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CANCER ............................................................................................................................................... 6 DEFINITION .......................................................................................................................................... 6 ANTI CANCER DRUGS ........................................................................................................................... 6 DOXORUBUCINE: ................................................................................................................................. 7 MECHANISM OF ACTION:..................................................................................................................... 7 INDICATIONS: ...................................................................................................................................... 7 HOW IT IS GIVEN:................................................................................................................................. 7 DOSAGE: .............................................................................................................................................. 8 Usual Adult Dose for Breast Cancer: ..................................................................................................... 8 Usual Adult Dose for Hodgkin's disease:............................................................................................... 8 SIDE EFFECTS: ...................................................................................................................................... 8 FLUOROURACIL: .................................................................................................................................. 9 MECHANISM OF ACTION:..................................................................................................................... 9 DOSING: .............................................................................................................................................. 9 DRUG INTERACTIONS: .......................................................................................................................... 9 SIDE EFFECTS: ...................................................................................................................................... 9 USES: ................................................................................................................................................. 10 CYTARABINE: ..................................................................................................................................... 11 MECHANISM OF ACTION:................................................................................................................... 11 CLINICAL USE OR INDICATION: ........................................................................................................... 11 HOW THIS DRUG IS GIVEN: ................................................................................................................ 11 DOSAGE: ............................................................................................................................................ 12 SIDE EFFECTS: .................................................................................................................................... 12 GEFTINIBE: ........................................................................................................................................ 13 DRUG TYPE: ....................................................................................................................................... 13 MECHANISM OF ACTION:................................................................................................................... 13 INDICATIONS: .................................................................................................................................... 13 DOSING: ............................................................................................................................................ 13 ADVERSE EFFECTS: ............................................................................................................................. 13
LEUPROLIDE ...................................................................................................................................... 14 MECHANISM OF ACTION:................................................................................................................... 14 INDICATION: ...................................................................................................................................... 14 PREPARATIONS: ................................................................................................................................. 14 DOSING: ............................................................................................................................................ 14 SIDE EFFECTS: .................................................................................................................................... 14 CAPECITABINE: .................................................................................................................................. 15 USES: ................................................................................................................................................. 15 STRENGTH: ........................................................................................................................................ 15 DOSE: ................................................................................................................................................ 15 IN BREAST CANCER: ........................................................................................................................... 15 IN COLORECTAL CANCER .................................................................................................................... 15 HEXAMETHYLAMINE: ........................................................................................................................ 16 INDICATIONS: .................................................................................................................................... 16 STRENGTH: ........................................................................................................................................ 16 DOSAGE: ............................................................................................................................................ 16 ADMINISTRATION: ............................................................................................................................. 16 ADVERSE REACTIONS: ........................................................................................................................ 16 IFOSFOMIDE: ..................................................................................................................................... 17 INDICATIONS: .................................................................................................................................... 17 ADMINISTRATION: ............................................................................................................................. 17 TOXICITY: ........................................................................................................................................... 17 DOSE: ................................................................................................................................................ 18 Usual Adult dose ................................................................................................................................ 18 Usual Pediatric Dose .......................................................................................................................... 18 PRECAUTIONS: ................................................................................................................................... 18 MECHANISM OF ACTION:................................................................................................................... 18 MITOMYCIN: ..................................................................................................................................... 19 INDICATIONS: .................................................................................................................................... 19 ADMINISTRATION: ............................................................................................................................. 19 DOSE: ................................................................................................................................................ 19 SIDE-EFFECTS AND SPECIAL PRECAUTIONS: ........................................................................................ 19
Hepatic: ............................................................................................................................................. 19 MECHANISM OF ACTION:................................................................................................................... 20 VINCRISTINE .......................................................................................................................................... 21 Oncovin, Vincasar PFS .......................................................................................................................... 21 DOSING FORMS & STRENGTHS: ......................................................................................................... 21 Injectable solution: ............................................................................................................................ 21 Acute Leukemia: ................................................................................................................................ 21 Combination Therapy: ....................................................................................................................... 21 Cancers: ............................................................................................................................................. 21 Other Indications & Uses: .................................................................................................................. 21 ADVERSE EFFECTS: ............................................................................................................................. 21 CONTRAINDICATIONS: ....................................................................................................................... 22 CAUTIONS:......................................................................................................................................... 22 PACLITAXEL: ...................................................................................................................................... 23 SIDE EFFECTS: .................................................................................................................................... 23 DRUG INTERACTIONS: ........................................................................................................................ 