9

Consumer
Chemistry 9
Quarter 4 – Week 7
Anticancer Drugs

Name of Learner: _______________________________________

Grade Level: _______________________________________
Section: _______________________________________
Date: _______________________________________
 CONSUMER CHEMISTRY LEARNING ACTIVITY SHEET

I. Learning Competency with Code

The learners should be able to describe the properties, mode of action and effects of
anticancer drugs.

II. Background Information for Learners

MANAGEMENT OF CANCER
Treatment options offered to cancer patients should be based on realistic and achievable
goals for each specific type of cancer.
 
Possible treatment goals:
1. Complete eradication of malignant disease (cure)
2. Prolonged survival and containment of cancer cell growth (control)
3. Relief of symptoms associated with the disease (palliation)
 
Modalities commonly used in cancer treatment:
A. Surgery
B. Radiation therapy
C. Chemotherapy
D. Biologic response modifier (BRM)
 
SURGERY
 Surgical removal of the entire cancer remains the ideal and most frequently used
treatment method.
 Diagnostic surgery - Biopsy - usually performed to obtain a tissue sample for
analysis of cells suspected to be malignant
 Local excision surgery - for removal of a small mass of cancer and that small margin
of normal tissue that is easily accessible
 Wide excision surgery - include removal of the primary tumor, lymph nodes, adjacent
involved structures, and surrounding tissues that may be high risk for tumor spread.
o Example: Mastectomy - surgery to remove all breast tissue from a breast as a
way to treat or prevent breast cancer.
o Modified radical mastectomy - surgery to remove the entire breast, including
skin, areola, nipple and most axillary lymph nodes.
 Care for patients undergoing surgery: before the surgery - education about the
surgical process, after the surgery - care to avoid complications such as infection,
bleeding, and organ dysfunction; need for proper nutrition and medication
information
 
RADIATION THERAPY
 Ionizing radiation is used to interrupt cellular growth
 Can be used to cure localized cancers such as thyroid carcinoma, testicular
seminomas, cancers of the head and neck and uterine cervix
 May also be used to control malignant disease when a tumor cannot be removed
surgically
 Some side effects are experienced by patients receiving radiation therapy: fatigue,
weakness, anorexia. This is associated with substances released when tumor cells
break down. These effects are temporary and subside with the end of treatment.
 
CHEMOTHERAPY
 Antineoplastic agents are used in an attempt to destroy tumor cells by interfering
with cellular functions and reproduction.
 Used primarily to treat systemic disease rather than localized or tumors that can be
treated with surgery or radiation.
 May be combined with surgery or radiation therapy or both to:
a. To reduce tumor size before surgery/radiation
b. To destroy remaining tumor cells after surgery/radiation
c. To treat some forms of leukemia

Cell Kill and the Cell Cycle

The administration of certain chemotherapeutic agents is coordinated with the cell cycle.
 
Actively proliferating cells within a tumor (growth function) - most sensitive to
chemotherapeutic agents
Nondividing cells - capable of proliferation
 The least sensitive to antineoplastic medications
 Potentially dangerous
 Must be destroyed to eradicate a cancer completely
 This is killed by repeated cycles of chemotherapy - these are killed as they begin
active cell division
 
The cell cycle time is the time required for one tissue cell to divide and reproduce two
identical daughter cells. The cell cycle of any cell has four distinct phases, each with a vital
underlying function:
 
1. G1 phase - RNA and protein synthesis occur
2. S phase - DNA synthesis occurs
3. G2 phase - premitotic phase; DNA synthesis is
complete, mitotic spindle forms
4. Mitosis
 
G0 - resting or dormant phase of cells
 Can occur after mitosis and during the G1 phase
 During this phase, the dangerous cells are not actively
dividing but have the potential for replicating.
 
