DIT cancer drugs (only on things specific to the drugs) Flashcards
Methotrexate mechanism?
S phase specific antimetabolite
Just like trimethoprim. DHF analog so no THF recharged and available for dUMP to dTMP
What is leucovorin?
Folic acid, basically. Used for helping fix myelosuppression from methotrexate
won’t save 5FU
5 Flurouracil mechanism?
Pyrimidine analogue.
activated to 5F-dUMP to covaenlty bind folic acid and no thymidylate synthase activity
no dTMP and no DNA
Basal cell skin cancer and actinic keratosis treated with what?
5-FU
What is uridine?
Rescue for 5FU when myelosuppression
What 6-mercaptopurine?
purine analog, obviously. inhibits purine synthesis
What is significance of 6 mercaptopurine metabolism?
xanthine oxidase. So more toxicity if patient is on allopurinol
What is 6-thioguanine?
works like 6 mercaptopurine except not metabolized by xanthine oxidase
can be given with allopurinol
What is cytarabine?
CyTarabine is a pyrimidine analogue (C and T). it inhibits DNA polymerase
(its like acyclovir or rifampin, but for human DNA!)
Mechanism of cyclophosphamide?
covalently cross link DNA so cell can’t replicate
Guanine specifically
what cancer drug can cause hemorrhagic cystitis? It also causes increased risk of bladder cancer (TCC).
how do you prevent it?w
KNOW THIS
cyclophosphamide b/c acrolein is toxic metabolite
Prevent with mesna
What are the nitrosoureas? What is the mechanism?
What is important about them?
What is the mnemonic?
Put nitro in your mustang! (mustines)
Carmstine, lomustine, semustine, streptozocin
alkylating agent. Needs bioactivation. BUT CAN CROSS BBB.
cross links DNA
Toxicity of nitrosoureas?
Crosses BBB so CNS tox
What is the mechanism of busulfan?
side effect?
X links DNA (alkylating agent again)
Pulmonary fibrosis is side effect (and busulfan tan but whatever)
Mechanism of rubicins?
generate free radicals
also intercalate DNA and causes breaks!
Side effect of rubicins?
CArdiotoxic (dilated cardiomyopathy) and heart failure
heart muscle susceptible b/c low levels superoxide dismutase. Rubicins make oxidative radicals
What is dexrazoxane?
Iron chelating agent that prevents cardiotoxicity of the rubicins?
What is mechanism of dactinomycin?
Intercalates DNA
What anticancer drug is used in pediatric cancers a lot?
Mnemonic
Dactinomycin
Children ACT out! dACTinomycin
Bleomycin mechanism?
Free radical formation which causes DNA to break (BLeo BLasts DNA)
Side effect of bleomycin?
Pulmonary fibrosis (same as busulfan, easy to remember b/c start with B’s)
Methotrexate can cause fibrosis too
What three anticancer drugs cause pulm fibrosis?
Busulfan, bleomycin and methotrexate
What is a adriamycin?
It is a poor named rubicin
The platinum containing anti caner drugs work how?
Cross linkDNA. they are the ___platins
What cancer drugs have genitourinary association?
What is the bonus toxicity?
Platins are for treating testicular, ovarian and bladder cancer
But nephrotoxic also ototoxic
What drugs are nephrotoxic and ototoxic? 4 categories
Vanco
__platins
aminoglycosides
loop diuretics
What does Etoposide and teniposide work on?
Etoposide and Teniposide inhibit topo 2 (which unwinds DNA upstream
Step 1 likes testicular cancer (thats fucked up). What is a common regimen for treatment? mnemonic
Eradicate Ball Cancer
Etoposide
Bleomycin (or Ifosfamide)
Cisplatin
Mechanism for ironotecan and topotecan?
Inhibit topo1.
Diarrhea
Vincristine and vinblastine work how?
side effect?
Block polymerization of microtubules
Neuro toxicity. vinBLASTINE blasts bone marrow
Paclitaxel and taxels mechanism?
Hyperstabalize (TAXing to keep them polymerized)
Drugs that stabilize microtubules? not all cancer drugs
Microtubules G C very poorly
Mebendazole griseofulvan colchicine Vincristine/blastine paclitaxel
KNOW!
Mechanism of hydroxyurea?
Inhibtis ribonucleotide reductase
Prednisone mechanism as anti cancer drug?
May trigger apoptosis
especially lymph stuff (makes sense since immunosuppressant)
Mnemnoic for side effect of prednisone?
BAM CUSHINGOID
Buffalo hump amenorrhea moon facies crazy (psychosis) ulcers skin changes (acne) htn (aldosterone agonism) infection necrosis of femoral head glaucoma/cataracts osteoporosis immunosuppression diabetes
Tamoxifen mechanism?
SERM
estrogen receptor affect
Antagonist in breast
Agonist in bone and partial agonist in endometrium
ER breast cancer
Can prevent breast cancer if BRCA
increased risk of endometrial carcinoma (b/c overstimulation), but it stimulates less than estrogen, so helps there too. weird
Rolixefene mechanism?
SERM
Estrogen antagonist in breast and endometrium
Agonist in bone.
USED FOR OSTEOPOROSIS
Mechanism of trastuzumab?
Toxicity?
Her2 tyrosinekinase receptor monoclonal antibody for it
The trastuzumab trashy whore hurt my heart. CARDIOTOXIC
Rituxumab mechanism?
anti CD20
can help with lymphoma, leukemia, RH arthritis..
Imatinib mechanism?
nib means inhibitor, not monoclonal antibody
It is for BCR-ABL tyrosine kinse in (and if philly chromosome is anywhere else)