DRUGS ACTING ON THE GONADAL AND REPRODUCTIVE SYSTEM, PROGESTINS, ANTIPROGESTINS
All right assam to come everybody let’s begin our lesson now all right so uh today we are going to talk more on the drugs which are acting on the gonadal and reproductive system and today our major focus would be on progestins and anti-progestins wait yes yes sir you’re right all right okay so uh after that wait a minute all right so today we’ll talk about
Progestins and antiprogestins okay and after that in one lecture i will cover up hormonal contraceptives and then uh in the other lecture i will talk about androgens and anabolic steroids and anti-androgens i can cover up literally all of these remaining topics in one lecture but i think it’s better if i break it into chunks and you guys are given time to
Think about it to read about it the reason why i uh i don’t uh make my lectures really wrong the reason is only this that i want you all to go back on that same topic using the textbooks that you have and then i want you to explore on that topic within that period only okay so do not leave it for the last moment so let’s start all right so the first one we
Will talk about progesterone and then we’ll talk about anti-progesterone i’m sure when i’ll say the terminology progestin so one of the hormones progesterone would definitely come up into your mind so let’s read about it what are they and how they’re benefiting us so the structure the most important natural progestin is progesterone okay uh wait a minute let
Me get the point okay so which is synthesized by ovaries testes and adrenaline adrenals synthetic progesterones include the 19 nor compounds such as nore ethyn drone all of these agents are potent oral progesterones derived from testosterone some have androgenic activity so several the uh several synthetic derivatives of progesterone have progesterone activity
Including megastrong medroxy progesterone acetate and hydroxy progesterone caparate gonads include noren gastimate and disogestal these agents have reduced androgenic activity drosperinone is a spiral lactone analog with anti-mineralocorticoid anti-androgenic and progesterone stational activity we’ll talk about these in more detail okay now is actions and
Pharmacological properties of progesterones progestins bind to intracellular receptors that alter the transcription of target genes i’m sure by now you must have understood how exactly proteins are manufactured so there are two isoforms of progesterone receptor just like the one we had for estrogen uh pra prb both are derived from the same gene progesterone
Slow the mitotic activity of the estrogen stimulated uterus cause vascularization of the endometrium i’m sure you all remember endometrium the layer which is the innermost one and induce a more glandular appearance and function why is it doing so because of the reason this drug is actually preparing uterus for the zygote to get implanted all right so progesterone
Slightly decrease triglycerides and hdl but they slightly increase ldl depending on the preparation and dose if you want to know more about hdl and ldl you should watch the video which i’ll upload in a while uh that would be related to the cardiovascular system it is actually made for your juniors but you can also look at it all right so uh depending on the
Preparation and wait a minute okay preparation and dose progestins also increase lipoprotein lipase so this is an enzyme that will break it up so progestins increase basal and stimulate it in lean secretion and stimulate appetite progesterone is extensively bound to cortical steroid binding globulin in the plasma and is not administered orally because of rapid
Hepatic metabolism progestins are eliminated by hydroxylation to uh pregnancy wait a minute pregnancy diol and conjugation with glucuronic acid and subsequent urinary excretion so the therapeutic uses are progestins are used for contraception alone or in combination with estrogens progestins may be administered orally by deport injection as a vaginal gel and
As a slow release intrauterine device these agents are used in the treatment of endometrial cancer and endometrial hyperplasia i’m sure you all must have remember hyperplasia means that the number of cells increase okay so what happens is you look here this is the hyperplasia of endometrium progestins control abnormal uterine bleeding especially let’s say when
There is a miscarriage so um and the ladies usually have spotting so then they take this medicine so that um and they hope it will work and you try and will get thick enough to support the baby um the fetus uh this uh so if you know it will be protected it will survive anyways so progestins are used to delay menstruation for surgical and post-operative reasons
And we also use it during hajj okay uh semigases used to stimulate appetite in patients with cancer or aids so these agents are used diagnostically to evaluate endometrial function in amenorrhea now let’s talk about anti progestins methylprestone ru486 it’s a brand name okay all right so before stone is a nor ethan drone derivative with potent anti-progesterone
And anti-glucocorticoid activities miflipristone acts as a competitive endergonist of progesterose neuron and glucocorticoid receptors method pristone has been approved for use to induce medical abortion in the first trimester so it is you it is combined with a parental or intravaginal application of prostaglandin 48 hours after the entire progestin to induce
Labor it causes myometrial contractions and blastocyte detachment and explosion explosion this combination is approximately 99 percent effective it is used as an emergency post cortical uh sorry post-coital contraceptive and is very effective if used within 72 hours of intercourse relatively infrequent side effects of mifra stone include bleeding nausea and
Abdominal pain thank you so much everybody i hope you all will study now
Transcribed from video
PROGESTINS AND ANTIPROGESTINS By Fiz Teach