Term
| Myelosuppressive tx drug list |
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Definition
| Epoetin alfa Filgrastim Leucovorin Oprelvekin Sargramostim |
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Term
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Definition
Busulfan
Carboplatin
Carmustine (BCNU)
Chlorambucil
Cisplatin
Cyclophosphamide
Lomustine (CCNU)
Mechlorethamine
Melphalan
Procarbazine
Temozolamide
Thiotepa |
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Term
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Definition
5FU
6MP
6TG
Azacitidine
Capecitabine
Cytarabine (araC)
Gemcitabine
Methotrexate |
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Term
| Antibiotic (antineoplastic) drug list, S/E |
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Definition
Bleomycin
Dactinomycin
Doxorubicin
MitomycinC
Usually myelosuppression (not bleomycin!) |
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Term
| Epipodophyllotoxic drug list |
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
| Miscellaneous cancer drug list |
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Definition
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Term
| Cancer is characterized by... |
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Definition
Uncontrolled cell proliferation including decreased apoptosis
decreased differentiation
invasion
metastasis |
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Term
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Definition
| Rapidly dividing cells including normal, noncancerous cells (GI, hair) |
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Term
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Definition
G0: resting, differentiation
G1: getting ready for DNA synthesis (synthesizing necessary compounds), 18-30h
S: DNA replication and repair (doubling of chromosomes), 16-20h
G2: getting ready for mitosis (synthesizing necessary compounds), 2-10h
M: mitosis, 30min-1h |
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Term
| Cell cycle nonspecific (CCNS) drug characteristics |
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Definition
Alkylating agents (guanine N7, O6) = intercalate/cross-link DNA (if have 2 reactive groups) or make ssDNA breaks (if have 1 reactive group), misreading of DNA and inhibition of synthesis of everything,
Kills G1 and S cells best b/c nucleotides become unpaired and are susceptible to alkylation
Toxicity expressed as cells enter S
Can kill at any phase (works in G0 due to the background DNA repair)
Killing is dose/concentration dependent = give in 1 big dose (like gentamicin) |
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Term
| Radiation "works" because... |
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Definition
Normal cells can efficiently and effectively repair the damage overnight
Cancer cells can't repair the damage as quickly or as well |
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Term
| Doxorubicin: CCNS/CCS, class, MOA |
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Definition
CCNS
Antibiotic (anthracycline)
Intercalates, inhibits TopoII, DNA strand scission = single and double strand breaks, cells die in G2 |
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Term
| CCNS drug list (most are alkylating agents) |
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Definition
Busulfan
Carboplatin
Carmustine (BCNU)
Chlorambucil
Cisplatin
Cyclophosphamide
Dactinomycin
Doxorubicin
Lomustine (CCNU)
Mechlorethamine
Melphalan
MitomycinC
Procarbazine
Temozolamide
Thiotepa
Topotecan |
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Term
| Cell cycle specific (CCS) drug characteristics |
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Definition
Kill in specific phases of cell cycle (obvi)
Killing is time/exposure dependent = regular, small doses (like PCN)
Most effective in hematologic cancers and tumors with lots of cells in the "growth fraction" |
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Term
| G1 phase drugs and phys. effects |
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Definition
Corticosteroids
Suppress mitosis, cause apoptosis in non-dividing cells |
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Term
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Definition
Antimetabolites = structural analogs of naturally occuring basis for DNA/RNA synthesis = 5FU, 6MP, 6TG, azacitidine, capecitabine, cytarabine, gemcitabine, hydroxyurea, methotrexate
Usually myelosuppressive |
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Term
| 5FU, capecitabine: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Inhibits thymidylate synthase |
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Term
| 6MP, 6TG: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Inhibits purine (A, G) synthesis |
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Term
| Methotrexate: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Inhibits DHF reductase |
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Term
| Cytarabine: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Inhibits DNA polymerase |
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Term
| Azacitidine: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Incorporated into DNA, RNA |
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Term
| Hydroxyurea: CCNS/CCS, class, MOA |
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Definition
CCS S phase
Antimetabolite
Inhibits ribonucleotide reductase |
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Term
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Definition
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Term
| Bleomycin: CCNS/CCS, class, MOA |
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Definition
CCS G2 phase
Antibiotic
O2 free radicals fragment DNA, cells accumulate in G2 |
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Term
| Etoposide: CCNS/CCS, class, MOA |
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Definition
