draditithegreat
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Drugs......for reference! all anti_cancers covered!
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09.20.05 (3 years ago)
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Cancer Drugs
General Information On Chemotherapy
Cell Structure
Methods of Administering Anticancer Drugs
Drugs Used In Cancers
Chemotherapeutic families
Alkylating agents :
BCNU (Carmustine) Busulphan CCNU (Lomustine)
Chlorambucil Cyclophosphamide Dacarbazine
Hexamethylmelamine Ifosfamide Mechlorethamine
MeCCNU (Semustine) Melphalan Mitomycin-C
Procarbazine Streptozotocin Thiotepa
Antimetabolites :
Cytarabin 5-Fluorouracil 5- FUdR
Gemcitabine Hydroxyurea 6 Mercaptopurine
Methotrexate 6 Thioguanine
The Platinum Family :
Carboplatin Cisplatin Oxaliplatin
Topoisomerase Interactive Agents :
Dactinomycin Etoposide Irinotecan
Mitoxantrone Teniposide (VM - 16) Topotecan
Anthracyclines :
Daunorubicin Doxorubicin Epirubicin
Idarubicin
Antimicrotubule Agents
A.Vinca Alkaloids Vinblastine Vincristine Vindesine
Vinorelbine
B. Taxanes Docetaxel Paclitaxel
Hormonal Therapy
A. Anti Androgen Flutamide
B. Anti Estrogen Tamoxifen
C. Aromatase
Inhibitors Aminoglutethimide Letrozole
D. Progesterones Medroxiprogesterone and Megesterol
Differentiating Agent :
All - trans retinoic acid
Miscellaneous Drugs :
Bleomycin, L-Asparaginase, Biphosphonates
Radiation and Chemotherapy Protectors :
Amifostine CSF Leucovorin
UromitexanA
Immunological Agents: Interferon Alfa-2a
General Information On Chemotherapy
Cancer is a disease in which there is uncontrolled multiplication and spread within the body of abnormal forms of the body's own cells.
Chemotherapy with cytotoxic drugs is the main or only method of treatment for only a few cancers. But it is increasingly used as an adjuvant to surgery or radiotherapy in a range of common cancers.
There are other chemical approaches to cancer treatment - immunotherapy and the use of biological response modifiers (e.g. interferon, interleukin).
Compared with chemotherapy of bacterial diseases, chemotherapy of cancer presents a difficult problem. It has been possible to find drugs with selective toxicity in many microorganisms because microorganisms have biochemical processes other than human cells and are also qualitatively different. But although cancer cells are abnormal, it has proved difficult to find general exploitable differences between the cancer cells and normal body cells.
Cancer cells differ from normal cells in that they can manifest three characteristics not seen in normal cells.
Uncontrolled proliferation - Some cancer cells multiply slowly and some fast. It is therefore not universally true that the cancer cells proliferate faster than normal cells. The main difference is that the cancer cell multiplication is not controlled by the processes that regulate normal tissue or organ growth. Though they are characterized by an inability to undergo differentiation, they are still capable of cell division.
Invasiveness - Normal cells during differentiation maintain and respect their own areas and mostly damaged or dead cells are replaced of the same type. Cancer cells invade tissues in the other layers of the organ and spread to neighboring tissues.
Metastasis - Cancer cells form secondary tumors after they are released from the primary tumor and reach other sites through blood vessels or lymphatics or after being shed into body cavities.
Cell Structure
All living cells have an inner core called nucleus surrounded by cytoplasm and are covered by a cell membrane. The nucleus contains chromosomes formed by the gene material. The gene materials are formed by DNA (deoxyribonucleic acid) which consists of two chains of amino acids, coiled around each other. The sequence of the amino acids is specific for each person, like his name or signature or finger print. Hence DNA analysis can identify individuals.
The multiplication of cells is under the control of the genes. DNA grows by forming its replicas and forms fresh cells. In the normal programming of the body, this multiplication is a controlled process. Sometimes, if there are genetic errors, either natural or inherited or produced by external chemicals, carcinogens or viruses, the abnormal genes multiply - but do not respect nor are they controlled by any restrictions, thus producing cells which are rebels and behave as such. Cancer cells are characterized by abnormal chromosome structures and uncontrolled growth usually accompanied by loss of cellular differentiation (anaplasia).
The main aim of drugs is to control the proliferation of such abnormal cancerous cells without affecting the normal cells. Most anticancer drugs are anti-proliferative and therefore will also affect rapidly dividing normal cells. Hence they are likely to depress bone marrow, to impair healing, to depress growth, to cause sterility and hair loss and to be teratogenic (cause birth defects).
By the time a cancer is detected, it has generally metastasized, presenting a much more difficult problem. The basic approach is the removal or destruction of cancer cells, minimizing toxic effects to normal cells.
There are some drugs that stimulate the immune system to destroy those neoplastic cells not killed by anticancer drugs and these are of importance. Unfortunately, since currently available agents also effect some rapidly multiplying normal cells like bone marrow, their use involves weighing the benefit against toxicity, hence the advances in cancer drug research are much slower than in antibacterial drugs.
Methods of Administering Anticancer Drugs.
Intravenous. Most drugs are given as intravenous infusion suitably diluted with saline over a period of 15-30 minutes. These are generally preceded or followed by fluid infusions like saline, glucose etc. which will help to eliminate the drug rapidly from the body and reduce its toxicity.
Intra-arterial. Some drugs are given into the blood vessels (arteries) supplying a particular organ so that the drug reaches the special organ in a higher concentration before it is diluted on reaching the rest of the circulation.
