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anticancer drugs 1 Flashcards

1
Q

What are the different modalities of cancer treatment?

A
  • Surgery
  • Radiation therapy
  • Systemic therapy
  • Gene therapy
  • Alternative therapy

These modalities encompass various approaches to treating cancer, including traditional and innovative methods.

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2
Q

What is the role of surgery in cancer treatment?

A
  • Preventing
  • Diagnosing
  • Staging of cancer
  • Definitive therapy for localized tumors
  • Debulking to decrease tumor size
  • Palliative care to relieve pain
  • Facilitator for IV catheter insertion

Surgery is one of the oldest forms of cancer treatment and serves multiple purposes in the management of cancer.

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3
Q

What is radiation therapy?

A

High doses of ionizing radiation directed at cancerous tissue to eradicate localized tumor masses

Radiation therapy can be used curatively or palliatively and may damage normal tissues.

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4
Q

What are the objectives of chemotherapy?

A
  • Cure
  • Palliative
  • Adjuvant
  • Neoadjuvant
  • Salvage

These objectives represent different strategies for using chemotherapy based on the patient’s disease status.

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5
Q

What factors influence dosing in chemotherapy?

A
  • Body weight
  • Body surface area (BSA)
  • Area under the curve (AUC)

BSA is particularly important as it correlates with cardiac output and affects drug elimination.

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6
Q

What is combination chemotherapy?

A

Combining multiple agents to enhance effectiveness

This approach aims to overcome resistance, target different phases of the cell cycle, and minimize overlapping toxicities.

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7
Q

What are the common routes of administration for chemotherapy?

A
  • Intravenous (IV)
  • Oral (PO)
  • Subcutaneous (SQ)
  • Intrathecal (IT)
  • Intraarterial
  • Intraperitoneal
  • Intravesical
  • Hepatic artery infusion

The route of administration can significantly affect the drug’s efficacy and side effects.

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8
Q

What defines a complete response (CR) to chemotherapy?

A

Disappearance of all clinical, gross, and microscopic disease for a minimum of 1 month after treatment cessation

A CR indicates a significant positive outcome from therapy.

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9
Q

What is stable disease in the context of chemotherapy response?

A

Tumor that neither grows nor shrinks significantly (less than 25% change in size)

This indicates a lack of progression, which can be an important outcome in treatment assessment.

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10
Q

What is drug resistance in chemotherapy?

A
  • Decreased activation of prodrugs
  • Decreased uptake of drugs
  • Changes in target enzymes
  • Alterations in drug-induced damage repair
  • Increased drug inactivation
  • Decreased apoptosis

Drug resistance can significantly hinder the effectiveness of chemotherapy.

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11
Q

What are the classes of antineoplastic agents?

A
  • Antimetabolites
  • Antimitotic agents
  • Alkylating agents
  • Antibiotics
  • Topoisomerase inhibitors
  • Hormones
  • Immunomodulators
  • Antiangiogenic agents
  • Monoclonal antibodies
  • Adjuvants
  • Novel agents

Each class has a unique mechanism of action and application in cancer treatment.

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12
Q

What is meant by dose intensity in chemotherapy?

A

Specific dose delivered over a specific period of time

Dose intensity is crucial for maximizing treatment efficacy.

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13
Q

Fill in the blank: The primary goal of neoadjuvant chemotherapy is to _______.

A

[decrease the tumor burden or shrink the tumor before definitive therapy]

This approach is often used before surgery or radiation.

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14
Q

True or False: Dose density refers to the lengthening of intervals between doses to maximize drug effects.

A

False

Dose density actually involves shortening the intervals between doses.

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15
Q

What are the common toxicities associated with cytotoxic drugs?

A
  • Bone marrow depression
  • Impaired wound healing
  • Sterility
  • Alopecia
  • Gastrointestinal damage
  • Immunosuppression

These toxicities can limit the use of certain drugs and affect patient quality of life.

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16
Q

What are folic acid analogs used for in DNA synthesis?

