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Pharmacology - Chen
Oncology
| Question | Answer |
|---|---|
| Name the available nitrogen mustards (alkylating agents)(#5) | Mechlorethamine Cyclophosphamide Ifosfamide Melphalan Chlorambucil |
| Name the available ethylenimines/methylamines alykylating agents(Aziridines)(#3) | Thiotepa Hexamethylmelamine (HMM) Triethylenrmelamine (TEM) |
| Name the available alkyl sulfonate alkylating agents (#1) | Busulfan |
| Name the available nitrosoureas (alkylating agents) (#4) | Carmustine (BCNU)Bis Chloroethyl Lomustine (CCNU)Chloroethyl Cyclohexyl Semustine (Methyl-CCNU) Streptozocin |
| Name the available azines/hydrazines (alkylating agents) (triazines)(#2) | Darcarbazine(DTIC) - Azine Procarbazine(Matulane)- Hydrazine |
| Name the available Platins (alkylating agents) (#3) | Cisplatin Carboplatin Oxaliplatin |
| Which alkylating agent is the most reactive, readily hydrolyzed, and reactive in aqueous solution | Mechlorethamine (Mustargen) Nitrogen Mustard |
| Which component of DNA is most sensitive to alkylation? Which is 2nd most important? | 1) N-7 of guanine 2) oxygen at C6 |
| Regimen: COP Name indications for this regimen | C: Cyclophosphamide O: Oncovin - Vincristine P: Prednisone Indication: lymphomas and chronic leukemias |
| Regimen: CMF Name indications for this regimen | C: Cyclophosphamide M: Methotrexate (anti-metabolite) F: 5-fluorouracil (anti-metabolite) Adjuvant therapy post-mastectomy, Ovarian carcinoma, pancreatic carcinoma |
| Regimen: CP Name indication for this regimen | C: Cyclophosphamide P: Cisplatin Indication: Ovarian Carcinoma |
| What toxicities are commonly associated with alkylating agents? | NVD, Alopecia, Cystitis, Hematological Toxicity (anemia, thrombocytopenia, leukopenia) |
| With which groups of alkylating agents is "pneumonitis" associated? Which antimetabolite demonstrates this adverse effect? | Busulfan and Nitrosoureas Methotrexate |
| With which alkylating agents is "renal/bladder" toxicity mainly associated? [Hemorrhagic Cystitis] | Cyclophosphamide, Ifosfamide |
| Which agents are known to cross the blood brain barrier and cause CNS toxicity? | Ifosfamide, Dacarbazine, Procarbazine Thiotepa |
| Which agents are vesicants and may cause vein damage, and ulceration? | Nitrosoureas Nitrogen Mustards (Mechlorethamine) |
| Regimen: MOPP Name indications for this regimen | Mechlorethamine Oncovin (Vincristine) Procarbazine Prednisone Indication: Hodgkin's Disease |
| Which compound is a byproduct of Cyclophosphamid/Ifosfamide metabolism and is the known cause of its nephrotoxicity? | Acrolein |
| Name the alkylating agents that are also known to be prodrugs? | Cyclophosphamide, Ifosfamide, Cisplatin, Oxaliplatin, Carboplatin |
| Explain the Metabolism of Cyclophosphamide (Metabolism, T 1/2, Excretion) What is its active metabolite? | Prodrug - Activated by P450 Hydroxylation T1/2: 16 hrs Excretion: Urine Phosphoramide Mustard - active metabolite |
| With which drugs do cyclophosphamide have drug-drug interactions? | Inducers and Inhibitors of 3A4 |
| What does MESNA stand for and for what condition is it used? | Mercapto Ethane Sulfonate Sodium (NA) ---Used to reduce acrolein toxicity to the bladder induced by cyclophosphamide and ifosfamide |
| Which drug is approved by the FDA for testicular cancer? (3rd Line) How is it administered? | Ifosfamide - Slow IV Infusion Administer with fluid and MESNA |
