Cyclophosphamide Injection: 200mg/15ml, 500mg/30ml, 1g/50ml
Cyclophosphamide Tablets: 50mg
Cyclophosphamide:9 | 8
Cyclophosphamide is an alkylating agent of a nitrogen mustard type. It has a wide spectrum of antitumor and immunosuppressive activity.

Mechanism of Action:
Cyclophosphamide is inactive in its parent form.
The main effect of cyclophosphamide is caused by its metabolite phosphoramide mustard.
Phosphoramide mustard forms DNA crosslinks between (interstrand crosslinkages) and within (intrastrand crosslinkages) DNA strands at guanine N-7 positions. This leads to cell death.
It is a cell cycle non specific drug.

Adverse effects:
  • Anorexia
  • Vomiting
  • Hair loss
  • Leucopinea
  • Sterility may occur

Drug Interaction:
  • Chloramphenicol retards the metabolism of Cyclophosphamide.
  • Drugs that stimulate the hepatic P450 system such as Phenobarbital and phenytoin, increases the rate of metabolic activation of cyclophosphamide.
  • Cyclophosphamide accelerates the anticoagulant effect of warfarin.
  • The risk of doxorubicin induced cardiotoxicity may be increased when it is given with Cyclophosphamide
Dose:
2-3 mg/kg/day oral
10-15mg/kg i.v.

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Methotrexate Injection: 25mg/ml
Methotrexate Tablets: 2.5mg
Methotrexate:5 | 8 | 4
Methotrexate is the most common antineoplastic agent as it can be used for many malignancies.
Four to six cycles of the treatment over three to six months are commonly given for breast cancer.

Mechanism of Action:
Methotrexate inhibits DNA, RNA and Protein Synthesis.

Adverse effects:
  • It exerts major toxicity on bone marrow-low doses given repeatedly cause megaloblastic anemia.
  • Desquamation and bleeding may occur in GIT
  • It may also cause thrombocytopenia.
  • Some women who receive methotrexate experience mouth sores following the treatment.

Drug Interaction:
  • Methotrexate interacts with alcohol, aspirin containing products and NSAIDS.
Dose:
15-30 mg /day for 5 days orally, or
20-40 mg/m2 body surface area i.m. or i.v. twice weekly.

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Fluorouracil Injection: 50mg/ml
5-Flurouracil:4
5-Fluorouracil is an anticancer drug that is given intravenously. It is pyrimidine analog. It belongs to the class of drug, Antimetabolites.
This drug is most often given with both cyclophosphamide and methotrexate.

Mechanism of Action:
The parent drug is inactive. It is converted in the body to the corresponding nucleotide 5-fluoro-2-deoxyuridine monophosphate, which inhibits thymidilate synthetase and blocks the conversion of dexoyuridilic acid to deoxythymidylic acid.
DNA cannot be synthesized.

Adverse effects:
  • Bone marrow suppression
  • Mucositis
  • Dermatitis
  • Diarrhea
  • Cardiac toxicity
  • Inflammation of the mucous membrane lining the mouth, stomach and intestine

Drug Interaction:
  • 5-fluorouracil interacts with alcohol, warfarin and phenytoin.
Dose:
12mg/kg/day i.v. for 4 days than 6mg/kg i.v. on alternate days

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Vinblastine Sulphate Injection- 1mg/ml
Vincristine Sulphate Injection -1mg/ml
Vinca Alkaloids: 9 | 4 | 7
Vinblastine and Vinblastine are called as vinca alkaloids. Both are antineoplastic with mitotic inhibition property.

Mechanism of Action:
Vinca alkaloids are cell cycle specific and act in the mitotic phase of the cell division. Both binds to the micro tubular protein-tubulin, prevent its polymerization and assembly of microtubules, cause disruption of mitotic spindle. The chromosomes fail to move apart during mitosis which means, metaphase arrest occurs.

