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41 Cards in this Set

  • Front
  • Back
4 classes of Microtubule Targeting Agents?
-vinca alkyloids
-taxanes
-epothilones
- and estramustine
Vinca alkaloids?
vincristine, vinblastine, vindesine, vinorelbine
Taxanes?
paclitaxel, docetaxel
Epothilones?
ixabepilone
The microtubule structure is composed of?
α- and β- heterodimers
All anti-micotubular drugs are ___phase specific?
M phase
Microtubules are required for?
cell shape, transport of vesicles, signaling and mitosis
Vinca alkyloids based on the catharanthine stucture?
vincristine, vinblastine, vindesine,
Vinca alkyloids based on the induline stucture?
vinorelbine
Vinca alkyloids can cause neuropathy due to?
Neuron sensitivity to drugs that affect microtubules
Vinca alkyloid MOA?
binds β-tubulin, blocking its ability to polymerize with α-tubulin into microtubules
• M phase-specific
Vinca alkyloids are extensively metabolized by?
CYP-3A4
Vinca alkyloids require?
dose reduction for hepatic impairment
Vinblastine is given IV and is used to treat?
Lymphomas, lung cancer, prostate cancer and melanoma
Vinblastine is also a strong ______?
Vesicant
Vincristine is given IV and is used to treat?
ALL, Lymphoma and pediatric solid timors
The major toxicity associated with Vincristine is?
neuropathy
True or false, vincristine is not a vesicant like vinblastine?
false, vincristine and vinblastine are both vesicants
True or false, all vinca alkyloids are potent 3A4 inhibitors that require dose adjustments for hepatic impairment?
True
Vinca alkaloids are derivatives of the sap from the _______________?
Madagascar periwinkle
Taxanes are derived from the?
Western yew tree
Modifying the R1 and R2 groups on taxanes makes the drugs more ____and_____.
water soluble and poten
The MOA of taxanes?
Bind Beta-tubulin subunit, thus promoting polymerization
The taxane structure responsible for activity is the?
8 membered hexane ring
Paclitaxel is used to treat?
breast, lung, ovarian and head and neck cancer
The IV vehicle for Paclitaxel is?
50%ehtanol and 50% polyethoxylated castor oil (CREMOPHOR EL)
Albumin bound Paclitaxel is?
Abraxane
Paclitaxel pharmacokinteics are?
Non-linear (dose-dependent)
Myelosuppression due to Paclitaxel treatment is alleviated by?
Filgrastim (NEUPOGEN) a granulocyte colony-stimulating factor (G-CSF) analog
Hypersensitivity reactions (e.g. dyspnea, chest pain,
hypotension) caused by paclitaxel can be prevented by?
dexamethasone and antihistamines
The vehicle in Docetaxel is?
polysorbate 80
Docetaxel is used to treat?
Lung, prostate, ovarian, breast and head and neck cancers
The primary clinical toxicity associated with Decetaxel is?
Severe myelosuppression
Ixabepilone MOA?
binds to β-tubulin, promoting the
polymerization of microtubules
Ixabepilone is used to treat?
breast cancer
True or false, all plant derived microtubule drugs are potent 3A4 inhibitors?
True
The non-plant derived antimicrotubule is?
Estrmustine
The antimicrotubule in oral dosage is?
Estrmustine
Estramustine is based on?
Estradiol
Estramustine is used to treat?
prostate cancer
The functional group on estramustine is?
a nitrogen mustard
-however, estramustine does not function as a nitrogen mustard. The function is that of a microtubule inhibitor