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Oncodrugs
Oncology drugs of interest for 3rd year Pharmacology course
| Question | Answer |
|---|---|
| R-CVP drug combo stands for? | Rituximab Cyclophosphamide Vincristine (aka Oncovin) Prednisolone |
| BEACOPP drug combo stands for? | Bleomycin Etoposide Adriamycin Cyclophosphamide Oncovin (aka Vincristine) Procarbazine Prednisolone |
| DHAP drug combo stands for? R-DHAP is? | (R in R-DHAP is Rituximab) DexametHasone Ara C (aka cytarabine) cisPlatin |
| Rituximab MOA? | Non-cell cycle specific - Chimeric Monoclonal Antibody against CD20 which is found mainly on B-Cells. Used in lymphomas and leukaemias. |
| Cyclophosphamide MOA? | Cell cycle specific Mustard Alkylating agent Prodrug - Adds Alkyl group to Guanine on DNA. Used in Hodgekin's Lymphomas and B-Cell lymphomas. |
| Vincristine (aka Oncovin) MOA? | Cell cycle specific - Mitotic inhibitor - binds to Tubulin dimers preventing polymerisation onto Actin microtubules. Used In B-Cell lymphomas and Hodgekin's Lymphomas |
| Alkylating agents | #Cell cycle specific |
| Prednisolone/Prednisone MOA? | #Prednisone is prodrug of Prednisolone(via liver) - Immunosuppression??against side effects?? Used in Hodgekin's Lymphoma and B-Cell Lymphomas |
| Bleomycin MOA? | Antitumour antibiotic - binds to DNA, forms Fe2+ complex(pseudoenzyme) to produce superoxide free radicals and thus DNA & protein damage. Used in Hodgekin's Lymphoma |
| Etoposide MOA? | Inhibits topoisomerase II to cause strand breakage leading to apoptosis. Used in Hodgekin's Lymphoma. |
| Adriamycin(aka Doxorubicin) MOA? | Antitumour antibiotic. Intercalation with DNA, binds to 2 bases and pushes structure through the chain. DNA cannot be read, blocks polymerase and topoisomerase activity. Used in Hodgekin's Lymphoma |
| Procarbazine MOA? | #Alkylating agent- Prodrug thats activated in liver to yield azo-procarbazine & hyrogen peroxide- used in Hodgekin's lymphoma |
| Dexamethasone MOA? | Used against oncopharm side effects, amplifies 5HT3 antagonism(i.e. ondansetron). Useful against onco-caused oedema. |
| Cytarabine(aka Ara-C) MOA? | Pyrimidine Analogue- blocks DNA strand elongation & by having an upside down -OH group on C-2, meaning the next phosphate cannot bind and the DNA chain terminates- cycle specific - inhibits reduction of CDP & dCDP |
| Cisplatin MOA? | [2Cl 2NH3 Pt] Metal-based Alkylating agent- performs intra & inter-strand crosslinking & DNA-protein cross-linking. NH3 groups bind onto 2 parallel guanines & proteins becomes bound. DNA cannot be used and causes apoptosis. Can cross cell membranes & B |
| Ifosfamide MOA? | Alkylating agent Prodrug: P450s add -OH and open ring that can then passively degrade into 4 alkylating & DNA/protein damaging chemicals including Acrolein |
| Cancer chemo drug classes? | Non-specific cytotoxics Antimetabolites Steroidal/hormonal Asparagine Immunotherapy |
| Fludarabine MOA? | #2-fluoro-adenine arabinoside #Performs both the purine & pyrimidine axis of effects |
| Antimetabolite subclasses | Antifolates Pyrimidine analogues Purine analogues |
| Non-specific cytotoxics subclasses | Alkylating agents Antitumour antibiotics (inc Anthracyclines) Misc |
| Name some Alkylating agents | Cyclophosphamide Ifosphamide Lomustine Chlorambucil Melphalan Uramustine Oestramustine Procarbazine Dacarbazine Altretamine Cisplatin Carboplatin |
| Name some Antitumour antibiotics | Anthracyclines Actinomycin Bleomycin Doxorubicin (Adriamycin) |
| Name some Pyrimidine Antimetabolites | 5-FdUMP (5-fluoro-deoxy-Uracil monophosphate) Tegafur-Uracil (Tegafur = 5-FU prodrug) Cytarabine (Ara-C/Cytosine Arabinoside) |
| Name some Purine Antimetabolites | 6-Thioguanine(6-TG) Mercaptopurine |
| General antimetabolite resistance mechanisms? | Reduced drug uptake (i.e. HGPRT deletion for 6-Thioguanine) Increased metabolising enzyme expression(i.e. Ara-C deamination-inert) More disseminating target enzymes (polymerases) Low levels of cofactors(i.e. folate) |
| 6-Thioguanine (6-TG) MOA? | Purine antimetabolite. Similar to Mercaptopurine. Contains sulphur double bonded. Looks like guanine- HPRT adds ribose & phosphate - incorporated into DNA. Cannot be methylated leading to continual single strand breaks and thus to cell stress & apoptosi |
| Mercaptopurine | Purine antimetabolite. Similar to 6-TG- contains sulphur double bonded. HPRT adds ribose. Phosphate added. Incorporated into DNA. Cannot be methylated, causes strand breaks leading to cell stress & apoptosis. Used in Non-Hodgekin's Lymphoma. |
| Hormonal therapy drug classes? | SERMs(Selective Estrogen Receptor Modulators) SERDs(Selective Estrogen Receptor Down-regulators) Aromatase Inhibitors |