23 DOSAGE AND INDICATIONS:............................................................................................................... 23 INDICATION AND DOSAGE: ................................................................................................................ 24 CONTRAINDICATIONS: ....................................................................................................................... 24 SPECIAL PRECAUTIONS: ..................................................................................................................... 24 ADVERSE DRUG REACTIONS: .............................................................................................................. 24 FOLINIC ACID: .................................................................................................................................... 25 MECHANISM OF ACTION:................................................................................................................... 25 INDICATIONS: .................................................................................................................................... 25 SIDE EFFECTS: .................................................................................................................................... 25 DOSE AND DOSAGE FORM: ................................................................................................................ 25 ETOPOSIDE: ....................................................................................................................................... 26 MECHANISM OF ACTION:................................................................................................................... 26 INDICATIONS: .................................................................................................................................... 26 SIDE EFFECTS: .................................................................................................................................... 26 DOSE AND DOSAGE FORM: ................................................................................................................ 26 Usual Adult Dose for Sickle Cell Anemia ........................................................................................ 26
Usual Adult Dose for Chronic Myelogenous Leukemia .................................................................. 26 HYROXYUREA: ................................................................................................................................... 27 INDICATIONS: .................................................................................................................................... 27 CONTRAINDICATIONS: ....................................................................................................................... 27 DOSE: ................................................................................................................................................ 27 COUNCELLING POINTS OR PRECAUTIONS:.......................................................................................... 27 DEXTRAZOXONE: ............................................................................................................................... 28 BRAND NAMES: ................................................................................................................................. 28 INDICATIONS: .................................................................................................................................... 28 CONTRAINDICATIONS: ....................................................................................................................... 28 DOSE: ................................................................................................................................................ 28 COUNCELLING POINTS / PRECAUTIONS:............................................................................................. 28 ADMINISTRATION: ............................................................................................................................. 29 INDICATION: ...................................................................................................................................... 29 CONTRAINDICATIONS: ....................................................................................................................... 29 DOSAGE AND ADMINISTRATION: ....................................................................................................... 29 DRUG INTERACTIONS: ........................................................................................................................ 29 ADVERSE EFFECTS: ............................................................................................................................. 30 OVERDOSE SYMPTOMS: ..................................................................................................................... 30 TAMOXYIN: ....................................................................................................................................... 30 MECHANISM OF ACTION:................................................................................................................... 31 INDICATIONS: .................................................................................................................................... 31 CONTRAINDICATIONS: ....................................................................................................................... 31 DOSAGE AND ADMINISTRATION: Adults ............................................................................................ 31 DRUG INTERACTIONS: ........................................................................................................................ 31 ADVERSE EFFETCS: ............................................................................................................................. 31 CISPLATIN: ......................................................................................................................................... 32 PHARMACOLOGICAL CLASS:............................................................................................................... 32 MECHANISM OF ACTION:................................................................................................................... 32 INDICATIONS: .................................................................................................................................... 32 ADVERSE REACTIONS: ........................................................................................................................ 32 Pulmonary: ........................................................................................................................................ 32
IDIOSYNCRATIC REACTIONS: .............................................................................................................. 33 Integument and Mucous Membranes: ............................................................................................... 33 ASPARAGINASE ................................................................................................................................. 33 CONTRAINDICATION: ......................................................................................................................... 33 DRUG INTERACTIONS: ........................................................................................................................ 33 DOSAGE FORM: ................................................................................................................................. 33 USUAL ADULT DOSE: .......................................................................................................................... 33 BLEOMYCINE BRAND NAME CONTRAINDICATIONS CYCLOPHOSPHAMIDE 29 29 ..29 ..30
Benzene and other chemicals Drinking excess alcohol Environmental toxins, such as certain poisonous mushrooms and a type of poison that can grow on peanut plants (aflatoxins) Excessive sunlight exposure Genetic problems Obesity Radiation Viruses
is that cancerous cells which are initially suppressed by a specific drug may develop a resistance to that drug. For this reason cancer chemotherapy may consist of using several drugs in combination for varying lengths of time.
DOXORUBICIN
TRADE NAME:
Adriamycin, Rubex
MECHANISM OF ACTION:
Doxorubicin interacts with DNA by intercalation and inhibition of macromolecular biosynthesis.This inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. Doxorubicin stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication. The planar aromatic chromophore portion of the molecule intercalates between two base pairs of the DNA, while the six-membered daunosamine sugar sits in the minor groove and interacts with flanking base pairs immediately adjacent to the intercalation site, as evidenced by several crystal structures
INDICATIONS:
Doxorubicin is commonly used to treat some leukemias and Hodgkin's lymphoma, as well as cancers of the bladder, breast, stomach, lung, ovaries, thyroid, soft tissue sarcoma, multiple myeloma, and others
HOW IT IS GIVEN:
Doxorubicin is given by injection or drip (infusion) in one of the following ways:
y y y
through a fine tube inserted into the vein, usually in the back of your hand (cannula) through a fine, plastic tube inserted under the skin and into a vein near your collarbone (central line) Into a fine tube inserted into a vein in the crook of your arm (PICC line).
Chemotherapy is usually given as a course of several sessions (or cycles) of treatment over a few months. The length of your treatment and the number of cycles you have will depend on the type of cancer you're being treated for. Your nurse or doctor will discuss your treatment plan with you.
Before you begin your treatment your doctor will arrange for you to have blood tests. You'll usually be given anti-sickness drugs before and/or during your treatment.
SIDE EFFECTS:
y y y y y y y y y Hair lost Feeling sick (nausea) or being sick (vomiting) Risk of infection Bruising or bleeding Anemia Sore mouth Taste changes Discolored urine Tiredness (fatigue)
FLUOROURACIL
TRADE NAMES:
Carac, Efudex, Fluoroplex
MECHANISM OF ACTION:
Topical fluorouracil is a drug that is used to treat conditions of the skin in which there is rapid multiplication (division) of cells, for example, skin cancer. In order to multiply or divide, cells must produce DNA for each new cell. The DNA is critical since it is the genetic material that directs the activity of all cells Production of DNA depends on the production of RNA which serves as a messenger during the production of DNA. Fluorouracil prevents the formation of RNA which, in turn, prevents the formation of DNA. As a result, cells cannot multiply. With continued treatment, the remaining cells also die
DOSING:
The cream or solution is applied once or twice daily after washing the area that is to be treated with plain water. The course of treatment continues for up to four weeks. A tiny amount of the cream should be gently rubbed into all of the treated areas with a fingertip. It is important to apply it to all of the skin and not just visible lesions
DRUG INTERACTIONS:
There are no known drug interactions with topical fluorouracil.