| Which drug is approved 1st line for treatment of testicular cancer? | Cisplatin |
| Name the 4 Curable Cancers | 1.) Choriocarcinoma in Women 2.) Hodgkin's Disease 3.) Testicular Carcinoma 4.) Some cases of acute leukemia |
| Regimen: MP For which Neoplasia is this regiment 1st Line | Melphalan Prednisone First Line: Multiple Myeloma (Ovarian Cancer, Breast Cancer) |
| With alkylating agents drugs is N/V infrequent? | nitrogen mustards: Melphalan, Chlorambucil |
| Which alkylating agent is the slowest acting? For which cancer is this drug first line? | Chlorambucil Chronic Lymphocytic Leukemia (CLL) |
| What is the dose limiting toxicity of Chlorambucil? | Myelosuppression |
| Regimen: DT Name indications for this regimen | Dacarbazine Tamoxifen Indication: Malignant Melanoma |
| What combination treats leukemia NOT solid tumors? | Pentostatin, 6-MP & Cladaribine |
| Regimen: FAM Name indications for this regimen | 5FU Adriamycin Mitomycin Indication: Solid Tumors such as colorectal cancer |
| Regimen: GP Name indications for this regimen | Gemcitabine CisPlatin Indication: Pancreatic Cancer, NSCLC |
| Regimen: POMP Name indications for this regimen | 6-MP Oncovin (Vincristine) MTX Prednisone Acute Lymphoblastic Leukemia (ALL) |
| Regimen: PVB Name indications for this regimen | CisPlatin Vinblastine Bleomycin Metastatic Testicular Cancer (curative), Ovarian Carcinoma, Bladder carcinoma, lung carcinoma |
| Regimen: SMF Name indications for this regimen | Streptozocin Mitomycin 5FU Malignant Pancreatic Islet Cell Tumors |
| Which drugs are cell specific tot he M Phase (mitotic-short phase)? | Vinca Alkaloids: Vincristine, Vinblastine, Vinorelbine, Vindesine Paclitaxel (Taxol) |
| Which drug is used for treatment of breast cancer and colorectal cancer and causes kidney toxicity | Cisplatin |
| Which drugs are specific to S Phase (DNA synthesis)? | Antimetabolites: MTX, 5FU, 6TG, 6MP, Cytarabine, Azacytidine Misc: Hydroxyurea Camptothecins: Topotecan and Irinotecan |
| Which drug is a radiation sensitizer? | Taxol (Paclitaxel) |
| To which cell cycle phases is bleomycin specific to? | G2 and M phase |
| Name the Available Epidophyllotoxins? To which cell cycle phase do these drugs act on? | Etoposide Teniposide S and G2 phases |
| Imatinib Mesylate (Gleevec) Name the indications? | Chronic Myelogenous Leukemia (CML) Gastointestinal Stromal Tumor (GIST) |
| Which drug treats solid tumors, is M phase specific, causes neurotoxicity and Myelosuppression? | Vincristine |
| Methotrexate belongs to which type of Antimetabolite class? | Pteridine (Folic Acid Analog) |
| Name the Pyrimidine Analog Antimetabolites | 5FU Cytarabine Gemcitabine |
| Name the Purine Analog Antimetabolites | 6MP 6TG Pentostatin |
| Which anti-metabolites are indicated for Hairy Cell Leukemia? | Pentostatin Cladarabine |
| Regimen: FOLFOX Name the components and indication | Folinic Acid 5FU Oxaliplatin Colorectal Cancer |
| Melphalan is a part of which class of Alkylating Agents? Which side effects are less/not present which are common with other alkylating agents? | Melphalan is a Nitrogen Mustard NVD are infrequent Alopecia does not occur at standard doses |
| For which cancers if Busulfan indication? Name 3 of its unique adverse effects | Indicated for CML and CGL Pneumonitis, hepatic venoocclusive disease, hyperuricemia |
| Which class of alkylating agents are known to cross the blood brain barrier and used in treatment of various brain tumors? | Nitrosoureas Carmustine, Lomustine |
