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Anti Estrogens, SERM’s, Aromatase Inhibitors

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Yeah hi students i am dr badrinath in this video we will see the anti-is frozen easter eggs i have completed one video just to watch it after that you come to this video because it is a anti-estrogen serums scrum yes selective estrogen receptor modulator sems aromatase inhibitors here for different phases of the estrogen that we are going to four different

Parts of the estrogen see first estrogen i have completed natural estrogen synthetic estrogen the tunnel i have completed in the video my past video in this video we will complete all the remaining three parts anti-estrogen which works against the estrogen is called as a anti-estrogen clomiphene citrate full restaurant full western full restaurant like that you

Can remember clow my fin citrate next is so it works against the antistroger aromatase inhibitors it stops the synthesis of the estrogen so synthesis estrogen will not be there in the body estrogen will not be synthesized in the body okay and so that there is no effects of estrogen serums having a deal rule a very wonderful role like a tamax if and rallocks

If a number of times it was appeared in a competitive examination that we are going to be seeing it is having a dual action serums it is having a agonist property of historian antagonistic property of historian also both ok that point you have to keep in your mind very strongly strong fix fix fix okay and this is the syllabus unit 5 as per your university here

Read the point which i highlighted with the reading that is your syllabus is trojan okay first we will see anti-estrogen detail all three sections we will see in detail one by one we will see anti-estrogen which works against the estrogen so clone fin citrate first one tablets is available see here from aventis company very famous company clomid it is available

Clomiphene citrate anti-estrogen whenever in the body in the females body or in the male body excess estrogen is there then you have to take this tablets excess is frozen because it is doing some extra function unnecessary estrogen if is there excess then you have to take this tablet it acts as a pure antagonist in all the human tissues not only male the female

Also both it binds to both estrogen receptor er alpha is there here beta is there two types of receptors are there it has it got a two isomers which one this chlorophyll citrate juclomephene enclophine these are the two isomers one is c summary trans isomer same side trans opposite side cis means the same trans means against one is above one below like that some

Groups will be changed pharmacokinetics it is well absorbed orally orally you can be take okay it deposited in the adipose tissue fat tissue adipose tissue is nothing but a fat issue so it go and deposits in the fat long half life six days once you take a tablet six days need not to take that much of long half life so weekly one tablet like that you can keep

In your mind largely metabolized and excreted in the bile also bile bile secretion and indications when you have to take this clomiphene citrate clomiphene citrate indication when you have to take infertility due to the failure of ovulation when ovulation is failure see here reproductive system is not working because of in such a case you can give that long

Because excess estrogen will fail the pregnancy excess is closer normal estrogen is enough for it favors the pregnancy excess is frozen dangerous it acts like a contraceptive okay in such a case you can begin to add the in vitro fertilization see here in vitro that is in the test tube in the petri plate that how the sperm is coming and entering into the egg see

Here in vitro in vitro fertilization okay and also it is also useful in the oligospermia see here this is a normal sperm this is the oligosperm less spermatozoa in the male in such a case you can give this drug chlamyfin citrate anti-frozen one more drug is there full restaurant full western like that it is a seven alpha alkyl derivative it is also known as is

Very very important second point selective estrogen receptor down regulator down it downs to the regulation of the okay mechanism of action is there that is it binds with the estrogen receptor dimerization of the estrogen receptor so that estrogen receptor will become a weak it doesn’t interact with the estrogen because dimerization of estrogen receptor will

Be takes place this is the this is indication c when you have to give this drug means generally in the breast cancer doctors are prescribing tamoxifen see sometimes after if the patient is using for breast cancer tamoxifen for a longer time after one year or two years it doesn’t work time oxygen resistance will come in such a cases this drug is full restraint

You have to take okay injection is available see this is the injection 250 mg monthly im injection only monthly see here very good now monthly and the serums now we will come to the serums selective estrogen receptor modulator see these serums are very important it is having a dual action it works as a estrogen it works against the estrogen also it’s a very

Interesting one see keep in your mind estrogen will do good for our body and also estrogen will do bad for our body both whenever estrogen will do good for these serums will do a will encourage that estrogen whenever estrogen will do bad the serums will again is to the east region okay overall serums are good that point you have to keep in mind final goal of

Serum is body benefits it works against it works agonists select serums here you can see this is the goal this here i have explained i wrote the same point it produces a beneficial east frozen effect it produces beneficial estrogen effect in certain tissue whereas a producing antagonistic activity in the tissue such as a breast endometrium whereas a histogenic

Action may maybe when estrogen is harmful the serum will help you okay when estrogen is good serums also will help you however both finally default program serums are good default program this is the thing how it action seek core repressor it suppresses the estrogen receptor these are the that’s why estrogen receptor will become inactive here see co-activators

It activates the estrogen so estrogen receptor will become active see this inactive estrogen receptor will become active active estrogen receptor will become inactive due to the serums that is agonists are antagonists see here these serums will do make it mix of both so that’s why i shown the both color it becomes a partial partially active partially inactive like

That these serums will convert either active receptor inactive receptor finally it become optimized receptor partially active partially inactive okay and here finally we will get inactive here active ear okay like that it modifies tamoxifen citrate it is a non-steroidal compound tamoxifen it acts as a anti it is a very good tamoxifen see it works as an antagonist