SIDE EFFECTS:
With application of fluorouracil, initially there usually is a mild to severe stinging or burning sensation or irritation. It also sensitizes the skin to sun and promotes sunburn. After five to ten days of treatment, the sun-damaged parts of treated skin can become red and irritated. If exposure to sun is unavoidable, sunscreen with SPF of 15 or greater should be used, especially during summer months and mid-day. Fluorouracil also may cause prolonged hypo-pigmentation (lightening of the skin), which is more noticeable in dark-skinned persons. Such individuals may wish to first test fluorouracil in cosmetically unimportant areas
Certain areas are more sensitive to severe irritation, including skin folds, the lips, and the eyelids. Make-up may increase the irritation. Occasionally, one or more of the following complications may arise: excessive inflammation resulting in ulcer formation, persistent white marks or scarring, and secondary bacterial infections.
USES:
The chemotherapy agent 5-FU, which has been used against cancer for about 40 years, acts in several ways, but principally as a thymidylate synthase inhibitor. Interrupting the action of this enzyme blocks synthesis of the pyrimidine thymidine, which is a nucleoside required for DNA replication Thymidylate synthase methylates deoxyuridine monophosphate (dUMP) into thymidine monophosphate (dTMP). Administration of 5-FU causes a scarcity in dTMP, so rapidly dividing cancerous cells undergo cell death via thymineless death Some of its principal uses are in colorectal cancer, and pancreatic cancer, in which it has been the established form of chemotherapy for decades (platinum-containing drugs approved for human use in the US since 1978 are also very well established). It is sometimes used in the treatment of inflammatory breast cancer, an especially aggressive form of breast cancer.
CYTARABINE:
TRADENAME:
Cytosar-U Tarabine PFS Depocyt (longer-lasting liposomal formulation)
MECHANISM OF ACTION:
Cytosine arabinoside interferes with the synthesis of DNA. It is an antimetabolic agent.Its mode of action is due to its rapid conversion into cytosine arabinoside triphosphate, which damages DNA when the cell cycle holds in the S phase (synthesis of DNA). Rapidly dividing cells, which require DNA replication for mitosis, are therefore most affected. Cytosine arabinoside also inhibits both DNA[5] and RNA polymerases and nucleotide reductase enzymes needed for DNA synthesis. Ant imetabolit es are classified according to the substances wit h which they int erfere. y y y y Folic acid antagonist: Methotrexate. Pyrimidine antagonist: 5-Fluorouracil, Foxuridine, Cytarabine, Capecitabine, and Gemcitabine. Purine antagonist: 6-Mercaptopurine and 6-Thioguanine. Adenosine deaminase inhibitor: Cladribine, Fludarabine and Pentostatin.
DOSAGE:
In the induction therapy of acute non-lymphocytic leukemia, the usual cytarabine dose in combination with other anticancer drugs is 100 mg/m2/day by continuous IV infusion (days 1 to 7) or 100 mg/m2 IV every 12 hours (days 1 to 7). Cytarabine has been used intrathecally in acute leukemia in doses ranging from 5 to 75 mg/m2 of body surface area. The most frequently used dose was 30 mg/m2 every 4 days until cerebrospinal fluid findings were normal, followed by one additional treatment. The dosage schedule is usually governed by the type and severity of central nervous system manifestations and the response to previous therapy.
SIDE EFFECTS:
One of the unique toxicities of cytarabine is cerebellar toxicity when given in high doses. Toxicity:Low blood counts, Your white and red blood cells and platelets may temporarily decrease. This can put you at risk for infection, anemia and/or bleeding. GI disturbances, stomatitis, conjunctivitis, pneumonitis, fever, and dermatitis. Rarely, myelopathy has been reported after high dose or frequent intrathecal Ara-C administration
GEFTININB
TRADE NAME:
Iressa
MECHANISM OF ACTION:
Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Thus the function of the EGFR tyrosine kinase in activating the anti-apoptotic Ras signal transduction cascade is inhibited, and malignant cells are inhibited.
INDICATIONS:
For the treatment of locally advanced or metastatic non-small cell lung cancer, after failure of both platinum-based and taxane-based chemotherapies.
DOSING:
Gefitinib is taken by mouth. The dose is 250 mg once daily. The dose is the same for men or women of any age or weight, and gefitinib can be taken with or without food.
ADVERSE EFFECTS:
Acne is reported very commonly. Other common adverse effects (1% of patients) include: diarrhoea, nausea, vomiting, anorexia, stomatitis, dehydration, skin reactions, paronychia, asymptomatic elevations of liver enzymes, asthenia, conjunctivitis, blepharitis, interstitial lung disease that causes inflammation within the lung. Infrequent adverse effects (0.11% of patients) include: interstitial lung disease, corneal erosion, aberrant eyelash and hair growth.
