Anticancer Drugs

Anticancer Drugs

ANTICANCER DRUGS ANTIMETABOLITES Fluorouracil-5

Methotrexate

ANTIBIOTICS Doxorubicin

Daunorubicin

ALKYLATING AGENTS Ifosfamide

Cyclophosphamide

MICROTUBULE INHIBITORS Vincristine

Vinorelbine

Vinblastine

STEROID HORMONES AND THEIR ANTAGONISTS Prednisone

Principles of Cancer Chemotherapy • Ideally, anticancer drugs should interfere only with cellular process that are unique to malignant cells. Unfortunately, most currently available anticancer drugs do not specifically recognize neoplastic cells but, rather, affect all proliferating cells- both normal and abnormal.

Antimetabolites •

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Antimetabolites are structurally related to normal compound within the cell.

Methotrexate Methorexate is structurally related to folic acid, and act as an antagonist of that vitamin by inhibiting dihydrofolate reductaes – the enzyme that convert folic acid to its active, coenzyme form, tetrahydrofolic acid (FH ).

Methotrexate • Therapeutic uses: MTX, usually in combination with other drugs, is effective against acute lymphoma in children, breast cancer, and head and neck carcinomas. In addition, low- dose MTX is effective as a single agent certain inflammatory diseases, such as severe psoriasis and rheumatoid arthitis

Methotrexate •

Adverse effects: 1. Commonly observed toxicities: to nausea, vomiting and diarrhea,. 2. Renal damage: Alkalinization of the urine and hydration help to prevent this problem. 3. Hepatic function: MTX may lead to fibrosis or cirrhosis Hepatotixic agent.

Methotrexate 4. Pulmonary toxicity 5. Neurologic toxicities 6. Contraindications: Because MTX is teratogenic in experimental animals and is an abortifacient, it should be avoided in pregnancy.

Alkylating Agents • Alkylation of DNA is probably the crucial cytotoxic reaction that is lethal to the tumor cell. They are used in combination with other agents to treat a wide variety of lymphatic and solid cancers. • Cyclophosphamide

Cyclophosphamide and Ifosfamide •

These drugs are very closely related mustard agents that share most of the same toxicities 1. Mechanism of action: Cyclophosphamide is the most commonly used alklating agent. Both cyclophosphamide and ifosfamide

Steroid Hormones and Their Antagonists •

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Prednisone is a potent, synthetic, antiinflammatory corticosteroid with less mineralocorticoid activity than cortisol. For patient with acute lymphocytic leukemia.

Prednisone • Mechanism of action: prednisone itself is inactive, and must first be reduced to prednisolone. • Adverse effects: prednisone has many of the adverse effects associated with glucocorticoids. It can predispose to infection (due to its immunosuppressant action) and to ulcers and pancreatitis.