Oral. Some drugs are absorbed orally and are given safely by the oral route. This is the most convenient method for the patients.
Topical. Sometimes drugs are given into body cavities to get maximum concentration at the cancer affected areas for action on organs in those cavities. These are washed out after a short time.
The drugs may be given -
Into the cerebral spinal fluid in brain metastasis.
Into peritoneal cavity.
Into the pleural cavities .
Most anticancer drugs produce side effects.
Bone marrow Leukopenia, lymphocytopenia and resulting infections,
Immunosuppression
Thrombocytopenia
Anemia
GI Tract Oral or intestinal ulceration
Diarrhea
Hair follicles Alopecia
Gonads Menstrual irregularities, including premature menarche, impaired Spermatogenesis
Wounds Impaired healing
Fetus Teratogenesis (especially during first trimester)
Specific drugs and their dose Limiting Side Effects.
CYDARINE Dabur
Bleomycin Pulmonary fibrosis (bleomycin lung)
Busulfan Pulmonary fibrosis (busulfan lung)
Doxorubicin Cardiotoxicity
Cisplatin Nephrotoxicity/peripheral neuropathy
Carboplatin Myelosuppression
Cyclophosphamide Hemorrhagic cystitis
Vincristine Neurotoxicity
Cytarabine Cerebral damage
Make sure that patient is not sensitive to the drug about to be administered. If necessary, do a preliminary skin test. Watch for any reactions in the first few minutes.
Many of the side effects are common to most anti cancer drugs.
Nausea and vomiting.
Bone marrow depression- RBC, WBC and Platelet counts go down.
Hair loss (alopecia).
Hence patients must be prepared for them and to handle them.
Doctors should take measures to reduce these as much as possible.
Each drug must be studied before administering it to patients during pregnancy and lactation and in new born children.
BCNU (Carmustine)
Pharmacology
Nitrosourea. Alkylates DNA by forming chloroethyl diazonium hydroxide resulting in intrastrand cross-links in DNA.
Therapeutics
Given intravenously 200 mg/m2 every 6 weeks.
Common Uses
Used in brain tumors, multiple myeloma, refractory Hodgkin's disease, non Hodgkin's lymphoma, malignant melanoma; Also in high dose regimens/bone marrow transplant regimens for breast cancer, neuroblastoma, gliomas, melanoma and sarcoma.
Side Effects
Nausea, vomiting, leukopenia, thrombocytopenia, pulmonary fibrosis; with high doses, hepatotoxicity and venoocclusive disease of liver.
Busulphan
Pharmacology
Alkyl sulfonate. Interferes with DNA by cross linking of strands.
Therapeutics
Orally effective. Major degree of specificity for granulocytes and is hence useful in myelogenous leukemia.
Common Uses
Chronic myeloid leukemia
Side Effects
Myelosuppression, pulmonary fibrosis.
MYLERAN Burroughs Wellcome
BUSUPHAN Elder
CCNU(Lomustine)
Pharmacology
A nitrosourea, which in aqueous solution undergoes molecular decomposition and alkylates DNA intrastrand crosslinks and prevents replication. It is highly lipid soluble and crosses the blood brain barrier and thus is useful in brain tumors.
Therapeutics
Given orally.
Common Uses
Primary and metastatic brain tumors, advanced Hodgkin's disease.
Side effects
Delayed myelosuppression, dose dependent nephrotoxicity, vomiting, nausea, liver toxicity and carcinogenecity.
LOMUSTINE Biddle Sawyer
Chlorambucil
Pharmacology
Orally effective alkylating agent inhibiting DNA biosynthesis by cross linking and breakdown of DNA strands.
Therapeutics
Given orally. One of the earliest drugs to be put to use. Still useful as part of chemotherapy combinations.
Common Uses
Hodgkin's disease, CLL, macroglobulinemia
Side Effects
Nausea, vomiting, carcinogenecity and pulmonary fibrosis.
LEUKERAN Burroughs Wellcome
Cyclophosphamide
Pharmacology
An alkylating prodrug activated in the liver.
Therapeutics
Can be given orally or intravenously. The commonest chemotherapeutic agent used at present.
Common Uses
Breast cancer, NHL, leukemia, Hodgkin's disease, Burkitt's lymphoma, endometrial cancer, small cell lung cancer, multiple myeloma,sarcomas, high dose regimen for lymphomas and solid tumors.
Side Effects
Myelosuppression, usually severe, but both nadir and recovery are usually faster than most other chemotherapeutic agents. Nausea and vomiting, acute sterile haemorrhagic cystitis (prophylactic hydration and administration of the free radical scavenger Mesna help), alopecia and carcinogenecity.
LEDOXAN Dabur
CYCLOXAN Biochem
ELDAMIDE Elder
ENDOXAN German Remedies
ENDOXAN-ASTA German Remedies
CYCRAM VHB
Dacarbazine
Pharmacology
It is a monofunctional alkylating agent and tetrazine derivative. It releases highly reactive diazonium ions, which crosslink DNA strands. The molecules are unstable on exposure to light.
Therapeutics
Given intravenously.
Common Usesz
Single agent activity against malignant melanoma. Also useful in soft tissue sarcomas and Hodgkin's disease.
Side Effects
Myelosuppression, nausea and vomiting, local reactions at the site of injection, carcinogenic risk, delayed hepatic toxicity, which can sometimes prove fatal.