LEUPROLIDE
TRADE NAME:
EligardTM, Lupron, Lupron Depot, ViadurTM
MECHANISM OF ACTION:
Leuprolide acts as an agonist at pituitary GnRH receptors. By interrupting the normal pulsatile stimulation and the desensitization of the GnRH receptors; it indirectly down regulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) leading to hypogonadism and thus a dramatic reduction in estradiol and testosterone levels in both sexes. Testosterone promotes the growth of prostate cancer. Therefore, leuprolide is used in treating prostate cancer to slow the growth of the cancer. Estrogens promote the growth of fibroids (benign tumors of the uterus) and areas of endometriosis (abnormal uterine tissue that exists outside of the uterus). Leuprolide is used to reduce the production of estrogen and treat both fibroids and endometriosis.
INDICATION:
y y y Prostate cancer Breast, ovarian and endometrial cancer Also used in non-cancerous conditions such as endometriosis, infertility, benign prostatic hypertrophy (BPH).
PREPARATIONS:
Leuprolide injection: 5 mg/ml. Lupron Depot microspheres for injection: 3.75, 7.5, 11.25, 15, 22.5 and 30 mg.
DOSING:
Leuprolide is injected under the skin (subcutaneously). Lupron Depot is injected into muscle (intramuscularly).
SIDE EFFECTS:
The most common side effects of leuprolide are aches and pain, headaches, hot flashes and irritation at the injection site. Leuprolide also may cause impotence, shrinking of the testes and breast enlargement in men. Depression, rare cases of suicidal behavior, low blood pressure, convulsions, joint pain and muscle aches have been reported in post-marketing surveillance.
CAPECITABINE
BRAND NAMES:
Xeloda
USES:
y y y
Adjuvant in colorectal cancer Stage III Dukes' C - used as first-line monotherapy. Metastatic colorectal cancer - used as first-line monotherapy, if appropriate. Metastatic breast cancer - used in combination with docetaxel, after failure of anthracycline-based treatment. Also as monotherapy, if the patient has failed paclitaxelbased treatment, and if anthracycline-based treatment has either failed or cannot be continued for other reasons (i.e., the patient has already received the maximum lifetime dose of an anthracycline).
STRENGTH:
Xeloda 150, 350 and 500 mg film-coated tablet pack contains 60 film-coated tablets (6 blisters of 10 tablets).
IN COLORECTAL CANCER
Recommended dose: 1,250 mg/m2 administered orally twice daily (morning and evening; equivalent to 2,500 mg/m2 total daily dose) for 2 weeks followed by a 1 week rest period given as 3 week cycles. Capecitabine tablets should be swallowed with water within 30 minutes after a meal. Alternate dose: 1,000 mg/m2 administered orally twice daily (morning and evening; equivalent to 2,000 mg/m2 total daily dose) for 2 weeks with 1 week rest may be may be appropriate.
HEXAMETHYLAMINE
TRADE NAME:
Hexalen, altretamine, Hexastat
INDICATIONS:
Palliative treatment of persistent or recurrent ovarian cancer
STRENGTH:
50 mg Capsule
DOSAGE:
Refer to individual protocols. Oral: y y y y Adults: 4-12 mg/kg/day in 3-4 divided doses for 21-90 days Alternatively: 240-320 mg/m2/day in 3-4 divided doses for 21 days, repeated every 6 weeks Alternatively: 260 mg/m2/day for 14-21 days of a 28-day cycle in 4 divided doses Alternatively: 150 mg/m2/day in 3-4 divided doses for 14 days of a 28-day cycle
ADMINISTRATION:
Administer total daily dose as 3-4 divided doses after meals and at bedtime.
ADVERSE REACTIONS:
y y y y y y y y Central nervous system: Peripheral sensory neuropathy, neurotoxicity (21%; may be progressive and dose-limiting) Gastrointestinal: Nausea/vomiting (50% to 70%), anorexia (48%), diarrhea (48%) Hematologic: Anemia, thrombocytopenia (31%), leukopenia (62%), neutropenia 1% to 10%: Central nervous system: Seizures Gastrointestinal: Stomach cramps Hepatic: Alkaline phosphatase increased <1%: Alopecia, depression, dizziness, hepatotoxicity, rash, tremor
IFOSFAMIDE
It is a nitrogen mustard alkylating agent used in the treatment of cancer.
TRADE NAMES:
y y y Mitoxana Ifex Holoxan
INDICATIONS:
It is given as a treatment for a variety of cancers, including:
y y y y y y y y
Testicular cancer Breast cancer Lymphoma (Hodgkin's and Non-Hodgkin's) Soft tissue sarcoma Osteogenic sarcoma (Bone cancer) Lung cancer Cervical cancer Ovarian cancer
ADMINISTRATION:
It is a white powder which, when prepared for use in chemotherapy becomes a clear, colorless fluid. The delivery is intravenous. Ifosfamide is often used in conjunction with Mesna to avoid internal bleeding in the patient, in particular hemorrhagic cystitis. Ifosfamide is given quickly, and in some cases can be given in as little as an hour.
