Medrogestone

Medrogestone Uses, Dosage, Side Effects, Food Interaction and all others data.

Medrogestone (INN), also known as 6,17α-dimethyl-6-dehydroprogesterone, is a progestational agent derived from 17-methylprogesterone. It was conceived as an alternative for an orally effective contraceptive option. It was developed by Ayerst, approved in Canada in 1969 and its current status is cancelled post-marketing. It was never approved by the FDA.

Medrogestone was created as a more potent and orally active option of progesterone. In pre-clinical trials, medrogestone was proven to have four times more progestational activity than progesterone with a similar duration effect than the one found for 17-hydroxyprogesterone. Medrogestone was also able to maintain pregnancy and prevented ovulation in ovariectomized rats. Administration of medrogestone, alone or with premarin, prevented pregnancy, as well as it suppressed ovarian weight increase by nearly 100% of the tested individuals. Medrogestone does not produce any androgenic effect but it presented a marked anti-androgenic effect. It did not present an oestrogenic effect, nor changes in organ weight or histological appearance in adrenal glands or thymus and it does not present any anti-inflammatory effects.

Medrogestone
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Medrogestone
Generic	Medrogestone
Medrogestone Other Names	Medrogestone
Type
Formula	C₂₃H₃₂O₂
Weight	Average: 340.507 Monoisotopic: 340.24023027
Protein binding	Medrogestone, as presented for all progestogens, is highly bound to plasma proteins. It is mainly bound to albumin but it also binds to other plasma proteins like sex hormone binding globulin or corticosteroid-binding globulin. The pharmacokinetics of medrogestone will depend on the degree of plasma protein bindind which makes this characteristic the main regulator of the tissue availability of medrogestone.
Groups	Approved, Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Medrogestone is a progestin used as an adjunct to control secondary amenorrhea and dysfunctional bleeding in adolescent and adult females, and treat endometrial shedding in menopausal women.

Medrogestone is indicated as adjunct to treat endometial shedding in menopausal women, to treat secondary amenorrhea, to induce menses and to treat dysfunctional uterine bleeding in adult and adolescent women.

Medrogestone is also used to associated treatment for these conditions: Hormone Replacement Therapy

How Medrogestone works

Medrogestone is a progestogen, thus its action is done under the same profile. These type of molecules are steroid hormones that bind and activate the progesterone receptor. Its action may involve the suppression of gonadotropic hormones from the anterior portion of the pituitary gland and secondary suppression of testosterone. Medrogestone presents structural similarities to testosterone which allows it to compete for the androgen-receptor-protein receptor sites in prostatic cells. Administration of medrogestone diminishes the response to endogenous hormones in tumor cells due to a reduction in hormone steroid receptors; this effect will translate into cytotoxic or antiproliferative effects.

Toxicity

There were reports of increased urinary flow rates and total micturition volumes as well as sexual dysfunction and hyperglycemia.

Food Interaction

No interactions found.

Elimination Route

When administered, medrogestone presents a very rapid gastrointestinal absorption with a bioavailability of 100%. The maximum serum concentration of medrogestone is 10-15 ng/ml.