Two main groups of cytotoxic drugs, classified by their effects on cell progression
through the cell cycle:
 
1. CELL CYCLE PHASE-NON-SPECIFIC DRUGS
 These drugs act at all stages of proliferation, but not in the G0-resting phase.
 Increasing dosage also increases the number of cells killed
 These drugs are given at very high doses over a short period, cause the reduced
stem cell functions of the bone marrow, but at the same time achieving a very high
tumor cell kill
 These are used in hematological malignancies such as leukemias and lymphomas
 Example drugs:
o Alkylating agents of cycle-non-specific drugs (e.g. cyclophosphamide,
melphalan)
 o Nitrosoureas (e.g. cis-chloroethylnitrosourea CCNU, lomustine and bis-
chloroethylnitrosourea BCNU, carmustine)
 
2. CELL CYCLE PHASE-SPECIFIC DRUGS
 These drugs act only at a specific phase in the cell cycle.
 The more rapid the cell turnover, the more effective they are.


 
Principles of cytotoxic chemotherapy
1. Cells have discrete periods of the cell cycle during which they are sensitive to
cytotoxic drugs
2. Cytotoxic drugs are not totally selective in their toxicity to cancer cells.
3. Drugs are used in combination to increase efficacy, to inhibit the development of
resistance and to minimize toxicity.
 
Drugs used in Cancer Chemotherapy
1. Alkylating Agents
 Particularly effective when cells are dividing rapidly, but are not phase-specific.


 Mechanism of Action: Alkylations of DNA
within the nucleus. Alkylation of guanine
can result in miscoding through abnormal
base pairing, this is the cross-linking of DNA. Guanine pairs with another Guanine.
This leads to DNA strand breakage preventing cellular replication.

 
2. Antimetabolites
 Compete with analogues in the making of nucleic acids
 Partial selectivity for malignant cells
  Act in the S-phase of the cell
 Mechanism of Action (Antifolate
analogues, e.g. Methotrexate) - Folic acid
is required in the synthesis of thymidylate
(precursor, imagine - a raw ingredient) for
DNA synthesis. Methotrexate is a
competitor to the formation of
dihydrofolate reductase. This means that
because of structural similarities,
Methotrexates takes the place of Folic acid
in this reaction leading to unsuccessful
DNA synthesis. Thus, methotrexate
prevents nucleic acid synthesis and
causes cell death.

 
3. Natural product cancer chemotherapy drugs
 Example is Vinca Alkaloids (sample drugs: Vinblastine and Vincristine)


 Derived from the periwinkle plant Vinca rosea
 Mechanism of action -
Vinca alkaloids binds
to Beta-tubulin, a
protein that forms the
microtubules which
are essential for the
formation for the
mitotic spindle. This
inhibitory effect
results in mitotic
arrest in metaphase,
stopping cell division, which then leads to cell death.

 
 
4. Antibiotics
 Example - Anthracyclines (example drugs
Doxorubicin and daunorubicin)
 Antibiotic produced by Streptomyces peucetius
 Mechanism of action:
1. Intercalation between adjacent base pairs in
DNA, leading to fragmentation of DNA and
inhibition of DNA repair
 2. Membrane binding alters membrane function and contributes to cardiotoxicity
3. Free-radical formation also causes cardiotoxicity

 
Common complication of Cancer Chemotherapy
1. Nausea and vomiting
 Can be a day after administration, lasts for 2-4 days after therapy
 Can be caused by stimulation of the gastrointestinal tract
 Patients are given anti-emetic to treat this symptom
2. Extravasation with tissue necrosis
 This results to local reactions like irritation or severe tissue death of the skin
and surrounding blood vessels
 This is caused when the drug inadvertently or accidentally leaks into the
surrounding tissue
 Skin grafting may be necessary if it is severe enough
3. Bone marrow suppression
 This is the reduction in bone marrow activity resulting in reduced production of
blood cells
 The bone marrow cannot produce the necessary blood cells such as red
blood cells (oxygen carriers in blood), white blood cells (the body's antibodies)
and platelets (for blood clotting)
  Recovery is aided with support blood products and hematopoietic growth
factors (stimulates formation of blood cells)
4. Infection
 Most common and life-threatening complication of chemotherapy
 Patient is isolated as prevention but patient's own normal gastrointestinal
bacteria can be problematic
 Treatment is done with broad-spectrum antibiotics
5. Alopecia
 Hair loss is a common side effect of cancer treatment
 This is discussed early to the patient for supportive care like wigs
6. Infertility and teratogenesis
 Cytotoxic drugs impair fertility (ability to produce a child) and cause fetal
abnormalities
 In women, there is loss of menstruation but resumes after treatment
 In men, there could be a loss of sperm in semen and recovery can occur after
several years
 Men are advised sperm storage before chemotherapy
 Contraceptives are advised for couple with chemotherapy as this causes fetal
malformation
7. Second malignancy
 Development of a secondary cancer
 This is a delayed treatment complication

III. Activity 1 Word Search

Directions: Identify words from the puzzle that pertains to management of cancer. Encircle
the words or write it in a separate piece of paper.

