Principles and definitions + alkylating agents Flashcards
What is growth fraction?
cytotoxic drugs are more effective against tumors that have high growth fraction(high turn over rate). Normal cells with high growth fraction, e.g. bone marrow, will show more side effects from chemo therapy.
What is the Log-kill hypothesis?
A fixed percentage of tumor cells that are killed from a certain anticancer drug.
Where do we use drugs with cell-sycle specificity?
In cancers with high growth fraction, e.g lymphomas and leukemias
S phase specific drugs general picture?
This class of drugs is called antimetabolites, as they “mimick” certain metabolites of the S phase
G2 specific anticancer drug?
bleomycin
M phase anticancer drugs work by …….
inhibiting microtubules
Vinblastine and Vincristine moa?
inhibit polymerasation of microtubules
Paclitaxel moa?
inhibits depolymerization of microtubules - therby creating an overly stable and rigid microtubule which prevents cell division
Which drugs work in G0 phase?
drugs that can work on cells that are in rest - slow growing tumors.
- Alkylating agents
- Antitumor antibiotics
- Nitrosoureas
- Cisplatin
Cyclophosphamide moa?
attack guanine N7 rendering DNA dysfunctional
What i acrolein?
toxic metabolite of cyclophosphamide. May result in hemorrhagic cystitis
Cisplatin moa?
alkylating agent that cross-links DNA strands
Cisplatin side effects?
One of the worst to cause nausea and vomiting
ondansetron area of use?
antiemetic to cure side effects of chemo therapy
Ondansetron moa?
binds to 5H-T3 serotonin receptor
Procarbazine moa and area of use?
alkylating agent used to treat Hodgkin
procarbazine side effect?
bone marrow suppression and leukemogenic
Doxorubicin moa?
- interaclator
- forms free radicals
- inhibits topoisomerase
Doxorubicin side effects?
delayed congestive hert failure due to damage to myocardium from free radicals(heart can not metabolize these very well)
Dexrazoxane area of use?
prevent myocardial free radical damage from doxorubicin
General moa of alkylating agents?
They target nitrogens( esp. N-7 of guanine) and oxygens and purines and pyrimidines
Busulfan moa and area of use?
Busulfan inhibits granulocytopoiesis. It is used in CML
Name 3x Nitrosoureas and a handy “special effect” that they have
Carmustine, lomustine, semustine. They are lipophilic and cross the BBB.
S phase alkylating agents?
Methotrexate
6-mercaptopurine
Hydroxyurea
Cytarabine
Bleomycin and busulfan side effects?
pulmonary fibrosis
