药品信息:

类别:雌激素、黄体酮及类似合成药（Oestrogens & Progesterones & Related Synthetic Drugs）

适应症：绝经后妇女的更年期症状，如潮热、阵发性出汗、睡眠障碍、情绪抑郁、易怒、头痛及头晕，预防妇女绝经后骨矿物质丢失，治疗萎缩性阴道炎。

用法用量：1片/日，连续口服。应在停经1年后开始治疗。如果由序贯雌激素疗法转换为本药，应在月经后开始用药，即为序贯激素治疗周期开始当日用药。

注意事项：开始治疗前，应作全面体格检查，特别是血压，乳房及腹部和妇科检查。定期检查肝功能。如果阴道流血或滴血持续发生，或在治疗停止后短期内发生，则有必要作活检以排除恶性子宫肿瘤的可能性。如发生静脉血栓栓塞，黄疸，偏头痛突然发作，突然的视力障碍，血压显著升高应立刻停药。

禁忌：已知或疑有乳癌、雌激素依赖性肿瘤（如子宫内膜癌），有乳癌病史者，代谢性卟啉病患者。

剂型规格：片剂：（日历盘包装）28片

FDA批准的治疗内分泌病新药--Activella片剂
Activella是雌二醇和炔诺酮醋酸酯联合用药的血管舒缩症状，外阴及阴道萎缩，与绝经相关的用于治疗骨质疏松症。 Activella提供含有1毫克和0.5毫克雌二醇炔诺酮醋酸酯肠溶片。 Activella是由诺和诺德销售。
2002年3月8日報導──據《Menopause》雜誌1/2月份報導的一項多中心、前瞻性隨機雙盲臨床試驗的結果顯示，Activella為一種新型的賀爾蒙替代治療(HRT)藥物，可以減輕停經期後症狀，並且所引起的子宮出血和出血點症狀，要比Prempro輕，而且在控制脂肪代謝方面有著助益的作用。
加拿大伯靈頓Vermont醫科大學的Julia V. Johnson醫師，和他的同事們寫道：「影響HRT藥物連續使用的最重要的影響因素是子宮的出血，而服用Activella的患者在緩解停經期後症狀的同時，所導致的子宮出血也較少。」
在我們為期6個月的研究中，有438名健康的停經期後婦女服用Prempro (馬雌賀爾蒙合成物0.625 mg，並結合2.5 mg的醋酸鹽助孕劑)，或Activella (17beta-雌二醇1 mg結合黃體素醋酸鹽0.5 mg)，前者是在美國用於連續性合併HRT治療中採用的最廣泛藥物。
接受Activella治療的婦女，在對子宮出血的控制方面，要優於服用Prempro的婦女，這在停經1或2年的婦女，接受治療的前3個月中尤其明顯。在研究組中，有71.4%的服用Activella的婦女，和40.0%的服用Prempro的婦女，沒有出血子宮出血(p=0.005)，有54.8%的Activella服用的婦女，和17.1%的服用Prempro的婦女，沒有出血子宮出血，也沒有產生出血點(p=0.001)。
服用Activella的婦女三酸甘油脂濃度降低了8.5%，而服用Prempro的婦女三酸甘油脂濃度升高了11.7%(p<0.001)，而總膽固醇濃度，分別降低9.1%和6.9%。
在編者附錄中，奧古斯塔喬治亞州醫科大學的R. Don Gambrell, Jr.醫師寫道：「為了提高連續的使用率，HRT所用的藥物對每個婦女應當個別化。沒有一種藥物是適合所有的停經期後的婦女，但是經由多種的途徑和治療辦法，每個個體應當能達到最佳的治療效果。」
Novo Nordisk Pharmaceuticals，一家從事供應歐洲市場雌二酮/黃體素醋酸鹽銷售的公司，對這項研究提供贊助。

【原产地英文商品名】Activella 1mg/0.5mg/tablet 28tabs/pack
【原产地英文药品名】estradiol/norethindrone acetate 1mg/0.5mg/tablet 28tabs/pack
【中文参考商品译名】诺更宁 1毫克/0.5毫克/片 28片/包
【中文参考药品译名】雌二醇, 炔诺酮片 1毫克/0.5毫克/片 28片/包
【生产厂家中文参考译名】诺和诺德制药公司
【生产厂家英文名】Novo Nordisk Pharmaceuticals

INDICATIONS

Activella 1.0 mg/0.5 mg and 0.5 mg/0.1 mg are indicated in women who have a uterus for the:

1. Treatment of moderate to severe vasomotor symptoms associated with menopause.

2. Prevention of postmenopausal osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and non-estrogen medications should be carefully considered.