DT - CARE Criticare
DACZIN Indon
DACARZINE Khandelwal
DTI-KOREA Shree Ganesh
DTIC-VHB VHB
Hexamethylmelamine (Altretamine)
Pharmacology
Synthetic small molecule alkylating agent. It is a prodrug. Alkylates DNA.
Common Uses
Maximum activity in ovarian carcinoma in combination chemotherapy. Also tried in bronchogenic carcinoma, cervical cancer, breast cancer and lymphomas.
Side effects
Nausea, vomiting, peripheral neuropathy, CNS effects; mild myelosuppression.
Ifosfamide
Pharmacology
A nitrogen mustard group alkylating agent. Activated in the body, but slower than cyclophosphamide and its analogues.
Therapeutics
Given intravenously.
Common Uses
Soft tissue sarcomas, non small cell lung cancers, germ cell testicular cancers, cervical cancer.
Side effects
Hemorrhagic cystitis, nausea, vomiting, alopecia, myelosuppression.
IPAMIDE Dabur
HOLOXAN German Remedies
Mechlorethamine (Nitrogen Mustard)
Pharmacology
Mechlorethamine is the first prototype antitumor alkylating agent.
Therapeutics
It is rarely used except as a component in standard treatment regimens of Hodgkin's disease.
MeCCNU (Semustine)
Pharmacology
A nitrosourea. A bifunctional alkylating agent.
Therapeutics
It is clinically equal or less active than the other nirosoureas BCNU (carmustine) or CCNU (lomustine).
Side effects
Delayed myelosuppression, dose dependent nephrotoxicity, vomiting, nausea, liver toxicity and carcinogenecity.
Melphalan
Pharmacology
A nitrogen mustard alkylating agent of the amino acid phenylalanine. Causes cell death by alkylation of DNA and prevention of replication.
Therapeutics
Given orally or intravenously.
Common Uses
High dose chemotherapy combinations preceding bone marrow transplantation regimens for breast cancer, ovarian cancer, testicular cancer and multiple myeloma.
Side effects
Leukopenia, thrombocytopenia in non transplant regimens; in BMT, high myelosuppression, nausea, vomiting, diarrhea and alopecia.
ALKERAN Burroughs Wellcome
Mitomycin C
Pharmacology
Antibiotic from Streptomyces caespitosus. An aziridine derivative alkylating drug. Activated in the body to form an antitumor alkylating agent in hypoxic cells and hypoxic tumor regions.
Therapeutics
Given intravenously.
Common Uses
Adenocarcinoma of stomach, pancreas, colon and breast, small cell and non small cell lung cancer; as a hypoxic cell selective cytotoxic agent in combination with radiation in head and neck cancer.
Instilled intravesically for 3 hours in transitional cell carcinoma.
Side effects
Myelosuppression, nephrotoxicity, interstitial pneumonitis, nausea and vomiting.
MITOMYCIN-C Biochem
MITOPLUS VHB
Procarbazine
Pharmacology
Synthetic molecule originally prepared as a Mono Amine Oxidase inhibitor (MAO inhibitor). A prodrug, it undergoes oxidation of the hydrazine moiety in the liver and forms alkylating and methylating products which cause DNA and RNA cross links, methyl adducts and strand breaks.
Therapeutics
Given orally.
Common Uses
Lymphomas, Hodgkin's disease, brain tumors.
Side effects
Pancytopenia; can cause negative interactions with other drugs such as antidepressants and sympathomimetics because of its MAO inhibitor effect.
Streptozotocin
Pharmacology
Naturally occurring nitrosourea isolated from Streptomyces achromogenes. More hydrophilic than other nitrosoureas. Adds a methyl group to the O6 position of guanine in DNA.
Therapeutics
Given intravenously.
Common uses
Beta and non - beta islet cell pancreatic tumors, Hodgkin's disease, colon carcinoma, hepatoma, pancreatic ductal carcinoma.
Side effects
Gluconeogenesis interference; irreparable damage to beta islet cells of the pancreas can cause diabetes.
Thiotepa
Pharmacology
An aziridine alkylating agent. A prodrug activated in the body. Acts by bifunctional alkylating process to bind DNA.
Therapeutics
Given intravenously in doses of 0.2 mg / kg.
Common uses
Lymphoma, malignant melanoma, colon carcinoma and childhood solid tumors; intravesically in bladder tumors; intracavitary instillation in malignant effusions.
Side effects
Mild myelosuppression, local reactions.
TESPAMINE VHB
Cytarabin
Pharmacology
An antimetabolite which is a cytidine analogue. It affects DNA polymerase activity acting as chain terminator, by interfering with elongation and replication of DNA strands.
Therapeutics
Given intravenously at an infusion rate of usually 100 - 200 mg/m2/day; high doses can go upto
2 - 3 grams /day. It is also given intrathecally in meningeal leukemia and other meningeal neoplasms. Also given intra peritoneally in ovarian cancers.
Common Uses
Acute non lymphoblastic leukemia, blastic phase of CML, NHL.
Side Effects
Myelosuppression, anorexia, nausea and vomiting, epithelial ulceration, sometimes perforation; hepatic dysfunction, intrahepatic cholestasis and pancreatitis.
In high doses can cause seizures, cerebral and cerebellar dysfunction, polyneuropathies, pulmonary edema.
Intrathecal administration can precipitate fever, seizures and alterations in mentation.
CYTARINE Dabur
CYTABIN Cadila Health Care
CYTARABIN Shree Ganesh
CYTROSAR (preservative free) VHB
5-Fluorouracil
Pharmacology
.
It is an antimetabolite. It is a pyrimidine antagonist to the base uracil required for DNA synthesis.
