What is cyclophosphamide?
Cyclophosphamide is a cancer drug that interferes with the growth and spread of cancer cells in the body. Cyclophosphamide is used to treat several types of cancer. Cyclophosphamide is also used to treat nephrotic syndrome (kidney disease) in children
Mechanism of action
Cyclophosphamide drug is converted into active alkylating metabolites mainly in the liver by the multifunctional microsomal oxidase system. These metabolites interfere with the growth of rapidly proliferating malignant cells.
It is thought that the mechanism of action includes creating a connection between the two molecular strands of DNA and RNA and inhibiting the protein production of the tumor cell.
Pharmacodynamics
Cyclophosphamide is an anticancer agent in the class of alkylating agents and is used to treat various cancers. Alkylating agents are known for their ability to add alkyl groups to many electron-negative groups under the conditions present in the cell.
They stop tumor growth by attaching guanine bases to the strands of the DNA helix—attacking the DNA directly. This action makes the branches unable to open and separate. Since this is necessary for DNA replication, cells can no longer divide.
In addition, these drugs add methyl or other alkyl groups to molecules where they do not belong, in turn inhibiting their proper use by base-pairing and causing DNA miscoding. Alkylating agents are nonspecific cell cycle.
Alkylating agents work by three different mechanisms, all of which cause the same end result, which is DNA dysfunction and ultimately cell death.
Pharmacokinetics
– Cyclophosphamide is well absorbed through the digestive tract. After oral consumption, the maximum blood concentration is reached within one hour. It passes through the blood-brain barrier in a limited amount.
– The distribution volume of cyclophosphamide is 30-50 liters. 20% of cyclophosphamide is protein bound without dose-dependent changes.
– Metabolism of cyclophosphamide is hepatic. 75% of cyclophosphamide is activated by cytochrome P450 isoforms.
Cyclophosphamide is mainly excreted as metabolites. 10-20% is excreted unchanged in urine and 4% is excreted in bile following IV administration.
– The half-life of cyclophosphamide is 3-12 hours. Total body clearance 7.6 ± 63 L/kg. is.
Uses of cyclophosphamide
Ovarian cancer, malignant diseases, children’s nephrotic syndrome
Usual adult dose for malignant diseases
Intravenous:
When used alone, the initial dose for patients without blood defects is 40 to 50 mg/kg, usually in divided doses over 2 to 5 days.
A maintenance dose of 10 to 15 mg/kg may be administered every 7 to 10 days or 3 to 5 mg/kg twice weekly.
Edible:
Usual dose: initial and maintenance dose 1 to 8 mg/kg/day.
* The usual adult dose for ovarian cancer for use in the treatment of epithelial ovarian cancer is 600 mg/m2 intravenously on the first day of treatment in combination with carboplatin or cisplatin. Repeat the course every 28 days.
Children’s usual dose for malignant diseases
Intravenous:
When used alone, the initial dose for patients without blood defects is 40 to 50 mg/kg, usually in divided doses over 2 to 5 days.
A maintenance dose of 10 to 15 mg/kg may be administered every 7 to 10 days or 3 to 5 mg/kg twice weekly.
Edible:
Usual dose: initial and maintenance dose 1 to 8 mg/kg/day.
Usual dose for children for nephrotic syndrome, recommended dose:
5.2 to 3 mg/kg/day orally for 60 to 90 days.
prohibited usage
Hypersensitivity to this drug and its compounds, severe decrease in bone marrow activity
Side effects of cyclophosphamide
Nausea, vomiting, diarrhea, weakness, decrease in blood platelets, decrease in blood neutrophils, decrease in blood leukocytes, anemia, Steven Johnson syndrome, baldness, anorexia, malaise, pain, renal tubular necrosis, inflammation of the bleeding ureters, inflammation of the hemorrhagic colon.
Warnings
1- Carcinogenicity, mutagenicity and impaired fertility may occur in patients treated with cyclophosphamide.
2- Hemorrhagic cystitis may occur in patients treated with cyclophosphamide.
3- Although following the recommended dose of cyclophosphamide, some examples of cardiac dysfunction have been reported. Cyclophosphamide has been reported to potentiate doxorubicin-induced cardiotoxicity.
4- Treatment with cyclophosphamide may cause significant suppression of immune responses. Serious infections, sometimes fatal, may occur in immunosuppressed patients. In patients with viral infections, bacterial, fungal, protozoal, or helminthic infections, treatment with cyclophosphamide should not be performed, or should be discontinued, or the dosage should be reduced.
5- Anaphylactic reactions have been reported with the use of cyclophosphamide; Death has also been reported in relation to this event. The possibility of cross-sensitivity with other alkylating agents has been reported.
Recommended tips
A- In patients treated with cyclophosphamide, if any of the following conditions are met, care
Especially in relation to the possibility of toxicity, the following should be done:
1- Leukopenia (reduction of leukocytes)
2- Thrombocytopenia (decrease in platelets)
3- Tumor cell leakage from the bone marrow
4- History of X-ray treatment
5- History of treatment with other cytotoxic agents
6- Liver dysfunction
7- Renal dysfunction
B- During the treatment, the patient’s hematological record (especially neutrophils and platelets) should be monitored regularly to detect the degree of hematopoietic suppression. Urine should also be tested regularly for the presence of red blood cells, which may indicate hemorrhagic cystitis.
Use in pregnancy
D (In this group of drugs, the studies and the results show the existence of risk for the human fetus. When the use of the drug is unavoidable for pregnant women and the possible risks are accepted, the doctor prescribes the drug.)
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