Side effects:
  • Headache
  • Anemia
  • Convulsions
  • Hair loss
  • Diarrhea
  • Nerve Damage
  • Damage to veins
  • Photophobia

Drug Interaction:
  • It may cause interaction with antigout medications, live virus vaccines and doxorubicin.
Dose:
Vinblastine--0.1-0.15 mg/kg i.v. weekly * 3 doses.
Vincristine—1.5-2mg/m2 body surface area i.v. weekly.

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Paclitaxel Injection - 3mg/5ml, 100mg/16.7ml and 260mg/43.4ml.
Paclitaxel:4 | 8
Paclitaxel is antineoplastic drug originally obtained from bark of Western yew tree.

Mechanism of Action:
Paclitaxel is called a mitotic inhibitor. Cells grow by a process called mitosis. Paclitaxel attaches to the rapidly growing cancer cells while they are in a division process. Hence the division cannot be completed. The cancer cells cannot divide into new cells and it cannot grow and metastasize.

Adverse effects:
  • Nausea and vomiting
  • Anorexia
  • Elevated liver enzymes
  • Hypotension
  • Edema
  • Bradycardia

Drug Interaction:
  • It increases myelosupression with Cisplatin.
  • Paclitaxel's effects are increased by verapamil, diazepam, vincristine, ketoconazole and quinidine.
Dose:
175mg/m2 by i.v. infusion over 3 hrs, repeated every 3 weeks.

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Docetaxel Injection - 40mg/ml
Docetaxel:4 | 9
Docetaxel belongs to the drug class called taxane. It is a semi synthetic taxane that is derived from the needles of the European yew tree. It is a more potent congener of Paclitaxel.

Mechanism of Action:
Docetaxel is also a mitotic inhibitor. Cells grow by a process called mitosis. Paclitaxel targets rapidly growing cancer cell. It at to attaches them while they are in a division process, and prevents them from completing the division process. Since the cancer cells cannot divide into new cells, it cannot metastasize.
Docetaxel is cell cycle specific, with activity in the M phase.

Adverse effects:
  • Arrhythmias
  • Hypotension
  • Heart failure
  • Myelosuppression is dose limiting with neutropenia

Drug Interaction:
  • Drugs that inhibit or activate cytochrome P450 enzyme system. Such drugs include, Cyclosporine, Ketoconazole, Erythromycin,etc.
Dose:
35-40mg per m2 i.v. weekly for 3-6 weeks followed by 1-2 week rest.

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Lyophilized Doxorubicin Hydrochloride Injection - 10mg/ml and 50mg/25ml.
Doxorubicin:8 | 9 | 6
Doxorubicin is a antitumor antibiotic. It is made from the bacterium Streptomyces.
Doxorubicin can be used to treat early-stage breast cancer, HER2-positive breast cancer, and metastatic breast cancer.
Doxorubicin is sometimes combined with Cyclophosphamide and/or 5-fluorouracil to make a combination of breast-cancer chemotherapy drugs.

Mechanism of Action:
Doxorubicin is a cell cycle non-specific, but is most effective in the S phase. It slows or stops the growth of cancer cells. This drug gets inside the DNA of cancer cells and inhibits protein synthesis thus preventing cell replication process.

Adverse effects:
  • Allergic reaction to Doxorubicin
  • May harm fetus in pregnant women
  • Hand Foot Syndrome
  • Possible future infertility
  • Myelosuppression is dose limiting
  • Cardio toxicity is acute and or chronic.

Drug Interaction:
  • Not Known
Dose:
60-75 mg/m2 BSA slow i.v. injection every 3 weeks.

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Gemcitabine Hydrochloride Injection- 200mg and 1gm
Gemcitabine:3
Gemcitabine is a member of a general group of chemotherapy drugs known as antimetabolites. It is used in breast cancer.

Mechanism of Action:
It prevents cells from making DNA and RNA by interfering with the making of nucleic acids, which stops cell replication, leading to cell death.

