Dienogest

Dienogest is a Contraceptive agent belonging to the pharmacological class of Progestins.

Dienogest is FDA-approved for treating symptoms of endometriosis, including pelvic pain, in adults.

Dienogest rapidly absorbs and binds primarily to serum albumin (90%), bypassing corticosteroid-binding globulin (CBG) or Sex hormone-binding globulin(SHBG) upon oral intake. CYP3A4 mediates its complete metabolism, producing inactive metabolites swiftly excreted, mainly via urine, within 24 hours.

The most common side effects of Dienogest include acne, headache, depressed mood, breast discomfort, nausea, and ovarian cysts.

Dienogest is available as a tablets.

The molecule is available in India, the United States, Canada, the United Kingdom, Australia, Germany, France, Italy and Japan.

Dienogest is a Contraceptive agent belonging to the pharmacological class of Progestins.

Dienogest has a powerful progestagenic effect in the endometrium and, after prolonged use, causes endometrial atrophy. It functions as an agonist at the progesterone receptor (PR) with a weak affinity comparable to progesterone. On endometrial tissue, it stimulates antiproliferative, immunologic, and antiangiogenic effects. Dienogest inhibits oestradiol's trophic effects on the eutopic and ectopic endometrium by lowering the amount of oestradiol produced naturally. When dienogest is taken continuously, the body creates a moderately hypoestrogenic and hyper-progestogenic environment, leading to the first decidualization of endometrial tissue. As an antagonist of androgen receptors, it helps with androgenic symptoms like hirsutism and acne.

The time required for Dienogest typically takes several months to exhibit noticeable effects after administration.

The peak plasma concentration (Cmax) occurs within 1-2 hours after ingestion.

The time taken to reach peak plasma concentration (tmax) for Dienogest is approximately 1 to 2 hours after oral administration.

Dienogest is available as a tablet.

Tablet: To be swallowed whole with water/liquid. Do not chew, crush or break it. Doing this may release the entire dosage at once, raising the risk of adverse effects.

As the physician recommends, take the medication orally once as directed.

Endometriosis is a disorder in which the tissue similar to the womb's lining begins to increase outside of it. The most common symptoms are back or lower abdominal pain, menstrual pain, pain during and after sexual activity, constipation, diarrhea, and nausea. It may also make conception difficult. Dienogest works by stopping the growth of endometriosis tissue and the lining of your womb from occurring too quickly. This will help with the symptoms anyone might be experiencing. In addition to additional medications or treatments to help control endometriosis, this medication must be taken consistently.

Orally: Patients take Dienogest orally as tablets, swallowing them whole with water. Maintaining a consistent daily schedule for optimal effectiveness, regardless of meals, is advisable. Adhering actively to these instructions is crucial, as ensuring regularity in dosage, timing, and handling potential food interactions enhances the medication's efficacy and safety profile. Ensuring strict adherence to prescribed guidelines allows for the best possible management of the condition while minimizing the risk of complications.

The dosage and duration of treatment should be as per the treating physician's clinical judgment.

Dienogest is available in the form of tablets.

It is necessary to take the tablets consistently regardless of vaginal bleeding. A pack should always be started without interruption after it is finished.

If a patient misses taking a tablet, one should take one tablet immediately and then resume taking the next tablet at her regular time the following day. Vomiting, diarrhea, or missed tablets (if they happen within 3–4 hours of taking the tablet) may lessen Dienogest's effectiveness. A tablet that is not absorbed because of diarrhea or vomiting should also be replaced with one tablet.

Maintain optimal health by adopting fibrous foods, iron, essential fatty acids, and antioxidants diet. Consistent adherence to prescribed dosages and timing maximizes effectiveness. Inform healthcare providers of concurrent medications or supplements while taking Dienogest. Regular medical check-ups are advisable to monitor potential adverse effects. Promptly report any encountered side effects or unusual symptoms. Adherence to prescribed guidelines and seeking medical guidance ensures Dienogest's safe and effective use.

The dietary restriction should be individualized as per patient requirements.

The adverse reactions related to Dienogest can be categorized as

The clinically relevant drug interactions of Dienogest are briefly summarized here.

The common side effects of Dienogest include acne, headaches, depression, migraines, gastrointestinal disturbances, breast discomfort, nausea, vomiting, abdominal pain, abnormal menstrual bleeding, hot flushes, vaginal bleeding, asthenic conditions, weight gain, sleep disorders, nervousness, loss of libido, hair loss, back pain, breast enlargement, ovarian cysts, and irritability.

