Activelle

Activelle is a combined hormone replacement medicine in tablet form that contains estradiol (a natural estrogen) and norethisterone acetate (a progestin). It is used to treat menopausal symptoms in women whose last menstrual period was at least 12 months ago.

The continuous combination of both hormones means that menstrual bleeding no longer occurs – unlike with sequential products. Activelle relieves typical menopausal symptoms such as hot flashes, sleep disturbances and vaginal dryness.

The progestin norethisterone protects the lining of the uterus from the growth-promoting effect of estrogen.

Activelle compensates for the hormone deficiency after menopause:

Estradiol (estrogen):

• Replaces the body's own estrogen that is missing
• Relieves vasomotor symptoms (hot flashes, night sweats)
• Improves vaginal moisture
• Protects against bone loss

Norethisterone acetate (progestin):

• Protects the lining of the uterus (endometrium)
• Prevents endometrial hyperplasia
• Continuous administration = no bleeding

Continuous combined therapy: Both hormones are taken every day (no cycle), so bleeding usually does not occur.

Activelle is suitable for:

• Postmenopausal women (last bleeding > 12 months ago)
• Moderate to severe menopausal symptoms
• Women with an intact uterus (progestin protection needed)

Advantages:

• Bleeding-free (continuous therapy)
• One tablet once a day

Not suitable:

• Perimenopausal women (still having menstrual periods)
• Women after a hysterectomy (no progestin needed)
• In case of contraindications to HRT

Activelle film-coated tablets:

• 1 mg estradiol + 0.5 mg norethisterone acetate
• 1 tablet daily, continuously without a break

Starting therapy:

• No earlier than 12 months after the last menstrual period
• When switching from sequential HRT: after completion of the cycle

Duration of therapy:

• As short as possible, with regular review (at least annually)

How to take:

• 1 tablet daily with a little water
• Always at the same time of day
• Regardless of meals
• Continuously without a break

If you forget a dose:

• Take it within 12 hours
• After more than 12 hours, do not take the missed tablet any more
• Then continue as usual
• Do not take a double dose

Important:

• Regular check-ups
• Breast examination and mammography as recommended

Do not use in case of:

• Current or previous breast cancer, or suspected breast cancer
• Current or previous estrogen-dependent malignant tumors, or suspicion thereof
• Unexplained vaginal bleeding
• Untreated endometrial hyperplasia
• Active or previous thrombosis/pulmonary embolism
• Known thrombophilic disorders (e.g. protein C, protein S or antithrombin deficiency)
• Current or previous arterial thromboembolic disease (e.g. angina pectoris, heart attack)
• Acute or previous liver disease, as long as liver function values have not returned to normal
• Porphyria
• Hypersensitivity to the active substances or to any of the excipients

Use with caution in case of:

• Risk factors for thrombosis
• Uterine fibroids
• Endometriosis
• Gallstone disease
• Migraine
• Diabetes mellitus
• High blood pressure

Pregnancy/breastfeeding: Contraindicated.

Very common (about 10-20%):

• Breast pain or breast tenderness
• Vaginal bleeding (mostly in the first months of treatment)

Common (1-10%):

• Headache
• Nausea
• Weight gain
• Depression or worsening of depression

Uncommon (0.1-1%):

• Abdominal pain
• Bloating
• Nervousness
• Leg cramps

Rare but serious:

• Venous thromboembolism
• Increased risk of breast cancer with long-term therapy
• Stroke
• Gallstone disorders

Note: Most side effects are mild and improve during the first few months.

Interactions:

• CYP3A4 inducers (carbamazepine, phenytoin, rifampicin, St. John's wort) – reduced estrogen effect
• CYP3A4 inhibitors – increased estrogen levels
• Thyroid hormones – dose adjustment may be necessary

Important: St. John's wort can significantly reduce the effectiveness of HRT!