Hormones

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Chapter: Medicinal Chemistry : Antineoplastic Agents

Hormones: Mitotane, Diethylstilbesterol, Progesterone, Prednisone, Tamoxifen, Letrozole


Antineoplastic Agents - SYNTHESIS AND DRUG PROFILE

Hormones

 

Mitotane


Synthesis


Properties and uses: It is indicated only for treating adrenal cortex carcinoma.

 

Diethylstilbesterol


Synthesis


Properties and uses: Diethylstilbesterol is a white crystalline powder, practically insoluble in water, and soluble in alcohol and alkali hydroxides solutions. It is used for pallative therapy and produces relief in primary as well as metastatic prostrate carcinoma.

Assay: Dissolve the sample in ethanol and dilute with the same solvent. To the resulting solution, add dipotassium hydrogen phosphate solution. Prepare in the same manner, a reference solution using diethylstilbestrol reference standard. Irradiate with mercury lamp and measure the absorbance of the irradiated solutions at the maximum of 418 nm, using water as a blank.

Dosage forms: Diethylstilbestrol pessaries B.P., Diethylstilbestrol tablets B.P.

 

Progesterone


17-Acetyl-10,13-dimethyl-1,7,8,10,11,12,13,15,16,17-decahydro-2H-cyclopenta[a]phenanthren-3(6H,9H,14H)-one

Synthesis


Properties and uses: Progesterone exists as white crystalline powder or colourless crystals, practically insoluble in water, soluble in ethanol, sparingly soluble in acetone and fatty oils. Progestins are pallative in 50% cases of advanced and metastatic endometrial carcinoma.

Assay: Dissolve the sample in alcohol, dilute with the same solvent, and measure the absorbance at 241 nm using ultraviolet spectrophotometer.

Dosage forms: Progesterone injection B.P.

 

Prednisone


Synthesis


Properties and uses: Prednisone is a white crystalline powder, practically insoluble in water, slightly soluble in alcohol and methylene chloride. It is predominantly used in cancer chemotherapy, and in the treatment of acute exacerbations of multiple sclerosis. In paediatrics, it is widely used to treat nephrosis, rheumatic caslitis, leukaemia, and tuberculosis.

Assay: Dissolve the sample in alcohol, dilute with the same solvent, and measure the absorbance at 238 nm using ultraviolet spectrophotometer.

 

Tamoxifen


Synthesis


Properties and uses: Tamoxifen citrate is a white crystalline powder, slightly soluble in water and acetone, but freely soluble in methanol. It is a nonsteroidal antiestrogen for palliative therapy of breast cancer in postmenopausal women. The drug competes with estrogens for cytosol estrogen receptors, and thus, blocks estrogens effects in the target tissue.

Assay: Dissolve the sample in anhydrous acetic acid and titrate with 0.1 M perchloric acid using naphtholbenzein as indicator.

Dosage forms: Tamoxifen citrate tablets I.P., Tamoxifen tablets B.P.

 

Letrozole


Synthesis


Properties and uses: Letrozole is a white or yellowish crystalline powder, practically insoluble in water, soluble in methylene chloride, and sparingly soluble in methanol. It is used for the treatment of breast carcinoma.

Assay: It is assayed by adopting liquid chromatography technique.

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