Save
Busy. Please wait.
Log in with Clever
or
show password
Forgot Password?
Don't have an account?  Sign up 
Sign up using Clever
or
Username is available taken
show password


Make sure to remember your password. If you forget it there is no way for StudyStack to send you a reset link. You would need to create a new account. Your email address is only used to allow you to reset your password. See our Privacy Policy and Terms of Service.

Already a StudyStack user? Log In

Reset Password
Enter the associated with your account, and we'll email you a link to reset your password.
focusNode
Didn't know it?
click below
 
Knew it?
click below
Don't Know
Remaining cards (0)
Know
0:00
edit
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.

  Normal Size     Small Size show me how

Anti-cancer

Anti-cancer medications

TermDefinition
What is the MoDA of aminopterin? Folic acid analogue -> competes for DHFR folate binding site -> blocks tetrahydrofolate synthesis -> inhibit DNA/RNA/protein synthesis
What drugs are nitrogen mustards? Melphalan, cyclophosphamide
What is the MoDA of nitrogen mustards? 2 chloroethyl side chains -> covalently link alkyl group to nucleic acid/protein chemical moieties -> inter/intrastrand DNA cross-linking -> strand scission due to endonuclease attack in attempt to repair alkylated DNA -> inhibit DNA/RNA synthesis
What is the clinical use of melphalan? Nitrogen mustards -> DNA inter/intrastrand crosslinking via alkylation -> Phe precursor -> L-phenylalanine mustard -> Phe accumulated in melanomas (melanin precursor) -> relatively selective drug
What is the clinical use of cyclophosphamide? Nitrogen mustards -> DNA inter/intrastrand crosslinking via alkylation -> broad application for lymphoid tumours, breast/lung/ovary/endometrium carcinomas -> good oral absorption (liver CYP450) -> immunosuppressant (dangerous long-term)
What drugs are nitrosoureas? What is their MoDA, clinical usage and pharmacokinetics? Lomustine, carmustine, semustine -> alkylating/carbamolyating agents -> interstrand crosslinks -> long CH2 chains -> hydrophobic -> pass through BBB -> effective for brain tumours -> don't need CSF delivery -> oral administration
What is the MoDA of mitomycin C? Alkylates DNA at G -> interstrand cross-linking -> prevent strand separation during DNA replication/transcription
What is the MoDA of cisplatin? DNA intrastrand cross-linking -> binds to 2 neighbouring guanines -> major bending of DNA -> physical block of Pt adduct on template strand -> inhibits DNA Pol -> inhibit DNA replication
What are the side effects and idiosyncracies of cisplatin? Nephrotoxic, neurotoxic, transplatin is ineffective
What is the MoDA of doxorubicin and daunorubicin? Anthracycline -> hydroxyguinone moiety -> generates free radicals -> attack DNA/induce DNA cleavage/lipid peroxidation in cardiac tissue
What is the MoDA of mitoxantrone? Anthracycline analogue w/ modified structure -> type II Topo inhibitor
What drugs are anthracyclines? Doxorubicin/daunorubicin, mitoxantrone -> damage DNA by non-covalent intercalation -> inhibit type II Topo
What is the MoDA of methotrexate? Inhibits DHFR -> similar to bacterial trimethoprim, similar to protozoa pyrimethamine -> compete w/ folic acid for active transport into mammalian cells
What is the MoDA of leucovorin? Salvage normal tissues from folate depletion -> readily converted to other reduced folic acid derivatives (doesn't require DHFR) -> allows some pyrimidine synthesis even w/out DHFR -> selective for normal cells w/out high tetrahydrofolate requirement
What is the MoDA of 5-fluorouracil? dUMP analogue -> pyrimidne antagonist -> incorporated into rRNA/mRNA/DNA -> disrupt further transcription/translation -> FdUMP inhibition of thymidylate synthetase -> cytotoxic
What is the MoDA of 6-mercaptopurine? Hypoxanthine/guanine analogue -> purine antagonist -> activated and incorporated into nucleic acids -> nt synthesis inhibition
What is the MoDA of etoposide? Eukaryotic type II Topo inhibitors -> stabilise DNA breaks -> cel lrepair machinery overwhelmed -> cell death
What is the MoDA and clinical use of camptothecins and topotecan? Mammalian type I Topo inhibitors -> inhibit DNA replication/transcription -> treat ovarian cancer
