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35 Cards in this Set

  • Front
  • Back
5 Classes of Natural Products
1. Vinca Alkaloids
2. Taxanes
3. Epipodophyllotoxins
4. Camptothecin derivatives
5. Antibiotics

These are two of the most powerful plant derived anti-tumor agents known.
The vinca alkaloids:
Vincristine and vinblastine
MOA of vinca alkaloids
Binds Tublin in a 1:1 molar ratio, shifts equilibrium to favor depolarization --> disrupts microtubule formation
Consequene of vinca alkaloids
(-) spindle formation and mitosis

Cytoskeletal movement disrupted
Do vinca alkaloids hang around in the plasma?
Nope, they rapidly disappear
Toxicity of Vincristine
Secretion of ADH
Toxicity of Vinblastine
Myelosuppression and mucositis
Vinorelbine and toxicity
Synthetic derivation of vinblastine, more specific for microtubules
Toxicity leads to granulocytopenia.
Name two Taxanes
Paclitaxel (Taxol)
Docetaxel (Taxotere)- synthetic analoge of Taxol
Where does Taxol come from?
The bark of the western yew tree Taxus brevifolia
Principle use for Taxol (Paclitaxel)
Breast and ovarian cancer
Also used for the prevention of restenosis in coronary artery stents
MOA of Paclitaxel
Promotes STABILIZATION and assembly of microtubules by inhibiting disassembly --> blocks reorganization of spindle fibers during mitosis
PK and Admin of Taxol
Continuous i.v.
Metabolized by liver
Toxicities of Paclitaxel
Neutropenia, mucositis, cardiac arrythmias in pts. who have recieved other cardiotoxic drugs
Name two epipodophyllotoxins
VP-16 (Etoposide)
VM-26 (Teniposide)
Where do epipdophyllotoxins come from?
Semisynthetic glycosidic derivatives of a podophyllotoxin derived from the mandrake plant.
(Now, I thought the mandrake plant was used to revive people who had been petrified?) :)
When do you use epipdophyllotoxins?
(It's a useful son of a gun)
Treatment of Hodgkins, diffuse histiocytic lymphoma, small cell carcinoma
MOA of Epipodophyllotoxins?
(-) Topoisomerase II

Epipodophy II otoxins
Toxicities of epipodophyllotoxins
Camptothecin derivatives: name two, derived from
Irinotecan and topotecan
Plant alkaloid camptothecin
Use of Irinoteca and its toxicities
Lung and colon cancer
Neutropenia and diarrhea
MOA of Camptothecin derivatives
(hit in the review)
(-) of Topoisomerase I
Dactinomycin (Actinomycin D)
Antibiotic that intercalates between adjacent G:C Base pairs.
Low [] (-) RNA syn, High [] (-) DNA synthesis and RNA synthesis
PK of Act D (t1/2 too!)
Rapidly absorbed into tissues, mostly excreted unchanged
t1/2 = 36 hours
Toxicities of Act. D
Name 4 Anthracyclines (these are antibiotics too)

*most widely used
MOA of Anthracyclines
DNA intercalation
Introduction of single stranded breaks
PK of Daunorubicin and Doxorubicin
Rapidly taken up into the heart, kidney, liver, lung, and spleen

Significant metabolism by the liver
Toxicities of Anthracyclines
Myelosuppression, mucositis, cardiotoxicity manifested by arrythmias and digitalis unresponsive CHF.

Cardiotoxicity reduces glutathione peroxidase (more susceptible to oxidative injury)
What can we give to reduce cardiotoxicity from Anthrcyclines?
Dexrazoxane- Fe chelator (-) free radical formation
Antibiotics used for chemotherapy
Antibiotic w/DNA binding region and Fe binding region
MOA of Bleomycin (take a deep breath)
Depurination and depyrimidation --> strand breaks

The detailed version: The S peptide binds to DNA, bridging the A2-Fe2+ complex into a postion in which oxidation is facilitated
PK of Bleomycin
Found in high [] in skin, lung, and tumor tissue
Eliminated by kidneys
Toxicities of Bleomycin
Subacute or chronic pneumonitis
Skin lesions