IMMUNE PHARMACOLOGY-PART-III

ANTI CANCER DRUGS-1.ALKYLATING AGENTS

The anticancer drugs are coming under many classifications as we have seen in the previous post. Here we deal with the first one by the chronological order.

A.Alkylating Agents:-

1.Nitrogen Mustards and Nitroso-ureas:-

These are a group of cell cycle-nonspecific compounds that transfer an alkyl group usually to the 7th nitrogen atom of the guanine residues in one or both strands of DNA and thereby disrupt the DNA growth and kill the cell.

Mechlorethamine: 

This drug binds with the N-7 atom of guanine in DNA. This in turn leads to the damage of the DNA strand by cross-linking and thereby killing the cell.

Uses

Used as one of the ingredients in the treatment recipe for Hodkin's Disease

The Recipe is MOPP:-

1Mechlorethamine

2.Oncovin(Vincristine)

3.Procarbazine

4.Prednisone

Used in non-Hodkin's lymphomas 

Administered via I.V. route.

Side effects:-

1.Bonemarrow suppression.

2.Nausea and vomiting.

3.Lacrimation (Tears flow)

Cyclophosphamide 

This drug is metabolized to an active metabolite, phosphoramide mustard a nitrogen mustard compound have the same mechanism of action of crosslinking the DNA strand of the cancerous cell and thereby killing it.

Cyclophosphamide is metabolized in the liver by a cytochrome-P-450 enzyme.

Uses

1.Ovarian and breast carcinoma

2.Hodkin's and non-Hodkin's lymphomas

3.All kinds of leukemias like acute and chronic lymphocytic leukemia

4.Multiple myeloma

5.Neuroblastoma

6.Lung cancer

7.Wilm's tumor

8.Cervix sarcomas

9.Testis sarcomas

10.Soft tissues sarcomas

11.As an immunosuppressive agent in organ transplantations

Administered by mouth.

Side effects:-

1.Hemorrhagic cystitis

2.Nausea and vomiting

3.Bone marrow suppression

4.Skin pigmentation

5.Severe alopecia(Hair loss)

6.Gonadal suppression

Melphalan

It is phenylalanine, an amino acid derivative of nitrogen mustard. The mechanism of action is cross-links with DNA and RNA and thereby kill the cells.

Uses

1.Ovarian and breast cancers

2.Multiple myeloma

Side effects

1.Bone marrow suppression

2.Leucopenia

3.Thrombocytopenia

Chlorambucil

A nitrogen mustard compound have similar action

Uses

1.Chronic lymphocytic leukemia

2.Primary macroglobulinemia

3.Hodkin's disease

4.Non-Hodkin's lymphomas

2.Ethyleimines and Methylimines-Hexamethylemelamine:-

Hexamethylemelamine:-

It is used in Ovarian cancer

Thiotepa  

It is used in Bladder, breast and ovarian cancers 

3.Alkylsulphonates

1.Busulphan:-

Acting by cross-linkage

Uses

1.Chronic granulocytic leukemia

2.Chronic myelocytic leukemia

Side effects

1.Bone Marrow Suppression

2.Hyperuricemia

3.Amenorrhea

4.Impotence

....To be continued in next post