CCS G2 phase
Epipodophyllotoxin
Stabilizes the topoisomerase II-DNA bond, topoII is inhibited, dsDNA breaks remain (b/c topoII also rejoins dsDNA) |
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Term
| Late G2(/early M) phase drug list |
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Definition
| Vinca alkaloids/"spindle poisons" = vinblastine, vincristine |
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Term
| Vincristine, vinblastine: CCNS/CCS, class, MOA |
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Definition
CCS late G2(/early M) phase
Vinca alkaloid/"spindle poison"
Bind to tubulin, prevent microtubule assembly, mitotic filaments can't form, cells arrest in late G2 |
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Term
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Definition
Paclitaxel
(Vinblastine
Vincristine) |
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Term
| Paclitaxel: CCNS/CCS, class, MOA |
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Definition
CCS M phase
Taxane
Enhances polymerization of tubulin, promotes microtubule assembly and stabilizes them against depolymerization, loss of dynamic instability, anaphase can't happen, mitotic arrest
Phosphorylates BCL2, turns it off, restores apoptosis |
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Term
| Normal rapidly proliferating tissues, S/E from chemo collateral damage |
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Definition
Bone marrow: myelosuppression
GI mucosa: n/v, stomatitis
Hair follicles: alopecia (regrowth), post-radiation therapy (no regrowth)
Ovary/testis: amenorrhea/azoospermia |
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Term
| Myelosuppression consequences |
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Definition
Anemia
Hemorrhage
Infections, fever
Leukopenia (neutropenia) |
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Term
| Drug for myelosuppressive anemia |
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Definition
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Term
| Drug for myelosuppressive hemorrhage |
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Definition
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Term
| Oprelvekin (IL11): class, MOA |
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Definition
Myelosuppression tx
Megakaryocyte growth factor to counter thrombocytopenic hemorrhage |
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Term
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Definition
Myelosuppression tx
Granulocyte-CSF to counter leukopenic/neutropenic infection |
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Term
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Definition
Myelosuppression tx
Granulocyte-macrophage-CSF to counter leukopenic/neutropenic infection |
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Term
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Definition
Neutrophil count <1000
Recovery can be rapid (14-21 days) or delayed (50+ days) |
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Term
| Leucovorin (rescue): class, MOA |
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Definition
Methotrexate myelosuppression tx
Normal cells take up the drug and use it for THF synthesis, tumor cells can't take it up |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Doxorubicin (anthracyclines) |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
| Drugs toxic to skin, nails |
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Definition
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Term
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Definition
Carmustine
Cisplatin
Mechlorethamine
MitomycinC
Thiotepa |
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Term
| p.o. alkylating agents (BuChCy LoMe PrTe) |
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Definition
Busulfan
Chlorambucil
Cyclophosphamide
Lomustine
Melphalan
Procarbazine
Temozolamide |
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Term
| Alkylating agent toxicity |
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Definition
Dose-limiting: myelo- and immunosuppresion
N/V within 30-60min of tx (pretreat with 5HT3 blockers)
Secondary leukemias (AML)
Amenorrhea/azoospermia
Hepatic veno-occlusive disease (HVOD, b/c obliterates small hepatic vein branches), portal htn, esophageal varices, rupture, internal bleeding, death
PF with busulfan, chlorambucil, melphalam, nitirosureas = carmustine and lomustine |
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Term
| Drugs used to tx heme-onc and solid tumors (usually in combination with other drugs) |
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Definition
| Alkylating agents = busulfan, carboplatin, carmustine, chlorambucil, cisplatin, cyclophosphamide, lomustine, mechlorethamine, mephalan, procarbazine, temozolamide, thiotepa |
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Term
| Cyclophosphamide toxicity |
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Definition
Myelo-, immunosuppression (used in organ transplantation)
n/v
Non-hemorrhagic and hemorrhagic cystitis (b/c concentrates in urine so need adequate hydration/urination)
SIADH (b/c of the hydration/urination) |
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Term
Hematuria but no WBCs in the urine
I should be thinking... |
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Definition
| Cyclophosphamide toxicity |
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Term
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Definition
Injected into urinary bladder to tx superficial bladder cancers, the peritoneal cavity, and the CSF to tx CNS metastases
(BCG = bovine TB also used for the superficial bladder cancers b/c stimulates the immune system to come and fight the cancer) |
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Term
| Busulfan: application, method of admin, S/E |
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Definition
Kill bone marrow for marrow transplant
p.o.