TOXICITY:
Hemorrhagic cystitis is rare when ifosfamide is given together with mesna. A common and dose-limiting side-effect is encephalopathy (brain dysfunction).. The symptoms of ifosfamide encephalopathy can range from mild (difficulty concentrating, fatigue), to moderate (delirium, psychosis), to severe (nonconvulsive status epilepticus, coma) Low white blood cell count. (This can put you at increased risk for infection. See low blood counts). Low platelet count. (This can put you at increased risk for bleeding. See low blood counts).
Hair loss. Nausea and vomiting. Usually occurs 3-6 hours after therapy and may last up to 3 days.
PRECAUTIONS:
Use with caution in patients with renal or hepatic impairment. Unless clinically essential, initial or repeat doses should not be given to patients with a white blood cell count less than 1500 to 2000/mm3 and/or a platelet count less than 50,000/mm3. Ifosfamide should be discontinued if neurologic symptoms of somnolence, irritability, anxiety, confusion, hallucinations, or coma are observed.
MECHANISM OF ACTION:
Ifosfamide is an alkylating agent. This is a type of antineoplastic agent that works by interfering with DNA in a number of ways. Extra molecules, called alkyl groups, are added to DNA, which causes it to break apart as the cell tries to replace them. Ifosfamide also interferes with the bonds between DNA strands, stopping them from separating, which is a step required in DNA replication. By replacing bases (important components of DNA) alkylating agents also create mismatching, another way to stop DNA being reproduced properly. All these changes occur when a cell is preparing to divide, and the permanent damage they cause results in cessation of division and cell death.
MITOMYCIN
TRADE NAMES:
Mutamycin
INDICATIONS:
Used in the treatment of:
y y y
ADMINISTRATION:
MITOMYCIN-C 2 mg POWDER FOR INJECTION MITOMYCIN-C 10 mg POWDER FOR INJECTION
DOSE:
12 - 14 mg/m once a month or every 35 days by intravenous infusion. The crystals are dissolved in 200 mL of a 5% glucose solution which is then administered over a period of 30 minutes, preferably with Vitamin B Compound.
Hepatic:
Hepatic disorders may occur.
Renal:
since haemolytic uraemic syndrome and proteinuria, haematuria, oedema, and hypertension may occur, monitor the patients carefully by periodical examinations. If any abnormal findings are observed, discontinue administration, or adequate measures should be taken.
Gastrointestinal:
Anorexia, nausea and vomiting, and stomatitis may occur.
Hypersensitivity:
Hypersensitivity reactions such as rash may occur.
Urinary:
Cystitis, haematuria, or atrophy of the bladder caused by bladder instillation therapy may occur.
Respiratory:
STORAGE INSTRUCTIONS:
Store below 25C. Protect from light. The product reconstituted with water, saline or 5% glucose solution is stable at room temperature for 6 hours. KEEP OUT OF REACH OF CHILDREN.
MECHANISM OF ACTION:
Mitomycin C is a potent DNA crosslinker. A single crosslink per genome has shown to be effective in killing bacteri. Both alkylations are sequence specific for a guanine nucleoside in the sequence. Mitomycin is also used as a chemetherapeutic agent in Glaucoma Surgery Mitomycin is activated in vivo to a bifunctional and trifunctional alkylating agent. Binding to DNA leads to cross-linking and inhibition of DNA synthesis and function. Mitomycin is cell cycle phase-nonspecific
VINCRISTINE
TRADE NAME:
Oncovin, Vincasar PFS
1mg/mL
Acute Leukemia:
1.4 mg/sq.meter IV qWeek
Hodgkin's Disease, Non Hodgkin's Malignant Lymphomas, Rhabdomyosarcoma, Neuroblastoma, and Wilm's Tumor
ADVERSE EFFECTS:
y y y y y y y y y y y y y y y y y Alopecia (20-70%) Peripheral neuropathy Paresthesia Sensory loss Acute uric acid nephropathy Loss of deep-tendon reflexes Hypertension Hypotension Nausea and Vomiting Constipation Paralytic ileus Myelosuppression Leukopenia Gait changes Jaw pain Aspermia Amenorrhea
CONTRAINDICATIONS:
The needle should be properly positioned in the vein before this product is injected. Leakage to surrounding tissue during IV administration may cause considerable irritation. Immediately discontinue the injection, and introduce any remaining portion of the dose into another vein. Local injection of hyaluronidase and the application of moderate heat to the area of leakage will help disperse the drug and may minimize the discomfort and possibility of cellulitis. Intrathecal use may be fatal.
CAUTIONS:
Intrathecal administration will result in death Bone marrow depression, neuropathy, neuromuscular dz, neurotoxic agents, ototoxic agents, pulmonary dz, hepatic impairment, and potential CYP3A4 intxns, avoid extravasation Withhold if neurotoxicity develops-usually reversible Potential for jaw/parotid pain, hoarseness & dysphagia d/t cranial neuropathy y y y Vesicant Avoid pregnancy Risk of paralytic ileus
PACLITAXEL
TRADE NAMES:
Taxol , Onxal
SIDE EFFECTS:
Low blood counts. Your white and red blood cells and platelets may temporarily decrease. This can put you at increased risk for infection, anemia and/or bleeding. y Hair loss y Arthralgias and myalgias, pain in the joints and muscles. (see pain) Usually temporary occurring 2 to 3 days after Paclitaxel, and resolve within a few days. y Peripheral neuropathy (numbness and tingling of the hands and feet) y Nausea and vomiting (usually mild) y Diarrhea y Mouth sores y Hypersensitivity reaction. Fever, facial flushing, chills, shortness of breath, or hives after Paclitaxel is given (see allergic reaction). Less common side effects (occurring in 10-29%) for patients receiving Paclitaxel:
y y y y y y
Swelling of the feet or ankles (edema). Increases in blood tests measuring liver function. These return to normal once treatment is discontinued. (see liver problems). Low blood pressure (occurring during the first 3 hours of infusion). Darkening of the skin where previous radiation treatment has been given (radiation recall - see skin reactions). Nail changes (discoloration of nail beds - rare).
