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Chapter: Clinical Pharmacology: Antineoplastic drugs

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Vinca alkaloids

Vinca alkaloids are nitrogenous bases derived from the periwin-kle plant. These drugs are cell cycle–specific for the M phase and include: · vinblastine · vincristine · vinorelbine.

A subclass of antineoplastic drugs known as natural products in-cludes:

 

·                 vinca alkaloids

 

·                 podophyllotoxins.

 

 

Vinca alkaloids

 

Vinca alkaloids are nitrogenous bases derived from the periwin-kle plant. These drugs are cell cycle–specific for the M phase and include:

 

·                 vinblastine

 

·                 vincristine

 

·                 vinorelbine.

Pharmacokinetics

 

After I.V. administration, the vinca alkaloids are well distributed throughout the body.

Metabolism and excretion

 

Vinca alkaloids undergo moderate liver metabolism before being eliminated through different phases, primarily in stool with a small percentage eliminated in urine.

Pharmacodynamics

Vinca alkaloids may disrupt the normal function of the microtu-bules (structures within cells that are associated with the move-ment of DNA) by binding to the protein tubulin in the microtu-bules.

Separation anxiety

With the microtubules unable to separate chromosomes properly, the chromosomes are dispersed throughout the cytoplasm or arranged in unusual groupings. As a result, formation of the mitot-ic spindle is prevented, and the cells can’t complete mitosis (cell division).

Under arrest

 

Cell division is arrested in metaphase, causing cell death. There-fore, vinca alkaloids are cell cycle–specific for the M phase. Inter-ruption of the microtubule function may also impair some types of cellular movement, phagocytosis (engulfing and destroying micro-organisms and cellular debris), and CNS functions.

Pharmacotherapeutics

 

Vinca alkaloids are used in several therapeutic situations:

 

·                 Vinblastine is used to treat metastatic testicular cancer, lym-

·                 phomas, Kaposi’s sarcoma (the most common acquired immuno-deficiency syndrome [AIDS]–related cancer), neuroblastoma (a highly malignant tumor originating in the sympathetic nervous system), breast cancer, and choriocarcinoma.

·                 Vincristine is used in combination therapy to treat Hodgkin’s disease, non-Hodgkin’s lymphoma, Wilms’ tumor, rhabdomyosar-coma, and acute lymphocytic leukemia.

·                 Vinorelbine is used to treat non–small-cell lung cancer. Itmay also be used in the treatment of metastatic breast cancer, cisplatin-resistant ovarian cancer, and Hodgkin’s disease.

Drug interactions

 

Vinca alkaloids can interact with other drugs.

 

§    Erythromycin may increase the toxicity of vinblastine.

 

§    Vinblastine decreases the plasma levels of phenytoin.

 

§    Vincristine reduces the effects of digoxin.

 

§    Asparaginase decreases liver metabolism of vincristine, increas-ing the risk of toxicity.

 

§    Calcium channel blockers enhance vincristine accumulation, in-creasing the tendency for toxicity. (See Adverse reactions to vin-ca alkaloids.)

 

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