Classification of Neoplastic Drugs

CLASSIFICATION OF NEOPLASTIC DRUGS

Q. 1 Which is not an Antimetabolite? 
 A

Methotrexate

 B 5 Fluorouracil 
 C

Gemcitabine

 D Vinca alkaloids
Q. 1 Which is not an Antimetabolite? 
 A

Methotrexate

 B 5 Fluorouracil 
 C

Gemcitabine

 D Vinca alkaloids
Ans. D

Explanation:

Vinca alkaloids REF: Harrison’s 17th edition chapter 8, KDT, Goodman Gillman

See APPENDIX-37 for “CLASSIFICATION OF CANCER CHEMOTHERAPY AGENTS”


Q. 2 All are true about Ifosfamide except 
 A

It is nitrogen mustard

 B

Metabolised by CYP3 A4 to form active metabolite

 C

Chloracetaldehyde is active form

 D

Less neurotoxic than cyclophosphamide

Q. 2 All are true about Ifosfamide except 
 A

It is nitrogen mustard

 B

Metabolised by CYP3 A4 to form active metabolite

 C

Chloracetaldehyde is active form

 D

Less neurotoxic than cyclophosphamide

Ans. D

Explanation:

Less neurotoxic than cyclophosphamide [Ref: K.D.T. 6/e p 822; Goodman Gilman 11/e p 1327­1328]

  • Ifosfamide is a synthetic analogue of cyclophosphamide.
  • It is a nitrogen mustard alkylating agent.
  • Ifosfamide is a cyclophosphamide analogue thus it has all the potential adverse effects of cyclophosphamide.
  • Ifosfamide metabolite, rather than the parent drug is responsible for toxicity of Ifosfamide.
  • Ifosfamide is a prodrug that requires metabolic activation by microsomal liver enzymes to produce biologically active compounds.
  • Activation is mediated by cytochrome p450 – CYP3A4 and deactivated by CYP3A-4 AND CYP2B6.
  • The metabolic activation of Ifosfamide is an autoinducible process and besides producing active cytotoxic
  • metabolites it also results in generation of some toxic metabolic byproducts that are responsible for its side effects.
  • The two well known toxic nzetabolities of Ifosfamide are acrolein and chloracetaldehyde.

“Acrolein is responsible for Ifosfamide induced hemorrhagic cystitis where as chloroacetaldehyde is responsible for renal tubular damage and neutrotoxicity”.

  • Acrolein                                   – Hemorrhagic cystitis
  • Chloroacetaldehyde             – Nephrotoxicity (Renal tubular danage)

– Neurotoxicity

  • At equivalent doses, the rate of chloroacetaldehyde generation with ifosfamide is 40 times greater than with cyclophosphamide.

-This explains why cyclophosphamide although structurally related has virtually no nephrotoxicity and less neurotoxic.

Goodman Gilman Says

–   At equivalent doses, the rate of chloroacetaldehyde generation with ifosfamide is 40 times greater than with cyclophosphamide therefore it produces more platelet suppression, neurotoxicity, urothelial damage.

Neurotoxicity in ifosfamide

  • Neurotoxity in ifosfamide is caused by the active metabolite of ifosfamide i.e., chloralacetaldehyde
  • These metabolites enter brain and produce neurological symptoms which are encephalopathy and seizure.
  • These symptoms almost always resolve with discontinuation of the drug.
  • Patients who have mild to moderate symptoms can continue to receive the drug.