Therapeutics
It is given intravenously, and rarely by oral route. However, bio availability is erratic when given orally.; A cream is also available for skin cancers, and eye drops for conjunctival and superficial eye cancers.
Common Uses
Adenocarcinoma of the gastro intestinal tract, pancreas, breast.
Side Effects
Gastrointestinal toxicity, myelosuppression, alopecia.
FIVOFLO Dabur
FLURACIL Biochem
5-FU KOREA Shree Ganesh
ONCOURCIL T.D.P.L.
FUdR (Floxuridine)
Pharmacology
Antimetabolite against natural pyrimidines with action similar to 5FU.
Therapeutics
Given intravenously 0.2mg/kg/d for up to 14 days (7mg/ m2/d).Its first pass effect after HAI is 95% and little drug escapes into systemic circulation.
Common Uses
It has been mainly used for Hepatic Arterial Infusion (HAI). Patients with liver-only metastasis who failed to systemic 5FU may respond to HAI, FUdR. Also tried intraperitoneally, absorbed into portal circulation.
Side effects
Nausea and vomiting, oral mucositis, diarrhea; myelosuppression occurs less often. Systemic toxicity is less with FUdR, while local reactions predominate: gastritis, duodenitis, frank ulcer, and chances of sepsis. HAI may produce cholestatic jaundice and biliary sclerosis.
Gemcitabine
Pharmacology
Pyramidine analogue of deoxycytidine. The drug is phosphorylated to the 5' diphosphate (dFdCDP) and 5' triphosphate (dFdCTP) variants. dFdCDP inhibits ribonucleotide reductase, thus decreasing the pools of dATP, dCTP, dGTP and dTTP.
Therapeutics
Commonly, 30 minutes intravenous infusion weekly for 3 weeks followed by a week's rest. The usual dose is 1,000 mg / m2.
Common Uses
Non small cell lung cancer (NSCLC), small cell lung cancer (SCLC), metastatic breast cancer, pancreatic cancer, refractory ovarian cancer, hormone refractory prostate cancer, head and neck cancer.
Side effects
Myelosuppression, nausea, vomiting, hematuria, proteinuria, skin rash, 'flu' like symptoms, central or peripheral edema, abnormal liver function tests, occasionally alopecia and bronchospasm.
GEMZAR Eli Lilly (Lilly Oncology)
Hydroxyurea
Pharmacology
Synthetic cytotoxic drug, inhibits ribonucleotide reductase, responsible for conversion to deoxyribose form.
Therapeutics
Given orally 20 - 30 mg/kg single daily dose. Dose to be titrated as per response.
Common Uses
Myeloproliferative disorders, CML, radiosensitizer in the treatment of epithelial malignancies including cervical, head and neck and non small cell lung cancers.
Side effects
Myelosuppression, skin rash, hyperpigmentation, nausea, vomiting, teratogenic potential.
HYDAB Dabur
HYDROX-L BDH
URDOX Cadilla Healthcare
NEODREA VHB
6 Mercaptopurine
Pharmacology
An antimetabolite inhibiting purine synthesis, reactions and incorporation into nucleic acids.
Therapeutics
Oral dose - 70 - 100 mg/ m2/ day.
Common Uses
ALL
Side effects
Myelosuppression, nausea, vomiting, anorexia, diarrhea, stomatitis, hepatotoxicity.
EMPURINE Dabur
MERCAPTHOL Arvind Remedies
PURI-NETHOL Burroughs Wellcome
PURINETONE VHB
Methotrexate
Pharmacology
An antifolate antimetabolite. Inhibits dihydrofolate reductase, which builds up folate pool in the cells, necessary for the synthesis and methylation of purine and pyrimidine bases.
Therapeutics
Given orally as well as parenterally.
Common Uses
Leukemia, breast cancer, head and neck cancer, lymphoma, osteogenic sarcoma, urothelial cancers and choriocarcinoma.
Side effects
Myelosuppression, nausea, vomiting, mucositis, dose dependent nephrotoxicity, acute and chronic hepatotoxicity, pneumonitis, hypersensitivity reactions; after intrathecal therapy, acute and chronic neurotoxicity, encephalopathy.
ZEXATE Dabur
CYTOTREX BDH
NEOTREXATE Biddle Sawyer
BIOTREXATE Biochem
TRIXILEM Elder
MTX-KOREA Shree Ganesh
TEVATREX SPPL
ONCOTREX Sun Pharma
ONOTREX TDPL
METHOTREXATE VHB
6-Thioguanine
Pharmacology
Antimetabolite, a purine antagonist. A structural analogue of guanine, precursor to natural nucleotides. Inhibits purine synthesis and interconversion reactions, and forms fraudulent nucleotides.
Therapeutics
Given orally 100 mg / m2 twice a day for 7 days.
Common uses
Acute leukemias; remission, induction and maintenance therapy in acute myelogenous leukemia.
Side effects
Myelosuppression, nausea, vomiting.
THIOGUANINE-VHB VHB
Carboplatin
Pharmacology
A platinum analogue to cisplatin, with significantly less gastrointestinal and nephrotoxicity. Inhibits DNA biosynthesis.
Therapeutics
Cyclical intravenous infusion.
Common Uses
Used as an alternative to cisplatin in genitourinary, ovarian and testicular cancers.
Side Effects
Nausea and vomiting, leukopenia, thrombocytopenia, alopecia, ototoxicity, rarely neuropathy and hepatic dysfunction.