IV. Activity 2 Cytotoxic Drugs Checklist

Directions Place a check mark on the correct category that is being described by each
statement, or a check mark on both if the statement refers to both categories.
Cell Cycle Phase-Non- Cell Cycle Phase-Specific
Specific Drugs Drugs
 Act at all stages of
proliferation
Act at a specific phase in
the cell cycle
Effectivity depends on the
drug dosage
Effectivity depends on the
cell turnover
Toxicity is not totally
selective to cancer cells
only

V. Activity 3 Jumbled Letters

Directions Unscramble the letters to form the correct words that is being described by each
statement.
Chemotherapy Drugs Mechanism of Action Answer
ACTIONBIIT Membrane binding alters
membrane function and
contributes to cardiotoxicity
SALADKILO Binds to Beta-tubulin, a
protein that forms the
microtubules which are
essential for the formation for
the mitotic spindle
ATIMETABLESINTO Takes the place of Folic acid
in this reaction leading to
unsuccessful DNA synthesis
S T A G N A T E Y A N G K I L Alkylation of guanine leading
L to DNA strand breakage

VI. Activity 4 Cause and Effect

Directions Write the cause of some of the complications of cancer chemotherapy.
 (Cause)
Nausea and
vomiting
______________

(Cause) Extravasion
with tissue
______________ necrosis

(Cause)
Infection
______________

VII. Guide Questions

What is you best advice if you know someone who is undergoing cancer treatment?
___________________________________________________________________
___________________________________________________________________

VIII. Reflection
Do you agree with this quotation? Then support your answer with 2-3 sentences.
“Prevention is a very important part of solving the problem of cancer.”
___________________________________________________________________
___________________________________________________________________

IX. Reference for learners

Hinkle, J.L. & Cheever, K.H. (2014). Brunner and Suddarth’s Textbook of Medical-Surgical Nursing 10th
Edition. Wolters Kluwer Health/Lippincott Williams and Wilkins.
Katzung, B. G. (2012). Basic & clinical pharmacology. McGraw-Hill Medical.
Mohammad Abrar Khan. (16:21:12 UTC). Vinca Alkaloids as Anticancer Agents (Looking back and
peering ahead). https://www.slideshare.net/AbrarKhan94/vinca-alkaloids-as-anticancer-agents-
looking-back-and-peering-ahead
Ritter, J., Lewis, L., Mant, T., & Ferro, A. (2012). A Textbook of Clinical Pharmacology and Therapeutics,
5Ed. Taylor and Francis.
Saleh, Y., Abdelkarim, O., Herzallah, K., & Abela, G. S. (2020). Anthracycline-induced cardiotoxicity:
Mechanisms of action, incidence, risk factors, prevention, and treatment. Heart Failure Reviews.
https://doi.org/10.1007/s10741-020-09968-2
IX. Answer Key

Activity 1
Activity 2
Cell Cycle Phase-Non- Cell Cycle Phase-Specific
Specific Drugs Drugs
Act at all stages of proliferation /
Act at a specific phase in the cell /
cycle
Effectivity depends on the drug /
dosage
Effectivity depends on the cell /
turnover
Toxicity is not totally selective to / /
cancer cells only
Activity 3
Antibiotic
Alkaloids
Antimetabolites
Alkylating Agents
Activity 4

Stimulation of gastrointestinal Nausea and

tract vomiting

Extravasion
Drugs leaking to surrounding tissue with tissue
necrosis

Drugs are not toxicity specific, they

also kill body cells that fight infection Infection

Prepared by:

TIFFANY MAE L. GO