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Synthetic steroid (STEAR)

Tibolone drug interactions: a practical overview

Drug interactions are the single biggest cause of preventable medication problems. Tibolone (Tibolone) interacts to varying degrees with several classes of medication and with a smaller list of foods. This page summarises the practically important ones at 2.5mg, framed for a real-world prescription review rather than an exhaustive PDF list.

High-priority interactions for Tibolone

For Tibolone, the most clinically relevant interactions are typically with strong CYP3A4 inhibitors and inducers, with cardiovascular medications (notably nitrates for several Synthetic steroid (STEAR) agents), with central nervous system depressants, and with medications affecting blood pressure or heart rate. Tibolone is a prodrug; on absorption it is rapidly converted to three active metabolites (3α-OH-tibolone, 3β-OH-tibolone and Δ4-tibolone) with different tissue-selective activity.

Working with the pharmacist

A pharmacist review of all current medications is the practical safeguard against unintended interactions with Tibolone. According to the prescribing information for Tibolone, the full medication list — prescription, OTC, supplements and recreational substances — should be reviewed before starting and at every dose change at 2.5mg.

Frequently asked questions

What's the most important Tibolone interaction to know?

For most Synthetic steroid (STEAR) medications, the highest-priority interaction is with nitrate medications used for chest pain — this combination is often a hard contraindication. After that, strong CYP3A4 inhibitors (some antifungals, macrolides) are the next concern at routine 2.5mg doses.

Do I need to tell the pharmacist about supplements?

Yes. Supplements and herbal products can interact with Tibolone in ways that prescription drug-drug interaction databases miss. The pharmacist needs the complete picture — including supplements like St John's Wort, grapefruit-containing products and high-dose vitamins — to flag risks at 2.5mg.

Products containing Tibolone

More on Tibolone

The information on this website is provided for reference and educational purposes only. It does not replace consultation with a qualified healthcare professional.