Drugs Flashcards
Mecholoroethamine
Class: Alkylating agent Mechanism: Interstrand and intrastrand crosslinks - DNA adducts CCNS/CCS: CCNS Administered: IV Resistance: Apoptosis, MDR, increased DNA repair Side effects: Nausea, vomiting, myelosuppression (dose limiting factor)
Cyclophosphamide
Class: Alkylating agent Mechanism: Interstrand and intrastrand crosslinks - DNA adducts CCNS/CCS: CCNS Administered: IV + Oral - it is broken down in lover to its active form Resistance: Apoptosis, MDR, increased DNA repair Side effects: Nausea, vomiting, sterile hemorrhagic cystitus, alopecia - mesna is administer to help with bladder problems and the patient is given forced hydration
Cisplatin
Class: Alkylating agent Mechanism: Interstrand and intrastrand crosslinks - DNA adducts CCNS/CCS: CCNS Administered: IV Resistance: Apoptosis, MDR, increased DNA repair Side effects: Severe nausea and vomiting, otatoxicity, peripheral nephrotoxicity, nephrotoxicity is the dose limiting factor
Methotrextate
Class: Anti metabolite Mechanism: 1. Mimics folic acid. 2. It inhibits formation of bases from DHFR, so no DNA and RNA can be made CCNS/CCS: CCS Administered: IV + Orally Resistance: Decreased concentration of the drug in cancer cells and increase in [DHFR] Side effects: Bone marrow depression and GI tract
6-Mecarptopurine
Class: Anti metabolite Mechanism: 1. Purine analog. 2. It inhibits the synthesis of AMP and GMP. 3. Inactivated by Thiopurine Methyl Reductase CCNS/CCS: CCS Administered: Orally Resistance: Decrease in levels of HPRT and increase in alkaline phosphatase activity. Side effects: Bone marrow depression
6-Thiopurine
Class: Anti metabolite Mechanism: 1. Purine analog. 2. It inhibits the DNA and RNA synthesis 3. Inactivated by Thiopurine Methyl Reductase CCNS/CCS: CCS Administered: Orally Resistance: Decrease in levels of HPRT and increase in alkaline phosphatase activity. Side effects: Bone marrow depression
5-Fluorouracil
Class: Anti metabolite Mechanism: 1. Inhibits the synthesis of thymidine 2. Inhibits thimidylate synthase enzyme CCNS/CCS: CCS Administered: IV Resistance: Increase in [Thimidylate Synthase] and overexpression of DPD Side effects: Bone marrow depression + GI tract
Gemcitabine
Class: Anti metabolite Mechanism: 1. Inhibits polymerase and end chain terminator CCNS/CCS: CCS Administered: IV Resistance: ??? Side effects: Bone marrow depression + GI tract
Doxorubicin
Class: Anti tumor antibody Mechanism: 1. Binds with DNA, does not form adducts 2. Releases free radicals when close to DNA CCNS/CCS: CCNS Administered: IV Resistance: MDR Side effects: Alopecia and cardiotoxicity, drug Dexrazoxane is given to control cardiotoxicity.
Daunorubicin
Class: Anti tumor antibody Mechanism: 1. Binds with DNA, does not form adducts 2. Releases free radicals when close to DNA CCNS/CCS: CCNS Administered: IV Resistance: MDR Side effects: Alopecia and cardiotoxicity, drug Dexrazoxane is given to control cardiotoxicity.
Bleomycin
Class: Anti tumor antibody Mechanism: 1. Releases free radicals CCNS/CCS: CCS Administered: IV Resistance: MDR Side effects: Pulmonary toxicity and fibrosis
Vinblastin
Class: Microtubule poisons Mechanism: 1. Inhibits polymerization 2. Promotes depolymerization CCNS/CCS: CCS Administered: IV Resistance:??? Side effects: Nausea, vomiting, alopecia, bone marrow supression
Vincristine
Class: Microtubule poisons Mechanism: 1. Inhibits polymerization 2. Promotes depolymerization CCNS/CCS: CCS Administered: IV Resistance:??? Side effects: Peripheral neurotoxicity and less bone marrow suppression than vinblastin
Paclitaxel
Class: Microtubule poisons Mechanism: 1. Excessive stabilization of microtubules CCNS/CCS: CCS Administered: in cremaphore nanoparticles that causes severe inflammatory response Resistance: MDR Side effects: Neuropathy and bone marrow depression
Docataxel
Class: Microtubule poisons Mechanism: 1. Excessive stabilization of microtubules CCNS/CCS: CCS Administered: in cremaphore nanoparticles that causes severe inflammatory response Resistance: MDR Side effects: Neuropathy and bone marrow depression
Irinotaxen
Class: Topoisomerase inhibitor Mechanism: SN-38 is its active form, converted by esterase CCNS/CCS: CCS Administered: IV Resistance: Inactivated by glucouridination by UGT1A1 and reduction in esterase levels Side effects: Nausea, vomiting and Diarrhea (dose limiting)
Flutamide
Class: Androgen inhibitor Mechanism: 1. Inhibits the binding of androgens to their receptors 2. It is taken with radiation when treating testicular cancer CCNS/CCS: CCNS Administered: IV Resistance: ??? Side effects: Nausea, hot flushes and Transient hepatic effects
Tamoxifen
Side effects: Fatigue, headache and vaginal bleeding
Lestrozole
Class: AI Mechanism: 1. Inhibits the conversion of andrgoens CCNS/CCS: CCNS Administered: Orally Resistance: ??? Side effects: Headache, nausea , fatigue, hot flushes
Anastrazole
Class: AI Mechanism: 1. Inhibits the conversion of andrgoens CCNS/CCS: CCNS Administered: Orally Resistance: ??? Side effects: Headache, nausea , fatigue, hot flushes
Trastuzumab
Cardiomyopathy
Imatinab
Class: Tyrosine kinase inhibitor Mechanism: 1. Inhibits the tyrosine kinase receptors in BCR/ABL for Chronic Mylogenous Leukemia 2. Inhibits FIT receptor in Gastrointestinal Sarcoma Tumor (GIST) CCNS/CCS: CCNS Administered: Orally Resistance: ??? Side effects: Myelosuppression, edema and hepatotoxicity
Dasatinab
Class: Tyrosine kinase inhibitor Mechanism: 1. Inhibits the tyrosine kinase receptors in BCR/ABL for Chronic Mylogenous Leukemia 2. Inhibits FIT receptor in Gastrointestinal Sarcoma Tumor (GIST) CCNS/CCS: CCNS Administered: Orally Resistance: ??? Side effects: Myelosuppression, edema and hepatotoxicity
Gefitinab
Class: Tyrosine kinase inhibitor Mechanism: 1. Inhibits EGFR tyrosine kinase 2. For non-small cell lung cancer CCNS/CCS: CCNS Administered: Orally Resistance: ??? Side effects: Fever and dyspnea
