Eximestane is one of the drug which is classified as aromatase inhibitor. And particularly Eximistane is an irreversible inhibitor of this enzyme aromatase. And this drug is used in the treatment of postmenopausal breast cancer.
But this drug is not indicated for the treatment of breast cancer in pre menopausal women because Aromatase enzyme is more significant in post menopause lumen compared with the pre menopausal woman. That’s why it is not indicated for the treatment of breast cancer in pre menopausalumen. And this Eczema stain is one of the steroidal drug. Because of its steroidal structure, this drug can strongly bind to this enzyme Aromatase. That’s why it acts as irreversible enzyme inhibitor.
So today in this we are going to see how this drug acts in the pre menopausal women. Ovary acts as an important source for production of estrogens from the ovary. Estrogens like estrodiol can be produced which can be converted into estrone. But in the post menopause lumen estrogens are not produced from the ovary because of menopause, they are going to be derived from the Androgens. So testosterone is one of the important source.
Exemestane tablets Mechanism precautions & side effects
And android is the androstein Dion. This testosterone can be converted into estrodiol and androstein Dion can be converted into estrone. Both of these conversions are mediated by one of the enzyme aromatase. That’s why exemptane blocks this enzyme. Thereby it inhibits the synthesis of estrogens from Androgens.
So this synthesis takes in the peripheral tissues which increases in soft estrogens. So circulatory estrogen levels are increased by the accurate of aromatase enzyme. So androstin Dione and Testosterone are the important source for estrogen synthesis in the post menopause lumen. And this conversion is mediated by the enzyme aromatase. So here Androstin Dione can be converted into estrone and testosterone can be converted into estrodiol.
This estrone can be converted into estrodiol. So the final mediator is the estrodiol which can act on the peripheral tissues which are responsive to the oestrogen. For instance, in the breast tissue, estrogen receptors are located within the cytoplasm where they are coupled with estrogen responsive elements. Now estradiol can bind to these estrogen receptors which is going to be dimerized and internalized within the nucleus to interact with the DNA. This produce the estrogen response resulting in the proliferation of the breast tissue leading to increased progression of breast cancer.
Ezmistin is a steroidal aromatase inhibitor. Because of its steroidal structure it can easily bind to this aromatase enzyme. Thereby it can inhibit the activity of this enzyme. When this enzyme is inhibited andostein Dione and estocerone cannot be converted into estrogens. So this results in the decrease in of estrogens in postmenopausal women.
When these estrogen levels are reduced, the activation of estrogen receptors is going to be reduced. So this results in the decreased proliferation and progression of breast cancer. In this way Eczemistain can be used for the treatment of breast cancer in postmenopausal women. Now let us the precautions of this drug. One of the important precautions of Eczemistain is that this drug can reduce the bone mineral density, so it can increase the risk of osteoporosis.
Particularly, this effect can also be observed with endodrug tamoxifen, which is a estrogen receptor antagonist. Since it’s the breast cancer, initially, tamoxifen can be used followed by Eczemistain. So both of these drugs can reduce the bone mineral density. So in such patients, this drug should be carefully given and the reduction of bone mineral density is more pronounced on prolonged treatment. So when this exemption is used for greater than one year, the bone mental density is going to be reduced.
Similarly, in the early stage of breast cancer, women may have some deficiency of vitamins. Particularly the 25 hydroxy vitamin deficiency can be observed in the woman with early stage of breast cancer. In such patients, Eczema stain should be carefully given. So before the treatment with Eczema stain, vitamin D level should be checked and during the treatment, vitamin D supplementation can be given. In order to reduce the deficiency observed in the early stage of breast cancer, this supplementation is more important as Eczemistain reduce a bone mineral density.
So if a woman is already having low vitamin D levels, it further increase the risk of bone fractures and osteoporosis. Similarly, eximistane can produce some fatal toxicity. So in the pregnant woman, this drug should not be used as it produced some harmfulness to the fetus. What are the side effects? The important side effect of Eczema stain is the hot flushes.
So women can experience some hot sensation with redness of the skin, particularly at the face, neck and arms, which is commonly observed with many of the hormone responsive tracts. Similarly, other side effects mainly include fatigue, arthrosia, joint pain, headache, insomnia, lack of sleep and excessive sweating can be observed with this eximistane. Now let us the chemical nature of this type. So this is a structure of eximistine. We can see that it is hang the steroidal nucleus.
So this structure is hang the androstane nucleus with two double bonds. So we can write this as androstar one four diane and we can also observe two ketone groups at third portion and 17th portion. So 317 Dion and a methylene group is attached at the 6th portion. So six methylene, that is a complete name of Eczemistaine. How it is given this drug is given as a tablet form at a strength of 20 FMG and this drug is given at a dose of 20 FMG as once daily after meal.
For early stage of breast cancer, this drug can be used as adjuvant after tamoxifen therapy up to five years. But for the advanced stage of breast cancer, this drug can be used for treatment after tamoxifen therapy. So that’s about this drug exemptane which is a steroidal aromatase inhibitor. Because of steroidal structure, it can produce irreversible inhibition of this enzyme. And this drug is indicated for the treatment of breast cancer in postmenopausal woman heart pressures.
Arthralgia and fitting are the important side effects produced by this drug. And when this drug is prescribed for longer periods, the bone mineral density may be reduced and vitamin D supplementation may be required in those patients with any deficiency of vitamin D. So that’s about this drug exemptane. That’s for today. Hope you have enjoyed this.
