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Year II Pharmacology > Chemotherapy I & 2 > Flashcards

Chemotherapy I & 2 Flashcards

1
Q

Anti-metabolic are __?__ phase specific and target __?__

A

S phase specific

Target DNA replication

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2
Q

Anti-metabolite tage acute or chronic cancers?

A

Acute

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3
Q

Name 3 anti-metaobolites

A

Methotrexate
5FU
Cytrabine (ara-C)

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4
Q

Methotrexate
Target
SE
Rescue drug

A 
•	Folic acid analogue supposed to stop dihydrofolate reductase (DHFR)
•	Derived from aminopterin
•	Uses
o	CNS
o	Lymphoma
o	Breast
o	H& N
o	Lung
•	Side Effects
o	Renal failure (alkanaized urine)
o	Rescued by leucovorin
o	Highly resistant (trimetrexate is new agent)p
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5
Q
  1. Lovocurine
A
  1. Methotrexate & potentiates the action of 5FU
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6
Q

5FU
mechanism
Use
Not a rescue but something that perpetuates the action of 5FU

A 
•	Inhibits Thymidylate synthase
•	Uses
o	Breast
o	GI
•	Leucovorin can potentiate action of 5FU
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7
Q

Cytarabine
Mechanism (does 2 things)
Severe SE
Use

A

• Nucleoside analogue (ribose converted to arabinose)
• Inhibits DNA polymerase alpha
• If incorporated into DNA: chain elongation & DNA ligation
• Uses
o AML (induction therapy with Daunorubicin)
o Lymphoma
• Side Effects
o Cerebellar toxicity

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8
Q 
Alkylaing Angents
Phase specific?
Mechansim
Dose response curve?
SE
Can cause?
A
  • Bind DNA
  • Phase non-specific
  • Linear dose response curve
  • Nausea
  • Marrow suppression
  • Mutagenesis
  • Secondary cancers: AML & MDS (difficult to treat)
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9
Q

Name 3 alkylating agents

A

Mechlorethamine
Cyclophosphamide
Cisplatin

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10
Q

Cyclophasmpahide

  • Use?
  • Actived by which organ?
  • Very specific SE?
  • Rescued by?
A 
•	Most widely uses
•	Activated by liver p450
•	Side effects
o	Hemorrhagic cystitis 
o	caused by acrolein metabolite 
o	Rescued by MESNA (2-mercaptoethane sulfonate)
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11
Q

Cisplating

  • Mechanism
  • Use
  • SE (2)
A 
•	Bi-functional alkylating agent
•	Used in: breast, ovarian, head & neck cancers
•	Side effects
- 	Renal insufficiency
Neuropathy & hearing loss
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12
Q

Mechlorethamine

  • This drug was the ?
  • mechanism
  • This drug is OK for use in
  • SE
A 
•	G-cross linking
•	1st chemotherapy agent
•	Non-enzymatic hydrolysis OK in patients with renal/hepatic failure
•	Myelosuppression is dose limiting
•	Secondary Cancer
o	Leukemia
o	Lymphoma
o	MDS
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13
Q

Difference between topoisomerase I & II

A
  • Topoisomerase I: Single stranded DNA breaks

* Topoisomerase II: Double stranded breaks

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14
Q

Name the
1 Topo I inhibitor
Mechanism
Use

A

Epipodophyllotoxins Etoposide or VP-16

•	Topo I inhibitor
•	Single stranded DNA breaks
•	Uses
o	Lung
o	Ovarian
o	Colorectal
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15
Q

Name the 2 Topo 2 inhibitors

A

Anthracycline

Daunorubicin Doxorubicin

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16
Q

Only SE of Epipodophyllotoxins

Etoposide or VP-16

A

• Neutropenia

17
Q

Daunorubicin & danxorubicine

  • Mechanism
  • Uses
  • SE
A 
•	Intercalate into DNA & bind G residues
•	Stabilizes DNA-Topo II intermediate
•	DNA fragmentation
•	Uses
o	Hematologic malignancies
o	Brest
o	Lung
o	GI
o	GU cancers
•	Side Effects
o	Hepatotoxicity
o	CHF
o	Vesicants (blisters)
18
Q

Immunomodulatory Drugs

  • Main SE
  • Name the 3
  • Which one is used to treat MM
A 
•	Thalidomide
o	GVHD
o	MM
•	Lenalidomide
o	MM
o	MDS
o	SE: Neuropathy
•	Pomalidomide
o	MM
19
Q

Protesomal Inhbitors

  • Name 2 agents
  • Mechanism
  • Uses
A 
Velcade & Carfilzomib
•	Activates unfolded protein stress response pathway & apoptosis
•	Uses
o	Multiple myeloma
o	Mantle cell lymphoma
20
Q

Microtubule Inhibitors

  • Name 3 agents
  • Which two share the same mechanism, describe that mechanism
  • Mechanism of he 3rd
A

Vinblastine & vincristine
• M phase specific
• Bind tubulin

Taxol
• Stabilizes microtubules preventing depolymerization

21
Q

Vinicristine (use male or female)

Viniblastine (male or female)

A 
Vinicristine (female)
•	neuropathy 
Breast & cervix
•	Lung
•	Sarcoma
•	Lymphoma
•	Used with drugs whose primary toxicity in bone marrow related

Viniblastine (male)
Uses
•	Testicular
•	Lymphoma
SE
•	 Bone marrow
22
Q

Immune enhancing cytokines/growth factors

A
  • IL-2: Melanoma & renal carcinoma
  • IFNs (a, B, g): RCCs, NHL, melanoma, CML & MS
  • SC administration
23
Q

Bone marrow prolifereation

A

• G-CSF: MDS, neutropenia & severe infection
GM-CSF: MDS, neutropenia & severe infection
• Epo (rarely used): Anemia due to chemotherapy but worse outcomes with breast, NSC, H&N, lymphoid & cervical
• Thrombopoietin
• Subcutaneous or IV
• SE: bone pain, fever & headache, excess Epo can cause HTN & stroke

24
Q

Rituximan & tiuxetan target

25
Q

Gemtuzmab

A

CD33 immature myeloid cells AML

26
Q

Cetuximab

A
  • EGFR
  • Colorectal
  • H&N cancers
27
Q

Bevacizumab

A
  • VEGF
  • Colorectal
  • H&N
  • Breast
  • Kidney
28
Q

Name the only DNA methylation agents

  • Mechanism
  • Uses
A

5-Azacytidine
• Induce cellular differentiation
• AML & MDS

Year II Pharmacology (14 decks)

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