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Anti-Cancer Drugs 2
Anti-Cancer Drugs 2 ( only 1/2 the lecture)
| Question | Answer |
|---|---|
| ** The Other Half of This Lec. is in aferdo01's StudyStack ** | . |
| Alkylating agents = ? | * Nitrogen mustards and Nitrosoureas |
| Nitrogen mustards ? | * melphalan --- ifosfamide |
| Nitrosoureas ? | * carmustine --- lomustine |
| Platinum compounds | * cisplatin --- carboplatin |
| *Nitrogen Mustards* .... Melphalan and Ifosfamide uses ? | * Melphalan = Ovarian cancer and multiple myeloma...... * Ifosfamide = testicular cancer |
| Nitrogen Mustard (Mel. and Ifo.) MOA = ? | * Alkylate DNA at N7 of guanine (a base) by CROSS-LINKING the cells --> apoptosis... * Unique Thing = Good in both actively dividing and resting cells ! |
| Melphalan SEs = ? | * BLACK BOX = Bone marrow suppression (dose limiting) and Hypersensitivity reactions...... * Pulmonary toxicity (cause fibrosis/pneumoitis) |
| Ifosfamide SEs = ? | * BLACK BOX = CNS toxicity, Hemorrhagic cystitis, and Nephrotoxicity (can cause renal failure)...... * TmT of Cystitis = Hydration and MESNA........ * Other tox. = dose limiting BMD, Caridotoxicity, and Pulmonary Toxicity again |
| *Nitrosoureas*.... Carmustine use ? | * UNIQUE: Can cross BBB so REALLY good for BRAIN tumors/cancers |
| Carmustine MOA = ? | * Interferes with DNA & RNA function by alkylation and cross-linking and by carbamylation of amino acids in protein...... * Simple Terms: Alkylates (messes DNA up) and Modifies Proteins (carbamylation) |
| Lomustine use = ? | * Also use in Brain tumors, but also can use for Multiple myeloma, Hodgkin's lymphoma |
| Lomustine MOA = ? | * Inhibits DNA & RNA synthesis by alkylation of DNA and carbamylation of DNA polymerase.... * Simple Terms: Modifies the DNA polymerase |
| Carmustine and Lomustine SEs = ? | * Worst DRUG for BMD ! --> thrombocytopenia and leukopenia..... * The BMD can be delayed,dose related, etc, so need to monitor it ATLEAST 6 months after a dose is given.... * CNS, renal, hepatic & pulmonary toxicity are also dose limiting |
| *Platinum complexes*.... Cisplatin use = ? | * One of the most commonly used drugs ..... * Colon in testicular, ovarian, and bladder |
| Cisplatin MOA = ? | *Water replaces chloride and Creates reactive molecule, which bind to guanine and causes inter- and intra- strand DNA crosslinks ....... * CCNS (kills in all cell cycle stages) |
| How to prevent Cisplatin toxicity ? | * Give Chloride, b/c low Cl creates a favorable environment for the drug to work --> Toxicity |
| Cisplatin ACUTE SEs = ? | * WORST Drug for N/V = High Emetic Frequency ( so give an antiemetic before)...... * BLACK BOX: Hypersensitivity / Anaphylactic-like reactions (need loaded up with -roids, antihists., or epi. before tmt to prevent this) |
| Cisplatin DELAYED SEs = ? | *pop up days --> weeks later..... * BLACK BOX: Nephrotoxicity - One of the most nephrotoxic drugs..... * BLACK BOX: Ototoxicity in KIDS (need to monitor YRS later) |
| Used to treat DELAYED SEs = ? | * Hydration with Chloride...... * Also give Amifostine |
| Carboplatin use = ? | * drug is a 2nd generation analog.....* Ovarian cancer |
| Carboplatin SEs = ? | * Same MOA as Cis..... * SEs = Less TOXIC in everything, except for BMD (dose limiting) |
| *Antimetabolites*.... Methotrexate Use = ? | * LOTS: Treatment of leukemias; lymphomas -- Breast cancer -- Lung cancer -- GVHD (prophylaxis) -- Psoriasis -- Rheumatoid arthritis |
| MTX MOA = ? | * Depletes TMP --> Prevents regenerated folate from being reactivated to be used to make the TMP..... * SIMPLE: inhibits dihydrofolate reductase (DHFR) --> low TMP for DNA synth. |
| MTX SEs = ? | * BLACK BOX: BMD (dose-limiting, GI, Hepatotoxic, Pneumonitis, Derm. issues, and Renal Issues |
| *Antimetabolites - Pyrimidine analogs*.... 5-Fluorouracil (5-FU) Use = ? | * Widely Used agent in the Tmt of Breast Cancer, Topical for Basal Cancer, and for Colorectal Cancer |
| 5-Fluorouracil MOA = ? | * Converted in target cells to 5F-dUMP (nucleobase to nucleoside to nucleotide)... * 5F-dUMP covalently binds to thymidylate synthetase with FH4 (reduced folate, which Blocks conversion of dUMP to TMP...* Leads to cell death by depleting TTP |
| 5-FU can also ? | * Also converted to FdUTP and FUTP, which Inhibits DNA & RNA synthesis.... * Unique bc this drug can inhibit BOTH RNA and DNA..... * Also, it is a suicide inhibitor = binds permanently |
| 5-FU SEs = ? | * Classic Anti-Cancer SEs, nothing major.... * GI, BMD, N/V |
| Gemcitabine Use = ? | * breast, non-small cell lung, pancreatic, ovarian cancer... * Nothing Big stands out |
| Gemcitabine MOA = ? | * Is a Deoxycytidine analog (phosphorylated to mono-, di-, and triphosphate)...... * inhibits ribonucleotide reductase = lowers dNTPs (lowers diphospahtes).... * inhibits DNA polymerase ..... * incorporates into DNA (chain termination) |
| Gemcitabine SEs = ? | * Toxicity – Myelosuppression (neutropenia) (dose limiting) |
| *Hydroxyurea* Use = ? | * Lots.... * Melanoma, chronic myelocytic leukemia (CML), ovarian cancer; management of sickle cell patients |
| Hydroxyurea MOA = ? | * Inhibits ribonucleotide reductase... * Inhibition results in depletion of intracellular dNTP pools leading to inhibition of DNA synthesis |
| Hydroxyurea SEs = ? | * BLACK BOX: Developing a Secondary Malignancy...... * Myelosuppression (dose limiting)..... * Cutaneous Vasculitic issues (look like ulcers on the body) |
Created by:
thamrick800
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