KEMOCARB Dabur
CARBOPLAN Octan
TEVACARB SPPL
CARBOTINOL VHB
ONCOCARBIN AQ TDPL
Cisplatin
Pharmacology
It is a platinum derivative. Acts by inhibiting DNA synthesis and interferes with DNA replication, without affecting normal RNA and protein synthesis.
Therapeutics
Given intravenously. 1 mg/ml powder is dissolved in 500 ml of 0.9% NaCl with pre and post chemotherapy hydration,and antiemetics. Can also be given intraperitoneally, usually at 100 or 200 mg/m2 with the same precautions of hydration. Regional intra-arterial has also been described.
Common Uses
Testicular and ovarian cancers, head and neck, lung and bladder cancers.
Side Effects
Severe nausea and vomiting, nephrotoxicity, neurotoxicity (ototoxicity), myelosuppression
KEMOPLAT Dabur
CISPLATIN Biochem
NEOPLAT Biological E
CYTOPLATIN 10 Cipla
CYTOPLATIN 50 Cipla
PLATICARE Criticare
BLASTOLEM Elder
PLATICIS German Remedies
AQUAPLAT Khandelwal
TUMOTIN Max
CISPLAN Natco
CISPLATIN - KOREA Shree Ganesh
CISPLATINUM KOREA Shree Ganesh
TEVAPLATIN SPPL
ONCOPLATIN-AQ TDPL
Oxaliplatin
Pharmacology
It is a platinum derivative. Acts by inhibiting DNA synthesis and interferes with DNA replication, without affecting normal RNA and protein synthesis.
Therapeutics
Given intravenously. Good hydration, like all platinum analogues, is a must.
Common Uses
Testicular and ovarian cancers, head and neck, lung and bladder cancers.
Side effects
Less nephrotoxic than cisplatin; there may be sensory neuropathy, nausea and vomiting.
Dactinomycin (Actinomycin D)
Pharmacology
Antitumor antibiotic obtained from Streptococcus parvullus. Binds to DNA by intercalation, blocks DNA and RNA synthesis; causes topoisomerase mediated single strand breaks in DNA.
Therapeutics
Given intravenously.
Common Uses
Wilm's tumor, Ewing's sarcoma, embryonal rhabdomyosarcoma, gestational choriocarcinoma.
Side Effects
Myelosuppression, severe nausea and vomiting, stomatitis, diarrhea, extravasation can cause soft tissue damage and ulceration.
It is a radiosensitizer and can cause skin and gastrointestinal toxicity.
DACMOZEN VHB
Etoposide
Pharmacology
Semisynthetic epipodophyllotoxin. Acts by topoisomerase II inhibition of DNA. Original etoposide solutions interact with acrylic material to produce cracks and leaks.
Therapeutics
Given orally and intravenously.
Common Uses
Small cell lung cancer, refractory testicular tumors, monocytic leukemia.
Side effects
Myelosuppression, hypersensitivity reactions (GIT, vasomotor and pulmonary), therapy associated acute non lymphocytic leukemia (t-ANLL), nausea, vomiting, alopecia, somnolence.
FYTOSID Dabur
BIOPOSIDE Biochem
BEPOSID Biological E
ETOSID CAPSULES Cipla
ETOSID INJ Cipla
LASTET Khandelwal
TOPOK Max
EPOSED Octan
ASIDE Shree Ganesh
TEVASIDE SPPL
ETOPUL VHB
Irinotecan
Pharmacology
A plant alkaloid derivative of camptothecin: CPT-11 topoisomerase I inhibitor.
Therapeutics
Given intravenously as infusion.
Common Uses
Metastatic colorectal cancer, pancreatic cancer.
Side effects
Reversible myelosuppression, diarrhea, facial flushing and abdominal cramps during infusion, late onset cholera type diarrhea not responsive to loperamide or codeine, mild nausea and vomiting, low grade fever, alopecia at higher doses.
IRINOTEL Dabur
CAMPTO Rhone-Poulenc
Mitoxantrone
Pharmacology
Synthetic anthracenedione compound allied to the anthracyclines. Acts by inhibiting Topoisomerase II - DNA, preventing the enzyme from completing the replication program of DNA.
Therapeutics
Given intravenously 10 - 12 mg / m2 every 3 - 4 weeks.
Common Uses
Prostate cancer, soft tissue sarcomas, refractory acute leukemias, childhood and adult AML, non Hodgkin's lymphomas, breast cancer.
Side effects
Myelosuppression, nausea, vomiting, stomatitis, alopecia; less cardio-toxic than anthracyclines, but reduces LVEF.
ONCOTRAN TDPL
Teniposide (VM - 16)
Pharmacology
Epipodophyllotoxin. Inhibits relegation of DNA cleaved by Topoisomerase II and induce protein-linked breaks.
Therapeutics
Its pharmacological action and therapeutic uses are similar to etoposide.
Topotecan
Pharmacology
Derivative of plant alkaloid Camptotheca acuminata. It is a camptothecin. It reacts with Topoisomerase I and prevents resealing of DNA single strands.
Therapeutics
Given intravenously
Common uses
As a combination drug tried in ovarian cancer, small-cell lung cancer, soft tissue sarcoma.
Side effects
Reversible myelosuppression; anemia, diarrhea.
TOPOTEL Dabur
Daunorubicin
Pharmacology
Anti tumor anthracyclin antibiotic derived from Streptomyces species. Forms covalent topoisomerase - DNA complexes preventing ligation relegation reactions. Intercalates into DNA strands causing single stranded and double stranded breaks.
Therapeutics
Given intravenously.
