Metrinor

Metrinor2mg

Type:10 Tablets

Generic Name:Dienogest

Manufacturer:Popular Pharmaceuticals Ltd.

Price:500.00

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Indication

Treatment of endometriosis.

Administration

May be taken with or without food.

Adult Dose

1 tab daily w/o interruption, taken preferably at the same time each day.

Contraindication

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.

Mode of Action

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.

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).

Side Effect

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.

Interaction

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.

Alternative brand of Metrinor

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