The mainstays for decreasing the risk of postmenopausal osteoporosis are weight bearing exercise, adequate calcium and vitamin D intake, and when indicated, pharmacologic therapy.

Postmenopausal women require an average of 1500 mg/day of elemental calcium. Therefore, when not contraindicated, calcium supplementation may be helpful for women with suboptimal dietary intake. Vitamin D supplementation of 400-800 IU/day may also be required to ensure adequate daily intake in postmenopausal women.

Activella 1.0 mg/0.5 mg is also indicated in women who have a uterus for the:

3. Treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.

DOSAGE AND ADMINISTRATION
Use of estrogen, alone or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Patients should be re-evaluated periodically as clinically appropriate (e.g., 3 to 6 month intervals) to determine if treatment is still necessary (See BOXED WARNINGS and WARNINGS). For women who have a uterus, adequate diagnostic measures, such as endometrial sampling, when indicated, should be undertaken to rule out malignancy in cases of undiagnosed persistent or recurring abnormal vaginal bleeding.

Activella therapy consists of a single tablet to be taken once daily.

1.For the treatment of moderate to severe vasomotor symptoms associated with menopause, and the prevention of postmenopausal osteoporosis. When prescribing solely for the prevention of postmenopausal osteoporosis, therapy should only be considered for women at significant risk of osteoporosis and non-estrogen medications should be carefully considered.

Activella 1.0 mg/0.5 mg
Activella 0.5 mg/0.1 mg
2.For the treatment of moderate to severe symptoms of vulvar and vaginal atrophy. When used solely for the treatment of symptoms of vulvar and vaginal atrophy, topical vaginal products should be considered.

Activella 1.0 mg/0.5 mg
Patients should be started at the lowest dose.

HOW SUPPLIED
Activella 1.0 mg/0.5 mg is a white, film-coated tablet, engraved with NOVO 288 on one side and the APIS bull on the other. It is round, 6mm in diameter and bi-convex. (NDC 0169-5174-02). It is supplied as 28 tablets in a calendar dial pack dispenser. Store in a dry place protected from light.

Activella 0.5 mg/0.1 mg is a white, film-coated tablet, engraved with NOVO 291 on one side and the APIS bull on the other. It is round, 6mm in diameter and bi-convex. (NDC 0169-5175-10). It is supplied as 28 tablets in a calendar dial pack dispenser. Keep the container in the outer carton.

Store at 25° C (77° F), excursions permitted to 15-30° C (59-86° F). [See USP Controlled Room Temperature.]

Drug/Laboratory Test Interactions
Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, and beta-thromboglobulin; decreased levels of anti-factor Xa and antithrombin III, decreased antithrombin III activity, increased levels of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.
Increased thyroid-binding globulin (TBG) levels leading to increased circulating total thyroid hormone levels as measured by protein-bound iodine (PBI), T4 levels (by column or by radioimmunoassay), or T3 levels by radioimmunoassay. T3 resin uptake is decreased, reflecting the elevated TBG. Free T4 and free T3 concentrations are unaltered. Patients on thyroid replacement therapy may require higher doses of thyroid hormone.
Other binding proteins may be elevated in serum (i.e., corticosteroid binding globulin (CBG), SHBG) leading to increased total circulating corticosteroids and sex steroids, respectively. Free hormone concentrations may be decreased. Other plasma proteins may be increased (angiotensinogen/rennin substrate, alpha-1 antitrypsin, ceruloplasmin).
Increased plasma HDL and HDL2cholesterol subfraction concentration, reduced LDL cholesterol concentration, increased triglyceride levels.
Impaired glucose tolerance.
Reduced response to metyrapone test.