Common Uses
ALL, AML, Kaposi's sarcoma.
Side Effects
Myelosuppression, alopecia, local extravasation reactions with delayed and difficult healing, acute and chronic cardiac toxicity.
DAUNOMYCIN Pharmacia and Upjohn
DAUNOCIN (Lyophilised) VHB
Doxorubicin(Adriamycin)
Pharmacology
Antitumor anthracyclin antibiotic. Forms covalent topoisomerase - DNA complexes preventing DNA replication. Also intercalates into DNA strands, causing single and double strand breaks.
Therapeutics
Given intravenously, sometimes intrapleurally and intraarterially.
Common Uses
Cancers of the breast, endometrium, ovary, salivary gland, esophagus, stomach, adrenocortical carcinoma, Ewing's sarcoma, hepatoblastoma, soft tissue sarcomas, Kaposi's sarcoma, pleural mesothelioma, thymoma.
Side Effects
Myelosuppression, alopecia, acute and chronic cardiac toxicity, nausea and vomiting, mucositis.
ADRIM Dabur
DOXORUBICIN-INJ Biochem
DOXOBIN Biological E
DOXOCARE Criticare
DOXOLEM Elder
DOXORUBICIN Khandelwal
KLASINOMYCIN Khandelwal
TUMODOX Max
RUBINAT Octan
ONCODRIA T.D.P.L.
ADROSAL VHB
Epirubicin
Pharmacology
Anthracycline derivative. Acts on Topoisomerase II. Inhibits relegation of DNA cleaved by Topoisomerase II and induces protein-linked breaks.
Therapeutics
Given orally. Also intraarterially for well defined nonresectable metastatic and primary tumors of the liver. It has a substantial first pass effect.
Common Uses
Active in metastatic breast cancer. Used in cervical cancer, advanced nasopharyngeal cancer.
Side effects
Cardiotoxicity.
Idarubicin (Idamycin)
Pharmacology
Anthracycline. Acts on Topoisomerase II. Inhibits relegation of DNA cleaved by Topoisomerase II and induces protein-linked breaks.
Therapeutics
Given intravenously 12mg/m2 intravenously daily for 3 days with cytarabine.
Common Uses
Acute myelogenous leukemia.
Side effects
Nausea, vomiting, Bone marrow suppression, cardiotoxicity.
Vinblastine
Pharmacology
Vinca alkaloid . Acts by disruption of microtubules and metaphase arrest of mitotic spindles at low concentrations.
Therapeutics
Given intravenously as a brief infusion, 6 mg/ m2 weekly, or as a 5 day infusion, 1.5 - 2 mg / m2 / day.
Common uses
Advanced Hodgkin's disease and other lymphomas, combination drug of second choice in lung cancer, germ cell cancers of the testes, choriocarcinoma, carcinomas of the breast and the urinary bladder, Kaposi's sarcoma.
Side effects
Neutropenia, neurotoxicity less severe than vincristine, nausea, vomiting, alopecia; potent vesicant and should not be administered subcutaneously, intramuscularly or intraperitoneally.
CYTOBLASTIN Cipla
Vincristine
Pharmacology
Vinca alkaloid . Acts by disruption of microtubules and metaphase arrest of mitotic spindles at low concentrations.
Therapeutics
Given intravenously. In children greater than 10 kg, a bolus of 2 mg / m2 is usually recommended; for adults, 1.4 mg / m2. Also, can be tried as a 5 day infusion.
Common uses
Wilm's tumor, CML, CLL, lymphomas, Ewing's sarcoma, multiple myeloma, lung cancers, childhood cancers and rhabdomyosarcoma.
Side effects
Neurotoxicity, severe autonomic toxicity (particularly severe constipation), alopecia; potent vesicant and should not be administered subcutaneously, intramuscularly or intraperitoneally.
VINCRISTINE Biochem
CYTOCRISTIN Cipla
ONCOCRISTINE-AQ TDPL
Vindesine
Pharmacology
Vinca alkaloid . Basically desacetyl vinblastine. Acts by disruption of microtubules and metaphase arrest of mitotic spindles at low concentrations.
Therapeutics
Given intravenously as many schedules; weekly, or a biweekly bolus of 2 - 4 mg / m2, 5 day infusion; prolonged infusions 1.2 - 2 mg / m2 / day for 2 - 5 days every 3 - 4 weeks.
Common uses
ALL, non small cell lung cancer (NSCLC), in combination with drugs like cisplatin or mitomycin - C
Side effects
Neutropenia, neurotoxicity, alopecia.
Vinorelbine
Pharmacology
Vinca alkaloid . Semisynthetic Vinblastine derivative. Acts by disruption of microtubules and metaphase arrest of mitotic spindles at low concentrations.
Therapeutics
Given intravenously. Oral use still experimental.
Common uses
Advanced NSCLC, either alone or in combination with cisplatin. Also active in advanced ovarian and breast cancers and lymphoma.
Side effects
Neutropenia, neurotoxicity less severe than other Vinca alkaloids, alopecia.
VINELBINE Dabur
Docetaxel
Pharmacology
Synthetic antineoplastic drug producing sustained mitotic block affecting microtubules. It is a taxane derivative. The microtubules are stabilized inhibiting normal process of mitosis, promoting disassembly.
Therapeutics
Intravenous infusion 50 - 100 mg/m2 as a1 hour infusion, preceded by dexamethasone 8mg twice a day from one day before and H2 blockers half an hour before starting infusion.
