Classification :1. Progesterone derivatives 2. 19-Nor testosterone derivatives. Progestogens: i. Progesterone (Alza) ii. Hydroxyprogesterone caproate iii. Norethindrone (Norethiesterone, Micronor) iv. Norgestrel (Ovrette, Ovval)
Steroids - Drugs Acting on Endocrine System
PROGESTOGENS
The natural
progestational hormone or progestogen is progesterone, which is secreted mainly
by the corpus luteum in the second part of the menstrual cycle. Small amounts
are also secreted by the testis in the male and the adrenal cortex in both
sexes, and large amounts are secreted by the placenta.
Progestogens
could be broadly classified into two major classes:
1. Progesterone derivatives
2. 19-Nor testosterone derivatives
Synthesis
Method-I From: Diosgenin
Method-II From: Ergosterol
Properties: It exists as white crystalline powder, insoluble in water and in
alcohol.
Dose: The dose for uterine bleeding is 5–10 mg injected per day up to
5–10 days. For habitual abortion, the dosage is 5–20 mg twice or thrice a week
by IM injection.
Synthesis
Properties and uses: It exists as white crystalline powder, insoluble
in water, it is more potent than progesterone, and has longer duration with
short onset of action.
Synthesis
Properties and uses: It exists as white crystalline powder, insoluble
in water. It is an important oral contraceptive and has the ability to postpone
menstruation and prevent ovulation by suppressing pituitary gonadotropin. It is
used in combination with mestranol and ethinestradiol.
Assay: Dissolve the sample in tetrahydrofuran, add silver nitrate, and
titrate the solution with 0.1 N NaOH. Determine the end point
potentiometrically.
Dose: The oral dose for contraception is 2.5–10 mg daily for 21 days.
Synthesis
Properties and uses: It exists as white crystalline powder, insoluble
in water, slightly soluble in alcohol. Used as an oral contraceptive.
Dose: The oral dose as a single agent is 75 μg per day.
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