DRUG INTERACTIONS:
other drugs that may decrease bone marrow function (e.g., azathioprine, trimethoprim/sulfamethoxazole), drugs affecting liver enzymes that remove paclitaxel from your body (such as azole antifungals including ketoconazole, macrolide antibiotics including erythromycin, rifamycins including rifabutin, St. John's wort, certain anti-seizure medicines including phenytoin).
FOLINIC ACID
INDICATION AND DOSAGE:
Antidote for methotrexate toxicity Adult: 15 mg every 6 hr for 10 doses starting 24 hr after the start of methotrexate infusion. Continue admin until serum levels of methotrexate is <0.05 micromolar. May also be given via IM/IV injection Oral Folate-deficient megaloblastic anaemia Adult: 15 mg daily. Intravenous Adjunct to fluorouracil in colorectal cancer Adult: 200 mg/m2 BSA by slow IV inj over at least 3 min followed by 370 mg/m2 fluorouracil by IV inj. Treatment is given for 5 consecutive days and repeated at intervals of 28 days for 2 courses. Subsequently, may repeat at 4-5 wkly intervals if the patient has recovered completely from the toxic effects of the prior treatment course. Intramuscular Folate-deficient megaloblastic anaemia Adult: Up to 1 mg/day.
CONTRAINDICATIONS:
Hypersensitivity, pernicious anaemia and other megaloblastic anaemias secondary to vit B12deficiency, intrathecal and intraventricular admin.
SPECIAL PRECAUTIONS:
Undiagnosed megaloblastic anaemia, folate dependent tumors; pregnancy. Monitor calcium levels in patients receiving combined 5-Fluorouracil/Folinic acid treatment. To be given parenterally in the presence of GI toxicity, nausea or vomiting. Monitor serum levels of methotrexate to determine the optimal dose and duration of folinic acid admin. Monitor CBC, electrolytes and liver function tests before and regularly during treatment.
ETOPOSIDE
TRADE NAMES:
Etopul, Etoside
MECHANISM OF ACTION:
Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme, preventing religation of the DNA strands. This causes errors in DNA synthesis and promotes apoptosis of the cancer
INDICATIONS:
It is used as a form of chemotherapy for cancers such as Ewing's sarcoma, lung cancer, testicular cancer, lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme. It is often given in combination with other drugs. It is also sometimes used in a conditioning regimen prior to a bone marrow or blood stem cell transplant
SIDE EFFECTS:
y fever, chills, body aches, flu symptoms; y white patches or sores inside your mouth or on your lips; y pale skin, easy bruising or bleeding, unusual weakness; y feeling like you might pass out; y severe nausea and vomiting; y black, bloody, or tarry stools; or y Coughing up blood or vomit that looks like coffee grounds.
HYDROXY UREA:
TRADE NAMES:
Hydra,Hydrea and Hydrine
MECHANISM OF ACTION:
One mechanism of action is thought to be based on its reduction of production of deoxyribonucleotides via inhibition of the enzyme ribonucleotide reductase by scavenging tyrosyl free radicals as they are involved in the reduction NDPs.
INDICATIONS:
Hydroxyurea is used for the following indications:
y y y y
Myeloproliferative disease (primarily polycythemia vera and essential thrombocytosis) Sickle-cell disease (breaks down cells that are prone to sickle, as well as increasing fetal hemoglobin content) AIDS Psoriasis
SIDE EFFECTS:
y drowsiness, nausea, vomiting and diarrhea, constipation, mucositis, anorexia, stomatitis, bone marrow toxicity (which may take 721 days to recover after the drug has been discontinued), alopecia (hair loss), skin changes, abnormal liver enzymes, creatinine and blood urea nitrogen.
DEXRAZOXANE
TRADE NAMES:
Zinecard and Cardioxane.
INDICATIONS:
It reduces the incidence and severity of cardiomyopathy associated with doxorubicin administration in women with metastatic breast cancer who have received a cumulative doxorubicin and will continue to receive doxorubicin therapy to maintain tumor control. It is believed to work by preventing the release of certain chemicals (iron-mediated free radicals) in the body. These chemicals are thought to be part of the reason why doxorubicin causes damage to the heart.
CONTRAINDICATIONS:
a. b. c. d. Chemotherapy regimens that do not contain an anthracycline. Pregnancy. Moderate to Severe Kidney Impairment. Decreased Functions of Bone Marrow.
DOSE:
Dexrazoxane 250mg,500mg/per vial. Powder for IV infusion after reconstitution and dilution.
TAMOXIFEN
INTRODUCTION:
Tamoxifen is an antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxytamoxifen.
