
Formula | C10H12FN5O4 |
Weight | Average: 285.235 Monoisotopic: 285.087332049 |
Protein binding | 19-29% |
Groups | Approved |
Therapeutic Class | Cytotoxic Chemotherapy |
Manufacturer | |
Available Country | Netherlands |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fludarabinefosfaat - PCH Phosphate is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to or whose disease has progressed during treatment with at least one standard alkylating-agent containing regimen. The safety and effectiveness of Fludarabinefosfaat - PCH Phosphate in previously untreated or non-refractory patients with CLL have not been established.
Fludarabinefosfaat - PCH is also used to associated treatment for these conditions: B-cell chronic lymphocytic leukemia/prolymphocytic leukemia/small lymphocytic lymphoma refractory, Refractory Non-Hodgkin's lymphoma
How Fludarabinefosfaat - PCH works
Fludarabinefosfaat - PCH phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase and DNA primase, thus inhibiting DNA synthesis. The mechanism of action of this antimetabolite is not completely characterized and may be multi-faceted.
Dosage
Fludarabinefosfaat - PCH dosage
Intravenous (Adult):
Chronic lymphocytic leukaemia:25 mg/m2BSA daily given by bolus inj or by IV infusion over 30 minutes for 5 consecutive days. Courses may be repeated every 28 days, usually for up to 6 cycles.Oral (Adult):
Chronic lymphocytic leukaemia:40 mg/m2BSA daily for 5 consecutive days. Courses may be repeated every 28 days, usually for up to 6 cycles.
Side Effects
Fever, chills, cough, dyspnoea, pneumonia; GI disturbances, stomatitis; oedema; tumour lysis syndrome; skin rashes; haemolytic anaemia, haemorrhagic cystitis; neurological disturbances including peripheral neuropathy, agitation, confusion, visual disturbances and coma. Progressive encephalopathy and blindness (high doses).
Precaution
Routine monitoring of blood counts and Hb conc. Monitor for signs of autoimmune haemolytic anaemia; elderly. Avoid contact with skin and eyes; avoid inhalation. Myelosuppression may be cumulative and severe increasing risk of opportunistic infections. Increased risk of tumour lysis syndrome in patients with high tumour burden.
Interaction
Co-administration with pentostatin may lead to pulmonary toxicity. Reduced metabolic activation of fludarabine with cytarabine. Reduced therapeutic efficacy with dipyridamole and other adenosine uptake inhibitors.
Food Interaction
- Take with or without food. Administration with food delays absorption, but not to a clinically significant extent.
Fludarabinefosfaat - PCH Drug Interaction
Minor: levofloxacin, levofloxacinUnknown: lorazepam, lorazepam, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, meperidine, meperidine, heparin, heparin, furosemide, furosemide, vitamin a topical, vitamin a topical, bioflavonoids, bioflavonoids, sotalol, sotalol
Fludarabinefosfaat - PCH Disease Interaction
Major: infections, hemolytic anemia, myelosuppressionModerate: peripheral neuropathy, renal dysfunction, transfusion/graft-vs-host disease
Elimination Route
Bioavailability is 55% following oral administration.
Half Life
20 hours
Clearance
- 117-145 mL/min [patients with B-cell CLL receiving IV administration of a single dose of 40 mg/m^2.
Pregnancy & Breastfeeding use
Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
Renal impairment (CrCl <30 mL/min); decompensated haemolytic anaemia. Pregnancy and lactation. Concomitant use of live vaccines.
Special Warning
Renal Impairment:
- CrCl 30-70: May reduce the doses by up to 50%
- Severe impairment: Avoid
Storage Condition
Refrigerate at 2-8° C
Innovators Monograph
You find simplified version here Fludarabinefosfaat - PCH
Fludarabinefosfaat - PCH contains Fludarabine see full prescribing information from innovator Fludarabinefosfaat - PCH Monograph, Fludarabinefosfaat - PCH MSDS, Fludarabinefosfaat - PCH FDA label