| Why can Tamoxifen cause endometrial cancers? | It has estrogen agonism in the endometrium |
| SERM subclasses? | Tamoxifen-like 'Fixed-ring' compounds |
| List some Tamoxifen-like SERMs | Toremifene Droloxifene Idoxifene |
| List some 'fixed-ring' SERMs | Raloxifene Arzoxifene EM-800 |
| Which are supposedly better and why? Tamoxifen-like or Fixed-ring SERMs. | Fixed-ring SERMs because: -No agonism in endometrium -Agonism in bone -Potent antiestrogens in breast |
| Why is estrogen receptor agonism a good thing in bone? | Prevents bone dimineralisation |
| Tamoxifen for what? MOA? And why is it a poor drug? | Breast Cancer Estrogen receptor competitive antagonism. Allows dimers to form, only deactivates AF2 ER site- ER is agonised & can bind DNA and bind AF1 cofactor. |
| Goserelin for what? MOA? | Pre-menopausal Breast Cancer. GnRH antagonism at anterior pituitary. Also used in reproductive assistance. |
| SERMs for what? MOA? | Breast cancer. Estrogen receptor antagonism. |
| SERDs for what? MOA? | Breast cancer. Estrogen receptor antagonism and down-regulation. |
| Why does antiestrogenic activity cause apoptosis? | Cell goes into mitogenic crisis. |
| What breast cancers cant Estrogen receptor antagonists treat? | Estrogen receptor negative tumours (dedifferentiated / progressed) |
| How does a temporary tumour flare occur after oestrogen antagonism? | In response to ACTH & LH/FSH output which increases oestrogen output. Oestrogen normally negative feedbacks their release. Fades once system has worked round. |
| List some SERDs | Fulvestrant, SR-16234, ZK-191703 |
| Aromatase Inhibitors for what? MOA? | #Aromatase converts androgens to estrogens |
| List some Aromatase inhibitors | Anastrozole Aminoglutethimide |
| What is 'additive hormonal manipulation' for? | Used in addition to the primary hormonal therapy. Reduce oestrogen secretion/synthesis. Can have sterility or masculinising effect. |
| List some 'additive hormonal therapies' | GnRH agonists- Goserelin, Leuprorelin Androgens- Calusterone |
| CMF drug combo is what? | Cyclophosphamide Methotrexate 5-FU |
| Methotrexate MOA? | Folic acid analogue. Inhibits dihydrofolate reductase (DHFR) which converts dihydrofolate (folic acid derivative) to tetrahydrofolate which is necessary for DNA synth |
| Plant Alkaloid classes? | Microtubule inhibitors Topoisomerase inhibitors |
| Antimetabolite classes? | Antifolates Pyrimidine antagonists |
| Microtubule inhibitor targets | Mitotic spindle Skeletal spindle Polymerised/depolymerised balance disruption |
| Microtubule inhibitor subclasses | Vinca Alkaloids Taxanes |
| List some Vinca Alkaloid Microtubule inhibitors | Vincristine Vinblastine Vinorelbine |
| Vinca Alkaloid Microtubule inhibitors MOA? | Cell-cycle dependent. GTP-dependent binding to tubulin- blocks further polymerisation. Dysfunctional spindle apparatus frozen in metaphase leading to apoptosis. |
| Plant alkaloid (microtubule/ topoisomerase inhibitor) resistance mechanisms? | P-glycoprotein mediated efflux Altered tubulin or enzyme structure |
| Microtubule inhibitor adverse effects? | Hyperuricaemia (use allopurinol) N/V/D Alopecia Extravasation Vinblastine - potent myelosuppression Vincristine - peripheral neuropathy |
| List some Taxane Microtubule inhibitors | Paclitaxel Doxetaxel |
| Taxane Microtubule inhibitors for? | Advanced ovarian & metastatic breast cancer |
| Taxane microtubule inhibitors MOA? | Bind reversibly to tubulin to cause stabalisation (instead of inhibition). Unusually stable Tubulin fails to depolymerise after metaphase. Leads to apoptosis. |
| Taxane microtubule inhibitor adverse effects? | Serious hypersensitivity- premed with dexamethasone/ diphenhydramine Neutropenia Peripheral Neuropathy Alopecia Bradycardia |
| Topoisomerase inhibitor subclasses? | Camtothecins Podophyllotoxin analogues (mandrake plant) |
| List some Podophyllotoxin analogue topoisomerase inhibitors | Etoposide Teniposide |
| Podophyllotoxin analogue topoisomerase inhibitors MOA? | Cell cycle specific. Target mainly topoisomerase II- drug binds enzyme-DNA complex, while maintaining transiently cleavable form- remains in cleavable form. DNA strands break. |
| Podophyllotoxin analogue Topoisomerase inhibitor uses? | Oat cell lung carcinoma Refractory testicular carcinoma |
| Topoisomerase inhibitor adverse effects? | Myelosuppression N/V Alopecia Anaphylaxis Hypotension |
| Camtothecin topoisomerase inhibitor MOA? | Inhibit topoisomerase I (cuts/ religates STRANDED DNA). |
| List some Camtothecin topoisomerase inhibitors and their uses | Toptecan- Ovarian cancer Irinotecan- 5-FU resistant colorectal cancer |
Created by:
seeriktus
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