📋 Clinical Overview

Tibolone is a synthetic steroid with tissue-specific estrogenic, progestogenic, and weak androgenic properties. It is used primarily for the management of menopausal symptoms and the prevention of postmenopausal osteoporosis. Unlike conventional hormone replacement therapy (HRT), it does not stimulate the endometrium, eliminating the need for a progestogen in women with an intact uterus.

💊 Dosage & Administration

Adult: 2.5 mg orally once daily. Treatment should be initiated at least 12 months after the last natural menstrual period or immediately after surgical menopause.

Note: Tablet should be swallowed whole with water, preferably at the same time each day, with or without food. Treatment is continuous (no break). If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose. Do not double the dose.

⚠️ Contraindications

Known, past, or suspected breast cancer
Known or suspected estrogen-dependent neoplasia (e.g., endometrial cancer)
Undiagnosed genital bleeding
Active or recent arterial thromboembolic disease (e.g., angina, myocardial infarction, stroke)
Active or history of venous thromboembolism (DVT, PE)
Active or recent liver disease, or history of liver disease as long as liver function tests have failed to return to normal
Porphyria
Hypersensitivity to Tibolone or any excipient

🔬 Mechanism of Action

Tibolone itself is inactive. After oral administration, it is converted into three active metabolites that exert tissue-specific effects. In bone, brain, and vagina, the 3α-OH and 3β-OH metabolites exert estrogenic effects, relieving symptoms and preventing bone loss. In the endometrium, the Δ4-isomer exerts a progestogenic effect, preventing estrogenic stimulation and hyperplasia. The Δ4-isomer also contributes to androgenic effects, which may improve libido and sense of well-being.

🤕 Side Effects

Weight gain
Abdominal pain
Headache
Dizziness
Vaginal bleeding/spotting (especially in first few months)
Breast pain/discomfort
Increased facial hair growth (hirsutism)
Acne
Seborrhea
Edema

🤰 Special Populations

Pregnancy: Category X. Contraindicated. Not indicated for use in women of childbearing potential. If pregnancy occurs during therapy, discontinue immediately.

Driving: May cause dizziness, visual disturbances, or drowsiness in some patients. Patients should be cautioned about operating machinery or driving until they are certain the medication does not affect them adversely.

🔄 Drug Interactions

Enzyme Inducers (Carbamazepine, Phenytoin, Rifampicin, St. John's Wort)	Markedly increase metabolism of Tibolone, reducing its therapeutic efficacy. May lead to breakthrough bleeding and loss of bone protection.	Major
Warfarin and other Coumarin Anticoagulants	Tibolone may potentiate the anticoagulant effect, increasing the risk of bleeding. Close monitoring of INR is required.	Moderate
Insulin and Oral Hypoglycemics	Tibolone may decrease glucose tolerance, potentially requiring adjustment of antidiabetic therapy.	Moderate
Corticosteroids	Potential additive effect on bone mineral density. Increased risk of edema.	Moderate

Livial