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Anticancer Drugs
Anticancer drugs
7
Pharmacology
Graduate
11/08/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Log Kill Hypothesis
Definition

Rodent Leukemia Model

Resembles first order kinetics

A constant fraction is being eliminated

ex.  If you start with 100 tumor cells and 50% is eliminated every time then with one half life you have 50 tumor cells, with two half lives you have 25 cells. 

Most solid tumors do not follow this model.

Term
Gompertzian kinetics
Definition

Most solid tumors display Gompertzian kinetics

As the tumor grows larger less cells are actively proliferating.

Each dose does not kill a constant fraction of cells.

Term
Drug Resistant Cells in Tumors
Definition

Major Problem in Chemotherapy

May occur de novo

Gene amplification

P-glycoprotein-mediates efflux of multiple drugs

Term
General Principles of Combination Chemotherapy
Definition

Goal is to produce maximum efficacy with tolerable toxicity

1. Each drug individually active against tumor

2. Mechanisms of interaction produce optimum effect (synergistic)

3. Drugs that have different major toxic effects

4. Other:optimum drug dosage, optimum drug scheduling

Term
Adjuvant Chemotherapy
Definition
Chemotherapy AFTER surgery
Term
Neoadjuvant Therapy
Definition
Chemotherapy BEFORE surgery
Term
Bis(chloroethyl)amines
Definition

Alkylating Agents

Drugs: Mechlorethamine

Melphalan

Cyclophosphamide

Chlorambucil

Involves the formation of cyclic imonium or carbonium ion intermediate that Rxs with tissue nucleophiles --> alkylation of molecules.

Interferes with nucleic acid synthesis and function.

With bifunctional agents 2nd group can be activated and alkylated 2nd nucleophile.

Resistance involves DNA repair of DNA

Toxicites: Myelosupression, GI (nausea, vomiting), reproductive, carcinogenesis also possible.

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