Heria (Tibolone)

Heria is indicated for the management of symptoms that arise from estrogen deficiency during the menopausal transition.

• Alleviation of vasomotor symptoms such as hot flashes and night sweats.
• Improvement of urogenital atrophy manifestations, including vaginal dryness, itching, and dyspareunia.
• Support of bone mineral density to help reduce the risk of osteoporotic fractures.
• Mitigation of mood changes, irritability, and sleep disturbances linked to hormonal fluctuations.
• Consideration as an alternative for women with contraindications to estrogen‑only therapy.

• Tibolone is metabolized in the liver to three active metabolites that selectively bind estrogen, progesterone, and androgen receptors. The Δ4‑isomer exerts estrogenic effects on bone and the central nervous system, while the 3α‑hydroxy metabolite provides progestogenic activity that opposes endometrial stimulation. The 3β‑hydroxy metabolite displays weak androgenic activity, contributing to libido and muscle mass maintenance. These combined actions produce a balanced hormonal profile that mimics natural ovarian hormone output during the reproductive years.

Like all hormone therapies, Heria may cause adverse reactions that vary in frequency and severity. Patients should report any new or worsening symptoms to their healthcare provider.

Common

• Nausea, abdominal discomfort, or dyspepsia, often mild and transient.
• Breast tenderness or mild enlargement, which may fluctuate with the menstrual cycle.
• Headache or transient dizziness, typically resolving without intervention.
• Irregular vaginal bleeding or spotting, especially during the initial weeks of therapy.

Serious

• Deep vein thrombosis or pulmonary embolism, presenting as leg swelling, pain, or shortness of breath.
• Stroke or transient ischemic attack, characterized by sudden neurological deficits such as weakness or speech changes.
• Liver function abnormalities, including elevated enzymes or jaundice, indicating possible hepatic injury.

Before starting Heria, clinicians should evaluate individual risk factors and counsel patients on necessary precautions to minimize potential complications. A thorough medical history, physical examination, and baseline laboratory testing are recommended.

• History of thromboembolic disease, such as deep vein thrombosis or pulmonary embolism.
• Uncontrolled hypertension or cardiovascular disease.
• Active or past hormone‑dependent cancers, including breast or endometrial carcinoma.
• Liver disease or abnormal liver function tests.
• Pregnancy, breastfeeding, or intention to become pregnant.
• Smoking or use of tobacco products, which increase thrombotic risk.
• Severe hyperlipidemia or uncontrolled diabetes.

Heria can interact with other medicines, affecting its efficacy or safety; clinicians should review a patient’s medication list before prescribing.

Avoid

• Combined oral contraceptives or estrogen‑containing hormone therapy, which may increase thrombotic risk.
• Anticoagulants such as warfarin, because tibolone may alter coagulation parameters.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) that can reduce tibolone plasma levels.
• Tamoxifen or other selective estrogen receptor modulators, as combined estrogenic activity may alter therapeutic outcomes.

Use with caution

• Antiplatelet agents (e.g., aspirin, clopidogrel) – monitor for bleeding.
• Selective serotonin reuptake inhibitors (SSRIs) – may exacerbate mood changes.
• Thyroid hormone replacement – tibolone can affect thyroid‑binding globulin levels.
• CYP2C19 inhibitors (e.g., fluoxetine) – may increase tibolone concentrations, requiring monitoring.