Introduction ,Classification: 1.Alkylating agents e.g. Chlorambucil, Mitomycin ,Cyclophosphamide ,Busulphan, Cisplatin 2.Antimetabolites e.g. Methotrexate ,Mercaptopurine ,Azathioprine ,Fluorouracil 3.Antibiotice e.g. Daunorubicin ,Actinomycin.

1. ANTI-NEOPLASTIC DRUGS
By SHAIKH SANIYA
M. Pharmacy

2. CONTENT• Introduction
• Classification: 1.Alkylating agents
1. Chlorambucil
2. Mitomycin
3. Cyclophosphamide
4. Busulphan
5. Cisplatin
2.Antimetabolites
1) Methotrexate
2) Mercaptopurine
3) Azathiopurine
4) Fluorouracil
3.Antibiotice
1. Daunorubicin
2. Actinomycin

3. INTRODUCTION
• Neoplasm (neo-new; plasm-form) is an abnormal growth of cells, also known
as a tumor. Neoplastic diseases are conditions that cause tumor growth.
• Cancer is not one disease but a group diseases affecting different organs and
systems of the body.
• The different forms of cancer possess certain feature:
1. It is a disease characterized by excessive cell
Proliferation. It is generally results in tumors
2. The tumor only ,expands in size but also invades
the surrounding cells and when nerve ending are affected
and pain is experienced.

4. 3.The cancer cells can detach themselves from the parent tumors move to another
location and new cancerous growth is established. This is called metastasis.

5. • A cancer cell that arises from mesodermal cells, is called
sarcoma.
• A tumor developed from all three embryonic layers is called
teratoma.

6. THERE ARE SEVEN SIGNS OF CANCER
ABBREVIATED AS CAUTION

7. • The drugs used in treating of neoplasm ae called antineoplastic drugs.
• Antineoplastic drugs are medications used to treat cancer.
• Antineoplastic drugs are also called anticancer, chemotherapy, chemo, cytotoxic,
or hazardous drugs.
• These drugs come in many forms.
• Some are liquids that are injected into the patient and some are pills that patients
take.

8. CLASSIFICATION
(1) Alkylating agents:- e.g. chlorambucil, busulfan, cyclophosphamide.
(2) Antimetabolites:- e.g. azathiopurine , fluorouracil, methotrexate,
mercaptopurines.
(3) Plant products:-vinca alkaloids
(4) Antibiotics :- e.g. actinomycin's , daunorubicin, mitomycin
(5) Miscellaneous:- e.g. cisplatin

9. ALKYLATING AGENTS
• An alkylating antineoplastic agent is an alkylating agent used in cancer treatment
that attaches an alkyl group to DNA.
• Alkylating agents are drugs that damage the DNA of cancer cells to keep them
from making more copies of themselves. They are the oldest type
of chemotherapy.
• Biological alkylating agents bring about alkylation of certain nucleophilic groups of
proteins and basic nitrogen e.g. DNA nucleosides
• Examples: chlorambucil, mitomycin , cyclophosphamide, busulphan and cisplatin

11. 1.CHLORAMBUCIL
Physical properties
• It is white crystalline powder having slight odor.
• Insoluble in water and soluble in alcohol and chloroform
Chemical properties
• The substance is treated with HCl and precipitated is washed with water.
• The washing when treated with potassium mercuric iodide, a buff colored
precipitate is obtained

12. Storage
• It is stored in tightly closed containers.
Uses : It is used to treat
1. Hodkinson disease
2. Chronic lymphocytic leukemia
3. Malignant lymphomas
4. Breast cancer
Pharmaceutical formulation : chlorambucil tablets
Brand name : lukeran

13. 2.MITOMYCIN
Physical properties
• It is blue violet crystalline powder
• Soluble in water
Stability & Storage
• It is stable at room temperature but is affected by air and light.
• It is stored in tightly closed containers.

14. Uses
1. Stomach cancer
2. Breast cancer
3. Lung cancer
4. Bladder cancer
5. Cervical cancer
Pharmaceutical formulation : mitomycin injection.
Brand name: mutamycin

15. 3.CYCLOPHOSPHAMIDE
Physical properties:
• White crystalline powder.
• Odorless and bitter taste.
• Soluble in water and alcohol.
• Its 2% solution has a pH 4 to 6
Chemical properties :
1. When its aqueous solution is boiled with silver nitrate solution, a white precipitate
is obtained.
2. It is oxidized in liver to give phosphamide mustard with the loss of acrolein.

16. Stability & Storage
• It is discolored on exposure to light and is unstable at temperature 30oC.
• It is stored in tightly closed, light resistant containers.
Uses
1. Breast cancer
2. Hodkins disease
3. Malignant lymphomas
4. Ewing's sarcoma
5. Neuroblastoma
6. Myeloma

17. Pharmaceutical formulation : cyclophosphamide injection.
cyclophosphamide tablets
Brand name: cycloxan, endoxan- Asta

18. 4.BUSULPHAN
Physical properties
• It is white crystalline powder
• odorless.
• Slightly soluble in water and soluble in acetone.
Chemical properties:
1. When it is heated with sodium hydroxide solution, it gives an intense,
characteristic pyridine like odor.
2. It Alkylates cysteine residue in protein.