| Which drug's structure resembles glucose and is therefore sensitive to the pancreas? | Streptozocin |
| Which alkylating agent lacks cress resistance with other mustard-type alkylating agents? | Procarbazine |
| What is the most common side effect of Procarbazine? What is it's effect on metabolism of other substances? | Leukopenia and Thromobocytopenia 3A4 Inhibitor MAO Inhibitor |
| Explain the mechanisms of drug resistance associated with Cisplatin | 1.) Overexpression of MRP 2 and MRP 6 2.) Elevated GSH |
| Compare Toxicities of Cisplatin, Carboplatin, and Oxaliplatin | Renal Toxicity: Cis > Carbo > Oxali Carboplatin - Bone Marrow Suppression Oxaliplatin - Peripheral Neuropathy |
| Which drug is used as a rescue agent against the renal toxicity associated with Cisplatin? What other toxicity is this drug useful for? What side effects are associated with this drug? | Amifostine Xerostomia in patients receiving radiation to head and neck Side Effects: HOTN, severe N/V |
| Which Anti-metabolite drug is not specific to the S phase? | Gemcitabine |
| Which ABC transporters efflux MTX out of cells to cause MTX resistance? In which form is methotrexate not subject to this efflux? | MRP 1 - 5 Avoids efflux in glutamylated form by (FPGS) |
| 6MP is subject to efflux by which ABC transporters? | MRP 4/5 |
| What is rescue therapy for Methotrexate? How does it work? | Leucovorin Overcomes blockade of FH4 and inhibitos active transport of MTX into cells. |
| What is the prodrug of 5FU? What drug is 5FU converted to? | Capecitabine --> 5FU --> 5- Fluroxidine |
| What side effects are unique to 5FU? | Chest Pain and Cardiogenic Shock |
| What are the potential mechanisms of Methrotrexate Resistance? (5) | 1.) reduced RFC1 (folate carrier) 2.) Impaired Polyglutamate formation (FPGS) 3.) increases DHFR activity 4.) Increases TS Activity 5.) |
| What is the Active form of 5FU? What enzyme catalyzes this final step? | 5-fdUMP 5 Fluoro-deoxyuridine monophosphate 5FUdr --> 5-fdUMP via thymidine kinase |
| Name the possible mechanisms associated with 5FU resistance? | 1.) Loss or decreased activity of TP or TK 2.) Increased Ts activity 3.) overexpression of MRP5/8 |
| Which drug has the unique adverse effect of causing hyperbilirubinemia? | Capecitabine |
| Which drug has the unique adverse effect of causing cholestatic jaundice? What is this drug indicated for? | Cytarabine Indicated for AML |
| Which 2 drugs have a resitance mechanism associated with decreased deoxycytidine activity and increased cytidine deaminase activity? | Cytarabine - also MRP 8 Gemcitabine - also MRP 7 |
| What is the Active form of 5FU? What enzyme catalyzes this final step? | 5-fdUMP 5 Fluoro-deoxyuridine monophosphate 5FUdr --> 5-fdUMP via thymidine kinase |
| Name the possible mechanisms associated with 5FU resistance? | 1.) Loss or decreased activity of TP or TK 2.) Increased Ts activity 3.) overexpression of MRP5/8 |
| Which drug has the unique adverse effect of causing hyperbilirubinemia? | Capecitabine |
| Which drug has the unique adverse effect of causing cholestatic jaundice? What is this drug indicated for? | Cytarabine Indicated for AML |
| Which 2 drugs have a resitance mechanism associated with decreased deoxycytidine activity and increased cytidine deaminase activity? | Cytarabine - also MRP 8 Gemcitabine - also MRP 7 |
Created by:
Jmallada7
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