Vinca Alkaloids

Question 1

Vinca Alkaloids (general)

Answer 1

• Inhibit MT polymerization by binding to R-tubulin which inhibits MT assembly
• Induces mitotic arrest in Metaphase

Question 2

Vinblastine

Answer 2

- Cyto P450 metab in liver
Tox: N/V
- BM suppression 
- Alopeica 
- Potent vesicant (extravasation) 
(VinBLASTine BLASTS out of veins!)

Question 3

Vincristine

Answer 3

• Active against hematologic malignancies
  Tox: - Neurotox w/ periph neuropathy
• ANS Dysfunction- orthostatic hypotension, urinary retention, paralytic ileus
• Myelosuppression
• SIADH

Question 4

Taxanes (general)

Answer 4

• MT spindle poison that enhance MT polymerization
• Liver P450 metab (dose adjust for liver dysfunction)
• Tx for a broad range of SOLID tumors (breast, ovarian, NSCLC especially)
• Paclitaxel, Abraxane, Docetaxel

Question 5

Paclitaxel

Answer 5

Acute Tox: N/V, hypotension
- Hypersensitivity Rxn (5%)- can prevent with dexamethasone and diphenhydramine
Delayed Tox: Myelosuppression
- Neurotoxicity- Periph sensory neuropathy

Question 6

Abraxane (nab-Paclitaxel)

Answer 6

• Paclitaxel formed w/ a nano-particle size albumin carrier which increases delivery of drug to the tumor b/c it’s not recognized as foreign (no hypersensitivity rxn)
• Less overall tox. than paclitaxel
• Tx- breast, pancreatic, NSCLC

Question 7

Docetaxel

Answer 7

• Semi- synthetic taxane

Tx- breast, NSCLC, head and neck tumors

Question 8

Ixebeplinone

Answer 8

Epithilone B Agent
- Binds R-Tubulin subunits to stabilize MT
- Active in tumors that express p-glycoprotein or MT mutations
- Tx for breast cancer
Tox: Myelosuppression
- Hypersensitivity
- Neurotoxicity