Pharmacology: Antineoplastics II - 2
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What is the route of administration for 6 mercaptopurine?
What are the side effects of 6 mercaptopurine?
What are the indications of 6 mercaptopurine?
Acute lymphocytic leukemia (ALL) or CML
What DDIs does 6 mercaptopurine have?
- Metabolized by xanthine oxidase
- Allopurinol inhibits xanthine oxidase and will increase mercaptopurine toxicity
- 6 MP also metabolized by 6-thiopurine methyltransferase (TPMT) a genetic deficiency in this enzyme will cause toxicities
Azathioprine (Imuran) is active or a prodrug?
Azathioprine (Imuran) is metabolized to what?
What is Azathioprine (Imuran) used for?
As an immunosuppressant and for treating rheumatoid arthritis
6-thioguanine is an analog of what?
Guanine (with a sulfur on it)
What is the route of administration for 6-thioguanine?
What enzyme activates 6-thioguanine?
What is the MOA of 6-thioguanine?
- Ribose phosphate added
- Ribonucleotide reductase changes it to the deoxy form
- Incorporated into DNA
- Inhibits DNA polymerase
What phase of the cell cycle is 6-thioguanine active in?
What is the MOA of 6 Thioguanine?
- Damages DNA after incorporation
- Inhibits synthesis of AMP and GMP
Does 6-thioguanine have a DDI with allopurinol?
No, it is not degraded by xanthine oxidase
In general what type of disease are Purine antimetabolites used to treat?
Most purine analogs cause what adverse reaction that will need to be treated?
Tumor lysis syndrome
fludarabine (Fludara) is an Analog of what?
How is Fludarabine (Fludara) administered?
By what Mechanism of action does Fludarabine (Fludara) operate?
- Converted to 2-fluoro-ara-ATP
- Inhibits DNA polymerase and ribonucleotide reductase
What are the Side effects for Fludarabine (Fludara)?
- Bone marrow depression
- Rare neurological effects
What are the Indications for Fludarabine (Fludara)?
B-cell chronic lymphocytic leukemia (CLL)
Fludarabine (Fludara) has a Florine group for what reason?
To inhibit deaminase deactivation
Cladribine (Leustatin) is an analog of what?
Deoxyadenosine (with an additional chlorine)
What needs to occur to activate Cladribine (Leustatin)?
What is the Mechanism of action for Cladribine (Leustatin)?
- Incorporated into DNA
- Inhibits DNA synthesis and repair
- Induces DNA strand breaks.
Is Cladribine (Leustatin)resistant to deaminase, why or why not?
- Yes, resistant to adenosine deaminase specifically
- Due to Chlorine group
Why does Cladribine (Leustatin) have an extended half life?
Cl group reduces adenosine deaminase deactivation
What phase does Cladribine inhibit?
Is Cladribine (Leustatin) active against quiescent or dividing cells?
What type of tumor does Cladribine (Leustatin) have no activity against?
What is the indication for Cladribine (Leustatin)?
Hairy cell leukemia
What are the side effects of Cladribine (Leustatin)?
- Myelosuppression, nephrotoxicity and neurotoxicity
- Tumor lysis syndrome
What type of cancer is Cladribine (Leustatin) mainly used to treat?
Hydroxyurea (Hydrea) is what type of drug?
Ribonucleotide Reductase Inhibitor
What is the MOA of Hydroxyurea (Hydrea)?
- Inhibits ribonucleotide reductase = Rate limiting step of DNA synthesis
- Prevents formation of deoxy riboses
What are the indicatons for Hydroxyurea (Hydrea)?
- Chronic myelogenous leukemia
- Solid tumors
- Sickle cell anemia
What are the side effects Hydroxyurea (Hydrea)?
- Bone marrow depression (leukopenia)
- Stomatitis and GI ulceration
- Skin (hyperpigmentation and hyperkeratosis)
- Radiation sensitizer
- Radiation recall
What are the Vinca alkaloids?
- vinblastine (Velban)
- vincristine (Oncovin)
- vinorelbine (Navelbine)
What are the Vinca alkaloids derived from?
What is the mechanism of action for Vinca alkaloids?
- Disruption of microtubules for mitosis by:
- Aggregation of the free tubulin dimers so that they cannot form a polymer of microtubules
- Inhibits the mitosis phase of the cell cycle
What is a common side effect of all Vinca alkaloids?
All are severe vesicants
What are the side effects of vincristine?
Severe Neurotoxicity, mild bone marrow, alopecia
What are the side effects of vinorelbine?
Bone marrow, neurotoxicity, alopecia (toxicities are in between other vinca alkaloids)
What are the side effects of vinblastine:
Severe Bone marrow, mild neurotoxicity, alopecia
Which vincristine analog is commonly combined with Cisplatin?
How are the vinca alkaloids administered?
Which vincristine analog would you not want to combine with Cisplatin?
What are the indications for Vinca alkaloids?
Different for each one (don’t need to know them all)
What are the Taxanes?
- Paclitaxel (Taxol)
- Nanoparticle albumin-bound paclitaxel (Abraxane)
- Docetaxel (Taxotere)
Where are the Taxanes derived from?
Pacific Yew Tree bark
What are the benefits of Nanoparticle albumin-bound paclitaxel (Abraxane) over normal paclitaxel?
- Increases selectivity for tumor cells
- Decreases hypersensitivity reactions
- Causes a little less myelosupression
- May be more efficacious
What would you like to do?
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