Common Uses
Stage III and stage IV ovarian cancer, metastatic breast cancer, other tumors refractory to conventional therapies including non small cell lung cancer, head and neck cancers, esophageal and bladder cancers, germ cell tumors, lymphoma and Kaposi's sarcoma.
Side Effects
Myelosuppression, hypersensitivity reactions, fluid retention syndrome, pruritus, rash, erythema, desquamation, alopecia, moderate peripheral neurotoxicity, stomatitis.
DAXOTEL Dabur
TAXOTERE Rhone-Poulenc
Paclitaxel
Pharmacology
A taxane, originally isolated from the bark of Taxus brevifolia, now synthesized. Inhibits proliferation of cells by binding to microtubules, thus stabilizing them against depolymerisation and assembly, with an induction of a sustained mitotic block.
Therapeutics
Given intravenously, usually as a 3 hour or 96 hour infusion.
Common Uses
Advanced ovarian and breast cancers with metastasis. Combined with other drugs in primary induction therapy in suboptimally debulked stage III or IV ovarian cancer.
Also used in cancers refractory to conventional therapy; NSCLC and SCLC, head and neck cancers, esophageal and bladder cancers, germ cell malignancies, lymphoma and Kaposi's sarcoma.
Side effects
Neutropenia, hypersensitivity, peripheral neuropathy, optic nerve imbalances, cardiac rhythm irregularities, mucositis, alopecia, local reactions to injection sites.
INTAXEL Dabur
PAXTAL SPPL
Flutamide
Pharmacology
Antiandrogen. Pure androgen receptor antagonist at cellular level without any progestational effect.
Therapeutics
Given orally 250 mg three times a day.
Common Uses
Metastatic prostatic cancer.
Side effects
Diarrhea with or without abdominal discomfort, gynecomastia, rarely hepatotoxicity.
PROSTAMID BDH
CYTOMID-250 Cipla
FLUTACARE Criticare
DROGENIL Fulford
PLUTAMIDE Torrent
Tamoxifen
Pharmacology
Non steroidal anti estrogen which binds specifically to estrogen receptors.
Therapeutics
Given orally 10 mg twice a day usually.
Common uses
Adjuvant therapy in women with resected receptor positive breast cancer; in advanced metastatic breast cancer in post menopausal women; ovarian cancer refractory to other drugs or with elevated CA - 125.
Side effects
Hot flushes (artificial menopause), treated with concurrent low doses of Megestrol, retinal toxicity in high doses, predisposition to thromboembolic phenomenon and depression.
TAMOXIFEN Dabur
CYTOFEN BDH
TAMOXIFEN TABS Biochem
ELDTAM Elder
ONCOTAM Indon
MAMOFEN Khandelwal
TAMOXIFEN LYKA Lyka
TEVAFEN SPPL
ONCOMOX TDPL
TAMOFEN Torrent
Aminogluthethimide
Pharmacology
.
Aromatase inhibitor. Originally used to produce medical adrenalectomy. Suppresses postmenopausal estrogen synthesis by inhibiting conversion of circulating androgens to estrogens.
Therapeutics
Given orally starting from 250 mg / day and increased daily. Replacement hydrocortisone 100 mg / day started for a week and then tapered off to 40 mg / day.
Common Uses
Metastatic breast cancer; in adrenocortical cancers to reverse excess hormone production; upto 2 gm / day may be necessary. If combined with ketoconazole, the dose can be reduced as this drug also has a similar action.
Side Effects
Lethargy, orthostatic hypotension, nausea, vomiting, hypothyroidism, reversible agranulocytosis, rash.
Letrozole
Pharmacology
Non steroidal aromatase inhibitor with high specificity for inhibiting estrogen production. 180 times more potent than aminogluthethimide as an aromatase inhibitor in vitro.
Common Uses
Metastatic breast cancer.
Side effects
Headache.
Medroxyprogesterone and Megestrol
Pharmacology
17 - OH progesterone derivatives, which are primarily used as antiestrogens.
Therapeutics
Medroxyprogesterone is given orally in the form of 2.5 or 5 mg tablets and as depot injections of 100 - 400 mg / ml strength.
Megestrol is given orally as 20 - 40 mg tablets.
Common Uses
Medroxyprogesterone - metastatic breast and prostate cancer, metastatic endometrial cancer, in doses of 400 mg / week.
Megestrol is used in advanced breast cancer in doses of 160 mg / day (4 divided doses); hormone responsive endometrial cancer in doses of 320 mg / day; occasionally hormonal therapy of prostatic cancer in doses of 160 mg / day; also used to treat cancer related cachexia or AIDS in doses of 160 - 1600 mg / day. Low doses are used to treat hot flushes in women with breast cancer and in men after androgen ablative therapy.
Side effects
Appetite stimulation with resultant weight gain, Addison's disease due to suppression of adrenal steroid production, menstrual irregularities, increased susceptibility to infections and thromboembolic phenomenon.
All - trans retinoic acid
Pharmacology
.
Induces cellular differentiation and suppresses proliferation in various cellular lines.
Common Uses
Acute promyelocytic leukemia.
Side Effects
Skin dryness or itching, headache, pseudotumor cerebri, hypertriglyceridemia, hypercholesterolemia, hypercalcemia, leucocytosis, thrombosis, hepatotoxicity, congestive cardiac failure, bone pains, respiratory distress, weight gain.
Bleomycin
Pharmacology
An antibiotic obtained from Streptococcus verticellus. It binds to DNA resulting in singl3e or double strand breaks following free radical formation, resulting in chromosomal aberrations
Therapeutics
It can be given intravenously, subcutaneously or intramuscularly, as well as intracavitarily in malignant effusion.