A

They provide single carbon groups for the synthesis of precursors of DNA and RNA

Examples include Methotrexate, Trimetrexate, and Pemetrexed.

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17
Q

What is the key role of tetrahydrofolate (THF) in DNA synthesis?

A

THF acts as a cofactor providing single carbon groups for methylation processes

Specifically, it is involved in the methylation of uracil to thymidylate.

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18
Q

What is the mechanism of action for Methotrexate?

A

Inhibits dihydrofolate reductase (DHFR), leading to a deficiency of THF

This prevents one carbon transfer reactions necessary for purine and thymidylate synthesis.

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19
Q

What are the side effects of Methotrexate?

A

GI epithelial damage, bone marrow suppression, nephrotoxicity

High doses may lead to nephrotoxicity due to drug precipitation in renal tubules.

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20
Q

Fill in the blank: Methotrexate is a _______ antagonist.

A

folic acid

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21
Q

What are purine antagonists?

A

6-thiol analogues of endogenous purine bases

Examples include Mercaptopurine and Thioguanine.

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22
Q

What is the role of hypoxanthine guanine phosphoribosyl transferase (HGPRT) in the action of Mercaptopurine?

A

It metabolizes Mercaptopurine to its nucleotide form

The nucleotide form inhibits enzymes involved in purine nucleotide interconversion.

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23
Q

What is the mechanism of action for Fluorouracil?

A

Converted to fraudulent fluorodeoxyuridine monophosphate (FDUMP) which inhibits thymidylate synthase

FDUMP interacts with the folate cofactor without conversion to thymidylate.

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24
Q

What are the main therapeutic uses for Cytarabine?

A

Treatment of meningeal leukemia, acute non-lymphocytic leukemia, non-Hodgkin’s lymphomas

Often used in combination with other agents like anthracyclines.