Pregnancy Category X (FDA): When pregnant, avoid using. The risks outweigh the potential benefits. There are safer substitutes available.

Data regarding dienogest use in pregnant women are limited. Studies on animals and data from pregnant women exposed to dienogest do not indicate any unique risks to human pregnancy, fetal development, birth, or postpartum health. However, since endometriosis does not need to be treated during pregnancy, Visanne should not be given to expectant mothers.

Preclinical evidence shows that there are no unique risks for human pregnancy, fetal or embryonic development, delivery, or postpartum development.

Using Dienogest for treatment during lactation is not advised.

Dienogest may or may not be excreted in human milk. Dienogest excretion in breast milk has been reported in animal studies. It is necessary to weigh the advantages of both therapy for the mother and breastfeeding for the child when deciding whether to stop nursing or not to use Dienogest.

As per FDA, the safety and efficacy of Dienogest in Pediatric patients have not been established.

As per the FDA, the safety and efficacy of Dienogest in elderly patients above 65 have not been extensively studied or established.

Kidney Impairment: Not studied.

Hepatic Impairment: Patients with severe liver disease, either past or present, should not take dienogest.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Dienogest.

Overconsumption of Dienogest could lead to nausea, vomiting, abdominal pain, and irregular vaginal bleeding.

There is no specific antidote or treatment for overdosage of Dienogest, so treatment typically involves symptomatic and supportive measures. If ingestion is recent, gastric lavage or activated charcoal might be considered to limit absorption.

If vomiting arises due to a Dienogest overdose, administer anti-nausea medications. Ensure hydration using intravenous fluids. Severe symptoms could require hospitalization for close monitoring. While Dienogest is metabolized in the liver and excreted through urine, enhancing elimination via diuresis or hemodialysis isn't expected to eliminate the drug significantly. Yet, these measures might be considered based on severity. Continuous observation is crucial for complications. Timely medical intervention plays a key role in managing Dienogest overdose, ensuring careful monitoring and proper care to address symptoms and prevent complications.

After prolonged use, dienogest causes endometrial atrophy and has a powerful progestogenic effect on the endometrium. Additionally, it mediates an antiandrogenic effect that is roughly one-third that of cyproterone acetate. A dosage of 2 mg has a slight inhibitory effect on FSH and LH but inhibits the growth of ovarian follicles at 10 mm and keeps progesterone concentration low. Dienogest 1 mg/kg also directly prevents ovulation. Dienogest therapy successfully decreased the unpleasant symptoms and endometriotic lesions linked to endometriosis in clinical trials involving patients with the condition. Since it doesn't activate either ERβ or ERβ, dienogest doesn't exhibit any antiestrogenic activity; instead, it has hypoestrogenic effects because it has been demonstrated to reduce the relative expressions of ERβ and ERα. Its effects are neither mineralocorticoid nor glucocorticoid. Dienogest conjunction therapy successfully lessens the symptoms of hirsutism and acne in combination with combined oral contraceptive pills (COCP) and ethinyloestradiol. It also improves excessively heavy or prolonged menstrual bleeding.

Dienogest taken orally is almost entirely absorbed quickly. After a single ingestion, peak serum concentrations of 47 ng/mL are attained in approximately 1.5 hours. Ninety-one per cent is bioavailable. Within the 1–8 mg dose range, dienogest has dose-proportional pharmacokinetics.

Dienogest cannot bind to corticoid-binding globulin (CBG) or sex hormone-binding globulin (SHBG); it is bound to serum albumin. 90% of the total drug concentrations in serum are nonspecifically bound to albumin, with 10% of the drug concentrations present as free steroids.

Dienogest has an apparent volume of distribution (Vd/F) of 40 L.

Dienogest is entirely broken down by the established steroid metabolism pathways, resulting in the production of metabolites that are primarily endocrinologically inactive. Studies conducted both in vitro and in vivo have shown that the primary enzyme involved in dienogest metabolism is CYP3A4. Dienogest is the predominant fraction in plasma that remains unchanged due to the rapid excretion of metabolites.

64 mL/min is the metabolic clearance rate (Cl/F) from serum.

There are two stages in the reduction of dienogest serum levels. The half-life (t½) of the terminal disposition phase is roughly 9–10 hours. Following oral administration of 0.1 mg/kg, dienogest is excreted as metabolites, which are expelled at a urinary-to-fecal ratio of approximately 3:1. The excretion of urinary metabolites takes place over a period of 14 hours. About 86% of the oral dose is eliminated within 6 days after administration; the majority of this amount is excreted within the first 24 hours, mainly in the form of urine.