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DRUG MOA
Bifunctional alkylation
CLINICAL USE
Nitrogen Mustard MOPP regimen for HODGKINS LYMPHOMA Phosphoramide Mustard Sarcomas Prior to Bone Marrow transplantation Chronic B-cell lymphocytic leukemia and lymphoma Immunosuppressive therapy (SLE/ Rheumatoid therapy) Prior to Bone Marrow transplantation Gliomas; Brain tumors Multiple myeloma Bone marrow transplant ABVD regimen for HODGKINS LYMPHOMA Gliomas Radiation therapy
TOXICITY
Tissue necrosis
ANTIDOTE
ALKYLATING AGENTS
Mechlorethamine Cyclophosphamide Ifosfamide Melphalan Chlorambucil
Monofunctional alkylation
Busulfan Nitrosoureas
Penetrates the CSF Carmustine / BCNU
Dacarbazine Temozolomide
Acetaminophen predication
ANTIMETABOLITES
(1) FOLIC ACID ANALOGS Methotrexate
Inhibits DHFR enzyme (DIHYDROFOLATE REDUCTASE) S-phase specific Unable to polyglutamate methotrexate
Intrathecal prophylaxis in
lymphomas & leukemias Choriocarcinoma NON-HODGKINS LYMPHOMA Osteosarcoma Leukemia Urine alkalinization 1 line metastatic mesethelioma nd 2 line metastatic nonsmall cell lung cancer
st
rd
Leucovorin
Permetrexed
Capecitabine
(prodrug of 5-FU)
---Converted by Thymidine Phosphorylase to 5-FU Analog of 2-deoxycytidine Converted by Deoxycytidine kinase to an active for of 5 Induction of remission to ALL
Hand-foot syndrome
Cytarabine
Gemcitabine
monophosphate nucleotide --- Only drug effective for pancreatic cancer Mild therapy; no alopecia Myelosuppresion
(3) PURINE ANALOGS inhibits HGPRT enzymes Guanine analog Mercaptopurine Thioguanine Fludarabine Cladribine
Guanine analog
Induction of remission to ALL Induction of remission to AML Chronic lymphocytic leukemia Hairy cell leukemia
Myelosuppression Myelosuppression
Adenosine analog
Adenosine analog
ANTIMITOTIC
(1) VINCA ALKALOIDS
Vincristine
NON-HODGKINS LYMPHOMA together with CHOP (Cyclo, Prednisone, Doxorubicin) HODKINS LYMPHOMA together with MOPP (Meclorethamine, Prednisone, Procarbazine) HODGKINS LYMPHOMA together with ABVD (Doxorubicin, dacarbazine, bleomycin) Adjuvant and metastatic NSCLCA Neurotoxicity, numbness, tingling, loss of DTR
Myelosuppression
Vinblastine
Vinorelbine
Myelosuppression
Neutropenia
(2) EPIPODOPHYLLOTOXINS
Etoposide
Conditions lowering albumin levels will lead to increased free fraction, increasing toxicities Acute nonlymphocytic leukemia
TUMOR ANTIBIOTICS
(1) ANTHRACYCLINES Doxorubicin Daunorubicin Epirubicin Mitoxantrone Liposomal doxorubicin (2) BLEOMYCIN
Oxidative DNA damage Binds with Topoisomerase-II Generates free radicals Intercalates DNA Promotes apoptosis Lymphomas, Leukemia, Breast cancer, Sarcoma, SCLCA ALL and AML Breast Cancer Acute non-lymphocytic leukemia, hormone-resistant prostate cancer Ovarian cancer Lymphomas Less cardiotoxic Cardiotoxicity due to free radicals generated
(3) MITOMYCIN
ANAL CANCER!
Less cardiotoxic, less neutropenia Pulmonary fibrosis Decline in CO2 diffusion capacity Cutaneous toxicity HUS
PLATINUM COMPOUNDS forms DNA ADDUCTS which are recognized by MMR, that will promote apoptosis
Cisplatin
ALL Germ cell tumor Lung cancer Head and neck cancer Ovarian cancer Ovarian cancer Lung cancer GI cancer, Ovarian cancer Germ cell cancer Cervical cancer Pancreatic cancer Nephrotoxicity Most emetogenic Renal toxicity Ototoxicity Myelosuppression
Carboplatin Oxaliplatin
Less reactive than cisplatin, better tolerated Less neutropenia Less nephrotoxic, more neuropathic Hypersenistivity reactions Mimimal Bone marrow and GI toxicity Hyperglycemia, Hypoalbuminemia, protein C and S deficiency Adrenocortical carcinoma
L-asparaginase
Mitotane
Adrenocorticosteroids
Aromatase Inhibitors
Prevent formation of estrogen from adrenal gland and adipose tissue by inhibiting AROMATASE
CLINICAL USE Immunosuppresion Glucose intolerance Osteoporosis Water retention GI ulcers Bone mineral density, bone pains, increased fracture rates Musculoskeletal problems!
TOXICITY
Anti-Estrogen
For post-menopausal ER/PR+ breast cancer patients in adjuvant, neoadjuvant, metastatic setting Blocks estrogen receptors itself
GnRH analogs
Stimulates FSH and LH production by the pituitary gland then will late cause negative feedback inhibition Binds to androgen receptors and causes complete androgen blockade
Thrombosis risk Endometrial CA Hot flashes, nausea, vomiting, menstrual irregularities Initial flare reaction
Anti-androgen
Prostate cancer
Decreased libido Hot flashes Gynecomastia Mastodynia Paradoxical stimulation of androgen receptors
Interleukin-2
CLINICAL USE Expands T-cell response that is cytolytic for tumor cells Melanoma Renal cell carcinoma AML Filgrastim/ Lenograstim Expands population of neutrophil precursors Prophylaxis for chemotherapy induced neutropenia
ANTIDOTE
G-CSF
Fever Chills
TARGETED RESPONSE
DRUG CLINICAL USE Her2 receptor Vegf receptor Breast cancer Angiogenesis SIDE EFFECT CHF Hypersensitivity ANTIDOTE
MONOCLONAL ANTIBODIES
Traztuzimab Bevacizumab Cetuximab Panitumomab Rituximab Imatinib (Gleevec) Gefitinib Erlotinib Sunitinib Sorafenib
Hypertension, bleeding, proteinuria Hypersensitivity reactions Skin rashes Hypersensitivity reactions Hypersensitivity reactions Hypersensitivity reactions
EGFR receptor
Colorectal cancer Head and neck cancer Colorectal cancer B-cell lymphomas
Lapatinib
PROTEOSOME INHIBITOR
Bortezomib
Degrades proteosomes that denatures IKb Pancreatic neuroendocrine tumors Advanced renal cell cancer Advanced renal cell cancer
MTOR INHIBITOR
Everolimus Temsirolimus
Intrathecal Administration Can cross Blood Brain Barrier
Cytotoxic agent (Antimetabolite) Cytotoxic agent (Antimetabolite) Cytotoxic agent (Alkylating agent) Cytotoxic agent (Alkylating agent) Topoisomerase interactive agent