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What is Activella
NorethisteroneThe Generic name of this drug
Treatment SummaryNorethisterone, also known as norethindrone, is a type of synthetic hormone used to treat menstrual problems and endometriosis. It is a second-generation progestin, meaning it is more potent than other progestins, and is used in combination with other hormones for contraception and hormone replacement therapy. It was first developed in 1951 in Mexico City and was initially used to treat irregular menstruation, though it was not marketed as an oral contraceptive until 1962.
Neconis the brand name
Activella Overview & Background
Brand Name
Generic Name
First FDA Approval
How many FDA approvals?
Necon
Norethisterone
1967
347
Effectiveness
How Activella Affects PatientsNorethisterone is a synthetic hormone used in oral contraceptives and to treat other hormone-related conditions. It is more powerful than the natural progesterone hormone, and works to change the cervical and endometrial function. It may also inhibit hormones that help create eggs for fertilization. Taking this drug may slightly increase the risk of developing breast cancer, so patients should be aware of this and do regular breast self-exams.
How Activella works in the bodyNorethisterone works on a molecular level by binding to progesterone receptors, which causes changes in target genes. As a contraceptive, it thickens cervical mucus and makes the endometrium inhospitable for implantation. It also works to prevent follicle and corpus luteum development by suppressing the release of FSH and LH in a negative feedback loop. In menopausal women, it is used to suppress the growth of the endometrium and reduce the risk of endometrial cancer. It does not bind to other steroid receptors (like androgen or glucocorticoid) but may cause some adverse effects
When to interrupt dosage
The measure of Activella is contingent upon the diagnosed state, including Atrophic, Fracture and Hormone Replacement Therapy. The dosage amount varies, based on the technique of delivery (e.g. Oral or Tablet) specified in the table beneath.Condition
Dosage
Administration
Hot flashes
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Hormone Replacement Therapy
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Atrophic
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
female castration
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Low Testosterone
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
hypoestrogenism
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Therapeutic procedure
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Fracture
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Ovarian Failure
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Postmenopausal Osteoporosis
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Vasomotor System
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Oral Contraceptives
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Hormonal Contraception
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Estrogen Deprivation Symptoms
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Menopause
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Endometriosis
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Birth Control
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Osteoporosis
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Endometriosis
0.014 mg/hour, , 0.025 mg/hour, 0.5 mg, 0.1 mg, 5.0 mg, 1.0 mg, 0.35 mg, 1.5 mg, 0.8 mg, 2.7 mg, 4.8 mg, 0.75 mg, 0.4 mg, 2.25 mg, 30.0 mg, 3.0 mg
Transdermal, Patch, extended release, , Patch, extended release - Transdermal, Kit, Oral, Tablet, film coated, Tablet, film coated - Oral, Tablet, Tablet - Oral, Kit - Oral, Patch, Patch - Transdermal, Tablet, chewable, Tablet, chewable - Oral, Capsule - Oral, Capsule, Intramuscular; Oral; Topical
Warnings
Activella has eight contraindications and should be avoided when experiencing any of the conditions indicated in the following table.Activella ContraindicationsCondition
Risk Level
Notes
active liver disease
Do Not Combine
Thrombophilia
Do Not Combine
Vaginal Hemorrhage
Do Not Combine
Malignant Neoplasms
Do Not Combine
Benign hepatic neoplasm
Do Not Combine
Breast Cancer
Do Not Combine
Thromboembolism
Do Not Combine
Severe Hypersensitivity Reactions
Do Not Combine
Norethisterone may interact with Pulse Frequency
Common Activella Drug Interactions
Drug Name
Risk Level
Description
Astemizole
Major
The metabolism of Astemizole can be decreased when combined with Norethisterone.
Axitinib
Major
The metabolism of Axitinib can be decreased when combined with Norethisterone.
Cabazitaxel
Major
The metabolism of Cabazitaxel can be decreased when combined with Norethisterone.
Clomipramine
Major
The metabolism of Clomipramine can be increased when combined with Norethisterone.
Copanlisib
Major
The metabolism of Copanlisib can be decreased when combined with Norethisterone.
Activella Toxicity & Overdose RiskThe lowest toxic dose of oral contraceptives in mice has been found to be 6g/kg and 42mg/kg in women. There have been no reports of serious harm due to overdosing on oral contraceptives, including in children. People who take too much of this medication may experience nausea or vomiting, which are known side effects.
Activella Novel Uses: Which Conditions Have a Clinical Trial Featuring Activella?
Currently, there are 160 active studies assessing the potential of Activella to provide Birth Control, counteract Atrophic changes and reduce Low Testosterone.Condition
Clinical Trials
Trial Phases
Low Testosterone
15 Actively Recruiting
Phase 1, Phase 4, Phase 2, Not Applicable
Estrogen Deprivation Symptoms
0 Actively Recruiting
Oral Contraceptives
2 Actively Recruiting
Not Applicable
Endometriosis
30 Actively Recruiting
Phase 3, Not Applicable, Early Phase 1, Phase 2, Phase 4, Phase 1
Hormone Replacement Therapy
0 Actively Recruiting
Birth Control
31 Actively Recruiting
Not Applicable, Phase 3, Phase 4, Early Phase 1
Hot flashes
22 Actively Recruiting
Phase 2, Not Applicable, Phase 1, Phase 4, Early Phase 1
Therapeutic procedure
0 Actively Recruiting
Menopause
0 Actively Recruiting
Postmenopausal Osteoporosis
3 Actively Recruiting
Not Applicable, Phase 4
Atrophic
5 Actively Recruiting
Phase 2, Phase 4, Not Applicable
Osteoporosis
39 Actively Recruiting
Phase 1, Phase 2, Not Applicable, Early Phase 1, Phase 4, Phase 3
Fracture
0 Actively Recruiting
female castration
0 Actively Recruiting
hypoestrogenism
2 Actively Recruiting
Phase 4
Vasomotor System
0 Actively Recruiting
Endometriosis
1 Actively Recruiting
Phase 4
Ovarian Failure
2 Actively Recruiting
Not Applicable, Phase 1
Hormonal Contraception
0 Actively Recruiting
Activella Reviews: What are patients saying about Activella?