BRAND NAMES:
Nolvadex and Tamofen
INDICATIONS:
Tamoxifen citrate is used to treat metastasizing-breast cancer or to help prevent breast cancer in high-risk women.
CONTRAINDICATIONS:
Tamoxifen Citrate Tablets are contraindicated in patients with known hypersensitivity to the drug and women who are at high risk for or those with a history of blood clots. Tamoxifen is contraindicated in patients requiring concomitant coumarin-type anticoagulant therapy.
DOSE:
Tamoxifen tablets are available in a strength of 10 mg and 20 mg.
CISPLATIN
Cisplatin is a cancer medication that interferes with the growth of cancer cells and slows their growth and spread in the body.
ADMINISTRATION:
Cisplatin is administered through a vein (intravenously or IV) as an infusion. Patient may be given IV fluids for 8 to 12 hours before patient receive cisplatin.
INDICATION:
Metastatic testicular or ovarian tumors, advanced bladder cancer.
CONTRAINDICATIONS:
Pre-existing renal impairment; myelosuppression ; hearing impairment; history of allergic reactions to cisplatin or other platinum-containing compounds.
DRUG INTERACTIONS:
Aminoglycosides Potentiation of nephrotoxicity is possible. Lithium Cisplatin may transiently decrease lithium serum levels. Loop diuretics (e.g, furosemide) Potentiation of ototoxicity is possible.
Paclitaxel Paclitaxel clearance decreases when cisplatin is given immediately prior to paclitaxel, resulting in increased hematologic toxicity. Phenytoin Cisplatin may decrease absorption or increase metabolism, resulting in lower serum levels of phenytoin.
ADVERSE EFFECTS:
Cardiovascular: MI; cerebrovascular accident; cerebral arteritis; thrombotic microangiopathy. CNS: Peripheral sensory neuropathy with a glove-and-stocking distribution. GI: Nausea; vomiting; anorexia; transient LFT elevations. Hematologic: Bone marrow suppression. Hypersensitivity: Anaphylactic reaction. Metabolic: Hypomagnesemia; hypocalcemia; hypokalemia Renal: Dose-related and cumulative renal tubular damage. Special Senses: Tinnitus; high frequency hearing loss.
OVERDOSE SYMPTOMS:
Kidney failure, liver failure, deafness, ocular toxicity, significant myelosuppression, intractable nausea and vomiting, neuritis, death.
TRADE NAMES:
Platidiam Platimit Unistin
ASPARAGINASE
MECHANISM OF ACTION:
Administration of asparaginase hydrolyzes serum asparagine to nonfunctional aspartic acid and ammonia, depriving tumor cells of a required amino acid. Tumor cell proliferation is blocked.
INDICATIONS:
For the treatment of patients with acute lymphoblastic leukemia (ALL) as a component of a multiagent chemotherapeutic regimen.
CONTRAINDICATIONS:
Serious allergic reactions to asparaginase or other Escherichia coli derived L-asparaginases; serious thrombosis, pancreatitis, and serious hemorrhagic events with prior L-asparaginase therapy.
DRUG INTERACTIONS:
Vaccines, live The risk of live vaccineinduced adverse reactions may be increased by co administration of asparaginase. Use of live vaccines in patients receiving asparaginase should be deferred.
ADVERSE EFFETCS:
Cardiovascular: Sagittal sinus thrombosis, thrombosis. CNS: CNS hemorrhages, CNS thrombosis, coma, hallucinations, seizures. Hematologic: Coagulopathy, decreased fibrinogen, decreased protein C, decreased protein S and antithrombin III, increased PT, increased PTT. Hepatic: Elevated transaminases, hepatotoxicity (some fatal), hyperbilirubinemia, liver function abnormalities. Hypersensitivity: Anaphylaxis and serious allergic reactions. Metabolic: Glucose intolerance, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia.
BLEOMYCIN
BRAND NAMES:
Bleocin and Bleocip
PHARMACOLOGICAL CLASS:
Bleomycin (BLM) is an antitumoral antibiotic active against various animal and human tumors.
MECHANISM OF ACTION:
Bleomycin is a glycopeptide antibiotic with a unique mechanism of antitumor activity. The drug binds to guanosine-cytosine-rich portions of DNA via association of the "S" tripeptide and by partial intercalation of the bithiazole rings. A group of five nitrogen atoms arranged in a squarepyramidal conformation binds divalent metals including iron, the active ligand, and copper, an inactive ligand. Molecular oxygen, bound by the iron, can produce highly reactive free radicals and Fe (III). The free radicals produce DNA single-strand breaks at 3'-4' bonds in deoxyribose. This yields free base propenals, especially of thymine: cytotoxicity is cell-cycle-phase specific for G2 phase. Resistance to bleomycin in normal tissues can be correlated with the presence of a bleomycin hydrolase enzyme, which is in the cysteine proteinase family. The enzyme replaces a terminal amine with a hydroxyl, thereby inhibiting iron binding and cytotoxic activity. The low concentration of enzyme in the skin and lung may explain the unique sensitivity of these tissues to bleomycin toxicity. However, correlation of hydrolase levels with tumor cell sensitivity has thus far been negative.