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25
What is the mechanism of action of Hydroxyurea?
Inhibits ribonucleotide reductase by scavenging tyrosyl radicals ## Footnote This results in decreased synthesis of deoxyribonucleotides.
26
What are alkylating agents and their mechanism of action?
They alkylate DNA, causing mispairing, depurination, and cross-linking ## Footnote This leads to interference with DNA transcription and replication.
27
What are the main side effects of alkylating agents?
Bone marrow depression, GIT disturbances, depression of gametogenesis ## Footnote This may lead to sterility, especially in men.
28
Fill in the blank: Nitrogen Mustards are related to _______ gas.
mustard
29
What is a key characteristic of purine antagonists like Mercaptopurine?
They can be incorporated into DNA as fraudulent nucleotides ## Footnote This incorporation disrupts normal purine synthesis.
30
What is the role of thymidine kinase in Methotrexate resistance?
Converts thymidine to thymidylate, bypassing the inhibited reaction ## Footnote This allows for continued synthesis of thymidylate despite Methotrexate presence.
31
What are the mechanisms of resistance to 5-Fluorouracil?
Decreased enzyme activity, amplification of thymidylate synthase, altered synthase that is not inhibited by 5-FdUMP ## Footnote These changes reduce the drug's effectiveness.
32
What are nitrogen mustards related to?
Sulphur mustard, the 'mustard gas' used during the First World War. ## Footnote Examples include mechlorethamine, cyclophosphamide, and ifosfamide.
33
What is the prototype drug for nitrogen mustards?
Mechlorethamine. ## Footnote It is the most rapidly acting alkylating agent.
34
What are the therapeutic uses of mechlorethamine?
* Hodgkin’s disease * Solid tumors like breast, prostate, and ovarian carcinoma. ## Footnote Often used in combination with other antineoplastic drugs.
35
What are the side effects of mechlorethamine?
* Nausea and vomiting * Myelosuppression * Leukopenia * Thrombocytopenia * Alopecia and skin rash. ## Footnote Herpes zoster is frequently associated with treatment.
36
What is significant about cyclophosphamide?
It is inactive until metabolized in the liver by P450 mixed function oxidases. ## Footnote Ifosfamide is an analogue of cyclophosphamide.
37
What are the therapeutic uses of cyclophosphamide?
* Hodgkin’s disease * Other lymphomas * Carcinoma of lung, breast, cervix, and ovary * Immunosuppressant. ## Footnote It may be used in combination with other drugs.
38
What are the side effects of cyclophosphamide?
* Urinary tract hemorrhagic cystitis * Bone marrow depression * Nausea and vomiting * Alopecia * Testicular atrophy. ## Footnote Patients should be well hydrated to prevent urinary complications.
39
What is melphalan derived from?
Phenylalanine derivatives of nitrogen mustard. ## Footnote It can be taken orally.
40
What are the therapeutic uses of melphalan?
* Treatment of multiple myeloma * Ovarian carcinoma. ## Footnote Less effective in breast cancer treatment.
41
What are the side effects of melphalan?
* Mainly haematological toxicity * Nausea and vomiting * No alopecia (useful in women).
42
What is chlorambucil used for?
Treatment of chronic lymphocytic leukemia, breast, ovarian, and testicular carcinoma. ## Footnote It is the slowest acting nitrogen mustard.
43
What are the side effects of chlorambucil?
* Moderate myelosuppression * Amenorrhea * Pulmonary fibrosis * Dermatitis * Hepatotoxicity.
44
What is busulfan primarily used for?
It is used in chronic granulocytic leukemia and to prepare patients for bone marrow transplantation. ## Footnote It causes myelosuppression.
45
What are the side effects of busulfan?
* Myelosuppression (mainly thrombocytopenia) * Nausea, vomiting, and diarrhea * Sterility and amenorrhea * Fetal malformation. ## Footnote Hyperuricemia may occur due to extensive purine catabolism.
46
What are nitrosoureas known for?
They act both by alkylation and by other unknown mechanisms. ## Footnote Highly lipophilic and can cross the blood-brain barrier.
47
What are the therapeutic uses of nitrosoureas?
* Hodgkin’s diseases * Meningeal leukemia * Brain tumors * Gastrointestinal, breast, and renal cell carcinoma.
48
What are the side effects of nitrosoureas?
* Profound myelosuppression * Renal failure (especially with semustine) * Interstitial pulmonary fibrosis.
49
What is dacarbazine activated by?
N-demethylation in the liver. ## Footnote It subsequently releases an alkylating derivative in the target cell.
50
What are the therapeutic uses of dacarbazine?
Used in Hodgkin’s disease alone or in combination with doxorubicin, bleomycin, and vinblastine.
51
What are the side effects of dacarbazine?
* Nausea and vomiting * Myelosuppression * Flu-like syndrome * Hepatotoxicity and neurotoxicity. * Alopecia and facial flushing.
52
How do cisplatin and carboplatin interact with DNA?
They form a reactive diamine-platinum complex that interacts with DNA. ## Footnote Effective in treatment of solid tumors of the testes and ovary.
53
What are the main side effects of cisplatin?