19. Stability & Storage
• It is affected by air and light hence
• It is stored in tightly closed containers & light resistant containers
Uses
1. myelosclerosis
2. Chronic myeloid leukemia
3. Chronic granulocytic leukemia
4. Thrombocythemia

20. Pharmaceutical formulation : busulphan tablets
Brand name: busulfan , myelosam, myeleukon

21. 5.CISPLATIN
• Physical properties
• It is a white lyophilized powder.
• It melts at 207oC.
• It is slightly soluble in water and sparingly soluble in dimethylformamide.
Storage
It is stored in tightly closed containers

22. Uses
• Metastatic testicular carcinoma
• Metastatic ovarian carcinoma
• Advanced bladder carcinoma
• Cervical cancer
• Head and neck cancer
Pharmaceutical formulation : cisplatin injection
Brand name: platinol, aquaplat

23. ANTIMETABOLITES
• Antimetabolites are used in cancer treatment as they interfere with DNA production
and therefore cell division and tumor growth.
• Antimetabolite drugs are commonly used to treat leukemia, cancers of the breast,
ovary, and the gastrointestinal tract, as well as other types of cancers.
• Examples :
1) Methotrexate
2) Mercaptopurine
3) Azathiopurine
4) Fluorouracil

24. 1.METHOTREXATE
Physical properties
• It occurs as yellow to orange crystalline powder.
• It is slightly soluble in water
• Fully soluble in dilute solution of alkali hydroxides and carbonates.
Stability & Storage
• It is affected by air and light hence
• It is stored in tightly closed containers & light resistant containers

25. Uses: It is used to treat
1. Acute lymphocytic leukemias
2. Acute non-lymphocytic leukemias
3. Breast carcinoma
4. Ovarian cancer
5. Osteosarcoma
6. Head and neck cancer
7. Severe psoriasis
8. Medulloblastoma
9. Dermatomyositis

26. Pharmaceutical formulation : methotrexate injection
methotrexate tablet
Brand name: Biotrexate, Neotrexate

27. 2.MERCAPTOPURINE
Physical properties
1. It is yellow crystalline powder and is odorless.
2. It is slightly soluble in water but soluble in solution of alkali hydroxides.
Chemical properties
1. When saturated alcoholic solution is treated with alcoholic mercuric acetate
solution, a white precipitate is obtained.
2. When alcoholic solution is warmed with alcoholic lead acetate solution ,a yellow
precipitate is obtained.

28. Stability & Storage
• It is affected by air and light hence
• It is stored in tightly closed containers & light resistant containers
Uses : It is used to treat
1. Acute lymphatic leukemia.
2. Acute myelogenous leukemias
3. Chronic granulocytic leukemia
4. Nephrotic syndrome
5. choriocarcinoma

29. 3.AZATHIOPURIN
It is a chemotherapy drug that works by slowing or stopping the growth
of cancer cells.
Physical properties
1. It is pale yellow powder and is odorless.
2. Insoluble in water
3. Soluble in dilute alkali hydroxide
Chemical properties
When it is treated with Zn powder and HCl, the NO3 group is reduced to NH3 group.
The compound thus obtained is treat with NaNO2,,sulphamic acid and beta naphthol
solution is added. A pale pink color is produced.

30. Stability & Storage
• It is affected by air and light hence
• It is stored in tightly closed & light resistant containers
Uses : It is used treat acute lymphocytic leukemia
Pharmaceutical formulation : Azathiopurine injection
Azathiopurine tablet
brand name: Purinethol, Azamune

31. 4.FLUOROURACIL
Physical properties
• It is white powder
• odorless.
• Soluble in water and very slightly soluble in alcohol.
Stability & Storage
• It is affected by air and light hence
• It is stored in tightly closed & light resistant containers

32. • Uses :
1. Solar keratoses
2. It is used to treat neoplasm of
a) Gastro intestinal tract
b) Breast and pancreas
c) Respiratory tract
Pharmaceutical formulation: fluorouracil injection
Brand name: Flucel

33. ANTIBIOTICS
• Chemotherapy antibiotics are not
the same as the ones used to fight
bacterial infections.
• They inhibits the synthesis of
DNA and RNA.
• Antibiotics are used against
leukemia, bladder cancer,
testicular cancer, and sarcomas.

34. 1.DAUNORUBICIN
Physical properties :
1. Red crystalline powder
2. Available as lyophilized powder
3. Soluble in water.
Stability & Storage
• It is stable at room temperature
• It is stored in tightly closed & light resistant containers

35. Uses :
It is used to treat acute lymphocytic and granulocytic leukemias.
Brand name: cerubidine , cerubicide.

36. 2.ACTINOMYCIN
Physical properties
1. Bright red crystalline powder.
2. Lyophilized powder
3. Slightly soluble in water
4. Soluble in alcohol.
Stability & Storage
• It is affected light ,excessive heat and moisture hence
• It is stored in tightly closed & light resistant containers

37. Uses :
1. Wilms tumors
2. Ewing's sarcoma
3. Choriocarcinoma
4. Pelvic or limb tumors
Pharmaceutical formulation: dactinomycin injection
Brand name: lyovac, cosmagen

38. TERMS USED:
1. Teratoma : A tumor developed from all three embryonic layers is called teratoma.
2. Sarcoma : It is the general term for a broad group of cancers that begin in the
bones and in the soft (also called connective) tissues (soft tissue sarcoma).
3. Metastasis : The cancer cells can detach themselves from the parent tumors move
to another location and new cancerous growth is established. This is called
metastasis.

39. THANKYOU