Breast carcinoma cells and blood vessels that’s why this is a good agonist uterus cancer bone liver pituitary in such a case it acts as a agonist whereas i do good tamoxifen will do a good for it stops the breast cancer estrogen will cause is a breast cancer tamoxifen will stops the breast cancer okay and here what are the tamoxifen citrate estrogenic action

Decreases in total ldl improvement of bone mass very good bone mass because estrogen will reduces bone marrow whereas here stimulation of endometrial proliferation increases risk of deep v thrombosis anti-estrogenic action this is the thymosifene filling coated tablets it inhibits the human breast cancer cell that’s why it is good heart flushes uh heat from the face

Is called hot flashes pharmacokinetics it is effective orally excreted through the bile an indication when this tamoxifen is used primary best cancer first breast cancer tamoxifen breast cancer tamoxifen it is one of the biggest problem in indian population indian woman breast cancer is nowhere it is a leading so that’s why tamoxifen is having a bumper cells okay

Primary best cancer metastatic breast carcinoma male breast see male breast carcinoma also because it is used in the male breasts that is gynecomastia breast in the male is called a gynecomastia in that case also you can see that’s why here i kept the image gynecomastia here this breast development okay gynecomastia in that such a case this drug is very useful

Some other uses like a mccune arbitrary syndrome see here okay here i have defined what is a mechan herbality it affects the bone skin and cereal hormones and all this is the tamoxifen and cancer see here this is the estrogen see my cursor this is a estrogen this is estrogen receptor so when estrogen will go and binds here it forms a complex so estrogen receptor

Binds with the co activators like this okay that’s why it becomes a cancer estrogen will give a cancer tamoxifen molecule it go on binds with the estrogen receptor see here how it binds so that it avoids the co activators see co-activators will not come and joint with the estrogen receptor so that cancer will be stopped see here uterus cancer it is a tamoxifen

Will give a cancer of the uterus that is the biggest problem biggest problem it stops the breast cancer but it creates the uterus cancer here you can see tamoxifen it binds with the estrogen receptors okay here in the breast cancer it stops the co-activators whereas here it encourages the co-activators to come and join here that is the main problem co-activators

Will come and attract in the uterus cancer okay whereas in breast cancer co-activators will not come ralexifen it is a non-steroidal binding by binding to the both receptors er one and year two estrogen against bone and cardiovascular system antagonist endometrium here you can see dr redis is preparing the ralexif and hcl in forced banana basal women it is very

Very important it prevents the bone loss see all the women’s after menopause they will become very weak because bones will be lose one losing losing losing calcium in such a case rallocks if n is a good okay and these are the same it doesn’t elevate the post menopausal vasomotor symptoms the same running matter side effects of the relaxation these are the main

Hot flashes hot flashes means here she is feeling especially in the manifest hot flushes their face will become a heat intense feeling of the heat in the face is called as a hot flashes see this is the side effect hot flushes leg cramps vaginal bleeding increases the risk of deep vein thrombosis and uses it is approved in a second line agent for the prevention

And treatment of osteoporosis okay calcium you have to give regularly and you have to give generally hard flushes are common in the menopause and aromatize inhibitors see aromatize is a processor see here this is a process of aromatization in this process what happened testosterone will be converted into easter diol e2 estra diol ii this aromatization will be

Stopped by this aromatase inhibitor see here how ring a undergo a both are matched bringing a aromatization that is also important for that so this aromatization will give the estrogen aromatase inhibitors will prevent the synthesis of estrogen so aromatic inhibitors these are the group of drugs which inhibits the estrogen synthesis aromatization of the ring

Here of the testosterone is a final step for the production of estrogen same running matter aromatase inhibitors and the inactivators mechanism of action see non-steroidal steroid is there these are the eczema stage these are the example pharmaceutical anastrial azole letrozole very important very important names it binds the substrate binding site of aromatise

Whereas here it binds to heme part of the aromatize it is a reversible binding it is a irreversible binding steroidal non sub separately you have to learn the same process cholesterol is a starting material pregnant alone will come that is compulsory progesterone aldosterone see here our testosterone estradiol testosterone will be converted like this so whereas

The aromatase inhibitors are stopping this here also stopping here also stopping so that estrogen estradiol will not be formed example is letrozole tablets is available okay anastrozole tablets is also available which are orally active hundred percent bioavailability slow metabolism okay half life is 40 hours is there either and more anastrozole is more potent

Than the late result and x-mas stain is also there see here we can see okay one of the first generation of aromatase is amino glucose they inhibit the production of the estrogen in all the tissues body tissues wherever fat tissue uterine tissue breast wherever it may be like that it delays the reduction of the early breast cancer okay like that advantages and

Adverse effects of this thing accelerates the bone loss that is also some problems are there these are the advantages and finally this is the comparison as per your pharmacology tripathi book comparison of the serum aromatase inhibitors these are the aromatized inhibitor these are the serums tamoxifen we are comparing side by side not much important okay so i

End my session here thank you thank you for watching

Transcribed from video
Anti Estrogens, SERM's, Aromatase Inhibitors By PHARMA TRICKS FOR EXAMS