INDICATIONS:
Bleomycin for injection should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents. y Squamous Cell Carcinoma, Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin is poorer in patients with previously irradiated head and neck cancer. y Lymphomas, Hodgkin's disease, non-Hodgkin's lymphoma. y Testicular Carcinoma, Embryonal cell, choriocarcinoma, and teratocarcinoma.
IDIOSYNCRATIC REACTIONS:
In approximately 1% of the lymphoma patients treated with Bleomycin, an idiosyncratic reaction, similar to anaphylaxis clinically, has been reported. The reaction may be immediate or delayed for several hours, and usually occurs after the first or second dose. It consists of hypotension, mental confusion, fever, chills, and wheezing. Treatment is symptomatic including volume expansion, pressor agents, antihistamines, and corticosteroids.
Other:
Vascular toxicities coincident with the use of Bleomycin in combination with other antineoplastic agents have been reported. The events are clinically heterogeneous and may include myocardial infarction, cerebrovascular accident, thrombotic microangiopathy or cerebral arteritis.
CONTRAINDICATION:
Because of the possibility of developing Raynaud phenomenon, it is recommended that intralesional bleomycin is not performed in patients with peripheral vascular disease or collagen vascular disease. The use of bleomycin is not recommended in pregnancy and lactation because of the risks of the drug to the baby. It has been shown to cause birth defects in micei. It is contraindicated in patients who have demonstrated a hypersensitive or an idiosyncratic reaction to it.
DRUG INTERACTIONS:
Do not start, stop, or change the dosage of any medicines without your doctor's or pharmacists approval.Some products that may interact with this drug include: digoxin, drugs that may harm the kidneys (e.g., aminoglycosides such as gentamicin, cisplatin), phenytoin
DOSAGE FORM:
This medicine is available as an injection USUAL ADULT DOSE: For Squamous Cell Carcinoma: 0.25 to 0.50 units/kg (10 to 20 units/m2) intravenously, intramuscularly, or subcutaneously weekly or twice weekly.
For non-Hodgkin's Lymphoma: 0.25 to 0.50 units/kg (10 to 20 units/m2) intravenously, intramuscularly, or subcutaneously weekly or twice weekly. For Testicular Cancer: 0.25 to 0.50 units/kg (10 to 20 units/m2) intravenously, intramuscularly, or subcutaneously weekly or twice weekly. Improvement in testicular tumors is prompt and noted within 2 weeks. If no improvement is seen at this time, improvement is unlikely. For Hodgkin's Disease: 0.25 to 0.50 units/kg (10 to 20 units/m2) intravenously, intramuscularly, or subcutaneously weekly or twice weekly. After a 50% response, a maintenance dose of 1 unit daily or 5 units weekly intravenously or intramuscularly should be given. For Malignant Pleural Effusion: 60 units administered as a single bolus intrapleural injection.
CYCLOPHOSPHAMIDE
BRAND NAME:
CYCLOMIDE ENDOXAN ZYCRAM
MECHANISM OF ACTION:
These compounds crosslink DNA by adding an alkyl group (CnH2n+1) to the guanine base of DNA, at the number seven nitrogen atom of the imidazole ring. This induces inhibition of DNA replication, leading to cell death. CYC exerts its cytotoxic effect on both resting and dividing lymphocytes. Its precise mechanisms in treatment of autoimmune diseases are not well established. In patients with rheumatoid arthritis, CYC has been shown to suppress T-helper cell functions with prolonged reduction of B cells due to the slower rate of recovery of B lymphocytes from an alkylating agent
INDICATION:
Cyclophosphamide is used alone for the treatment of several types of cancers but often in combination with other drugs to treatbreast cancer, leukemia and ovarian cancer. It also is approved for treating nephrotic syndrome (a disease of the kidneys) in children. Unapproved uses include the treatment of Wegener's granulomatosis, severe rheumatoid arthritis, lupus erythematosus, advanced mycosis fungoides, and several of forms of vasculitis.
SIDE EFFECTS:
If you experience any of the following serious side effects, seek emergency medical attention or contact your doctor immediately: y an allergic reaction (shortness of breath; closing of your throat; difficulty breathing; swelling of your lips, face, or tongue; or hives); y blood in the urine; y black or tarry stools; y painful or difficult urination; y signs of infection such as fever; chills, or sore throat; y jaundice (yellowing of the skin or eyes); y lower back or side pain; y chest pain, difficulty breathing, or swelling; y unusual bleeding or bruising; or y Changes in bone marrow function (detected by blood tests). Other less serious side effects may be more likely to occur. Talk to your doctor if you experience y nausea, vomiting, or decreased appetite; y mouth sores; y abdominal pain; y diarrhea; y temporary hair loss;
CONTRAINDICATION:
Cyclophosphamide should not be used under the following circumstances: y evidence of haemorrhagic cystitis, acute systemic or urinary infection, drug- or radiation-induced urothelial toxicity y severe bone marrow impairment y presence of infections (as a result of immunosuppression induced by cytotoxic treatment) which could lead to fatal complications
DRUG INTERACTIONS:
Allopurinol enhances the ability of cyclophosphamide to reduce production of blood cells from the bone marrow. Cyclophosphamide increases the occurrence of heart failure that is caused by doxorubicin (Adriamycin), increases the action of blood thinners such as warfarin, and decreases the effectiveness of quinolone antibiotics DOSAGE FORM: It is available in both oral and IV.
References:
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