What is the MoDA of vinblastine and vincristine? Bind free tubulin dimers -> prevent microtubule assembly -> interfere w/ cell cytoskeleton
What drugs are vinca alkaloids and what are their side effects? Vinblastine and vincristine, neurotoxic -> cannot be given intrathecally into CSF -> must be given IV
What is the MoDA of paclitaxel? Disrupts eqbm btwn free tubulin dimers/microtubules -> shifts to assembly -> stabilisation of ordinary cytoplasmic microtubules/formation of abnormal microtubule bundles -> interfere w/ cell cytoskeleton
What is the MoDA of colchicine? Immunosuppressant -> treat gout -> affect tubulin formation in immune cells, treat MI -> clear leucocytes preventing unhelpful fibrosis response
What is the MoDA of tamoxifen? Anti-oestrogen -> binds to oestrogen receptor w/ lower affinity -> translocated to nucleus -> decrease transcription of oestrogen-responsive genes for breast cancer development/growth
What is the MoDA of toremifene? Tamoxifen analogue (anti-oestrogen) w/out agonist side effects (oestrogen effects in other tissues - bone/uterus) -> competitive inhibitor
What is the MoDA of anastrozole? Aromatase inhibitor -> prevent peripheral androgen conversion to oestradiol -> prevent signalling to oestrogen-driven breast cancer -> treat oestrogen-dependent breast cancer in post-menopausal women
What is the MoDA of goseraline? Synthetic GnRH analogue -> tonic signalling reduces LH production via -ve feedback -> no testosterone synthesis -> treat prostate cancer
What is the MoDA of flutamide? Anti-androgen antagonising endogenous nuclear receptors -> prevent testosterone binding to receptors -> treat prostate cancer
What is the MoDA of prednisone? Converted to prednisolone by liver enzymes -> bind to GR -> translocated to nucleus -> cancer cells commit suicide/anti-inflammatory cytolysis against lymphocytes -> effective against leukaemias
What is the MoDA of rituximab? Humanised mAb against CD20 -> transformed B cells in Hodgkin's lymphoma -> ADCC/complement/apotosis
What is the MoDA of trastuzumab? Humanised mAb against constitutively active HER2 -> prevent xcs mTOR/MAPK signalling -> prevent cell cycle progression from increase in p27 -> treat human breast cancers
What is the MoDA and side effects of bevacizumab? Humanised mAb against VEGF -> treat metastatic colorectal cancer -> antiangiogenic interferes w/ wound healing -> increased risk of bleeding/GI perforation
What is the MoDA of cetuximab? Human/mouse chimeric mAb against EGFR -> reduce signalling
What is the MoDA and side effects of gefitinib/erlotinib? Small molecule inhibitor of EGFR-associated Tyr K -> binds to ATP-binding site -> blocks dimerisation -> cannot autophosphorylate/set off signalling cascade -> treat advanced non-small cell lung cancer -> skin rashes, diarrhoea
What is the MoDA of imatinib mesylate? Inhibits constitutive Bcr-Abl protein K activity -> treat CML
What is the MoDA of mastinib? Inhibit c-kit Tyr K activity -> overexpressed in patients w/ GI stromal tumours
What is the MoDA of rapamycin? Small molecule inhibitor of checkpoint protein K -> mTOR -> inhibit cell proliferation
Created by: vykleung
Popular Pharmacology sets

 

 



Voices

Use these flashcards to help memorize information. Look at the large card and try to recall what is on the other side. Then click the card to flip it. If you knew the answer, click the green Know box. Otherwise, click the red Don't know box.

When you've placed seven or more cards in the Don't know box, click "retry" to try those cards again.

If you've accidentally put the card in the wrong box, just click on the card to take it out of the box.

You can also use your keyboard to move the cards as follows:

If you are logged in to your account, this website will remember which cards you know and don't know so that they are in the same box the next time you log in.

When you need a break, try one of the other activities listed below the flashcards like Matching, Snowman, or Hungry Bug. Although it may feel like you're playing a game, your brain is still making more connections with the information to help you out.

To see how well you know the information, try the Quiz or Test activity.

Pass complete!
"Know" box contains:
Time elapsed:
Retries:
restart all cards