Side effects:
  • Decreased white blood cell count with increased risk of infection
  • Decreased platelet count with increased risk of bleeding
  • Nausea
  • Vomiting
  • Loss of appetite
  • Cardio toxicity is acute and or chronic.
  • Abnormal blood tests which suggest that the drug is affecting the liver

Drug Interaction:
  • Bleomycin: Gemcitabine may enhance the toxic effects of Bleomycin. The risk of pulmonary toxicity may be increased.
  • Fluorouracil: Gemcitabine may increase the serum concentration of Fluorouracil.
Dose:
Gemcitabine is administered by the IV route, since it is extensively metabolized by the gastrointestinal tract.
Dose ranges from 1-1.2 g/m2 according to type of cancer treated.

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Epirubicin Hydrochloride Injection- 10mg and 50mg
Epirubicin:5 | 9
Epirubicin is a antineoplastic drug that is used to treat breast cancer that has spread to the lymph nodes.

Side effects:
  • Reddish urine (few days)
  • Nausea and vomiting
  • Mouth sores
  • Dehydration
  • Diarrhea
  • Signs of congestive heart failure
  • Damage to the skin if drug gets out of the vein
  • Harms the fetus if taken during pregnancy
  • Pain, burning or stinging at the injection site
  • Alopecia
  • Low blood cell counts (anemia, leucopenia, neutropenia, and thrombocytopenia)
  • Fatigue
  • Temporary or permanent loss of menstrual cycle in women
  • Hot flashes
  • Rash

Drug Interaction:
  • Cimetidine: It increases the drug AUC by 50% and should not be used with Epirubicin.
  • Cardio toxic Drugs: Cardiac toxicity is increased when the Epirubicin is used with other Cardio toxic drugs
  • Cytotoxic Drugs: Additional toxicities occur when Epirubicin is used with the cytotoxic drugs.
  • Heparin: Epirubicin is incompatible with Heparin. When used together, a precipitate is formed.
Dose:
The Standard dose is 100mg to 120mg per m 2 i.v. every three weeks, usually combined with Cyclophosphamide and 5-fluorouracil.

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Tamoxifen Tablets - 10mg and 20 mg
Tamoxifen:1 | 2
Tamoxifen is widely used to treat patients with breast cancer.
As an adjuvant therapy,it helps to prevent the relapse of breast cancer and helps to prevent the development of new cancers in the other breast. It is also used for the treatment of metastatic breast cancer. The drug slows or stops the growth of cancer cells that are present in the body.
Estrogen can promote the growth of breast cancer cells. Some breast cancers are classified as estrogen receptor-positive, which means that they have a protein to which estrogen will bind. As the estrogen grows, the cancer cells proliferate. Tamoxifen acts against the effects of estrogen on these cells.

Mechanism of Action:
Tamoxifen binds to estrogen receptors on tumors and other tissue targets to produces a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. Tamoxifen is a nonsteroidal agent with potent Antiestrogenic properties which compete with estrogen for binding sites in breast and other tissues. Tamoxifen causes cells to remain in the G0 and G1 phases of the cell cycle. Tamoxifen is Cytostatic as it stops the growth of the cancer cells but does not kill them.

Side effects:
  • Some serious side effects of Tamoxifen are blood clots, strokes , endometrial cancer and cataracts.
  • Other side effects of Tamoxifen are menopausal symptoms. The most common side effects include hot flashes and vaginal dryness, mood swings and low libido.
  • Some women experience irregular menstrual periods, headaches, fatigue, nausea and vomiting, irritation of the vagina and skin rash.
  • Men who take Tamoxifen may experience headaches, nausea and vomiting, skin rash and decreased sexual interest.

Drug Interaction:
  • Aminoglutethimide
  • Bromocriptine
  • Carbamazepine
  • Phenytoin
  • Primidone
  • Warfarin
  • Anastrazole
Dose:
Oral Dose of 10-20 mg twice daily.

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