Bronze hyperpigmentation, HVOD, PF, pseudo-Addison's |
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Term
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Definition
Carmustine
Lomustine
Temozolamide for primary and secondary, doesn't need bioactivation
All of these cross the BBB |
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Term
| Procarbazine: CCNS/CCS, class, MOA, method of admin |
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Definition
CCNS
Alkylating agent
Inhibits synthesis of everything, causes chromosomal breaks
p.o. |
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Term
| Cisplatin, carboplatin: method of admin, S/E |
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Definition
IV
n/v! (have to pretreat with 5HT3 blocker + dexamethasone)
Nephrotoxic, more so than carboplatin! (Peri-admin saline to decrease this)
High-frequency hearing loss
Sensory neuropathy |
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Term
| If something is super-emetic, that's because it... |
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Definition
| Kills enterochromafin cells, release 5HT3, serotonin syndrome |
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Term
| Gold standard for anti-emesis |
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Definition
| Dexamethasone but don't know why |
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Term
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Definition
Myelosuppression (rescued with leucovorin)
Nephrotoxic: excreted unchanged, sulfa drugs/NSAIDs/COX2 inhibitors decrease its renal clearance, insoluble in acidic urine so large doses can cause ppt in renal tubules (prevent with hydration and alkaline urine)
Other: mucositis, hemorrhagic enteritis, transient increase in LFTs (chronic tx small doses for arthritis can lead to hepatic fibrosis)
Intrathecal injection cause cause arachnoiditis = stiff neck, headache, fever |
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Term
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Definition
Antimetabolites (not methotrexate) = 5FU, azacitidine, capecitabine, cytarabine, gemcitabine
Usually myelosuppression (not cytarabine!) |
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Term
| 5FU: application, MOA, method of admin, S/E |
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Definition
Actinic keratoses, basal cell cancers
Its metabolite FdUMP irreversibly inhibits thymidylate synthetase, lack of thymidylate, blocks DNA synthesis
Topical, IV
Myelosuppression, photosensitivitiy, hyperpigmentation, diarrhea, hand-foot syndrome (eryhtematous desquamation) |
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Term
| Capecitabine: MOA, method of admin, S/E |
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Definition
Converted to 5FU by cells' thymidine phosphorylase (>>>in tumor cells)
Oral
Less toxic than IV 5FU |
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Term
| Cytarabine: application, MOA, method of admin, S/E |
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Definition
AML
Incorporated into DNA/RNA, inhibits DNA pol
IV, subcu
Conjunctivitis, jaundice, reversible cerebellar toxicity |
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Term
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Definition
Inhibits DNA methyltransferase, no methylation to turn off tumor suppressor genes = tumor suppressor genes stay on
Myelosuppression |
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Term
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Definition
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Term
| 6MP, 6TG: MOA, method of admin, S/E |
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Definition
HGPRT converts it to active form, inhibit purine nucleotide pathway enzymes, inhibit synthesis of everything
p.o.
Myelosuppression
6MP: allopurinol inhibition of xanthine oxidase inhibits degradation of 6MP |
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Term
| Bleomycin: method of admin, S/E |
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Definition
| IV, IM, subcu No myelosuppression! Pulmonary fibrosis Lethal ananphylaxis, esp. in lymphoma pt |
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Term
| Dactinomycin: MOA, method of admin, S/E |
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Definition
Intercalates in DNA, RNA synthesis can't proceed
IV
Myelo- and immunosuppresion, radiation "recall" |
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Term
| Doxorubicin: application, S/E |
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Definition
Carcinomas, sarcomas, heme cancers
Chronic heart failure, cumulative dose-related
Short-term myelosuppression |
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Term
| Etopside: method of admin, S/E |
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Definition
IV
Dose-limiting myelosuppresion, anaphylaxis, secondary leukemias |
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Term
| Topotecan: CCNS/CCS, class, MOA |
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Definition
CCNS
Camptothecin
Inhibit topoI, DNA damage |
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Term
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Definition
| Myelosuppression, some diarrhea |
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Term
| Vincristine, vinblastine: method of admin, S/E |
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Definition
IV
Vincris: dose-limiting neurotoxicity: loss of tendon reflexes, paresthesias, autonomic dysfunction
Little myelosuppression!
Vinblas: dose-limiting myelosuppression |
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Term
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Definition
| Myelosuppression, peripheral neuropathy, myalgias |
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Term
| Hydroxyurea: application, method of admin, S/E |
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Definition
SCD: turns on HbF gene
p.o.
Myelosuppression |
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