5Patient Review
4/7/2013 I've been on Activella for a couple of years now and it's been great. I got relief from my hot flashes immediately and have not had any problems since. I have gained about 10 pounds, but I can't say for sure if that's because of the medication or not.
5Patient Review
2/24/2015 I've been taking this drug for six months and it's really improved my quality of life. I no longer experience hot flashes, my mood is better, and my hair stopped falling out. When I first started taking the medication, I was very hungry; however, that only lasted a few weeks. Overall, I'm extremely pleased with the results.
5Patient Review
7/28/2014 I began to notice a change within 2 weeks with less hot flashes. Hot flashes did seem to get worse for the first week, However, are completely gone now. I am currently experiencing bleeding... is this normal? does it eventually stop?
5Patient Review
1/23/2015 This prescription has helped me so much. I was having hot flashes every hour and a half, which made it impossible to sleep at night. Now I don't have any hot flashes and I can finally get some rest!
5Patient Review
4/7/2018 I took Activelle for 20 years and had few complaints. I felt energetic and rarely experienced hot flashes. However, since tapering off the medication three months ago, I am feeling terrible. I ache all over, experience constant hot flashes, and generally feel depressed and sad. I have a mammogram scheduled for September, but in the meantime, is there anyone out there who can help me?
5Patient Review
7/19/2022 Activella has been a true game-changer for me. I had really bad mood swings and hot flashes prior to using this medication, and now I feel so much better. It's helped me cope in a big way.
5Patient Review
12/19/2013 I've been taking this drug for over five years. I haven't had any experience with hot flashes. Recently, my doctor lowered my dosage, and now I'm experiencing all the symptoms of menopause. I hope this is normal and not a problem that I'm going to dislike.
5Patient Review
8/9/2013 Activella has been fantastic in alleviating menopausal symptoms. No hot flashes, hormonal headaches, or mood swings. I feel like myself again, maybe better!
4.3Patient Review
7/28/2013 I had been taking Activella for four years with great results; however, I recently stopped taking the medication and have started to experience hot flashes and spotting again. I'm only 50 years old so I thought I was past menopause at this stage. Is it normal to start with hot flashes and spotting so soon after stopping meds? Thinking I should go back on Activella but had hoped it wasn't needed any longer.
4.3Patient Review
7/28/2014 I had been taking Activella for around 18 months when I started noticing some serious side-effects, like face swelling and hives. I stopped taking the drug to see if it was the cause, and sure enough, after a couple of weeks most of my symptoms subsided. If you're considering this medication, be aware that there are some possible risks.
4Patient Review
5/1/2013 This medication has been working great for my high blood pressure.
3.3Patient Review
8/26/2019 All of my menopause symptoms have been eased by this treatment except for my mood. I have also started spotting, and my chest has broken out in acne that is very stubborn. I truly hope the spotting doesn't turn into a full-blown period type of flow.
2.3Patient Review
4/17/2014 I was diagnosed pre-menopausal and put on Activella. After only one week, I experienced depression, fatigue, sleepiness, and a loss of appetite (which is actually good for me). I was previously taking elestrin and protosteron but had the same reaction to those medications.
2Patient Review
5/28/2013 I stopped taking this after only eight days because I saw no improvement in my symptoms. In fact, I may have even gotten worse. I'm now trying a natural remedy from the health food store.
1.7Patient Review
6/8/2014 I was prescribed this medication after being diagnosed as post menopausal. Unfortunately, I have been bleeding for three weeks straight since starting the meds.
1.7Patient Review
5/12/2021 After taking Activelle for seven months, I will be stopping tomorrow. I was diagnosed with deep vein thrombosis after a scan today. While it did take away hot flushes, it gave me something far worse in return.
Patient Q&A Section about activella
These questions and answers are submitted by anonymous patients, and have not been verified by our internal team.What is the generic for Activella?
"The version of Activella that contains estradiol-norethindrone is available commercially."
Answered by AI
Is Activella an HRT?
"Activella is a HRT tablet that contains both estrogen and progestin."
Answered by AI
What is Activella used for?
"This medication is a combination of two female hormones: an estrogen (such as conjugated estrogen, estradiol) and a progestin (such as medroxyprogesterone, norethindrone, norgestimate). It is used by women to help reduce symptoms of menopause (such as hot flashes, vaginal dryness)"
Answered by AI
Does Activella make you gain weight?
"In clinical studies, up to 9% of people who took Activella reported weight gain. The medication can also cause your body to hold onto fluids, which can look like swelling or weight gain."
Answered by AI