Common Uses
Testicular cancer, and squamous cancers of the cervix, skin, penis and lymphoma
Side Effects
Anaphylaxis, blistering, hyperkeratosis of the palms. Pulmonary fibrosis.
BLEOCHEM Biochem
BLEOCARE Criticare
BLEOCIN Khandelwal
OIL BLEO Khandelwal
BLEDMAX Max
ONCOBLEO TDPL
L-Asparaginase
Pharmacology
Enzyme obtained from bacteria like E.coli. Depletes the circulating asparagine by converting it to aspartic acid. Cancer cells of lymphoid origin cannot utilize aspartic acid, and their protein synthesis is affected. Normal cells can synthesize asparagine and are less affected.
Therapeutics
Given IV or IM 6000 IU/m2 three times a week for 3 to 4 weeks or daily 2000-5000IU/m2 for 10 to 20 days.
Common Uses
Lymphoid malignancies.
Side effects
Mild to severe hypersensitivity in 10% patients, usually in the second week. Decreases protein synthesis, clotting factors, contraindicated if there is a history of pancreatitis, antagonizes action of methotrexate.
LEUNASE Biochem
LEUCOGINASE VHB
Biphosphonates
Bisphosphonates are pyrophosphates such as etidronate, alendronate, and clodronate.
Pharmacology
Bisphosphonates get adsorbed to the hydroxyapatite crystals in the mineralized matrix, thereby reducing the solubility of the matrix and osteoclastic resorption. A stable bone matrix prevents signaling of osteoclasts to migrate to the site. They block attachment of osteoclast precursors to mineralized matrix, preventing transformation into mature, functioning osteoclasts. Bisphosphonates reduce bone turnover and, when used in combination with adequate hydration to increase renal excretion of calcium, reduce serum calcium concentrations. However, these drugs have no antineoplastic properties.
Therapeutics
Oral & intravenous.
Common Uses
In conjunction with standard antineoplastic therapy, for the treatment of osteolytic bone metastases of breast cancer1 and osteolytic bone lesions of multiple myeloma2 hypercalcemia of malignancy Paget's disease of bone.
Contraindications
Patients with clinically significant hypersensitivity to bisphosphonates.
Side effects
Fever, fluid overload, generalized pain, injection site reaction, fatigue, hypertension, abdominal pain, anorexia, constipation, nausea, vomiting, and dyspepsia urinary tract infection, headache, seizures bone pain, arthrosis, anemia, leukopenia, hypocalcemia, hypokalemia, hypomagnesemia and hypophosphatemia.
PAMIFOS Dabur
Amifostine
Pharmacology
.
A sulfur containing thiophosphate used as a protective agent
Therapeutics
Given intravenously.
Common Uses
Used as a nephroprotective agent during cisplatin therapy
Side Effects
Nausea, vomiting, hypotension
AMIPHOS Dabur
ETHYOL Fulford
CSF
Pharmacology
Granulocyte colony stimulating factor. Produces dose dependent increase of circulating neutrophils, accompanied by expansion of the myeloid components in the marrow.
Therapeutics
Given subcutaneously or intravenously following neutropenia due to any cause, especially following chemotherapy or bone marrow transplantation.
Side effects
Fever, malaise, myalgia, arthralgia.
GRANOCYTE Rhone-Poulenc
Leucovorin
Pharmacology
A folic acid derivative, which neutralizes the effects of folic acid antagonists like methotrexate, but potentiates the actions of 5 fluorouracil.
Therapeutics
Given as intramuscular or intravenous injection; sometimes intraarterial.
Common Uses
Reversal of methotrexate toxicity weight by weight. Leucovorin 15 - 500 mg / m2 enhances 5 FU benefits in colon cancer. Used intraarterially in combination with FUDR and dexamethasone in metastatic liver cancer.
Side effects
Mild and negligible.
LEUCOVORIN-DABUR Dabur
LEUCOVORIN CALCIUM Biochem
CALCIUM LEUCOVORIN Cynamide
FERBAN-KOREA Shree Ganesh
NYRIN VHB
Uromitexan
Pharmacology
Sulfhydryl compound. It is a free radical scavenger. Detoxifies urotoxic metabolites of cyclophosphamide and ifosfamide.
Therapeutics
Although orally absorbed, slow to achieve adequate urinary concentration. Hence given as an intravenous bolus or infusion. About 20 percent equivalent of the dose of cyclophosphamide is given 15 minutes before and 4 and 8 hours after. The timing of the uromitexan infusion is crucial, as it has a half life of 35 minutes and cyclophosphamide has a half life of 4 hours.
Common Uses
Used to prevent hemorrhagic cystitis following administration of cyclophosphamide / ifosfamide.
Side effects
Mild nausea, occasional vomiting, headache, limb pains, diarrhea.
MESNA German Remedies
HOLOXAN-MESNA German Remedies
Interferon Alfa-2a
Pharmacology
Interferons alpha, beta, and gamma are a family of proteins produced by cells in response to viral infections, or stimulation by double stranded RNA, antigens or mitogens. They can interfere with subsequent viral challenge. They have immunomodulatory and antiproliferative effects on malignant cells.
Therapeutics
Given as subcutaneous or intravenous injections.
Common Uses
Hairy cell leukemia, CML, cutaneous T - cell lymphoma, Kaposi's sarcoma, RCC.
Side effects
Fever, 'flu' like symptoms.
ALFERON Indon
REAFERON Torrent
HEBERON ALFAR USV
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