Cancer Pharm: Natural Products Flashcards
What is the MOA of the vinca alkaloids, vinblastine, vincristine, and vinorelbine; specific to which phase?
- Inhibit tubulin polymerization by DISRUPTING assembly of microtubules; especially those involved in mitotic spindle
- M-phase specific: results in mitotic arrest in metaphase
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AE’s of vinblastine?
- N/V, bone marrow suppression (vin-blast-tine), and alopecia
- Potent vesicant (blistering)
Vinblastine is used for what cancers?
Hodgkin’s and NHL’s, breast, and germ cell cancer
Vincristine is similar to vinblastine but has a higher affinity for what?
Axonal microtubules
What is the dose-limiting AE’s of Vincristine?
- Neurotoxicity –> Peripheral sensory neuropathy manifesting as:
- ANS dysfunction w/ orthostatic hypotension; urinary retention; paralytic ileus or constipation; CN palsies; ataxia; seizures; coma
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Which 2 vinca alkaloids are associated with SIADH as potential AE’s?
- Vincristine
- Vinorelbine
List 4 AE’s associated with Vinorelbine?
- N/V
- Transient elevations in LFT’s
- Neurotoxicity
- SIADH
Which vinca alkaloid can be used for pediatric tumors, rhabdomyosarcoma, neuroblastoma, Ewing’s sarcoma, and Wilms tumor?
Vincristine
Which 3 natural products work by binding to microtubules and enhancing tubulin polymerization causing cell death; which phase do they work in?
- Paclitaxel, Docetaxel, and Cabazitaxel (Taxanes)
- Work in the M phase
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Which 2 natural products are associated with hypersensitivity reactions as AE’s?
- Paclitaxel
- Docetaxel
What are acute vs. delayed dose limiting toxicities associated with Paclitaxel?
- Acute = N/V, hypotension, arrhythmias, hypersensitivity
- Delayed = myelosuppression, peripheral sensory neuropathy
Which form of paclitaxel is NOT associated w/ hypersensitivity rxns, has reduced myelosuppressive effects, and neurotoxicity more easily reversed?
Albumin-bound paclitaxel
What are the acute vs. delayed toxicities assoc. w/ Docetaxel?
- Acute = hypersensitivity
- Delayed = neurotoxicity, fluid retention, myelosuppression w/ neutropenia
Why is Cabazitaxel more useful in treating multi-drug resistant tumors than other taxanes?
Is poor substrate for P-glycoprotein
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How does Ixabepilone differ in its MOA from the taxanes?
Microtubule inhibitor that binds directly to β-tubulin subunits on microtubules —> dynamic inhibition of microtubule