* Nephrotoxicity * Ototoxicity. ## Footnote Carboplatin is more myelotoxic.
54
What are vinca alkaloids derived from?
Plant alkaloids extracted from the Periwinkle plant (Vinca Rosa).
55
What is the mechanism of action of vinca alkaloids?
They bind to tubulin, preventing spindle formation in mitosing cells. ## Footnote This leads to mitotic arrest at metaphase.
56
What are the therapeutic uses of vincristine?
* With prednisone for remission of acute leukemia * Lymphomas * Systemic Hodgkin’s disease.
57
What are the side effects of vincristine?
* Hair loss * Neuromuscular abnormalities * Paresthesia * Myelosuppression * GIT ulceration.
58
What is the mechanism of action of podophyllotoxins?
They bind to tubulin leading to mitotic arrest. ## Footnote Etoposide and teniposide inhibit DNA topoisomerase II leading to strand breaks.
59
What is the mechanism of action of podophyllotoxins?
It acts by binding to tubulin leading to mitotic arrest. ## Footnote Podophyllotoxins are used in cancer treatment due to their ability to disrupt cell division.
60
How do etoposide and teniposide exert their effects?
They act by inhibiting DNA topoisomerase II leading to strand breaks. ## Footnote These drugs are important in the treatment of various cancers.
61
What is a mechanism of resistance to podophyllotoxins?
Amplification of P-glycoprotein that facilitate drug efflux. ## Footnote This can lead to decreased drug efficacy.
62
List three therapeutic uses of podophyllotoxins.
* Monocytic Leukemia * Testicular cancer * Small cell carcinoma of the lung ## Footnote These uses highlight the versatility of podophyllotoxins in oncology.
63
What are the toxic effects associated with podophyllotoxins?
* Nausea * Vomiting * Alopecia * Hematopoietic and lymphoid toxicity ## Footnote These side effects can significantly impact patient quality of life.
64
What do camptothecins interfere with?
The activity of Topoisomerase I resulting in DNA damage. ## Footnote Camptothecins are important in treating specific types of cancers.
65
What is the active form of irinotecan?
SN-38 ## Footnote Irinotecan is a prodrug that is metabolized to this active inhibitor of Topoisomerase I.
66
List two therapeutic uses of topotecan.
* Metastatic ovarian cancer (cisplatin-resistant) * Small cell lung cancer ## Footnote Topotecan is used in cases where other treatments have failed.
67
What are the toxic effects of irinotecan?
* Severe diarrhea * Myelosuppression ## Footnote These side effects can be life-threatening and require careful management.
68
What is the mechanism of action of taxanes?
They are antimitotic agents that bind to tubulin and promote assembly of non-functional microtubules. ## Footnote This disrupts normal cell division.
69
What are the common toxic effects of paclitaxel?
* Neutropenia * Thrombocytopenia * Peripheral neuropathy ## Footnote Monitoring for these side effects is essential during treatment.
70
What is the primary therapeutic use of docetaxel?
Advanced breast cancer ## Footnote Docetaxel is often used in combination with other therapies.
71
How do anthracyclines exert their cytotoxic effects?
They intercalate between base pairs of DNA, inhibiting supercoiling and preventing DNA and RNA synthesis. ## Footnote This mechanism is critical for their effectiveness in chemotherapy.
72
What is a mechanism of resistance to anthracyclines?
Pleiotropic drug resistance due to P-glycoprotein production. ## Footnote This can lead to reduced effectiveness of treatment.
73
List three therapeutic uses of doxorubicin.
* Carcinomas of the breast * Endometrium * Ovaries ## Footnote Doxorubicin is a cornerstone in cancer treatment protocols.
74
What is the significant cardiac toxicity associated with doxorubicin?
Cumulative dose-related cardiac damage leading to dysrhythmias and heart failure. ## Footnote This necessitates careful monitoring of cardiac function during treatment.
75
What is dactinomycin primarily used for?
In treatment of gastrointestinal carcinoma with MTX. ## Footnote Dactinomycin has a unique mechanism and is used in specific cancer types.
76
What is the mechanism of action of bleomycin?
It forms a DNA-bleomycin-Fe2+ complex that leads to strand breaks in DNA. ## Footnote Bleomycin is cell cycle specific and acts at the G2 phase.
77
What are the therapeutic uses of bleomycin?
* Testicular cancer * Squamous cell carcinomas of the head and neck * Lymphomas ## Footnote Bleomycin is effective in a variety of tumor types.
78
What enzyme does L-asparaginase degrade?
L-asparagine ## Footnote This is significant in treating certain lymphoid cancers.
79
What are the side effects of L-asparaginase?
* Hemorrhage (due to clotting factor inhibition) * Hyperglycemia (due to insulin inhibition) * Hypoalbuminemia ## Footnote These side effects require monitoring and management during treatment.
80
What is the role of topoisomerase I and II in DNA replication?
Topoisomerase I nicks one strand to relieve supercoiling; Topoisomerase II removes two supercoils at a time. ## Footnote Inhibiting these enzymes is a strategy in cancer chemotherapy.

Oncology (2 decks)

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