Heria (Tibolone)

Heria is indicated for several therapeutic purposes related to the post‑menopausal period, focusing on symptom relief and bone health maintenance.

• Relief of moderate to severe vasomotor symptoms such as hot flashes and night sweats.
• Reduction of vaginal dryness and discomfort associated with estrogen deficiency.
• Prevention of postmenopausal bone loss and reduction of fracture risk.
• Improvement of mood and sleep disturbances linked to menopause.
• Adjunctive therapy for women who have undergone surgical menopause.
• Management of mild to moderate depressive symptoms that may accompany menopause.

• Tibolone is a synthetic steroid that undergoes hepatic metabolism to three major active metabolites. One metabolite binds to estrogen receptors (ERα and ERβ) producing estrogenic effects on bone, brain and urogenital tissues. A second metabolite interacts with progesterone receptors, providing progestogenic activity that counteracts endometrial stimulation. A third metabolite has affinity for androgen receptors, contributing to androgenic actions that improve libido and muscle tone. Together these actions modulate the hypothalamic‑pituitary‑ovarian axis and alleviate menopausal symptoms.

Adverse reactions reported with tibolone, the active component of Heria, vary in frequency and severity.

Common

• Headache, often mild to moderate in intensity.
• Nausea or gastrointestinal upset, including occasional abdominal discomfort.
• Breast tenderness or mild enlargement, usually transient.
• Vaginal discharge or spotting, typically non‑painful.
• Mood swings or mild depression, which may improve after continued therapy.

Serious

• Deep vein thrombosis or pulmonary embolism, presenting with leg pain, swelling or respiratory distress.
• Stroke or transient ischemic attack, characterized by sudden neurological deficits.
• Liver function abnormalities, indicated by elevated transaminases.
• Unexplained vaginal bleeding, which may signal endometrial changes.
• Endometrial hyperplasia or carcinoma (rare), requiring gynecologic evaluation.

When prescribing Heria, clinicians should evaluate individual risk factors, review the patient's medical history, and consider several precautionary measures to ensure safe and appropriate use.

• History of hormone‑dependent cancers such as breast or endometrial carcinoma.
• Active or past venous thromboembolism, including deep vein thrombosis or pulmonary embolism.
• Uncontrolled hypertension or cardiovascular disease.
• Liver disease or abnormal liver function tests.
• Undiagnosed abnormal uterine bleeding.
• Pregnancy, lactation, or intention to become pregnant.
• Severe migraines or known estrogen‑related headaches.
• Known hypersensitivity to tibolone or any excipients in the formulation.

Tibolone may interact with other medicines, altering its effectiveness or increasing the risk of adverse events.

Avoid

• Combined estrogen‑containing hormone therapy, which can increase thrombotic risk.
• Strong CYP3A4 inducers such as rifampin, carbamazepine, or phenytoin, which may reduce tibolone levels.
• Anticoagulants (e.g., warfarin) where additive clot‑prevention effects could be unpredictable.
• Selective estrogen receptor modulators (e.g., tamoxifen) because combined estrogenic activity may alter therapeutic outcomes.

Use with caution

• Antidepressants, especially SSRIs and SNRIs, which may affect mood‑related side effects.
• Antihypertensive agents, as tibolone can cause fluid retention.
• Herbal supplements like St. John’s wort that induce hepatic enzymes.
• Oral contraceptives, as overlapping hormonal effects may increase the risk of menstrual irregularities.