Norethindrone Acetate

DEA Class; Rx

Common Brand Names; Aygestin, Norlutate

Oral synthetic progestin with moderate androgenic and slight estrogenic activity relative to other progestins; norethindrone acetate a prodrug of norethindrone
Used as progestin-only (‘mini pill’) contraceptive and found in some combination oral contraceptives
Also used for hormonal imbalance (e.g., secondary amenorrhea, dysfunctional uterine bleeding, or endometriosis); in combination products for hormone replacement for postmenopausal women

Documented hypersensitivity

Arterial thromboembolic disease (stroke, MI), thrombophlebitis, DVT/PE, thrombogenic valvular disease, cerebral apoplexy

Known, suspected, or history of breast cancer; estrogen-dependent neoplasia, liver disease, liver tumors

Undiagnosed abnormal vaginal bleeding

Diabetes mellitus with vascular involvement

As diagnostic test for pregnancy

Norethindrone acetate is 2 times as potent as norethindrone

Patients with risk factors for arterial vascular disease (eg, hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (eg, personal history or family history of VTE, obesity, and systemic lupus erythematosus) should be managed appropriately

Family history of breast cancer and or DVT/PE, current/history of depression, endometriosis, DM, HTN, bone mineral density changes, renal/hepatic impairment, bone metabolic disease, SLE; conditions exacerbated by fluid retention (eg, migraine, asthma, epilepsy).

Discontinue if the following develop jaundice, any signs of VTE, migraine with unusual severity, significant blood pressure increase, increased risk of thromboembolic complications after surgery.

Discontinue medication pending examination if there is a sudden partial or complete loss of vision or if there is sudden onset of proptosis, diplopia, or migraine; if examination reveals papilledema or retinal vascular lesions, medication should be discontinued

Drug may cause some degree of fluid retention, conditions which might be influenced by this factor, such as epilepsy, migraine, cardiac or renal dysfunctions, may require careful observation

In cases of breakthrough bleeding, and in all cases of irregular bleeding per vagina,nonfunctional causes should be borne in mind; in cases of undiagnosed vaginal bleeding, adequate diagnostic measures indicated

Patients who have a history of clinical depression should be carefully observed and the drug discontinued if the depression recurs to a serious degree

Data suggest that progestin therapy may have adverse effects on lipid and carbohydrate metabolism; the choice of progestin, its dose, and its regimen may be important in minimizing these adverse effects, but these issues will require further study before they are clarified; women with hyperlipidemias and/or diabetes should be monitored closely during progestin therapy

Rare hepatic adenomas and focal modular hyperplasia, resulting in fatal intra-abdominal hemorrhage reported with therapy

Irregular menstrual bleeding is common with progestin only contraceptives; rule out nonpharmacologic causes of abnormal bleeding

Not for use prior to menarche

Pregnancy Category: X

Lactation: Excreted in breast milk; use caution