Q. 3

Ifosfamide belongs to which group of anticancer drugs‑

 A

Alkylating agents

 B

Antiimetobolites

 C

Mitotic inhibitors

 D

Topoisomerase inhibitors

Q. 3

Ifosfamide belongs to which group of anticancer drugs‑

 A

Alkylating agents

 B

Antiimetobolites

 C

Mitotic inhibitors

 D

Topoisomerase inhibitors

Ans. A

Explanation:

Alkylating agents [Ref: KDT 6 th/e p. 822; Goodman & Gilman 111h/e p. 1328]

  • Ifosfamide belongs to alkylating agent.
  • It is an analogue of cyclophosphamide.
  • It is used in combination for germ cell testicular cancer and is widely used to treat pediatric and adult sarcomas. Adverse effect of If osfamide:-
  • Ifosfamide has virtually the same toxicity profile as cyclophosphamide although it causes greater platelet suppression, neurotoxicity, nephrotoxicity and in the absence of mesna, urothelial damage.
  • When it is used in high doses (myeloablative doses) it causes severe neurological toxicity.
  • When it is used in nonmyeloablative or low doses it causes severe urinary tract abnormalities. Intravenous mesna is given together with ifosfamide to prevent urinary tract adverse effects.

Quiz In Between


Q. 4

Cyclophosphamide is?

 A

Alkylating agent

 B

Antitumor antibiotic

 C

Monoclonal antibody

 D

Antimetabolites

Q. 4

Cyclophosphamide is?

 A

Alkylating agent

 B

Antitumor antibiotic

 C

Monoclonal antibody

 D

Antimetabolites

Ans. A

Explanation:

Ans. is ‘a’ i.e., Alkylating agent


Q. 5

All are alkylating agents, except

 A

5-FU

 B

Melphalan

 C

Cyclophosphamide

 D

Chlorambucil

Q. 5

All are alkylating agents, except

 A

5-FU

 B

Melphalan

 C

Cyclophosphamide

 D

Chlorambucil

Ans. A

Explanation:

Ans. is ‘a’ i.e., 5 Fluorouracil


Q. 6

Which is not an Antimetabolite?

 A

Methotrexate

 B

5 Fluorouracil

 C

Gemcitabine

 D

Vinca alkaloids

Q. 6

Which is not an Antimetabolite?

 A

Methotrexate

 B

5 Fluorouracil

 C

Gemcitabine

 D

Vinca alkaloids

Ans. D

Explanation:

Ans. is ‘d’ i.e., Vinca alkaloids

Quiz In Between


Q. 7

Alkylating agents are all except ‑

 A

Buslfan

 B

Carmustine

 C

Dacarbazine

 D

Etoposide

Q. 7

Alkylating agents are all except ‑

 A

Buslfan

 B

Carmustine

 C

Dacarbazine

 D

Etoposide

Ans. D

Explanation:

Ans. is `d’ i.e., Etoposide


Q. 8

Nitrosoureas used in the treatment of cancer are‑

 A

Carmustine

 B

5FU

 C

Methotrexate

 D

Cisplatin

Q. 8

Nitrosoureas used in the treatment of cancer are‑

 A

Carmustine

 B

5FU

 C

Methotrexate

 D

Cisplatin

Ans. A

Explanation:

Ans. is ‘a’ i.e., Carmustine

Nitrosoureas

  • Nitrosoureas (Lomustine and carmustine) are highly lipid soluble alkylating agents – cross blood – brain barrier → Effective in meningeal leukaemias and brain tumours.
  • Nitrosoureas are highly lipid soluble and can cross blood brain barrier used in brain tumors like gliomas.
  • Because they cross BBB, most common adverse effects are nausea, vomiting and other CNS effects.
  • Bone marrow depression is peculiarly delayed, taking nearly 6 weeks to develop. → delayed neutropenia
  • Nitrosoureas can cause visceral fibrosis and renal damage.

Q. 9

Methotrexate is what class of anti cancer drug ‑

 A

Alkylating agents

 B

Antimetabolites

 C

Microtubule damaging agents

 D

Topoisomerase inhibitors

Q. 9

Methotrexate is what class of anti cancer drug ‑

 A

Alkylating agents

 B

Antimetabolites

 C

Microtubule damaging agents

 D

Topoisomerase inhibitors

Ans. B

Explanation:

Ans. is ‘b’ i.e., Antimetabolites 

Quiz In Between



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