Uses of Endosis: - Endometriosis Treatment of endometriosis. Hypersensitivity. Active venous thromboembolic disorder. Presence or history of arterial & CV disease (eg MI, CVA, ischemic heart disease); severe hepatic disease as long as liver function values have not returned to normal; benign or malignant liver tumors. DM w/ vascular involvement; known or suspected sex hormone-dependent malignancies; undiagnosed vag bleeding. Pregnancy. Childn prior to menarche.

Female Sex hormones

Dienogest acts as an agonist at the progesterone receptor (PR) with weak affinity that is comparable to that of progesterone but has a very potent progestagenic effect in the endometrium, causing endometrial atrophy after prolonged use. It promotes antiproliferative, immunologic and antiangiogenic effects on endometrial tissue. Dienogest reduces the level of endogenous production of oestradiol and thereby suppressing the trophic effects of oestradiol on both the eutopic and ectopic endometrium. Continous administration of dienogest results in hyperprogestogenic and moderately hypoestrogenic endocrine environment, which causes initial decidualization of endometrial tissue. It is an antagonist at androgen receptors, improve androgenic symptoms such as acne and hirsutism [A16570].

How to use Dienogest: Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Dienogest may be taken with or without food, but it is better to take it at a fixed time. Administration: May be taken with or without food. Adult Dose: 1 tab daily w/o interruption, taken preferably at the same time each day.

Increased clearance w/ enzyme inducers eg phenytoin, barbiturates, primidone, carbamazepine, rifampicin; oxcarbazepine, topiramate, felbamate, griseofulvin, nevirapine, St. John's wort-containing products. Increased plasma levels w/ enzyme inhibitors eg ketoconazole, itraconazole, fluconazole; cimetidine, verapamil; erythromycin, clarithromycin, roxithromycin; diltiazem; ritonavir, saquinavir, indinavir, nelfinavir; nefazodone, fluvoxamine, fluoxetine; grapefruit juice.

Hypersensitivity. Active venous thromboembolic disorder. Presence or history of arterial & CV disease (eg MI, CVA, ischemic heart disease); severe hepatic disease as long as liver function values have not returned to normal; benign or malignant liver tumors. DM w/ vascular involvement; known or suspected sex hormone-dependent malignancies; undiagnosed vag bleeding. Pregnancy. Childn prior to menarche.

Common - Acne - Headache - Depression - Breast discomfort Increased wt; depressed mood, sleep disorder, nervousness, loss of libido, altered mood; headache, migraine; nausea, abdominal pain or distension, flatulence, vomiting; acne; alopecia; back pain; breast discomfort, ovarian cyst, hot flush, uterine/vag bleeding including spotting; asthenic conditions, irritability.

There are limited data from the use of Dienogest in pregnant women. Animal studies and data from women exposed to Dienogest during pregnancy reveal no special risks on pregnancy, embryonic/fetal development, birth or development after birth for humans. However, Dienogest should not be administered to pregnant women because there is no need to treat endometriosis during pregnancy.Treatment with Dienogest during lactation is not recommended. Physiochemical properties and animal data indicate excretion of Dienogest in breast milk. A decision must be made whether to discontinue breastfeeding or to abstain from Dienogest therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.

Precaution: Obtain a complete medical history & perform physical & gynecological exam prior to initiation or reinstitution of therapy. Patients w/ history of extrauterine pregnancy or impairment of tube function, depression, chloasma gravidarum, gestational DM. Increased risk of MI or cerebral thromboembolism, DVT, pulmonary embolism; breast cancer, hepatic tumor. Adenomyosis uteri or uterine leiomyomata; recurrence of cholestatic jaundice &/or pruritus; persistent ovarian follicles. Rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Lactation. Adolescents (menarche to 18 yr).

Acute toxicity studies performed with Dienogest did not indicate a risk of acute adverse effects in case of inadvertent intake of a multiple of the daily therapeutic dose. There is no specific antidote. Dienogest 20-30 mg/day (10-15 times higher dose than in Dienogest) over 24 weeks of use were very well tolerated.

Keep in a cool and dry place. Protect from light. Keep out of the reach of children.

Female Sex hormones

Dienogest is a nortestosterone derivative with no androgenic but rather an antiandrogenic activity of approximately 1/3 of that of cyproterone acetate. Dienogest binds to the progesterone receptor of the human uterus with only 10% of the relative affinity of progesterone. Despite its low affinity to the progesterone receptor, dienogest has a strong progestogenic effect in vivo. Dienogest has no significant androgenic, mineralocorticoid or glucocorticoid activity in vivo. Dienogest acts on endometriosis by reducing the endogenous production of estradiol and thereby suppressing the trophic effects of estradiol on both the eutopic and ectopic endometrium. When given continuously, dienogest leads to a hypoestrogenic, hypergestagenic endocrine environment causing initial decidualization of endometrial tissue followed by atrophy of endometriotic lesions. Additional properties eg, immunologic and antiangiogenic effects, seem to contribute to the inhibitory action of dienogest on cell proliferation.

There are limited data from the use of Dienogest in pregnant women. Animal studies and data from women exposed to Dienogest during pregnancy reveal no special risks on pregnancy, embryonic/fetal development, birth or development after birth for humans. However, Dienogest should not be administered to pregnant women because there is no need to treat endometriosis during pregnancy.Treatment with Dienogest during lactation is not recommended. Physiochemical properties and animal data indicate excretion of Dienogest in breast milk. A decision must be made whether to discontinue breastfeeding or to abstain from Dienogest therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.